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Drug Dosage form Dosage Generic/Price Other/
Pharmacokinetics
Mechanism of Action/
FDA-approved indications
Side Effects
P = % of patients on placebo
who experienced side effect
Drug/Lab Interactions Precautions/
Contraindications
Amphetamine base

(Adzenys XR-ODT™)
Adzenys XR-ODT®
orally disintegrating tablet

  • 3.1 mg
  • 6.3 mg
  • 9.4 mg
  • 12.5 mg
  • 15.7 mg
  • 18.8 mg

  • Contains 50% immediate-release and 50% delayed-release amphetamine
  • Contains a 3:1 ratio of d- to l-amphetamine
ADHD
Children 6 - 12 years old
  • Starting: 6.3 mg once daily in the morning
  • Maximum: 18.8 mg once daily
  • Increase dose in increments of 3.1 or 6.3 mg per day at weekly intervals

Adolescents 13 - 17 years old
  • Starting: 6.3 mg once daily in the morning
  • Maximum: 12.5 mg once daily
  • Increase dose in increments of 3.1 or 6.3 mg per day at weekly intervals

Adults
  • Recommended dose: 12.5 mg once daily

Switching from Adderall XR

Equivalent doses
Adderall XR dose Adzenys XR-ODT dose
5 mg 3.1 mg
10 mg 6.3 mg
15 mg 9.4 mg
20 mg 12.5 mg
25 mg 15.7 mg
30 mg 18.8 mg
Adzenys XR-ODT
NO/$$$$

Other
  • Tablet is placed on tongue where it disintegrates
  • Do not crush or chew tablet
  • May take without regard to food
  • Leave tablet in blister pack until ready to take

Pharmacokinetics

  • Half-life (6 - 12 years):
    • d-isomer ∼ 9 - 10 hours
    • l-isomer ∼ 10 - 11 hours

  • Half-life (adults):
    • d-isomer ∼ 11 hours
    • l-isomer ∼ 14 hours

  • Time to max level: 5 hours
Mechanism of action
  • Amphetamines are CNS stimulants
  • Amphetamines are thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space
  • The mode of therapeutic action in ADHD is not known

FDA-approved indication

  • ADHD
Children 6 - 12 years
NOTE: Only side effects that occurred more than placebo and at an incidence ≥ 5% are listed.

  • Loss of appetite - 22%, P - 2%
  • Insomnia - 17%, P - 2%
  • Abdominal pain - 14%, P - 10%
  • Emotional lability - 9%, P - 2%
  • Vomiting - 7%, P - 4%
  • Nervousness - 6%, P - 2%
  • Nausea - 5%, P - 3%
  • Fever - 5%, P - 2%

Adults
NOTE: Only side effects that occurred more than placebo and at an incidence ≥ 5% are listed.

  • Dry mouth - 35%, P - 5%
  • Loss of appetite - 33%, P - 3%
  • Insomnia - 27%, P - 13%
  • Headache - 26%, P - 13%
  • Weight loss - 10%, P - 0%
  • Nausea - 8%, P - 3%
  • Agitation - 8%, P - 5%
  • Anxiety - 8%, P - 5%
  • Dizziness - 7%, P - 0%
  • Diarrhea - 6%, P - 0%
  • Tachycardia - 6%, P - 3%
  • Asthenia - 6%, P - 5%
  • Urinary tract infection - 5%, P - 0%
Drug interactions
  • MAO inhibitors - DO NOT COMBINE. Do not use within 14 days of taking an MAO inhibitor.
  • Antacids - antacids may increase the absorption of amphetamines thereby increasing exposure and risk of adverse events
  • Alpha blockers - amphetamines may counteract the effects of alpha blockers
  • Beta blockers - amphetamines may counteract the effects of beta blockers
  • Blood pressure medications - amphetamines may raise blood pressure and counteract the effects of blood pressure medications
  • Tricyclic antidepressants (TCAs) - amphetamines may potentiate the effects of TCAs and vice versa
  • Meperidine - amphetamines may potentiate the effects of meperidine
  • Antipsychotics - antipsychotics may reduce the effects of amphetamines
  • Lithium - lithium may block the effects of amphetamines
  • Proton pump inhibitors (ex. omeprazole, Prevacid, Nexium, etc.) - PPIs may increase the absorption of amphetamines thereby increasing exposure and risk of adverse events
  • Urinary alkalizers (e.g. acetazolamide, metolazone) - may decrease the clearance of amphetamines and increase exposure
  • Acidifying agents (ascorbic acid, fruit juices, etc.) - may decrease absorption of amphetamines
  • Phenobarbital - amphetamines may delay the absorption of phenobarbital
  • Phenytoin - amphetamines may delay the absorption of phenytoin

Lab interactions
  • Corticosteroid levels - amphetamines may cause elevations in corticosteroid levels
  • Drug abuse and dependence - amphetamines have the potential for drug abuse and dependence. Use caution in susceptible patients.
  • Heart disease - amphetamines may exacerbate and worsen heart disease. Avoid or use caution in susceptible patients.
  • Heart arrhythmias - amphetamines may exacerbate heart arrhythmias. Avoid use in susceptible patients.
  • Suppression of growth - stimulant medications can suppress growth rates in children. The effect appears to be directly related to dose and length of therapy. In studies, growth rates in children taking stimulants were 1 - 2 cm/year slower than controls. There is no conclusive evidence that stimulants affect adult height achieved. [1,2,3,4,5]
  • Hypertension - stimulants may raise blood pressure and worsen hypertension. Average blood pressure increase seen in trials was ∼ 2 - 4 mmHg. Average heart rate increase was 3 - 6 bpm.
  • Seizures - stimulants may lower the seizure threshold
  • Hyperthyroidism - stimulants may exacerbate symptoms of hyperthyroidism
  • Glaucoma - stimulants may worsen glaucoma
  • Psychosis - stimulants may worsen psychosis
  • Bipolar mania - stimulants may precipitate bipolar mania
  • Raynaud's phenomenon - stimulants may exacerbate Raynaud's phenomenon
  • Tourette's syndrome and tics - stimulants may worsen motor tics and tics associated with Tourette's syndrome
  • Visual changes - difficulties with accommodation and blurring of vision have been reported with stimulant medications
  • Liver disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.
  • Kidney disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.

Drug Dosage form Dosage Generic/Price Other/
Pharmacokinetics
Mechanism of Action/
FDA-approved indications
Side Effects
P = % of patients on placebo
who experienced side effect
Drug/Lab Interactions Precautions/
Contraindications
Amphetamine base

(Dyanavel XR®)
Dyanavel XR®
extended-release suspension

  • 2.5 mg/ml
  • Comes in 464 ml bottle
  • Suspension is bubblegum flavored
  • 2.5 mg of Dyanavel has the same amount of amphetamine found in a 4 mg strength amphetamine mixed salts product
  • Contains 3.2:1 ratio of d- to l-amphetamine
ADHD
Children ≥ 6 years old
  • Starting: 2.5 - 5 mg once daily in the morning
  • Maximum: 20 mg once daily
  • Increase dose in increments of 2.5 to 10 mg per day every 4 to 7 days
  • When switching from other amphetamine products, discontinue other product and titrate Dyanavel as above
  • Dyanavel is NOT equivalent to other amphetamine products on a mg-per-mg basis
Dyanavel XR
NO/$$$$

Other
  • Shake bottle before giving
  • May take without regard to food
  • Store at room temperature

Pharmacokinetics (adults)

  • Half-life:
    • d isomer ∼ 12 hours
    • l isomer ∼ 15 hours

  • Time to max level: 4 hours
Mechanism of action
  • Amphetamines are CNS stimulants
  • Amphetamines are thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space
  • The mode of therapeutic action in ADHD is not known

FDA-approved indication

  • ADHD
NOTE: Data is from one small study (n=108) in children aged 6 - 12 years lasting 1 week. Only side effects that occurred more than placebo and at an incidence ≥ 2% are listed.

  • Epistaxis - 3.8%, P - 0%
  • Allergic rhinitis - 3.8%, P - 0%
  • Upper abdominal pain - 3.8%, P - 2.1%

NOTE: Side effects typical of other amphetamines are also likely to be prevalent
Drug interactions
  • MAO inhibitors - DO NOT COMBINE. Do not use within 14 days of taking an MAO inhibitor.
  • Antacids - antacids may increase the absorption of amphetamines thereby increasing exposure and risk of adverse events
  • Alpha blockers - amphetamines may counteract the effects of alpha blockers
  • Beta blockers - amphetamines may counteract the effects of beta blockers
  • Blood pressure medications - amphetamines may raise blood pressure and counteract the effects of blood pressure medications
  • Tricyclic antidepressants (TCAs) - amphetamines may potentiate the effects of TCAs and vice versa
  • Meperidine - amphetamines may potentiate the effects of meperidine
  • Antipsychotics - antipsychotics may reduce the effects of amphetamines
  • Lithium - lithium may block the effects of amphetamines
  • Proton pump inhibitors (ex. omeprazole, Prevacid, Nexium, etc.) - PPIs may increase the absorption of amphetamines thereby increasing exposure and risk of adverse events
  • Urinary alkalizers (e.g. acetazolamide, metolazone) - may decrease the clearance of amphetamines and increase exposure
  • Acidifying agents (ascorbic acid, fruit juices, etc.) - may decrease absorption of amphetamines
  • Phenobarbital - amphetamines may delay the absorption of phenobarbital
  • Phenytoin - amphetamines may delay the absorption of phenytoin

Lab interactions
  • Corticosteroid levels - amphetamines may cause elevations in corticosteroid levels
  • Drug abuse and dependence - amphetamines have the potential for drug abuse and dependence. Use caution in susceptible patients.
  • Heart disease - amphetamines may exacerbate and worsen heart disease. Avoid or use caution in susceptible patients.
  • Heart arrhythmias - amphetamines may exacerbate heart arrhythmias. Avoid use in susceptible patients.
  • Suppression of growth - stimulant medications can suppress growth rates in children. The effect appears to be directly related to dose and length of therapy. In studies, growth rates in children taking stimulants were 1 - 2 cm/year slower than controls. There is no conclusive evidence that stimulants affect adult height achieved. [1,2,3,4,5]
  • Hypertension - stimulants may raise blood pressure and worsen hypertension. Average blood pressure increase seen in trials was ∼ 2 - 4 mmHg. Average heart rate increase was 3 - 6 bpm.
  • Seizures - stimulants may lower the seizure threshold
  • Hyperthyroidism - stimulants may exacerbate symptoms of hyperthyroidism
  • Glaucoma - stimulants may worsen glaucoma
  • Psychosis - stimulants may worsen psychosis
  • Bipolar mania - stimulants may precipitate bipolar mania
  • Raynaud's phenomenon - stimulants may exacerbate Raynaud's phenomenon
  • Tourette's syndrome and tics - stimulants may worsen motor tics and tics associated with Tourette's syndrome
  • Visual changes - difficulties with accommodation and blurring of vision have been reported with stimulant medications
  • Liver disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.
  • Kidney disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.

Drug Dosage form Dosage Generic/Price Other/
Pharmacokinetics
Mechanism of Action/
FDA-approved indications
Side Effects
P = % of patients on placebo
who experienced side effect
Drug/Lab Interactions Precautions/
Contraindications
Amphetamine salts

(Adderall®)
(Adderall XR®)
Adderall® - tablet
  • 5 mg
  • 7.5 mg
  • 10 mg
  • 12.5 mg
  • 15 mg
  • 20 mg
  • 30 mg

Adderall XR®
extended-release capsule

  • 5 mg
  • 10 mg
  • 15 mg
  • 20 mg
  • 25 mg
  • 30 mg

Adderall contains 4 amphetamine salts:
  • Dextroamphetamine saccharate
  • Amphetamine aspartate
  • Dextroamphetamine sulfate
  • Amphetamine sulfate

Each tablet contains equal parts of each salt
Adderall® tablet
ADHD
  • Children 3 - 5 years old
    • Starting: 2.5 mg once daily
    • Increase daily dose in increments of 2.5 mg at weekly intervals
  • Children ≥ 6 years old
    • Starting: 5 mg once or twice daily
    • Increase daily dose in increments of 5 mg at weekly intervals
    • Doses > 40 mg a day are rare
    • Give first dose on awakening and additional doses at intervals of 4 - 6 hours

Narcolepsy
  • Children 6 - 12 years old
    • Starting: 5 mg once daily
    • Increase daily dose in increments of 5 mg at weekly intervals
  • Children ≥ 12 years old
    • Starting: 10 mg daily
    • Increase daily dose in increments of 10 mg at weekly intervals
    • Usual dose 5 - 60 mg/day
    • Give first dose on awakening and additional doses at intervals of 4 - 6 hours

Adderall XR® capsule
ADHD
  • Children 6 - 12 years old
    • Starting: 10 mg once daily
    • Maximum: 30 mg once daily
    • Increase dose in increments of 5 - 10 mg at weekly intervals
  • Children 13 - 17 years old
    • Starting: 10 mg once daily
    • Increase dose in increments of 10 mg at weekly intervals
    • In trials, doses up to 40 mg/day were used
  • Adults
    • Starting: 20 mg once daily
    • Increase dose in increments of 10 mg at weekly intervals
    • In trials, doses up to 60 mg/day were used
Adderall® tablet
YES/$-$$ (60 tablets)

Adderall XR®
YES/$$$ (30 tablets)

Other
Adderall®
  • Tablets are scored and may be broken in two

  • May take without regard to food

Adderall XR®
  • May take without regard to food

  • Doses should be given in the morning to prevent insomnia

  • When switching from Adderall, give same total daily dose as once daily Adderall XR

  • Capsules may be opened and sprinkled on applesauce. Swallow applesauce whole, do not chew.

Pharmacokinetics
Adderall®
  • Half-life:
    • d isomer - ∼ 10 hours
    • l isomer - ∼ 13 hours
  • Time to max level: 3 hours

Adderall XR®
  • Half-life:
    • d isomer - ∼ 10 hours
    • l isomer - ∼ 13 hours
  • Time to max level: 7 hours
Mechanism of action
  • Amphetamines are CNS stimulants

  • Amphetamines are thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space

  • The mode of therapeutic action in ADHD is not known

FDA-approved indications

Adderall
  • ADHD
  • Narcolepsy

Adderall XR
  • ADHD
NOTE: Information from Adderall XR PI. Only side effects that occurred at an incidence of ≥ 3% and ≥ 3% more than placebo are listed.

Children (6 - 12 years old)
  • Loss of appetite - 22%, P - 2%
  • Insomnia - 17%, P - 2%
  • Upset stomach- 14%, P - 10%
  • Emotional lability - 9%, P - 2%
  • Vomiting - 7%, P - 4%
  • Nervousness - 6%, P - 2%
  • Fever - 5%, P - 2%
  • Weight loss* - 4%, P - 0%

*Weight loss is directly proportional to dose. In studies, average weight loss was 1.1 pound after 4 weeks for 10 mg dose and 2.8 pounds after 4 weeks for 20 mg dose
Adults
  • Dry mouth - 35%, P - 5%
  • Loss of appetite - 33%, P - 3%
  • Insomnia - 27%, P - 13%
  • Headache - 26%, P - 13%
  • Weight loss - 10%, P - 0%
  • Nausea - 8%, P - 3%
  • Agitation - 8%, P - 5%
  • Anxiety - 8%, P - 5%
  • Dizziness - 7%, P - 0%
  • Diarrhea - 6%, P - 0%
  • Tachycardia - 6%, P - 3%
  • Urinary tract infection - 5%, P - 0%
Drug interactions
  • MAO inhibitors - DO NOT COMBINE. Do not use within 14 days of taking an MAO inhibitor.
  • Antacids - antacids may increase the absorption of amphetamines thereby increasing exposure and risk of adverse events
  • Alpha blockers - stimulants may counteract the effects of alpha blockers
  • Beta blockers - stimulants may counteract the effects of beta blockers
  • Blood pressure medications - stimulants may raise blood pressure and counteract the effects of blood pressure medications
  • Tricyclic antidepressants (TCAs) - stimulants may potentiate the effects of TCAs and vice versa
  • Meperidine - stimulants may potentiate the effects of meperidine
  • Antipsychotics - antipsychotics may reduce the effects of stimulants
  • Lithium - lithium may block the effects of stimulants
  • Proton pump inhibitors (ex. omeprazole, Prevacid, Nexium, etc.) - PPIs may increase the rate of absorption of amphetamines
  • Urinary alkalizers (e.g. acetazolamide, metolazone) - may decrease the clearance of amphetamines and increase exposure
  • Acidifying agents (Ascorbic acid, fruit juices, etc.) - may decrease absorption of amphetamines
  • Phenobarbital - amphetamines may delay the absorption of phenobarbital
  • Phenytoin - amphetamines may delay the absorption of phenytoin

Lab interactions
  • Corticosteroid levels - amphetamines may cause elevations in corticosteroid levels
  • Drug abuse and dependence - stimulants have the potential for drug abuse and dependence. Use caution in susceptible patients.
  • Heart disease - stimulants may exacerbate and worsen heart disease. Avoid or use caution in susceptible patients.
  • Heart arrhythmias - stimulants may exacerbate heart arrhythmias. Avoid use in susceptible patients.
  • Suppression of growth - stimulant medications can suppress growth rates in children. The effect appears to be directly related to dose and length of therapy. In studies, growth rates in children taking stimulants were 1 - 2 cm/year slower than controls. There is no conclusive evidence that stimulants affect adult height achieved. [1,2,3,4,5]
  • Hypertension - stimulants may raise blood pressure and worsen hypertension. Average blood pressure increase seen in trials was ∼ 2 - 4 mmHg. Average heart rate increase was 3 - 6 bpm.
  • Seizures - stimulants may lower the seizure threshold
  • Hyperthyroidism - stimulants may exacerbate symptoms of hyperthyroidism
  • Glaucoma - stimulants may worsen glaucoma
  • Psychosis - stimulants may worsen psychosis
  • Bipolar mania - stimulants may precipitate bipolar mania
  • Raynaud's phenomenon - stimulants may exacerbate Raynaud's phenomenon
  • Tourette's syndrome and tics - stimulants may worsen motor tics and tics associated with Tourette's syndrome
  • Visual changes - difficulties with accommodation and blurring of vision have been reported with stimulant medications
  • Liver disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.
  • Kidney disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.

Drug Dosage form Dosage Generic/Price Other/
Pharmacokinetics
Mechanism of Action/
FDA-approved indications
Side Effects
P = % of patients on placebo
who experienced side effect
Drug/Lab Interactions Precautions/
Contraindications
Amphetamine sulphate

(Evekeo®)
Evekeo® - tablet
  • 5 mg
  • 10 mg
ADHD
  • Children 3 - 5 years old
    • Starting: 2.5 mg once daily
    • Increase daily dose in increments of 2.5 mg at weekly intervals
  • Children ≥ 6 years old
    • Starting: 5 mg once or twice daily
    • Increase daily dose in increments of 5 mg at weekly intervals
    • Doses > 40 mg a day are rare
    • Give first dose on awakening and additional doses at intervals of 4 - 6 hours

Narcolepsy
  • Children 6 - 12 years old
    • Starting: 5 mg once daily
    • Increase daily dose in increments of 5 mg at weekly intervals
  • Children ≥ 12 years old
    • Starting: 10 mg daily
    • Increase daily dose in increments of 10 mg at weekly intervals
    • Usual dose 5 - 60 mg/day
    • Give first dose on awakening and additional doses at intervals of 4 - 6 hours

Obesity
  • Children ≥ 12 years old
    • 5 - 10 mg given 30 - 60 minutes before each meal
    • Usual daily dose is 30 mg
Evekeo® tablet
NO/$$$$ (60 tablets)
  • Tablets are scored and may be broken in two

  • May take without regard to food
Mechanism of action
  • Amphetamines are CNS stimulants

  • Amphetamines are thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space

  • The mode of therapeutic action in ADHD is not known

  • In weight loss, amphetamines are thought to suppress appetite

FDA-approved indications

Evekeo
  • ADHD
  • Narcolepsy
  • Obesity
NOTE: Incidence of side effects for Evekeo are not well-defined. Amphetamine sulphate is a component of Adderall. Information from the Adderall XR PI is listed below. Side effects of Evekeo would be expected to be the similar, but may not be exactly the same. Only side effects that occurred at an incidence of ≥ 3% and ≥ 3% more than placebo are listed.

Children (6 - 12 years old)
  • Loss of appetite - 22%, P - 2%
  • Insomnia - 17%, P - 2%
  • Upset stomach- 14%, P - 10%
  • Emotional lability - 9%, P - 2%
  • Vomiting - 7%, P - 4%
  • Nervousness - 6%, P - 2%
  • Fever - 5%, P - 2%
  • Weight loss - 4%, P - 0%

Adults
  • Dry mouth - 35%, P - 5%
  • Loss of appetite - 33%, P - 3%
  • Insomnia - 27%, P - 13%
  • Headache - 26%, P - 13%
  • Weight loss - 10%, P - 0%
  • Nausea - 8%, P - 3%
  • Agitation - 8%, P - 5%
  • Anxiety - 8%, P - 5%
  • Dizziness - 7%, P - 0%
  • Diarrhea - 6%, P - 0%
  • Tachycardia - 6%, P - 3%
  • Urinary tract infection - 5%, P - 0%
Drug interactions
  • MAO inhibitors - DO NOT COMBINE. Do not use within 14 days of taking an MAO inhibitor.
  • Antacids - antacids may increase the absorption of amphetamines thereby increasing exposure and risk of adverse events
  • Alpha blockers - stimulants may counteract the effects of alpha blockers
  • Beta blockers - stimulants may counteract the effects of beta blockers
  • Blood pressure medications - stimulants may raise blood pressure and counteract the effects of blood pressure medications
  • Tricyclic antidepressants (TCAs) - stimulants may potentiate the effects of TCAs and vice versa
  • Meperidine - stimulants may potentiate the effects of meperidine
  • Antipsychotics - antipsychotics may reduce the effects of stimulants
  • Lithium - lithium may block the effects of stimulants
  • Proton pump inhibitors (ex. omeprazole, Prevacid, Nexium, etc.) - PPIs may increase the rate of absorption of amphetamines
  • Urinary alkalizers (e.g. acetazolamide, metolazone) - may decrease the clearance of amphetamines and increase exposure
  • Acidifying agents (Ascorbic acid, fruit juices, etc.) - may decrease absorption of amphetamines
  • Phenobarbital - amphetamines may delay the absorption of phenobarbital
  • Phenytoin - amphetamines may delay the absorption of phenytoin

Lab interactions
  • Corticosteroid levels - amphetamines may cause elevations in corticosteroid levels
  • Drug abuse and dependence - stimulants have the potential for drug abuse and dependence. Use caution in susceptible patients.
  • Heart disease - stimulants may exacerbate and worsen heart disease. Avoid or use caution in susceptible patients.
  • Heart arrhythmias - stimulants may exacerbate heart arrhythmias. Avoid use in susceptible patients.
  • Suppression of growth - stimulant medications can suppress growth rates in children. The effect appears to be directly related to dose and length of therapy. In studies, growth rates in children taking stimulants were 1 - 2 cm/year slower than controls. There is no conclusive evidence that stimulants affect adult height achieved. [1,2,3,4,5]
  • Hypertension - stimulants may raise blood pressure and worsen hypertension. Average blood pressure increase seen in trials was ∼ 2 - 4 mmHg. Average heart rate increase was 3 - 6 bpm.
  • Seizures - stimulants may lower the seizure threshold
  • Hyperthyroidism - stimulants may exacerbate symptoms of hyperthyroidism
  • Glaucoma - stimulants may worsen glaucoma
  • Psychosis - stimulants may worsen psychosis
  • Bipolar mania - stimulants may precipitate bipolar mania
  • Raynaud's phenomenon - stimulants may exacerbate Raynaud's phenomenon
  • Tourette's syndrome and tics - stimulants may worsen motor tics and tics associated with Tourette's syndrome
  • Visual changes - difficulties with accommodation and blurring of vision have been reported with stimulant medications
  • Liver disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.
  • Kidney disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.

Drug Dosage form Dosage Generic/Price Other/
Pharmacokinetics
Mechanism of Action/
FDA-approved indications
Side Effects
P = % of patients on placebo
who experienced side effect
Drug/Lab Interactions Precautions/
Contraindications
Dexmethylphenidate

(Focalin®)
(Focalin XR®)
Focalin® - tablet
  • 2.5 mg
  • 5 mg
  • 10 mg

Focalin XR®
Extended-release capsule

  • 5 mg
  • 10 mg
  • 15 mg
  • 20 mg
  • 25 mg
  • 30 mg
  • 35 mg
  • 40 mg
Focalin®
ADHD
  • Children ≥ 6 years old
    • Starting: 2.5 mg twice daily
    • Maximum: 10 mg twice daily
    • Doses should be given at least 4 hours apart
    • Increase dose by 2.5 - 5 mg at weekly intervals
    • For patients switching from methylphenidate, the recommended starting Focalin dose is one-half the methylphenidate dose

Focalin XR®
ADHD
  • Children ≥ 6 - 17 years old
    • Starting: 5 mg once daily
    • Maximum: 30 mg once daily
    • Increase dose by 5 mg at weekly intervals
    • For patients switching from methylphenidate, the recommended starting Focalin XR dose is one-half the methylphenidate dose
    • When switching from Focalin, total daily Focalin dose can be given as once daily Focalin XR dose

  • Adults
    • Starting: 10 mg once daily
    • Maximum: 40 mg once daily
    • Increase dose by 10 mg at weekly intervals
    • For patients switching from methylphenidate, the recommended starting Focalin XR dose is one-half the methylphenidate dose
    • When switching from Focalin, total daily Focalin dose can be given as once daily Focalin XR dose
Focalin® tablet
YES/$-$$ (#60)

Focalin XR® capsule
YES/$$$$ (#30)

25 and 35 mg doses only available as brand
Other
Focalin®
  • May take without regard to food

Focalin XR®
  • Capsules may be opened and sprinkled on applesauce. Swallow applesauce whole, do not chew.
  • May take without regard to food

Pharmacokinetics

Focalin®
  • Time to max level: 1 - 1.5 hours
  • Half-life: 2.2 hours

Focalin XR®
  • Time to max level: bimodal
    • First: 1.5 hours
    • Second: 6.5 hours

  • Half-life: 2 - 4.5 hours
Mechanism of action
  • Dexmethylphenidate is the more pharmacologically active d-enantiomer of racemic methylphenidate
  • Dexmethylphenidate is a CNS stimulant
  • Dexmethylphenidate is thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space
  • The mode of therapeutic action in ADHD is not known


FDA-approved indications

Focalin and Focalin XR
  • ADHD
NOTE: Information is from Focalin XR PI. Only side effects that occurred at an incidence of ≥ 5% and twice the incidence of placebo are listed.

Children
  • Gastrointestinal disorders - 38%, P - 19%
  • Decreased appetite - 30%, P - 9%
  • Psychiatric disorders - 26%, P - 15%
  • Headache - 25%, P - 11%
  • Upset stomach - 8%, P - 4%
  • Anxiety - 6%, P - 0%

NOTE: Information is from Focalin XR PI . Information is for 40 mg/day dose. Only side effects that occurred at an incidence of ≥ 3% and ≥ 3% more than placebo are listed.

Adults
  • Psychiatric disorders - 46%, P - 30%
  • Gastrointestinal disorders - 44%, P - 19%
  • Headache - 39%, P - 19%
  • Dry mouth - 20%, P - 4%
  • Anxiety - 11%, P - 2%
  • Upset stomach - 9%, P - 2%
  • Pharyngolaryngeal pain - 7%, P - 2%
  • Weight loss - In one study, adults lost an average of 3.74 pounds on Focalin XR
Drug interactions
  • MAO inhibitors - DO NOT COMBINE. Do not use within 14 days of taking an MAO inhibitor.
  • Heartburn medications (antacids, PPIs, H2 antagonists, etc.) - heartburn medications may alter the absorption of Focalin XR
  • Alpha blockers - stimulants may counteract the effects of alpha blockers
  • Beta blockers - stimulants may counteract the effects of beta blockers
  • Blood pressure medications - stimulants may raise blood pressure and counteract the effects of blood pressure medications
  • Warfarin - methylphenidate may inhibit warfarin metabolism and increase exposure. Monitor INR closely with concomitant use.
  • Phenobarbital - methylphenidate may inhibit phenobarbital metabolism and increase exposure. Monitor levels closely with concomitant use.
  • Phenytoin - methylphenidate may inhibit phenytoin metabolism and increase exposure. Monitor levels closely with concomitant use.
  • Tricyclic antidepressants (TCAs) - methylphenidate may inhibit the metabolism of tricyclic antidepressants and increase exposure. Use caution with concomitant use.
  • Meperidine - stimulants may potentiate the effects of meperidine
  • Antipsychotics - antipsychotics may reduce the effects of stimulants
  • Lithium - lithium may block the effects of stimulants

Lab interactions
  • Corticosteroid levels - stimulants may cause elevations in corticosteroid levels
  • Drug abuse and dependence - stimulants have the potential for drug abuse and dependence. Use caution in susceptible patients.
  • Heart disease - stimulants may exacerbate and worsen heart disease. Avoid or use caution in susceptible patients.
  • Heart arrhythmias - stimulants may exacerbate heart arrhythmias. Avoid use in susceptible patients.
  • Suppression of growth - stimulant medications can suppress growth rates in children. The effect appears to be directly related to dose and length of therapy. In studies, growth rates in children taking stimulants were 1 - 2 cm/year slower than controls. There is no conclusive evidence that stimulants affect adult height achieved. [1,2,3,4,5]
  • Hypertension - stimulants may raise blood pressure and worsen hypertension. In adult trials, average diastolic blood pressure increase seen with Focalin XR 40 mg was ∼ 2 mmHg (SD 8 mmHg). Average heart rate increase was 6 bpm (SD 10 bpm).
  • Seizures - stimulants may lower the seizure threshold
  • Hyperthyroidism - stimulants may exacerbate symptoms of hyperthyroidism
  • Glaucoma - stimulants may worsen glaucoma
  • Psychosis - stimulants may worsen psychosis
  • Bipolar mania - stimulants may precipitate bipolar mania
  • Raynaud's phenomenon - stimulants may exacerbate Raynaud's phenomenon
  • Tourette's syndrome and tics - stimulants may worsen motor tics and tics associated with Tourette's syndrome
  • Priapism - erections lasting more than 4 hours (priapism) have been reported with methylphenidate products
  • Visual changes - difficulties with accommodation and blurring of vision have been reported with stimulant medications
  • Liver disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.
  • Kidney disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.

Drug Dosage form Dosage Generic/Price Other/
Pharmacokinetics
Mechanism of Action/
FDA-approved indications
Side Effects
P = % of patients on placebo
who experienced side effect
Drug/Lab Interactions Precautions/
Contraindications
Dextroamphetamine sulfate

(Dexedrine®)
(Dexedrine spansule®)
Dexedrine® - tablet
  • 5 mg
  • 10 mg

Dexedrine® - solution
  • 5 mg/5 ml (1 mg/ml)

Dexedrine spansule®
Extended-release capsule

  • 5 mg
  • 10 mg
  • 15 mg
Dexedrine®
ADHD
  • Children 3 - 5 years old
    • Starting: 2.5 mg once daily
    • Increase daily dose in increments of 2.5 mg at weekly intervals
  • Children ≥ 6 years old
    • Starting: 5 mg once or twice daily
    • Increase daily dose in increments of 5 mg at weekly intervals
    • Doses > 40 mg a day are rare
    • Give first dose on awakening and additional doses at intervals of 4 - 6 hours

Narcolepsy
  • Children 6 - 12 years old
    • Starting: 5 mg/day given in divided doses
    • Increase daily dose in increments of 5 mg at weekly intervals
  • Children ≥ 12 years old
    • Starting: 10 mg/day given in divided doses
    • Increase daily dose in increments of 10 mg at weekly intervals
    • Usual dose 5 - 60 mg/day
    • Give first dose on awakening and additional doses at intervals of 4 - 6 hours

Dexedrine spansule®
ADHD
  • Children ≥ 6 years old
    • Starting: 5 - 10 mg once daily
    • Increase daily dose in increments of 5 mg at weekly intervals
    • Doses > 40 mg/day are rarely needed

Narcolepsy
  • Children 6 - 12 years old
    • Starting: 5 mg once daily
    • Increase daily dose in increments of 5 mg at weekly intervals
  • Children ≥ 12 years old
    • Starting: 10 mg once daily
    • Increase daily dose in increments of 10 mg at weekly intervals
    • Usual dose 5 - 60 mg/day
Dexedrine® tablet
YES/$$ (#60)

Dexedrine spansule®
YES/$$$ (#30)

Dexedrine solution
YES/$$$$ (300 ml)

Other
Dexedrine®
  • May take without regard to food
  • Tablets are scored so that they may be halved

Dexedrine spansule®
  • Swallow capsules whole
  • May take without regard to food

Pharmacokinetics
Dexedrine®
  • Time to max level: 3 hours
  • Half-life: 12 hours

Dexedrine spansule®
  • Time to max level: 8 hours
  • Half-life: 12 hours
Mechanism of action
  • Amphetamines are CNS stimulants
  • Amphetamines are thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space
  • The mode of therapeutic action in ADHD is not known


FDA-approved indications
  • ADHD
  • Narcolepsy
NOTE: Incidence of side effects for Dexedrine are not well-defined. Dextroamphetamine sulphate is a component of Adderall. Information from the Adderall XR PI is listed below. Side effects of Dexedrine would be expected to be the similar, but may not be exactly the same. Only side effects that occurred at an incidence of ≥ 3% and ≥ 3% more than placebo are listed.

Children (6 - 12 years old)
  • Loss of appetite - 22%, P - 2%
  • Insomnia - 17%, P - 2%
  • Upset stomach- 14%, P - 10%
  • Emotional lability - 9%, P - 2%
  • Vomiting - 7%, P - 4%
  • Nervousness - 6%, P - 2%
  • Fever - 5%, P - 2%
  • Weight loss - 4%, P - 0%

Adults
  • Dry mouth - 35%, P - 5%
  • Loss of appetite - 33%, P - 3%
  • Insomnia - 27%, P - 13%
  • Headache - 26%, P - 13%
  • Weight loss - 10%, P - 0%
  • Nausea - 8%, P - 3%
  • Agitation - 8%, P - 5%
  • Anxiety - 8%, P - 5%
  • Dizziness - 7%, P - 0%
  • Diarrhea - 6%, P - 0%
  • Tachycardia - 6%, P - 3%
  • Urinary tract infection - 5%, P - 0%
Drug interactions
  • MAO inhibitors - DO NOT COMBINE. Do not use within 14 days of taking an MAO inhibitor.
  • Antacids - antacids may increase the absorption of amphetamines thereby increasing exposure and risk of adverse events
  • Alpha blockers - stimulants may counteract the effects of alpha blockers
  • Beta blockers - stimulants may counteract the effects of beta blockers
  • Blood pressure medications - stimulants may raise blood pressure and counteract the effects of blood pressure medications
  • Tricyclic antidepressants (TCAs) - stimulants may potentiate the effects of TCAs and vice versa
  • Meperidine - stimulants may potentiate the effects of meperidine
  • Antipsychotics - antipsychotics may reduce the effects of stimulants
  • Lithium - lithium may block the effects of stimulants
  • Proton pump inhibitors (ex. omeprazole, Prevacid, Nexium, etc.) - PPIs may increase the rate of absorption of amphetamines
  • Urinary alkalizers (e.g. acetazolamide, metolazone) - may decrease the clearance of amphetamines and increase exposure
  • Acidifying agents (Ascorbic acid, fruit juices, etc.) - may decrease absorption of amphetamines
  • Phenobarbital - amphetamines may delay the absorption of phenobarbital
  • Phenytoin - amphetamines may delay the absorption of phenytoin

Lab interactions
  • Corticosteroid levels - amphetamines may cause elevations in corticosteroid levels
  • Drug abuse and dependence - stimulants have the potential for drug abuse and dependence. Use caution in susceptible patients.
  • Heart disease - stimulants may exacerbate and worsen heart disease. Avoid or use caution in susceptible patients.
  • Heart arrhythmias - stimulants may exacerbate heart arrhythmias. Avoid use in susceptible patients.
  • Suppression of growth - stimulant medications can suppress growth rates in children. The effect appears to be directly related to dose and length of therapy. In studies, growth rates in children taking stimulants were 1 - 2 cm/year slower than controls. There is no conclusive evidence that stimulants affect adult height achieved. [1,2,3,4,5]
  • Hypertension - stimulants may raise blood pressure and worsen hypertension. Average blood pressure increase seen in trials was ∼ 2 - 4 mmHg. Average heart rate increase was 3 - 6 bpm.
  • Seizures - stimulants may lower the seizure threshold
  • Hyperthyroidism - stimulants may exacerbate symptoms of hyperthyroidism
  • Glaucoma - stimulants may worsen glaucoma
  • Psychosis - stimulants may worsen psychosis
  • Bipolar mania - stimulants may precipitate bipolar mania
  • Raynaud's phenomenon - stimulants may exacerbate Raynaud's phenomenon
  • Tourette's syndrome and tics - stimulants may worsen motor tics and tics associated with Tourette's syndrome
  • Visual changes - difficulties with accommodation and blurring of vision have been reported with stimulant medications
  • Liver disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.
  • Kidney disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.

Drug Dosage form Dosage Generic/Price Other/
Pharmacokinetics
Mechanism of Action/
FDA-approved indications
Side Effects
P = % of patients on placebo
who experienced side effect
Drug/Lab Interactions Precautions/
Contraindications
Lisdexamfetamine

(Vyvanse®)
Vyvanse® - capsule
  • 10 mg
  • 20 mg
  • 30 mg
  • 40 mg
  • 50 mg
  • 60 mg
  • 70 mg
ADHD
  • Children ≥ 6 years and adults
    • Starting: 30 mg once daily
    • Maximum: 70 mg once daily
    • Increase dose in increments of 10 - 20 mg at weekly intervals

Binge eating disorder
  • Adults
    • Starting: 30 mg once daily
    • Target: 50 - 70 mg once daily
    • Maximum: 70 mg once daily
    • Increase dose in increments of 20 mg at weekly intervals
Vyvanse® capsule
NO/$$$$ (#30)

Other
  • May take without regard to food
  • Capsules may be opened and contents mixed with yogurt, water, or orange juice. Contents should be mixed until completely dispersed. Film coating left in glass is inactive ingredients. Active component dissolves completely.

Pharmacokinetics
  • Time to max level: 3.5 hours
  • Lisdexamfetamine is converted to dextroamphetamine
  • Half-life of dextroamphetamine is 12 hours
Mechanism of action
  • Lisdexamfetamine is a prodrug of dextroamphetamine
  • Amphetamines are CNS stimulants
  • Amphetamines are thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space
  • The mode of therapeutic action in ADHD is not known
  • The mode of action in binge eating disorder is thought to occur through appetite suppression

FDA-approved indications

  • ADHD
  • Moderate to severe binge eating disorder
NOTE: Only side effects that occurred at an incidence of ≥ 4% and twice the incidence of placebo are listed.

Children (6 - 12 years old)
  • Decreased appetite - 39%, P - 4%
  • Insomnia - 23%, P - 3%
  • Upper abdominal pain - 12%, P - 6%
  • Irritability - 10%, P - 0%
  • Vomiting - 9%, P - 4%
  • Weight loss* - 9%, P - 1%
  • Nausea - 6%, P - 3%
  • Dry mouth - 5%, P - 0%
  • Dizziness - 5%, P - 0%

*Average weight loss after 4 weeks of therapy was 0.9, 1.9, and 2.5 pounds, respectively, for patients receiving 30 mg, 50 mg, and 70 mg
Adults
  • Decreased appetite - 27%, P - 2%
  • Insomnia - 27%, P - 8%
  • Dry mouth - 26%, P - 3%
  • Diarrhea - 7%, P - 0%
  • Nausea - 7%, P - 0%
  • Anxiety - 6%, P - 0%
  • Anorexia - 5%, P - 0%
  • Feeling jittery - 4%, P - 0%
  • Weight loss - average weight loss after 4 weeks of therapy was 2.8 pounds, 3.1 pounds, and 4.3 pounds, respectively, for patients receiving final doses of 30 mg, 50 mg, and 70 mg
Drug interactions
  • MAO inhibitors - DO NOT COMBINE. Do not use within 14 days of taking an MAO inhibitor.
  • Alpha blockers - stimulants may counteract the effects of alpha blockers
  • Beta blockers - stimulants may counteract the effects of beta blockers
  • Blood pressure medications - stimulants may raise blood pressure and counteract the effects of blood pressure medications
  • Tricyclic antidepressants (TCAs) - stimulants may potentiate the effects of TCAs and vice versa
  • Meperidine - stimulants may potentiate the effects of meperidine
  • Antipsychotics - antipsychotics may reduce the effects of stimulants
  • Lithium - lithium may block the effects of stimulants
  • Urinary alkalizers (e.g. acetazolamide, metolazone) - may decrease the clearance of amphetamines and increase exposure
  • Urinary acidifiers (ex. ascorbic acid, etc.) - may increase the clearance of amphetamines and decrease exposure

Lab interactions
  • Corticosteroid levels - amphetamines may cause elevations in corticosteroid levels
  • Drug abuse and dependence - stimulants have the potential for drug abuse and dependence. Use caution in susceptible patients.
  • Heart disease - stimulants may exacerbate and worsen heart disease. Avoid or use caution in susceptible patients.
  • Heart arrhythmias - stimulants may exacerbate heart arrhythmias. Avoid use in susceptible patients.
  • Suppression of growth - stimulant medications can suppress growth rates in children. The effect appears to be directly related to dose and length of therapy. In studies, growth rates in children taking stimulants were 1 - 2 cm/year slower than controls. There is no conclusive evidence that stimulants affect adult height achieved. [1,2,3,4,5]
  • Hypertension - stimulants may raise blood pressure and worsen hypertension. Average blood pressure increase seen in trials was ∼ 2 - 4 mmHg. Average heart rate increase was 3 - 6 bpm.
  • Seizures - stimulants may lower the seizure threshold
  • Hyperthyroidism - stimulants may exacerbate symptoms of hyperthyroidism
  • Glaucoma - stimulants may worsen glaucoma
  • Psychosis - stimulants may worsen psychosis
  • Bipolar mania - stimulants may precipitate bipolar mania
  • Raynaud's phenomenon - stimulants may exacerbate Raynaud's phenomenon
  • Tourette's syndrome and tics - stimulants may worsen motor tics and tics associated with Tourette's syndrome
  • Visual changes - difficulties with accommodation and blurring of vision have been reported with stimulant medications
  • Liver disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.
  • Kidney disease
    • CrCl 15 - <30 ml/min: do not exceed 50 mg/day
    • CrCl < 15 ml/min: do not exceed 30 mg/day


Drug Dosage form Dosage Generic/Price Other/
Pharmacokinetics
Mechanism of Action/
FDA-approved indications
Side Effects
P = % of patients on placebo
who experienced side effect
Drug/Lab Interactions Precautions/
Contraindications
Methamphetamine hydrochloride

(Desoxyn®)
Desoxyn® - tablet
  • 5 mg
ADHD
  • Children ≥ 6 years old
    • Starting: 5 mg once or twice daily
    • Increase daily dose in increments of 5 mg at weekly intervals
    • Usual effective dose is 20 - 25 mg daily
    • Total daily dose may be given once daily or divided into two doses

Obesity
  • Children ≥ 12 years old and adults
    • Starting: 5 mg one-half hour before meals
    • Treatment should not exceed a few weeks

Desoxyn® tablet
YES/$$$$ (#60)
Other
  • May take without regard to food

Pharmacokinetics
  • Half-life: 4 - 5 hours
Mechanism of action
  • Amphetamines are CNS stimulants
  • Amphetamines are thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space
  • The mode of therapeutic action in ADHD is not known
  • In weight loss, amphetamines are thought to suppress appetite

FDA-approved indications
  • ADHD
  • Obesity
NOTE: Incidence of side effects for Desoxyn are not well-defined. Desoxyn is metabolized to amphetamine. Amphetamine is a component of Adderall. Information from the Adderall XR PI is listed below. Side effects of Desoxyn would be expected to be the similar, but may not be exactly the same. Only side effects that occurred at an incidence of ≥ 3% and ≥ 3% more than placebo are listed.

Children (6 - 12 years old)
  • Loss of appetite - 22%, P - 2%
  • Insomnia - 17%, P - 2%
  • Upset stomach- 14%, P - 10%
  • Emotional lability - 9%, P - 2%
  • Vomiting - 7%, P - 4%
  • Nervousness - 6%, P - 2%
  • Fever - 5%, P - 2%
  • Weight loss - 4%, P - 0%

Adults
  • Dry mouth - 35%, P - 5%
  • Loss of appetite - 33%, P - 3%
  • Insomnia - 27%, P - 13%
  • Headache - 26%, P - 13%
  • Weight loss - 10%, P - 0%
  • Nausea - 8%, P - 3%
  • Agitation - 8%, P - 5%
  • Anxiety - 8%, P - 5%
  • Dizziness - 7%, P - 0%
  • Diarrhea - 6%, P - 0%
  • Tachycardia - 6%, P - 3%
  • Urinary tract infection - 5%, P - 0%
Drug interactions
  • MAO inhibitors - DO NOT COMBINE. Do not use within 14 days of taking an MAO inhibitor.
  • Antacids - antacids may increase the absorption of amphetamines thereby increasing exposure and risk of adverse events
  • Alpha blockers - stimulants may counteract the effects of alpha blockers
  • Beta blockers - stimulants may counteract the effects of beta blockers
  • Blood pressure medications - stimulants may raise blood pressure and counteract the effects of blood pressure medications
  • Tricyclic antidepressants (TCAs) - stimulants may potentiate the effects of TCAs and vice versa
  • Meperidine - stimulants may potentiate the effects of meperidine
  • Antipsychotics - antipsychotics may reduce the effects of stimulants
  • Lithium - lithium may block the effects of stimulants
  • Proton pump inhibitors (ex. omeprazole, Prevacid, Nexium, etc.) - PPIs may increase the rate of absorption of amphetamines
  • Urinary alkalizers (e.g. acetazolamide, metolazone) - may decrease the clearance of amphetamines and increase exposure
  • Acidifying agents (Ascorbic acid, fruit juices, etc.) - may decrease absorption of amphetamines
  • Phenobarbital - amphetamines may delay the absorption of phenobarbital
  • Phenytoin - amphetamines may delay the absorption of phenytoin

Lab interactions
  • Corticosteroid levels - amphetamines may cause elevations in corticosteroid levels
  • Drug abuse and dependence - stimulants have the potential for drug abuse and dependence. Use caution in susceptible patients.
  • Heart disease - stimulants may exacerbate and worsen heart disease. Avoid or use caution in susceptible patients.
  • Heart arrhythmias - stimulants may exacerbate heart arrhythmias. Avoid use in susceptible patients.
  • Suppression of growth - stimulant medications can suppress growth rates in children. The effect appears to be directly related to dose and length of therapy. In studies, growth rates in children taking stimulants were 1 - 2 cm/year slower than controls. There is no conclusive evidence that stimulants affect adult height achieved. [1,2,3,4,5]
  • Hypertension - stimulants may raise blood pressure and worsen hypertension. Average blood pressure increase seen in trials was ∼ 2 - 4 mmHg. Average heart rate increase was 3 - 6 bpm.
  • Seizures - stimulants may lower the seizure threshold
  • Hyperthyroidism - stimulants may exacerbate symptoms of hyperthyroidism
  • Glaucoma - stimulants may worsen glaucoma
  • Psychosis - stimulants may worsen psychosis
  • Bipolar mania - stimulants may precipitate bipolar mania
  • Raynaud's phenomenon - stimulants may exacerbate Raynaud's phenomenon
  • Tourette's syndrome and tics - stimulants may worsen motor tics and tics associated with Tourette's syndrome
  • Visual changes - difficulties with accommodation and blurring of vision have been reported with stimulant medications
  • Liver disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.
  • Kidney disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.

Drug Dosage form Dosage Generic/Price Other/
Pharmacokinetics
Mechanism of Action/
FDA-approved indications
Side Effects
P = % of patients on placebo
who experienced side effect
Drug/Lab Interactions Precautions/
Contraindications
Methylphenidate hydrochloride

(Aptensio XR®)
Aptensio XR®
Extended-release capsule

  • 10 mg
  • 15 mg
  • 20 mg
  • 30 mg
  • 40 mg
  • 50 mg
  • 60 mg
ADHD
  • Children ≥ 6 years old
    • Starting: 10 mg once daily
    • Maximum: 60 mg once daily
    • Increase daily dose in increments of 10 mg at weekly intervals
Aptensio XR®
NO/$$$$ (#30)
Other
  • May take without regard to food
  • Capsules may be opened and sprinkled on applesauce. Swallow applesauce whole, do not chew.

Pharmacokinetics
  • Time to max level: bimodal
    • First: 2 hours
    • Second: 8 hours

  • Half-life: 5 hours
Mechanism of action
  • Methylphenidate is a CNS stimulant
  • Stimulants are thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space
  • The mode of therapeutic action in ADHD is not known

FDA-approved indications

Aptensio XR
  • ADHD
NOTE: Only side effects that occurred at an incidence of ≥ 3% are listed.

Children (≥ 6 years old)
  • Headache - 10.9%, P - 8.5%
  • Insomnia - 9.8%, P - 2.1%
  • Upper abdominal pain - 8.2%, P - 0%
  • Decreased appetite - 4.9%, P - 0%
  • Vomiting - 3.8%, P - 0%
  • Nausea - 3.8%, P - 2.1%
  • Dizziness - 2.2%, P - 2.1%
Drug interactions
  • MAO inhibitors - DO NOT COMBINE. Do not use within 14 days of taking an MAO inhibitor.
  • Alpha blockers - stimulants may counteract the effects of alpha blockers
  • Beta blockers - stimulants may counteract the effects of beta blockers
  • Blood pressure medications - stimulants may raise blood pressure and counteract the effects of blood pressure medications
  • Warfarin - methylphenidate may inhibit warfarin metabolism and increase exposure. Monitor INR closely with concomitant use.
  • Phenobarbital - methylphenidate may inhibit phenobarbital metabolism and increase exposure. Monitor levels closely with concomitant use.
  • Phenytoin - methylphenidate may inhibit phenytoin metabolism and increase exposure. Monitor levels closely with concomitant use.
  • Tricyclic antidepressants (TCAs) - methylphenidate may inhibit the metabolism of tricyclic antidepressants and increase exposure. Use caution with concomitant use.
  • SSRI antidepressants - methylphenidate may inhibit the metabolism of SSRI antidepressants and increase exposure. Use caution with concomitant use.
  • Meperidine - stimulants may potentiate the effects of meperidine
  • Antipsychotics - antipsychotics may reduce the effects of stimulants
  • Lithium - lithium may block the effects of stimulants
  • Halogenated anesthetics - sudden blood pressure increases may occur during surgery

Lab interactions
  • Corticosteroid levels - methylphenidate may cause elevations in corticosteroid levels
  • Drug abuse and dependence - stimulants have the potential for drug abuse and dependence. Use caution in susceptible patients.
  • Heart disease - stimulants may exacerbate and worsen heart disease. Avoid or use caution in susceptible patients.
  • Heart arrhythmias - stimulants may exacerbate heart arrhythmias. Avoid use in susceptible patients.
  • Suppression of growth - stimulant medications can suppress growth rates in children. The effect appears to be directly related to dose and length of therapy. In studies, growth rates in children taking stimulants were 1 - 2 cm/year slower than controls. There is no conclusive evidence that stimulants affect adult height achieved. [1,2,3,4,5]
  • Hypertension - stimulants may raise blood pressure and worsen hypertension. Average blood pressure increase seen in trials was ∼ 2 - 4 mmHg. Average heart rate increase was 3 - 6 bpm.
  • Seizures - stimulants may lower the seizure threshold
  • Hyperthyroidism - stimulants may exacerbate symptoms of hyperthyroidism
  • Glaucoma - stimulants may worsen glaucoma
  • Psychosis - stimulants may worsen psychosis
  • Bipolar mania - stimulants may precipitate bipolar mania
  • Raynaud's phenomenon - stimulants may exacerbate Raynaud's phenomenon
  • Priapism - erections lasting more than 4 hours (priapism) have been reported with methylphenidate products
  • Tourette's syndrome and tics - stimulants may worsen motor tics and tics associated with Tourette's syndrome
  • Visual changes - difficulties with accommodation and blurring of vision have been reported with stimulant medications
  • Liver disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.
  • Kidney disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.

Drug Dosage form Dosage Generic/Price Other/
Pharmacokinetics
Mechanism of Action/
FDA-approved indications
Side Effects
P = % of patients on placebo
who experienced side effect
Drug/Lab Interactions Precautions/
Contraindications
Methylphenidate hydrochloride

(Concerta®)
Concerta®
Extended-release tablet

  • 18 mg
  • 27 mg
  • 36 mg
  • 54 mg
ADHD
  • Children 6 - 12 years
    • Starting: 18 mg once daily
    • Maintenance: 18 - 54 mg once daily
    • Maximum: 54 mg once daily
    • Increase daily dose in increments of 18 mg at weekly intervals

  • Adolescents 13 - 17 years
    • Starting: 18 mg once daily
    • Maintenance: 18 - 72 mg once daily
    • Maximum: 72 mg once daily or 2 mg/kg/day, whichever is lower
    • Increase daily dose in increments of 18 mg at weekly intervals

  • Adults 18 - 65 years
    • Starting: 18 - 36 mg once daily
    • Maintenance: 18 - 72 mg once daily
    • Maximum: 72 mg once daily
    • Increase daily dose in increments of 18 mg at weekly intervals

Switching from regular methylphenidate to Concerta

Methylphenidate dose Concerta dose
5 mg 2 - 3 times a day 18 mg
10 mg 2 - 3 times a day 36 mg
15 mg 2 - 3 times a day 54 mg
20 mg 2 - 3 times a day 72 mg

Concerta®
YES/$$$-$$$$ (#30)
Other
  • May take without regard to food
  • Do not cut, chew, or dissolve tablet
  • Nonabsorbable tablet shell may be seen in stool. This is normal.

Pharmacokinetics
  • Time to max level: 6 - 10 hours
  • Half-life: 3.5 hours
Mechanism of action
  • Methylphenidate is a CNS stimulant
  • Stimulants are thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space
  • The mode of therapeutic action in ADHD is not known

FDA-approved indications
  • ADHD
Children (≥ 6 years old)
NOTE: Only side effects that occurred at an incidence of ≥ 2% are listed.

  • Upper abdominal pain - 6.2%, P - 3.8%
  • Vomiting - 2.8%, P - 1.6%
  • Nasopharyngitis - 2.8%, P - 2.2%
  • Insomnia - 2.8%, P - 0.3%
  • Fever - 2.2%, P - 0.9%

Adults
NOTE: Only side effects that occurred at an incidence of ≥ 3% are listed.

  • Headache - 22.2%, P - 15.6%
  • Dry mouth - 14%, P - 3.8%
  • Nausea - 12.8%, P - 3.3%
  • Insomnia - 12.3%, P - 6.1%
  • Dizziness - 6.7%, P - 5.2%
  • Weight loss - 6.5%, P - 3.3%
  • Irritability - 5.8%, P - 1.4%
  • Excessive sweating - 5.1%, P - 0.9%
  • Rapid heart rate - 4.8%, P - 0%
  • Depressed mood - 3.9%, P - 1.4%
  • Nervousness - 3.1%, P - 0.5%
  • Restlessness - 3.1%, P - 0%
  • Palpitations - 3.1%, P - 0.9%
Drug interactions
  • MAO inhibitors - DO NOT COMBINE. Do not use within 14 days of taking an MAO inhibitor.
  • Alpha blockers - stimulants may counteract the effects of alpha blockers
  • Beta blockers - stimulants may counteract the effects of beta blockers
  • Blood pressure medications - stimulants may raise blood pressure and counteract the effects of blood pressure medications
  • Warfarin - methylphenidate may inhibit warfarin metabolism and increase exposure. Monitor INR closely with concomitant use.
  • Phenobarbital - methylphenidate may inhibit phenobarbital metabolism and increase exposure. Monitor levels closely with concomitant use.
  • Phenytoin - methylphenidate may inhibit phenytoin metabolism and increase exposure. Monitor levels closely with concomitant use.
  • Tricyclic antidepressants (TCAs) - methylphenidate may inhibit the metabolism of tricyclic antidepressants and increase exposure. Use caution with concomitant use.
  • SSRI antidepressants - methylphenidate may inhibit the metabolism of SSRI antidepressants and increase exposure. Use caution with concomitant use.
  • Meperidine - stimulants may potentiate the effects of meperidine
  • Antipsychotics - antipsychotics may reduce the effects of stimulants
  • Lithium - lithium may block the effects of stimulants
  • Halogenated anesthetics - sudden blood pressure increases may occur during surgery

Lab interactions
  • Corticosteroid levels - methylphenidate may cause elevations in corticosteroid levels
  • Drug abuse and dependence - stimulants have the potential for drug abuse and dependence. Use caution in susceptible patients.
  • Heart disease - stimulants may exacerbate and worsen heart disease. Avoid or use caution in susceptible patients.
  • Heart arrhythmias - stimulants may exacerbate heart arrhythmias. Avoid use in susceptible patients.
  • Suppression of growth - stimulant medications can suppress growth rates in children. The effect appears to be directly related to dose and length of therapy. In studies, growth rates in children taking stimulants were 1 - 2 cm/year slower than controls. There is no conclusive evidence that stimulants affect adult height achieved. [1,2,3,4,5]
  • Hypertension - stimulants may raise blood pressure and worsen hypertension. Average blood pressure increase seen in trials was ∼ 2 - 4 mmHg. Average heart rate increase was 3 - 6 bpm.
  • Seizures - stimulants may lower the seizure threshold
  • Gastrointestinal obstruction - Concerta is formulated in a non deformable tablet and could potentially cause obstruction in patients with GI motility issues (ex. strictures, short gut syndrome, cystic fibrosis, Meckel's diverticulum)
  • Hyperthyroidism - stimulants may exacerbate symptoms of hyperthyroidism
  • Glaucoma - stimulants may worsen glaucoma
  • Psychosis - stimulants may worsen psychosis
  • Bipolar mania - stimulants may precipitate bipolar mania
  • Raynaud's phenomenon - stimulants may exacerbate Raynaud's phenomenon
  • Priapism - erections lasting more than 4 hours (priapism) have been reported with methylphenidate products
  • Tourette's syndrome and tics - stimulants may worsen motor tics and tics associated with Tourette's syndrome. In a study lasting 27 months, the cumulative incidence of new onset tics was 9% with Concerta.
  • Visual changes - difficulties with accommodation and blurring of vision have been reported with stimulant medications
  • Liver disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.
  • Kidney disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.

Drug Dosage form Dosage Generic/Price Other/
Pharmacokinetics
Mechanism of Action/
FDA-approved indications
Side Effects
P = % of patients on placebo
who experienced side effect
Drug/Lab Interactions Precautions/
Contraindications
Methylphenidate hydrochloride

(Daytrana® patch)
Daytrana® patch
  • 10 mg/9 hours (1.1 mg/hr)
  • 15 mg/9 hours (1.6 mg/hr)
  • 20 mg/9 hours (2.2 mg/hr)
  • 30 mg/9 hours (3.3 mg/hr)
ADHD
  • Children ≥ 6 years
    • Patch is applied to the hip area 2 hours before effect is needed
    • Patch is removed after 9 hours
      • Titration schedule
        • Titrate to dose that achieves desired effect
        • Week 1: 10 mg patch
        • Week 2: 15 mg patch
        • Week 3: 20 mg patch
        • Week 4: 30 mg patch

Daytrana®
NO/$$$$ (#30)
Other
  • Rotate application sites daily between hips
  • Avoid exposing patch to heat. Heat may increase absorption and drug exposure.
  • Oil-based products (petroleum jelly, olive oil, or mineral oil) may be used to help remove the patch
  • Showering, swimming, and water exposure can affect patch adherence
  • Used patches should be folded and flushed down the toilet to prevent accidental exposure

Pharmacokinetics
  • Time to max level: 10 hours after single application; 8 hours after repeat application
Mechanism of action
  • Methylphenidate is a CNS stimulant
  • Stimulants are thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space
  • The mode of therapeutic action in ADHD is not known

FDA-approved indications
  • ADHD
NOTE: Only side effects that occurred at an incidence of ≥ 2% are listed.

Children (≥ 6 years old)
  • Decreased appetite - 25.5%, P - 4.7%
  • Headache - 15.3%, P - 11.8%
  • Insomnia - 13.3%, P - 4.7%
  • Nausea - 12.2%, P - 2.4%
  • Vomiting - 10.2%, P - 4.7%
  • Weight decrease - 9.2%, P - 0%
  • Abdominal pain - 7.1%, P - 5.9%
  • Tics - 7.1%, P - 0%
  • Irritability - 7.1%, P - 4.7%
  • Application site reactions - 6.7%
  • Affect lability - 6.1%, P - 0%
  • Anorexia - 5.1%, P - 1.2%
Drug interactions
  • MAO inhibitors - DO NOT COMBINE. Do not use within 14 days of taking an MAO inhibitor.
  • Alpha blockers - stimulants may counteract the effects of alpha blockers
  • Beta blockers - stimulants may counteract the effects of beta blockers
  • Blood pressure medications - stimulants may raise blood pressure and counteract the effects of blood pressure medications
  • Warfarin - methylphenidate may inhibit warfarin metabolism and increase exposure. Monitor INR closely with concomitant use.
  • Phenobarbital - methylphenidate may inhibit phenobarbital metabolism and increase exposure. Monitor levels closely with concomitant use.
  • Phenytoin - methylphenidate may inhibit phenytoin metabolism and increase exposure. Monitor levels closely with concomitant use.
  • Tricyclic antidepressants (TCAs) - methylphenidate may inhibit the metabolism of tricyclic antidepressants and increase exposure. Use caution with concomitant use.
  • SSRI antidepressants - methylphenidate may inhibit the metabolism of SSRI antidepressants and increase exposure. Use caution with concomitant use.
  • Meperidine - stimulants may potentiate the effects of meperidine
  • Antipsychotics - antipsychotics may reduce the effects of stimulants
  • Lithium - lithium may block the effects of stimulants
  • Halogenated anesthetics - sudden blood pressure increases may occur during surgery

Lab interactions
  • Corticosteroid levels - methylphenidate may cause elevations in corticosteroid levels
  • Loss of skin color - Daytrana patch has caused permanent loss of skin color in some patients. In most cases, the loss of skin color was limited to the areas around where the patch was rotated. Time of onset for skin color loss ranged from 2 months to 4 years. This condition is referred to as chemical leukoderma. If patients notice changes in skin color, they should contact their healthcare provider immediately. [FDA drug safety communication]
  • Contact sensitization - Daytrana may cause sensitization to methylphenidate in rare cases. Signs of contact sensitization include erythema, edema, papules, and vesicles at the application site that do not improve within 48 hours or spread beyond the patch site.
  • Drug abuse and dependence - stimulants have the potential for drug abuse and dependence. Use caution in susceptible patients.
  • Heart disease - stimulants may exacerbate and worsen heart disease. Avoid or use caution in susceptible patients.
  • Heart arrhythmias - stimulants may exacerbate heart arrhythmias. Avoid use in susceptible patients.
  • Suppression of growth - stimulant medications can suppress growth rates in children. The effect appears to be directly related to dose and length of therapy. In studies, growth rates in children taking stimulants were 1 - 2 cm/year slower than controls. There is no conclusive evidence that stimulants affect adult height achieved. [1,2,3,4,5]
  • Hypertension - stimulants may raise blood pressure and worsen hypertension. Average blood pressure increase seen in trials was ∼ 2 - 4 mmHg. Average heart rate increase was 3 - 6 bpm.
  • Seizures - stimulants may lower the seizure threshold
  • Hyperthyroidism - stimulants may exacerbate symptoms of hyperthyroidism
  • Glaucoma - stimulants may worsen glaucoma
  • Psychosis - stimulants may worsen psychosis
  • Bipolar mania - stimulants may precipitate bipolar mania
  • Raynaud's phenomenon - stimulants may exacerbate Raynaud's phenomenon
  • Priapism - erections lasting more than 4 hours (priapism) have been reported with methylphenidate products
  • Tourette's syndrome and tics - stimulants may worsen motor tics and tics associated with Tourette's syndrome
  • Visual changes - difficulties with accommodation and blurring of vision have been reported with stimulant medications
  • Liver disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.
  • Kidney disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.

Drug Dosage form Dosage Generic/Price Other/
Pharmacokinetics
Mechanism of Action/
FDA-approved indications
Side Effects
P = % of patients on placebo
who experienced side effect
Drug/Lab Interactions Precautions/
Contraindications
Methylphenidate hydrochloride

(Metadate CD®)
(Metadate ER®)
Metadate CD®
Extended-release capsule

  • 10 mg
  • 20 mg
  • 30 mg
  • 40 mg
  • 50 mg
  • 60 mg

Metadate ER®
Extended-release tablet

  • 20 mg
Metadate CD®
ADHD
  • Children ≥ 6 years
    • Starting: 20 mg once daily
    • Maximum: 60 mg once daily
    • Increase daily dose in increments of 10 - 20 mg at weekly intervals

Metadate ER®
ADHD
  • Metadate ER tablets have a duration of action of 8 hours
  • They may be used to replace immediate-release methylphenidate tablets where appropriate
  • Metadate ER is a generic version of Ritalin-SR
Metadate CD®
YES/$$-$$$ (#30)

Metadate ER®
YES/$-$$ (#30)
Other
Metadate CD
  • May take without regard to food
  • Capsules may be opened and sprinkled on applesauce. Swallow applesauce whole, do not chew.

Metadate ER
  • May take without regard to food
  • Do not cut, crush, or chew tablet


Pharmacokinetics
Metadate CD
  • Time to max level: bimodal
    • First: 1.5 hours
    • Second: 4.5 hours
  • Half-life: 6.8 hours

Metadate ER
  • Duration of action: 8 hours
Mechanism of action
  • Methylphenidate is a CNS stimulant
  • Stimulants are thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space
  • The mode of therapeutic action in ADHD is not known

FDA-approved indications

Metadate CD and ER
  • ADHD
NOTE: Information is from the Metadate CD PI. Only side effects that occurred at an incidence of ≥ 5% and more than placebo are listed.

Children (≥ 6 years old)
  • Headache - 12%, P - 8%
  • Loss of appetite - 9%, P - 2%
  • Abdominal pain - 7%, P - 4%
  • Insomnia - 5%, P - 2%
Drug interactions
  • MAO inhibitors - DO NOT COMBINE. Do not use within 14 days of taking an MAO inhibitor.
  • Alpha blockers - stimulants may counteract the effects of alpha blockers
  • Beta blockers - stimulants may counteract the effects of beta blockers
  • Blood pressure medications - stimulants may raise blood pressure and counteract the effects of blood pressure medications
  • Warfarin - methylphenidate may inhibit warfarin metabolism and increase exposure. Monitor INR closely with concomitant use.
  • Phenobarbital - methylphenidate may inhibit phenobarbital metabolism and increase exposure. Monitor levels closely with concomitant use.
  • Phenytoin - methylphenidate may inhibit phenytoin metabolism and increase exposure. Monitor levels closely with concomitant use.
  • Tricyclic antidepressants (TCAs) - methylphenidate may inhibit the metabolism of tricyclic antidepressants and increase exposure. Use caution with concomitant use.
  • SSRI antidepressants - methylphenidate may inhibit the metabolism of SSRI antidepressants and increase exposure. Use caution with concomitant use.
  • Meperidine - stimulants may potentiate the effects of meperidine
  • Antipsychotics - antipsychotics may reduce the effects of stimulants
  • Lithium - lithium may block the effects of stimulants
  • Halogenated anesthetics - sudden blood pressure increases may occur during surgery

Lab interactions
  • Corticosteroid levels - methylphenidate may cause elevations in corticosteroid levels
  • Drug abuse and dependence - stimulants have the potential for drug abuse and dependence. Use caution in susceptible patients.
  • Heart disease - stimulants may exacerbate and worsen heart disease. Avoid or use caution in susceptible patients.
  • Heart arrhythmias - stimulants may exacerbate heart arrhythmias. Avoid use in susceptible patients.
  • Suppression of growth - stimulant medications can suppress growth rates in children. The effect appears to be directly related to dose and length of therapy. In studies, growth rates in children taking stimulants were 1 - 2 cm/year slower than controls. There is no conclusive evidence that stimulants affect adult height achieved. [1,2,3,4,5]
  • Hypertension - stimulants may raise blood pressure and worsen hypertension. Average blood pressure increase seen in trials was ∼ 2 - 4 mmHg. Average heart rate increase was 3 - 6 bpm.
  • Seizures - stimulants may lower the seizure threshold
  • Hyperthyroidism - stimulants may exacerbate symptoms of hyperthyroidism
  • Glaucoma - stimulants may worsen glaucoma
  • Psychosis - stimulants may worsen psychosis
  • Bipolar mania - stimulants may precipitate bipolar mania
  • Raynaud's phenomenon - stimulants may exacerbate Raynaud's phenomenon
  • Priapism - erections lasting more than 4 hours (priapism) have been reported with methylphenidate products
  • Tourette's syndrome and tics - stimulants may worsen motor tics and tics associated with Tourette's syndrome
  • Visual changes - difficulties with accommodation and blurring of vision have been reported with stimulant medications
  • Liver disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.
  • Kidney disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.

Drug Dosage form Dosage Generic/Price Other/
Pharmacokinetics
Mechanism of Action/
FDA-approved indications
Side Effects
P = % of patients on placebo
who experienced side effect
Drug/Lab Interactions Precautions/
Contraindications
Methylphenidate hydrochloride

(Methylin®)
Methylin®
Chewable tablet

  • 2.5 mg
  • 5 mg
  • 10 mg

Solution
  • 10 mg/5 ml (2 mg/ml)
  • 5 mg/5 ml (1 mg/ml)
Methylin®
ADHD
  • Children ≥ 6 years
    • Starting: 5 mg given before breakfast and lunch
    • Maximum: 60 mg a day
    • Increase daily dose in increments of 5 - 10 mg at weekly intervals

  • Adults
    • Typical dose is 10 mg given 2 to 3 times a day
    • Maximum: 60 mg a day
    • Doses should be given 30 - 45 minutes before a meal
    • Take last dose before 6 pm to prevent insomnia
Methylin®
YES/$$$$
(#60 tab or 600 ml)
Other
  • May take without regard to food
  • Chewable tablet should be taken with a full glass of water to prevent choking
  • Chewable tablet contains phenylalanine

Pharmacokinetics
  • Time to max level: 1 - 2 hours
  • Half-life: 3 hours
Mechanism of action
  • Methylphenidate is a CNS stimulant
  • Stimulants are thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space
  • The mode of therapeutic action in ADHD is not known

FDA-approved indications
  • ADHD
  • Narcolepsy
NOTE: Incidence of side effects with Methylin are not well-defined. Information from the Concerta PI is listed below. Side effects of Methylin would be expected to be the similar, but may not be exactly the same.

Children (≥ 6 years old)
  • Upper abdominal pain - 6.2%, P - 3.8%
  • Vomiting - 2.8%, P - 1.6%
  • Nasopharyngitis - 2.8%, P - 2.2%
  • Insomnia - 2.8%, P - 0.3%
  • Fever - 2.2%, P - 0.9%

Adults
  • Headache - 22.2%, P - 15.6%
  • Dry mouth - 14%, P - 3.8%
  • Nausea - 12.8%, P - 3.3%
  • Insomnia - 12.3%, P - 6.1%
  • Dizziness - 6.7%, P - 5.2%
  • Weight loss - 6.5%, P - 3.3%
  • Irritability - 5.8%, P - 1.4%
  • Excessive sweating - 5.1%, P - 0.9%
  • Rapid heart rate - 4.8%, P - 0%
  • Depressed mood - 3.9%, P - 1.4%
  • Nervousness - 3.1%, P - 0.5%
  • Restlessness - 3.1%, P - 0%
  • Palpitations - 3.1%, P - 0.9%
Drug interactions
  • MAO inhibitors - DO NOT COMBINE. Do not use within 14 days of taking an MAO inhibitor.
  • Alpha blockers - stimulants may counteract the effects of alpha blockers
  • Beta blockers - stimulants may counteract the effects of beta blockers
  • Blood pressure medications - stimulants may raise blood pressure and counteract the effects of blood pressure medications
  • Warfarin - methylphenidate may inhibit warfarin metabolism and increase exposure. Monitor INR closely with concomitant use.
  • Phenobarbital - methylphenidate may inhibit phenobarbital metabolism and increase exposure. Monitor levels closely with concomitant use.
  • Phenytoin - methylphenidate may inhibit phenytoin metabolism and increase exposure. Monitor levels closely with concomitant use.
  • Tricyclic antidepressants (TCAs) - methylphenidate may inhibit the metabolism of tricyclic antidepressants and increase exposure. Use caution with concomitant use.
  • SSRI antidepressants - methylphenidate may inhibit the metabolism of SSRI antidepressants and increase exposure. Use caution with concomitant use.
  • Meperidine - stimulants may potentiate the effects of meperidine
  • Antipsychotics - antipsychotics may reduce the effects of stimulants
  • Lithium - lithium may block the effects of stimulants
  • Halogenated anesthetics - sudden blood pressure increases may occur during surgery

Lab interactions
  • Corticosteroid levels - methylphenidate may cause elevations in corticosteroid levels
  • Drug abuse and dependence - stimulants have the potential for drug abuse and dependence. Use caution in susceptible patients.
  • Heart disease - stimulants may exacerbate and worsen heart disease. Avoid or use caution in susceptible patients.
  • Heart arrhythmias - stimulants may exacerbate heart arrhythmias. Avoid use in susceptible patients.
  • Suppression of growth - stimulant medications can suppress growth rates in children. The effect appears to be directly related to dose and length of therapy. In studies, growth rates in children taking stimulants were 1 - 2 cm/year slower than controls. There is no conclusive evidence that stimulants affect adult height achieved. [1,2,3,4,5]
  • Hypertension - stimulants may raise blood pressure and worsen hypertension. Average blood pressure increase seen in trials was ∼ 2 - 4 mmHg. Average heart rate increase was 3 - 6 bpm.
  • Seizures - stimulants may lower the seizure threshold
  • Hyperthyroidism - stimulants may exacerbate symptoms of hyperthyroidism
  • Glaucoma - stimulants may worsen glaucoma
  • Psychosis - stimulants may worsen psychosis
  • Bipolar mania - stimulants may precipitate bipolar mania
  • Raynaud's phenomenon - stimulants may exacerbate Raynaud's phenomenon
  • Priapism - erections lasting more than 4 hours (priapism) have been reported with methylphenidate products
  • Tourette's syndrome and tics - stimulants may worsen motor tics and tics associated with Tourette's syndrome
  • Visual changes - difficulties with accommodation and blurring of vision have been reported with stimulant medications
  • Liver disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.
  • Kidney disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.

Drug Dosage form Dosage Generic/Price Other/
Pharmacokinetics
Mechanism of Action/
FDA-approved indications
Side Effects
P = % of patients on placebo
who experienced side effect
Drug/Lab Interactions Precautions/
Contraindications
Methylphenidate hydrochloride

(Quillivant XR®)
(Quillichew ER™)
Suspension
Quillivant XR®
  • 5 mg/ml
  • Comes in bottles of 60, 120, 150, and 180 ml

Extended-release chewable tablet
Quillichew ER™
  • 20 mg scored
  • 30 mg scored
  • 40 mg unscored
ADHD
Quillivant XR®
  • Children ≥ 6 years
    • Starting: 20 mg once daily
    • Maximum: 60 mg once daily
    • Increase dose in increments of 10 - 20 mg at weekly intervals

Quillichew ER™
  • Children ≥ 6 years
    • Starting: 20 mg once daily
    • Maximum: 60 mg once daily
    • Increase dose in increments of 10 - 20 mg at weekly intervals
Quillivant XR®
NO/$$$$ (120 ml)

Quillichew ER™
NO/$$$$
Other
Quillivant XR
  • May take without regard to food
  • Shake bottle vigorously for at least 10 seconds before taking
  • Must be reconstituted before dispensing
  • Reconstituted suspension is good for 4 months
  • Store at room temperature

Quillichew ER
  • May take without regard to food
  • Tablet should be chewed
  • 20 and 30 mg tablets are scored and may be cut in half
  • Do not substitute Quillichew for other methylphenidate products on a mg-to-mg basis

Pharmacokinetics
Quillivant XR
  • Time to max level: 2 - 4 hours
  • Half-life: ∼ 5 hours

Quillichew ER
  • Time to max level: ∼ 5 hours
  • Half-life: ∼ 5.2 hours
Mechanism of action
  • Methylphenidate is a CNS stimulant
  • Stimulants are thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space
  • The mode of therapeutic action in ADHD is not known

FDA-approved indications

Quillivant XR, Quillichew ER
  • ADHD - in children ≥ 6 years old
NOTE: Data below is from trials involving Quillivant XR

Children (≥ 6 years old)
  • Affect lability - 9%, P - 2%
  • Excoriation - 4%, P - 0%
  • Insomnia - 2%, P - 0%
  • Tic - 2%, P - 0%
  • Decreased appetite - 2%, P - 0%
  • Vomiting - 2%, P - 0%
  • Motion sickness - 2%, P - 0%
  • Eye pain - 2%, P - 0%
  • Rash - 2%, P - 0%
Drug interactions
  • MAO inhibitors - DO NOT COMBINE. Do not use within 14 days of taking an MAO inhibitor.
  • Alpha blockers - stimulants may counteract the effects of alpha blockers
  • Beta blockers - stimulants may counteract the effects of beta blockers
  • Blood pressure medications - stimulants may raise blood pressure and counteract the effects of blood pressure medications
  • Warfarin - methylphenidate may inhibit warfarin metabolism and increase exposure. Monitor INR closely with concomitant use.
  • Phenobarbital - methylphenidate may inhibit phenobarbital metabolism and increase exposure. Monitor levels closely with concomitant use.
  • Phenytoin - methylphenidate may inhibit phenytoin metabolism and increase exposure. Monitor levels closely with concomitant use.
  • Tricyclic antidepressants (TCAs) - methylphenidate may inhibit the metabolism of tricyclic antidepressants and increase exposure. Use caution with concomitant use.
  • SSRI antidepressants - methylphenidate may inhibit the metabolism of SSRI antidepressants and increase exposure. Use caution with concomitant use.
  • Meperidine - stimulants may potentiate the effects of meperidine
  • Antipsychotics - antipsychotics may reduce the effects of stimulants
  • Lithium - lithium may block the effects of stimulants
  • Halogenated anesthetics - sudden blood pressure increases may occur during surgery

Lab interactions
  • Corticosteroid levels - methylphenidate may cause elevations in corticosteroid levels
  • Drug abuse and dependence - stimulants have the potential for drug abuse and dependence. Use caution in susceptible patients.
  • Heart disease - stimulants may exacerbate and worsen heart disease. Avoid or use caution in susceptible patients.
  • Heart arrhythmias - stimulants may exacerbate heart arrhythmias. Avoid use in susceptible patients.
  • Suppression of growth - stimulant medications can suppress growth rates in children. The effect appears to be directly related to dose and length of therapy. In studies, growth rates in children taking stimulants were 1 - 2 cm/year slower than controls. There is no conclusive evidence that stimulants affect adult height achieved. [1,2,3,4,5]
  • Hypertension - stimulants may raise blood pressure and worsen hypertension. Average blood pressure increase seen in trials was ∼ 2 - 4 mmHg. Average heart rate increase was 3 - 6 bpm.
  • Seizures - stimulants may lower the seizure threshold
  • Hyperthyroidism - stimulants may exacerbate symptoms of hyperthyroidism
  • Glaucoma - stimulants may worsen glaucoma
  • Psychosis - stimulants may worsen psychosis
  • Bipolar mania - stimulants may precipitate bipolar mania
  • Raynaud's phenomenon - stimulants may exacerbate Raynaud's phenomenon
  • Phenylketonuria (PKU) (Quillichew only) - Quillichew tablets contain phenylalanine (20, 30, 40 mg tablets contain 3, 4.5, and 6 mg respectively). Use caution in patients with PKU.
  • Priapism - erections lasting more than 4 hours (priapism) have been reported with methylphenidate products
  • Tourette's syndrome and tics - stimulants may worsen motor tics and tics associated with Tourette's syndrome
  • Visual changes - difficulties with accommodation and blurring of vision have been reported with stimulant medications
  • Liver disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.
  • Kidney disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.

Drug Dosage form Dosage Generic/Price Other/
Pharmacokinetics
Mechanism of Action/
FDA-approved indications
Side Effects
P = % of patients on placebo
who experienced side effect
Drug/Lab Interactions Precautions/
Contraindications
Methylphenidate hydrochloride

(Ritalin®)
(Ritalin LA®)
(Ritalin-SR®)
Ritalin® tablet
  • 5 mg
  • 10 mg
  • 20 mg

Ritalin LA®
Extended-release capsule
  • 10 mg
  • 20 mg
  • 30 mg
  • 40 mg
  • 60 mg

Ritalin-SR®
Extended-release tablet
  • 20 mg
Ritalin®
ADHD
  • Children ≥ 6 years
    • Starting: 5 mg given before breakfast and lunch
    • Maximum: 60 mg a day
    • Increase daily dose in increments of 5 - 10 mg at weekly intervals

  • Adults
    • Typical dose is 10 mg given 2 to 3 times a day
    • Maximum: 60 mg a day
    • Doses should be given 30 - 45 minutes before a meal
    • Take last dose before 6 pm to prevent insomnia

Ritalin LA®
ADHD
  • Children ≥ 6 years
    • Starting: 20 mg once daily
    • Maximum: 60 mg once daily
    • Increase dose in increments of 10 mg at weekly intervals
    • When switching from methylphenidate immediate-release products, total daily dose of methylphenidate may be given as once daily Ritalin LA dose

Ritalin-SR®
ADHD
  • Ritalin-SR tablets have a duration of action of 8 hours
  • They may be used to replace immediate-release methylphenidate tablets where appropriate
Ritalin®
YES/$-$$ (#60)

Ritalin LA®
YES
(20,30,40mg only)
$$-$$$ (#30)

Ritalin-SR®
YES/$-$$ (#30)
Other
Ritalin®
  • May take without regard to food
  • 10 and 20 mg tablets are scored so that they can be halved

Ritalin LA®
  • May take without regard to food
  • Capsules may be opened and sprinkled on applesauce. Swallow applesauce whole, do not chew.
  • Contains immediate-release beads and delayed-release beads

Ritalin-SR®
  • May take without regard to food
  • Do not cut, crush, or chew tablet

Pharmacokinetics
 Ritalin®
  • Time to max level: 1 - 2 hours
  • Half-life: 2 - 4 hours

Ritalin-SR®
  • Time to max level: 4.7 hours
  • Duration of action: 8 hours

Ritalin LA®
  • Contains immediate-release beads and delayed-release beads
  • Time to max level: bimodal
    • 2 hours
    • 5 - 7 hours
  • Half-life: 2 - 4 hours
Mechanism of action
  • Methylphenidate is a CNS stimulant
  • Stimulants are thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space
  • The mode of therapeutic action in ADHD is not known

FDA-approved indications

Ritalin and Ritalin-SR
  • ADHD
  • Narcolepsy

Ritalin LA
  • ADHD
NOTE: Incidence of side effects with Ritalin are not well-defined. Information from the Concerta PI is listed below. Side effects of Ritalin would be expected to be the similar, but may not be exactly the same.

Children (≥ 6 years old)
  • Upper abdominal pain - 6.2%, P - 3.8%
  • Vomiting - 2.8%, P - 1.6%
  • Nasopharyngitis - 2.8%, P - 2.2%
  • Insomnia - 2.8%, P - 0.3%
  • Fever - 2.2%, P - 0.9%

Adults
  • Headache - 22.2%, P - 15.6%
  • Dry mouth - 14%, P - 3.8%
  • Nausea - 12.8%, P - 3.3%
  • Insomnia - 12.3%, P - 6.1%
  • Dizziness - 6.7%, P - 5.2%
  • Weight loss - 6.5%, P - 3.3%
  • Irritability - 5.8%, P - 1.4%
  • Excessive sweating - 5.1%, P - 0.9%
  • Rapid heart rate - 4.8%, P - 0%
  • Depressed mood - 3.9%, P - 1.4%
  • Nervousness - 3.1%, P - 0.5%
  • Restlessness - 3.1%, P - 0%
  • Palpitations - 3.1%, P - 0.9%
Drug interactions
  • MAO inhibitors - DO NOT COMBINE. Do not use within 14 days of taking an MAO inhibitor.
  • Alpha blockers - stimulants may counteract the effects of alpha blockers
  • Beta blockers - stimulants may counteract the effects of beta blockers
  • Acid-suppressing drugs (antacids, PPIs, H2 antagonists, etc) - may alter the absorption of Ritalin LA
  • Blood pressure medications - stimulants may raise blood pressure and counteract the effects of blood pressure medications
  • Warfarin - methylphenidate may inhibit warfarin metabolism and increase exposure. Monitor INR closely with concomitant use.
  • Phenobarbital - methylphenidate may inhibit phenobarbital metabolism and increase exposure. Monitor levels closely with concomitant use.
  • Phenytoin - methylphenidate may inhibit phenytoin metabolism and increase exposure. Monitor levels closely with concomitant use.
  • Tricyclic antidepressants (TCAs) - methylphenidate may inhibit the metabolism of tricyclic antidepressants and increase exposure. Use caution with concomitant use.
  • SSRI antidepressants - methylphenidate may inhibit the metabolism of SSRI antidepressants and increase exposure. Use caution with concomitant use.
  • Meperidine - stimulants may potentiate the effects of meperidine
  • Antipsychotics - antipsychotics may reduce the effects of stimulants
  • Lithium - lithium may block the effects of stimulants
  • Halogenated anesthetics - sudden blood pressure increases may occur during surgery

Lab interactions
  • Corticosteroid levels - methylphenidate may cause elevations in corticosteroid levels
  • Drug abuse and dependence - stimulants have the potential for drug abuse and dependence. Use caution in susceptible patients.
  • Heart disease - stimulants may exacerbate and worsen heart disease. Avoid or use caution in susceptible patients.
  • Heart arrhythmias - stimulants may exacerbate heart arrhythmias. Avoid use in susceptible patients.
  • Suppression of growth - stimulant medications can suppress growth rates in children. The effect appears to be directly related to dose and length of therapy. In studies, growth rates in children taking stimulants were 1 - 2 cm/year slower than controls. There is no conclusive evidence that stimulants affect adult height achieved. [1,2,3,4,5]
  • Hypertension - stimulants may raise blood pressure and worsen hypertension. Average blood pressure increase seen in trials was ∼ 2 - 4 mmHg. Average heart rate increase was 3 - 6 bpm.
  • Seizures - stimulants may lower the seizure threshold
  • Hyperthyroidism - stimulants may exacerbate symptoms of hyperthyroidism
  • Glaucoma - stimulants may worsen glaucoma
  • Psychosis - stimulants may worsen psychosis
  • Bipolar mania - stimulants may precipitate bipolar mania
  • Raynaud's phenomenon - stimulants may exacerbate Raynaud's phenomenon
  • Priapism - erections lasting more than 4 hours (priapism) have been reported with methylphenidate products
  • Tourette's syndrome and tics - stimulants may worsen motor tics and tics associated with Tourette's syndrome
  • Visual changes - difficulties with accommodation and blurring of vision have been reported with stimulant medications
  • Liver disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.
  • Kidney disease - clearance is decreased. Use caution. Manufacturer makes no dosage recommendation.



Drug Dosage form Dosage Generic/Price Other/
Pharmacokinetics
Mechanism of Action/
FDA-approved indications
Side Effects
P = % of patients on placebo
who experienced side effect
Drug/Lab Interactions Precautions/
Contraindications
Atomoxetine
hydrochloride

(Strattera®)
Strattera® capsule
  • 10 mg
  • 18 mg
  • 25 mg
  • 40 mg
  • 60 mg
  • 80 mg
  • 100 mg
Strattera®
ADHD
  • Children and adolescents ≤ 70 kg (154 lbs)
    • Starting: 0.5 mg/kg/day for a minimum of 3 days
    • Maintenance: 1.2 mg/kg/day
    • Maximum: 1.4 mg/kg/day (do not exceed 100 mg)
    • Total daily dose may be given once daily in the morning or divided and given in the morning and late afternoon/evening
    • No additional benefit has been demonstrated with doses > 1.2 mg/kg/day

  • Adults and adolescents > 70 kg (154 lbs)
    • Starting: 40 mg a day for a minimum of 3 days
    • Maintenance: 80 mg a day
    • Maximum: 100 mg a day
    • Total daily dose may be given once daily in the morning or divided and given in the morning and late afternoon/evening

When taken with CYP2D6 strong inhibitors or in CYP2D6 poor metabolizers
  • Children and adolescents ≤ 70 kg (154 lbs)
    • Dosing: 0.5 mg/kg/day
    • Dose may be increased to 1.2 mg/kg/day if symptoms fail to improve after 4 weeks and the initial dose is well tolerated

  • Adults and adolescents > 70 kg (154 lbs)
    • Dosing: 40 mg a day
    • Dose may be increased to 80 mg a day if symptoms fail to improve after 4 weeks and the initial dose is well tolerated
Strattera®
NO/$$$$
Other
  • May take without regard to food
  • Swallow capsules whole. Do not open.
  • Strattera may be stopped without tapering


Pharmacokinetics
  • Half-life: 5 hours
  • Time to max level: 1 - 2 hours
Mechanism of action
  • Exact mechanism is unknown, but is thought to be related to selective inhibition of the presynaptic norepinephrine transporter

FDA-approved indications
  • ADHD
NOTE: Only side effects that occurred at an incidence ≥ 3% and ≥ 3% more than placebo are listed

Children and adolescents
  • Headache - 19%, P - 15%
  • Abdominal pain - 18%, P - 10%
  • Decreased appetite - 16%, P - 4%
  • Somnolence - 11%, P - 4%
  • Vomiting - 11%, P - 6%
  • Nausea - 10%, P - 5%
  • Fatigue - 8%, P - 3%
  • Irritability - 6%, P - 3%
  • Dizziness - 5%, P - 2%
  • Weight loss - 3%, P - 0%
  • Increase in heart rate (average bpm)
    • Extensive CYP2D6 metabolizers: 5 bpm
    • Poor CYP2D6 metabolizers: 9.4 bpm
  • Increase in blood pressure (≥ 15 - 20 mmHg) - 5 - 10% of patients in trials

Adults
  • Nausea - 26%, P - 6%
  • Dry mouth - 20%, P - 5%
  • Decreased appetite - 16%, P - 3%
  • Insomnia - 15%, P - 8%
  • Fatigue - 10%, P - 6%
  • Erectile dysfunction - 8%, P - 1%
  • Dizziness - 8%, P - 3%
  • Constipation - 8%, P - 3%
  • Somnolence - 8%, P - 5%
  • Abdominal pain - 7%, P - 4%
  • Urinary hesitancy - 6%, P - 1%
  • Ejaculation delay/disorder - 4%, P - 1%
  • Excessive sweating - 4%, P - 1%
  • Hot flash - 3%, P - 0%
  • Chills - 3%, P - 0%
  • Paresthesia - 3%, P - 0%
  • Increase in heart rate (average bpm)
    • Extensive CYP2D6 metabolizers: 7.5 bpm
    • Poor CYP2D6 metabolizers: 11 bpm
  • Increase in blood pressure (average mmHg)
    • Extensive CYP2D6 metabolizers: DBP 2.13, SBP 2.4
    • Poor CYP2D6 metabolizers: DBP 4.21, SBP 2.75
Drug interactions
  • MAO inhibitors - DO NOT COMBINE. Do not use within 14 days of taking an MAO inhibitor.
  • CYP2D6 strong inhibitors - atomoxetine is a CYP2D6 sensitive substrate. See Dosage for information on dosing with concomitant CYP2D6 strong inhibitors.
  • Blood pressure medications - atomoxetine may raise blood pressure and counteract the effects of blood pressure medications
  • Vasopressors (e.g. dopamine, dobutamine) - atomoxetine may raise blood pressure and potentiate the effects of pressor agents
  • Albuterol (oral and IV) - atomoxetine may potentiate the cardiac effects of systemically-administered albuterol (oral and IV) resulting in increased heart rate and blood pressure. These effects have not been seen with inhaled albuterol.
  • Narrow angle glaucoma - DO NOT USE. Atomoxetine may cause pupillary dilation.
  • Pheochromocytoma - DO NOT USE. Atomoxetine may potentiate elevated blood pressure and tachyarrhythmia.
  • Cardiovascular disease - atomoxetine may raise blood pressure and heart rate. Use with caution in susceptible patients.
  • Suicidal ideation - in children and adolescents, atomoxetine may increase the risk of suicidal ideation. In trials, 0.4% of children reported suicidal ideation while taking atomoxetine.
  • Liver toxicity - there have been rare cases of liver injury in patients taking atomoxetine. Atomoxetine should be discontinued in patients with jaundice or laboratory evidence of liver injury. Liver function testing should be performed in patients with symptoms of liver disease (e.g. pruritus, dark urine, jaundice, right upper quadrant tenderness, or unexplained “flu like” symptoms)
  • Suppression of growth - atomoxetine may suppress growth, particularly in prepubertal children. In trials lasting 3 years, pre-pubertal children (girls ≤ 8 years old, boys ≤ 9 years old) started on atomoxetine gained an average weight of 2.1 kg less than predicted and obtained an average height of 1.2 cm less than predicted. Children who were older were not affected. It's unknown if atomoxetine affects adult height achieved.
  • Structural heart disease - sudden death has been reported in patients taking atomoxetine with structural heart disease. Avoid or use caution in susceptible patients.
  • Heart arrhythmias - atomoxetine may exacerbate heart arrhythmias. Avoid use in susceptible patients.
  • Psychosis - atomoxetine may worsen psychosis
  • Bipolar mania - atomoxetine may precipitate bipolar mania
  • Priapism - erections lasting more than 4 hours (priapism) have been reported in patients taking atomoxetine
  • Kidney disease - no dose adjustment necessary
  • Liver disease
    • Moderate (Child-Pugh Class B) - initial and target dose should be reduced to 50% of normal dose
    • Severe (Child-Pugh Class C) - initial and target dose should be reduced to 25% of normal dose

Drug Dosage form Dosage Generic/Price Other/
Pharmacokinetics
Mechanism of Action/
FDA-approved indications
Side Effects
P = % of patients on placebo
who experienced side effect
Drug/Lab Interactions Precautions/
Contraindications
Clonidine

(Kapvay®)
Kapvay®
Extended-release tablet
  • 0.1 mg
  • 0.2 mg
Kapvay®
ADHD
  • Children ≥ 6 years old
    • Starting: 0.1 mg at bedtime
    • Maintenance: 0.1 - 0.4 mg a day
    • Maximum: 0.4 mg a day
    • Increase dose in increments of 0.1 mg/day at weekly intervals
    • If a dose is missed, that dose should be skipped and the next dose should be taken as scheduled
    • When discontinuing, dose should be tapered by 0.1 mg/day every 3 - 7 days to avoid rebound hypertension

Dosing guidance
Total daily dose Morning dose bedtime dose
0.1 mg/day 0.1 mg
0.2 mg/day 0.1 mg 0.1 mg
0.3 mg/day 0.1 mg 0.2 mg
0.4 mg/day 0.2 mg 0.2 mg
Kapvay®
YES/$$$$
Other
  • May take without regard to food
  • Swallow tablet whole. Do not crush, cut, or chew.


Pharmacokinetics
  • Half-life: 12.6 hours
  • Time to max level: 6.5 hours
Mechanism of action
  • The sympathetic nervous system is the main "excitatory" nervous system in the body (opposite of parasympathetic system)
  • Increased sympathetic activity leads to increased awareness, stress, and adrenaline
  • Clonidine stimulates alpha-2 adrenergic receptors in the brain
  • Alpha-2 stimulation leads to decreased sympathetic nervous system activity
  • The mechanism of clonidine in ADHD is not completely understood

FDA-approved indications
  • ADHD - as monotherapy and as adjunctive therapy to stimulant medications
NOTE: Only side effects that occurred at an incidence ≥ 3% and ≥ 3% more than placebo are listed. Side effects listed are for 0.4 mg/day dose.

Children and adolescents
  • Somnolence - 31%, P - 4%
  • Fatigue - 13%, P - 1%
  • Nightmare - 9%, P - 0%
  • Insomnia - 6%, P - 1%
  • Constipation - 6%, P - 0%
  • Dry mouth - 5%, P - 1%
  • Slow heart rate* - 4%, P - 0%
  • Emotional disorder - 4%, P - 1%
  • Bedwetting - 4%, P - 0%
  • Tremor - 4%, P - 0%
  • Increased heart rate - 3%, P - 0%
  • Tearfulness - 3%, P - 0%
  • Decreased blood pressure and heart rate - clonidine lowers blood pressure and slows heart rate. In trials, the following effects were seen:

  • Values are placebo-subtracted mean change
SBP
(mmHg)
DBP
(mmHg)
Heart rate
(bpm)
0.2 mg/day -4 -4 -4
0.4 mg/day -8.8 -7.3 -7.7
Drug interactions
  • Tricyclic antidepressants - tricyclic antidepressants may counteract clonidine's hypotensive effects
  • Blood pressure medications - clonidine may potentiate the effects of blood pressure medications
  • CNS depressants (ex. alcohol, anticonvulsants, antihistamines, etc.) - clonidine may potentiate the effects of CNS depressants. Use caution.
  • Drugs that slow the heart rate - clonidine may potentiate the decrease in heart rate seen with some medications (ex. beta blockers, calcium channel blockers)
  • Tizanidine (Zanaflex®) - tizanidine is an alpha-2 agonist. It should not be taken with clonidine.
  • Rebound hypertension - rebound hypertension may occur with abrupt discontinuation. When discontinuing, reduce dose by no more than 0.1 mg every 3 - 7 days.
  • Decreased blood pressure and heart rate - clonidine may decrease blood pressure and heart rate (see Side effects). Monitor heart rate and blood pressure during usage.
  • Sinus node dysfunction and heart block - clonidine may worsen sinus node dysfunction and heart block. Use caution in susceptible patients.
  • Sedation and somnolence - clonidine causes somnolence and sedation in up to 38% of patients. Caution should be used before operating motor vehicles and other dangerous equipment.
  • Kidney disease - clearance is decreased. Use caution. Manufacturer makes no specific dosage recommendation.
  • Liver disease - clearance is decreased. Use caution. Manufacturer makes no specific dosage recommendation.

Drug Dosage form Dosage Generic/Price Other/
Pharmacokinetics
Mechanism of Action/
FDA-approved indications
Side Effects
P = % of patients on placebo
who experienced side effect
Drug/Lab Interactions Precautions/
Contraindications
Guanfacine

(Intuniv®)
Guanfacine®
Extended-release tablet
  • 1 mg
  • 2 mg
  • 3 mg
  • 4 mg
Intuniv®
ADHD
  • Children ≥ 6 years old
    • Starting: 1 mg once daily
    • Maintenance: 1 - 7 mg once daily (0.05 - 0.12 mg/kg/day)
    • Maximum: 7 mg once daily
    • Doses may be taken in the morning or evening
    • Doses > 4 mg/day have not been evaluated in children (6 - 12 years), and doses > 7 mg/day have not been evaluated in adolescents (13 - 17 years)
    • Increase dose in increments of 1 mg/day at weekly intervals
    • If 2 or more doses are missed, consider retitrating
    • When discontinuing, dose should be tapered by no more than 1 mg/day every 3 - 7 days to avoid rebound hypertension

Target dose ranges
Weight (kg) Target dosage range
25 - 33.9 2 - 3 mg/day
34 - 41.4 2 - 4 mg/day
41.5 - 49.4 3 - 5 mg/day
49.5 - 58.4 3 - 6 mg/day
58.5 - 91 4 - 7 mg/day
> 91 5 - 7 mg/day

When taken with a CYP3A4 modulator
Intuniv®
YES/$
Other
  • Do not take with high fat meals because absorption and exposure are increased
  • Swallow tablet whole. Do not crush, cut, or chew.
  • Intuniv should not be substituted for immediate-release guanfacine on a mg-per-mg basis because of differing pharmacokinetics

Pharmacokinetics
  • Half-life: 18 hours*
  • Time to max level: 6 hours*
  • *Data from study in adults
Mechanism of action
  • The sympathetic nervous system is the main "excitatory" nervous system in the body (opposite of parasympathetic system)
  • Increased sympathetic activity leads to increased awareness, stress, and adrenaline
  • Guanfacine stimulates alpha-2A adrenergic receptors in the brain
  • Alpha-2A stimulation leads to decreased sympathetic nervous system activity
  • The mechanism of guanfacine in ADHD is not completely understood

FDA-approved indications
  • ADHD - as monotherapy and as adjunctive therapy to stimulant medications
NOTE: Only side effects that occurred at an incidence ≥ 4% and at a rate approximately twice that of placebo are listed. Side effects listed are for 4 mg/day dose.

Children and adolescents
  • Somnolence - 51%, P - 11%
  • Headache - 28%, P - 19%
  • Fatigue - 15%, P - 3%
  • Abdominal pain - 15%, P - 9%
  • Dizziness - 10%, P - 4%
  • Hypotension* - 8%, P - 3%
  • Lethargy - 7%, P - 3%
  • Nausea - 6%, P - 2%
  • Dry mouth - 7%, P - 1%
  • Constipation - 4%, P - 1%
  • Nightmare - 4%, P - 0%
  • Decreased blood pressure and heart rate - Guanfacine lowers blood pressure and slows heart rate. In trials, the following effects were seen:

  • Values are maximum average change from baseline
SBP
(mmHg)
DBP
(mmHg)
Heart rate
(bpm)
1 mg/day -4.3 -3.4 -4.8
2 mg/day -5.5 -3.3 -3.1
3 mg/day -5.4 -4.4 -6.5
4 mg/day -8.2 -5.4 -8.6
Drug interactions
  • CYP3A4 strong inhibitors/inducers - guanfacine is a CYP3A4 sensitive substrate. See Guanfacine dosing with CYP3A4 modulators for dosing recommendations with strong CYP3A4 inhibitors and inducers
  • Blood pressure medications - guanfacine may potentiate the effects of blood pressure medications
  • CNS depressants (ex. alcohol, anticonvulsants, antihistamines, etc.) - guanfacine may potentiate the effects of CNS depressants. Use caution.
  • Drugs that slow the heart rate - guanfacine may potentiate the decrease in heart rate seen with some medications (ex. beta blockers, calcium channel blockers)
  • Tizanidine (Zanaflex®) - tizanidine is an alpha-2 agonist. It should not be taken with guanfacine.
  • Rebound hypertension - rebound hypertension may occur with abrupt discontinuation. When discontinuing, reduce dose by no more than 1 mg every 3 - 7 days.
  • Decreased blood pressure and heart rate - guanfacine may decrease blood pressure and heart rate (see Side effects). Monitor heart rate and blood pressure during usage.
  • Sinus node dysfunction and heart block - guanfacine may worsen sinus node dysfunction and heart block. Use caution in susceptible patients.
  • Sedation and somnolence - guanfacine causes somnolence and sedation. Caution should be used before operating motor vehicles and other dangerous equipment.
  • Kidney disease - clearance is decreased. Use caution. Manufacturer makes no specific dosage recommendation.
  • Liver disease - clearance is decreased. Use caution. Manufacturer makes no specific dosage recommendation.



    GUANFACINE DOSING WITH CYP3A4 MODULATORS


  • See CYP3A4 for a list of inducers and inhibitors
Guanfacine dosing recommendations with CYP3A4 modulators
Starting guanfacine while currently
on a CYP3A4 modulator
Continuing guanfacine while adding
a CYP3A4 modulator
Continuing guanfacine while stopping
a CYP3A4 modulator
Strong
CYP3A4 inhibitor
Half the guanfacine dose Half the guanfacine dose Increase dose to recommended level
Strong
CYP3A4 inducer
Consider doubling the dose Consider doubling the dose
over 1 - 2 weeks
Decrease dose to recommended level
over 1 - 2 weeks



  • DSM-5 CRITERIA FOR ADHD

  • Reference [6]
DSM-5 ADHD DIAGNOSTIC CRITERIA
Inattention - ≥ 6 of the following present in children up to 9 years; ≥ 5 symptoms present in adolescents and adults

  • Often fails to give close attention to details and makes careless mistakes in schoolwork, at work, or during other activities (e.g., overlooks or misses details, work is inaccurate).
  • Often has difficulty sustaining attention in tasks or play activities (e.g., has difficulty remaining focused during lectures or conversations or when reading lengthy writings)
  • Often does not seem to listen when spoken to directly (e.g., mind seems elsewhere, even in the absence of any obvious distraction)
  • Often does not follow through on instructions and fails to finish schoolwork, chores, or duties in the workplace (e.g., starts tasks but quickly loses focus and is easily sidetracked; does not finish schoolwork, household chores, or tasks in the workplace)
  • Often has difficulty organizing tasks and activities (e.g., has difficulty managing sequential tasks and keeping materials and belongings in order; has messy, disorganized work; has poor time management; tends to fail to meet deadlines)
  • Often avoids, dislikes, or is reluctant to engage in tasks that require sustained mental effort (e.g., doing schoolwork or homework; preparing reports, completing forms, or reviewing lengthy papers)
  • Often loses things necessary for tasks or activities (e.g., school materials, pencils, books, tools, wallets, keys, paperwork, eyeglasses, or mobile phones)
  • Is often easily distracted by extraneous stimuli (in older adolescents and adults, may include unrelated thoughts)
  • Is often forgetful in daily activities (e.g., performing chores and running errands, returning telephone calls, paying bills, and keeping appointments)
Hyperactivity and impulsivity - ≥ 6 of the following present in children up to 9 years; ≥ 5 symptoms present in adolescents and adults

  • Often fidgets with or taps hands or feet or squirms in seat
  • Often leaves seat in situations in which one is expected to remain seated (e.g., leaves his or her place in the classroom or office)
  • Often runs about or climbs in situations in which it is inappropriate. (In adolescents or adults, this symptom may be limited to feeling restless.)
  • Often is unable to play or engage in leisure activities quietly
  • Often is “on the go,” acting as if “driven by a motor” (e.g., is unable to be still or feels uncomfortable being still for an extended period of time in restaurants or meetings; other people may perceive him or her as being restless and difficult to keep up with)
  • Often talks excessively
  • Often blurts out an answer before a question has been completed (e.g., completes people’s sentences and “jumps the gun” in conversations, cannot wait for next turn in conversation)
  • Often has difficulty waiting his or her turn (e.g., while waiting in line)
  • Often interrupts or intrudes on others (e.g., butts into conversations, games, or activities or uses other people’s things without asking or receiving permission; adolescents or adults may intrude in or take over what others are doing)
The above symptoms from each category must meet the following criteria:

  • Symptoms must be present for ≥ 6 months to a degree that is inconsistent with the person’s developmental level and that directly affects social and academic or occupational activities
  • Several symptoms of inattention or hyperactivity and impulsivity were present before 12 years of age
  • Symptoms occur in ≥ 2 settings (e.g., at home, school, or work or with friends or relatives)
  • There is clear evidence that the symptoms interfere with or reduce the quality of social, academic, or occupational functioning
  • The symptoms do not occur exclusively during the course of schizophrenia or another psychotic disorder and are not better accounted for by another mental disorder (e.g., a mood disorder, an anxiety disorder, a dissociative disorder, or a personality disorder)



  • PRICING

    • $ = 0 - $50
    • $$ = $51 - $100
    • $$$ = $101 - $150
    • $$$$ = > $151

    • Pricing based on one month of therapy at standard dosing in an adult
    • Pricing based on survey of GoodRX.com®, HEB®, and Costco®, [accessed 7/2015]
    • Pricing may vary by region and availability


  • REFERENCES

  • 1 - Manufacturer's Package Insert for each drug listed
  • 2 - PMID 24571756 NEJM review
  • 3 - PMID 25180281 height study
  • 4 - PMID 20605163 height study
  • 5 - PMID 16040876 - height MA
  • 6 - PMID 24224626 - NEJM Adult ADHD review