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Drug Dosage form Dosage Lab monitoring
NOTE: Lab ranges may vary by lab
Generic/Price Other Mechanism of Action/
FDA-approved indications
Side Effects
Drug Interactions Precautions/
Contraindications
Lithium

(Lithobid®)
Lithium capsule
  • 150 mg
  • 300 mg
  • 600 mg

Lithium tablet
  • 300 mg

Lithium extended-release tablet (Lithobid®)
  • 300 mg
  • 450 mg
Bipolar - Acute mania
Lithium
  • Dosing: 1200 - 1800 mg a day given in three divided doses

Bipolar - Maintenance therapy
Lithium
  • Dosing: 300 mg three to four times a day
  • Adjust dose based on serum levels
  • Once stable, total daily dose may be given once daily in the evening [2]

Extended-release tablet (Lithobid®)
  • Dosing: 900 - 1200 mg a day given in 2 divided doses
  • Adjust dose based on serum levels
  • When switching from lithium immediate-release to extended-release, use the same total daily dose
Monitoring therapy
  • Baseline labs: TSH, Free T4, Free T3, BMP (electrolytes, Ca, Cr, BUN)
  • Check lithium level 1 week after starting therapy, and 1 week after dose changes. Check lithium level at least once every 3 months (may be less frequent in stable patients). Check levels more frequently if taking interacting-drugs or if patient has risk factors for toxicity.
  • Check thyroid function and BMP every 6 - 12 months, depending on the patient and risk factors

Levels
  • Lithium levels should be drawn right before the next dose is due (trough levels)
  • Recommended levels vary slightly depending on the reference
  • Acute mania: 0.8 - 1.4 mmol/L
  • Long-term therapy: 0.6 - 1.0 mmol/L
  • Potentially toxic: > 1.5 mmol/L
  • Reference: LabCorp®, PI, 2

Pharmacokinetics
  • Half-life: 14 - 30 hours
  • Time to steady state: 2 - 7 days [5]
Capsule
YES/$

Tablet
YES/$

Extended-release
YES/$
Other
  • May take without regard to food. Food may decrease stomach upset.
  • Do not crush, cut, or chew extended-release tablets

Signs of lithium toxicity
  • diarrhea
  • vomiting
  • tremor (common side effect)
  • loss of coordination
  • muscle weakness
  • drowsiness

Mechanism of action
  • Mechanism not completely understood
  • Alters sodium transport in nerve and muscle cells and increases intraneuronal metabolism of catecholamines
  • Increases GABA activity
  • Increases serotonin function
  • Blocks dopamine-receptor supersensitivity [2]

FDA-approved indications
  • Acute bipolar mania

  • Maintenance therapy for bipolar disorder
NOTE: Incidence of side effects not well-defined

  • Hand tremor - up to 50% of patients
  • Increased thirst - up to 33% of patients
  • Increased urination - up to 33% of patients
  • Memory and concentration impairment
  • Lethargy
  • Nausea
  • Diarrhea
  • Weight gain
  • Hair loss
  • Lithium is excreted unchanged into the renal tubule, 80% is then reabsorbed in the proximal tubule. Medications that affect renal tubular electrolyte absorption may affect lithium clearance. Nephron diagram
  • Lithium does not undergo liver metabolism
  • Thiazide diuretics - may increase lithium levels
  • Loop diuretics - may increase lithium levels
  • ENAC inhibitors - may increase lithium levels
  • Aldosterone antagonists - may increase lithium levels
  • NSAIDs (ibuprofen, naprosyn, etc.) - may increase lithium levels. In studies, average trough lithium levels increased by 15 - 20% in patients taking NSAIDs.
  • COX-2 inhibitors (celecoxib, Celebrex® etc.) - may increase lithium levels
  • ACE inhibitors - may increase lithium levels
  • ARBs - may increase lithium levels
  • Carbamazepine - may increase risk of neurotoxic effects
  • Topiramate - may increase lithium levels
  • Phenytoin - may increase risk of neurotoxic effects
  • Serotonergic medications - lithium has serotonergic activity. It may potentiate serotonergic effects of other drugs.
  • Acetazolamide - may decrease lithium levels
  • Methyldopa - may increase lithium levels
  • Metronidazole - may increase lithium levels
  • Calcium channel blockers - may increase risk of neurotoxicity
  • Antidepressants that act on serotonin - may increase risk of neurotoxicity
  • Pramlintide - pramlintide may alter lithium absorption
  • GLP-1 analogs (Byetta®, etc.) - GLP-1 analogs may alter lithium absorption
  • Neuromuscular blocking agents - lithium may prolong the action of neuromuscular blockers
  • Theophylline - may decrease lithium levels
  • Kidney disease - DO NOT USE in significant kidney disease
  • Sodium depletion - DO NOT USE
  • Dehydration - DO NOT USE
  • Brugada syndrome - DO NOT USE
  • Significant cardiovascular disease - DO NOT USE
  • Decreased sodium intake - may raise lithium levels
  • Diabetes insipidus - excessive water loss in the kidneys can occur with lithium
  • Hypothyroidism - lithium may cause an elevation of TSH levels (up to 33% of patients). Clinical hypothyroidism is less frequent.
  • Hyperparathyroidism - lithium may increase parathyroid hormone levels
  • High calcium levels - lithium-induced hyperparathyroidism may lead to high calcium levels
  • Decreased kidney function - lithium may cause a decrease in kidney function over time
  • Pregnancy - lithium may increase the risk of birth defects
  • Psoriasis - lithium may worsen psoriasis
  • Serotonin syndrome - lithium has serotonergic activity
  • EKG changes - lithium may cause T-wave flattening or inversion on an EKG
  • Liver disease - no recommendations made. Use caution.




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

(Buspar®)
Buspirone tablet
  • 5 mg
  • 7.5 mg
  • 10 mg
  • 15 mg
  • 30 mg
Anxiety disorders
  • Starting: - 7.5 mg twice a day
  • Maintenance: 10 - 15 mg twice a day
  • Max: 60 mg a day
  • Increase dose by 5 mg per day at intervals of 2 - 3 days

With CYP3A4 strong inhibitors
  • Consider buspirone dose of 2.5 mg once or twice a day. See Drug Interactions.
5 mg, 10 mg, 15 mg
YES/$

7.5 mg, 30 mg
YES/$-$$
Other
  • Food increases absorption. To maintain a consistent effect, take either with or without food on a consistent basis; either always with or always without food.
  • 15 mg tablet is scored to provide 5, 7.5, 10, and 15 mg dose depending on where cut
  • Tablets may be cut in half

Lab interactions
  • May cause false-positive urine catecholamines. Stop for at least 48 hours prior to testing.
Mechanism of action
  • Mechanism not completely understood
  • Binds serotonin (5-HT1A) receptors
  • Binds D2-dopamine receptors

FDA-approved indication
  • Anxiety disorders
  • Dizziness - 12%, P - 3%
  • Drowsiness- 10%, P - 9%
  • Nausea- 8%, P - 5%
  • Headache- 6%, P - 3%
  • Nervousness- 5%, P - 1%
  • MAO inhibitors - DO NOT COMBINE
  • CYP3A4 inducers and inhibitors - Buspirone is a CYP3A4 sensitive substrate. CYP3A4 inhibitors and inducers may affect buspirone levels. Buspirone dose adjustments may be necessary when taken with these medications. See Dosing for more.
  • Diltiazem - may increase buspirone levels
  • Verapamil - may increase buspirone levels
  • Erythromycin - may increase buspirone levels. Buspirone dose of 2.5 mg twice a day recommended.
  • Grapefruit juice - may increase buspirone levels. Do not drink large amounts when taking buspirone.
  • Itraconazole - may increase buspirone levels. Buspirone dose of 2.5 mg once a day recommended.
  • Nefazodone - may increase buspirone levels. buspirone may increase nefazodone levels. Buspirone dose of 2.5 mg once a day recommended.
  • Rifampin - may decrease buspirone levels
  • Cimetidine - may increase buspirone levels
  • Diazepam - buspirone may increase diazepam levels
  • Serotonergic medications - buspirone has serotonergic activity. It may potentiate serotonergic effects of other drugs.
  • Haloperidol - buspirone may increase haloperidol levels
  • Serotonin syndrome - buspirone has serotonergic activity
  • Liver disease - severe disease - DO NOT USE; other - use caution
  • Kidney disease - severe disease - DO NOT USE; other - use caution



  • 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 2/2015]
    • Pricing may vary by region and availability



  • References:
  • 1 - Manufacturer's Package Insert for each drug listed
  • 2 - PMID 8047085
  • 3 - PMID 22265699
  • 4 - ISBN-10: 1-85433-441-7, Management of bipolar in adults. NICE Clinical Guidelines
  • 5 - Qwest® diagnostics CLICK HERE