Estrogen pills
Estrogen patches
Other estrogen products
Progestins
Combination products
Hormone injections
Other related pages
OTHER STUDIES




Drug Dosage forms Dosing Other/Price
Cenestin®

(conjugated estrogens)
Tablet
  • 0.30 mg
  • 0.45 mg
  • 0.625 mg
  • 0.90 mg
  • 1.25 mg
Menopausal vasomotor symptoms
  • Starting: 0.45 mg once daily
  • Titrate to desired effect. Use lowest effective dose.

Menopausal vulvar and vaginal atrophy
  • Dosing: 0.30 mg once daily
  • Titrate to desired effect. Use lowest effective dose.
Other
Price
  • No generic
  • 30 tablets - $$$
Enjuvia®

(conjugated estrogens)
Tablet
  • 0.30 mg
  • 0.45 mg
  • 0.625 mg
  • 0.90 mg
  • 1.25 mg
Menopausal vasomotor symptoms
  • Starting: 0.30 mg once daily
  • Titrate to desired effect. Use lowest effective dose.

Menopausal vulvar and vaginal atrophy
  • Dosing: 0.30 mg once daily
  • Titrate to desired effect. Use lowest effective dose.
Other
Price
  • No generic
  • 30 tablets - $$
Premarin®

(conjugated estrogens)
Tablet
  • 0.30 mg
  • 0.45 mg
  • 0.625 mg
  • 0.90 mg
  • 1.25 mg
Menopausal vasomotor symptoms
  • Starting: 0.30 mg once daily
  • Titrate to desired effect. Use lowest effective dose.
  • May be given continuously or in cyclical regimens (25 days on drug followed by 5 days off)

Menopausal vulvar and vaginal atrophy
  • Dosing: 0.30 mg once daily
  • Titrate to desired effect. Use lowest effective dose.
  • May be given continuously or in cyclical regimens (25 days on drug followed by 5 days off)

Prevention of postmenopausal osteoporosis
  • Dosing: 0.30 mg once daily
  • May be given continuously or in cyclical regimens (25 days on drug followed by 5 days off)

Hypogonadism
  • Dosing: 0.30 - 0.625 mg once daily given cyclically (3 weeks on followed by one week off)
  • Titrate to desired effect. Use lowest effective dose.

Female castration or primary ovarian failure
  • Dosing: 1.25 mg once daily given cyclically (3 weeks on followed by one week off)
  • Titrate to desired effect. Use lowest effective dose.

Palliative metastatic breast cancer treatment
  • Dosing: 10 mg three times a day for at least 3 months

Palliative advanced prostate cancer treatment
  • Dosing: 1.25 - 2.5 mg three times a day
Other
Price
  • No generic
  • 30 tablets - $$$

Drug Dosage forms Dosing Other/Price
Estrace®

(estradiol)
Tablet
  • 0.50 mg
  • 1.0 mg
  • 2.0 mg
Menopausal vasomotor symptoms
  • Dosing: 1 - 2 mg once daily given cyclically (3 weeks on followed by one week off)
  • Titrate to desired effect. Use lowest effective dose.
  • Reevaluate need for therapy periodically

Menopausal vulvar and vaginal atrophy
  • Dosing: 1 - 2 mg once daily given cyclically (3 weeks on followed by one week off)
  • Titrate to desired effect. Use lowest effective dose.
  • Reevaluate need for therapy periodically

Prevention of postmenopausal osteoporosis
  • Dosing: 0.50 - 2 mg once daily
  • Lowest effective dose has not been determined

Hypoestrogenism due to hypogonadism, castration, or primary ovarian failure
  • Dosing: 1 - 2 mg once daily
  • Titrate to desired effect. Use lowest effective dose.

Palliative metastatic breast cancer treatment
  • Dosing: 10 mg three times a day for at least 3 months

Palliative advanced prostate cancer treatment
  • Dosing: 1 - 2 mg three times a day
Other
Price
  • Generic available
  • 30 tablets - $

Drug Dosage forms Dosing Other/Price
Ogen®

(estropipate)
Tablet
  • 0.75 mg
  • 1.5 mg
  • 3.0 mg
Menopausal vasomotor symptoms
  • Dosing: 0.75 - 6 mg once daily given cyclically (three weeks on followed by one week off)
  • Titrate to desired effect. Use lowest effective dose.
  • Reevaluate need for therapy periodically
  • If patient is still menstruating, start on Day 5 of bleeding

Menopausal vulvar and vaginal atrophy
  • Dosing: 0.75 - 6 mg once daily given cyclically (three weeks on followed by one week off)
  • Titrate to desired effect. Use lowest effective dose.
  • Reevaluate need for therapy periodically

Prevention of postmenopausal osteoporosis
  • Dosing: 0.75 mg once daily for 25 days of a 31-day cycle each month

Hypogonadism
  • Dosing: 1.5 - 9 mg once daily given for the first 3 weeks of a cycle followed by 8 - 10 days off
  • Titrate to desired effect. Use lowest effective dose.

Female castration or primary ovarian failure
  • Dosing: 1.5 - 9 mg once daily given for the first 3 weeks of a cycle followed by 8 - 10 days off
  • Titrate to desired effect. Use lowest effective dose.
Other
Price
  • Generic available
  • 30 tablets - $

Drug Dosage forms Dosing Other/Price
Menest®

(esterified estrogens)
Tablet
  • 0.30 mg
  • 0.625 mg
  • 1.25 mg
  • 2.5 mg
Menopausal vasomotor symptoms
  • Dosing: 1.25 mg once daily given cyclically (three weeks on followed by one week off)
  • Titrate to desired effect. Use lowest effective dose.
  • Reevaluate need for therapy periodically
  • If patient is still menstruating, start on Day 5 of bleeding

Menopausal vulvar and vaginal atrophy
  • Dosing: 0.30 - 1.25 mg once daily given cyclically (three weeks on followed by one week off)
  • Titrate to desired effect. Use lowest effective dose.
  • Reevaluate need for therapy periodically

Hypogonadism
  • Dosing: 2.5 - 7.5 mg/day given in divided doses for 20 days followed by 10 days off
  • Titrate to desired effect. Use lowest effective dose.

Female castration or primary ovarian failure
  • Dosing: 1.25 mg once daily given cyclically (three weeks on followed by one week off)
  • Titrate to desired effect. Use lowest effective dose.

Palliative metastatic breast cancer treatment
  • Dosing: 10 mg three times a day for at least 3 months

Palliative advanced prostate cancer treatment
  • Dosing: 1.25 - 2.5 mg three times a day
Other
Price
  • No generic
  • 30 tablets - $$

Drug Dosage forms Dosing Other/Price
Osphena®

(ospemifene)
Tablet
  • 60 mg
Dyspareunia due to menopause
  • Dosing: 60 mg once daily with food
  • Ospemifene is a selective estrogen receptor modulator (SERM). It has an agonistic effect on the endometrium. A progestin should be considered in women with a uterus.
  • Use for shortest duration necessary
  • See SERM activity table
Other
  • Take with food. Food increases absorption.
  • See ospemifene below for contraindications, precautions, side effects, and drug interactions

Price
  • No generic
  • 30 tablets - $$$$




Drug Dosage forms Dosing Other/Price
Alora®

(estradiol)
Patch
  • 0.025 mg/24 hour
  • 0.050 mg/24 hour
  • 0.075 mg/24 hour
  • 0.10 mg/24 hour
Menopausal vasomotor symptoms
  • Dosing: 0.050 mg/day patch applied twice weekly
  • Titrate to desired effect. Use lowest effective dose.
  • Reevaluate need for therapy periodically
  • In women with an intact uterus, may be given cyclically (3 weeks on followed by 1 week off)

Menopausal vulvar and vaginal atrophy
  • Dosing: 0.050 mg/day patch applied twice weekly
  • Titrate to desired effect. Use lowest effective dose.
  • Reevaluate need for therapy periodically
  • In women with an intact uterus, may be given cyclically (3 weeks on followed by 1 week off)

Hypogonadism, female castration, primary ovarian failure
  • Dosing: 0.050 mg/day patch applied twice weekly
  • Titrate to desired effect. Use lowest effective dose.
  • Reevaluate need for therapy periodically

Prevention of postmenopausal osteoporosis
  • Dosing: 0.025 mg/day patch applied twice weekly
  • 0.025 mg/day is the lowest dose that has been shown to be effective
Other
Price
  • No generic
  • 8 patches - $$
Climara®

(estradiol)
Patch
  • 0.025 mg/24 hour
  • 0.0375 mg/24 hour
  • 0.050 mg/24 hour
  • 0.060 mg/24 hour
  • 0.075 mg/24 hour
  • 0.10 mg/24 hour
Menopausal vasomotor symptoms
  • Dosing: 0.025 mg/day patch applied once weekly
  • Titrate to desired effect. Use lowest effective dose.
  • Reevaluate need for therapy periodically

Menopausal vulvar and vaginal atrophy
  • Dosing: 0.025 mg/day patch applied once weekly
  • Titrate to desired effect. Use lowest effective dose.
  • Reevaluate need for therapy periodically

Hypogonadism, female castration, primary ovarian failure
  • Dosing: 0.025 mg/day patch applied once weekly
  • Titrate to desired effect. Use lowest effective dose.
  • Reevaluate need for therapy periodically

Prevention of postmenopausal osteoporosis
  • Dosing: 0.025 mg/day patch applied once weekly
Other
Price
  • Generic available
  • 4 patches - $-$$
Menostar®

(estradiol)
Patch
  • 0.014 mg/24 hour
Prevention of postmenopausal osteoporosis
  • Dosing: 0.014 mg/day patch applied once weekly
  • In women with a uterus, it is recommended that they receive a progestin for at least 14 days every 6 to 12 months and undergo an endometrial biopsy at yearly intervals or as clinically indicated
Other
Price
  • No generic
  • 4 patches - $$$
Minivelle®

(estradiol)
Patch
  • 0.025 mg/24 hour
  • 0.0375 mg/24 hour
  • 0.050 mg/24 hour
  • 0.075 mg/24 hour
  • 0.10 mg/24 hour
Menopausal vasomotor symptoms
  • Dosing: 0.0375 mg/day patch applied twice weekly
  • Titrate to desired effect. Use lowest effective dose.
  • Reevaluate need for therapy periodically

Prevention of postmenopausal osteoporosis
  • Dosing: 0.025 mg/day patch applied twice weekly
Other
Price
  • No generic
  • 8 patches - $$$
Vivelle-dot®

(estradiol)
Patch
  • 0.025 mg/24 hour
  • 0.0375 mg/24 hour
  • 0.050 mg/24 hour
  • 0.075 mg/24 hour
  • 0.10 mg/24 hour
Menopausal vasomotor symptoms
  • Dosing: 0.0375 mg/day patch applied twice weekly
  • Titrate to desired effect. Use lowest effective dose.
  • Reevaluate need for therapy periodically
  • In women with an intact uterus, may be given cyclically (3 weeks on followed by 1 week off)

Menopausal vulvar and vaginal atrophy
  • Dosing: 0.0375 mg/day patch applied twice weekly
  • Titrate to desired effect. Use lowest effective dose.
  • Reevaluate need for therapy periodically
  • In women with an intact uterus, may be given cyclically (3 weeks on followed by 1 week off)

Hypogonadism, female castration, primary ovarian failure
  • Dosing: 0.0375 mg/day patch applied twice weekly
  • Titrate to desired effect. Use lowest effective dose.
  • Reevaluate need for therapy periodically

Prevention of postmenopausal osteoporosis
  • Dosing: 0.025 mg/day patch applied twice weekly
  • In women with an intact uterus, may be given cyclically (3 weeks on followed by 1 week off)
Other
Price
  • Generic available
  • 8 patches - $$




Drug Dosage forms Dosing Other/Price
Premarin® vaginal cream

(conjugated estrogens)
Vaginal cream
  • 0.625 mg/gram
  • Comes in 30 gram tube
  • Comes with applicator that delivers 0.5, 1, 1.5, and 2 gram doses
Atrophic vaginitis and kraurosis vulvae
  • Starting: 0.5 grams intravaginally in a cyclic regimen (daily for 21 days followed by 7 days off)
  • Dose may be titrated up to 2 grams/day to achieve desired effect. Use lowest effective dose.

Dyspareunia due to menopause
  • Starting: 0.5 grams intravaginally in a twice weekly (for example Monday and Thursday) continuous regimen or in a cyclic regimen (daily for 21 days followed by 7 days off)
Other
Price
  • No generic
  • 30 gram tube - $$$$
Estrace® vaginal cream

(estradiol)
Vaginal cream
  • 0.01% cream
  • Comes in 42.5 gram tubes
  • Comes with applicator that delivers 1, 2, 3, and 4 gram doses
Vulvar and vaginal atrophy
  • Starting: 2 - 4 grams intravaginally for 1 - 2 weeks, then reduce to half initial dose for another 1 - 2 weeks
  • Maintenance: 1 gram one to three times a week
  • Use lowest effective dose
  • Reevaluate need for therapy periodically
Other
Price
  • No generic
  • 42.5 gram tube - $$$$

Drug Dosage forms Dosing Other/Price
Elestrin® gel

(estradiol)
Gel pump
  • 0.06% gel
  • Each pump delivers 0.87 grams of gel which contains 0.52 mg of estradiol
  • Comes in 35 gram pump that delivers 30 metered doses
Menopausal vasomotor symptoms
  • Starting: 0.87 grams (0.52 mg of estradiol) once daily
  • Titrate to desired effect. Use lowest effective dose.
  • Apply a thin layer to upper arm
Other
Price
  • No generic
  • 1 pump - $$
Estrogel® gel

(estradiol)
Gel pump
  • 0.06% gel
  • Each pump delivers 1.25 grams of gel which contains 0.75 mg of estradiol
  • Comes in a 50 gram pump that delivers 32 doses
Menopausal vasomotor symptoms
  • Dosing: 1.25 grams (0.75 mg of estradiol) once daily
  • Apply a thin layer over the entire arm on the inside and outside from wrist to shoulder

Menopausal vulvar and vaginal atrophy
  • Dosing: 1.25 grams (0.75 mg of estradiol) once daily
  • Apply a thin layer over the entire arm on the inside and outside from wrist to shoulder
Other
Price
  • No generic
  • 1 pump - $$$
Divigel® gel

(estradiol)
Gel packets
  • Comes in individual packets available in 3 doses
  • 0.25 mg packet
  • 0.50 mg packet
  • 1.0 mg packet
  • Comes in cartons of 30 packets
Menopausal vasomotor symptoms
  • Starting: 0.25 mg once daily
  • Titrate to desired effect. Use lowest effective dose.
  • Apply to skin of upper thigh. Alternate between thighs. Application surface area should be 5 - 7 inches.
  • Do not wash application site within 1 hour of applying gel
  • Allow gel to dry before dressing
Other
Price
  • No generic
  • 30 packets - $$$

Drug Dosage forms Dosing Other/Price
Estring®
vaginal ring

(estradiol)
Vaginal ring
  • Each ring contains 2 mg of estradiol
Menopausal vulvar and vaginal atrophy
  • Dosing: 1 ring placed intravaginally every 3 months
  • Ring is placed as high as possible into the upper one-third of the vaginal vault
  • Reevaluate need for therapy periodically
  • If ring falls out, rinse with lukewarm water and reinsert
  • Estring should not be felt when placed properly
Other
Price
  • No generic
  • 1 ring - $$$$
Femring®
vaginal ring

(estradiol)
Vaginal ring
  • 0.05 mg/day ring
  • 0.10 mg/day ring
Menopausal vasomotor symptoms
  • Starting: 0.05 mg/day ring intravaginally every 3 months
  • Titrate to desired effect. Use lowest effective dose.
  • Ring is placed as high as possible into the upper vagina
  • Reevaluate need for therapy periodically
  • If ring falls out, rinse with lukewarm water and reinsert
  • Femring should not be felt when placed properly

Menopausal vulvar and vaginal atrophy
  • Starting: 0.05 mg/day ring intravaginally every 3 months
  • Titrate to desired effect. Use lowest effective dose.
  • Ring is placed as high as possible into the upper vagina
  • Reevaluate need for therapy periodically
  • If ring falls out, rinse with lukewarm water and reinsert
  • Femring should not be felt when placed properly
Other
Price
  • No generic
  • 1 ring - $$$$
Vagifem®
vaginal tablet

(estradiol)
Vaginal tablet
  • 10 mcg
  • Each tablet comes with single-use applicator
Menopausal atrophic vaginitis
  • Starting: 10 mcg tablet inserted intravaginally once daily for 2 weeks, followed by 1 tablet twice weekly (for example Tuesday and Friday)
Other
Price
  • No generic
  • 8 tablets - $$$-$$$$

Drug Dosage forms Dosing Other/Price
Evamist®
spray

(estradiol)
Spray
  • Each spray contains 1.53 mg of estradiol
  • Comes in 8.1 ml spray bottle that delivers 56 sprays
Menopausal vasomotor symptoms
  • Dosing: 1 - 3 sprays once daily
  • Titrate to desired effect. Use lowest effective dose.
  • Spray on inner surface of forearm starting at elbow. Do not overlap sprays.
  • Allow spray to dry for 2 minutes before covering with clothing
  • Do not wash spray site for at least one hour
Other
Price
  • No generic
  • 1 bottle - $$$




Drug Dosage forms Dosing Other/Price
Aygestin®

(norethindrone)
Tablet
  • 5 mg
Secondary amenorrhea and abnormal uterine bleeding
  • Dosing: 2.5 - 10 mg once daily for 5 - 10 days
  • Withdrawal bleeding usually occurs within 3 - 7 days after stopping norethindrone
  • Endometrium should be adequately primed with endogenous or exogenous estrogen
  • See abnormal uterine bleeding for more

Endometriosis
  • Starting: 5 mg once daily for 2 weeks. Increase dose by 2.5 mg/day every 2 weeks until 15 mg/day is reached.
  • Continue therapy for 6 - 9 months as tolerated
Other
Price
  • Generic available
  • 30 tablets - $-$$
Prometrium®

(progesterone)
Capsule
  • 100 mg
  • 200 mg
Secondary amenorrhea
  • Dosing: 400 mg once daily at bedtime for 10 days

Prevention of endometrial hyperplasia in women receiving estrogens
  • Dosing: 200 mg once daily at bedtime for 12 sequential days out of each 28-day cycle
Other
Price
  • Generic available
  • 30 capsules - $$-$$$
Provera®

(medroxy-
progesterone)
Tablet
  • 2.5 mg
  • 5 mg
  • 10 mg
Secondary amenorrhea
  • Dosing: 5 - 10 mg once daily for 5 - 10 days
  • A dose for inducing an optimum secretory transformation of an endometrium that has been adequately primed with either endogenous or exogenous estrogen is 10 mg once daily for 10 days
  • Withdrawal bleeding usually occurs within 3 - 7 days after stopping medroxyprogesterone

Abnormal uterine bleeding
  • Dosing: 5 - 10 mg once daily for 5 - 10 days starting on the calculated 16th or 21st day of the menstrual cycle
  • To produce an optimum secretory transformation of an endometrium that has been adequately primed with either endogenous or exogenous estrogen, 10 mg of Provera daily for 10 days beginning on the 16th day of the cycle is suggested
  • Withdrawal bleeding usually occurs within 3 - 7 days after stopping medroxyprogesterone
  • See abnormal uterine bleeding for more

Prevention of endometrial hyperplasia in women receiving estrogens
  • Dosing: 5 - 10 mg once daily for 12 - 14 consecutive days each month. Dosing may begin on the first or 16th day of each cycle.
  • Use lowest effective dose
Other
Price
  • Generic available
  • 30 tablets - $
Crinone®
gel

(progesterone)
Gel
  • 4% gel (45 mg per applicator)
  • 8% gel (90 mg per applicator)
  • Comes in single-use vaginal applicator that contains 1.45 grams of gel
Secondary amenorrhea
  • Starting: 45 mg intravaginally every other day for 6 doses
  • If 4% gel does not work, may increase to 8%
  • Dosage increases can only be accomplished by increasing the strength (4% to 8%). Administering more gel does not increase absorption.

Assisted reproductive technology
  • Supplementation: 90 mg once daily
  • Replacement: 90 mg twice daily
  • If pregnancy occurs, may continue for up to 10 - 12 weeks
Other
Price
  • No generic
  • 6 applicators - $$$




Drug Dosage forms Dosing Other/Price
Activella®
Mimvey®
Lopreeza®
Amabelz®

(estradiol, norethindrone)
Tablet
  • Estradiol : Norethindrone
    • 0.5 mg : 0.1 mg
    • 1 mg : 0.5 mg
Menopausal vasomotor symptoms
  • Dosing: 1 tablet once daily
  • Titrate to desired effect. Use lowest effective dose.

Menopausal vulvar and vaginal atrophy
  • Dosing: 1 mg/0.5 mg once daily

Prevention of postmenopausal osteoporosis
  • Dosing: 1 tablet once daily
  • Titrate to desired effect. Use lowest effective dose.
Other
  • See estrogens below for side effects, contraindications, precautions, and drug interactions
  • See progestins below for side effects, contraindications, precautions, and drug interactions

Price
  • Generic available
  • 28 tablets - $$
Angeliq®
(estradiol, drospirenone)
Tablet
  • Drospirenone : Estradiol
    • 0.25 mg : 0.5 mg
    • 0.5 mg : 1.0 mg
Menopausal vasomotor symptoms
  • Dosing: 0.25/0.5 - 0.5/1 mg once daily
  • Titrate to desired effect. Use lowest effective dose.

Menopausal vulvar and vaginal atrophy
  • Dosing: 0.5/1 mg once daily
Other
  • See estrogens below for side effects, contraindications, precautions, and drug interactions
  • See progestins below for side effects, contraindications, precautions, and drug interactions
  • Angeliq contains drospirenone which has antialdosterone activity. Hyperkalemia may occur in susceptible patients and with certain medications. See drospirenone below.

Price
  • No generic
  • 28 tablets - $$$$
Femhrt®
Fyavolv®
Jevantique®
Jevantique Lo®
Jinteli®

(ethinyl estradiol, norethindrone)
Tablet
  • Femhrt, Jevantique Lo, Fyavolv
  • EE : Norethindrone
    • 0.0025 mg : 0.5 mg

  • Femhrt, Jevantique, Fyavolv, Jinteli
  • EE : Norethindrone
    • 0.0050 mg : 1 mg
Menopausal vasomotor symptoms
  • Dosing: 1 tablet once daily

Prevention of postmenopausal osteoporosis
  • Dosing: 1 tablet once daily
Other
  • See estrogens below for side effects, contraindications, precautions, and drug interactions
  • See progestins below for side effects, contraindications, precautions, and drug interactions

Price
  • Generic available
  • 28 tablets - $-$$
Duavee®

(bazedoxifene,
conjugated estrogens)
Tablet
Conjugated estrogens : Bazedoxifene
  • 0.45 mg : 20 mg
Menopausal vasomotor symptoms
  • Dosing: 1 tablet once daily

Prevention of postmenopausal osteoporosis
  • Dosing: 1 tablet once daily
Other
  • May take without regard to food. Swallow tablets whole.
  • Bazedoxifene is a SERM. Bazedoxifene helps to prevent endometrial hyperplasia, therefore women with a uterus do not need to take a progestin with Duavee.
  • See Duavee below for contraindications, precautions, side effects, and drug interactions
  • See SERM activity table for more

Price
  • No generic
  • 30 tablets - $$$
Premphase®

(medroxyprogesterone, conjugated estrogens)
Tablet
  • 14 maroon tablets -
    0.625 mg of conjugated estrogens

  • 14 light-blue tablets -
    0.625 mg of conjugated estrogens + 5 mg medroxyprogesterone
Menopausal vasomotor symptoms
  • Dosing: 1 tablet once daily

Menopausal vulvar and vaginal atrophy
  • Dosing: 1 tablet once daily

Prevention of postmenopausal osteoporosis
  • Dosing: 1 tablet once daily
Other
  • See estrogens below for side effects, contraindications, precautions, and drug interactions
  • See progestins below for side effects, contraindications, precautions, and drug interactions

Price
  • No generic
  • 28 tablets - $$$-$$$$
Prempro®

(conjugated estrogens, medroxyprogesterone)
Tablet
  • Conjugated estrogens : Medroxyprogesterone
    • 0.3 mg : 1.5 mg
    • 0.45 mg : 1.5 mg
    • 0.625 mg : 2.5 mg
    • 0.625 mg : 5 mg
Menopausal vasomotor symptoms
  • Dosing: 1 tablet once daily
  • Titrate to desired effect. Use lowest effective dose.

Menopausal vulvar and vaginal atrophy
  • Dosing: 1 tablet once daily
  • Titrate to desired effect. Use lowest effective dose.

Prevention of postmenopausal osteoporosis
  • Dosing: 1 tablet once daily
Other
  • See estrogens below for side effects, contraindications, precautions, and drug interactions
  • See progestins below for side effects, contraindications, precautions, and drug interactions

Price
  • No generic
  • 28 tablets - $$$-$$$$

Drug Dosage forms Dosing Other/Price
Climara pro®

(estradiol, levonorgestrel)
Patch
  • Each patch delivers 0.045 mg/day of estradiol and 0.015 mg/day of levonorgestrel
  • Comes in carton of 4 patches
Menopausal vasomotor symptoms
  • Dosing: one patch once weekly

Prevention of postmenopausal osteoporosis
  • Dosing: one patch once weekly
Other
  • Apply to lower abdomen or the upper quadrant of the buttocks. Avoid waistline or areas where patch may be rubbed.
  • Rotate application site
  • Do not expose patch to sun for prolonged periods
  • See estrogens below for side effects, contraindications, precautions, and drug interactions
  • See progestins below for side effects, contraindications, precautions, and drug interactions

Price
  • No generic
  • 4 patches - $$$
Combipatch®

(estradiol, norethindrone)
Patch
  • Estradiol : Norethindrone
    • 0.05 mg/0.14 mg
    • 0.05 mg/0.25 mg
    • Strengths reflect mg/day delivered
    • Comes in carton of 8 patches
Menopausal vasomotor symptoms
  • Dosing: one patch twice weekly
  • Titrate to desired effect. Use lowest effective dose.

Menopausal vulvar and vaginal atrophy
  • Dosing: one patch twice weekly
  • Titrate to desired effect. Use lowest effective dose.

Hypogonadism, female castration, primary ovarian failure
  • Dosing: one patch twice weekly
  • Titrate to desired effect. Use lowest effective dose.
Other
  • Apply to lower abdomen. Avoid waistline or areas where patch may be rubbed.
  • Rotate application site
  • Do not expose patch to sun for prolonged periods
  • See estrogens below for side effects, contraindications, precautions, and drug interactions
  • See progestins below for side effects, contraindications, precautions, and drug interactions

Price
  • No generic
  • 8 patches - $$$




Drug Dosage forms Dosing Other/Price
Premarin® injection

(conjugated estrogens)
Vial
  • 25 mg
Abnormal uterine bleeding
  • Dosing: 25 mg intravenously every 4 - 6 hours for 24 hours [3]
  • May also be given intramuscularly, although IV is preferred.
  • Premarin injection may cause significant nausea. Administer with anti nausea medication.
  • See abnormal uterine bleeding for more
Other
Price
  • No generic
  • 1 vial - ?
Depo-estradiol® injection

(estradiol cypionate)
Vial
  • 5 mg/ml
  • Comes in 5 ml vial
Menopausal vasomotor symptoms
  • Dosing: 1 - 5 mg intramuscularly every 3 - 4 weeks
  • Titrate to desired effect. Use lowest effective dose.
  • Reevaluate need for therapy periodically

Menopausal vulvar and vaginal atrophy
  • Dosing: 1 - 5 mg intramuscularly every 3 - 4 weeks
  • Titrate to desired effect. Use lowest effective dose.
  • Reevaluate need for therapy periodically

Hypogonadism
  • Dosing: 1.5 - 2 mg intramuscularly once monthly
  • Titrate to desired effect. Use lowest effective dose.
Other
Price
  • No generic
  • 1 vial - $$
Delestrogen® injection

(estradiol valerate)
Vial
  • 10 mg/ml
  • 20 mg/ml
  • 40 mg/ml
  • Comes in 5 ml vials
Menopausal vasomotor symptoms
  • Dosing: 10 - 20 mg intramuscularly every 4 weeks
  • Titrate to desired effect. Use lowest effective dose.
  • Reevaluate need for therapy periodically

Menopausal vulvar and vaginal atrophy
  • Dosing: 10 - 20 mg intramuscularly every 4 weeks
  • Titrate to desired effect. Use lowest effective dose.
  • Reevaluate need for therapy periodically

Hypogonadism
  • Dosing: 10 - 20 mg intramuscularly every 4 weeks
  • Titrate to desired effect. Use lowest effective dose.

Palliative treatment of advanced prostate cancer
  • Dosing: 30 mg intramuscularly every 1 - 2 weeks
Other
Price
  • Generic available
  • 1 vial - $$-$$$$



Estrogen side effects
NOTE: information is from the Premarin PI. Information is for the 0.625 mg/day dose in women who had a uterus. Only side effects that occurred at an incidence ≥ 2% more than placebo are listed. P = % of patients on placebo who experienced side effect.

  • Vaginal hemorrhage - 13%, P - 0%
  • Abdominal pain - 11%, P - 6%
  • Breast pain - 11%, P - 8%
  • Flatulence - 6%, P - 2%
  • Endometrial hyperplasia - 5%, P - 0%
  • Vaginitis - 5%, P - 0%
  • Weakness - 5%, P - 1%
  • Back pain - 5%, P - 1%
  • White or yellow vaginal discharge - 5%, P - 2%
  • Yeast infection - 4%, P - 2%
  • Metrorrhagia (menstrual bleeding at irregular intervals) - 3%, P - 0%
  • Uterine spasm - 3%, P - 1%
  • Pelvic pain - 3%, P - 1%
  • Leg cramps - 3%, P - 1%
  • Itching - 3%, P - 1%
  • Dysmenorrhea (painful menses) - 3%, P - 1%
  • Cervix disorder - 2%, P - 0%
  • Application site reactions (patches) - may occur with patches

Estrogen contraindications
  • Estrogens are contraindicated in the following conditions:
    • Undiagnosed abnormal genital bleeding
    • Known, suspected, or history of breast cancer
    • Known or suspected estrogen-dependent neoplasia
    • Active deep vein thrombosis (DVT), pulmonary embolism (PE), or a history of these conditions (See hormone therapy during anticoagulation for VTE for more on this topic)
    • Active or recent arterial thromboembolic disease (for example, stroke and MI), or a history of these conditions
    • Know hypersensitivity
    • Known liver impairment or disease
    • Known protein C, protein S, or antithrombin deficiency, or other known thrombophilic disorders
    • Known or suspected pregnancy

Estrogen precautions
Women's Health Initiative (WHI) study
  • The WHI study was a large (over 27,000 subjects), randomized controlled trial that evaluated the long-term risks of hormone replacement therapy in postmenopausal women. The study had two arms. In one arm, women with a uterus were randomized to Prempro® or placebo. In the other arm, women who had no uterus were randomized to Premarin® or placebo.
  • The study measured a number of outcomes, and they are presented in our WHI study results tables

Estrogen precautions
  • Women with a uterus - estrogen therapy increases the risk of endometrial hyperplasia. Progestins reduce the risk. In general, women with a uterus who are taking estrogens should receive a progestin either daily in a continuous regimen or for 10 days out of the cycle in cyclical regimens. Women without a uterus (s/p hysterectomy) do not need a progestin.
  • Endometrial cancer - unopposed estrogen therapy increases the risk of endometrial cancer. Adding a progestin may help reduce the risk.
  • Stroke - in the WHI study, estrogen therapy increased the risk of stroke
  • Deep vein thrombosis (DVT) - in the WHI study, estrogen therapy increased the risk of deep vein thrombosis (DVT)
  • Gallbladder disease - estrogen therapy may increase the risk of gallbladder disease
  • Surgery and immobilization - because of the increased risk of venous thromboembolism, estrogens should be discontinued at least 4 - 6 weeks before surgery that is associated with an increased risk of thromboembolism, or during periods of prolonged immobilization.
  • Hypothyroidism - estrogens increase levels of thyroid-binding globulin. Women with normal thyroid function can compensate by making more thyroid hormone. Women with hypothyroidism may require an increase in levothyroxine dosage.
  • Retinal vascular thrombosis - has been reported in women taking estrogens. Discontinue medication if sudden visual changes occur.
  • Plasma lipids - estrogens may raise triglyceride and HDL levels while decreasing LDL levels
  • Liver disease - estrogen levels may be increased. Estrogens may exacerbate cholestatic jaundice in susceptible women.
  • Fluid retention - estrogens may cause fluid retention. Use caution in susceptible patients (e.g. kidney failure, heart failure).
  • Hypocalcemia - estrogens may worsen hypocalcemia
  • Elevated blood pressure - estrogens may raise blood pressure in some patients
  • Endometriosis - estrogens may exacerbate endometriosis. For women with residual endometriosis s/p hysterectomy, consider addition of a progestin.
  • Hereditary angioedema - estrogens may exacerbate hereditary angioedema
  • Exacerbation of other conditions - estrogens may exacerbate asthma, diabetes mellitus, epilepsy, migraine, porphyria, systemic lupus erythematosus, and hepatic hemangiomas
  • Platelets and clotting factors - estrogens may increase levels and activity of platelets and clotting factors
  • Binding proteins - estrogens may increase levels of binding proteins (e.g. corticosteroid binding globulin, sex hormone-binding globulin). Other plasma proteins may also be increased (e.g. angiotensinogen/renin substrate, alpha-1-antitrypsin, ceruloplasmin)
  • Photosensitivity - estrogens may cause photosensitivity. Limit sun exposure and/or wear sunscreen to help prevent reactions.

Estrogen + progestin therapy
  • Pulmonary embolism (PE) - in the WHI study, estrogen + progestin therapy increased the risk of pulmonary embolism
  • Myocardial infarction - in the WHI study, women taking estrogen + progestin therapy had a borderline nonsignificant increase in risk of myocardial infarction
  • Dementia - in the WHI study, estrogen + progestin therapy increased the risk of developing probable dementia in women ≥ 65 years old
  • Invasive breast cancer - in the WHI study, estrogen + progestin therapy increased the risk of developing invasive breast cancer


Estrogen drug interactions



Progestin side effects
NOTE: the incidence of side effects from progesterone and progestins is not well-defined. Information below is from the Provera PI.

  • Genitourinary system
    • Abnormal uterine bleeding (irregular, increase, decrease), change in menstrual flow, breakthrough bleeding, spotting, amenorrhea, changes in cervical erosion and cervical secretions
  • Breasts
    • Breast tenderness, mastodynia or galactorrhea has been reported
  • Cardiovascular
    • Thromboembolic disorders including thrombophlebitis and pulmonary embolism have been reported
  • Gastrointestinal
    • Nausea, cholestatic jaundice
  • Skin
    • Sensitivity reactions consisting of urticaria, pruritus, edema and generalized rash have occurred. Acne, alopecia and hirsutism have been reported.
  • Eyes
    • Neuro-ocular lesions, for example, retinal thrombosis, and optic neuritis
  • Central nervous system
    • Mental depression, insomnia, somnolence, dizziness, headache, nervousness
  • Miscellaneous
    • Hypersensitivity reactions (for example, anaphylaxis and anaphylactoid reactions, angioedema), rash (allergic) with and without pruritus, change in weight (increase or decrease), pyrexia, edema/fluid retention, fatigue, decreased glucose tolerance.

Progestin contraindications
  • Progestins are contraindicated in the following conditions:
    • PEANUT ALLERGY (Prometrium®) - Prometrium capsules contain peanut oil
    • Undiagnosed abnormal genital bleeding
    • Known, suspected, or history of breast cancer
    • Known or suspected estrogen- or progesterone-dependent neoplasia
    • Active deep vein thrombosis (DVT), pulmonary embolism (PE), or a history of these conditions (See hormone therapy during anticoagulation for VTE for more on this topic)
    • Active or recent arterial thromboembolic disease (for example, stroke and MI), or a history of these conditions
    • Know hypersensitivity
    • Known liver impairment or disease
    • Known or suspected pregnancy

Progestin precautions
Women's Health Initiative (WHI) study
  • The WHI study was a large (over 27,000 subjects), randomized controlled trial that evaluated the long-term risks of hormone replacement therapy in postmenopausal women. The study had two arms. In one arm, women with a uterus were randomized to Prempro® or placebo. In the other arm, women who had no uterus were randomized to Premarin® or placebo.
  • The study measured a number of outcomes, and they are presented in our WHI study results tables

Progestin precautions
  • Women with a uterus - estrogen therapy increases the risk of endometrial hyperplasia. Progestins reduce the risk. In general, women with a uterus who are taking estrogens should receive a progestin either daily in a continuous regimen or for 10 days out of the cycle in cyclical regimens. Women without a uterus (s/p hysterectomy) do not need a progestin.
  • Endometrial cancer - unopposed estrogen therapy increases the risk of endometrial cancer. Adding a progestin may help reduce the risk.
  • Stroke - in the WHI study, women taking Prempro (conjugated estrogens + medroxyprogesterone) had an increased risk of stroke when compared to placebo. The risk of stroke was also increased in women who took conjugated estrogens only. The strength of association between stroke and progesterone is unknown.
  • Deep vein thrombosis (DVT) - in the WHI study, women taking Prempro (conjugated estrogens + medroxyprogesterone) had an increased risk of DVT when compared to placebo. The risk of DVT was also increased in women who took conjugated estrogens only. The strength of association between DVT and progesterone is unknown.
  • Surgery and immobilization - because of the increased risk of venous thromboembolism, estrogen + progestin therapy should be discontinued at least 4 - 6 weeks before surgery that is associated with an increased risk of thromboembolism, or during periods of prolonged immobilization.
  • Pulmonary embolism (PE) - in the WHI study, women taking Prempro (conjugated estrogens + medroxyprogesterone) had an increased risk of PE when compared to placebo. The strength of association between PE and progesterone is unknown.
  • Dementia - in the WHI study, women ≥ 65 years old taking Prempro (conjugated estrogens + medroxyprogesterone) had an increased risk of probable dementia when compared to placebo. The strength of association between dementia and progesterone is unknown.
  • Invasive breast cancer - in the WHI study, women taking Prempro (conjugated estrogens + medroxyprogesterone) had an increased risk of invasive breast cancer when compared to placebo. The risk of invasive breast cancer was not increased in women who took conjugated estrogens only. The strength of association between invasive breast cancer and progesterone is unknown.
  • Heart attack - in the WHI study, women taking Prempro (conjugated estrogens + medroxyprogesterone) had a borderline nonsignificant increased risk of heart attack when compared to placebo. The strength of association between heart attack risk and progesterone is unknown.
  • Endometriosis - estrogens may exacerbate endometriosis. For women with residual endometriosis s/p hysterectomy, consider addition of a progestin.
  • Hypothyroidism - estrogen + progestin therapy may increase levels of thyroid-binding globulin. Women with normal thyroid function can compensate by making more thyroid hormone. Women with hypothyroidism may require an increase in levothyroxine dosage.
  • Elevated blood pressure - progestins may raise blood pressure in some patients
  • Plasma lipids - progestins may raise triglyceride and HDL levels while decreasing LDL levels
  • Liver disease - progestin levels may be increased
  • Fluid retention - progestins may cause fluid retention. Use caution in susceptible patients (e.g. kidney failure, heart failure).
  • Exacerbation of other conditions - estrogen + progestin therapy may exacerbate asthma, diabetes mellitus, epilepsy, migraine, porphyria, systemic lupus erythematosus, and hepatic hemangiomas
  • Platelets and clotting factors - estrogen + progestin therapy may increase levels and activity of platelets and clotting factors
  • Binding proteins - estrogen + progestin therapy may increase levels of binding proteins (e.g. corticosteroid binding globulin, sex hormone-binding globulin). Other plasma proteins may be increased (e.g. angiotensinogen/renin substrate, alpha-1-antitrypsin, ceruloplasmin)


Progestin drug interactions
  • CYP3A4 inducers and inhibitors - progestins are metabolized by CYP3A4. CYP3A4 inducers may decrease progestin levels and CYP3A4 inhibitors may increase progestin levels.

Drospirenone
Angeliq contains the progestin drospirenone. Drospirenone has antialdosterone properties which means it may contribute to hyperkalemia when taken by itself and/or when combined with other potassium-raising medications.

  • Contraindications - Angeliq is contraindicated in women with kidney or liver impairment. It is also contraidicated in women with adrenal insufficiency.
  • Drug interactions
    • CYP3A4 strong inhibitors - Use caution and consider monitoring potassium levels when taking Angeliq with strong CYP3A4 inhibitors
    • Drugs that may raise potassium - Angeliq may raise potssium levels when taken with other drugs that raise potassium such as ACE inhibitors, angiotensin receptor blockers, aldosterone antagonists, and NSAIDs. In studies involving postmenopausal women who were taking ACE inhibitors or ARBs, drospirenone 3 mg once daily for a month raised potassium levels an average of 0.11 mEq/L while placebo-treated patients saw an average increase of 0.08 mEq/L.



Osphena® prescribing information
Mechanism of action
  • Ospemifene is a selective estrogen receptor modulator (SERM). SERMs act as estrogen receptor agonists (stimulate) in some tissues and as estrogen receptor antagonists (block) in other tissues. See SERM activity table for more.

    • Ospemifene has the following activities:
      • Endometrium - neutral to partial agonist
      • Vagina - agonist
      • Breast - antagonist
      • Bone - osteoclast formation - neutral; bone resorption - antagonist; bone formation - agonist [2]

Contraindications
  • Undiagnosed abnormal genital bleeding
  • Known or suspected estrogen-dependent neoplasia
  • Active deep vein thrombosis (DVT), pulmonary embolism (PE), or a history of these conditions
  • Active or recent arterial thromboembolic disease (for example, stroke and MI), or a history of these conditions
  • Know hypersensitivity
  • Known or suspected pregnancy

Precautions
  • Stroke - in the WHI study, estrogen therapy increased the risk for stroke. In the clinical trials for ospemifene (duration of treatment up to 15 months), the incidence rates of thromboembolic and hemorrhagic stroke were 0.72 and 1.45 per thousand women, respectively in the ospemifene group and 1.04 and 0 per thousand women in the placebo group.
  • Venous thromboembolism (VTE) - in the WHI study, estrogen therapy increased the risk for VTE. In ospemifene clinical trials, the incidence of DVT was 1.45 per thousand women in the ospemifene group and 1.04 per thousand women in the placebo group.
  • Endometrial thickening and endometrial cancer - ospemifene is a partial agonist in endometrial tissue. It causes endometrial thickening in some women (in trials, ≥ 5 mm thickening was seen in 60.1 per thousand women treated with ospemifene vs. 21.2 per thousand women treated with placebo). Endometrial thickening may lead to endometrial hyperplasia and cancer. The addition of a progestin to ospemifene therapy may decrease the risk of endometrial hyperplasia and cancer.
  • Surgery and immobilization - because of the increased risk of venous thromboembolism, ospemifene should be discontinued at least 4 - 6 weeks before surgery that is associated with an increased risk of thromboembolism, or during periods of prolonged immobilization.
  • Uterine polyps - in trials, uterine polyps occurred at an incidence of 5.9 per thousand women in the ospemifene group vs. 1.8 per thousand women in the placebo group
  • Breast cancer - ospemifene has not been studied adequately in women with breast cancer and therefore should not be used
  • Kidney disease - no dose adjustment necessary
  • Liver disease
    • Mild to moderate (Child-Pugh A/B) - no dose adjustment necessary
    • Severe (Child-Pugh C) - has not been studied. DO NOT USE.

Side effects
NOTE: P = % of patients taking placebo who experienced side effect
  • Hot flush - 7.5%, P - 2.6%
  • Vaginal discharge - 3.8%, P - 0.3%
  • Muscle spasm - 3.2%, P - 0.9%
  • Excessive sweating - 1.6%, P - 0.6%
  • Genital discharge - 1.3%, P - 0.1%

Drug interactions
  • Ospemifene is primarily metabolized by CYP3A4 and CYP2C9. CYP2C19 also contributes to its metabolism. Drugs that inhibit both CYP3A4 and CYP2C9 may increase exposure to ospemifene.
  • Other estrogens and SERMs - DO NOT COMBINE. Ospemifene should not be used with estrogens or other SERMs
  • Fluconazole (Diflucan®) - DO NOT COMBINE. Fluconazole is a moderate CYP3A / strong CYP2C9 / moderate CYP2C19 inhibitor. Exposure to ospemifene is increased.
  • Rifampin - rifampin is a strong CYP3A4 / moderate CYP2C9 / moderate CYP2C19 inducer. Exposure to ospemifene is decreased.
  • Ketoconazole - ketoconazole is a strong CYP3A4 inhibitor. Exposure to ospemifene is increased by 1.4-fold. Use caution in chronic dosing.
  • Highly protein-bound drugs - ospemifene is 99% bound to serum proteins. It may affect the protein binding of other drugs.



Duavee® prescribing information
Mechanism of action
  • Duavee contains bazedoxifene and conjugated estrogens
  • Bazedoxifene is a selective estrogen receptor modulator (SERM). SERMs act as estrogen receptor agonists (stimulate) in some tissues and as estrogen receptor antagonists (block) in other tissues. See SERM activity table for more.

    • Bazedoxifene has the following activities:
      • Endometrium - neutral to antagonist
      • Vagina - unknown
      • Breast - antagonist
      • Bone - agonist [2]

Contraindications
Precautions
  • Bazedoxifene helps to prevent endometrial hyperplasia, therefore women with a uterus do not need to take a progestin with Duavee
  • Precautions with Duavee are the same as those with conjugated estrogens (see estrogen precautions above)

Side effects
NOTE: P = % of patients taking placebo who experienced side effect. Only side effects that occurred at an incidence ≥ 2% more than placebo are listed
  • Muscle spasm - 9%, P - 6%
  • Nausea - 8%, P - 5%
  • Diarrhea - 8%, P - 5%
  • Upper abdominal pain - 7%, P - 5%
  • Dizziness - 5%, P - 3%

Drug interactions
  • CYP3A4 inducers and inhibitors - estrogens are partially metabolized by CYP3A4. CYP3A4 inducers may decrease estrogen levels and CYP3A4 inhibitors may increase estrogen levels.
  • Uridine Diphosphate Glucuronosyltransferase (UGT) - bazedoxifene undergoes metabolism by the UGT enzyme in the intestinal tract and liver. Metabolism of bazedoxifene may be increased by UGT inducers (e.g. rifampin, phenobarbital, carbamazepine, phenytoin). A reduction in bazedoxifene exposure may lead to endometrial hyperplasia.