FEMALE HORMONE MEDICATIONS




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Elestrin® gel (estradiol)

Dosage forms

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
  • Comes in package of one or two pumps

Dosing

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

Generic / Price

  • No generic
  • 1 pump - $$$

Other

  • Prime pump before first use
  • Wash hands after applying
  • Apply after bathing. Allow 2 hours after applying before swimming.
  • Sunscreen may increase absorption. Do not apply sunscreen until at least 25 minutes after applying Elestrin. Do not apply sunscreen to the Elestrin application site for 7 or more days in a row.
  • Gel may be transferred through skin contact to other people. Cover application site after it dries.

Estrogel® gel (estradiol)

Dosage forms

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

Dosing

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

Generic / Price

  • No generic
  • 1 pump - $$$

Other

  • Pump must be primed 3 times before first use
  • Use of lotion one hour after application increases estradiol absorption
  • Wash hands after applying
  • Apply after bathing. Do not swim for as long as possible after applying.
  • Gel may be transferred through skin contact to other people. Cover application site after it dries.

Divigel® gel (estradiol)

Dosage forms

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

Dosing

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

Generic / Price

  • No generic
  • 30 packets - $$$

Other

  • Sunscreens and lotions may increase the absorption of estradiol
  • Apply after bathing. Allow application to dry before swimming.
  • Gel may be transferred through skin contact to other people. Cover application site after it dries.



Premarin® injection (conjugated estrogens)

Dosage forms

Vial
  • 25 mg

Dosing

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

Generic / Price

  • No generic
  • 1 vial - ?

Other

  • Premarin injection is for short-term use to stop significant abnormal uterine bleeding

Depo-estradiol® (estradiol cypionate)

Dosage forms

Vial
  • 5 mg/ml
  • Comes in 5 ml vial

Dosing

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.

Generic / Price

  • No generic
  • 1 vial - $$$

Other

  • Store at room temperature
  • Storage at low temperatures may result in the separation of some crystalline material which redissolves readily on warming

Delestrogen® (estradiol valerate)

Dosage forms

Vial
  • 10 mg/ml
  • 20 mg/ml
  • 40 mg/ml
  • Comes in 5 ml vials

Dosing

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

Generic / Price

  • Generic available
  • 1 vial - $

Other

  • Inject in upper, outer quadrant of gluteus
  • Store at room temperature
  • Storage at low temperatures may result in the separation of some crystalline material which redissolves readily on warming



Alora® patch (estradiol)

Dosage forms

Patch
  • 0.025 mg/24 hour
  • 0.050 mg/24 hour
  • 0.075 mg/24 hour
  • 0.10 mg/24 hour
  • Comes in carton of 8 patches

Dosing

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

Generic / Price

  • No generic
  • 8 patches - $$$

Other

  • Recommended application site is lower abdomen. The upper quadrant of the buttocks or outer aspect of the hip may also be used. Rotate application site allowing 1 week before using same site again. DO NOT apply to breasts.
  • In women who are switching from oral estrogens, allow 1 week from discontinuing pills before applying patch unless symptoms return

Climara® (estradiol)

Dosage forms

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
  • Comes in carton with 4 patches

Dosing

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

Generic / Price

  • Generic available
  • 4 patches - $-$$

Other

  • Recommended application site is lower abdomen or upper quadrant of the buttocks. Rotate application site. DO NOT apply on or near breasts.
  • In women who are switching from oral estrogens, allow 1 week from discontinuing pills before applying patch unless symptoms return

Menostar® (estradiol)

Dosage forms

Patch
  • 0.014 mg/24 hour
  • Comes in package with 4 patches

Dosing

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

Generic / Price

  • No generic
  • 4 patches - $$$$

Other

  • Recommended application site is lower abdomen. Rotate application site. DO NOT apply on or near breasts.

Minivelle® (estradiol)

Dosage forms

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
  • Comes in package with 8 patches

Dosing

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

Generic / Price

  • No generic
  • 8 patches - $$$$

Other

  • Recommended application site is lower abdomen or buttocks. Rotate application site allowing 1 week before using same site again. DO NOT apply to breasts.

Vivelle-dot® (estradiol)

Dosage forms

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
  • Comes in carton with 8 patches

Dosing

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)

Generic / Price

  • Generic available
  • 8 patches - $

Other

  • Recommended application site is the trunk of the body including the abdomen and buttocks. Rotate application site allowing 1 week before using same site again. DO NOT apply to breasts.
  • In women who are switching from oral estrogens, allow 1 week from discontinuing pills before applying patch unless symptoms return



Cenestin® (conjugated estrogens)

Dosage forms

Tablet
  • 0.30 mg
  • 0.45 mg
  • 0.625 mg
  • 0.90 mg
  • 1.25 mg

Dosing

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.

Generic / Price

  • No generic
  • 30 tablets - $$$

Other

  • May take without regard to food
  • Cenestin contains a blend of 9 synthetic estrogenic substances

Enjuvia® (conjugated estrogens)

Dosage forms

Tablet
  • 0.30 mg
  • 0.45 mg
  • 0.625 mg
  • 0.90 mg
  • 1.25 mg

Dosing

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.

Generic / Price

  • No generic
  • 30 tablets - $$

Other

  • May take without regard to food
  • Enjuvia contains a blend of 10 synthetic estrogenic substances

Premarin® (conjugated estrogens)

Dosage forms

Tablet
  • 0.30 mg
  • 0.45 mg
  • 0.625 mg
  • 0.90 mg
  • 1.25 mg

Dosing

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

Generic / Price

  • No generic
  • 30 tablets - $$$$

Other

  • May take without regard to food
  • Premarin contains a mixture of conjugated estrogens purified from pregnant mares' urine

Estrace® (estradiol)

Dosage forms

Tablet
  • 0.50 mg
  • 1.0 mg
  • 2.0 mg

Dosing

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

Generic / Price

  • Generic available
  • 30 tablets - $

Other

  • May take without regard to food

Menest® (esterified estrogens)

Dosage forms

Tablet
  • 0.30 mg
  • 0.625 mg
  • 1.25 mg
  • 2.5 mg

Dosing

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

Generic / Price

  • No generic
  • 30 tablets - $$-$$$$ depending on dose

Other

  • May take without regard to food
  • Esterified estrogens are a mixture of the sodium salts of the sulfate esters of the estrogenic substances, principally estrone, that are of the type excreted by pregnant mares

Ogen® (estropipate)

Dosage forms

Tablet
  • 0.75 mg
  • 1.5 mg
  • 3.0 mg

Dosing

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.

Generic / Price

  • Generic available
  • 30 tablets - $

Other

  • May take without regard to food
  • Estropipate is a natural estrogenic substance prepared from purified crystalline estrone, solubilized as the sulfate and stabilized with piperazine

Osphena® (ospemifene)

Dosage forms

Tablet
  • 60 mg

Dosing

Dyspareunia due to menopause
  • Dosing: 60 mg once daily with food
  • Food increases absorption
  • Use for shortest duration necessary
  • Ospemifene has an agonistic effect on the endometrium. A progestin should be considered in women with a uterus.

Generic / Price

  • No generic
  • 30 tablets - $$$$

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]

Side effects



Side effect Osphena Placebo
Hot flush 7.5% 2.6%
Vaginal discharge 3.8% 0.3%
Muscle spasm 3.2% 0.9%
Excessive sweating 1.6% 0.6%
Genital discharge 1.3% 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.

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.



Evamist® spray (estradiol)

Dosage forms

Spray
  • Each spray contains 1.53 mg of estradiol
  • Comes in 8.1 ml spray bottle that delivers 56 sprays

Dosing

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

Generic / Price

  • No generic
  • 1 bottle - $$$

Other

  • Spray bottle should be primed 3 times before first use
  • Spray may be transferred through skin contact to other people. Cover application site after it dries.
  • Sunscreen applied 1 hour after Evamist may reduce absorption



Estrace® vaginal cream (estradiol)

Dosage forms

Vaginal cream
  • 0.01% cream
  • Comes in 42.5 gram tubes
  • Comes with applicator that delivers 1, 2, 3, and 4 gram doses

Dosing

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

Generic / Price

  • Generic available
  • 42.5 gram tube - $$$

Other

  • Estrace vaginal cream is absorbed systemically and therefore carries all the same risks of oral Estrace
  • The North American Menopause Society states that progesterone therapy is not necessary with low-dose vaginal estrogen therapy in women who have a uterus [4]

Premarin® vaginal cream (conjugated estrogens)

Dosage forms

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

Dosing

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)

Generic / Price

  • No generic
  • 30 gram tube - $$$$

Other

  • Premarin vaginal cream is absorbed systemically and therefore carries all the same risks of oral Premarin
  • Premarin vaginal cream may weaken latex barrier contraceptive methods (e.g. condom)
  • Premarin vaginal cream contains a mixture of conjugated estrogens blended to represent the estrogen content of a pregnant mares' urine
  • The North American Menopause Society states that progesterone therapy is not necessary with low-dose vaginal estrogen therapy in women who have a uterus [4]



Estring® (estradiol)

Dosage forms

Vaginal ring
  • Each ring contains 2 mg of estradiol

Dosing

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

Generic / Price

  • No generic
  • 1 ring - $$$$

Other

  • Systemic absorption of estradiol does occur
  • Estring may be expelled during bowel movement straining
  • Estring may not be suitable for women with narrow, short, or stenosed vaginas
  • Remove Estring if vaginal infection occurs and reinsert after infection clears
  • The North American Menopause Society states that progesterone therapy is not necessary with low-dose vaginal estrogen therapy in women who have a uterus [4]

Femring® (estradiol)

Dosage forms

Vaginal ring
  • 0.05 mg/day ring
  • 0.10 mg/day ring

Dosing

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

Generic / Price

  • No generic
  • 1 ring - $$$$

Other

  • Systemic absorption of estradiol does occur
  • Femring may not be suitable for women with narrow, short, or stenosed vaginas
  • Femring may be expelled during bowel movement straining
  • Femring may be left in place during local treatment of a vaginal infection
  • The North American Menopause Society states that progesterone therapy is not necessary with low-dose vaginal estrogen therapy in women who have a uterus [4]

Imvexxy® vaginal insert (estradiol)

Dosage forms

Vaginal insert
  • 4 mcg
  • 10 mcg
  • Comes in package of 18 inserts (starter pack) or 8 inserts (maintenance)

Dosing

Dyspareunia secondary to menopause
  • Dosing: Insert one daily at approximately the same time for 2 weeks, followed by one twice weekly, every three to four days (for example, Monday and Thursday)
  • Start with the 4 mcg dose and titrate to effect
  • Insert with the smaller end up for a depth of about two inches into the vaginal canal

Generic / Price

  • No generic
  • 8 inserts - $$$$

Other

  • Systemic absorption of estradiol may occur
  • The North American Menopause Society states that progesterone therapy is not necessary with low-dose vaginal estrogen therapy in women who have a uterus [4]

Vagifem® vaginal tablet (estradiol)

Dosage forms

Vaginal tablet
  • 10 mcg
  • Each tablet comes with single-use applicator

Dosing

Menopausal atrophic vaginitis
  • Dosing: 10 mcg tablet inserted intravaginally once daily for 2 weeks, followed by 1 tablet twice weekly (for example Tuesday and Friday)

Efficacy


Generic / Price

  • Generic available
  • 8 tablets - $$

Other

  • Systemic absorption of estradiol does occur
  • The North American Menopause Society states that progesterone therapy is not necessary with low-dose vaginal estrogen therapy in women who have a uterus [4]



Intrarosa® vaginal insert (prasterone)

Dosage forms

Vaginal insert
  • Each insert contains 6.5 mg of prasterone
  • Comes in box with 28 bullet-shaped inserts and applicator

Dosing

Moderate to severe dyspareunia
  • Administer one insert once daily at bedtime using the provided applicator

Generic / Price

  • No generic
  • 28 inserts - $$$$

Mechanism of action

  • Prasterone is also known as dehydroepiandrosterone (DHEA)
  • DHEA is a weak androgen produced by the adrenal glands. In certain tissues, it is converted into active metabolites of estrogen and testosterone. Its mechanism in treating dyspareunia is unknown.
  • Intrarosa is absorbed systemically and in pharmacokinetic studies, patients receiving Intrarosa had slight increases in estradiol and testosterone levels

Side effects

  • Vaginal discharge - vaginal discharge is the most frequently reported side effect of Intrarosa occurring in up to 14% of treated women
  • Abnormal PAP smear - in a 52-week trial (n=521) without a control group, 2.1% of women had an abnormal PAP smear

Drug interactions

  • None known

Contraindications

  • Undiagnosed abnormal genital bleeding - Any postmenopausal woman with undiagnosed, persistent or recurring genital bleeding should be evaluated to determine the cause of the bleeding before consideration of treatment with Intrarosa

Precautions

  • Breast cancer - estrogen is a metabolite of prasterone. Estrogen therapy is contraindicated in women with known or suspected breast cancer.
  • Kidney disease - has not been studied
  • Liver disease - has not been studied



Crinone® gel (progesterone)

Dosage forms

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

Dosing

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

Generic / Price

  • No generic
  • 6 applicators - $$$

Other

  • Do not administer other local vaginal products within 6 hours of Crinone gel
  • Small, white globules may appear as a vaginal discharge after usage



Aygestin® (norethindrone)

Dosage forms

Tablet
  • 5 mg

Dosing

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

Generic / Price

  • Generic available
  • 30 tablets - $

Other

  • Manufacturer makes no specific recommendation regarding food

Prometrium® (progesterone)

Dosage forms

Capsule
  • 100 mg
  • 200 mg

Dosing

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

Generic / Price

  • Generic available
  • 30 capsules - $$

Other

  • PATIENTS WITH PEANUT ALLERGY SHOULD NOT TAKE. Prometrium contains peanut oil.
  • Prometrium may cause dizziness and drowsiness. Take at bedtime.
  • Food increases absorption. Manufacturer makes no specific recommendation regarding food.

Provera® (medroxyprogesterone)

Dosage forms

Tablet
  • 2.5 mg
  • 5 mg
  • 10 mg

Dosing

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

Generic / Price

  • Generic available
  • 30 tablets - $

Other

  • Food increases absorption. Manufacturer makes no specific recommendation regarding food.



Estradiol + norethindrone | Activella® | Mimvey® | Lopreeza® | Amabelz®

Dosage forms

Tablet
  • Estradiol : Norethindrone
    • 0.5 mg : 0.1 mg
    • 1 mg : 0.5 mg

Dosing

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.

Generic / Price

  • Generic available
  • 28 tablets - $

Angeliq® (drospirenone + estradiol)

Dosage forms

Tablet
  • Drospirenone : Estradiol
    • 0.25 mg : 0.5 mg
    • 0.5 mg : 1.0 mg

Dosing

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

Generic / Price

  • No generic
  • 28 tablets - $$$$

Other

  • Angeliq contains drospirenone which has antialdosterone activity. Hyperkalemia may occur in susceptible patients and with certain medications.
  • See drospirenone below for more

Bijuva® (estradiol + progesterone)

Dosage forms

Capsules
  • Each capsule contains estradiol 1 mg and progesterone 100 mg

Dosing

Menopausal vasomotor symptoms
  • Dosing: One capsule every evening with food
  • Food increases the absorption of progesterone

Generic / Price

  • No generic
  • 30 capsules - $$$$

Duavee® (conjugated estrogens + bazedoxifene)

Dosage forms

Tablet
  • Conjugated estrogens : Bazedoxifene
    • 0.45 mg : 20 mg

Dosing

Menopausal vasomotor symptoms
  • Dosing: 1 tablet once daily
  • 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 SERM activity table for more.
Prevention of postmenopausal osteoporosis
  • Dosing: 1 tablet once daily
  • 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 SERM activity table for more.

Generic / Price

  • No generic
  • 30 tablets - $$$$

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]

Side effects


Side effect Duavee Placebo
Muscle spasm 9% 6%
Nausea 8% 5%
Diarrhea 8% 5%
Upper abdominal pain 7% 5%
Dizziness 5% 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.

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 below)

Femhrt® | Jevantique® | Fyavolv® | Jinteli® (norethindrone + ethinyl estradiol)

Dosage forms

Tablet
  • Norethindrone : Ethinyl estradiol
    • 0.5 mg : 2.5 mcg (Femhrrt, Fyavolv, Jevantique Lo)
    • 1 mg : 5 mcg (Femhrt, Fyavolv, Jinteli, Jevantique)

Dosing

Menopausal vasomotor symptoms
  • Dosing: 1 tablet once daily
Prevention of postmenopausal osteoporosis
  • Dosing: 1 tablet once daily

Generic / Price

  • Generic available
  • 28 tablets - $

Prefest® (estradiol + norgestimate)

Dosage forms

Tablet
  • Prefest comes in a blister pack that alternates between 3 peach tablets and 3 white tablets
  • Each peach tablet contains estradiol 1 mg and each white tablet contains estradiol 1 mg / norgestimate 0.09 mg
  • The 3-day phases are alternated continuously during treatment

Dosing

Menopausal vasomotor symptoms and/or vulvar and vaginal atrophy
  • Dosing: 1 tablet once daily
Prevention of postmenopausal osteoporosis
  • Dosing: 1 tablet once daily

Generic / Price

  • No generic
  • 30 tablets - $$$$

Premphase® (conjugated estrogens + medroxyprogesterone)

Dosage forms

Tablet
  • 14 maroon tablets: 0.625 mg of conjugated estrogens
  • 14 light-blue tablets: 0.625 mg of conjugated estrogens + 5 mg medroxyprogesterone

Dosing

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

Generic / Price

  • No generic
  • 28 tablets - $$$$

Prempro® (conjugated estrogens + medroxyprogesterone)

Dosage forms

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

Dosing

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

Generic / Price

  • No generic
  • 28 tablets - $$$$



Climara Pro® (estradiol + levonorgestrel)

Dosage forms

Patch
  • Each patch delivers 0.045 mg/day of estradiol and 0.015 mg/day of levonorgestrel
  • Comes in carton of 4 patches

Dosing

Menopausal vasomotor symptoms
  • Dosing: one patch once weekly
Prevention of postmenopausal osteoporosis
  • Dosing: one patch once weekly

Generic / Price

  • No generic
  • 4 patches - $$$$

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

Combipatch® (estradiol + norethindrone)

Dosage forms

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

Dosing

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.

Generic / Price

  • No generic
  • 8 patches - $$$

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



  • 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
Estrogen side effects
Side effect Premarin 0.625 mg/day Placebo
Vaginal hemorrhage 13% 0%
Abdominal pain 11% 6%
Breast pain 11% 8%
Flatulence 6% 2%
Endometrial hyperplasia 5% 0%
Vaginitis 5% 0%
Weakness 5% 1%
Back pain 5% 1%
White or yellow vaginal discharge 5% 2%
Yeast infection 4% 2%
Metrorrhagia (menstrual bleeding at irregular intervals) 3% 0%
Uterine spasm 3% 1%
Pelvic pain 3% 1%
Leg cramps 3% 1%
Itching 3% 1%
Dysmenorrhea (painful menses) 3% 1%
Cervix disorder 2% 0%






























  • References [PMID 25423325, PMID 25210448, PMID 10874566]
SERM ACTIVITY TABLE
SERM Product Endometrium Vagina Breast Bone
formation
Hypothalamus
Bazedoxifene Duavee® Neutral to
Antagonist
No data Neutral to
Antagonist
Agonist ?
Clomiphene Clomid® Antagonist ? ? Agonist Antagonist
Ospemifene Osphena® Neutral to
Partial agonist
Agonist Antagonist Agonist ?
Raloxifene Evista® Neutral to
Partial agonist
Neutral Antagonist Agonist ?
Tamoxifen Nolvadex® Neutral to
Agonist
Agonist Antagonist Agonist ?






Pricing legend
  • $ = 0 - $50
  • $$ = $51 - $100
  • $$$ = $101 - $150
  • $$$$ = > $151
  • Pricing based on one month of therapy at standard dosing in an adult
  • Pricing based on information from GoodRX.com®
  • Pricing may vary by region and availability