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GENITO URINARY SYSTEM AND SEX HORMONES › SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM › PROGESTOGENS AND ESTROGENS IN COMBINATION › Progestogens and estrogens, sequential preparations
medroxyprogesterone and estrogen
G03FB06
Forms & Strengths
- Oral tablet: 1.5 mg medroxyprogesterone acetate / 0.03 mg ethinyl estradiol
- Oral tablet: 2.5 mg medroxyprogesterone acetate / 0.05 mg ethinyl estradiol
- Oral tablet: 5 mg medroxyprogesterone acetate / 0.025 mg conjugated estrogens
- Oral tablet: 2.5 mg medroxyprogesterone acetate / 0.625 mg conjugated estrogens
- Oral tablet: 5 mg medroxyprogesterone acetate / 0.625 mg conjugated estrogens
Adult Dosing
- Vasomotor symptoms / Postmenopausal therapy: 1 tablet (conjugated estrogens/medroxyprogesterone acetate 0.625/2.5 mg or 0.625/5 mg) orally once daily continuously
- Secondary amenorrhea: 2.5 mg to 10 mg medroxyprogesterone daily for 10 days with estrogen therapy
- Contraception: 1 tablet (ethinyl estradiol/medroxyprogesterone) orally once daily according to 28-day regimen
Pediatric Dosing
- Not indicated for pediatric use
- Safety and efficacy not established in pre-menarchal pediatric patients
Indications
- Treatment of moderate to severe vasomotor symptoms associated with menopause in women with an intact uterus
- Treatment of vulvar and vaginal atrophy associated with menopause
- Prevention of postmenopausal osteoporosis in women with an intact uterus
- Combination formulations used for oral contraception in select regions
Mechanism of Action
- Estrogen binds to nuclear receptors, promoting hepatic synthesis of transport proteins, clotting factors, and decreasing bone resorption
- Progestin (medroxyprogesterone) transforms proliferative endometrium into secretory endometrium
- Combined therapy reduces the risk of endometrial hyperplasia and carcinoma induced by unopposed estrogen in women with a uterus
Contraindications
- Known or suspected pregnancy
- Undiagnosed abnormal genital bleeding
- Known, suspected, or history of breast cancer
- Known or suspected estrogen- or progestin-dependent neoplasia
- Active deep vein thrombosis, pulmonary embolism, or history of these conditions
- Active or recent arterial thromboembolic disease (e.g., stroke, myocardial infarction)
- Liver dysfunction or disease
- Known hypersensitivity to any of the components
Adverse Reactions
- Breast tenderness and enlargement
- Breakthrough bleeding, spotting, or changes in menstrual flow
- Headache and migraine
- Nausea, abdominal cramps, bloating
- Edema and weight changes
- Thromboembolism (DVT, PE, stroke, myocardial infarction)
- Gallbladder disease
- Hypertension
- Elevated risk of breast cancer and probable dementia with long-term use in older women
Drug Interactions
- CYP3A4 inducers (e.g., rifampin, carbamazepine, St. John's wort) decrease estrogen and progestin concentrations and efficacy
- CYP3A4 inhibitors (e.g., erythromycin, ketoconazole) may increase plasma concentrations
- Anticoagulants: Estrogens may diminish the efficacy of anticoagulant therapy
- Insulin and oral hypoglycemics: Hormone therapy may impair glucose tolerance, requiring dosage adjustment
- Thyroid hormone replacement: Estrogen increases thyroid-binding globulin, potentially increasing the need for thyroid hormone
Curated Content: Needs Vetting Before Put to Clinical Use