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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, fixed combinations
progesterone and estrogen
G03FA04
Forms & Strengths
- Tablets: 0.5mg estradiol/0.1mg norethindrone, 0.5mg estradiol/0.2mg norethindrone, 1mg estradiol/0.5mg norethindrone
- Patches: 0.025mg estradiol/0.0025mg levonorgestrel, 0.05mg estradiol/0.0025mg levonorgestrel
- Vaginal rings: 0.015mg estradiol/0.02mg etonogestrel
- Injectables: 1mg estradiol cypionate/10mg medroxyprogesterone
- Oral solutions: 0.625mg conjugated estrogens/2.5mg medroxyprogesterone
Adult Dosing
- Menopausal symptoms: 0.3-1.25mg conjugated estrogens + 1.5-5mg medroxyprogesterone for 3 weeks on, 1 week off
- Contraception: 0.02-0.035mg ethinyl estradiol + 0.1-0.25mg levonorgestrel daily
- Hormone replacement therapy: 0.025-0.1mg transdermal estradiol twice weekly, + 2.5-5mg oral medroxyprogesterone for 12-14 days
- Dysmenorrhea: 0.02-0.1mg ethinyl estradiol + 0.1-2mg norethindrone daily for 20 days
Pediatric Dosing
- Contraception: not for use in children under 16 years, for 16-17 years individualize dose
- Primary ovarian insufficiency: not established, do not use before menarche
Indications
- Moderate-to-severe menopausal vasomotor symptoms
- Prevention of osteoporosis in postmenopausal women
- Treatment of vulvar and vaginal atrophy in postmenopausal women
- Contraception
- Primary ovarian insufficiency
Mechanism of Action
- Estrogen component: binds to estrogen receptors to stimulate growth and maintenance of female reproductive tissues
- Progestin component: opposes estrogen-induced stimulation of the endometrium, preventing endometrial hyperplasia
- Regulation of gonadotropins to prevent follicular maturation and ovulation in contraception
Contraindications
- Undiagnosed abnormal uterine bleeding
- Known or suspected estrogen-dependent neoplasia
- Known liver tumors or active liver disease
- Pregnancy or breastfeeding
- History of thrombophlebitis, thromboembolic disorders, or severe hypertension
Adverse Reactions
- Nausea and vomiting
- Breast tenderness and discharge
- Irregular vaginal bleeding
- Thromboembolic events
- Cholestatic jaundice
- Migraine
- Fluid retention
- Increased risk of endometrial cancer with unopposed estrogen use
Drug Interactions
- Inducers of CYP3A4 (e.g., rifampin) decrease estrogen and progestin levels
- Inhibitors of CYP3A4 (e.g., ketoconazole) increase estrogen and progestin levels
- Barbiturates, phenytoin, carbamazepine, and other hepatic enzyme inducers may decrease effectiveness
- Concomitant use of grapefruit juice may increase levels
Curated Content: Needs Vetting Before Put to Clinical Use