Drug intelligence / Profile preview

medroxyprogesterone acetate + estradiol

Development stage
Phase 2
Lead developer
World Health Organization
Modality
Small Molecules
Administration
Intramuscular
01

Overview

Medroxyprogesterone acetate + estradiol is a combination hormonal medication primarily used for contraception and hormone replacement therapy. This combination contains two key components: medroxyprogesterone acetate (a synthetic form of progesterone) and estradiol (a form of estrogen)[4][2]. ## Formulations and Administration The medication is typically administered as an intramuscular injection on a monthly basis[2][4]. The standard dosage for contraception is 0.5 mL containing 5 mg estradiol cypionate (EC) and 25 mg medroxyprogesterone acetate (MPA)[4]. For contraceptive purposes, the first injection should be given within the first 5 days of a normal menstrual period, within 5 days of a complete abortion, or 4-6 weeks postpartum depending on breastfeeding status[2]. ## Mechanism of Action As a contraceptive, this combination works primarily by preventing ovulation[3]. The hormones stop a woman's egg from fully developing each month, making it unable to accept sperm and thus preventing fertilization[3]. The medication also causes changes in cervical mucus and the uterine lining, making it harder for sperm to reach the uterus and for a fertilized egg to attach to the uterus[2]. ## Medical Uses The primary uses of medroxyprogesterone acetate + estradiol include: 1. **Contraception**: Effective as a once-monthly injectable birth control method[2][4] 2. **Hormone Replacement Therapy**: Used to treat menopausal symptoms such as hot flashes, vaginal dryness, and other symptoms associated with menopause[1][7] 3. **Prevention of Osteoporosis**: Helps prevent bone loss in postmenopausal women[1][7] ## Brand Names This combination has been marketed under several brand names including: - Lunelle (in the United States)[2][3][4] - Cyclofem (internationally)[4] ## Side Effects and Risks Common side effects include: - Irregular menstrual periods (typically improves with time)[4] - Headaches[4] - Hair loss[4] - Depression[4] - Nausea[4] - Breast pain[4] More serious risks include: - Blood clots[2][4][7] - Stroke or heart attack, especially in smokers over 35[2][7] - Potential increased risk of certain cancers[3] ## Contraindications This medication should not be used in individuals with: - Pregnancy or recent childbirth[2][4] - History of stroke or blood clots[2][7] - Circulation problems, especially if caused by diabetes[2] - Hormone-related cancers such as breast or uterine cancer[2][7] - Abnormal vaginal bleeding[2][7] - Liver disease or liver cancer[2][7] - Severe high blood pressure[2] - Migraine headaches with aura[2] - Heart valve disorders[2] ## Current Status While this combination was approved for use in the United States in 2000, it is no longer commercially available there[4]. However, it remains approved for use in 18 countries worldwide, including Mexico, Thailand, and Indonesia[4].

Brand names
LunelleCyclofemCyclo-ProveraHRP-112HRP112HRP 112
Other names
EC/MPAEstradiol cypionate/medroxyprogesterone acetate
02

Targets

PR (Progesterone receptor)ESR1 (ERα)GR (Glucocorticoid receptor)ESR2 (ERβ)AR (Adrenergic receptors)

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