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noretynodrel and estrogen

G03FA09

Forms & Strengths

Combination oral contraceptive: Norethynodrel 5 mg to 9.85 mg with mestranol 0.075 mg to 0.15 mg (historical/legacy formulations)

Adult Dosing

Contraception: 1 tablet daily starting on day 5 of the menstrual cycle for 20 days, followed by 7 days off or placebo (historical regimen)

Pediatric Dosing

Safety and efficacy established only after menarche
Post-menarche adolescent females: Same as adult dosing

Indications

Prevention of pregnancy (historical first combined oral contraceptive)
Treatment of hypermenorrhea and endometriosis (historical)

Mechanism of Action

Suppression of gonadotropins (FSH and LH) via estrogen and progestin feedback
Inhibition of ovulation
Alteration of cervical mucus to impede sperm penetration
Modification of the endometrium to prevent implantation

Contraindications

Known or suspected pregnancy
Active thrombophlebitis or thromboembolic disorders
History of deep vein thrombosis or pulmonary embolism
Cerebrovascular or coronary artery disease
Known or suspected carcinoma of the breast or estrogen-dependent neoplasia
Undiagnosed abnormal genital bleeding
Hepatic tumor or active liver disease
Hypersensitivity to any component

Adverse Reactions

Venous thromboembolism and arterial thrombosis
Hypertension
Nausea, vomiting, abdominal cramps
Breakthrough bleeding, spotting, amenorrhea
Breast tenderness, enlargement, or secretion
Headache, migraine, dizziness
Weight changes, edema
Melasma, rash

Drug Interactions

CYP3A4 inducers (e.g., rifampin, barbiturates, carbamazepine, phenytoin) decrease contraceptive efficacy
CYP3A4 inhibitors (e.g., ketoconazole, erythromycin) may increase plasma hormone levels
Anticoagulants: Efficacy of anticoagulant therapy may be altered
Antidiabetic agents: Estrogens may raise blood glucose, requiring dosage adjustment
Lamotrigine: Hormonal contraceptives may decrease plasma concentrations

Curated Content: Needs Vetting Before Put to Clinical Use