HAILEY FE 1/20
Clinical safety rating
cautionComprehensive clinical and safety monograph for HAILEY FE 1/20 (HAILEY FE 1/20).
Combination oral contraceptive containing ethinyl estradiol and norethindrone. Suppresses gonadotropin (FSH and LH) release via negative feedback on the hypothalamic-pituitary-ovarian axis, inhibiting ovulation. Also alters cervical mucus and endometrial lining to impair sperm penetration and implantation.
| Metabolism | Ethinyl estradiol is primarily metabolized via CYP3A4 hydroxylation and conjugation (glucuronidation/sulfation). Norethindrone is metabolized by reduction, hydroxylation, and conjugation, primarily via CYP3A4. |
| Excretion | Renal (approximately 50-60% as metabolites, including glucuronide conjugates of ethinyl estradiol and norethindrone, and about 20% as unchanged norethindrone); Fecal (approximately 30-40% as metabolites); Biliary (minor, with enterohepatic circulation of ethinyl estradiol conjugates). |
| Half-life | Ethinyl estradiol: approximately 17 ± 5 hours (terminal); Norethindrone: approximately 8 ± 2 hours (terminal). Clinical context: Steady-state reached within 7-10 days; once-daily dosing maintains effective concentrations for contraceptive efficacy. |
| Protein binding | Ethinyl estradiol: approximately 97-98% bound to albumin (primarily) and sex hormone-binding globulin (SHBG); Norethindrone: approximately 93-95% bound to albumin and SHBG. |
| Volume of Distribution | Ethinyl estradiol: approximately 2-4 L/kg; Norethindrone: approximately 4-6 L/kg. Clinical meaning: Extensive tissue distribution, with accumulation in adipose tissue and reproductive organs. |
| Bioavailability | Oral: Ethinyl estradiol ~40-45% (first-pass metabolism); Norethindrone ~60-65% (first-pass metabolism). |
| Onset of Action | Oral: Contraceptive effect begins after 7 consecutive daily doses; peak serum concentrations of ethinyl estradiol and norethindrone occur at 1-2 hours post-dose. |
| Duration of Action | Oral: 24-hour dosing interval; contraceptive protection maintained with consistent daily dosing; missed doses increase pregnancy risk. |
| Molecular Weight | Ethinyl estradiol: 296.40 Da; Norethindrone: 298.42 Da |
| Action Class | Estrogen-progestin combination oral contraceptive |
One tablet orally once daily for 21 consecutive days followed by 7 days of placebo tablets.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. Contraindicated in severe renal impairment or acute renal failure due to risk of hyperkalemia. |
| Liver impairment | Contraindicated in patients with active liver disease or Child-Pugh class B or C cirrhosis. For Child-Pugh class A, use with caution and monitor liver function. |
| Pediatric use | Not indicated for use before menarche. For post-menarchal adolescents, same dosing as adults: one tablet orally once daily for 21 days, then 7 days of placebo. |
| Geriatric use | Not indicated for use in postmenopausal women. No specific geriatric dosing adjustments; consider increased risk of thromboembolic events and cardiovascular disease. |
| 1st trimester | Hailey FE 1/20 is contraindicated in pregnancy due to risk of fetal harm. Use during first trimester is not recommended; however, large epidemiological studies have not found an increased risk of birth defects with oral contraceptive use prior to conception or early pregnancy. |
| 2nd trimester | Use during second trimester is contraindicated. Oral contraceptives should be discontinued if pregnancy is suspected or confirmed. |
| 3rd trimester | Use during third trimester is contraindicated. There is a potential risk of feminization of male fetuses and other adverse effects on fetal development. Additionally, hormonal contraceptives may affect lactation. |
Clinical note
Comprehensive clinical and safety monograph for HAILEY FE 1/20 (HAILEY FE 1/20).
| Placental transfer | Ethinyl estradiol and norethindrone cross the placenta. Studies have shown detectable levels in fetal tissues and cord blood after maternal administration. |
| Breastfeeding | Hailey FE 1/20 contains ethinyl estradiol and norethindrone. Estrogens and progestins are excreted in human milk in small amounts. Use during breastfeeding may reduce milk production and alter milk composition. The American Academy of Pediatrics considers combined oral contraceptives compatible with breastfeeding after postpartum day 21, but progestin-only contraceptives are preferred. Caution is advised, especially in early postpartum period. |
| Lactation Rating | L3 - Limited data, potential adverse effects; use with caution. |
| Teratogenic Risk | First trimester: No increased risk of major birth defects in large epidemiological studies. Second and third trimesters: Use is not recommended due to potential adverse effects on fetal development, including possible estrogenic effects and association with congenital anomalies in animal studies. Fetal risk cannot be ruled out. |
| Fetal Monitoring | Monitor blood pressure, glucose tolerance, and liver function. Assess for symptoms of depression, jaundice, and thromboembolic events. No specific fetal monitoring required, but discuss risks with pregnant women. |
| Fertility Effects | No known permanent effects on fertility. Return to fertility may be delayed after discontinuation; normal menstrual cycles typically resume within 1-3 months. |
■ FDA Black Box Warning
Cigarette smoking increases risk of serious cardiovascular events (e.g., stroke, myocardial infarction, thromboembolism) from combination oral contraceptives. Risk increases with age (>35 years) and heavy smoking (≥15 cigarettes/day). Women who are >35 years old and smoke should not use this product.
| Common Effects | Nausea, Vomiting, Headache, Breast tenderness, Weight changes, Irregular menstrual bleeding, Mood changes, Acne |
| Serious Effects | Venous thromboembolism (deep vein thrombosis, pulmonary embolism), Arterial thromboembolism (myocardial infarction, stroke), Hepatic adenoma or hepatocellular carcinoma, Hypertension, Gallbladder disease, Cholestatic jaundice, Optic neuritis or retinal thrombosis |
Known or suspected pregnancyCurrent or past history of thrombophlebitis or thromboembolic disordersCerebrovascular or coronary artery diseaseKnown or suspected carcinoma of the breast or endometriumUndiagnosed abnormal genital bleedingCholestatic jaundice of pregnancy or jaundice with prior oral contraceptive useHepatic adenoma or carcinomaActive liver disease with abnormal liver functionKnown hypersensitivity to any component of the productHeavy smoking (≥15 cigarettes per day) and age ≥35 years
| Precautions | Increased risk of thrombotic disorders including venous thromboembolism, stroke, and myocardial infarction., Discontinue if sudden partial or complete loss of vision or onset of proptosis, diplopia, migraine., Elevated blood pressure; use caution in hypertension., Gallbladder disease; increased risk of gallstones., Carbohydrate and lipid metabolism effects; use caution in diabetes and hyperlipidemia., Hepatic neoplasia; discontinue if jaundice or liver dysfunction., Chloasma; avoid sun or UV exposure., Bleeding irregularities; may cause breakthrough bleeding and spotting., Possible decreased efficacy with concomitant enzyme-inducing drugs. |
| Food/Dietary | No specific food interactions. Grapefruit juice may increase estrogen levels; avoid excessive consumption. St. John's Wort may reduce efficacy. Consistent intake with or without food is recommended to maintain steady-state levels. |
| Clinical Pearls | Contains ethinyl estradiol 20 mcg and norethindrone 1 mg. Consider lower estrogen dose for patients with estrogen-sensitive migraines or history of thromboembolism. Monitor for breakthrough bleeding, especially in first 3 cycles. CYP3A4 inducers like rifampin may reduce efficacy. Check pregnancy test before initiating if delayed menses. Use with caution in patients with hypertriglyceridemia. |
| Patient Advice | Take one tablet daily at the same time, in the order listed on the pack. · If you miss a dose, take it as soon as remembered; if more than 24 hours late, use backup contraception. · Common side effects: nausea, breast tenderness, spotting, and headache. · Report signs of blood clots: sudden leg pain, chest pain, or shortness of breath. · Smoking increases risk of serious cardiovascular side effects, especially if over 35 years old. · Antibiotics (except rifampin) do not reduce effectiveness; inform your provider about all medications. |
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