HAILEY 1.5/30
Clinical safety rating
cautionComprehensive clinical and safety monograph for HAILEY 1.5/30 (HAILEY 1.5/30).
Combination oral contraceptive containing ethinyl estradiol and desogestrel. Ethinyl estradiol suppresses gonadotropin release via negative feedback on the hypothalamic-pituitary axis; desogestrel, a progestin, inhibits ovulation and alters cervical mucus and endometrial receptivity.
| Metabolism | Ethinyl estradiol undergoes hepatic metabolism primarily via CYP3A4; desogestrel is rapidly metabolized to its active metabolite etonogestrel via hydroxylation and dehydrogenation, further metabolized via CYP2C9 and CYP3A4. |
| Excretion | Approximately 40% renal (as metabolites), 32% fecal (as metabolites), and <1% unchanged in urine. |
| Half-life | Terminal elimination half-life of ethinyl estradiol is 13-27 hours (mean 17 hours); for norgestimate, active metabolite norelgestromin has half-life 12-30 hours (mean 19 hours). Steady state reached after 7-14 days. |
| Protein binding | Ethinyl estradiol: ~98% bound to albumin; norelgestromin: ~99% bound to albumin and SHBG. |
| Volume of Distribution | Ethinyl estradiol: 2.3-4.0 L/kg; norelgestromin: 2.0-3.5 L/kg. Indicates extensive tissue distribution. |
| Bioavailability | Oral: Ethinyl estradiol 40-55% (first-pass metabolism); norelgestromin: ~80% (as metabolite of norgestimate). |
| Onset of Action | Oral: Contraceptive effect begins after 7 days of continuous dosing; maximum effect after 1 cycle. |
| Duration of Action | Contraceptive protection persists for 24 hours per daily dose; missed doses >24 hours increase pregnancy risk. |
| Molecular Weight | Ethinyl estradiol: 296.4 Da; Levonorgestrel: 312.4 Da |
| Action Class | Oral Contraceptive; Estrogen/Progestin Combination |
One tablet (ethinyl estradiol 0.03 mg, levonorgestrel 0.15 mg) orally once daily at the same time each day for 21 days, followed by 7 placebo tablets. For continuous cycling, may take active tablets daily without placebo.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. Not studied in severe impairment, but estrogen metabolites may accumulate; use caution. |
| Liver impairment | Contraindicated in acute liver disease or severe hepatic impairment (Child-Pugh C). For mild to moderate (Child-Pugh A or B), use is not recommended due to altered hormone clearance; if used, monitor liver function and consider lower estrogen dose. |
| Pediatric use | Postmenarchal adolescents: Same adult dosing (one tablet daily). Safety and efficacy not established in premenarchal girls. |
| Geriatric use | Not indicated for postmenopausal women; contraindicated after menopause due to increased risk of cardiovascular events. No specific geriatric dose. |
| 1st trimester | Contains ethinyl estradiol 30 mcg and levonorgestrel 150 mcg. Contraindicated during pregnancy. Use in T1 is associated with a very low risk of teratogenicity based on large cohort studies; however, recommended to discontinue if pregnancy is suspected. |
| 2nd trimester | Contraindicated. Estrogens may feminize male fetus; progestins may cause ambiguous genitalia. Not indicated for use during pregnancy. |
| 3rd trimester | Contraindicated. Possible risk of liver dysfunction, jaundice, and other adverse effects in the neonate. Discontinue if pregnancy occurs. |
Clinical note
Comprehensive clinical and safety monograph for HAILEY 1.5/30 (HAILEY 1.5/30).
| Placental transfer | Both components cross the placenta; ethinyl estradiol has limited transfer, levonorgestrel readily crosses. |
| Breastfeeding | Combined hormonal contraceptives may reduce milk production and quality, especially in early postpartum period. Small amounts of steroids are excreted in breast milk. Consider alternative contraception if breastfeeding. |
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | FDA Pregnancy Category X. Combined hormonal contraceptives (CHCs) are contraindicated in pregnancy. First trimester exposure is associated with a low risk of fetal malformations; however, CHCs should be discontinued if pregnancy occurs. Second and third trimester exposure may increase risks of fetal adverse outcomes, including but not limited to congenital anomalies and fetal demise. Use is not recommended at any trimester. |
| Fetal Monitoring | Monitor blood pressure monthly, assess for thromboembolic symptoms (leg pain, chest pain, dyspnea), monitor liver function and signs of hepatic adenoma. Rule out pregnancy before initiation and at any missed menses. No specific fetal monitoring required if pregnancy occurs; standard prenatal care advised. |
| Fertility Effects | CHCs prevent ovulation and implantation; fertility returns promptly after discontinuation. No permanent adverse effects on fertility. Post-use, normal ovulatory cycles typically resume within 1-3 months. |
■ FDA Black Box Warning
Cigarette smoking increases the risk of serious cardiovascular side effects from combination oral contraceptive use. This risk increases with age and with heavy smoking (15 or more cigarettes per day) and is quite marked in women over 35 years of age. Women who use combination oral contraceptives should be strongly advised not to smoke.
| Common Effects | Nausea, 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, Cerebrovascular accident, Retinal thrombosis |
Thrombophlebitis or thromboembolic disordersCerebrovascular or coronary artery diseaseKnown or suspected pregnancyLiver adenoma, carcinoma, or significant liver diseaseUndiagnosed abnormal genital bleedingKnown or suspected breast cancerHypersensitivity to any component
| Precautions | Increased risk of thromboembolic disorders, Cigarette smoking increases cardiovascular risk, Elevated blood pressure, Gallbladder disease, Hepatic neoplasia, Carbohydrate and lipid effects, Ocular lesions, Headache/migraine, Bleeding irregularities, Depression |
| Food/Dietary | No significant food interactions. Grapefruit juice may slightly increase estrogen levels but not clinically relevant. A high-fat meal may delay absorption but does not reduce efficacy. Avoid excessive alcohol as it may increase liver enzymes and theoretically reduce efficacy. |
| Clinical Pearls | HAILEY 1.5/30 is a combination oral contraceptive containing ethinyl estradiol 30 mcg and levonorgestrel 1.5 mg. It is a monophasic pill with 21 active tablets. Counsel patients that missed pills increase pregnancy risk, especially if more than one active pill is missed. Use back-up contraception for 7 days if a dose is missed. Consider increased risk of venous thromboembolism (VTE) in smokers over 35, obese patients, or those with thrombophilia. Nausea may be reduced by taking with food or at bedtime. Spotting is common in first 3 cycles; if persistent, rule out pregnancy or other causes. |
| Patient Advice | Take one pill daily at the same time for 21 days, then 7 placebo pills. · If you miss a pill, follow the package insert instructions for missed doses and use back-up contraception (e.g., condoms) for 7 days. · Do not smoke while taking this medication, especially if over age 35, due to increased risk of blood clots. · Common side effects include nausea, breast tenderness, and spotting, which usually improve after 3 cycles. · Seek immediate medical attention for symptoms of blood clots: sudden leg pain/swelling, chest pain, shortness of breath, or severe headache. · Antibiotics (except rifampin) do not reduce effectiveness; however, certain drugs like rifampin, griseofulvin, and some anticonvulsants may decrease efficacy. · Store at room temperature, away from moisture and heat. |
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