ALTAVERA
Clinical safety rating
cautionComprehensive clinical and safety monograph for ALTAVERA (ALTAVERA).
Combination of ethinyl estradiol and desogestrel: ethinyl estradiol suppresses gonadotropin release, inhibiting ovulation; desogestrel (progestin) causes cervical mucus thickening and endometrial atrophy, preventing implantation.
| Metabolism | Ethinyl estradiol: primarily metabolized by CYP3A4; undergoes sulfation and glucuronidation. Desogestrel: rapidly converted to active metabolite etonogestrel via CYP2C9 and CYP2C19; further metabolism by CYP3A4. |
| Excretion | Renal excretion of metabolites and unchanged drug: ~30% (levonorgestrel) and ~20% (ethinyl estradiol) in urine; biliary/fecal elimination: ~40-50% as conjugates and metabolites. |
| Half-life | Levonorgestrel: terminal elimination half-life 25±10 hours; ethinyl estradiol: 13±7 hours. Clinical context: steady-state concentrations achieved within 5-7 days; contraceptive efficacy requires consistent daily dosing. |
| Protein binding | Levonorgestrel: 98-99% bound to sex hormone-binding globulin (SHBG) and albumin; ethinyl estradiol: 98% bound to albumin. |
| Volume of Distribution | Levonorgestrel: Vd ~1.8 L/kg (suggesting extensive tissue distribution). Ethinyl estradiol: Vd ~2.4 L/kg. |
| Bioavailability | Oral bioavailability: levonorgestrel ~100% (nearly complete); ethinyl estradiol ~45-50% (first-pass hepatic metabolism). |
| Onset of Action | Oral: inhibition of ovulation begins within 1-2 days of first tablet; full contraceptive effect after 7 consecutive days (if started within 5 days of menses). |
| Duration of Action | 24-hour dosing interval; contraceptive protection lasts for entire cycle if taken daily. Missed dose requires backup contraception for 7 days. |
| Molecular Weight | Ethinyl estradiol: 296.4 Da; Levonorgestrel: 312.4 Da |
1 tablet (ethinyl estradiol 0.03 mg / levonorgestrel 0.15 mg) orally once daily for 21 days, followed by 7 placebo days.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. Contraindicated in severe renal disease or acute renal failure due to potential fluid retention. |
| Liver impairment | Contraindicated in severe hepatic dysfunction (Child-Pugh class B or C). Use caution in mild to moderate impairment (Child-Pugh A); monitor liver enzymes. |
| Pediatric use | Not indicated for use before menarche. For postmenarchal adolescents, same dosing as adults (1 tablet daily, 21/7 regimen) after evaluation of risks. |
| Geriatric use | Not indicated for postmenopausal women. No specific geriatric dosing; consider increased risk of thromboembolism, cardiovascular disease, and metabolic effects in older women of reproductive age. |
| 1st trimester | Contraindicated due to risk of fetal harm; oral contraceptive use in early pregnancy associated with congenital anomalies. |
| 2nd trimester | Not recommended; continued use may affect fetal development, but evidence of major malformations is limited. |
| 3rd trimester | Avoid; may increase risk of neonatal complications such as jaundice and fluid imbalance. |
Clinical note
Comprehensive clinical and safety monograph for ALTAVERA (ALTAVERA).
| Placental transfer | Both ethinyl estradiol and levonorgestrel cross the human placenta with transfer ratios approximately 50% for levonorgestrel. |
| Breastfeeding | Small amounts of ethinyl estradiol and levonorgestrel are excreted into breast milk; use may reduce milk production and composition. Use only if benefits outweigh risks. |
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | ALTAVERA contains ethinyl estradiol and levonorgestrel. First trimester: Inadvertent exposure during organogenesis is associated with a very low absolute risk of cardiovascular defects (relative risk 1.2-1.4) and no consistent increase in other major malformations. Second and third trimesters: No known teratogenic effects, but theoretical risks from estrogenic effects (e.g., feminization of male fetus). Postnatal: No increased risk of long-term developmental effects from pregnancy exposure. |
| Fetal Monitoring | Monitor blood pressure at each visit, assess for signs of thrombosis, and perform liver function tests if symptoms of hepatic dysfunction. In pregnancy, routine fetal ultrasound for anatomy (if exposure in first trimester). No specific fetal monitoring indicated beyond standard prenatal care. |
| Fertility Effects | Reversible suppression of ovulation. Fertility returns promptly (within 1-3 cycles) after discontinuation. No evidence of permanent impairment or delayed conception. Long-term use does not increase risk of infertility. |
■ FDA Black Box Warning
Cigarette smoking increases risk of serious cardiovascular events from combined oral contraceptives. Risk increases with age (especially >35 years) and with number of cigarettes smoked. Women who use combined hormonal contraceptives should be strongly advised not to smoke.
| Serious Effects |
Known or suspected pregnancyHistory of thromboembolic disorders or strokeCurrent or past history of breast cancer or other estrogen-sensitive neoplasiaActive liver disease or impaired liver functionUncontrolled hypertension (>160/100 mmHg)Migraine with aura, especially in women over 35 years
| Precautions | Thrombotic disorders: risk of venous thromboembolism (VTE), stroke, myocardial infarction; discontinue if thrombotic event occurs., Hepatic disease: discontinue if jaundice or liver function abnormalities develop., Hypertension: monitor blood pressure; discontinue if uncontrolled., Carbohydrate metabolism: may affect glucose tolerance; monitor diabetic patients., Depression: discontinue if significant depression occurs., Gallbladder disease: increased risk of cholelithiasis. |
| Food/Dietary | No significant food interactions. Alcohol does not affect efficacy but may increase risk of adverse effects such as nausea. Grapefruit juice has no known interaction. Avoid excessive alcohol consumption due to potential hepatotoxicity. |
| Clinical Pearls | ALTAVERA is a combined oral contraceptive (COC) containing ethinylestradiol and levonorgestrel. It inhibits ovulation via suppression of gonadotropins. Counsel patients to take at the same time daily to maintain efficacy. Missed pill management: if missed within 12 hours, take immediately; if >12 hours, take last missed pill and use backup contraception for 7 days. Be aware of increased VTE risk, especially in smokers over 35. May reduce effectiveness of lamotrigine; monitor seizure control. Initiate on the first day of menses or first Sunday after onset. |
| Patient Advice | Take one tablet daily at the same time each day, with or without food. · If you miss a pill by less than 12 hours, take it as soon as you remember. If more than 12 hours, take the missed pill and use a backup method (e.g., condoms) for the next 7 days. · Smoking increases your risk of serious cardiovascular side effects, especially if you are over 35 years old. Do not smoke while taking this medication. · Seek immediate medical attention if you experience sudden severe headache, chest pain, leg pain/swelling, or vision changes (symptoms of blood clots). · This medication does not protect against HIV or other sexually transmitted infections. · If you are taking lamotrigine or other anticonvulsants, tell your doctor; your seizure medication may be less effective. · Store at room temperature away from moisture and heat. |
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