ESTARYLLA
Clinical safety rating
cautionComprehensive clinical and safety monograph for ESTARYLLA (ESTARYLLA).
Estarylla is a combination oral contraceptive containing ethinyl estradiol and norgestimate. It suppresses gonadotropin release (FSH and LH) via estrogen and progestin, inhibiting ovulation. Additionally, it increases cervical mucus viscosity and alters endometrial receptivity, impeding sperm penetration and implantation.
| Metabolism | Ethinyl estradiol is primarily metabolized by CYP3A4, with conjugation to glucuronides and sulfates. Norgestimate is rapidly metabolized to its active metabolite, norelgestromin, and further to levonorgestrel; involvement of CYP2C19 and CYP3A4 in norgestimate metabolism is noted. |
| Excretion | Renal: ~55% as metabolites, ~27% unchanged; Fecal: ~45% as metabolites |
| Half-life | Terminal elimination half-life of ethinyl estradiol is approximately 13-16 hours; clinical context: steady-state achieved within 5-7 days |
| Protein binding | Ethinyl estradiol: 97-98% bound to albumin, with minor binding to sex hormone-binding globulin |
| Volume of Distribution | Ethinyl estradiol: approximately 2.8 L/kg; indicates extensive tissue distribution |
| Bioavailability | Oral: approximately 55% due to first-pass metabolism; consistent in healthy females |
| Onset of Action | Oral: within 24 hours for contraceptive effect; maximal effect after 7 days of consistent dosing |
| Duration of Action | Contraceptive protection persists for the entire 21-day active pill cycle; 7-day placebo interval allows withdrawal bleeding; missed pills reduce efficacy within 48-72 hours |
| Molecular Weight | 310.4 |
One tablet (0.02 mg ethinyl estradiol and 0.15 mg desogestrel) orally once daily for 21 days, followed by 7 days of placebo. Hormone-free interval of 7 days.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. Not recommended for use in severe renal impairment or end-stage renal disease due to lack of data. |
| Liver impairment | Contraindicated in Child-Pugh class B and C (moderate to severe hepatic impairment). Use with caution in Child-Pugh class A; dose adjustment not specifically defined, but alternative contraception recommended. |
| Pediatric use | Approved for use in postmenarchal adolescents: same dosing as adults (one tablet daily for 21 days, then 7 days placebo). No weight-based dosing required. |
| Geriatric use | Not indicated in postmenopausal women. No specific geriatric dosing; contraindicated in women over 60 years due to increased thromboembolic risk. |
| 1st trimester | Contraindicated due to risk of fetal harm; use in early pregnancy may be associated with congenital defects. |
| 2nd trimester | Contraindicated; estrogen/progestin combinations may cause fetal harm. |
| 3rd trimester | Contraindicated; may cause adverse effects on fetal development. |
Clinical note
Comprehensive clinical and safety monograph for ESTARYLLA (ESTARYLLA).
| Placental transfer | Estrogens and progestins cross the placenta; degree of transfer varies but significant. |
| Breastfeeding | Excreted in human milk; may reduce milk production and affect nursing infant. Use only if benefits outweigh risks. |
| Lactation Rating | L5 (Contraindicated) |
| Teratogenic Risk | Estarylla (ethinyl estradiol/levonorgestrel) is a combined oral contraceptive. Use during pregnancy is contraindicated. First trimester: No strong evidence of major malformations from inadvertent exposure, but increased risk of cardiovascular and limb defects in some studies. Second and third trimesters: Associated with fetal harm, including cardiovascular effects (e.g., congenital heart defects) and possible estrogenic effects, though data are limited. Postnatal effects: Potential long-term developmental effects unknown. Overall risk is low but not zero; avoid use in pregnancy. |
| Fetal Monitoring | No specific fetal monitoring required for inadvertent use; if pregnancy is suspected, discontinue. For women using during pregnancy (contraindicated), consider ultrasound for fetal anatomy if exposure occurred in first trimester. No routine maternal monitoring beyond standard prenatal care. |
| Fertility Effects | Estarylla is a contraceptive; it inhibits ovulation and prevents pregnancy. After discontinuation, fertility returns rapidly, typically within one menstrual cycle. No long-term negative impact on future fertility; does not cause infertility. May cause temporary menstrual irregularity upon cessation. |
■ FDA Black Box Warning
Cigarette smoking increases the risk of serious cardiovascular side effects from combination oral contraceptives. This risk increases with age (especially in women over 35 years of age) and with the number of cigarettes smoked. Women who use combination hormonal contraceptives should be strongly advised not to smoke.
| Common Effects | Anorgasmia decreased orgasm in women Decreased libido Delayed ejaculation Fatigue Increased sweating Insomnia difficulty in sleeping Nausea Sleepiness |
| Serious Effects |
Pregnancy (known or suspected)Breast cancer (current or history)Undiagnosed abnormal uterine bleedingLiver disease (acute or chronic with abnormal function)Thromboembolic disorders (current or history)
| Precautions | Thrombotic disorders: Increased risk of venous thromboembolism (VTE) and arterial thromboembolism (e.g., MI, stroke). Discontinue if thrombotic event occurs., Cardiovascular disease: Avoid in women with uncontrolled hypertension, diabetes with vascular involvement, or history of thromboembolic disease., Cigarette smoking: Strongly advise cessation, especially in women over 35., Liver disease: Discontinue if jaundice or cholestasis develops; contraindicated in acute viral hepatitis or severe cirrhosis., Hormone-dependent malignancies: Increased risk of breast cancer (current use) and cervical cancer; avoid if known or suspected breast cancer., Gallbladder disease: Increased risk of gallstones., Carbohydrate and lipid metabolism: Monitor glucose and lipids in predisposed patients; may impair glucose tolerance and increase triglycerides., Headache: Evaluate if new-onset or worsening migraine, especially with focal neurological symptoms., Uterine bleeding: Rule out pregnancy if amenorrhea occurs; irregular bleeding may require evaluation., Depression: Monitor for mood changes; discontinue if severe depression recurs., Angioedema: Risk in women with hereditary angioedema. |
| Food/Dietary | There are no known significant food interactions. Grapefruit juice may increase estrogen levels but clinical significance is unclear; consider moderate intake. |
| Clinical Pearls | Estarylla is a combination oral contraceptive containing ethinyl estradiol and norgestimate. It is indicated for prevention of pregnancy. Monitor for thromboembolic events, especially in smokers over 35. Counsel on missed dose management: take as soon as remembered, use backup contraception if more than 24 hours late. May reduce menstrual cramps and acne. Not recommended in patients with history of estrogen-dependent neoplasia, liver disease, or uncontrolled hypertension. |
| Patient Advice | Take one pill daily at the same time each day. · If you miss a pill, take it as soon as remembered; use backup contraception if more than 24 hours late. · Do not smoke while taking this medication, especially if over 35. · Report any signs of blood clots: leg pain, chest pain, shortness of breath, or sudden vision changes. · This medication does not protect against HIV or other STDs. |
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