ESTARYLLA
Clinical safety rating: caution
Comprehensive 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 |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ESTARYLLA (ESTARYLLA).
| Breastfeeding | Estarylla is excreted in breast milk in small amounts (ethinyl estradiol: M/P ratio ~0.2; levonorgestrel: M/P ratio ~0.3-0.4). Combined hormonal contraceptives may reduce milk production and affect milk composition, especially in early postpartum. Use is generally not recommended until breastfeeding is well-established (at least 6 weeks postpartum). For later use, progestin-only methods are preferred. Monitor infant for jaundice and growth. |
| 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. |
■ 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 |
["Known or suspected pregnancy","Current or past venous thrombosis (e.g., deep vein thrombosis, pulmonary embolism)","Current or past arterial thrombosis (e.g., myocardial infarction, stroke) or prodromal conditions (e.g., angina, transient ischemic attack)","Known thrombophilic disorders (e.g., Factor V Leiden, prothrombin mutation, antithrombin deficiency)","History of cerebrovascular or coronary artery disease","Uncontrolled hypertension (sustained >160/100 mmHg)","Diabetes mellitus with nephropathy, retinopathy, neuropathy, or other vascular disease","Headaches with focal neurological symptoms (e.g., migraine with aura) in women over 35","Current or past breast cancer, or other estrogen- or progestin-sensitive cancer","Active liver disease (e.g., acute viral hepatitis, severe cirrhosis) or benign/malignant liver tumors","Undiagnosed abnormal uterine bleeding","Hypersensitivity to any component of Estarylla","Use of highly active antiretroviral therapy (HAART) containing ritonavir or direct-acting antivirals for hepatitis C (e.g., ombitasvir/paritaprevir/ritonavir) due to potential for hepatotoxicity"]
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| 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. |
| 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."] |