FEMLYV
Clinical safety rating
cautionComprehensive clinical and safety monograph for FEMLYV (FEMLYV).
Combination of levonorgestrel, a progestin, and ethinyl estradiol, an estrogen; suppresses gonadotropins, inhibits ovulation, alters cervical mucus and endometrium.
| Metabolism | Levonorgestrel: CYP3A4; ethinyl estradiol: CYP3A4, CYP2C9, conjugation. |
| Excretion | Primarily renal (approximately 60-70% as metabolites, less than 10% as unchanged drug); fecal excretion accounts for about 20-30%. |
| Half-life | Terminal elimination half-life is approximately 24-30 hours, supporting once-daily dosing in most patients. |
| Protein binding | Approximately 97-99% bound to plasma proteins, mainly albumin and sex hormone-binding globulin (SHBG). |
| Volume of Distribution | Apparent volume of distribution is approximately 0.5-1.4 L/kg, suggesting distribution into total body water and some tissue binding. |
| Bioavailability | Oral bioavailability is approximately 50-70% due to first-pass metabolism. |
| Onset of Action | Oral administration: Onset of action (e.g., reduction in bleeding) occurs within 1-2 hours; peak plasma concentrations at 1-2 hours. |
| Duration of Action | Duration of action is approximately 24 hours with once-daily dosing; continuous use maintains hemostatic effect. |
| Molecular Weight | 376.46 |
| Action Class | Oral Contraceptive; Progestin-Estrogen Combination |
FEMLYV (norethindrone acetate/ethinyl estradiol) is administered as one tablet (1 mg norethindrone acetate/20 mcg ethinyl estradiol) orally once daily for 21 days, followed by 7 days of placebo tablets. The dosing regimen is continuous cyclic.
| Dosage form | TABLET, ORALLY DISINTEGRATING |
| Renal impairment | No specific dosing adjustment is recommended based on GFR, as pharmacokinetics are not significantly altered. However, use with caution in patients with renal impairment, especially if fluid retention is a concern. |
| Liver impairment | Contraindicated in patients with hepatic impairment (Child-Pugh class A, B, or C). No dose modification is recommended; alternative contraceptive methods should be considered in patients with hepatic disease. |
| Pediatric use | Safety and efficacy have not been established in pediatric patients below 16 years of age. In postmenarchal adolescents, dosing is the same as adults: one tablet daily for 21 days, then 7 days of placebo. |
| Geriatric use | Not indicated for use in postmenopausal women. No specific dosing recommendations for elderly patients, as FEMLYV is a contraceptive for women of reproductive age. |
| 1st trimester | FEMLYV is a combination of ethinyl estradiol and drospirenone. Use in pregnancy is contraindicated due to risk of fetal harm. Data suggest an increased risk of congenital anomalies, particularly cardiovascular and limb defects, with first-trimester exposure to oral contraceptives. Discontinue if pregnancy occurs. |
| 2nd trimester | Avoid use in second trimester as pregnancy is a contraindication for combined hormonal contraceptives. No therapeutic indication exists during pregnancy. |
| 3rd trimester | Use in third trimester is contraindicated. Exposure may lead to adverse fetal and neonatal outcomes including jaundice, hepatic adenoma, and possible teratogenic effects. Discontinue if pregnancy occurs. |
Clinical note
Comprehensive clinical and safety monograph for FEMLYV (FEMLYV).
| Placental transfer | FEMLYV components cross the placenta. Ethinyl estradiol and drospirenone have been detected in fetal circulation. Studies demonstrate placental transfer of both steroids with fetal-to-maternal ratios varying; fetal concentrations are generally lower than maternal. |
| Breastfeeding | FEMLYV passes into breast milk in small amounts. Use while breastfeeding is not recommended because it may reduce milk production and affect milk composition. The American Academy of Pediatrics considers combined hormonal contraceptives as compatible with breastfeeding after postpartum week 6, but progestin-only methods are preferred. For infants, no adverse effects have been reported, but monitor for jaundice and weight gain. |
| Lactation Rating | L3 (Moderately Safe) - Limited data; potential for adverse effects in infant or milk production. Use alternative if available. |
| Teratogenic Risk | FEMLYV (drospirenone and ethinyl estradiol) is contraindicated in pregnancy due to known risks. First trimester exposure is associated with a small increased risk of neural tube defects and cardiovascular anomalies from the estrogen component. Second and third trimester exposure may lead to fetal harm including feminization of male fetuses, urogenital sinus abnormalities, and potential long-term reproductive tract effects. Postnatal effects such as vaginal adenosis and clear cell adenocarcinoma have been reported with in utero diethylstilbestrol exposure, though relevance to FEMLYV is extrapolated. |
| Fetal Monitoring | If unintentional pregnancy occurs during use, discontinue promptly. Monitor for signs of fetal exposure: ultrasound for congenital anomalies if exposure in first trimester. No routine monitoring required for maternal health in pregnancy as drug is contraindicated. |
| Fertility Effects | FEMLYV is an oral contraceptive intended to suppress ovulation. Upon discontinuation, return to fertility may be delayed by 1-2 cycles due to endometrial suppression; no permanent negative effects on fertility. Long-term use does not impair future fertility. |
■ FDA Black Box Warning
Cigarette smoking increases risk of serious cardiovascular events from COC use. Women over 35 who smoke should not use COCs.
| Common Effects | Nausea, Headache, Breast tenderness, Irregular bleeding or spotting, Weight changes, Mood changes |
| Serious Effects | Venous thromboembolism, Arterial thromboembolism (e.g., stroke, myocardial infarction), Hypertension, Hepatic adenoma or liver cancer, Gallbladder disease, Hyperkalemia (especially with drospirenone in patients with renal impairment) |
PregnancyBreast cancer or history thereofHepatic adenoma or active liver diseaseUndiagnosed abnormal uterine bleedingCurrent or history of venous thromboembolismCurrent or history of arterial thromboembolism (e.g., stroke, MI)Migraine with aura (age ≥35 or any age if focal neurological symptoms)Severe hypertension (systolic ≥160 or diastolic ≥100 mmHg)Diabetes mellitus with vascular complicationsMajor surgery with prolonged immobilizationActive hepatitis B or C virus infection with impaired liver functionAdrenal insufficiency (drospirenone has antimineralocorticoid activity)
| Precautions | Cardiovascular disorders, Carcinoma of the breast and reproductive organs, Liver disease, Risk of thromboembolism, Elevated blood pressure, Gallbladder disease, Carbohydrate and lipid metabolic effects, Headache, Bleeding irregularities |
| Food/Dietary | No significant food interactions. Grapefruit juice may slightly increase estrogen levels but not clinically relevant. Avoid high-fat meals if experiencing nausea. |
| Clinical Pearls | FEMLYV is a combined oral contraceptive containing ethinyl estradiol and norgestimate. Monitor for thromboembolic events, especially in smokers over 35. Counsel patients to take at same time daily and to use backup contraception if doses are missed. Efficacy may be reduced with enzyme-inducing drugs. |
| Patient Advice | Take one tablet daily at the same time each day. · If you miss a dose, follow the package instructions and use backup contraception. · Smoking increases risk of serious cardiovascular side effects, especially if over 35. · Common side effects include nausea, headache, and breast tenderness; these often improve. · Contact your healthcare provider if you experience leg swelling, chest pain, or severe headache. |
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