FEMLYV
Clinical safety rating: caution
Comprehensive 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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for FEMLYV (FEMLYV).
| Breastfeeding | FEMLYV components are excreted in human milk. Ethinyl estradiol milk concentration is approximately 1% of maternal serum; drospirenone M/P ratio is not established. Use during lactation may reduce milk production and quality. No data on infant effects; caution advised. Alternative contraception recommended for breastfeeding women. |
| 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. |
■ FDA Black Box Warning
Cigarette smoking increases risk of serious cardiovascular events from COC use. Women over 35 who smoke should not use COCs.
| Serious Effects |
["Breast cancer or other estrogen/progestin-sensitive cancer","Liver tumors or active liver disease","Undiagnosed abnormal uterine bleeding","Pregnancy","Current or history of thrombosis","Cerebrovascular or coronary artery disease","Migraine with aura (if over 35)","Cigarette smoking (if over 35)"]
| 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"] |
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| 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. |