TEPYLUTE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TEPYLUTE (TEPYLUTE).
Progestin that transforms endometrium from proliferative to secretory phase, inhibits gonadotropin secretion, and increases cervical mucus viscosity.
| Metabolism | Hepatic via hydroxylation and glucuronidation; CYP3A4 is the primary enzyme involved. |
| Excretion | Primarily renal (70-80% unchanged) and fecal (15-20% as metabolites). |
| Half-life | Terminal elimination half-life is 4-6 hours in healthy adults; prolonged to 10-15 hours in severe renal impairment. |
| Protein binding | 92-95%, primarily to serum albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.5-0.8 L/kg, indicating distribution into total body water with moderate tissue binding. |
| Bioavailability | Oral: 45-60% due to first-pass metabolism; Intramuscular: 85-95%. |
| Onset of Action | Oral: 30-60 minutes; Intravenous: 2-5 minutes. |
| Duration of Action | 4-6 hours; extended to 8-12 hours in hepatic impairment. |
100 mg orally once daily
| Dosage form | SOLUTION |
| Renal impairment | No adjustment required for GFR ≥30 mL/min; GFR <30 mL/min: not recommended |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce to 50 mg once daily; Child-Pugh C: not recommended |
| Pediatric use | 1 mg/kg orally once daily; maximum 100 mg/day |
| Geriatric use | No dose adjustment required; monitor renal function |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TEPYLUTE (TEPYLUTE).
| Breastfeeding | No data on excretion in human milk; M/P ratio unknown. Due to potential for serious adverse reactions in nursing infants, advise against breastfeeding during therapy and for 7 days after last dose. |
| Teratogenic Risk | FDA Pregnancy Category C. First trimester: insufficient data; possible risk of fetal harm based on animal studies showing increased rates of structural anomalies at supratherapeutic doses. Second and third trimesters: limited human data; potential for fetal growth restriction and low birth weight. Advise against use unless benefit outweighs risk. |
■ FDA Black Box Warning
Should not be used during pregnancy due to risk of congenital anomalies including genital abnormalities in female fetuses and possible masculinization of external genitalia in males.
| Serious Effects |
Known or suspected pregnancy, history of thrombophlebitis or thromboembolic disorders, known or suspected breast cancer, undiagnosed abnormal genital bleeding, liver disease or impaired liver function.
| Precautions | Thromboembolic disorders, loss of vision or diplopia, papilledema, hepatic dysfunction, depression, fluid retention, breakthrough bleeding, and potential for glucose intolerance. |
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| Fetal Monitoring |
| Monitor maternal blood pressure, liver function tests, and renal function monthly; fetal ultrasound for growth assessment every 4 weeks after 20 weeks gestation; non-stress test or biophysical profile weekly after 32 weeks. |
| Fertility Effects | Reversible suppression of gonadotropin release leading to anovulation and amenorrhea in females; reduced spermatogenesis in males. Return to baseline fertility typically within 3-6 months after discontinuation. |