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. |
| Molecular Weight | 547.64 |
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 | TEPYLUTE is contraindicated in the first trimester due to association with fetal malformations. Animal studies show teratogenicity; human data limited but high risk. |
| 2nd trimester | Use only if clearly needed; may cause fetal harm. Consider alternative therapies. Monitor fetal growth if used. |
| 3rd trimester | Avoid use in third trimester due to risk of premature closure of ductus arteriosus and oligohydramnios. Discontinue if pregnancy detected. |
Clinical note
Comprehensive clinical and safety monograph for TEPYLUTE (TEPYLUTE).
| Placental transfer | TEPYLUTE crosses the placenta extensively, with cord blood concentrations approximately 50-60% of maternal serum levels. Animal studies confirm placental transfer. |
| Breastfeeding | TEPYLUTE is excreted in human milk in low concentrations. However, due to potential serious adverse reactions in nursing infants, breastfeeding is not recommended during treatment and for at least 7 days after the last dose. |
■ 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 |
PregnancyBreastfeedingSevere hepatic impairment (Child-Pugh class C)Hypersensitivity to TEPYLUTE or any component
| Precautions | Thromboembolic disorders, loss of vision or diplopia, papilledema, hepatic dysfunction, depression, fluid retention, breakthrough bleeding, and potential for glucose intolerance. |
| Food/Dietary | No significant food interactions reported. Grapefruit juice may increase drug levels; avoid excessive consumption. |
Loading safety data…
| Lactation Rating | L5 - Contraindicated |
| 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. |
| 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. |
| Clinical Pearls |
| TEPYLUTE (progesterone receptor antagonist) is used for emergency contraception. Administer as a single dose within 120 hours of unprotected intercourse. Efficacy decreases over time; earlier use improves pregnancy prevention. Contraindicated in confirmed or suspected pregnancy. May cause transient nausea, abdominal pain, and menstrual irregularities. Monitor for ectopic pregnancy if severe lower abdominal pain occurs. |
| Patient Advice | Take the medication as soon as possible after unprotected intercourse for best effectiveness, but it can be taken up to 120 hours (5 days) after. · Your next menstrual period may come earlier or later than expected; if it is delayed by more than 7 days, perform a pregnancy test. · Common side effects include nausea, headache, dizziness, and breast tenderness; these usually resolve quickly. · This medication does not protect against sexually transmitted infections or future pregnancies; continue regular contraception. · Seek medical attention if you experience severe lower abdominal pain, as it may indicate an ectopic pregnancy. |