CURRETAB
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CURRETAB (CURRETAB).
Progesterone receptor agonist; induces secretory changes in endometrium, inhibits pituitary gonadotropin secretion, and has anti-estrogenic effects.
| Metabolism | Hepatic via CYP3A4; major metabolites are 6-beta-hydroxyprogesterone and 5-alpha-dihydroprogesterone. |
| Excretion | Primarily renal (60-70% as metabolites, <10% unchanged); biliary/fecal (20-30%) |
| Half-life | Terminal elimination half-life of medroxyprogesterone acetate (MPA) is approximately 12-17 hours (mean ~14 h) for oral administration; with intramuscular depot, half-life extends to ~6-7 weeks due to slow absorption from injection site |
| Protein binding | Highly protein bound (90-95%), primarily to albumin and sex hormone-binding globulin (SHBG) |
| Volume of Distribution | Approximately 0.6-1.5 L/kg (mean ~0.9 L/kg), indicating extensive distribution into tissues, with accumulation in adipose tissue |
| Bioavailability | Oral: ~100% (well absorbed, but undergoes first-pass metabolism with ~0.6-10% systemic availability of parent drug; however active metabolite is formed). Intramuscular: 100% bioavailability as prodrug ester is hydrolyzed to MPA. |
| Onset of Action | Oral: 1-2 hours for peak plasma concentration; clinical effect (e.g., endometrial secretory changes) begins within hours but full therapeutic effect may take several days to weeks. Intramuscular depot: onset within 24-48 hours for contraceptive effect |
| Duration of Action | Oral: duration of action ~12-24 hours per dose; requires daily dosing. Intramuscular depot: duration ~14 weeks (contraceptive) or 3-4 weeks for other indications |
5 mg orally once daily for 10 consecutive days per cycle, beginning on day 16 of the menstrual cycle.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for renal impairment. Not studied in dialysis. |
| Liver impairment | Contraindicated in severe hepatic impairment (Child-Pugh C). For mild to moderate impairment (Child-Pugh A or B), use with caution; no specific dose adjustment guidelines available. |
| Pediatric use | Safety and efficacy not established in pediatric patients. No recommended dosing. |
| Geriatric use | No specific dose adjustment recommended. Use with caution due to potential increased sensitivity to progestational effects and concomitant comorbidities. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CURRETAB (CURRETAB).
| Breastfeeding | Small amounts of medroxyprogesterone acetate are excreted in breast milk (M/P ratio not reported). Available data show no adverse effects on nursing infants at typical doses, but potential for progestin-related effects (e.g., jaundice, hormonal imbalances) cannot be excluded. Avoid use in nursing mothers unless clearly necessary. |
| Teratogenic Risk | First trimester: High risk. Medroxyprogesterone acetate is a progestin with androgenic activity, associated with masculinization of female fetuses and possible hypospadias in males. Use contraindicated for pregnancy testing or maintenance of pregnancy due to risk of congenital anomalies including VACTERL association. Second and third trimesters: Potential for genital abnormalities in female fetuses exposed in utero. Per FDA Pregnancy Category X, risk outweighs any possible benefit. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Known/suspected pregnancy","Undiagnosed vaginal bleeding","Breast cancer (known/suspected)","Active DVT/PE or history of thromboembolic disorders","Severe hepatic impairment","Hypersensitivity to medroxyprogesterone acetate or any component"]
| Precautions | ["Thrombotic disorders (DVT, PE, stroke, MI) - discontinue if occur","Ophthalmic effects (e.g., retinal thrombosis)","Fluid retention - monitor in cardiac/renal conditions","Depression - discontinue if severe","Hepatic impairment","Elevated blood pressure","Hypercalcemia in breast cancer patients","Gallbladder disease","Carbohydrate metabolism effects - monitor in diabetes","Uterine bleeding - exclude malignancy","Endometriosis - exacerbation possible","Drowsiness/dizziness during treatment"] |
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| Fetal Monitoring | Monitor pregnancy status prior to initiation (negative pregnancy test). During use, monitor for signs of fetal androgenic effects if inadvertent exposure occurs; consider ultrasound for fetal growth and anatomy if exposure during first trimester. Monitor maternal blood pressure, glucose, and for thromboembolic events. |
| Fertility Effects | Medroxyprogesterone acetate suppresses ovulation by inhibiting gonadotropin release, leading to delayed return to fertility (up to 18 months after discontinuation). No permanent impact on fertility, but prolonged use may cause anovulation and menstrual irregularities. |