PREPIDIL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PREPIDIL (PREPIDIL).
Dinoprostone (PGE2) stimulates myometrial contractions and cervical ripening by increasing intracellular calcium and promoting collagenase activity.
| Metabolism | Rapidly metabolized via 15-hydroxyprostaglandin dehydrogenase in the lungs and other tissues; also undergoes beta-oxidation and reduction. |
| Excretion | Primarily renal: 50-70% as metabolites, 10-15% as unchanged drug; fecal: 20-30% via bile. |
| Half-life | Terminal elimination half-life: 8-12 hours (intravaginal administration). |
| Protein binding | >90% bound to albumin and α-fetoprotein. |
| Volume of Distribution | ~2-3 L/kg indicating extensive tissue distribution. |
| Bioavailability | Intravaginal: 5-10% (uterine first-pass); oral: ~50% (extensive hepatic metabolism). |
| Onset of Action | Intravaginal: 30-60 minutes to initial cervical ripening; oral: 15-30 minutes to uterine activity. |
| Duration of Action | Intravaginal: 8-12 hours (sustained release for cervical ripening); intravenous: 2-4 hours after cessation. |
Intravaginal: 0.5 mg dinoprostone gel inserted into posterior vaginal fornix every 6 hours as needed for cervical ripening; maximum total dose 1.5 mg (3 doses) within 24 hours.
| Dosage form | GEL |
| Renal impairment | No dosage adjustment required for renal impairment; use caution in severe impairment due to potential fluid retention. |
| Liver impairment | No established guidelines; use caution in severe hepatic impairment (Child-Pugh class C) due to altered drug metabolism. |
| Pediatric use | Not indicated for pediatric use. |
| Geriatric use | Not indicated for use in elderly patients; contraindicated in postmenopausal women. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PREPIDIL (PREPIDIL).
| Breastfeeding | Not applicable; dinoprostone is used intrapartum and rapidly metabolized, with minimal transfer to breast milk. No M/P ratio data available. Avoid breastfeeding during administration; may resume after drug washout. |
| Teratogenic Risk | PREPIDIL (dinoprostone) is a prostaglandin E2 used for cervical ripening. No evidence of teratogenicity in first trimester due to lack of exposure during organogenesis; use is restricted to third trimester for induction of labor. Fetal risks include uterine hyperstimulation, fetal distress, and meconium passage. Category C: animal studies show adverse effects. |
■ FDA Black Box Warning
Not to be used in women with hypersensitivity to prostaglandins, severe fetal distress, or when immediate delivery is required.
| Serious Effects |
["Hypersensitivity to prostaglandins","Severe fetal distress","Chorioamnionitis","History of prior cesarean section or major uterine surgery","Cephalopelvic disproportion","Non-reassuring fetal status"]
| Precautions | ["Uterine hyperstimulation","Fetal distress","Placental abruption","Maternal hemorrhage"] |
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| Fetal Monitoring | Continuous fetal heart rate monitoring and uterine activity assessment via tocodynamometry or intrauterine pressure catheter. Monitor for maternal vital signs, signs of uterine hyperstimulation or tetanic contractions. |
| Fertility Effects | No known effects on fertility; dinoprostone is used for cervical ripening and induction of labor at term, not associated with long-term reproductive impairment. |