PREPIDIL
Clinical safety rating
cautionComprehensive clinical and safety monograph for PREPIDIL (PREPIDIL).
Comprehensive clinical and safety monograph for PREPIDIL (PREPIDIL).
Cervical ripening and induction of labor at term
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. |
| Molecular Weight | 352.47 |
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 | Contraindicated: risk of spontaneous abortion and teratogenic effects due to prostaglandin E2 activity. |
| 2nd trimester | Contraindicated: used only for cervical ripening and induction of labor at term; not indicated in second trimester. |
| 3rd trimester | Used for cervical ripening and induction of labor under close monitoring; may cause uterine hyperstimulation and fetal distress. |
Clinical note
Comprehensive clinical and safety monograph for PREPIDIL (PREPIDIL).
| Placental transfer | Crosses placenta rapidly; fetal plasma levels are approximately 20% of maternal levels after vaginal administration. |
| Breastfeeding | Minimal excretion into breast milk due to rapid metabolism; considered compatible with breastfeeding when used short-term for induction of labor. |
| Lactation Rating | L2 (Safer) |
| 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. |
| 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. |
■ 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 |
Known hypersensitivity to prostaglandinsUnexplained vaginal bleeding during pregnancyPlacenta previa or vasa previaHistory of Cesarean section or major uterine surgeryCephalopelvic disproportionFetal distress where immediate delivery is not feasibleUmbilical cord prolapseCord presentationActive genital herpes infectionMultiple gestation (relative, but often contraindicated)Previous major uterine or cervical surgeryNon-vertex presentation
| Precautions | Uterine hyperstimulation, Fetal distress, Placental abruption, Maternal hemorrhage |
| Food/Dietary | No known food interactions. Maintain normal diet unless otherwise instructed by healthcare provider. |
| Clinical Pearls | Prepidil (dinoprostone) is a prostaglandin E2 analogue used for cervical ripening. Administer intracervically; ensure patient is in lithotomy position for insertion. Monitor uterine activity and fetal heart rate continuously. Do not use in patients with hypersensitivity to prostaglandins, severe hypertension, or known pelvic inflammatory disease. Discontinue if hyperstimulation occurs; may use terbutaline as tocolytic. |
| Patient Advice | This medication is used to prepare the cervix for labor induction. · You will be monitored closely during administration. · Report any excessive or painful contractions, or bleeding. · Avoid sexual intercourse during treatment. · Inform your doctor of any allergies or medical conditions. |
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