PROSTIN E2
Clinical safety rating
cautionComprehensive clinical and safety monograph for PROSTIN E2 (PROSTIN E2).
Comprehensive clinical and safety monograph for PROSTIN E2 (PROSTIN E2).
Induction of labor at term (FDA approved)Cervical ripening before induction of labor (FDA approved)Evacuation of uterine contents in missed abortion or intrauterine fetal death up to 28 weeksManagement of benign hydatidiform molePostpartum hemorrhage off-label use
Dinoprostone (PGE2) is a naturally occurring prostaglandin that stimulates uterine smooth muscle contractions and cervical ripening by binding to EP receptors, leading to increased intracellular calcium and myometrial contractility. It also promotes cervical softening through collagenase activation and glycosaminoglycan changes.
| Metabolism | Rapidly metabolized in the lungs, liver, and kidneys by 15-hydroxyprostaglandin dehydrogenase and prostaglandin reductase. Metabolites are excreted primarily in urine. |
| Excretion | Primarily metabolized in the lungs, liver, and kidneys; >90% of metabolites excreted renally, with <5% unchanged in urine; minor biliary/fecal elimination. |
| Half-life | Terminal elimination half-life is approximately 2-3 minutes for dinoprostone due to rapid enzymatic metabolism; clinical effects are short-lived, requiring continuous infusion for sustained action. |
| Protein binding | Approximately 80-90% bound to serum albumin. |
| Volume of Distribution | Vd is about 0.1-0.2 L/kg, indicating limited distribution primarily to extracellular fluid; consistent with rapid clearance and small tissue binding. |
| Bioavailability | Intravaginal: 10-20% (due to first-pass pulmonary metabolism); intracervical: low systemic absorption (minimal bioavailability); oral: <10% due to extensive first-pass metabolism. |
| Onset of Action | Intravaginal: onset of uterine contractions within 15-60 minutes; intracervical: cervical ripening begins within 1-3 hours; intravenous: immediate, within minutes. |
| Duration of Action | Intravaginal: 2-4 hours per dose; intracervical: up to 12 hours; intravenous: effects persist as long as infusion continues, dissipating within 15-30 minutes after discontinuation. |
| Molecular Weight | 352.46 |
Cervical ripening: 0.5 mg (1 suppository) intravaginally; repeat every 4-6 hours if needed, up to 3 doses in 24 hours. Induction of labor: 2.5 mg (1 suppository) intravaginally every 3-5 hours, maximum 10 mg/24 hours.
| Dosage form | SUPPOSITORY |
| Renal impairment | No specific dose adjustment required in renal impairment; use with caution in severe renal dysfunction (e.g., GFR <30 mL/min) due to potential for fluid retention. |
| Liver impairment | No specific dose adjustment required in hepatic impairment; use with caution in severe hepatic dysfunction (Child-Pugh class C) due to altered metabolism. |
| Pediatric use | Not indicated for pediatric use; no established dosing guidelines. |
| Geriatric use | No specific dose adjustment required; use with caution due to increased risk of uterine hyperstimulation and cardiovascular effects in older women. |
| 1st trimester | Category C: Animal studies show risk but human data are inadequate. Use only if clearly needed. |
| 2nd trimester | Category C: Use only if clearly needed due to potential for uterine hyperstimulation. |
| 3rd trimester | Category C: Risk of uterine hyperstimulation and fetal distress. Use only for indicated obstetrical procedures. |
Clinical note
Comprehensive clinical and safety monograph for PROSTIN E2 (PROSTIN E2).
| Placental transfer | Crosses placenta rapidly; can induce uterine contractions and affect fetal heart rate. |
| Breastfeeding | Excretion into breast milk unknown. Due to rapid metabolism and short half-life, risk to infant is likely low. Use cautiously. |
| Lactation Rating | L3: Limited data - possibly safe. |
| Teratogenic Risk | FDA Pregnancy Category C. First trimester: No adequate human studies; animal studies suggest potential risk. Second and third trimesters: Used for cervical ripening and labor induction; risk of uterine hyperstimulation and fetal distress. Not associated with structural anomalies when used at term. |
| Fetal Monitoring | Continuous fetal heart rate monitoring and uterine activity monitoring (tocography). Monitor maternal vital signs, uterine hyperstimulation, and signs of placental abruption or uterine rupture. |
| Fertility Effects | No known adverse effects on fertility. Used for cervical ripening in non-pregnant women for certain procedures; no negative impact on conception. |
■ FDA Black Box Warning
Should be used only by trained medical personnel in a hospital setting with immediate access to facilities for managing complications such as uterine hyperstimulation, fetal distress, and emergency cesarean section.
| Serious Effects |
Hypersensitivity to dinoprostoneAcute pelvic inflammatory diseasePlacenta previaUnexplained vaginal bleedingPrior cesarean section or major uterine surgeryNon-vertex presentationCephalopelvic disproportionFetal distressMaternal cardiovascular, hepatic, or renal disease
| Precautions | Uterine hyperstimulation may occur, leading to fetal distress or uterine rupture, especially in patients with prior cesarean section or uterine surgery., Monitor uterine activity, fetal heart rate, and cervical status continuously during administration., Use with caution in patients with cardiovascular, renal, or hepatic impairment., Risk of amniotic fluid embolism, disseminated intravascular coagulation (DIC) in missed abortion cases., Prostaglandins may cause hypotension, bronchospasm, or pyrexia. |
| Food/Dietary | No clinically significant food interactions reported. Maintain hydration and light diet as tolerated during labor. |
| Clinical Pearls | Monitor uterine contractility and fetal heart rate continuously during administration. Avoid use in patients with active pelvic inflammatory disease or hypersensitivity. Have oxytocin and tocolytics available for uterine hyperstimulation. For cervical ripening, use lowest effective dose and limit exposure to 12-24 hours. |
| Patient Advice | This medication is used to start or strengthen labor contractions or to soften and dilate the cervix. · You will be closely monitored during treatment for contractions and your baby's heart rate. · Report any excessive or prolonged contractions, vaginal bleeding, or severe abdominal pain immediately. · Avoid sexual intercourse and strenuous activity while using this medication. · Do not attempt to use this medication at home unless specifically instructed by your healthcare provider. |
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