CARBOPROST TROMETHAMINE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CARBOPROST TROMETHAMINE (CARBOPROST TROMETHAMINE).
Carboprost tromethamine is a synthetic prostaglandin F2α analog that binds to prostaglandin F2α receptors, causing myometrial contractions, vasoconstriction, and luteolysis. It increases intracellular calcium, leading to sustained uterine contraction and expulsion of uterine contents.
| Metabolism | Primarily metabolized via oxidation at the C15 position by 15-hydroxyprostaglandin dehydrogenase, followed by reduction of the C13-14 double bond, and beta/omega oxidation. Metabolites are excreted mainly in urine. |
| Excretion | Primarily metabolized in the lungs, liver, and kidneys; less than 5% of the dose is excreted unchanged in urine; the remainder is eliminated via biliary and fecal routes as metabolites. |
| Half-life | Approximately 8 minutes (intravenous); clinical effects diminish rapidly due to rapid metabolism, but the uterotonic effect is sustained by continuous infusion or repeated intramuscular dosing. |
| Protein binding | Approximately 80% bound to plasma albumin. |
| Volume of Distribution | 0.9-1.6 L/kg, indicating extensive distribution into tissues. |
| Bioavailability | Intramuscular: approximately 85-95%; oral: negligible due to rapid first-pass metabolism; intravenous: 100%. |
| Onset of Action | Intramuscular: 3-5 minutes; Intravenous: immediately (within 1 minute); Intrauterine (for abortion): within 15 minutes. |
| Duration of Action | Intramuscular: 2-3 hours; Intravenous: 1 hour (duration of infusion); Intrauterine: 8-10 hours (single injection). Clinical use: For postpartum hemorrhage, a single intramuscular dose provides prolonged uterotonic effect; repeat doses may be needed. |
250 mcg intramuscularly every 1.5 to 3.5 hours, may be increased to 500 mcg if inadequate response; maximum total dose 2 mg.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment recommended based on GFR; use with caution in severe renal impairment. |
| Liver impairment | No specific dose adjustment recommended; contraindicated in severe hepatic failure. |
| Pediatric use | Not recommended for pediatric use; safety and efficacy not established. |
| Geriatric use | No specific dose adjustment; use with caution due to potential for increased sensitivity to adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CARBOPROST TROMETHAMINE (CARBOPROST TROMETHAMINE).
| Breastfeeding | Limited data; carboprost tromethamine is excreted into breast milk in unknown amounts. M/P ratio is not established. Short-term use for postpartum hemorrhage likely poses minimal risk to the infant, but breastfeeding should be avoided during administration and for 24 hours after due to potential GI effects. |
| Teratogenic Risk | Carboprost tromethamine is contraindicated in pregnancy due to its oxytocic properties. It can cause uterine hypertonus, rupture, and fetal distress. In the first trimester, it is an abortifacient; second and third trimester exposure may lead to premature delivery, fetal hypoxia, and death. There is no evidence of teratogenicity from inadvertent exposure, but use is avoided unless for termination or postpartum hemorrhage. |
■ FDA Black Box Warning
Carboprost tromethamine is contraindicated in patients with acute pelvic inflammatory disease. Use with caution in patients with history of asthma, hypotension, or hypertension. Not for intravenous administration. Risk of uterine rupture if used in patients with prior cesarean section or uterine surgery.
| Serious Effects |
["Acute pelvic inflammatory disease","Hypersensitivity to carboprost tromethamine or any component","IV administration (contraindicated due to risk of vasospasm)"]
| Precautions | ["May cause bronchospasm; use caution in asthmatics","May elevate blood pressure; monitor in hypertensive patients","Risk of uterine rupture in patients with prior uterine surgery or grand multiparity","May cause fever, chills, nausea, vomiting, diarrhea; monitor for fluid and electrolyte imbalance","Not for intravenous injection (severe vasospasm and injection site reactions)"] |
| Food/Dietary | No known food interactions. However, if experiencing gastrointestinal side effects like diarrhea, maintain adequate hydration and electrolyte balance. Avoid excessive caffeine or alcohol, which may exacerbate vasomotor symptoms. |
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| Fetal Monitoring | Monitor uterine activity (tone, frequency, duration of contractions), fetal heart rate during intrapartum use, maternal blood pressure (may cause hypertension), heart rate, and signs of bronchospasm. Watch for excessive bleeding, uterine rupture, and fluid overload. |
| Fertility Effects | Carboprost tromethamine induces luteolysis in some animal species, potentially impairing fertility by disrupting early pregnancy. In humans, its use is restricted to obstetric indications and may disrupt implantation if used inadvertently. Effect on long-term fertility is not documented. |
| Clinical Pearls | Carboprost tromethamine is a synthetic prostaglandin F2α analogue used for postpartum hemorrhage due to uterine atony unresponsive to conventional management. Administer deep intramuscularly; avoid intravenous injection as it may cause severe hypertension and bronchospasm. Monitor for excessive bleeding, vital signs, and uterine tone. Contraindicated in acute pelvic inflammatory disease, active cardiac, pulmonary, or hepatic disease. Use with caution in asthma, hypertension, and seizure disorders. Dosage: 250 mcg (1 mL) IM, may repeat at 15-90 minute intervals if needed, maximum 2 mg (8 doses). |
| Patient Advice | This medication is given as an injection to stop severe bleeding after childbirth. · You may experience side effects such as nausea, vomiting, diarrhea, fever, chills, flushing, headache, or dizziness. · Report immediately if you have chest pain, difficulty breathing, or severe abdominal pain. · Breastfeeding is generally safe but consult your healthcare provider. · Do not drive or operate machinery until you know how the medication affects you. |