Carboprost Tromethamine

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Belgium: Prostin 15M; Bulgaria: Prostin 15M; Czech Republic: Prostin 15M; Denmark: Prostinfenem; Luxembourg: Prostin/15M; Netherlands: Prostin/15M; Slovakia: Prostin 15M; Sweden: Prostinfenem; UK: Hemabate.

North America

Canada: Hemabate; USA: Hemabate.

Drug combinations

Chemistry

Carboprost Tromethamine: C~21~H~36~O~5~ C~4~H~11~NO~3~. Mw: 489.64. (1) Prosta-5,13-dien-1-oic acid, 9,11,15-trihydroxy-15-methyl-, (5Z,9α,11α,13E,15S)-, compound with 2-amino-2-(hydroxymethyl)-1,3-propanediol (1:1); (2)(Z)-7-[(1R,2R,3R,5S)-3,5-Dihydroxy-2-[(E)-(3S)-3-hydroxy-3-methyl-1-octenyl]cyclopentyl]-5-heptenoic acid compound with 2-amino-2-(hydroxymethyl)-1,3-propanediol (1:1); (3)(15S)-15-Methylprostaglandin F~2α~ tromethamine. CAS-58551-69-2; CAS-35700-23-3 (carboprost)(1977).

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Pharmacologic Category

Oxytocics; Prostaglandin. (ATC-Code: G02AD04).

Mechanism of action

Synthetic derivative of prostaglandin F~2α~. Stimulates uterine smooth muscle. Increases amplitude and frequency of uterine contractions throughout pregnancy (uterine response increases with the duration of pregnancy). After delivery, uterine contractions impede uterine blood flow. Produces cervical dilation. Produces contraction of vascular smooth muscle (risk of increased blood pressure). Causes stimulation of the smooth muscle of the gastrointestinal tract, increasing gastrointestinal motility. Stimulates transient bronchoconstriction in some patients.

Therapeutic use

Termination of intrauterine pregnancy during the second trimester (weeks 13-20 of gestation, dated from the first day of the last menstrual period). To induce abortion after membrane rupture. Treatment of postpartum hemorrhage in the presence of uterine atony that has not responded to usual therapy.

Pregnancy and lactiation implications

Teratogenic effects not observed in animal studies. Use not indicated if fetus has reached a stage of viability in utero. Complete abortion may not be induced in ~20% of cases. Excretion in breast milk unknown.

Unlabeled use

Hemorrhagic cystitis.

Contraindications

Hypersensitivity to carboprost tromethamine or any component of the formulation. Acute pelvic inflammatory disease. Active cardiac, pulmonary, renal, or hepatic dysfunction.

Warnings and precautions

Increased blood pressure or transient pyrexia may be observed with treatment. Use with caution in adrenal insufficiency, anemia, history of asthma, cardiovascular disease, compromised (scarred) uterus, diabetes mellitus, renal impairment, or seizure disorder. Concomitant use of antiemetic and antidiarrheal agents is recommended to decrease incidence of gastrointestinal side-effects. Large amounts of benzyl alcohol have been associated with toxicity (fatal «gasping syndrome») in neonates. Proliferation of long bones reported in neonates receiving long-term therapy with alprostadil (prostaglandin E~1~); no evidence that short-term administration of carboprost has similar effects on bone. Potent oxytocic agent. Carboprost does not affect the fetoplacental unit. Risk of cervical trauma. Transient fever (i.e. temperature elevations >1.1°C) reported in approximately 12.5% of patients. When used for termination of pregnancy, may be difficult to distinguish drug-induced temperature elevations from post-abortion endometritis. Chorioamnionitis may contribute to postpartum uterine atony and hemorrhage; individuals with chorioamnionitis experiencing postpartum hemorrhage have failed to respond to carboprost.

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