Carboprost Tromethamine

Indications

Terminating pregnancy between the 13th and 20th weeks of gestation. In the following conditions related to second trimester abortion:
  • Failure of expulsion of the fetus during the course of treatment by another method;
  • Premature rupture of membranes in intrauterine methods with loss of drug and insufficient or absent uterine activity;
  • Requirement of a repeat intrauterine instillation of drug for expulsion of the fetus;
  • Inadvertent or spontaneous rupture of membranes in the presence of a previable fetus and absence of adequate activity for expulsion.
Treatment of postpartum hemorrhage due to the uterus failing to return to its normal size and who have not responded to conventional treatments.

Description

Carboprost is a synthetic prostaglandin analogue of PGF2α that acts to increase the contractions of the uterus (womb) and can trigger abortion in early pregnancy. This also helps to control excessive bleeding after delivery.

Pharmacology

Carboprost tromethamine administered intramuscularly stimulates in the gravid uterus myometrial contractions similar to labor contractions at the end of a full term pregnancy. Whether or not these contractions result from a direct effect of carboprost on the myometrium has not been determined. Nonetheless, they evacuate the products of conception from the uterus in most cases.

Postpartum, the resultant myometrial contractions provide hemostasis at the site of placentation.

Carboprost tromethamine also stimulates the smooth muscle of the human gastrointestinal tract. This activity may produce the vomiting or diarrhea or both that is common when carboprost tromethamine is used to terminate pregnancy and for use postpartum. In laboratory animals and also in humans carboprost tromethamine can elevate body temperature. With the clinical doses of carboprost tromethamine used for the termination of pregnancy, and for use postpartum, some patients do experience transient temperature increases.

In laboratory animals and in humans large doses of carboprost tromethamine can raise blood pressure, probably by contracting the vascular smooth muscle. With the doses of carboprost tromethamine used for terminating pregnancy, this effect has not been clinically significant. In laboratory animals and also in humans carboprost tromethamine can elevate body temperature. With the clinical doses of carboprost tromethamine used for the termination of pregnancy, some patients do experience temperature increases. In some patients, carboprost tromethamine may cause transient bronchoconstriction.

Dosage & Administration

Abortion: An initial dose of 1 ml of Carbestop (containing the equivalent of 250 mcg of Carboprost) is to be administered intramuscularly. Subsequent doses of 250 mcg should be administered at 1½ to 3½ hour intervals depending on uterine response. An optional test dose of 100 mcg (0.4 ml) may be administered initially. The dose may be increased to 500 micrograms (2 ml) if uterine contractility is judged to be inadequate after several doses of 250 mcg (1 ml). The total dose administered of Carbestop should not exceed 12 mg and continuous administration of the drug for more than 2 days is not recommended.

For Refractory Postpartum Uterine Bleeding: An initial dose of 250 mcg of Carbestop (1 ml) is to be given deep, intramuscularly (IM). If needed the dose of 1 ml may be repeated between 15 to 90 minutes. The total dose of Carbestop should not exceed 2 mg (8 doses).

Interaction

Carboprost may augment the activity of other oxytocic agents. Concomitant use with other oxytocic agents is not recommended.

Contraindications

  • Hypersensitivity to Carboprost
  • Acute pelvic inflammatory disease

Side Effects

The most frequent adverse reactions observed are related to its contractile effect on smooth muscle, especially gastrointestinal effects like vomiting, nausea, diarrhea and pyrexia. Endometritis, retained placental fragments, and excessive uterine bleeding occurred as the most common complications after abortion with Carboprost.

Pregnancy & Lactation

Pregnancy category C. Animal studies do not indicate that Carboprost is teratogenic, however, it has been shown to be embryotoxic in rats and rabbits and any dose which produces increased uterine tone could put the embryo or fetus at risk.

Precautions & Warnings

  • Use Carboprost by medically trained personnel in a hospital which can provide immediate intensive care and acute surgical facilities.
  • Use Carboprost cautiously in patients with a history of asthma, hypo- or hypertension, cardiovascular, renal or hepatic disease, anemia, jaundice, diabetes or epilepsy and compromised (scarred) uteri.
  • In few patients with chorioamnionitis, uterus may not respond to Carboprost.
  • Cervix should always be carefully examined immediately post-abortion.

Therapeutic Class

Drugs acting on the Uterus

Storage Conditions

Store at 2-8°C. Do not freeze. Keep away from light. Once the ampoule has been opened, the product should be used immediately.

Available Brand Names