Carboprost Trometamol

(BANM, rINNM)
Synonyms: Carboprost trométamol; Carboprost Tromethamine (USAN); Carboprostum Trometamoli; Carboprostum trometamolum; Kaboprosttrometamol; Karboprost z trometamolem; Karboprostas trometamolis; Karboprostitrometamoli; Karboprosttrometamol; U-32921E.
Cyrillic synonym: Карбопрост Трометамол.

💊 Chemical information

Chemical formula: C21H36O5,C4H11NO3 = 489.6.
CAS — 58551-69-2.
ATC — G02AD04.
ATC Vet — QG02AD04.

Description.

Carboprost trometamol is a compound of carboprost with trometamol in a ratio of 1:1.

Pharmacopoeias.

In Eur. and US.

Ph. Eur. 6.2

(Carboprost Trometamol). A white or almost white powder. Soluble in water. Store at a temperature below −15°.

USP 31

(Carboprost Tromethamine). A white to off-white powder. Soluble in water. Store at −25° to −10°.

💊 Adverse Effects and Precautions

As for Dinoprostone. Carboprost may cause bronchospasm and, less frequently, dyspnoea and pulmonary oedema. Patients with cardiopulmonary disorders should be monitored for reductions in arterial-oxygen content. Once a prostaglandin has been given to terminate pregnancy it is essential that termination take place; if the prostaglandin is unsuccessful other measures should be used.

Effects on the fetus.

Congenital abnormalities have been reported in pregnancies carried to term after failed termination using prostaglandins, including carboprost.

Effects on the neonate.

For a report of inadvertent intramuscular administration of carboprost to a neonate, see under Dinoprostone.

Effects on the uterus.

For reference to hyperstimulation and uterine rupture after use of prostaglandins, including carboprost, for termination of pregnancy or induction of labour, see Dinoprostone.

💊 Uses and Administration

Carboprost is a synthetic 15-methyl analogue of dinoprost (prostaglandin F 2 α ; below). It is a uterine stimulant with a more prolonged action than dinoprost; the presence of the methyl group delays inactivation by enzymic dehydrogenation. Carboprost is used for the termination of pregnancy and for the treatment of refractory postpartum haemorrhage due to uterine atony that is not controlled by oxytocin and ergot preparations. It is usually given intramuscularly as the trometamol salt but doses are expressed in terms of carboprost. Carboprost trometamol 1.3 micrograms is equivalent to about 1 microgram of carboprost. For the termination of second trimester pregnancy (between 13 and 20 weeks of gestation) the equivalent of 250 micrograms of carboprost is given by deep intramuscular injection and repeated every 1 1 ⁄ 2 to 3 1 ⁄ 2 hours depending on the uterine response. If necessary the dose may be increased to 500 micrograms, but the total dose given should not exceed 12 mg, and continuous use for more than 2 days is not recommended. If preferred, a test dose of 100 micrograms may be given initially. Carboprost trometamol has also been given intra-amniotically in a dose equivalent to 1 mg of carboprost over five minutes; this dose may be repeated after 24 hours if termination has not occurred and the membranes are intact. A total dose of 5 mg should not be exceeded. Carboprost methyl given as vaginal pessaries has been tried for termination of pregnancy in the second trimester. For the treatment of postpartum haemorrhage the equivalent of 250 micrograms of carboprost is given by deep intramuscular injection as the trometamol salt at intervals of about 90 minutes; the interval may be reduced if necessary, but should not be less than 15 minutes. A total dose of 2 mg should not be exceeded.

Haemorrhagic cystitis.

Carboprost trometamol instilled into the bladder successfully controlled cyclophosphamide-induced haemorrhagic cystitis in 15 of 24 bone marrow transplant patients.1 The dose consisted of 50 mL of solutions containing 2 to 10 micrograms/mL instilled four times daily for 7 days.
1. Ippoliti C, et al. Intravesicular carboprost for the treatment of hemorrhagic cystitis after marrow transplantation. Urology 1995; 46: 811–15.

💊 Preparations

USP 31: Carboprost Tromethamine Injection.

Proprietary Preparations

Belg.: Prostin/15M; Canad.: Hemabate; Cz.: Prostin 15M; Denm.: Prostinfenem; India: Prostodin; Neth.: Prostin/15M; NZ: Prostin 15M; Swed.: Prostinfenem; UK: Hemabate; USA: Hemabate.
Published October 18, 2018.