The success rate of carboprost tromethamine in treating persistent bleeding caused by uterine atony is 84-96% [1]. It also has a significant effect on improving blood hypercoagulability and maintaining hemodynamic stability. Carboprost tromethamine has a significant effect on preventing postpartum hemorrhage after cesarean section.

Metabolism/Metabolic Products Metabolism occurs in the lungs and liver. Metabolic products are excreted in urine.

[1]. Effect of carboprost tromethamine in prevention of postpartum hemorrhage in cesarean section. Pak J Pharm Sci. 2018 Sep;31(5(Special)):2257-2262.

[2]. A comparison of oxytocin and carboprost tromethamine in the prevention of postpartum hemorrhage in high-risk patients undergoing cesarean delivery. Exp Ther Med. 2014 Jan;7(1):46-50. Epub 2013 Nov 1.

Carboprost is a nonsteroidal abortifacient effective in early and mid-pregnancy. Carboprost tromethamine is the tromethamine salt of a naturally occurring prostaglandin F2α (PGF2α) analogue with oxytocin activity (15S)-15 methyl. Carboprost mimics the action of endogenous PGF2α, activating G protein-coupled receptors—prostaglandin F receptors—on smooth muscle cells, thereby causing smooth muscle contraction. When administered intramuscularly to a pregnant woman, the drug induces uterine muscle contraction, initiating corpus luteum dissolution and ultimately leading to labor. In addition, carboprost's effects on vascular smooth muscle and gastrointestinal sphincters can cause increased blood pressure and, respectively, vomiting or diarrhea. See also: Carboprost (containing the active ingredient). Drug Indications Carboprost is used to terminate pregnancy between 13 and 20 weeks of gestation (calculated from the first day of the last normal menstrual period), and in the following situations associated with mid-trimester miscarriage: 1. Failure to expel the fetus during other treatments; 2. Premature rupture of membranes during intrauterine abortion, resulting in drug loss and uterine atony or absence of contractions; 3. Requirement of re-infusion of the drug to expel the fetus; 4. Accidental or spontaneous rupture of membranes due to fetal demise and uterine atony. It can also be used to treat postpartum hemorrhage caused by uterine atony, especially when conventional treatments are ineffective. Mechanism of Action Carboprost is a synthetic prostaglandin. It binds to prostaglandin E2 receptors, causing uterine muscle contractions, thereby inducing labor or expelling the placenta. Prostaglandins are naturally present in the human body and act on multiple sites, including the uterus. They act on the uterine muscles, causing uterine contractions.

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Pharmacodynamics
Intramuscular carboprost tromethamine can stimulate contractions of the myometrium in pregnant women, similar to labor contractions in late term pregnancy. Whether these contractions are caused by carboprost acting directly on the myometrium is unclear. However, in most cases, these contractions help expel pregnancy products. Postpartum, the resulting myometrial contractions can stop bleeding at the placental implantation site. Carboprost tromethamine can also stimulate the smooth muscle of the human gastrointestinal tract. This effect may cause vomiting, diarrhea, or both, which is more common when carboprost tromethamine is used for termination of pregnancy and postpartum. In both experimental animals and humans, carboprost tromethamine can increase body temperature. At clinical doses used for termination of pregnancy and postpartum, some patients experience a transient increase in body temperature. In both experimental animals and humans, high doses of carboprost tromethamine can increase blood pressure, possibly due to its vasoconstrictive effect on smooth muscle. At doses used for termination of pregnancy, this effect is not clinically significant. Carboprost tromethamine can increase body temperature in both laboratory animals and humans. Some patients experience elevated body temperature when terminating pregnancy with clinical doses of carboprost tromethamine. In certain patients, carboprost tromethamine may cause transient bronchoconstriction.

C21H36O5.C4H11NO3

489.64

489.33

58551-69-2

35700-23-3 (Carboprost)58551-69-2 (tromethamine)

5281074

White to off-white solid powder

1.153g/cm3

536.6ºC at 760 mmHg

95-105 °C

292.4ºC

1.794

8

9

15

34

527

5

CCCCC[C@@](C)(/C=C/[C@H]1[C@@H](C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O)O.C(C(CO)(CO)N)O

UMMADZJLZAPZAW-XOWPVRJPSA-N

InChI=1S/C21H36O5.C4H11NO3/c1-3-4-9-13-21(2,26)14-12-17-16(18(22)15-19(17)23)10-7-5-6-8-11-20(24)25;5-4(1-6,2-7)3-8/h5,7,12,14,16-19,22-23,26H,3-4,6,8-11,13,15H2,1-2H3,(H,24,25);6-8H,1-3,5H2/b7-5-,14-12+;/t16-,17-,18+,19-,21+;/m1./s1

(Z)-7-((1R,2R,3R,5S)-3,5-Dihydroxy-2-((S,E)-3-hydroxy-3-methyloct-1-en-1-yl)cyclopentyl)hept-5-enoate tris(hydroxymethyl)aminomethane salt

Carboprost tromethamine

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~125 mg/mL (~255.29 mM)
DMSO : ~100 mg/mL (~204.23 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.11 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (5.11 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (5.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 4: 50 mg/mL (102.12 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

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 (Please use freshly prepared in vivo formulations for optimal results.)