carboprost tromethamine

Action and Spectrum

Actions and Spectrum: 

The mechanism of action of carboprost tromethamine involves binding to prostaglandin receptors in the smooth muscle of the uterus, causing it to contract and reduce bleeding.

It also has vasoconstrictive effects on blood vessels, further contributing to its hemostatic properties. The spectrum of activity of carboprost tromethamine is limited to the uterus and its blood vessels.

Treating other types of bleeding or other parts of the body is impractical. Additionally, it should only be used in women who have given birth or have a viable fetus, as it can induce uterine contractions and potentially cause harm to a developing fetus. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Epistaxis 

Hyperthermia 

Asthma 

Coughing 

Flushing 

Nervousness 

Sleep disorder 

Flushing 

Wheezing 

Chest pain 

Hypertension 

Palpation 

Chest tightness 

Chills/shivering 

Drowsiness 

Faintness 

Lethargy 

Lightheadedness 

Syncope 

Tachycardia 

Anxiety 

Dizziness 

Vasovagal syndrome 

Vertigo 

Dystonia 

Headache 

Rash 

Dysmenorrhea-like pain 

Breast tenderness 

Gagging/retching 

Drowsiness 

Dry throat 

Hot flashes 

Thyroid storm 

Nervousness 

Sleep disturbance 

Temperature elevation 

Endometritis 

Black Box Warning

Black box warning: 

• Potent oxytocic agent; strictly adhere to the prescribed dosage 
• Only medically qualified staff should give the substance in a hospital setting that can offer rapid treatment and acute surgical facilities. 

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Hypersensitivity: carboprost tromethamine should not be used in individuals with known hypersensitivity or allergy to the drug. 
• Asthma: The drug can cause bronchospasm and respiratory distress in individuals with a history of asthma. 
• Active cardiac, pulmonary, renal, or hepatic disease: carboprost tromethamine can exacerbate these conditions and should not be used in individuals with active disease. 
• Coagulation disorders: The drug can increase the risk of bleeding in individuals with coagulation disorders 
• Suspected or confirmed sepsis: carboprost tromethamine can cause fever and exacerbate infection in individuals with sepsis 
• Women with a history of cesarean section or major uterine surgery: carboprost tromethamine can increase the risk of uterine rupture in women with a history of cesarean section or major uterine surgery. 
• Fetal distress: The drug can cause fetal distress and should not be used in distress or nonreassuring fetal status. 

Caution: 

• Hypertension: The drug can cause an increase in blood pressure and should be used cautiously in individuals with hypertension 
• Anemia: carboprost tromethamine can cause anemia due to blood loss during uterine contractions and should be used cautiously in individuals with preexisting anemia 
• Glaucoma: The drug can increase intraocular pressure and should be used cautiously in individuals with glaucoma. 
• Epilepsy: The drug can cause seizures and should be used cautiously in individuals with a history of epilepsy. 
• Pulmonary disease: carboprost tromethamine can cause respiratory distress and should be used cautiously in individuals with pulmonary disease 
• Liver or kidney disease: The drug is metabolized and excreted through the liver and kidneys and should be used cautiously in individuals with liver or kidney disease 
• Use with other uterotonic agents: carboprost tromethamine should not be used in conjunction with other uterotonic agents, as this can increase the risk of adverse effects. 

Pregnancy / Lactation

Pregnancy consideration: C 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.   

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

carboprost tromethamine is a synthetic analog of prostaglandin F2 alpha. It acts as a potent uterotonic agent by binding to specific prostaglandin receptors in the smooth muscle of the uterus, causing it to contract and reducing bleeding. The drug also has vasoconstrictive effects on blood vessels, further contributing to its hemostatic properties. 

Pharmacodynamics: 

• The pharmacodynamics of carboprost tromethamine are primarily related to its effects on the smooth muscle of the uterus and blood vessels. 
• carboprost tromethamine acts as a potent uterotonic agent by binding to specific prostaglandin receptors in the smooth muscle of the uterus, leading to increased frequency and strength of uterine contractions. These contractions reduce bleeding and promote the expulsion of the placenta and any remaining products of conception. 
• The drug also has vasoconstrictive effects on blood vessels, further contributing to its hemostatic properties. Vasoconstriction of blood vessels can decrease blood flow to the uterus, reducing bleeding and increasing blood pressure. 
• In addition to its effects on the uterus and blood vessels, carboprost tromethamine can stimulate gastrointestinal smooth muscle and cause bronchoconstriction. These effects are due to its actions on specific prostaglandin receptors in these tissues.

Pharmacokinetics: 

Absorption 

carboprost tromethamine is administered by intramuscular injection and rapidly absorbed into the systemic circulation. Maximum plasma concentrations are achieved within 15 to 30 minutes after injection.  

Distribution 

carboprost tromethamine is highly bound to plasma proteins and has a small distribution volume of approximately 0.2 L/kg. The drug does not cross the blood-brain barrier or the placenta. 

Metabolism 

carboprost tromethamine is metabolized primarily in the liver, which undergoes beta-oxidation to form inactive metabolites. The drug has a short half-life of approximately 40 minutes 

Elimination and Excretion 

carboprost tromethamine and its metabolites are excreted primarily in the urine, with approximately 55% of the drug and its metabolites eliminated within 8 hours of administration. The remainder of the drug is eliminated in the feces. 

Adminstartion

Administration: 

• carboprost tromethamine is administered by intramuscular injection. The recommended dose for preventing and treating postpartum hemorrhage is 250 mcg (1 mL) every 15 to 90 minutes, up to a maximum of 12 doses. The dosage and frequency of administration may be adjusted based on the severity of the bleeding and the patient’s response to treatment. 
• carboprost tromethamine should only be administered by a healthcare professional trained in its use and familiar with the potential adverse effects of the drug. The injection should be given deep into the muscle, such as the upper outer quadrant of the gluteal or lateral thigh muscles 
• It is essential to monitor the patient’s vital signs, including blood pressure and heart rate, during and after the administration of carboprost tromethamine, as the drug can cause an increase in blood pressure and other adverse effects 

Patient Information Leaflet

Patient information leaflet 

Generic Name: carboprost tromethamine 

Why do we use carboprost tromethamine? 

carboprost tromethamine is a medication primarily used in obstetrics to prevent and treat postpartum hemorrhage. It is also sometimes used in the management of incomplete abortion