Index
It is available in an injectable form and administered directly into a muscle.
Carboprost (international common name, trade names for tromethamine salts Hemabate, Tham) is a synthetic prostaglandin analog of PGF2α (specifically, it is 15-methyl-PGF2α) with oxytocic properties.
Indications
Carboprost induces contractions and can be used to abort pregnancy early in pregnancy, between weeks 13 and 20.
Also, to stop bleeding after delivery. Carboprost belongs to a group of medicines called prostaglandins—these work by causing uterine contractions.
- Early pregnancy between weeks 13 and 20 of gestation (calculated from the first day of the last average menstrual period). Death of the expulsion of the fetus during treatment by another method.
- Premature rupture of membranes in intrauterine processes with loss of drug and insufficient or absent uterine activity. Requirement of a repeated intrauterine instillation of medicine for the expulsion of the fetus.
- Involuntary or spontaneous rupture of membranes in the presence of a pre-predictable fetus and absence of adequate activity for removal.
Carboprost Dosing Information
Usual adult dose for abortion:
I am starting dose: 250 mcg (1 ml) once by deep intramuscular injection with a tuberculin syringe.
Subsequent doses of 250 mcg (1 ml) can be given at 1.5 to 3.5-hour intervals depending on uterine response.
Maximum total dose: 12 mg. Duration of therapy: no more than two successive days.
Usual adult dose for postpartum bleeding:
The starting dose is 250 mcg (1 ml) once by deep intramuscular injection. Additional amounts can be given at 15 to 90-minute intervals if necessary.
Like other potent oxytocic agents, carboprost should be used only with strict adherence to recommended dosages. Carboprost should be used by medically trained personnel in a hospital that can provide immediate intensive care and acute surgical facilities.
Mechanism of action
Carboprost is a synthetic prostaglandin. It binds to the prostaglandin E2 receptor, causing contractions of the myometrium, causing labor induction or the expulsion of the placenta.
Prostaglandins occur naturally in the body and act at various sites in the body. They work on the muscles of the uterus, causing them to contract. It is used in postpartum hemorrhage caused by uterine atony not controlled by other methods.
A study has shown that Carboprost tromethamine is more effective than oxytocin in preventing postpartum hemorrhage in high-risk patients undergoing cesarean section.
Carboprost is also used for the termination of pregnancy in the second trimester. Tagless use:
- Hemorrhagic cystitis.
- Pelvic inflammatory disease.
Contraindications
It is contraindicated in severe cardiovascular, kidney, and liver diseases. It is also contraindicated in acute pelvic inflammatory disease.
Hypersensitivity to Carboprost or any of its components is also a contraindication. Use caution in asthmatic patients as Carboprost can cause bronchospasm.
Some side effects of Carboprost can occur that generally do not require medical attention. These side effects may go away during treatment as your body adjusts to the medicine.
Also, your healthcare professional can educate you on ways to prevent or reduce some of these side effects. Precautions:
- Asthma.
- Anemia.
- Jaundice.
- Mellitus diabetes.
- Seizure disorders
- Past uterine surgery.
Adverse effects
The adverse effects of this medicine are generally transient and reversible when therapy is finished. Check with your doctor right away if you experience any of the following side effects while taking Carboprost:
- Diarrhea (is the most common, it can be sudden in the beginning).
- Redness or hot flashes.
- Fever.
- A cold.
- Nausea and vomiting
Serious side effects have been reported with Carboprost. Symptoms of an overdose include:
- Irritation.
- Tos.
- Dyspnoea.
- Hypertension.
- Redness
- Pyrexia.
Transient pyrexia may be due to the effect of Carboprost on hypothalamic thermoregulation. A rise in temperature exceeding 2 degrees Fahrenheit has been reported in approximately 12.5% of patients who received the recommended dosage regimen.
In all cases, the temperature returned to normal when therapy ended. Along with its necessary effects, Carboprost can cause some unwanted effects. Although not all of these side effects can occur, if they do occur, they may need medical attention.
Pretreatment or concurrent administration of antiemetics and antidiarrheals considerably decreases the very high incidence of gastrointestinal side effects common with all prostaglandins used for abortion.
Storage and availability
Carboprost is supplied with its tromethamine salt derivative in 1-milliliter ampoules containing a 250 microgram/milliliter solution of the active drug. The drug should be refrigerated at a temperature between 2 – 8 degrees Celsius.
Synthesis
A significant deactivating metabolic transformation of natural prostaglandins in the enzymatic oxidation of the C-15 hydroxyl to the corresponding ketone. With the activity retention, methylation prevents this form giving the C-15 tertiary carbinol series.
This molecular characteristic is quickly introduced into Corey’s lactone stage by reaction with Grignard’s methyl reagent or trimethylaluminum.
The resulting mixture of tertiary carbinols is transformed into oxytocic Carboprost by standard transformations, including the separation of diastereomers so that the final product is the C-15 analog. This diastereomer is free of prostaglandin side effects than the C-15 (S) isomer.
Interactions with other medications
If you use other drugs or over-the-counter products at the same time, the effects of Carboprost may change. This can increase your risk of side effects or make your medicine not work properly.
Tell your doctor about all medications, vitamins, and herbal supplements you are using, so your doctor can help you prevent or manage drug interactions.
Is this drug or product addictive or habit-forming?
Most medications do not have the potential for addiction or abuse. The government generally classifies medicines that can be addictive as controlled substances.
