Carbetocin

Carbetocin

Carbetocin is a synthetic oxytocin analog used to induce labor or as a tocolytic. It is indicated to control postpartum hemorrhage due to uterine atony associated with uterine inertia, as well as in the prevention and treatment of uterine muscle syndrome during the third trimester of pregnancy. It is available in injection form in a 20ml vial.

Uses For

Carbetocin is mainly used to induce labor and control postpartum hemorrhage associated with uterine atony due to uterine inertia. Additionally, it can also be used to prevent and treat uterine muscle syndrome during the third trimester of pregnancy.

Mechanism Of Action

The active component of the drug, Carbetocin , is a delta receptor agonist with a much higher potency than oxytocin. Its mechanism of action involves binding to isotocin receptors, which are expressed in both the myometrium and endometrium, to induce uterine contraction. Additionally, carbetocin has vasopressin-like properties, which can lead to vasoconstriction. This results in improved uterine perfusion, delaying postpartum hemorrhage.

How Long Does It Take To Work?

Carbetocin starts to work within 5-10 minutes after administration and its effects can last anywhere from 2-4 hours. In some cases, it can take up to 30 minutes for the drug to start producing its effects.

Absorption

Carbetocin is rapidly and completely absorbed after intravenous administration.

Route of Elimination

Carbetocin is mainly eliminated via renal excretion. After intravenous administration, there is typically a rapid decline in plasma levels over 4 to 6 hours, with a median elimination half life of 3.7 hours.

Dosage

A single intravenous dose of 100 mcg of carbetocin injection is administered by bolus injection, slowly over 1 minute, only when infant delivery has been completed by caesarean section under epidural or spinal anaesthesia. carbetocin is to be used as a single dose only.

The recommended dose of Carbetocin is 2 mL, corresponding to 100 mcg given intravenously, which is repeated 1 to 4 hours depending on the intensity of uterine contractions. If the effect does not occur, a further single dose can be used up to 8 hours after the previous dose. The maximum dose is 500 mcg over a 24-hour period.

Administration

Carbetocin should be administered intravenously at a rate of 1 mL per minute. It should not be administered intramuscularly or subcutaneously.

Side Effects

Common side effects of Carbetocin include headache, dizziness, nausea, vomiting, abdominal discomfort, diarrhea, flushing, hypertension, and tachycardia. Rarely, more serious side effects such as pulmonary edema, arrhythmia, and cardiac arrest have been reported.

Toxicity

The pharmacologic effects of Carbetocin are dose-dependent. Overdoses of Carbetocin can result in an excessive uterine contraction, which can lead to uterine rupture. Additionally, it is important to note that the maximum recommended dose of Carbetocin is 500 mcg over a 24-hour period.

Precautions

Carbetocin should not be used in individuals with hypothyroidism, adrenal insufficiency, hypertension, cardiac disorders, and hepatic impairment. Additionally, Carbetocin should not be used in individuals with previous cesarean delivery or induced labor. Finally, special caution should be taken when administering Carbetocin to geriatric patients or those with high-risk factors for adverse reactions.

Interaction

Carbetocin is known to interact with antidiuretic hormones such as vasopressin and methothine, as well as with drugs used to treat hypertension and diabetes.

Disease Interaction

Carbetocin is contraindicated in individuals with congenital or acquired uterine abnormalities, as it can cause uterine rupture. Additionally, it is contraindicated in individuals with oligohydramnios, postpartum infection, and prior myocardial infarction.

Drug Interaction

Carbetocin is known to interact with drugs used in the treatment of hypertension, diabetes, and antidiuretic hormones. Therefore, it is recommended to closely monitor the patient's response and blood pressure when administering Carbetocin in combination with these drugs.

Food Interactions

Carbetocin should be taken approximately 30 minutes before meal or 2 hours after meal. Additionally, antacid medications should not be taken within 2 hours of administering Carbetocin as they could interfere with absorption.

Pregnancy Use

Carbetocin is not recommended for use in pregnant women, as it has the potential to cause uterine contractions that could lead to uterine rupture. If necessary, it should be used in pregnant women only after careful consideration of the potential risks.

Lactation Use

Carbetocin should not be used in nursing mothers, as it is not known whether or not it is excreted in breast milk. If necessary, it should be used in nursing mothers only after careful consideration of the potential risks.

Acute Overdose

Carbetocin should not be used in excess of the recommended dose due to the possibility of excessive uterine contractions leading to uterine rupture. In case of acute overdose, supportive measures should be taken as necessary.

Contraindication

Carbetocin is contraindicated in individuals with congenital or acquired uterine abnormalities, as it can cause uterine rupture. Additionally, it is contraindicated in individuals with hypothyroidism, adrenal insufficiency, hypertension, cardiac disorders, hepatic impairment, prior myocardial infarction, oligohydramnios, and postpartum infection.

Use Direction

Carbetocin should be dissolved in 10 ml of sterile water prior to administration. The recommended dose is 2 mL (100 mcg), which should be administered intravenously at a rate of 1 mL per minute. It should not be administered intramuscularly or subcutaneously. The maximum dose is 500 mcg over a 24-hour period.

Storage Condition

Carbetocin should be stored in a cool (5°C - 30°C) and dry place away from direct sunlight or moisture.

Volume of Distribution

The volume of distribution of Carbetocin is not known.

Half Life

After intravenous administration, the elimination half life of Carbetocin is 3.7 hours.

Clearance

The clearance of Carbetocin is not known.

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