Intramuscular, Intravenous Prophylaxis of postpartum haemorrhage due to uterine atony after vaginal delivery
Adult: 100 mcg as a single dose via slow IV inj over 1 minute or IM inj to be given as soon as possible after delivery of the infant, preferably before the removal of the placenta.
Intravenous Prophylaxis of postpartum haemorrhage due to uterine atony after caesarean section
Adult: Under epidural or spinal anaesthesia: 100 mcg as a single dose via slow IV inj over 1 minute to be given as soon as possible after delivery of the infant, preferably before the removal of the placenta.
Renal Impairment
Contraindicated.
Hepatic Impairment
Contraindicated.
Contraindications
Hypersensitivity to carbetocin or oxytocin. Serious CV disorders, epilepsy. Hepatic and renal impairment. The use of carbetocin at any stage prior to delivery of the infant is not appropriate due to its prolonged uterotonic effects that persist for several hours. Therefore, carbetocin must not be administered during pregnancy and labour before delivery of the infant for any reason (including electively or medically induced labour). Carbetocin should not be used for the induction of labour.
Special Precautions
Patient with eclampsia or pre-eclampsia, migraine, asthma, CV disease, or any state wherein rapid addition of extracellular water may cause a hazard for an overburdened system. Lactation.
Adverse Reactions
Significant: May produce antidiuretic effect, which may lead to the risk of hyponatraemia or water intoxication. Blood and lymphatic system disorders: Anaemia. Cardiac disorders: Tachycardia. Gastrointestinal disorders: Abdominal pain, nausea, vomiting, metallic taste. General disorders and administration site conditions: Feeling of warmth, chills, pain, pyrexia. Musculoskeletal and connective tissue disorders: Back pain, muscular weakness. Nervous system disorders: Headache, tremor, dizziness. Respiratory, thoracic and mediastinal disorders: Chest pain, dyspnoea. Skin and subcutaneous tissue disorders: Pruritus, diaphoresis. Vascular disorders: Hypotension, flushing.
Monitoring Parameters
Monitor patient for persistent postpartum bleeding; in case persistent vaginal or uterine bleeding occurs after administration, determine and consider the possible causes (e.g. retained placental fragments, genital tract lacerations, blood coagulation disorders). Closely monitor blood pressure, particularly in patients with eclampsia or pre-eclampsia.
Overdosage
Symptoms: Uterine hyperstimulation with strong (hypertonic) or prolonged (tetanic) contractions which may result in uterine rupture or postpartum haemorrhage. Hyponatraemia and water intoxication may also occur in severe cases. Management: Symptomatic and supportive treatment. Oxygen should be given. In case of water intoxication, restrict fluid intake, promote diuresis, correct electrolyte imbalance and control convulsions that may occur.
Drug Interactions
Severe hypertension may occur when given 3-4 hours after prophylactic administration of a vasoconstrictor in conjunction with caudal-block anaesthesia. May enhance the blood pressure enhancing effect of ergot alkaloids (e.g. methylergometrine). Prostaglandins may potentiate the effect of carbetocin. Certain inhalation anaesthetics (e.g. halothane, cyclopropane) may enhance the hypotensive effect and weaken the effect of carbetocin on the uterus.
Action
Description: Mechanism of Action: Carbetocin is a synthetic analogue of oxytocin with a longer duration of activity. It selectively binds to oxytocin receptors in the uterine smooth muscle, thereby stimulating rhythmic uterine contractions and increasing both the frequency of existing contractions and uterine tone. Additionally, it enhances uterine involution early in postpartum. Onset: 1.2 ± 0.5 minutes (IV). Duration: Approx 60 minutes (IV); approx 120 minutes (IM). Pharmacokinetics: Absorption: Bioavailability: 77% (IM). Time to peak plasma concentration: 30 minutes (IM). Distribution: Enters breast milk (small amount). Volume of distribution: 22 L. Excretion: Via urine (<1% as unchanged drug). Terminal elimination half-life: 33 minutes (IV); 55 minutes (IM).
Chemical Structure
Carbetocin Source: National Center for Biotechnology Information. PubChem Database. Carbetocin, CID=16681432, https://pubchem.ncbi.nlm.nih.gov/compound/Carbetocin (accessed on Jan. 21, 2020)
Storage
Vial: Store below 30°C. Do not freeze. Protect from light. Pre-filled syringe: Store between 2-8°C. Do not freeze. Protect from light.
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