- As a colourless solution stored in glass vials containing 5IU/ml of syntocinon for use as an IV bolus or infusion
- As a colourless solution stored in glass vials containing 100μg/ml of carbetocin for use as an IV bolus
- In combination with ergometrine as syntometrine
Oxytocin analogues
Oxytocin analogues
- Oxytocin is a naturally occurring posterior pituitary octapeptide hormone which acts both centrally and peripherally
- It is an agonist at the oxytocin G-protein coupled receptor in the uterus, promoting calcium release and increase contractility
- Peripheral actions therefore include uterine contraction, as well as the let-down reflex involved in breastfeeding
- Therefore both short- (syntocinon) and long- (carbetocin) acting oxytocin analogues may be used in obstetric anaesthetic practice
- For the induction or augmentation of labour (IV infusion)
- To increase uterine tone following delivery to reduce bleeding inc. in the management of PPH
- Oxytocin: as either slow IV boluses (up to 10IU) or via infusion (40IU over 4hrs)
- Carbetocin: diluted up to 10ml in 0.9% NaCl and given as a slow IV bolus of up to 100μg
- Syntometrine: IM
- The ED90 of oxytocin is reportedly only 0.35IU, so our 5IU boluses are more than enough to cause contraction
- Rapid bolus administration may cause hypotension with marked compensatory tachycardia and increase in cardiac output
- May also cause ECG changes including ST segment, T-wave and QTc changes
- Due to its similarity with vasopressin it has a weak anti-diuretic effect that is only apparent with prolonged use
- May cause nausea and vomiting
- Increases renal blood flow in animal models
- Rash and/or anaphylaxis possible
- Overdose or toxicity can cause hyperstimulation ± uterine rupture
Absorption
- Inactivated by chymotrypsin when given orally so only available via parenteral routes
Metabolism
- Primarily hepatic and renal metabolism by oxytocinase enzymes
- Should not be co-administered with:
- Blood products as these may contain plasma oxytocinase which inactivate the drug
- Suxamethonium as it may reduce efficacy and increase dose requirements
Excretion
- Oxytocin has a short elimination half-life of 4mins (1 - 7mins), hence infusions may be required
- Carbetocin has a duration of action of up to 7x that of oxytocin