FRCA Notes


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
  • 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

  • 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