Drugs influencing uterine

contractility
Dr Thilanka seneviratne
MBBS, MD, DCH, MRCPCH
Senior Lecturer
Department of Pharmacology
 Objectives

• Describe the mechanism of action,

pharmacokinetics, adverse effects of
drugs influencing uterine contractility.
 Drugs causing uterine
contractions

• Oxytocin
• Ergometrine
• prostaglandines
 Ergometrine
• Ergot alkaloid
• Rapidly & completely absorbed after IM
injection
• Given IV., IM.
• Eliminated by liver
• Adverse effects
– Nausea, vomiting, hypertension
• Mechanism of action:
• Binds with alpha adrenergic receptors
• Increase intracellular calcium
• Cause myometrial contractions
 Ergometrine
• Sustained contraction of uterine smooth
muscle
• Uterine contractions occur immediately
after IV administration & last up to 45 min

• Used in PPH
Oxytocin
 Oxytocin
• Coordinated synchronous myometrial
contractions
• Induction of labour
• Half life 6 min; given as i.v. infusion
• Dose needed to be adjusted closely with
the uterine contractions.
• Heat-sensitive; needs cold storage

• Adverse effects
– Nausea, vomiting
– Water retention
 Carbetocin
• Heat-stable synthetic analogue of oxytocin
• Cold-chain transport & cold storage not
needed
 Prostaglandins
• Dinoprost (PGF2 alpha) dinoprostone (PGE2)
– Induction of labour
– Terminate pregnancy
– Vaginal gel, pessary, i.v.

– ADR: Vomiting, diarrhea, headache, pyrexia

• Carboprost (PG F2)
– PPH unresponsive to ergometrine &
oxytocin
– Deep i.m. injection
– ADR: hypertension, Asthma, pulmonary
oedema

• Gemeprost( PGE1)
• Vaginal gel, pessaries
• Induction of late therapeutic abortions
 Uterine relaxants
• To inhibit premature labour

• Oxytocin antagonists
– Atosiban (i.v. infusion)
– No major adverse effects

• β2 agonists
– Salbutamol, terbutaline, ritodrine (i.v. infusion)
– Tachycardia, hypokalaemia, hypotension,
– LVF
 Uterine relaxants
• Calcium channel blockers
– Nifedipine (oral)

• COX inhibitors
– Indomethacin (oral, POG < 32 weeks)

• Magnesium sulphate
– Crosses placenta
– Maternal neuromuscular blockade
 Summary
• Drugs causing uterine contractions act by
increasing intracellular calcium level in
myometrial cells by various pathways.
• Oxytocin, ergometrine, prostaglandins
cause uterine contractions.
• Beta adrenergic agonist, calcium channel
blockers cause uterine relaxation.
• Thank You