Q.

Ou tli ne briefly t he ph ar ma co lo gy of o xyto ci n

Overview
•Oxytocin ---endogenous polypeptide hormone released from posterior pituitary----
synthesis from paraventricular cellof hypothalamus
•synthetic water soluble polypeptide of eight amino acid that used in obstetric parctice

Preparation
•Also available in synthretic form
•Syntocinon- synthetic oxytocin --Octapeptide used as synthetic preparation to cause
uterine constriction
•Prepared as syntocinon
•Available in 5 u/ml or 10 u/ml

Structures activity relationship

•? Octapeptide ---or ? nonapeptide

chemical compound
• syntheticly prepared oxytocin

synthesis
• identical to ---natural hormone ---secreted from posterior pituitary
• not secreted from posterior pituitary

Formula structure

structure activity relationship

• naturally occuring nona, octa peptide
• comprised of S-S bond----imporatant for activity

combination of compound
• synthetic oxytocin---can be combine with ergot
• ergot---alkaloid from fungus
• combination of oxytocin and ergot---known as syntocinon

Mechanism of action
drug target
•smooth muscle cell receptor

drug action bind to receptor

•smooth muscle receptor activated----increase in permeability to K+
•effect –decerase membrane potential
•increase excitability of uterine smooth muscle
•effect coordinated , regular uterine
•Action on gravid uterus and breast milk duct

Clinical use
Augmentation of labour
•Used in obstetric to cause uterine constriction
•Uterine constriction ---as induction of labour

Post-partum
•Uterine contraction post-delivery
•Also to prevent PPH

Lactation
•To induce lactation

Dose and administration

• Onset – 30 sec- 1 minutes – IV, 2 minutes - Im
• Duration of action – 3-5 minutes IV, IM – 60 minutes

Pharmacokinetic
Absorbtion
•Poor oral bioavailibility
•Reason; inactivation by chymotripsin as a first pass effect
•Has to be administered parentally
•Also can be given, intranasal

Pharmacodynamic
CVS
HR
•Tachycardia ---then hypotension ---non-specific ST changes

SVR
•Causes vasodilation ---manifestated as flushing
•Vasodilation ---decrease SVR---hypotension

BP
•Hypotension ----initiate baroceptor reflex
•Baroreceptor reflex ---reflex tachycardia---net increase in cardiac output
•Anesthetic implication ---further aggravate hypotension produced by concurrent
anesthetic agent
Other
•Has very little antiduretic action
•But may cause water intoxication after prolonged infusion particularly if given with 50%
dextrose

Drugs interaction
Suxamethonium
•Antagozed effect of sux

Blood transfusion
•Inactivated with blood transfusion

Contraindication

Adverse effect
Placental blood flow
Foetal well being

HEMABATE

Why do you use oxytocin but not ergometrine for induction of labour
Where does ergot come from? Fungus