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Q.Outline briefly the pharmacology of oxytocin
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 parcticePreparation
Also available in synthretic form
Syntocinon- synthetic oxytocin --Octapeptide used as synthetic preparation to causeuterine constriction
Prepared as syntocinon
Available in 5 u/ml or 10 u/mlStructures activity relationship
? Octapeptide ---or ? nonapeptidechemical compound
syntheticly prepared oxytocinsynthesis
identical to ---natural hormone ---secreted from posterior pituitary
not secreted from posterior pituitaryFormula structurestructure activity relationship
naturally occuring nona, octa peptide
comprised of S-S bond----imporatant for activitycombination of compound
synthetic oxytocin---can be combine with ergot
ergot---alkaloid from fungus
combination of oxytocin and ergot---known as syntocinonMechanism of actiondrug target
 
smooth muscle cell receptordrug 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 ductClinical useAugmentation of labour
Used in obstetric to cause uterine constriction
Uterine constriction ---as induction of labourPost-partum
Uterine contraction post-delivery
Also to prevent PPHLactation
To induce lactationDose and administration
Onset – 30 sec- 1 minutes – IV, 2 minutes - Im
Duration of action – 3-5 minutes IV, IM – 60 minutesPharmacokineticAbsorbtion
Poor oral bioavailibility
Reason; inactivation by chymotripsin as a first pass effect
Has to be administered parentally
Also can be given, intranasalPharmacodynamicCVSHR
Tachycardia ---then hypotension ---non-specific ST changesSVR
Causes vasodilation ---manifestated as flushing
Vasodilation ---decrease SVR---hypotensionBP
Hypotension ----initiate baroceptor reflex
Baroreceptor reflex ---reflex tachycardia---net increase in cardiac output
Anesthetic implication ---further aggravate hypotension produced by concurrentanesthetic agent
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