sympathomimetics Flashcards
α adrenoreceptors have greater affinity for synthetic or natural catecholamines
natural
α1 higher affinity for phenylephrine or clonidine
phenylephrine(Clonidine selectively binds to α2 rec)
α1 is which g linked receptor
Gq
α2 is which g linked receptor
Gi
what is the location of α1 and α2 receptors?
α1 — post synaptic memberane of effector organs V.C (skin & abdominal viscera
α2 on presynaptic memberane and also on b cells of pancreas
functions of α1
vasoconstriction
mydriasis
urinary retention
glycogenolysis
Dec renin release
functions of α2
feedback inhibition of N.E release
insulin release reduction
β receptor — affinity for natural or synthetic catecholamines
synthetic
β1 — affinity for epi and N.E
Equal
β2 — affinity for epi and N.E
more for epi
action of β1
ACTION ON HEART
HR inc
Contractility inc
AV conduction inc
ACTION ON KIDNEY
Renin Inc
BP inc
β2 action
bronchodilation
Skeletal vasculature bed– vasodilation– p.r dec
insulin inc
gi motility dec
inhibition of labor
CNS penetration of Catecholamines
poor
why are catechlamines rapidly deactivated
rapid metabolization by COMT
Non Catecholamines: Amphetamine. Long duration →why?
Aren’t inactivated by COMT.
b) Poor substrates for MAO.
2. High CNS penetration.
what is the effect of epi on systolic BP
INCREASES
due to action on alpha 1 and Beta 1 receptors