Symphathomimetics Flashcards
Catecholamines
Metabolized rapidly, not effective orally, do not penetrate CNS readily
Epi, NE, Iso, DA, Dobutamine
Non-catecholamines
Alpha agonists Beta2 selective agonists Amphetamines, Tyramine (Indirect acting) Mixed acting Methylphenidate
Direct actions
Agonists of alpha or beta receptors
Indirect actions
Release NE or block NE reuptake
Mixed actions
May release NE but also act on receptor
Alpha 1 adrenergic effects
Constrict BV - increase BP Dilate pupils Contract spleen *Contract uterus Contract bladder sphincter Mild glycogenolysis in liver Ejaculation Erects hair
Alpha 2 adrenergic effects
*Inhibit insulin release
Relax GI smooth muscle
Autoreceptors inhibit release
CNS effects
Beta 1 adrenergic effects
Increase HR and CO
Stimulate Renin
Think heart
Beta 2 adrenergic effects
Relax bronchioles *Relax uterus Relax skeletal BV and coronary BV Glycogenolysis and lipolysis *Stimulate insulin and renin Relax bladder Relax GI smooth muscle
Reserpine
Blocks formation of NE
Cocaine
Blocks uptake of NE - increased NE in terminal (increase in BP)
Blocks uptake tyramine - decreased displacement of NE to terminal (no increase in BP)
Beta receptor G protein
Stimulates
Alpha receptor G protein
Inhibits
A1 and A2 catecholamine potency
Epi > NE > Iso
B2 catecholamine potency
Iso > Epi > NE
B1 catecholamine potency
Iso > Epi = NE
MAO
Destroys NE
Need to sequester so it isn’t destroyed
NE reuptake
Major mechanism of terminating signal
Dopamine effects
CNS neurotransmitter
D1 - increase renal blood flow
D2 - nerve endings
Baroreceptor response to increase BP (phenylephrine)
Increase firing
Increase parasympathetics at heart
Decrease sympathetics at BV
Baroreceptor response to decrease BP (histamine)
Decrease firing
Increase sympathetics at heart
Increase sympathetics at BV
Heart and Epi
Increase HR and CO
Increase work and consumption of energy
BV and Epi
Greater affinity for beta2 at low dose (vasodilate)
High dose, alpha1 dominates (vasoconstriction)
Skeletal and coronary dilate
Everything else except brain constricts