Adrenergic agonists Flashcards
Second messenger system of alpha 1
Coupled to PLC in vascular smooth muscle. Gaq stimulates PLC, releasing IP3 and DAG. IP3 signals for more intracellular calcium -> increased contraction and vasoconstriction
Second messenger system of alpha 2
Inhibits AC, reduces cAMP, reducing PKA activation. Less calcium influx during membrane depol and decreased release of NT.
Also causes vasoconstriction through blockade of MLCK phosphorylation, allowing for MLCK to remain active and cause vasoconstriction.
Second messenger system of beta 1
Adenylyl cyclase increases cAMP, activates PKA, phosphorylates calcium channels for increased inward calcium current and faster nodal cell depolarization. Also increases L-type calcium channels, releasing more calcium each time the heart pumps.
Order of affinity for A1
epi>NE»isoproterenol
Order of affinity for A2
epi>NE»isoproterenol
Order of affinity for B1
isoproterenol>epi=NE
Order of affinity for B2
isoproterenol>epi»NE
Differing affinities at different concentrations of epinephrine
At low doses, it has more affinity for beta receptors. Alpha effects will mask this at higher concentrations.
Toxicity of epinephrine
Arrhythmias
Toxicity of norepinephrine
Ischemia
Toxicity of dopamine
Hypotension at low rates
Ischemia at high rates
Toxicity of isoproterenol
Tachyarrhythmias
Toxicity of terbutaline/albuterol
Tremor
Tachycardia
Tolerance
Toxicity of phenylephrine
Hypertension
Toxicity of clonidine
Dry mouth
Hypertensive crisis after acute withdrawal