Konorev Adrenergic Agonist Drugs Flashcards
Which drugs are direct alpha agonists?
Phenylephrine, Clonidine
Which drugs are direct mixed agonists?
Norepinephrine, Epinephrine
Which drugs are direct ß agonists?
Dobutamine, Isoproterenol, Terbutaline, Albuterol
Which drugs are direct DA agonists?
Dopamine, Fenoldopam
What type of GPCR are alpha1 receptors associated with?
Gq
What type of GPCR are alpha2 receptors associated with?
Gi
What type of GPCR are ß receptors associated with?
Gs
What type of GPCR are D1 and D5 receptors associated with?
Gs
What type of GPCR are D2-D4 receptors associated with?
Gi
What are the major effects of activation of alpha1 receptors?
Vascular contraction, pupillary dilator m. contraction (dilation), increased heart contraction, prostate contraction
What are the major effects of activation of alpha2 receptors?
Platelet aggregation, inhibition of NT release, vascular contraction, inhibition of lipolysis
What are the major effects of activation of ß1 receptors?
Increase force/rate of heart contraction, increase renin release
What are the major effects of activation of ß2 receptors?
SM relaxation, increased K+ uptake in SkM, activation of gluconeogenesis/glycogenolysis
What are the major effects of activation of ß3 receptors?
Relax detrusor m., activate lipolysis
What is the major effect of activation of D1 receptors?
Dilation of renal blood vessels
What is the major effect of activation of D2 receptors?
Modulate NT release from nerve endings
Which receptor(s) does Epinephrine activate? What are the major effects of Epinephrine?
alpha1 = alpha2, ß1 = ß2; Increase HR/contraction force, increase systolic BP, relax bronchial SM, increase K+ uptake in SkM (m. tremors), increase glycogenolysis/gluconeogenesis
Which receptor(s) does Norepinephrine activate? What are the major effects of Norepinephrine?
alpha1 = alpha2, ß1; Vasoconstriction, increase cardiac contraction but reduce HR, increase PVR
Which specific receptor does Nepi not activate and what is the effect of that?
ß2, no bronchodilation and vasodilation
Which receptor(s) does Phenylephrine activate? What are the major effects of Phenylephrine?
alpha1 > alpha2; Mydriasis, vasoconstriction, increased BP, bradycardia
Which receptor(s) does Clonidine activate? What are the major effects of Clonidine?
alpha2 > alpha1; Decreases SNS activity by acting at level of brainstem; decreases BP, bradycardia
Which receptor(s) does Isoproterenol activate? What are the major effects of Isoproterenol?
ß1 = ß2; Increases CO, vasodilation, decrease arterial pressure, bronchodilation
Which receptor(s) does Dobutamine activate? What are the major effects of Dobutamine?
ß1; Inotropic actions
Which receptor(s) do Terbutaline and Albuterol activate? What are the major effects of Terbutaline and Albuterol?
ß2; Bronchodilation, uterine relaxation
Which receptor(s) does Dopamine activate? What are the major effects of Dopamine?
D1 = D2; D1 –> vasodilation of renal vasculature, D2 –> suppress Nepi release