Adrenergics Flashcards
What is the signal transduction pathway for beta receptors
Accumulate cAMP and activate PKA
What is the signal transduction pathway for alpha 2 receptors
Decrease cAMP and inhibit PKA
What are the three mechanisms of action for indirect acting adrenergic drugs?
Reuptake blocker (cocaine), MAO inhibitor (selegine, phenelzine), and releasing agents (Amphetamines, methylphenidate)
What alpha adrenergic agonists prefer a1>a2?
phenylephrine, methoxamine
What alpha adrenergic agonists prefer a2>a1
Clonidine, methyNE
What is the receptor selectivity for NE
a1=a2; B1>B2
What is the receptor selectivity for epinephrine?
a1=a2; B1=B2
What beta adrenergic agonists prefer B1>B2
Dobutamine
What Beta adrenergic agonists select both B R equally
isoproterenol
What Beta adrenergic agonists prefer B2»B1
Albuterol, terbutaline, ritodrine
What Dopamine agonists prefer D1 & D2 equally
dopamine
What dopamine receptor agonists prefer D1»D2
Fenoldopam
What are the effects of epinephrine and the corresponding receptor?
Cardiac function - B1 - increase HR, contractility
Vascular tone - B2, a1 - inc systolic BP, same MAP
Respiratory - B2 - relax s. m. - a1 - dec secretion, congestion
skeletal m - B2 - tremor, inc K uptake
Elevate Blood Glucose - B2- inc liver glycogenolysis - a2/B2 - inhibit insulin release
Increase blood FFA - B
Increase renin release - B1
What are the effects of NE and the corresponding receptor
Cardiac stimulation - B1 - pump harder but dec HR
Potent vasoconstriction - a1
Why does NE decrease HR
The rise in BP is detected by the baroreceptors, which tell the hard to pump slower
What are the effects of dopamine and what are the corresponding receptors
vasodilation of the renal, cerebral, mesenteric, coronary a. - D1
Activation presynaptic D2 - suppress NE release
What is the signal transduction pathway for alpha 1 R
IP3, DAG, MAPK, PI3K,
These stimulate cell growth
What is the effects of phenylephrine
a1>a2. mydriasis (pupillary dilation), decongestion, severe vasoconstriction (inc BP)
What happens to phenylephrine is you block the baroreflex
The drug is 10x more potent on vasoconstriction
What are the effects of clonidine
a2>a1. Central effect on the a2 receptors in the brainstem, which decreases NE output –> lower BP and HR
What are the effects of isoproterenol
B1=B2. Increase cardiac output (B1), vasodilation / bronchodilation (B2). Therefore keeping BP about the same
What are the effects of dobutamine
B1>B2. Increase cardiac output
What are the effects of terbutaline, albuterol
B2>B1. Bronchodilation, relax uterus
Are indirect adreneric agonists polar or nonpolar
nonpolar