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Adrenergic Pharmaco3

Qs and As about adrenergic pharmacology

QuestionAnswer
What kinds of drugs cause mydriasis? Alpha-1 agonists and alpha-2 antagonists
Mydriasis = Pupillary dilation due to contraction of pupillary dilator (radial) muscle
Miosis = Pupillary constriction due to contraction of circular pupillary muscle
What drugs are selective alpha-1 agonists? Phenylephrine and Methoxamine
Uptake I Reuptake of neurotransmitter into presynaptic varicosity via transporters
Uptake II Uptake of neurotransmitter into postsynaptic cell via receptors
Autoreceptor Presynaptic receptors that provide negative feedback: activated by neurotransmitter (NT) released into synaptic cleft; inhibit further NT release from presynaptic cell
Major effects of ACTIVATING beta-2 adrenergic receptors (5) RELAXATION 1. Increase cAMP 2. Vasodilation of vascular smooth m. 3. Relax smooth m (bladder, bronchi, uterus) 4. Increase insulin release 5. Increase glycogenolysis
Major effects of ACTIVATING beta-1 adrenergic receptors (4) EFFECTS ON HEART 1. Increase cAMP 2. Increase chronotropy (heart rate) 3. Increase inotropy (force of contraction) 4. Increase dronotropy (conduction velocity)
Major effects of ACTIVATING alpha-2 adrenergic receptors (4) 1. Some constriction of vascular smooth muscle (extrajunctional R's) 2. Platelet aggregation 3. Inhibit insulin secretion 4. INHIBIT CATECHOLAMINE RELEASE FROM PRESYNAPTIC NEURONS --> OVERALL DECREASE IN SYMPATHETIC TONE
Major effects of ACTIVATING alpha-1 adrenergic receptors (5) 1. (+)PIP2-->IP3-->PKC--> incr intracellular Ca2+ 2. Vasoconstriction --> incr BP 2. Smooth m. constriction (bladder, uterus, bronchi) 3. Pupillary dilator m. constriction --> mydriasis 4. Downregulate renin-angiotension 5. Increase glycogenolysis
What is the one receptor type that is ACTIVATED by epinephrine but is NOT ACTIVATED by norepinephrine? Beta-2 receptors
What drugs are selective alpha-2 agonists? Clonidine (pre- and postsynaptic) and Methyldopa (presynaptic only)
What drugs are nonselective alpha receptor agonists? Epinephrine, Norepinephrine (also have beta agonist effects)
Three drugs that prevent reuptake (uptake I) at presynaptic adrenergic varicosities: Amphetamine, Cocaine, Guanethidine
Why do cocaine and amphetamine have opposite effects of guanethidine? All 3 drugs prevent uptake I. Guanethidine also displaces NE from presynaptic vesicles leading to depletion. Cocaine + amphetamine increase extracellular [NE] without promoting degradation. (Amphetamine is also a weak MAO inhibitor)
Created by: eemolee27
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