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FIU - Alpha blockers and agonists
Alpha blockers and agonists
25
Pharmacology
Professional
01/03/2012

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Term
Phentolamine, mode of action, effect, use, avoid?
Definition
Non-selective alpha receptor blocker, causes vasodilation and drop in bp, emergency use for very high blood pressure that includes non-functional precapillary sphincters, leading to edema seen in pheochromocytoma (catecholamine secreting tumors); avoid beta blockers to lower bp (with cocaine induced HTN too) because opens constricting alpha receptors to increased catecholamines.
Term
Effect of overstimulation of alpha receptor?
Definition
Acute urine retention due to G protein activation, leading to increase IP3 and DAG, leading to increase in cytosolic Ca.
Term
Alpha-1A receptor blocker effect? Type of Alpha-1 receptors in prostate?
Definition
Called uroselective blockers, used for relief of lower urinary tract symptoms (LUTS) due to bladder outlet obstruction (BOO) and Benign Prostatic Hypertrophy (BPH); 70% alpha receptors in prostate are alpha 1A, rest 1D.
Term
Doxasosin mode of action, selectivity, use, side effects, derived from?
Definition
selective alpha 1 blocker but non-uroselective; used for BPH symptoms; SE: orthostatic hypotension; quinozoline derivative
Term
Terazosin mode of action, selectivity, use, side effect, derived from?
Definition
selective alpha 1 blocker but non-uroselective; used for BPH symptoms; SE: orthostatic hypotension; quinozoline derivative
Term
Alfuzosin mode of action, use, selectivity, use, derived from
Definition
selective alpha 1 blocker and fuctionally uroselective (more selective for alpha 1A than other drugs; used for BPH symptoms; quinozoline derivative
Term
Tamsulosin mode of action, use, selectivity, use, derived from, brand name
Definition
selective alpha 1A blocker and uroselective; used for BPH symptoms; sulfone-methyl-amine derivative, Flomax
Term
Silodosin mode of action, use, selectivity, use, advantage, brand name
Definition
selective alpha 1A blocker and highly uroselective; used for BPH symptoms; No orthostatic hypotension (lack of effect in vasculature); Rapaflo
Term
How are alpha 1 selective but non-uroselective drugs marketed?
Definition
To lower BP and address BPH symptoms in older males.
Term
alpha 2 receptors location? controls? effect? side effects?
Definition
Presynaptic; controls neurotransmitter release; shuts down sympathetic nervous system (analgesia and sedation); SE: dry mouth and parotid pain
Term
imitazol 1 receptors location? controls? effect? side effects?
Definition
Presynaptic; controls neurotransmitter release; shuts down sympathetic nervous system/allows parasympathetic NS to dominate (lowers bp); SE: bradycardia, constipation (strange because not parasympathetic effect), water retention (co-administer diuretic).
Term
clonidine and clonidine-like drugs mode of action
Definition
centrally acting alpha 2 and imidazoline 1 receptor agonists
Term
-osin
Definition
selective alpha 1 blocker
Term
alpha-methyldopa mode of action, use
Definition
centrally acting alpha 2 selective agonist (also a competitive inhibitor of DOPA decarboxylase which reduces production of all catecholamines lowering sympathetic effects in peripheral NS) aka clonidine-like; and used to lower bp during pregnancy (category B)
Term
clonidine mode of action, use, side effect? ending
Definition
centrally acting agonist at both alpha 2 and imadazoline receptors; lowers bp; as IV some activation of alpha 1 receptors = vasoconstriction; -nidine or -midine except methyldopa
Term
dex-medetomidine mode of action; use
Definition
centrally acting alpha 2 agonist only; sedative anxiolytic (antianxiety) w/o respiratory depression
Term
moxonidine mode of action, effect; use
Definition
centrally acting, selective imidazoline 1 receptor agonist ;decreases sympathetic nervous system activity; used to lower bp
Term
clonidine-like drug side effects?
Definition
sedation, dry mouth and nasal mucosa, bradycardia, orthostatic hypotension, impotence, constipation/nausea/gastric upset, fluid retention and edema (concurrent thiazide diuretic necessary), rebound hypertension
Term
Peripherally acting alpha 1 receptor agonist uses
Definition
for hypotensive states (vasoconstriction), as a mydriatic (pupil dilation), nasal decongestant (constricts capillaries in sinuses)
Term
oxymetazoline mode of action, use
Definition
peripheral alpha 1 agonist; nasal decongestant
Term
xylometazoline mode of action, use
Definition
peripheral alpha 1 agonist; nasal decongestant and mydriatic
Term
phenylephrine mode of action, use, brand name
Definition
peripheral alpha 1 agonist; nasal decongestant, Sudafed
Term
norepinephrine mode of action, effect, overdose effect?
Definition
more selective as alpha receptor agonist; vasoconstriction; have a bp but not perfusion
Term
ephinephrine mode of action, effect
Definition
more selective as beta receptor agonist; inotrophic
Term
alpha 1 agonist side effects? Suggested use?
Definition
headache, reflex bradycardia, excitability and restlessness, increased afterload (work of heart), angina if coronary artery disease, nasal decongestant rebound effect: receptor reuptake. ALSO: nasal vasoconstriction -> systemic uptake -> systemic vasoconstriction -> acidosis -> vasodilation (causes headache); Don't use continuously
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