Term
| Phentolamine, mode of action, effect, use, avoid? |
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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. |
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Term
| Effect of overstimulation of alpha receptor? |
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Definition
| Acute urine retention due to G protein activation, leading to increase IP3 and DAG, leading to increase in cytosolic Ca. |
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Term
| Alpha-1A receptor blocker effect? Type of Alpha-1 receptors in prostate? |
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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. |
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Term
| Doxasosin mode of action, selectivity, use, side effects, derived from? |
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Definition
| selective alpha 1 blocker but non-uroselective; used for BPH symptoms; SE: orthostatic hypotension; quinozoline derivative |
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Term
| Terazosin mode of action, selectivity, use, side effect, derived from? |
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Definition
| selective alpha 1 blocker but non-uroselective; used for BPH symptoms; SE: orthostatic hypotension; quinozoline derivative |
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Term
| Alfuzosin mode of action, use, selectivity, use, derived from |
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Definition
| selective alpha 1 blocker and fuctionally uroselective (more selective for alpha 1A than other drugs; used for BPH symptoms; quinozoline derivative |
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Term
| Tamsulosin mode of action, use, selectivity, use, derived from, brand name |
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Definition
| selective alpha 1A blocker and uroselective; used for BPH symptoms; sulfone-methyl-amine derivative, Flomax |
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Term
| Silodosin mode of action, use, selectivity, use, advantage, brand name |
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Definition
| selective alpha 1A blocker and highly uroselective; used for BPH symptoms; No orthostatic hypotension (lack of effect in vasculature); Rapaflo |
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Term
| How are alpha 1 selective but non-uroselective drugs marketed? |
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Definition
| To lower BP and address BPH symptoms in older males. |
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Term
| alpha 2 receptors location? controls? effect? side effects? |
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Definition
| Presynaptic; controls neurotransmitter release; shuts down sympathetic nervous system (analgesia and sedation); SE: dry mouth and parotid pain |
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Term
| imitazol 1 receptors location? controls? effect? side effects? |
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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). |
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Term
| clonidine and clonidine-like drugs mode of action |
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Definition
| centrally acting alpha 2 and imidazoline 1 receptor agonists |
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Term
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Definition
| selective alpha 1 blocker |
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Term
| alpha-methyldopa mode of action, use |
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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) |
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Term
| clonidine mode of action, use, side effect? ending |
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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 |
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Term
| dex-medetomidine mode of action; use |
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Definition
| centrally acting alpha 2 agonist only; sedative anxiolytic (antianxiety) w/o respiratory depression |
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Term
| moxonidine mode of action, effect; use |
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Definition
| centrally acting, selective imidazoline 1 receptor agonist ;decreases sympathetic nervous system activity; used to lower bp |
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Term
| clonidine-like drug side effects? |
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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 |
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Term
| Peripherally acting alpha 1 receptor agonist uses |
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Definition
| for hypotensive states (vasoconstriction), as a mydriatic (pupil dilation), nasal decongestant (constricts capillaries in sinuses) |
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Term
| oxymetazoline mode of action, use |
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Definition
| peripheral alpha 1 agonist; nasal decongestant |
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Term
| xylometazoline mode of action, use |
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Definition
| peripheral alpha 1 agonist; nasal decongestant and mydriatic |
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Term
| phenylephrine mode of action, use, brand name |
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Definition
| peripheral alpha 1 agonist; nasal decongestant, Sudafed |
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Term
| norepinephrine mode of action, effect, overdose effect? |
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Definition
| more selective as alpha receptor agonist; vasoconstriction; have a bp but not perfusion |
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Term
| ephinephrine mode of action, effect |
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Definition
| more selective as beta receptor agonist; inotrophic |
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Term
| alpha 1 agonist side effects? Suggested use? |
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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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