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43 Cards in this Set
- Front
- Back
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alpha 1 receptor distribution
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- arteriole + vein smooth muscle
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alpha 2 receptor distribution
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- presynaptic adrenergic nerve terminals
- coronary + renal arteriole smooth muscle |
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beta 1 receptor distribution
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- Heart
- Kidney JG cells - presynaptic adrenergic nerve terminals - adipose tissue |
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beta 2 receptor distribution
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- vascular smooth muscle (EXCEPT skin + brain)
- bronchial smooth muscle - liver |
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alpha 1 agonist response
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- **vasoconstriction**
- close sphincters in bladder + urethra - dilate pupil (mydriasis) |
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alpha 2 agonist response
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- **inhibition of NE release**
- **vasoconstriction** - inhibit sympathetic neurotransmission (at presynaptic) |
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Beta 1 agonist response
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- increase HR
- increase contractility - increase AV node conduction speed - increase renin release - increase NE release - stimulate lipolysis |
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Beta 2 agonist response
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- vasodilation
- bronchodilation - uterine, bladder relaxation - pupil constriction (eye dilator muscle relax) - stimulate glycogenolysis (+other hypoglycemic responses) |
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Alpha 2 agonist clinical uses
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- blood pressure lowering
- sedation |
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list alpha agonists in order from greatest a1 effect => greatest a2 effect
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a1>a2 =>=>=>=> a2>a1
Norepinephrine | Epinephrine | Dopamine | alpha-Methyldopa | Clonidine | Dexmedetomidine |
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alpha 2 agonist adverse effects
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- sedation
- dry mouth - bradycardia - rebound withdrawal (esp clonidine) |
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Reserpine MoA + effects?
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- inhibit NE uptake to storage vesicles
- decrease peripheral resistance - decrease myocardial contractility =>=> sedation, decreased blood pressure |
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alpha-1 receptor antagonist effects
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- antihypertensive
- less reflex tachycardia than non-selective agents |
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Beta-1 receptor blocker effects
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- reduced heart rate
- slow AV nodal conduction - decrease BP |
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Beta 2 receptor blocker effects
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- bronchoconstriction
- inhibit hypoglycemic response (liver activity, decreased GI motility) - vasoconstriction |
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Beta 2 receptor indications
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- CAD (angina, MI)
- tachyarrhythmia - CHF - Hypertension - hypertrophic cardiomyopathy - alcohol withdrawal - hyperthyroidism - glaucoma - pheochromocytoma - varices - tremor - prophylaxis for vascular headaches |
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Nonselective Beta-blockers
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Carvedilol
Labetalol Propranolol Nadolol Timolol |
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Selective Beta blockers
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Atenolol
Betaxolol Bisoprolol Esmolol Metoprolol Nebivolol |
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Beta-blocker adverse effects
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- bradycardia
- CHF - hypotension - conduction problems - bronchospasm - withdrawal - lipid alterations - Hypoglycemia/hyperglycemia - Raynaud's - Peripheral Vascular Disease - Sexual dysfunction |
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Propranolol metabolism?
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first-pass
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Site of metoprolol metabolism?
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Liver
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Site of Atenolol metabolism?
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Kidneys
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Atenolol trade name
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Tenormin
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Tenormin is?
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Atenolol
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Lopressor is?
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Metoprolol
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Propranolol trade name?
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Inderal
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Inderal is?
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Propranolol
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Propranolol selectivity?
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non-selective
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Propranolol duration of action?
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- short AND long-acting forms available
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Atenolol specificity?
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B1-specific
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Metoprolol specificity?
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B1-specific
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Atenolol duration of action?
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Long
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Metoprolol duration of action?
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Long
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Nadolol trade name?
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Corgard
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Esmolol trade name?
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Brevibloc
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Nadolol site of metabolism?
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Renal elimination
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Esmolol duration of activity?
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Short , IV only, critical care use, HL = 9 min
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Labetolol trade name?
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Normodyne
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Normodyne is?
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Labetalol
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Corgard is?
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Nadolol
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Brevibloc is?
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Esmolol
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Which Beta-blocker also has a-1 blocker activity?
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Labetalol
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carvedilol trade name?
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Coreg
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