Term
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Definition
-non-selective A receptor antagonist
-also blocks acetylcholine, histamine, and serotonin
-irreversible antagonist resulting from covalent modification of receptor
-administration: oral
-uses: pheochromocytoma, hypertensive crisis |
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Term
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Definition
-non-selective A receptor antagonist
-competitive (reversible) blocker
-potent vasodilator, but induces pronounced reflex tachycardia
-block of presynaptic A2 receptors may promote release of NE
-also blocks 5-HT receptors, and is a muscarinic and histamine receptor agonist
-administration:parenteral
-uses: pheochromocytoma, hypertensive crisis |
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Term
| Prazosin, Terazosin, Doxazosin |
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Definition
-A1 receptor antagonists
-"Quinazolines"
-vary in half life: prazosin 3 hrs, terazosin 12 hrs, doxazosin 20 hrs.
-undergo extensive metabolism, excreted mainly in the bile
-vasodilators
-relaxation of smooth muscle in enlarged prostate and in bladder base
-"first dose" effect
-administration: oral
-uses: hypertension, BPH |
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Term
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Definition
-A receptor antagonist
-derivatives of Lysergic Acid
-product of the grain fungus Claviceps purpura
-5 major alkaloids based on R and R'; Ergotamine the most common
-used in treatment of migraine
-Ergots possess strong oxytocic action |
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Term
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Definition
-A2 receptor antagonist
-indole alkaloid
-found in Rubaceae and related trees. Also in Rauwolfia Serpentina
-blockade of A2 receptors increases sympathetic discharge
-folklore suggests use in the treatment of male impotence |
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Term
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Definition
-non-selective B antagonist
-lipophilic
-local anesthetic properties
-blockade is activity-dependent
-pharmacologic effects: decreased cardiac output and heart rate, reduced renin release, increase VLDL, decrease HDL, inhibit lipolysis, inhibit compensatory glycogenolysis and glucose release in response to hypoglycemia, increase bronchial airway resistance |
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Term
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Definition
-non-selective B receptor antagonist
-less lipophilic than propranolol
-long half life: ~20 hours
-mostly excreted unchanged in urine
-administered: oral
-uses: hypertension angina, migraine |
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Term
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Definition
-non-selective B receptor antagonist
-thiadiazole nucleus with morpholine ring
-administered: oral, opthalmic
-uses: hypertension, angina, migraine, glaucoma |
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Term
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Definition
-non-selective B receptor antagonist
-possesses "intrinsic sympathomimetic activity" (ISA)
-non-selective B partial agonist
-less likely to cause bradycardia and lipid abnormalities
-administered: oral
-uses: hypertension, angina, migraine |
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Term
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Definition
-non-selective B receptor antagonist
-possesses "Intrinsic sympathomimetic activity" (ISA)
-non-selective B partial agonist
-less likely to cause bradycardia and lipid abnormalities
-administered: oral, opthalmic
-uses: hypertension, glaucoma |
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Term
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Definition
-selective B1 receptor antagonist
-"cardioselective"
-less bronchoconstriction
-moderate lipophilicity
-half-life: 3-4 hours
-significant first-pass metabolism
-administered: oral, parenteral
-uses: hypertension, angina, antiarrhythmic, congestive heart failure |
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Term
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Definition
-selective B1 receptor antagonist
-"cardioselective"
-less bronchoconstriction
-low lipophilicity
-half-life: 6-9 hours
-administered: oral, parenteral
-uses: hypertension, angina |
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Term
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Definition
-selective B1 receptor antagonist
-very short acting
-rapid hydrolysis by esterases found in red blood cells
-administered: parenteral; note: incompatible with sodium bicarbonate
-uses: supraventricular tachycardia, atrial filbrillation/flutter, perioperative hypertension |
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Term
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Definition
-non-selective B receptor antagonist
-A1 receptor antagonist
-two asymmetric carbons (1 and 1')
-(1R,1'R)-isomer possesses B blocking activity
-(1S,1'R)-isomer possesses greatest A1 receptor blocking activity
-B blocking activity prevents reflex tachycardia normally associated with A1 receptor antagonists
-administered: oral, parenteral
-uses: hypertension, hypertensive crisis |
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Term
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Definition
-non-selective B receptor antagonist
-A1 receptor antagonist
-both enantiomers antagonize A1 receptors
-only (S)-enantiomer possesses B blocking activity
-B blocking activity prevents reflex tachycardia normally associated with A1 receptor antagonists
-administered: oral
-uses: hypertension, congestive heart failure (types II and III) |
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Term
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Definition
-catecholamine depleter
-indole alkaloid obtained from the root of Rauwolfia serpentina
-block vesicular monoamine transporters
-deplete vesicular pool of NE
-slow onset of action
-sustained effect (weeks)
-used in treatment of hypertension
-may precipitate depression |
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Term
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Definition
-aromatic quaternary ammonium
-precise mechanism unknown
-displace and release NE and prevent further release (depletion)
-local anesthetic
-administered: parenteral
-uses: antiarrhythmic (ventricular fibrillation) |
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