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- D. ALPHA RECEPTOR BLOCKING DRUGS <tab5-2>
-
- 1. Prazosin: Prazosin is an a1-selective blocking drug. It is much more
- useful for the treatment of hypertension than the less selective α-
- blockers phentolamine and phenoxybenzamine because it evokes little if
- any reflex tachycardia. Prazosin has also been used in the treatment of
- congestive heart failure (see Chapter 4). Terazosin is a newer, somewhat
- longer-acting a1-selective agent. Its therapeutic and adverse effects
- are very similar to those of prazosin.
- Indications:
- * Hypertension.
- * Congestive heart failure (unlabeled).
- * Raynaud's syndrome (unlabeled).
- Contraindications, Adverse Reactions, and Overdose Toxicity:
- * Severe postural hypotension after the first dose especially in
- hypovolemic (eg, diuresed) patients. Syncope may result. The effect is
- best managed by starting therapy with the minimum dose (1 mg) ad-
- ministered just after going to bed. The effect usually diminishes rapid-
- ly after the first dose and the dosage can then be incremented as re-
- quired.
- * Dizziness, headache, and sedation occur in 5-10% of patients at the
- start of therapy, diminishing thereafter.
- * Fluid retention often occurs in patients not also treated with a
- diuretic.
- * Overdose: Hypotension and CNS depression have been reported.
- Interactions: The drug would be expected to have additive effects with
- all other antihypertensive agents.
-
- 2. Phenoxybenzamine: Phenoxybenzamine is an irreversible α-receptor
- blocker. It produces a powerful but nonselective sympathoplegia; com-
- pensatory responses include tachycardia and fluid retention.
- Indications:
- * Pheochromocytoma
- * Reduction of urinary bladder sphincter tone in urinary bladder dis-
- orders (unlabeled). Contraindications and warnings:
- * Orthostatic hypotension (warning), especially if it would result in
- risk of stroke or myocardial ischemia (true of all hypotensive agents).
- Adverse effects and Overdosage Toxicity:
- * Excessive alpha sympathetic blockade: hypotension, nasal congestion,
- miosis, and impairment of ejaculation.
- * Nausea, vomiting, diarrhea.
- * Sedation.
-
- 3. Phentolamine: Phentolamine is a competitive alpha receptor blocking
- drug. It is not selective for α1 or α2 receptors.
- Indications:
- * Treatment of acute hypertensive reactions in patients with
- pheochromocytoma. It is also approved for use as a provocative test for
- pheochromocytoma, although this test is hazardous (because of the risk
- of excessive hypotensive response) and has been superseded by measure-
- ment of urinary or plasma catecholamines and their metabolites.
- Phentolamine is also labeled for the treatment of tissue necrosis due to
- extravasation of norepinephrine or dopamine.
- * Management of hypertensive crises arising from excessive
- sympathomimetic action as in MAO inhibitor drug reactions and rebound
- hypertension following clonidine withdrawal (unlabeled).
- Contraindications and warnings: Same as for phenoxybenzamine.
- Adverse effects:
- * Sympathoplegic adverse effects, similar to those listed for
- phenoxybenzamine but shorter in duration (15 min to 2 hr as compared to
- 24 to 48 hr for phenoxybenzamine).
- * Gastrointestinal stimulation with increased acid secretion, nausea,
- vomiting, and diarrhea.
- * Overdose is characterized by transient hypotension that can usually be
- managed by administration of fluids.
-