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StatPearls . Treasure Island (FL): StatPearls Publishing; 2020 Jan-.
Indications
The indication for the use of an alpha-receptor modifying medication depends on which receptor is the target: the alpha-1 receptor or the alpha-2 receptor. Alpha-1 receptors bind catecholamines including, both epinephrine and norepinephrine. In instances in which there is hypoperfusion secondary to decreased cardiac output or decreased systemic vasculature resistance, alpha-1 receptors become stimulated. It is worth noting that these compounds are not purely selective for the alpha receptor, and often engage beta-adrenergic receptors as well. The use of alpha-1 agonists is common in all types of shock, cardiopulmonary resuscitation, and heart failure decompensation. Alpha-1 agonists, such as phenylephrine, are also used to treat upper airway congestion as stimulating the receptor leads to a decreased mucus secretion. Alpha-antagonists, colloquially known as alpha-blockers, work in the peripheral vasculature and inhibit the uptake of catecholamines in smooth muscle cells resulting in vasodilation and blood pressure lowering. Alpha-antagonists, including doxazosin, prazosin, and phentolamine – are primarily used in the treatment of hypertension and urinary retention.
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Alpha-blockers have significant use in the setting of pre-operative pheochromocytoma care. Alpha-blockers are also used off-label for the treatment of post-traumatic stress disorder (PTSD). Alpha-2 stimulation reduces the sympathetic outflow from the vasomotor center centrally and increases vagal tone. Peripheral presynaptic alpha-2 receptors may also reduce sympathetic tone. Alpha-2 agonists, including clonidine and guanfacine – are used as anti-hypertensives, as well.
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Both clonidine and guanfacine are used for behavior modification in children with attention deficit disorder, as well as in adults with PTSD as well.
Alpha-1 agonists
FDA approved indications
Oral agents
Midodrine
Treatment of symptomatic orthostatic hypotension
Topical agents
Naphazoline/naphazoline-pheniramine
Topical ocular vasoconstriction
Use for the relief of redness in the eye/itching (pheniramine)
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