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Phenylephrine is a selective α 1-adrenergic receptor agonist with minimal to no β-adrenergic receptor agonist activity or induction of norepinephrine release. [5] [8] [15] It causes constriction of both arteries and veins. [12] Phenylephrine was patented in 1933 [16] and came into medical use in 1938. [17] It is available as a generic medication.
Alpha 2 receptors are associated with sympatholytic properties. Alpha-adrenergic agonists have the opposite function of alpha blockers . Alpha adrenoreceptor ligands mimic the action of epinephrine and norepinephrine signaling in the heart, smooth muscle and central nervous system, with norepinephrine being the highest affinity.
The mechanisms of sympathomimetic drugs can be direct-acting (direct interaction between drug and receptor), such as α-adrenergic agonists, β-adrenergic agonists, and dopaminergic agonists; or indirect-acting (interaction not between drug and receptor), such as MAOIs, COMT inhibitors, release stimulants, and reuptake inhibitors that increase the levels of endogenous catecholamines.
Phenylephrine is the main ingredient used in many common over-the-counter congestion products. It is safe to use, but an independent advisory committee to the FDA agreed Tuesday that it is ...
An adrenergic agonist is a drug that stimulates a response from the adrenergic receptors. The five main categories of adrenergic receptors are: α 1 , α 2 , β 1 , β 2 , and β 3 , although there are more subtypes, and agonists vary in specificity between these receptors, and may be classified respectively.
Oral phenylephrine is ineffective and “should almost never be used,” said Dr. Purvi Parikh, an allergist and immunologist at Allergy & Asthma Associates of Murray Hill in New York City.
Phenylephrine has been sold for more than 75 years, predating the agency’s own regulations on drug effectiveness. “It is the FDA’s role to ensure that drugs are safe and effective,” Dr. ...
Many tricyclic antidepressants, tetracyclic antidepressants, antipsychotics, ergolines, and some piperazines like buspirone, trazodone, nefazodone, etoperidone, and mepiprazole antagonize α 1-adrenergic receptors as well, which contributes to their side effects such as orthostatic hypotension.