About: Phenylephrine     Goto   Sponge   NotDistinct   Permalink

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  • Phenylephrine is a sympathomimetic amine that acts predominantly on α-adrenergic receptors. It is mainly used to treat nasal congestion, but may also be useful in treating hypotension and shock, hypotension during spinal anaesthesia, prolongation of spinal anaesthesia, paroxysmal supraventricular tachycardia, symptomatic relief of external or internal hemorrhoids, and to increase blood pressure as an aid in the diagnosis of heart murmurs. (en)
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  • approved (en)
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  • 2.1 to 3.4 hours (en)
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  • Phenylephrine is mainly used to treat nasal congestion, but may also be useful in treating hypotension and shock, hypotension during spinal anaesthesia, prolongation of spinal anaesthesia, paroxysmal supraventricular tachycardia, symptomatic relief of external or internal hemorrhoids, and to increase blood pressure as an aid in the diagnosis of heart murmurs. (en)
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Title
  • Phenylephrine (en)
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http://linked.open...mechanismOfAction
  • In general, &alpha;<sub>1</sub>-adrenergic receptors mediate contraction and hypertrophic growth of smooth muscle cells. &alpha;<sub>1</sub>-receptors are 7-transmembrane domain receptors coupled to G proteins, G<sub>q/11</sub>. Three &alpha;<sub>1</sub>-receptor subtypes, which share approximately 75% homology in their transmembrane domains, have been identified: &alpha;<sub>1A</sub> (chromosome 8), &alpha;<sub>1B</sub> (chromosome 5), and &alpha;<sub>1D</sub> (chromosome 20). Phenylephrine appears to act similarly on all three receptor subtypes. All three receptor subtypes appear to be involved in maintaining vascular tone. The &alpha;<sub>1A</sub>-receptor maintains basal vascular tone while the &alpha;<sub>1B</sub>-receptor mediates the vasocontrictory effects of exogenous &alpha;<sub>1</sub>-agonists. Activation of the &alpha;<sub>1</sub>-receptor activates G<sub>q</sub>-proteins, which results in intracellular stimulation of phospholipases C, A<sub>2</sub>, and D. This results in mobilization of Ca<sup>2+</sup> from intracellular stores, activation of mitogen-activated kinase and PI<sub>3</sub> kinase pathways and subsequent vasoconstriction. Phenylephrine produces its local and systemic actions by acting on &alpha;<sub>1</sub>-adrenergic receptors peripheral vascular smooth muscle. Stimulation of the &alpha;<sub>1</sub>-adrenergic receptors results in contraction arteriolar smooth muscle in the periphery. Phenylephrine decreases nasal congestion by acting on &alpha;<sub>1</sub>-adrenergic receptors in the arterioles of the nasal mucosa to produce constriction; this leads to decreased edema and increased drainage of the sinus cavities. (en)
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