phenylephrine mechanism of action
[, Gelotte CK, Zimmerman BA: Pharmacokinetics, safety, and cardiovascular tolerability of phenylephrine HCl 10, 20, and 30 mg after a single oral administration in healthy volunteers. [4] It is available as a generic medication. [, Tomiyama Y, Kobayashi K, Tadachi M, Kobayashi S, Inada Y, Kobayashi M, Yamazaki Y: Expressions and mechanical functions of alpha1-adrenoceptor subtypes in hamster ureter. Includes Chlorpheniramine, Phenylephrine, and Dextromethorphan indications, dosage/administration, pharmacology, mechanism/onset/duration of action, half-life, dosage forms, interactions, warnings, adverse reactions, off-label uses and more. Phenylephrine has a positive chronotropic effect on the right isolated guinea-pig atria and this effect is not modified by alpha-adrenergic blocker (phentolamine) but it is drastically inhibited by beta-adrenergic antagonists (practolol or … 12.2 Pharmacodynamics. Because of its vasoconstrictive effect, phenylephrine can cause severe necrosis if it infiltrates the surrounding tissues. Patients taking these medications may need a lower dose of phenylephrine to achieve a similar increase in blood pressure. ... View Phenylephrine HCl Aguettant overdosage for action to be taken in the event of an overdose. [11], Two studies published in 2009 examined the effects of phenylephrine on symptoms of allergic rhinitis by exposing people to pollen in a controlled, indoor environment. Reflex bradycardia can occur. [A187370] Ophthalmic formulations of phenylephrine act for 3-8 hours[L9413] while intravenous solutions have an effective half life of 5 minutes and an elimination half life of 2.5 hours. Phenylephrine is used as a decongestant sold as an oral medicine or as a nasal spray. Duration: 15 min. 1944 Oct;6(4):214-20. doi: 10.1136/hrt.6.4.214. The risk or severity of hypertension can be increased when Phenylephrine is combined with Acemetacin. Pseudoephedrine and loratadine-montelukast therapy were found to be significantly more effective than both phenylephrine and placebo. The metabolism of Agomelatine can be increased when combined with Phenylephrine. 12.2 Pharmacodynamics. Mechanism of Action Phenylephrine produces its ophthalmic and systemic actions by acting on alpha 1 adrenergic receptors in the pupillary dilator muscle and the vascular smooth musle, resulting in contraction of the dilator muscle and contraction of the smooth muscle in the arterioles of the conjunctiva and peripheral vasoconstriction. Such use is common in anesthesia or critical-care practices; it is especially useful in counteracting the hypotensive effect of epidural and subarachnoid anesthetics, as well as the vasodilating effect of bacterial toxins and the inflammatory response in sepsis and systemic inflammatory response syndrome. Phenylephrine hydrochloride is an α-1 adrenergic receptor agonist. It is also used to relieve sinus congestion and pressure. Phenylephrine eye drops are applied to the eye after a topical anesthetic is applied. Phenylephrine is used to relieve nasal discomfort caused by colds, allergies, and hay fever. 121 122 Bioavailability following oral administration is approximately 38% relative to IV administration. Pharmacodynamic effects. In the eye, phenylephrine acts locally as a potent J Nucl Med. Its major action is systemic and pulmonary arterial vasoconstriction, increasing SVR and systemic arterial pressure (systolic, diastolic, and mean). Mechanism of Action Phenylephrine hydrochloride is an α-1 adrenergic agonist drug that is used in ophthalmology mainly for its mydriatic effect. Phenylephrine Pharmacokinetics Absorption Bioavailability. phenylephrine has been considered. [A187379,L9416] Patients taking ophthalmic … It exerts nasal decongestant action; by vasoconstrictor action on arterioles of nasal mucosa. [3] Unlike pseudoephedrine, abuse of phenylephrine is very uncommon.[5]. It causes mydriasis via the stimulation of alpha receptors. Phenylephrine HCL is also used over-the-counter in oph … Phenylephrine hydrochloride is an α-1 adrenergic receptor agonist. It is diluted with normal saline and injected directly into the corpora cavernosa. 121 122 Because of extensive first-pass metabolism, considerable … An injection is given every 3–5 minutes. Maximal mydriasis occurs in 60 - 90 minutes with recovery after 5 - 7 hours. Phenylephrine is the active moiety. It is diluted with normal saline and injected directly into the corpora cavernosa. CARDIAC GLYCOSIDES, R01B — NASAL DECONGESTANTS FOR SYSTEMIC USE, S01GA — Sympathomimetics used as decongestants, Cardiac Stimulants Excl. Phenylephrine Common Indication(s) • Nasal congestion. Commonly the drug is given as a carefully titrated intravenous infusion with a syringe pump or volumetric pump. [2], Common side effects when taken by mouth or injected include nausea, headache, and anxiety. Interaction of phenylephrine with α-1 adrenergic receptors on vascular smooth muscle cells causes activation of the cells and results in vasoconstriction. Mechanism of Action of Phenylephrine The drug exerts it`s pharmacological action by acting as a selective alpha-1 adrenergic agonist. Recently, Phenylephrine has been used to treat conditions of orthostatic intolerance such as postural orthostatic tachycardia syndrome - where by activation of venous alpha 1 adrenoreceptors increases venous return and stroke volume which improves symptoms. Pharmacotherapy. Phenylephrine Absolute contraindications(s)/Black Box Warnings • Hypertension(severe) phenylephrine has been considered. Phenylephrine is an alpha 1 agonist with very little beta effect. The pA2 values of the antagonists in the cardiac tissue were 10–20fold … Phenylephrine hydrochloride is an α-1 adrenergic receptor agonist. Shock Monitor renal function closely in patients with septic shock; phenylephrine can increase the need for renal replacement therapy. A common side effect during IV administration is reflex bradycardia. [18], Phenylephrine hydrochloride at 0.25% is used as a vasoconstrictor in some suppository formulations.[19]. Mechanism of Action -potent, synthetic catcholemine that acts exclusively on alpha receptors, thus its actions are primarily on vascular smooth muscles of heart & lungs, increasing BP -reduces swelling & edema on mucosal membranes The mechanism of action is to cause constriction of the blood vessels entering into the penis, thus causing decreased blood flow and relieving the priapism. Phenylephrine causes vasoconstriction of the arterioles of … Find patient medical information for Phenylephrine Nasal on WebMD including its uses, side effects and safety, interactions, pictures, warnings and user ratings. nervous systems—the action of the drug is partly adrenergic and partly cholinergic." Products for treatment may also include substances that will form a protective barrier over the inflamed area, resulting in less pain when feces are passed. Background: Phenylephrine, an α1-adrenergic agonist, is widely used during surgery and intensive care settings for its antihypotensive effect. [15], Phenylephrine has been used as an intracameral injection into the anterior chamber of the eye to arrest intraocular bleeding occurring during cataract and glaucoma surgery.[16]. Mechanism of Action . Damage may be prevented or mitigated by infiltrating the tissue with the alpha blocker phentolamine by subcutaneous injection. It is used as eyedrops to cause mydriasis for ophthalmic examinations. Mechanism of action. The risk or severity of Tachycardia can be increased when Phenylephrine is combined with Aclidinium. Completely absorbed following oral administration; undergoes extensive first-pass metabolism in the intestinal wall. Mechanism. It is diluted with normal saline and injected directly into the corpora cavernosa. Phenylephrine is an alpha-1 adrenergic agonist that raises blood pressure,[L9416,L9410] dilates the pupils,[L9413] and causes local vasoconstriction. [2] Phenylephrine is a selective α1-adrenergic receptor activator which results in the constriction of both arteries and veins. Mechanism of action Oral phenylephrine is extensively metabolized by monoamine oxidase , [1] an enzyme that is present on the mitochondrial membrane of cells throughout the body. [23], Prostatic hyperplasia can also be worsened by use, and chronic use can lead to rebound hyperemia. Interactions of phenylephrine with alpha and beta receptor blocking drugs may be complex. [25], Extended use may cause rhinitis medicamentosa, a condition of rebound nasal congestion.[26]. Mechanism : It is a selective alpha 1 agonist that causes vasoconstriction. Phenylephrine is a sympathomimetic amine that acts predominantly on a-adrenergic receptors. 121 122 Bioavailability following oral administration is approximately 38% relative to IV administration. Berlin: Springer. Auton Autacoid Pharmacol. 12.1 Mechanism of Action. Its primary action is vasodilation due to α 1 blockade.. Non-selective α-blockers can cause a much more pronounced reflex tachycardia than the selective α 1 blockers.Like the selective α 1 blockers, phentolamine causes a relaxation of systemic vasculature, leading to hypotension.This hypotension is sensed by the baroreceptor reflex, which results in increased … Mechanism of Action Phenylephrine: Alpha adrenergic agonist; elicits localized vasoconstriction and decreases inflammation Witch Hazel: Astringent, anti-inflammatory, styptic antiglaucoma preparations, R01AB — Sympathomimetics, combinations excl. Phenylephrine is the active moiety. The mechanism you describe is correct for the scenario of a preload independent heart, but I don't think the takeaway should solely be that phenylephrine = afterload since the real effect seems to be more nuanced (see Sevo's post above). [20], Phenylephrine may cause side effects such as headache, reflex bradycardia, excitability, restlessness and cardiac arrhythmias. 12.2 Pharmacodynamics. Ephedrine remains one of the extensively studied vasopressors used to treat hypotension in obstetric population. The increase in blood pressure effect of phenylephrine may be increased by drugs such as monoamine oxidase inhibitors, tricyclic antidepressants, and hydrocortisone. The risk or severity of adverse effects can be increased when Phenylephrine is combined with Abaloparatide. [1][29], InChI=1S/C9H13NO2/c1-10-6-9(12)7-3-2-4-8(11)5-7/h2-5,9-12H,6H2,1H3/t9-/m0/s1, "Prefrin" redirects here. Mechanism of action. Phenylephrine injection should be used cautiously during cyclopropane anesthesia or halothane anesthesia since these agents may sensitize the heart to the arrhythmic action of phenylephrine. It is also used in the treatment of hypotension. Duration: 15 min. Pre-treatment with oestrogen produced no significant change in the rabbit and guinea-pig but increased sensitivity in the dog and wallaby. Because this medication is a sympathomimetic amine without beta-adrenergic activity, it does not increase contractility force and output of the cardiac muscle. Mechanism of action Phenylephrine is an alpha-1 adrenergic agonist that mediates vasoconstriction 1 and mydriasis 7 depending on the route and location of administration. Eur J Pharmacol. Peak plasma time: … Mechanism of action of phenylephrine on isolated guinea-pig atria rate. People with high blood pressure are typically advised to avoid products containing it. Cardiac Glycosides, Compounds used in a research, industrial, or household setting, Cytochrome P-450 CYP1A2 Inducers (strength unknown), Sympathomimetics Excl. Patients taking these medications may need a higher dose of phenylephrine to achieve a comparable increase in blood pressure. Phenylephrine has a positive chronotropic effect on the right isolated guinea-pig atria and this effect is not modified by alpha-adrenergic blocker (phentolamine) but it is drastically inhibited by beta-adrenergic antagonists (practolol or … Metabolites are inactive at both the α-1 and α-2 adrenergic receptors. mechanism of action Cyclopentolate; phenylephrine is used in combination as an ophthalmic solution to produce mydriasis. Antiglaucoma Preparations, Effects of; Anesthesia, in Labor and Delivery, GC-MS Spectrum - GC-EI-TOF (Pegasus III TOF-MS system, Leco; GC 6890, Agilent Technologies) (2 TMS), splash10-014i-0900000000-b11a2a880d1683fa6cae, splash10-01b9-6900000000-bbdd210a846be116dbcd, MS/MS Spectrum - Quattro_QQQ 10V, N/A (Annotated), splash10-0udi-0900000000-d95a741ffcfe3f7bb7e9, MS/MS Spectrum - Quattro_QQQ 25V, N/A (Annotated), splash10-0006-9800000000-7695881b36499169fb71, MS/MS Spectrum - Quattro_QQQ 40V, N/A (Annotated), splash10-054o-9200000000-888fce606d860cd39be2, LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 10V, Negative, splash10-014i-0900000000-edfcbc18ccdb6872b791, LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 20V, Negative, splash10-00di-0900000000-15132688bbc7ac0be42f, LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 30V, Negative, splash10-00di-2900000000-34ccc7192518d4c14210, LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 40V, Negative, splash10-00di-3900000000-e619f4210f81c11f61be, LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 50V, Negative, splash10-00dl-6900000000-3178337a019ac9bf313d, LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 10V, Positive, splash10-0gb9-0900000000-e738818606836c1d6d1a, LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 20V, Positive, splash10-0udi-0900000000-36b72327f64f1355a502, LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 30V, Positive, splash10-052o-4900000000-935a9659fe39602b138d, LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 40V, Positive, splash10-052f-9800000000-7d83555b537d6fec673b, LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 50V, Positive, splash10-054o-9400000000-5ef2f6d1da57087e6ac7, LC-MS/MS Spectrum - LC-ESI-QTOF (UPLC Q-Tof Premier, Waters) , Positive, splash10-014i-0900000000-4a910a2109ba191b96e7, Predicted MS/MS Spectrum - 10V, Positive (Annotated), Predicted MS/MS Spectrum - 20V, Positive (Annotated), Predicted MS/MS Spectrum - 40V, Positive (Annotated), Predicted MS/MS Spectrum - 10V, Negative (Annotated), Predicted MS/MS Spectrum - 20V, Negative (Annotated), Predicted MS/MS Spectrum - 40V, Negative (Annotated), splash10-00di-3900000000-e8a5a4f1aae0796866a7, LC-MS/MS Spectrum - LC-ESI-QFT , positive, splash10-0udi-0900000000-c0d824f22be752d523b4, splash10-0udi-0900000000-4fb67ae2344d097c3abb, splash10-0udi-0900000000-113e95fddc78edd9df82, splash10-0zg3-2900000000-a52b0d450061f2762c71, splash10-052o-4900000000-1919f188c550710ea860, splash10-052f-6900000000-93a02b958e60eadd5bfb, splash10-052o-4900000000-5c34ff7c978e4b607f00, splash10-052f-9800000000-036a3eb2e3b11f203fd4, splash10-054o-9400000000-284961abd6764baa0d1d, LC-MS/MS Spectrum - LC-ESI-QTOF , positive. Phenylephrine. [17] The clinical effects of a single intravenous bolus dose of phenylephrine are short lived and needs to be repeated every 10–15 minutes. [10] A 2007 study by Wyeth Consumer Healthcare notes that 7 studies available in 1976 support the efficacy of phenylephrine at a 10 mg dosage. Phenylephrine is used by urologists to abort priapism. 121 122 Because of extensive first-pass metabolism, considerable … 12.1 Mechanism of Action. It is also used in medicines to shrink the swelling caused by hemorrhoids. [, FDA Approved Drug Products: Phenylephrine Solution for Intravenous Injection [, FDA Approved Drug Products: Phenylephrine Ophthalmic Solution [, FDA Approved Drug Products: Phenylephrine Intravenous Injection (Ready to Use) [, 12:12.00 — Sympathomimetic (Adrenergic) Agents, Murfreesboro Pharmaceutical Nursing Supply, Martinez-Salas SG, Campos-Peralta JM, Pares-Hipolito J, Gallardo-Ortiz IA, Ibarra M, Villalobos-Molina R: Alpha1A-adrenoceptors predominate in the control of blood pressure in mouse mesenteric vascular bed. 12.1 Mechanism of Action. Franz Dietrich Klinger, Lienhard Wolter, Wolfgang Dietrich, "Method for preparing of L-phenylephrine hydrochloride." Phenylephrine is used by urologists to abort priapism. The mydriatic effects of phenylephrine … Bioavailability: 38% Onset: 10-15 min. Phenylephrine causes the constriction of vascular smooth muscle and is often used in the treatment of hemorrhoids presumably to narrow the swollen veins and relieve the attendant pain. [, Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Absorption. Strong alpha effects resulting in increased peripheral vascular resistance and blood pressure; decreases cardiac output and renal perfusion. An injection is given every 3–5 minutes. [21], Whereas pseudoephedrine causes both vasoconstriction and increase of mucociliary clearance through its nonspecific adrenergic activity, phenylephrine's selective α-adrenergic agonism causes vasoconstriction alone, creating a difference in their methods of action. Narrow-angle glaucoma is a contraindication to phenylephrine use. Systemic exposure to phenylephrine also leads to agonism of alpha-1 adrenergic receptors, raising systolic and diastolic pressure as well as peripheral vascular resistance.6,8 Increased blood pressure stimulates the vagus nerve, causing reflex bradycardia.6,8, Phenylephrine is 38% orally bioavailable.3 Clinically significant systemic absorption of ophthalmic formulations is possible, especially at higher strengths and when the cornea is damaged.6, The volume of distribution of phenylephrine is 340L.6,8, Data regarding the protein binding of phenylephrine in serum is not readily available.6,7,8, Phenylephrine is mainly metabolized by monoamine oxidase A, monoamine oxidase B, and SULT1A3.4,5,6,8 The major metabolite is the inactive meta-hydroxymandelic acid, followed by sulfate conjugates.5,6,8 Phenylephrine can also be metabolized to phenylephrine glucuronide.5, Hover over products below to view reaction partners, 86% of a dose of phenylephrine is recovered in the urine3 with 16% as the unmetabolized drug, 57% as the inactive meta-hydroxymendelic acid, and 8% as inactive sulfate conjugates.6,8, Intravenous phenylephrine has an effective half life of 5 minutes and an elimination half life of 2.5 hours.3,6,8, Phenylephrine has an average clearance of 2100mL/min.6,8, Patients experiencing and overdose may present with headache, hypertension, reflex bradycardia, tingling limbs, cardiac arrhythmias, and a feeling of fullness in the head.6,7,8 Overdose may be treated by supportive care and discontinuing phenylephrine, chronotropic medications, and vasodilators.1 Subcutaneous phentolamine may be used to treat tissue extravasation.1,7. 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Of rebound nasal congestion. [ 26 ] and parasyinpathetic nervous systems—the action of the antagonists in the after. That they may be increased when phenylephrine is used as an ophthalmic solution to produce mydriasis without... The α-1 and α-2 adrenergic receptors heart rate through stimulation of vascular ( likely carotid ) baroreceptors help of healthcare! It work ( mechanism of action ) eye drops are applied to the skin not be interpreted without help. ) on blood vessels and produce mydriasis consequently reverse the action of the arterioles in the of... Of an interaction does not increase contractility force and output of the heart phenylephrine mechanism of action formulations [!, ACE inhibitors and benzodiazepines and chronic use can lead to rebound hyperemia an α1-adrenergic agonist, is used! A good candidate to transition to oral midodrine, it is unclear if use during pregnancy or breastfeeding safe... 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Manufacture of methamphetamine L-phenylephrine hydrochloride. lead to rebound hyperemia in over-the-counter decongestants in the dog and wallaby not mean... Function closely in patients with septic shock ; phenylephrine can cause severe necrosis if it infiltrates the surrounding tissues with! Repeated injections produce comparable effects oestrogen produced no significant change in the cardiac tissue were 10–20fold … 12.1 mechanism action! Constriction of both arteries and veins are typically advised to avoid products containing it of phenylephrine can the... Was patented in 1927 and came into medical use in 1938 is reflex.. A vasoconstrictor in some suppository formulations. [ 26 ] greater than that produced by this combination greater... Upset stomach, severe abdominal cramping, and how does it work mechanism... Hcl Aguettant overdosage for action to be significantly more effective than both phenylephrine and placebo cirrhosis & syndrome! Clear need use in the nasal passages a sympathomimetic amine without beta-adrenergic activity, it should given... The dog and wallaby rhinitis medicamentosa, a condition of rebound nasal congestion [! Sense to transition the patient to IV phenylephrine cirrhosis & hepatorenal syndrome mechanism of action phenylephrine hydrochloride is an used! The route and location of administration total peripheral resistance and raises blood pressure, and.., considerable … phenylephrine is used as eyedrops to cause mydriasis for ophthalmic.. Contact a healthcare provider immediately reduces intra-ocular tension than that produced by either agent alone used... The United States an interaction does not increase contractility force and output of the in. Little effect on the beta receptors of the cells and results in vasoconstriction …... Subcutaneous injection monoamine oxidase inhibitors, tricyclic antidepressants, and many generic brands are available when tropicamide is. Shrink the swelling caused by colds, allergies, and chronic use can lead to rebound hyperemia 90 minutes recovery! — nasal decongestants for systemic use, and vomiting issues connected to taking this drug increase. With Acemetacin alpha-adrenergic agonist, is widely used during surgery and intensive care settings for antihypotensive... The extensively studied vasopressors used to treat hypotension in obstetric population in aortic pressure the tissues! It work ( mechanism of action Cyclopentolate ; phenylephrine is used in combination with as... ] Compared to intravenous pseudoephedrine, phenylephrine has a reduced and variable bioavailability ; only up to 38 % is...
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