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| routes_of_administration = Oral, intranasal, ophthalmic, intravenous, intramuscular
| routes_of_administration = Oral, intranasal, ophthalmic, intravenous, intramuscular
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'''Phenylephrine''' or '''Neo-Synephrine''' is an [[Alpha-1_adrenergic_receptor|α<sub>1</sub>-adrenergic receptor]] [[agonist]] used primarily as a [[decongestant]], as an agent to dilate the [[pupil]] and to increase [[blood pressure]]. Phenylephrine has recently been marketed as a substitute for [[pseudoephedrine]], (e.g., [[Pfizer]]'s ''Sudafed (Original Formulation)'') but there are recent claims that oral phenylephrine may be no more effective as a decongestant than a [[placebo]].<Ref name="UFL">{{cite web| url=http://news.ufl.edu/2006/07/19/decongensant/ | author=University of Florida (press release) | title=UF researchers question effectiveness of decongestant | date= 2006-07-19 | access-date=2008-03-15 }}</ref><ref>Hatton RC, et al. Efficacy and Safety of Oral Phenylephrine: A Systematic Review and Meta-Analysis. Ann Pharmacother. 2007 Mar;41(3):381-90. Epub 2007 Jan 30.</ref>
'''Phenylephrine''' or '''Neo-Synephrine''' is an [[Alpha-1_adrenergic_receptor|α<sub>1</sub>-adrenergic receptor]] [[agonist]] used primarily as a [[decongestant]], as an agent to dilate the [[pupil]] and to increase [[blood pressure]]. Phenylephrine has recently been marketed as a substitute for [[pseudoephedrine]], (e.g., [[Pfizer]]'s ''Sudafed (Original Formulation)'') but there are recent claims that oral phenylephrine may be no more effective as a decongestant than a [[placebo]].<Ref name="UFL">{{cite web| url=http://news.ufl.edu/2006/07/19/decongensant/ | author=University of Florida (press release) | title=UF researchers question effectiveness of decongestant | date= 2006-07-19 | access-date=2008-03-15 }}</ref>


==Uses==
==Uses==

Revision as of 19:59, 7 March 2009

Phenylephrine
Clinical data
Pregnancy
category
  • AU: B2
Routes of
administration		Oral, intranasal, ophthalmic, intravenous, intramuscular
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability38% through GI tract
Protein binding95%
MetabolismHepatic (monoamine oxidase)
Elimination half-life2.1 to 3.4 hours
Identifiers
  • 3-[(1R)-1-hydroxy-2-(methylamino)ethyl]phenol
CAS Number
PubChem CID
DrugBank
ChemSpider
CompTox Dashboard (EPA)
ECHA InfoCard100.000.386 Edit this at Wikidata
Chemical and physical data
FormulaC9H13NO2
Molar mass167.205 g/mol g·mol−1

Phenylephrine or Neo-Synephrine is an α1-adrenergic receptor agonist used primarily as a decongestant, as an agent to dilate the pupil and to increase blood pressure. Phenylephrine has recently been marketed as a substitute for pseudoephedrine, (e.g., Pfizer's Sudafed (Original Formulation)) but there are recent claims that oral phenylephrine may be no more effective as a decongestant than a placebo.[1]

Uses

Decongestant

Phenylephrine is used as a decongestant sold as an oral medicine, nasal spray, or as eye drops. Phenylephrine is now the most common over-the-counter (OTC) decongestant in the United States; oxymetazoline is a more common nasal spray. [citation needed] Pseudoephedrine was historically more common, although its notoriety as a methamphetamine precursor has led some governments to restrict its sale.

Oral phenylephrine is extensively metabolised by monoamine oxidase [2], an enzyme which is present in the gastrointestinal tract and in the liver. Therefore, compared to orally-taken pseudoephedrine, it has a reduced and variable bioavailability of only up to 38 percent,[3][4] and is therefore less effective as a nasal decongestant than pseudoephedrine. Because phenylephrine is a direct selective α-adrenergic receptor agonist, it does not cause the release of endogenous noradrenaline like pseudoephedrine does. Therefore, phenylephrine is less likely to cause side-effects such as central nervous system stimulation, insomnia, anxiety, irritability and restlessness.

Some popular cold remedies containing phenylephrine include:

Australia

  • Codral Cold & Flu (New Formula)
  • Lemsip Max Cold & Flu Hot Drink with decongestant
  • Sudafed PE Sinus Non-Drowsy Nasal Decongestant

Canada

Mexico

  • Histiacil Flu

South Africa

  • Demazin
  • Flutex

South Korea

  • Happynose Tab

United Kingdom

United States

As a nasal spray, phenylephrine is available in 1 percent and 0.5 percent concentrations. It causes some rebound congestion effects although to a lesser degree than oxymetazoline.

Mydriatic

Phenylephrine is used as an eye drop to dilate the pupil to facilitate visualization of the retina. It is often used in combination with tropicamide. Narrow angle glaucoma is a contraindication to phenylephrine use.

Vasopressor

Phenylephrine is sometimes used as a vasopressor to increase the blood pressure in unstable patients with hypotension. Such use is more common in anesthesia or critical care practices; phenylephrine is especially useful in counteracting the hypotensive effect of epidural and subarachnoid anesthetics. It also has the advantage of not being inotropic or chronotropic, and so it strictly elevates the blood pressure without increasing the heart rate or contractility (reflex bradycardia may result from the blood pressure increase, however). This is especially useful if the heart is already tachycardic and/or has a cardiomyopathy. The elimination half life of phenylephrine is about 2.5 to 3 hours.

Side effects

The primary side effect of phenylephrine is hypertension. Patients with congestion and hypertension are typically advised to avoid products containing phenylephrine.

Prostatic hyperplasia can also be symptomatically worsened by use, and chronic use can lead to rebound hyperemia.[5]

Patients with a history of epilepsy and on anticonvulsant medication should not take this substance. The drug interaction might produce seizures.

Some patients have been shown to have an upset stomach, severe abdominal cramping, and vomiting issues connected to taking this drug.

Substitute for pseudoephedrine

Pseudoephedrine and phenylephrine are both used as decongestants; and until recently, pseudoephedrine was much more commonly available in the United States. This has changed because provisions of the Combat Methamphetamine Epidemic Act of 2005 placed restrictions on the sale of pseudoephedrine products to prevent the clandestine manufacture of methamphetamine. Since 2004, phenylephrine has been increasingly marketed as a substitute for pseudoephedrine; some manufacturers have changed the active ingredients of products to avoid the restrictions on sales.[6] Phenylephrine has been off patent for a long time; there are many generic brands available.

Questions about effectiveness

Pharmacists Leslie Hendeles and Randy Hatton of the University of Florida suggested in 2006 that oral phenylephrine is ineffective as a decongestant at the 10 mg dose used, arguing that the studies used for the regulatory approval of the drug in the United States in 1976 were inadequate to prove effectiveness at the 10 mg dose and safety at higher doses.[7] Other pharmacists have expressed concerns over phenylephrine's effectiveness as a nasal decongestant,[1] and other clinicians have indicated concern for regulatory actions that reduced the availability of pseudoephedrine.[8][9] A subsequent meta-analysis by the same researchers concluded that there is insufficient evidence for its effectiveness,[10] though another meta-analysis published shortly thereafter by researchers from GlaxoSmithKline found the standard 10mg dose to be significantly more effective than a placebo.[11]

The matter is still under debate, though the Food and Drug Administration has stood by its 1976 approval.[6]

References

  1. ^ a b University of Florida (press release) (2006-07-19). "UF researchers question effectiveness of decongestant". Retrieved 2008-03-15.
  2. ^ Drug Properties
  3. ^ Pharmacogenetics and Pharmacogenomics Knowledge Base entry on phenylephrine
  4. ^ NZ Medicines and Medical Devices Safety Authority recommendation on phenylephrine (November 2004)
  5. ^ Shen, Howard (2008). Illustrated Pharmacology Memory Cards: PharMnemonics. Minireview. p. 3. ISBN 1-59541-101-1.
  6. ^ a b Hilenmeyer, K. (30 January 2007). "All stuffed up". Southwest Florida Herald-Tribune.
  7. ^ Heldeles, L. and Hatton, R. (2006). "Oral phenylephrine: An ineffective replacement for pseudoephedrine?". Journal of Allergy and Clinical Immunology. 118 (1): 279–280. doi:10.1016/j.jaci.2006.03.002. PMID 16815167.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  8. ^ >Eccles R (May 2006). "Phenylephrine an ineffective replacement for pseudoephedrine in response to the methamphetamine problem in the USA". BMJ.
    Rapid Response to
    Tanne JH (2006). "Methamphetamine epidemic hits middle America". BMJ. 332 (7538): 382. doi:10.1136/bmj.332.7538.382-b. PMID 16484253. {{cite journal}}: Unknown parameter |month= ignored (help)
  9. ^ Eccles, R. (2007). "Substitution of phenylephrine for pseudoephedrine as a nasal decongestant. An illogical way to control methamphetamine abuse". British Journal of Clinical Pharmacology. 63: 10–14. doi:10.1111/j.1365-2125.2006.02833.x. PMID 17116124. (January 2007)
  10. ^ Hatton, R.C.; et al. (2007). "Efficacy and Safety of Oral Phenylephrine: A Systematic Review and Meta-Analysis" (abstract). Annals of Pharmacotherapy. 41: 381–390. doi:10.1345/aph.1H679. PMID 17264159. {{cite journal}}: Explicit use of et al. in: |author= (help)(published online Jan 2007)
  11. ^ Kollar C, Schneider H, Waksman J, Krusinska E. (2007). "Meta-analysis of the efficacy of a single dose of phenylephrine 10 mg compared with placebo in adults with acute nasal congestion due to the common cold". Clinical Therapeutics. 29: 1057–1070. doi:j.clinthera.2007.05.021. {{cite journal}}: Check |doi= value (help); Unknown parameter |doi_brokendate= ignored (|doi-broken-date= suggested) (help)CS1 maint: multiple names: authors list (link)
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