Phenylephrine

  • (R) -3 - [1- hydroxy-2- methylaminoethyl ] phenol (IUPAC)
  • (R ) -1 - ( 3-hydroxyphenyl ) - 2 - (methylamino ) ethanol
  • Latin: Phenylephrinum
  • 59-42-7
  • 61-76-7 (hydrochloride)
  • C01CA06 S01GA05
  • R01AA04 R01AB01
  • R01BA03 S01FB01

Sympathomimetic

( R) - ( -)- phenylephrine hydrochloride

Attention

350 mg · kg -1 ( LD50, rat, oral)

Template: Infobox chemical / molecular formula search available

Phenylephrine is one of the direct-acting sympathomimetic with partially indirect effect. It acts as an agonist at the α1 - adrenoceptor. Phenylephrine is structurally identical with epinephrine to a lack of 4- hydroxy group, and is mainly used in Europe as a local vasoconstrictor, for example as the active ingredient of nasal drops for decongesting nasal mucous membranes in the interior. In eye drops, it acts as a mydriatic, that leads to a widening of the pupils. International is phenylephrine - including within the framework of obstetrics - used as a vasopressor. The effect is most comparable to that of noradrenaline.

Pharmacokinetics

After administration of tritiated (3H - phenylephrine ) by infusion or orally in humans, an analysis by ion-exchange and thin-layer chromatography excretion of 86 ( iv ) or 80 (po ) percent of the administered activity in the urine; which a full -intestinal absorption is assumed. The difference in the amount of free 3H- phenylephrine in the serum of 16 % of the administered dose in the iv Application compared to 2.6% in the oral, suggests a decreased bioavailability of the substance. The biological half-life of two to three hours, as well as the clearance of 2 L / h, which is comparable to structurally related amines.

The show metabolism to phenolic conjugates after oral ingestion or m - hydroxymandelic after intravenous injection that m - hydroxylated amines in the first- pass metabolism are conjugated mainly.

Trade names

  • Nasal Spray for Children ® ( CH)
  • Neosynephrine ® ( D)
  • Rexophtal ® UD N (CH)
  • Thalia ® ( A)
  • Vibrocil ® (A, CH)
  • Visadron ® ( D, A)
  • Metaoxedrin ® ( DK )
  • Mesatonum
CAS registry number PubChem Anatomical Therapeutic Chemical Classification System DrugBank Dangerous Substances Directive (67/548/EEC) Antihypotensive agent Enteral administration Serum (blood) Digital Object Identifier European Journal of Clinical Pharmacology
646863
de