Etilefrine

Etilefrine is a cardiac stimulant used as an antihypotensive. It is a sympathomimetic amine of the 3-hydroxy-phenylethanolamine series used in treating orthostatic hypotension of neurological, cardiovascular, endocrine or metabolic origin. Intravenous infusion of this compound increases cardiac output, stroke volume, venous return and blood pressure in man and experimental animals, suggesting stimulation of both α and β adrenergic receptors.[1][2][3][4][5] However, in vitro studies indicate that etilefrine has a much higher affinity for β1 (cardiac) than for β2 adrenoreceptors.[6]

Etilefrine
Clinical data
Other names(2-ethylamino-1-(3'-hydroxy-phenyl)ethanol
AHFS/Drugs.comInternational Drug Names
ATC code
Identifiers
IUPAC name
  • (RS)-3-[2-(ethylamino)-1-hydroxyethyl]phenol
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.010.829
Chemical and physical data
FormulaC10H15NO2
Molar mass181.235 g·mol−1
3D model (JSmol)
ChiralityRacemic mixture
SMILES
  • CCNCC(O)c1cc(O)ccc1
InChI
  • InChI=1S/C10H15NO2/c1-2-11-7-10(13)8-4-3-5-9(12)6-8/h3-6,10-13H,2,7H2,1H3 Y
  • Key:SQVIAVUSQAWMKL-UHFFFAOYSA-N Y
  (verify)

Intravenous etilefrine increases the pulse rate, cardiac output, stroke volume, central venous pressure and mean arterial pressure of healthy individuals. Peripheral vascular resistance falls during the infusion of 1–8 mg etilefrine but begins to rise at higher dosage. Marked falls in pulse rate, cardiac output, stroke volume and peripheral bloodflow, accompanied by rises in mean arterial pressure, occur when etilefrine is infused after administration of intravenous propranolol 2,5 mg. These findings indicate that etilefrine has both β1 and α1 adrenergic effects in man.

References
  1. Nusser E, Donath H, Russ W (August 1965). "[On the circulatory action of depot-Effortil in patients with hypotonic regulation circulator disorders]". Die Medizinische Welt (in German). 32: 1824–7. PMID 5320529.
  2. Mellander S (1966). "Comparative effects of acetylcholine, butyl-nor-synephrine (Vasculat), noradrenaline, and ethyl-adrainol (Effonti) on resistance, capacitance, and precapillary sphincter vessels and capillary filtration in cat skeletal muscle". Angiologica. 3 (2): 77–99. doi:10.1159/000157650. PMID 4380206.
  3. von Limbourg P, Just H, Lang KF (1973). "Positive inotrope Wirkung von Etilefrinhydrochlorid (EffortilR)". Kardiol. 586: 1.
  4. Tarnow J, Brückner JB, Eberlein HG, Patschke D, Reinecke A, Schmicke P (1973). "Experimentelle Untersuchungen zur Beeinflussung der Hämodynamik in tiefer Halothannarkose durch Dopamin, Glucagon, Effortil, Noradrenalin und Dextran". Anaesthesist. 22: 8–15.
  5. Carrera AL, Aguilera AM (1973). "Algunos effectos circulatorios de la m− oxifenil etanol etilmaina y sus modificaciones por el bloqueo α y β adrenergico". Arch. Inst. Cardiol. Mexico. 43: 279–287.
  6. Offermeier J, Dreyer AC (March 1971). "A comparison of the effects of noradrenaline, adrenaline and some phenylephrine derivatives on alpha-, beta- and beta- adrenergic receptors". South African Medical Journal = Suid-Afrikaanse Tydskrif vir Geneeskunde. 45 (10): 265–7. PMID 4396765.
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