Etilefrine Explained

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]

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.

External links

• Web site: Etilefrine . PubChem .
• Web site: Etilefrine . Kegg .

Notes and References

1. Nusser E, Donath H, Russ W . [On the circulatory action of depot-Effortil in patients with hypotonic regulation circulator disorders] . German . Die Medizinische Welt . 32 . 1824–7 . August 1965 . 5320529 .
2. Mellander S . 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 . 1966 . 4380206 . 10.1159/000157650 .
3. von Limbourg P, Just H, Lang KF . Positive inotrope Wirkung von Etilefrinhydrochlorid (EffortilR) . Kardiol . 586 . 1 . 1973 .
4. Tarnow J, Brückner JB, Eberlein HG, Patschke D, Reinecke A, Schmicke P . Experimentelle Untersuchungen zur Beeinflussung der Hämodynamik in tiefer Halothannarkose durch Dopamin, Glucagon, Effortil, Noradrenalin und Dextran . Der Anaesthesist . 22 . 8–15 . 1973 .
5. Carrera AL, Aguilera AM . 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 . 1973 .
6. Offermeier J, Dreyer AC . A comparison of the effects of noradrenaline, adrenaline and some phenylephrine derivatives on alpha-, beta₁- and beta₂- adrenergic receptors . South African Medical Journal = Suid-Afrikaanse Tydskrif vir Geneeskunde . 45 . 10 . 265–7 . March 1971 . 4396765 .