Naftidrofuryl, also known as nafronyl and sold under the brand name Praxilene among others, is a serotonin 5-HT2 receptor antagonist which is used as a vasodilator in the treatment of peripheral and cerebral vascular disorders. It is taken orally.
Medical uses Naftidrofuryl is used as a vasodilator in the treatment of peripheral and cerebral vascular disorders. It is also licensed for the treatment of intermittent claudication due to peripheral arterial disease. Historically, it has been used to treat sudden idiopathic hearing loss and acute tinnitus. Naftidrofuryl may be effective for relieving the pain of muscle cramps.
Adverse effects Naftidrofuryl has been associated with nausea, abdominal pain, and rash. Rarely, hepatitis and liver failure have been reported.
Pharmacology
Pharmacodynamics Naftidrofuryl acts as a selective antagonist of 5-HT2 receptors (with action as an inverse agonist of the 5-HT2A receptor specifically characterized).
Pharmacokinetics The oral bioavailability of naftidrofuryl is 20 to 78% in different studies. Its time to peak levels is 0.8 to 1.0 hours. There is some evidence that naftidrofuryl crosses the blood–brain barrier and penetrates into the central nervous system. The drug's plasma protein binding is 80%. It is metabolized in the liver. The elimination half-life of naftidrofuryl is 1.2 to 2 hours. Its half-life is longer in the elderly than in younger people. The drug's duration of effects is 2 to 3 hours and closely parallels circulating levels of naftidrofuryl.
History Naftidrofuryl was first described in the scientific literature by at least 1966.
Society and culture
Names Naftidrofuryl is the generic name of the drug and its (INNTooltip International Nonproprietary Name, BANTooltip British Approved Name, DCFTooltip Dénomination Commune Française, and JANTooltip Japanese Accepted Name. It is also known as naftidrofurile (DCITTooltip Denominazione Comune Italiana) or as nafronyl (USANTooltip United States Adopted Name. Naftidrofuryl is marketed under a variety of trade names, including Artocoron, Azunaftil, Di-Actane, Dusodril, Enelbin, Frilix, Gevatran, Iridus, Iridux, Luctor, Nafti, Naftilong, Naftodril, Nafoxal, Praxilene, Sodipryl Retard, Stimlor, and Vascuprax, among others.
Availability Naftidrofuryl is marketed and used widely throughout the world.
See also Serotonin 5-HT2A receptor antagonist Irindalone Ketanserin Sarpogrelate
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