Naftidrofuryl
Chemical compound
From Wikipedia, the free encyclopedia
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.[1][2][3][4][5] It is taken orally.[1]
| |
| Clinical data | |
|---|---|
| Trade names | Praxilene, others |
| Other names | Nafronyl; Naftidrofurile; Naftifurine; EU-1806; EU1806; LS-121; LS121 |
| AHFS/Drugs.com | International Drug Names |
| Routes of administration | Oral[1] |
| Drug class | Serotonin 5-HT2A receptor antagonist; Vasodilator |
| ATC code | |
| Legal status | |
| Legal status |
|
| Pharmacokinetic data | |
| Bioavailability | 20–78% (in different studies)[1] |
| Protein binding | 80%[1] |
| Metabolism | Hepatic[1] |
| Onset of action | 0.8–1.0 hours (Tmax)[1] |
| Elimination half-life | 1.2–2 hours[1] |
| Duration of action | 2–3 hours[1] |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| ChemSpider | |
| UNII | |
| ChEMBL | |
| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.045.960 |
| Chemical and physical data | |
| Formula | C24H33NO3 |
| Molar mass | 383.532 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
| (verify) | |
Medical uses
Naftidrofuryl is used as a vasodilator in the treatment of peripheral and cerebral vascular disorders.[1][2][5] It is also licensed for the treatment of intermittent claudication due to peripheral arterial disease.[1] Historically, it has been used to treat sudden idiopathic hearing loss and acute tinnitus.[6] Naftidrofuryl may be effective for relieving the pain of muscle cramps.[7]
Adverse effects
Naftidrofuryl has been associated with nausea, abdominal pain, and rash.[8][1] Rarely, hepatitis and liver failure have been reported.[1][8]
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).[1][5][9][10]
Pharmacokinetics
The oral bioavailability of naftidrofuryl is 20 to 78% in different studies.[1] Its time to peak levels is 0.8 to 1.0 hours.[1] There is some evidence that naftidrofuryl crosses the blood–brain barrier and penetrates into the central nervous system.[11][12] The drug's plasma protein binding is 80%.[1] It is metabolized in the liver.[1] The elimination half-life of naftidrofuryl is 1.2 to 2 hours.[1] Its half-life is longer in the elderly than in younger people.[1] The drug's duration of effects is 2 to 3 hours and closely parallels circulating levels of naftidrofuryl.[1]
History
Naftidrofuryl was first described in the scientific literature by at least 1966.[4]
Society and culture
Names
Naftidrofuryl is the generic name of the drug and its (INN, BAN, DCF, and JAN.[2][3][4][5] It is also known as naftidrofurile (DCIT) or as nafronyl (USAN.[2][3][4][5] 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.[2][3][4]
Availability
Naftidrofuryl is marketed and used widely throughout the world.[2][3]