Concise review: Therapeutic potential of flupirtine maleate

Abstract

Flupirtine is a non-opioid analgesic without antipyretic or antiphlogistic properties. Flupirtine is a centrally acting analgesic but the analgesic action of flupirtine does not depend on any central opioid effect. The fact behind this statement is that the pain-relieving property of flupirtine is not reduced by the opioid antagonistic drug naloxone. Flupirtine has been reported for its neuro-protective properties and possess a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties. Flupertine is transformed into two primary derivatives, 4-fluoro-hippuric acid and the Nacetylated analogue D13223. Both derivatives of are flupirtine pharmacologically active with 30% of the analgesic potency of the parent drug and further oxidized and then conjugated with glycine to form inactive metabolites, Recently, Flupirtine maleate has been introduced in Indian market in oral, intravenous and rectal dosage forms. The half life of flupirtine following intravenous administration was 1.8 hours, while the plasma elimination half life in healthy young volunteers following single dose administration of flupirtine by the intravenous, oral and rectal routes was 8.5, 9.6 and 10.7 hours respectively. There is plenty of literature available on the effect of Flupirtine maleate on chronic and acute pain management. These preliminary finding require confirmation in further comparative studies.
 Keywords: Flupirtine maleate, Naloxone, Opioid, NMDA