Fipexide, an effective cognition activator in the elderly: a placebo-controlled, double-blind clinical trial

Abstract

Forty geriatric in-patients with severe cognition disorders were randomly allocated to treatment with either 600 mg fipexide daily or placebo over a period of 3 weeks. Before and after treatment, the symptoms of cognitive performance (disorders of memory and attention, asthenia, apathy and disorders of coenaesthesia) were monitored and scored. Similarly, the Thurstone test (symbol matching test) was performed and time to completion, number of errors and exactitude index were recorded. Haemodynamics, haematology and haematochemistry investigations were made before and after treatment, and accessory symptoms of potential side-reactions were monitored by positive questioning. Treatment with fipexide was associated with a significant improvement in each and all monitored symptoms and signs to an average extent of 60%, whereas placebo was not. Similarly, the patients given fipexide experienced a significant improvement in the Thurstone test, in terms of time to completion (-22%), number of errors (-46%) and exactitude index (+60%); again, placebo was not associated with any significant improvement (variations, respectively, of -5%, -14%, and +24%). Overall, 85% of the patients given fipexide experienced clinical improvement to a greater or lesser degree, a significantly greater proportion than that associated with placebo (25%; p less than 0.001). Tolerance, both subjective and objective, was good in both treatment groups.

Induced Chiroptical Changes of a Water‐Soluble Cryptophane by Encapsulation of Guest Molecules and Counterion Effects

“…The next test compound was one that has recently been reported to form GSH adducts in microsomal and hepatocyte incubations 26, 27. This nootropic drug was designed and used as a treatment for cognitive disorders,28, 29 but was quickly withdrawn from the market due to severe and unexplained toxicity 30, 31. Since then, in vitro studies have shown the possibility of linking this toxicity to the formation of reactive metabolites26 and covalent binding to proteins 27.…”

Studies on the metabolism and the toxicological analysis of the nootropic drug fipexide in rat urine using gas chromatography–mass spectrometry

“…Its pharmacological effects were discussed to be, at least partially, mediated by modulating dopaminergic transmission [1][2][3][4][5][6][7]. FIP has been associated with several severe side effects including hepatic failure with emergency liver transplantation and drug fever [8][9][10].…”

Determining protein adducts of fipexide: mass spectrometry based assay for confirming the involvement of its reactive metabolite in covalent binding

“…Fipexide (Vigilor®, 1‐[2‐(4‐chlorophenoxy)acetyl]‐4‐(3,4‐methylenedioxybenzyl)piperazine), a nootropic drug, acts as a mild stimulant, affecting brain dopamine levels 1–6. It has been shown to increase short‐term memory, learning and cognition; however, it has been withdrawn from the market due to serious toxic effects 7–9.…”