Drug intelligence / Profile preview

difenidol

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Difenidol is a small molecule antivertigo and antiemetic agent. It is primarily indicated for the treatment of vertigo resulting from conditions such as Meniere's disease or surgery on the middle and inner ear. It is also used to control nausea and vomiting associated with various conditions and to prevent motion sickness. The drug's mechanism of action involves the inhibition of the vestibular system and the chemoreceptor trigger zone (CTZ) in the medulla, likely through muscarinic acetylcholine receptor antagonism. It also improves blood flow in the vertebral artery. Originally developed by Smith, Kline & French as Vontrol, it is now widely produced by various manufacturers, particularly in Asia, where it is often marketed as Cephadol.

Brand names
CephadolVontrol
Other names
diphenidoldifenidol hydrochloride
02

Targets

M1 (Muscarinic acetylcholine receptor M1)ADRA1A (α1A)CHRM4 (M4)CHRM3 (M3)Kir (Inward-rectifier potassium channels)CHRM2 (M2)

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