Drug intelligence / Profile preview

cloperastine

Development stage
Unknown
Modality
Small Molecules
Administration
Oral
01

Overview

Cloperastine is a centrally acting antitussive (cough suppressant) and antihistamine. It is used primarily for the relief of cough associated with upper respiratory tract infections and other conditions. The drug acts on the central nervous system, specifically affecting the cough center in the brainstem without depressing respiratory function or causing significant cardiocirculatory effects[1][2][3][5]. Its mechanism of action includes antagonism at histamine H1 receptor (antihistaminic), blockade of G protein-coupled inwardly rectifying potassium (GIRK) channels, sigma receptor agonism, and anticholinergic activity[3][5][6]. These combined actions contribute to its efficacy as an antitussive and its side effect profile, which may include sedation and thickening of bronchial secretions. Cloperastine was first introduced in Japan in 1972 and later marketed in several European countries[5]. It is available as various salts including hydrochloride and fendizoate.

Brand names
NitossilQuikSeki
Other names
cloperastincloperastinacloperastine hydrochloridecloperastine fendizoatecloperastine hybenzoate
02

Targets

SIGMAR1 (Sigma non-opioid intracellular receptor 1)mAChR (Muscarinic acetylcholine receptors)GIRK (G protein-coupled inward-rectifier potassium channel)HRH1 (Histamine H1 Receptor)

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