Drug intelligence / Profile preview

pentoxyverine

Development stage
Phase 1
Modality
Small Molecules
Administration
Oral
01

Overview

Pentoxyverine is a non-opioid centrally acting antitussive (cough suppressant) used to relieve cough associated with the common cold, flu, bronchitis, and sinusitis. It is available as an active ingredient in over-the-counter cough suppressants either alone or in combination with other agents such as guaifenesin and H1-receptor antagonists. Pentoxyverine exhibits antimuscarinic (anticholinergic), anticonvulsant, spasmolytic, bronchodilating, and local anesthetic properties. Its primary mechanism of action involves agonism at sigma-1 receptors in the central nervous system; it also acts as an antagonist at muscarinic receptors (notably M1 subtype). The drug suppresses the cough reflex by acting on the cough center in the brainstem. Unlike opioid antitussives such as codeine, pentoxyverine does not cause withdrawal symptoms and has a lower risk of respiratory depression[2][3][6]. The FDA has withdrawn oral gel formulations containing pentoxyverine citrate from use in the United States; however other forms remain marketed elsewhere[2].

Brand names
SolotussCertuss
Other names
pentoxyverine citratepentoxyverine hydrochloridecarbetapentane citratecarbetapentane hydrochloride
02

Targets

CHRM2 (M2)SIGMAR1 (Sigma non-opioid intracellular receptor 1)M1 (Muscarinic acetylcholine receptor M1)TMEM97 (Sigma-2 receptor complex (TMEM97/PGRMC1))HTR3A (5-hydroxytryptamine receptor 3A)

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