Drug intelligence / Profile preview

varenicline + hydroxyzine

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

Overview

Varenicline + hydroxyzine is a combination of two pharmaceutical agents: varenicline, a partial agonist of α4β2 nicotinic acetylcholine receptors indicated primarily for smoking cessation, and hydroxyzine, a first-generation antihistamine with sedative and anxiolytic properties. This combination has been studied in an open-label trial for potential synergistic effects in smoking cessation, specifically to reduce common side effects of varenicline such as nausea, stress, anxiety, and sleep disturbances, and to improve overall tolerability and compliance during nicotine withdrawal. Varenicline acts centrally to reduce cravings and withdrawal symptoms via dopaminergic pathways, while hydroxyzine acts as an antagonist at histamine H1 receptors and other neurotransmitter systems, producing sedation and anxiolysis[2][5][4].

02

Targets

HTR2A (Serotonin receptor 5-HT2A)HTR3A (5-hydroxytryptamine receptor 3A)HRH1 (Histamine H1 Receptor)mAChR (Muscarinic acetylcholine receptors)α4β2 nAChR (Nicotinic acetylcholine receptor alpha4 beta2 subtype)α4β4 nAChR (α4β4 nicotinic receptor)α6β2 nAChR (α6β2 nicotinic receptor)CHRNA7 (α7 nicotinic receptor)

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