Drug intelligence / Profile preview

varenicline + prazosin

Development stage
Unknown
Lead developer
Yale University
Modality
Small Molecules
Administration
Oral
01

Overview

Varenicline + prazosin is a combination therapy being investigated by Yale University for the treatment of heavy-drinking cigarette smokers. Varenicline is an FDA-approved smoking cessation aid that acts as a partial agonist at the alpha-4 beta-2 nicotinic acetylcholine receptor, reducing nicotine cravings and withdrawal symptoms. However, varenicline is frequently associated with sleep disturbances, including vivid dreams and insomnia. Prazosin, an alpha-1 adrenergic receptor antagonist traditionally used for hypertension and PTSD-related nightmares, is added to the regimen to mitigate these sleep-related side effects. Beyond improving sleep quality, the combination is being studied for its potential synergistic effects in reducing both nicotine dependence and heavy alcohol consumption in comorbid populations.

Other names
varenicline and prazosin
02

Targets

α4β2 nAChR (Nicotinic acetylcholine receptor alpha4 beta2 subtype)α6β2 nAChR (α6β2 nicotinic receptor)ADRA1A (α1A)α3β2 nAChR (α3β2 nicotinic receptor)CHRNA7 (α7 nicotinic receptor)

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