Varenicline Tartrate: A New Hope for Those Seeking to Quit Smoking

Smoking is a dangerous habit that harms millions of people worldwide. The World Health Organization (WHO) says smoking causes over seven million deaths every year, making it the top cause of preventable death. Nicotine, the main chemical in tobacco, is very addictive and quitting can be hard because of strong cravings and withdrawal symptoms. Even though many smokers struggle to quit, with replace rates ranging from 60-90%. This shows that better ways to help people stop smoking are needed. ^[1]

Varenicline tartrate is a medicine that helps people quit smoking. It works by affecting parts of the brain that react to nicotine. By partly activating this area, it reduces cravings and withdrawal symptoms, making quitting easier. Studies show that this medicine can make people two to three times more likely to quit compared to those who don’t use it. Varenicline tartrate gives new hope to smokers who want to overcome nicotine addiction. ^[2]

INTRODUCTION OF VARENICLINE TARTRATE

Varenicline tartrate is a special medicine are selective nicotinic acetylcholine receptor partial agonist, chemically designated as 7,8,9,10-tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3] benzazepine, (2R,3R)-2,3-dihydroxybutanedioate (1:1). C₁₃H₁₃N₃.C₄H₆O₆ is molecular formula of varenicline tartrate and molecular weight is 361.4 g/mol. There are white to off-white powder and its soluble in water and organic solvents. Its chemical structure is characterized by a pyrazino[2,3-h][3] benzazepine core, with a dihydroxybutanedioate moiety. This unique structural combination of molecules that allow it to work effectively on nicotine receptors, reducing cravings and withdrawal symptoms in smokers. ^[3]

Fig 1  Chemical Structure of Varenicline Tartrate

MECHANISM OF ACTION

Varenicline Tartrate exerts its therapeutic effect by selectively targeting the α4β2 nicotinic acetylcholine receptor (nAChR) subtype, which plays a crucial role in the reinforcing and rewarding effects of nicotine. Upon binding to the α4β2 nAChR, Varenicline tartrate partially activates the receptor, thereby reducing cravings and withdrawal symptoms associated with nicotine addiction. Additionally, Varenicline Tartrate competitively inhibits nicotine from binding to the α4β2 nAChR, diminishing the pleasurable effects of smoking. By modulating the activity of the α4β2 nAChR, Varenicline Tartrate decreases dopamine release, reduces the motivation to smoke and ultimately helps smokers overcome their addiction. ^[4]

Pharmacokinetics

Varenicline Tartrate is highly absorbed, reaching peak levels in 3-4 hours and spreading widely throughout the body. The breaks it down, mainly through glucuronidation and the body eliminates it through urine. With a 24-hour half-life, it is taken once daily. People with severe kidney problems may clear the drug more slowly leading to higher levels in their system. ^[5]

Pharmacodynamics

Varenicline Tartrate powerfully aids smoking cessation by partially stimulating the α4β2 nicotinic receptor, significantly reducing cravings and withdrawal symptoms. At the same time, it blocks nicotine from binding and diminishing the pleasure of smoking. This dual action effectively lowers the urge to smoke and making quitting easier. Its impact is dose-dependent, with the best results seen at 1-2 mg/day. ^[6]

Therapeutic uses  

Varenicline Tartrate is a highly effective aid for adults trying to quit smoking, helping to reduce cravings, ease withdrawal symptoms and prevent relapse. It is also used off-label to combat smokeless tobacco addiction and nicotine cravings in schizophrenia. Addictively it shows promise in treating other addictions, such as cocaine and cannabis dependence. Overall, it offers a powerful and valuable solution for those determined to overcome nicotine addiction and achieve a smoke-free life. ^[5]

Adverse effects

Varenicline Tartrate is generally well-tolerated but can cause side effects like nausea, headache, dizziness and insomnia. Some may experience vivid dreams or nightmares. Rare but serious risks include seizures, depression, anxiety, heart issues and in rare cases, suicidal thoughts. Careful patient selection and close monitoring help minimize these risks. ^[7]

Contraindications

Varenicline Tartrate is not recommended for those with severe psychiatric disorders, a history of suicidal behaviour or severe kidney disease, as it may worsen these conditions. It should also be avoided by those allergic to it. Pregnant or breastfeeding women should use it only if the benefits clearly outweigh the risks. ^[8]

Table 1:  Summary of Varenicline Tartrate ^[9]