Varenicline
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Drug Status
Government Approvals
None
WHO Essential Medicine
NO
Known Teratogen
NO
Pharmaceutical Class
Cholinergic Receptor Agonist and Partial Cholinergic Nicotinic Agonist
Controlled Drug Substance
No
Varenicline
Summary
Varenicline is primarily used to help adults quit smoking. It reduces cravings and withdrawal symptoms, making smoking less enjoyable. It's used in smoking cessation programs and may also help reduce dependence on other forms of tobacco.
Varenicline works by binding to nicotine receptors in the brain. It stimulates these receptors mildly to reduce withdrawal symptoms while blocking the pleasurable effects of smoking. This helps individuals gradually stop smoking without feeling intense urges.
Varenicline is taken orally, usually for 12 weeks or longer. The usual dose starts at 0.5 mg once daily for the first three days, then increases to 0.5 mg twice daily for the next four days. From day 8 onward, the standard dose is 1 mg twice daily.
Common side effects of Varenicline include nausea, headaches, trouble sleeping, abnormal dreams, and dry mouth. It can also cause mood changes, suicidal thoughts, depression, or seizures. Some people may experience dizziness, drowsiness, or concentration issues.
People with a history of severe depression, suicidal thoughts, kidney disease, or seizures should avoid Varenicline or use it with caution. It's not recommended for pregnant and breastfeeding women or children under 18 years. Also, drinking alcohol while taking Varenicline can increase the risk of mood changes and aggression.
Indications and Purpose
How does Varenicline work?
Varenicline is a partial agonist at nicotine receptors in the brain. It binds to these receptors, stimulating them mildly to reduce withdrawal symptoms while blocking nicotine’s effects from smoking. This prevents the pleasurable sensation from cigarettes, making it easier to quit.
Is Varenicline effective?
Yes, varenicline has been shown to significantly increase smoking cessation rates compared to placebo and nicotine replacement therapy (NRT). Studies suggest that patients who take varenicline for 12 weeks are more likely to quit smoking permanently. It works best when combined with behavioral support.
What is Varenicline?
Varenicline is a prescription medication used to help people quit smoking. It works by binding to nicotine receptors in the brain, reducing cravings and withdrawal symptoms while blocking the pleasurable effects of smoking. This helps individuals gradually stop smoking without feeling intense urges. It is available in tablet form and is usually taken for 12 weeks or longer.
Directions for Use
For how long do I take Varenicline?
The standard treatment duration is 12 weeks, but doctors may recommend continuing for another 12 weeks to prevent relapse. If a patient struggles to quit, they may continue using varenicline for longer periods under medical supervision.
How do I take Varenicline?
Varenicline should be taken with a full glass of water, after eating, to reduce nausea. It is taken once or twice daily, depending on the stage of treatment. Patients should start taking it one week before their planned quit date. Avoid taking it on an empty stomach to minimize gastrointestinal discomfort.
How long does it take for Varenicline to start working?
Varenicline starts working within one week, but its full effects become noticeable after several weeks of use. Most people experience reduced cravings and withdrawal symptoms within two to four weeks. Patients are advised to set a quit date before starting treatment to maximize its effectiveness.
How should I store Varenicline?
Store varenicline at room temperature (20-25°C) in a dry place away from moisture and heat. Keep it in its original packaging and out of reach of children. Do not store it in the bathroom, where humidity can affect its stability.
What is the usual dose of Varenicline?
The usual dose starts at 0.5 mg once daily for the first three days, then increases to 0.5 mg twice daily for the next four days. From day 8 onward, the standard dose is 1 mg twice daily. The total treatment duration is 12 weeks, but it may be extended if needed for long-term success.
Warnings and Precautions
Can I take Varenicline with other prescription drugs?
Varenicline has no major drug interactions, but it should be used cautiously with medications that affect mental health, kidney function, or seizure risk. Patients taking antidepressants, insulin, or blood thinners should inform their doctor, as dose adjustments may be needed.
Can Varenicline be taken safely while breastfeeding?
Varenicline passes into breast milk, and its effects on infants are unknown. Breastfeeding mothers should avoid using it unless the benefits outweigh the risks. Consulting a doctor for safer alternatives is recommended.
Can Varenicline be taken safely while pregnant?
Varenicline is not recommended during pregnancy due to limited safety data. Studies suggest potential risks to fetal development. Pregnant women trying to quit smoking should consider nicotine replacement therapy (NRT) or behavioral counseling as safer alternatives.
Is it safe to drink alcohol while taking Varenicline?
Drinking alcohol while taking varenicline can increase the risk of mood changes, aggression, or unusual behavior. Some users report feeling more intoxicated than usual after drinking alcohol. To stay safe, limit or avoid alcohol while taking varenicline, especially in the first few weeks.
Is it safe to exercise while taking Varenicline?
Yes, regular exercise is safe and even recommended while taking varenicline. Physical activity can reduce cravings, improve mood, and prevent weight gain after quitting smoking. If you feel dizzy or fatigued during exercise, take a break and stay hydrated.
Is Varenicline safe for the elderly?
Elderly patients can take varenicline, but lower doses may be required, especially in those with kidney impairment. They should be monitored for dizziness, confusion, or mood changes. Dose adjustments are often necessary for older adults.
Who should avoid taking Varenicline?
People with a history of severe depression, suicidal thoughts, kidney disease, or seizures should avoid varenicline or use it with caution. Pregnant and breastfeeding women should consult a doctor before use. It is not recommended for children under 18 years.
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