Varenicline

— THERAPEUTIC CATEGORIES —
  • Smoking

Varenicline Generic Name & Formulations

General Description

Varenicline (as tartrate) 0.5mg, 1mg; tabs.

Pharmacological Class

Nicotinic acetylcholine receptor agonist.

How Supplied

Contact supplier

Mechanism of Action

Varenicline binds with high affinity and selectivity at α4β2 neuronal nicotinic acetylcholine receptors. The efficacy of varenicline in smoking cessation is believed to be the result of its activity at α4β2 sub-type of the nicotinic receptor where its binding produces agonist activity, while simultaneously preventing nicotine binding to these receptors.

Varenicline Indications

Indications

Smoking cessation aid.

Varenicline Dosage and Administration

Adult

Provide patients with counseling and educational support. Set a target "quit date". Begin therapy 1 week before target quit date. Alternatively, may begin therapy and then quit smoking between Days 8 and 35 of treatment. Take after eating with a glass of water. Initially 0.5mg once daily on Days 1–3, then 0.5mg twice daily on Days 4–7, then 1mg twice daily thereafter. May reduce dose if intolerable nausea or other adverse effects occur. Treat for 12 weeks; may continue 12 more weeks if patient successfully stops smoking to further increase the likelihood of abstinence. Patients who are not able or willing to quit abruptly: consider a gradual approach; begin varenicline dosing and reduce smoking by 50% from baseline within the 1st four weeks, by an additional 50% in the next four weeks, and continue reducing with the goal of complete abstinence by 12 weeks; continue for a total of 24 weeks of treatment. If patient motivated to quit and did not succeed, encourage another attempt with varenicline once factors contributing to failed attempt have been addressed. Severe renal impairment: initially 0.5mg once daily; may titrate to max 0.5mg twice daily. ESRD with hemodialysis: max 0.5mg once daily if tolerated.

Children

≤16yrs: not recommended. 17–19yrs: not established.

Varenicline Contraindications

Not Applicable

Varenicline Boxed Warnings

Not Applicable

Varenicline Warnings/Precautions

Warnings/Precautions

Monitor for neuropsychiatric adverse events (eg, behavioral changes, agitation, depression, suicidal ideation); evaluate and consider dose reduction, continue therapy under closer monitoring, or discontinuation if occur. Pre-existing psychiatric disorders. History of seizures or other factors that can lower seizure threshold. Cardiovascular disease; monitor for new or worsening signs/symptoms. Renal impairment. Elderly. Pregnancy. Nursing mothers: monitor infant.

Varenicline Pharmacokinetics

Elimination

Renal. Half-life: ~24 hours.

Varenicline Interactions

Interactions

May affect alcohol tolerance; reduce alcohol consumption until effects are known. Smoking cessation may affect metabolism of other drugs (eg, warfarin, theophylline, insulin). Increased adverse effects with nicotine replacement therapy.

Varenicline Adverse Reactions

Adverse Reactions

Nausea, other GI effects (eg, constipation, flatulence, vomiting), sleep disturbance (eg, abnormal dreams, insomnia); nicotine withdrawal symptoms (due to smoking cessation), neuropsychiatric symptoms (may be serious), cardiovascular events; seizures, somnambulism, angioedema, hypersensitivity reactions, serious skin reactions (rare); discontinue if occurs.

Varenicline Clinical Trials

See Literature

Varenicline Note

Notes

Formerly known under the brand name Chantix.

Varenicline Patient Counseling

See Literature

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