Varni

Varenicline is indicated for use as an aid to smoking cessation treatment.

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

Electrophysiology studies in vitro and neurochemical studies in vivo have shown that varenicline binds to α4β2 neuronal nicotinic acetylcholine receptors and stimulates receptor-mediated activity, but at a significantly lower level than nicotine. Varenicline blocks the ability of nicotine to activate α4β2 receptors and thus to stimulate the central nervous mesolimbic dopamine system, believed to be the neuronal mechanism underlying reinforcement and reward experienced upon smoking. Varenicline is highly selective and binds more potently to α4β2 receptors than to other common nicotinic receptors ( >500-fold α3β4, >3,500fold α7, >20,000-fold α1βγδ), or to non-nicotinic receptors and transporters (> 2,000-fold). Varenicline also binds with moderate affinity (Ki = 350 nM) to the 5-HT3 receptor.

May increase intoxicating effects of alcohol.

Nasopharyngitis, bronchitis, sinusitis, increased wt, decreased &/or increased appetite, abnormal dreams, insomnia, headache, somnolence, dizziness, dysgeusia, dyspnea, cough, nausea, GERD, vomiting, constipation, diarrhea, abdominal distension & pain, toothache, dyspepsia, flatulence, dry mouth, rash, pruritus, arthralgia, myalgia, back pain, chest pain, fatigue, abnormal liver function test.

Use in Pregnancy: Category C. There are no adequate and well-controlled studies in pregnant women. Varenicline should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus

Use in Lactation: It is unknown whether varenicline is excreted in human breast milk. Animal studies suggest that varenicline is excreted in breast milk. A decision on whether to discontinue breast-feeding or to discontinue therapy with varenicline should be made taking into account the benefit of breast-feeding to the child and the benefit of varenicline therapy to the woman

Discontinue use if changes in behavior or thinking, agitation or depressed mood, anxiety, psychosis, mood swings, aggressive behavior, agitation, depressed mood, suicidal ideation & behavior. Concomitant use in patients attempting to quit smoking. Patients with history of seizures or other conditions that potentially lower seizure threshold. Report if patients had history of psychiatric illness prior to initiation. Hypersensitivity reactions including angioedema, swelling of the face, mouth (tongue, lips, gums), neck (throat & larynx) & extremities. Severe cutaneous reactions including Stevens-Johnson syndrome & erythema multiforme (rare).

Special Precautions for Disposal and Other Handling: No special requirements for disposal.

Drugs used in substance dependence