Varenicline: Indication, Dosage, Side Effect, Precaution

Generic Medicine Info Patient Medicine Information

This information is not country-specific. Please refer to the local prescribing information.

Generic Medicine Info

Indications and Dosage

Oral
Smoking cessation aid

Adult: 500 mcg once daily for the 1st 3 days, followed by 500 mcg bid for the next 4 days. Maintenance (wk 2-12): 1 mg bid. Initiate dose 1-2 wk prior to target quit date; may temporarily reduce dose to 500 mcg bid if adverse effects are not tolerable. Usual treatment duration: 12 wk. May continue for another 12 wk to reduce relapse in patients who have successfully quit after the initial treatment course.
Elderly: No dosage adjustment needed.

Special Patient Group

Dosage adjustments are required for elderly w/ decreased renal function.

Renal Impairment

Mild to moderate: No dosage adjustment needed. Severe: Initially 500 mcg once daily then increase to max 500 mcg bid after 3 days. Haemodialysis: Max 500 mcg once daily.

Hepatic Impairment

No dosage adjustment needed.

Special Precautions

Increased CV events (MI, stroke) in patients w/ underlying CV diseases may require immediate medical attention or discontinuation. Childn <18 yr. Pregnancy and lactation.

Adverse Reactions

Nausea (dose-related) and other GI disturbances, depression, headaches, dizziness, somnolence, fatigue, sleep disturbances (abnormal dreams, insomnia), increased appetite.
Potentially Fatal: Angioedema, Stevens-Johnson syndrome, erythema multiforme.

Pregnancy Category (US FDA)

PO: C

Patient Counseling Information

First signs of hypersensitivity or angioedema seek immediate medical attention. May impair ability to drive or operate machineries.

MonitoringParameters

Monitor for neuropsychiatric symptoms; atypical behaviour (suicidal ideation, suicidal behaviour) during and after therapy.

Drug Interactions

Increased incidence of adverse effects (nausea, vomiting) w/ transdermal nicotine. Increased exposure w/ cimetidine.

Lab Interference

Abnormal LFT.

Action

Description: Is a partial neuronal α₂β₂ nicotinic acetylcholine receptor agonist. It works as a smoking cessation aid by preventing nicotine stimulation of mesolimbic dopamine system. It also stimulates dopamine activity but to a much lesser extent than nicotine does, resulting in reduced craving and withdrawal symptoms.
Pharmacokinetics:
Absorption: Well absorbed from the GI tract. Bioavailability: Approx 90%. Time to peak plasma concentration: 3-4 hr.
Distribution: Plasma protein binding: <20%.
Metabolism: Minimal metabolism.
Excretion: Via urine (approx 92% as unchanged drug, <10% as metabolites). Elimination half-life: Approx 24 hr.

Storage

Store between 15-30°C.

MIMS Class

Drugs Used in Substance Dependence

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