Varenicline


Concise Prescribing Info
Indications/Uses
Smoking cessation aid.
Dosage/Direction for Use
Adult : PO 500 mcg once daily on days 1-3 followed by 500 mcg bid for days 4-7. Maintenance dose (wk 2-12): 1 mg bid.
Dosage Details
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.
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.
Disclaimer: This information is independently developed by MIMS based on Varenicline from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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