VARENICLINE

brands

Class

• Neuroscience-based Nomenclature: acetylcholine receptor partial agonist (ACh-RPA)
• Smoking cessation treatment; alpha 4 beta 2 partial agonist at nicotinic acetylcholine receptors

VARENICLINE commonly prescribed for

(Bold for FDA approved)

How VARENICLINE works

• Causes sustained but small amounts of dopamine release (less than with nicotine)

• Specifically, as a partial agonist at alpha 4 beta 2 nicotinic acetylcholine receptors, varenicline activates these receptors to a lesser extent than the full agonist nicotine and also prevents nicotine from binding to these receptors

• Most prominent actions are on mesolimbic dopaminergic neurons in the ventral tegmental area

How long until VARENICLINE works

• Recommended initial treatment trial is 12 weeks; an additional 12-week trial in individuals who stop smoking after 12 weeks may increase likelihood of long-term abstinence

Notable Side Effects

• Dose-dependent nausea, vomiting, constipation, flatulence

• Insomnia, headache, abnormal dreams

Life Threatening Side Effects

• Rare activation of agitation, depressed mood, suicidal ideation, suicidal behavior

• Rare seizures

weight gain

unusual

sedation

unusual

What to do about VARENICLINE side effects

• Wait

• Adjust dose

• If side effects persist, discontinue use

usual dosage range

• 1 mg twice daily

Dosage Forms

• Tablet 0.5 mg, 1 mg

long term use

• Treatment for up to 24 weeks has been found effective

habit forming

• No

Renal Impairment

• Severe impairment: initial dose 0.5 mg once daily; maximum recommended dose 0.5 mg twice daily

• End-stage renal disease undergoing hemodialysis: maximum recommended dose is 0.5 mg once daily if tolerated

• Removed by hemodialysis

Hepatic Impairment

• Dose adjustment not generally necessary

Cardiac Impairment

• Effective in patients with cardiovascular disease; small increased risk of certain cardiovascular adverse effects in these patients

Elderly

• Some patients may tolerate lower doses better

Children and Adolescents

• Not shown to be effective for patients 16 years and younger

Pregnancy

• Controlled studies have not been conducted in pregnant women

• Pregnant women wishing to stop smoking may consider behavioral therapy before pharmacotherapy

• Not generally recommended for use during pregnancy, especially during first trimester

Breast Feeding

• Unknown if varenicline is secreted in human breast milk, but all psychotropics are assumed to be secreted in breast milk

• Recommended either to discontinue drug or bottle feed