Black Box Warnings .
Neuropsychiatric Symptoms and Suicidality
monitor for serious neuropsychiatric events incl. behavior change, hostility, agitation, depression, and suicidality as well as worsening of preexisting psychiatric illness which have occurred in pts taking varenicline and after discontinuation; some cases possibly complicated by nicotine withdrawal sx, but also reported in pts who continue to smoke while taking varenicline; weigh varenicline risks vs. benefits of smoking cessation
Adult Dosing .
Dosage forms: 0.5,1
- [1 mg PO bid x11wk]
- Start: 0.5 mg PO qd x3 days, then 0.5 mg PO bid x4 days; Max: 2 mg/day; Info: give w/ food; start drug 1wk before quit date if quit date planned; stop smoking 8-35 days after starting drug if quit date unplanned; initial tx = 12wk (1 start pack + 2 cont. pack); may cont. additional 12wk if initial tx successful
- [adjust dose amount, frequency]
- CrCl <30: start 0.5 mg qd, may incr. to 0.5 mg bid; HD: 0.5 mg qd, no supplement
- [no adjustment]
Peds Dosing .
Peds dosing is currently unavailable or not applicable for this drug.
- hypersens. to drug/class/compon.
- pts <18 yo
- caution if renal impairment
- caution if psychiatric disorder or hx
- caution if cardiovascular dz
Drug Interactions .
nicotinic receptor partial agonist
Adverse Reactions .
- behavioral disturbance
- psychiatric disorder exacerbation
- hypersensitivity rxn
- Stevens-Johnson syndrome
- erythema multiforme
- peripheral vascular dz
- vision changes
- acute renal failure
- GI bleeding
- abnormal dreams
- respiratory disorders
- abdominal pain
- sleep disorders
- appetite changes
- emotional disturbance
- accidental injury
Lactation: Safety Unknown
Cr at baseline; s/sx depression, agitation, behavior changes, suicidality
Metabolism: liver minimally; CYP450: none
Excretion: urine (92% unchanged); Half-life: 24h
Subclass: Dependence, Nicotine
Mechanism of Action
agonizes and blocks alpha-4-beta-2 nicotinic acetylcholine receptors
Manufacturer: Pfizer Inc.
Approximate Retail Price
tablet, film coated:
- 1 mg (1 box, 56 tabs): $222.49
- 0.5 mg and 1 mg (1 box, 11 tabs and 42 tabs): $236.90
tablet, film coated:
- 0.5 mg (56 ea): $221.12
- 1 mg (56 ea): $204.24
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