Trade Names:Chantix- Tablets 0.5 mg- Tablets 1 mgChampix (Canada)
Binds with high affinity and selectivity to neuronal nicotinic acetylcholine receptors, which produces agonist activity while preventing nicotine binding to receptors.
Absorption is virtually complete and exhibits linear pharmacokinetics. C max occurs within 3 to 4 h. Steady state is reached within 4 days.
Plasma protein binding is 20% or less.
Minimal metabolism occurs.
Elimination half-life is approximately 24 h. Excretion is 92% unchanged in the urine.
Pharmacokinetics unchanged.Moderate Renal Function Impairment
Drug exposure increased 1.5-fold.Severe Renal Function Impairment
Drug exposure increased 2.1-fold.End-Stage Renal Disease
Drug exposure increased 2.7-fold.Hepatic Function Impairment
Pharmacokinetics should not be affected.Elderly
Pharmacokinetics in elderly patients (65 to 75 yr of age) are similar to that of younger patients.Gender
Pharmacokinetics not affected.Race
Pharmacokinetics not affected.Smoking status
Pharmacokinetics not affected.
Aid to smoking cessation.
PO 1 mg twice daily subsequent to the following titration: days 1 to 3, 0.5 mg once daily; days 4 to 7, 0.5 mg twice daily; day 8 to end of treatment, 1 mg twice daily.Severe Renal ImpairmentAdults
PO Start with 0.5 mg once daily, then titrate as needed to a max of 0.5 mg twice daily.End-stage renal disease
0.5 mg once daily max.
Store at 59° to 86°F.
Coadministration increased the systemic exposure of varenicline by 29%.Transdermal nicotine
The incidence of adverse reactions may be increased with coadministration.
None well documented.
Hypertension (at least 1%).
Headache, insomnia (19%); abnormal dreams (13%); dysgeusia (8%); fatigue/malaise/asthenia (7%); sleep disorder (5%); increased appetite (4%); somnolence (3%); decreased appetite, lethargy, nightmare (2%); anxiety, depression, disturbances in attention, dizziness, emotional disorder, irritability, restlessness, sensory disturbance (at least 1%); agitation, depressed mood, suicidal ideation, suicide (postmarketing).
Rash (3%); pruritus (1%); hot flush, hyperhidrosis (at least 1%).
Nausea (30%); flatulence (9%); constipation (8%); abdominal pain (7%); dry mouth (6%); dyspepsia, vomiting (5%); gastroesophageal reflux disease (1%); diarrhea, gingivitis, thirst (at least 1%).
Menstrual disorder, polyuria (at least 1%).
LFT abnormalities (at least 1%).
Arthralgia, back pain, muscle cramp, musculoskeletal pain, myalgia (at least 1%).
Upper respiratory tract disorder (7%); dyspnea (2%); epistaxis (at least 1%).
Chest pain, edema, influenza-like illness (at least 1%).
Observe patients for neuropsychiatric symptoms, including agitation, changes in behavior, depressed mood, suicidal behavior, and suicidal ideation.
Category C .
Safety and efficacy not established.
Use with caution because of the greater frequency of decreased renal function.
Use with caution.
Serious neuropsychiatric symptoms have been reported.
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