Pronunciation: var-EN-i-kleen TAR-trate
Class: Smoking deterrent
- Tablets 0.5 mg
- Tablets 1 mg
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.
Special PopulationsRenal Function Impairment
Mild Renal Function Impairment (CrCl > 50 mL/min to ≤ 80 mL/min)
Pharmacokinetics unchanged.Moderate Renal Function Impairment (CrCl ≥ 30 mL/min to ≤ 50 mL/min)
Drug exposure increased 1.5-fold.Severe Renal Function Impairment (CrCl < 30 mL/min)
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.
Indications and Usage
Aid to smoking cessation.
None well documented.
Dosage and AdministrationAdults
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. Max dose, 1 mg twice daily.Severe Renal Impairment (CrCl < 30 mL/min)
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 undergoing hemodialysis
0.5 mg once daily max.
- Should be taken after eating and with a full glass of water.
- Consider dosage reduction in patients unable to tolerate the adverse reactions.
- Treat for 12 wk. For patients who have successfully stopped smoking after 12 wk, an additional 12-wk course may increase the likelihood of long-term abstinence.
- Encourage patients who do not succeed in stopping smoking after 12 wk of initial therapy or who relapse to make another attempt once factors contributing to the failure have been identified and addressed.
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.
Laboratory Test Interactions
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/anorexia, lethargy, nightmare (2%); anxiety, depression, disturbances in attention, dizziness, emotional disorder, irritability, restlessness, sensory disturbance (frequent); aggression, agitation, anxiety, delusions, depression, hallucinations, homicidal ideation, hostility, mania, panic, paranoia, psychosis, suicidal ideation, suicide attempt, suicide (postmarketing).
Rash (3%); pruritus (1%); hot flush, hyperhidrosis (frequent); serious skin reactions (eg, erythema multiforme, Stevens-Johnson syndrome) (postmarketing).
Nausea (30%); flatulence (9%); constipation (8%); abdominal pain (7%); dry mouth (6%); dyspepsia, vomiting (5%); gastroesophageal reflux disease (1%); diarrhea, gingivitis, thirst (frequent).
Menstrual disorder, polyuria (frequent).
LFT abnormalities (frequent).
Arthralgia, back pain, muscle cramp, musculoskeletal pain, myalgia (frequent).
Upper respiratory tract disorder (7%); dyspnea (2%); epistaxis (frequent).
Chest pain, edema, influenza-like illness (frequent); hypersensitivity reactions, including angioedema (postmarketing).
Serious neuropsychiatric events, including but not limited to depression, suicidal ideation, suicide attempt, and completed suicide, have been reported in patients taking varenicline. Some reported cases may have been complicated by the symptoms of nicotine withdrawal in patients who stopped smoking.
All patients being treated with varenicline should be observed for neuropsychiatric symptoms, including changes in behavior, hostility, agitation, depressed mood, and suicide-related events such as ideation, behavior, and attempted suicide. These symptoms, as well as worsening of preexisting psychiatric illness and completed suicide, have been reported in some patients attempting to quit smoking while taking varenicline in the postmarketing experience. Symptoms were reported during and after discontinuation of varenicline treatment in patients with and without preexisting psychiatric disease.
Advise patients and caregivers that the patient should stop taking varenicline and contact a health care provider immediately if agitation, hostility, depressed mood, or changes in behavior or thinking that are not typical for the patient are observed, or if the patient develops suicidal ideation or suicidal behavior.
Weigh the risks of varenicline against the benefits of its use.
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.
Hypersensitivity reactions, including angioedema, have been reported.
Use with caution. Dose reduction and monitoring are recommended in patients with severe renal impairment.
Angina, nonfatal stroke, nonfatal MI, and transient ischemic attack have been reported.
Neuropsychiatric symptoms and suicidality
Serious neuropsychiatric symptoms, including depression and, rarely, suicidal ideation, have been reported.
Rare but serious skin reactions, including Stevens-Johnson syndrome and erythema multiforme, have been reported.
None well documented.
- Instruct patient to set a date to quit smoking and to initiate varenicline treatment 1 wk before the date.
- Advise patient to take the dose after eating and with a full glass of water.
- Instruct patient on the recommended dosage regimen.
- Inform patient that the adverse reactions (eg, nausea, insomnia) from treatment are usually transient and to notify health care provider if the reactions are persistently bothersome so that dosage modification can be considered.
- Provide patient with educational material and necessary counseling to support smoking cessation.
- Inform patient that some medications may require dose adjustment after smoking cessation.
- Advise women to notify health care provider if pregnant, planning to become pregnant, or breast-feeding because of the risks of smoking. Explain risks and benefits of smoking cessation.
- Instruct patients and caregivers to stop the product and contact health care provider if agitation, depressed mood, or changes in behavior that are not typical for the patient are observed, or if suicidal ideation or suicidal behavior develops.
- Advise patients to use caution while driving or operating machinery or engaging in other potentially hazardous activities until they know how varenicline may affect them.
- Inform patients that they may experience vivid, unusual, or strange dreams during treatment.
- Advise patients to stop taking the drug if a skin reaction rash with mucosal lesions occurs and to contact a health care provider immediately.
- Instruct patients to discontinue the drug and to immediately seek medical care if angioedema, with swelling of the mouth, face (eg, lip, gum, tongue), and neck (eg, larynx, pharynx) occur.
Copyright © 2009 Wolters Kluwer Health.
More about varenicline
- Other brands: Chantix