varenicline (systemic)

Contraindicated in:

Hypersensitivity;
Lactation: Lactation.

Use Cautiously in:

Severe renal impairment (↓ dose recommended if CCr <30 mL/min);
Stable cardiovascular disease (may ↑ risk of cardiovascular events);
Psychiatric illness;
Seizure disorders;
OB: Use during pregnancy only if potential maternal benefit outweighs potential fetal risk;
Pedi: Safety not established in children;
Geri: Consider age-related ↓ in renal function in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: flushing, hyperhidrosis, acne, dermatitis, dry skin, STEVENS-JOHNSON SYNDROME (SJS)

EENT: blurred vision, visual disturbances

GI: diarrhea, gingivitis, nausea, ↑appetite, ↑liver enzymes, constipation, dyspepsia, dysphagia, enterocolitis, eructation, flatulence, gallbladder disorder, GI bleeding, vomiting

Hemat: anemia

MS: arthralgia, back pain, musculoskeletal pain, muscle cramps, myalgia, restless legs

Neuro: ↓attention span, depression, dizziness, insomnia, irritability, restlessness, abnormal dreams, aggression, agitation, amnesia, anxiety, delusions, disorientation, dissociation, hallucinations, HOMICIDAL THOUGHTS/BEHAVIOR, hostility, mania, migraine, mood changes, panic, paranoia, psychosis, SEIZURES, sleepwalking, STROKE, SUICIDAL THOUGHTS/BEHAVIOR

Misc: accidental injury, chills, fever, HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA), mild physical dependence

Interactions ⬆ ⬇

Drug-drug:

Smoking cessation may ↓ metabolism of theophylline, warfarin, and insulin resulting in ↑ effects; careful monitoring is recommended.
Risk of adverse reactions (nausea, vomiting, dizziness, fatigue, headache) may be ↑ with nicotine replacement therapy (nicotine transdermal patches).
Concomitant use with alcohol may ↑ risk of worsening neuropsychiatric events

Availability ⬆ ⬇

(Generic available)

Tablets: 0.5 mg; 1 mg

Route/Dosage ⬆ ⬇

PO (Adults ): Treatment is started one wk prior to planned smoking cessation (may also begin dosing and then quit smoking between days 8 and 35 of treatment); 0.5 mg once daily on the first three days, then 0.5 mg twice daily for the next 4 days, then 1 mg twice daily.

Renal Impairment

PO (Adults ): CCr <30 mL/min: 0.5 mg daily, may ↑ to 0.5 mg twice daily.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Selectively binds to alpha₄, beta₂ nicotinic acetylcholine receptors, acting as a nicotine agonist; prevents the binding of nicotine to receptors.

Therapeutic effects:

Decreased desire to smoke.

Classifications ⬆ ⬇

Therapeutic Classification: smoking deterrents

Pharmacologic Classification: nicotine.agonists

Pharmacokinetics ⬆ ⬇

Absorption: 100% absorbed following oral administration.

Distribution: Unknown.

Metabolism/Excretion: Minimally metabolized; 92% excreted in urine unchanged.

Half-Life: 24 hr.

Canadian Brand Names ⬆ ⬇

Time/Action Profile ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
PO	unknown	3–4 hr	24 hr

Patient/Family Teaching ⬆ ⬇

Instruct patient to take varenicline as directed. Set a date to stop smoking. Start taking varenicline 1 wk before quit date. Patient may also begin varenicline and then quit smoking between days 8 and 35 of therapy. Begin with 0.5 mg/day for the first 3 days, then for the next 4 days take one 0.5 mg tablet in the morning and in the evening. After first 7 days, increase to 1 mg tablet in the morning and evening. Advise patient to read Medication Guide before starting therapy and with each Rx refill in case of changes.
Encourage patient to attempt to quit, even if they had early lapses after quit day.
Advise patient to stop taking varenicline and contact health care professional promptly if agitation, depressed mood, any changes in behavior that are not typical of nicotine withdrawal, or if suicidal thoughts or behavior; rash with mucosal lesions or skin reaction, or chest pain, pressure, or dyspnea occur. Encourage patient to reduce amount of alcohol consumed until effects of medication are known.
Provide patient with educational materials and counseling to support attempts to quit smoking.
Caution patient not to share varenicline with others. May be harmful.
May cause blurred vision, dizziness, and disturbance in attention. Caution patient to avoid driving and other activities requiring alertness until response to medication is known.
Inform patient that nausea, insomnia, and vivid, unusual, or strange dreams may occur and are usually transient. Advise patient to notify health care professional if these symptoms are persistent and bothersome; dose reduction may be considered.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications. Inform patient that some medications may require dose adjustments after quitting smoking.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Monitor breastfed infants for seizures and excessive vomiting.

section name header

Indications ⬇

Contraind./Precautions ⬆ ⬇