No

Smoking Cessation Aid

Treatment to aid smoking cessation for the relief of nicotine withdrawal symptoms

D (transdermal); X (chewing gum)

Hypersensitivity or allergy to nicotine or any components of the system the patient will be using; immediately post-MI; life-threatening arrhythmias; severe or worsening angina; active temporomandibular joint disease (gum only); pregnancy

The risk versus the benefits must be weighed for each of these groups: patients with CAD, serious cardiac arrhythmias, vasospastic disease. Use caution in patients with hyperthyroidism, pheochromocytoma, or insulin-dependent diabetes. Safety and efficacy have not been established in pediatric patients. Cautious use of topical nicotine in patients with certain skin diseases. Hypersensitivity to the topical products can occur. Dental problems may be worsened by chewing the gum. Urge patients to stop smoking completely when initiating therapy.

Chewing gum:

>10%:

Cardiovascular: Tachycardia

Central nervous system: Headache (mild)

Gastrointestinal: Nausea, vomiting, indigestion, excessive salivation, belching, increased appetite

Miscellaneous: Mouth or throat soreness, jaw muscle ache, hiccups

1% to 10%:

Central nervous system: Insomnia, dizziness, nervousness

Endocrine & metabolic: Dysmenorrhea

Gastrointestinal: GI distress, eructation

Neuromuscular & skeletal: Muscle pain

Respiratory: Hoarseness

Miscellaneous: Hiccups

<1% (Limited to important or life-threatening symptoms): Atrial fibrillation, erythema, itching, hypersensitivity reactions,

Transdermal systems:

>10%:

Central nervous system: Insomnia, abnormal dreams

Dermatologic: Pruritus, erythema

Local: Application site reaction

Respiratory: Rhinitis, cough, pharyngitis, sinusitis

1% to 10%:

Cardiovascular: Chest pain

Central nervous system: Dysphoria, anxiety, difficulty concentrating, dizziness, somnolence

Dermatologic: Rash

Gastrointestinal: Diarrhea, dyspepsia, nausea, xerostomia, constipation, anorexia, abdominal pain

Neuromuscular & skeletal: Arthralgia, myalgia

<1% (Limited to important or life-threatening symptoms): Atrial fibrillation, nervousness, tremor, taste perversion, thirst, itching, hypersensitivity reactions

Symptoms of overdose include nausea, vomiting, abdominal pain, mental confusion, diarrhea, salivation, tachycardia, respiratory and cardiovascular collapse

Treatment after decontamination is symptomatic and supportive; remove patch, rinse area with water and dry, do not use soap as this may increase absorption.

CYP2B6 and 2A6 enzyme substrate; CYP1A2 enzyme inducer

Cimetidine increases nicotine concentrations; therefore, may decrease amount of gum or patches needed.

Bupropion: Monitor for treatment-emergent hypertension in patients treated with the combination of nicotine patch and bupropion.

Store inhaler cartridge at room temperature not to exceed 30°C (86°F); protect cartridges from light

Nicotine is one of two naturally-occurring alkaloids which exhibit their primary effects via autonomic ganglia stimulation. The other alkaloid is lobeline which has many actions similar to those of nicotine but is less potent. Nicotine is a potent ganglionic and central nervous system stimulant, the actions of which are mediated via nicotine-specific receptors. Biphasic actions are observed depending upon the dose administered. The main effect of nicotine in small doses is stimulation of all autonomic ganglia; with larger doses, initial stimulation is followed by blockade of transmission. Biphasic effects are also evident in the adrenal medulla; discharge of catecholamines occurs with small doses, whereas prevention of catecholamines release is seen with higher doses as a response to splanchnic nerve stimulation. Stimulation of the central nervous system (CNS) is characterized by tremors and respiratory excitation. However, convulsions may occur with higher doses, along with respiratory failure secondary to both central paralysis and peripheral blockade to respiratory muscles.

Intranasal nicotine may more closely approximate the time course of plasma nicotine levels observed after cigarette smoking than other dosage forms

Absorption: Transdermal: Slow

Metabolism: In the liver, primarily to cotinine, which is 1/5 as active.

Half-life, elimination: 4 hours

Time to peak serum concentration: Transdermal: 8-9 hours

Elimination: Via the kidneys; renal clearance is pH-dependent

Gum: Chew 1 piece of gum when urge to smoke, up to 30 pieces/day; most patients require 10-12 pieces of gum/day

Transdermal patch (patients should be advised to completely stop smoking upon initiation of therapy): Apply new patch every 24 hours to nonhairy, clean, dry skin on the upper body or upper outer arm; each patch should be applied to a different site

Initial starting dose: 21 mg/day for 4-8 weeks for most patients

First weaning dose: 14 mg/day for 2-4 weeks

Second weaning dose: 7 mg/day for 2-4 weeks

Initial starting dose for patients <100 pounds, smoke <10 cigarettes/day, have a history of cardiovascular disease: 14 mg/day for 4-8 weeks followed by 7 mg/day for 2-4 weeks

In patients who are receiving >600 mg/day of cimetidine: Decrease to the next lower patch size

Benefits of use of nicotine transdermal patches beyond 3 months have not been demonstrated

Spray: 1-2 sprays/hour; do not exceed more than 5 doses (10 sprays) per hour; each dose (2 sprays) contains 1 mg of nicotine. Warning: A dose of 40 mg can cause fatalities.

No data reported

No information available to require special precautions

>10% of patients using chewing gum form of product experience excessive salivation, mouth, or throat soreness

Use exactly as directed; do not use more often than prescribed. Stop smoking completely during therapy.

Transdermal patch: Follow directions in package for dosing schedule and use. Do not cut patches. Apply to clean, dry skin in different site each day. Do not touch eyes; wash hands after application. You may experience dizziness or lightheadedness; use caution driving or when engaging in tasks requiring alertness until response to drug is known. For nausea, vomiting or GI upset, small frequent meals, chewing gum, frequent oral care may help. Report persistent vomiting, diarrhea, chills, sweating, chest pain or palpitations, or burning or redness at application site.

Spray: Follow directions in package. Blow nose gently before use. Use 1-2 sprays/hour; do not exceed 5 doses (10 sprays) per hour. Excessive use can result in severe (even life-threatening) reactions. You may experience temporary stinging or burning after spray.

Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Do not get pregnant during or for 1 month following therapy. Consult prescriber for instruction on appropriate barrier contraceptive measures. This drug may cause severe fetal defects. Do not breast-feed.

Patients should be instructed to chew slowly to avoid jaw ache and to maximize benefit; patches cannot be cut; use of an aerosol corticosteroid may diminish local irritation under patches

Inhalation: Each inhaler cartridge delivers 4 mg of nicotine

Patch, transdermal:

Habitrol™[OTC]: 21 mg/day; 14 mg/day; 7 mg/day (30 systems/box)

Nicoderm®[OTC]: 21 mg/day; 14 mg/day; 7 mg/day (14 systems/box)

Nicotrol®: 15 mg/day (gradually released over 16 hours)

ProStep®: 22 mg/day; 11 mg/day (7 systems/box)

Pieces, chewing gum, as polacrilex: 2 mg/square [OTC] (96 pieces/box); 4 mg/square (96 pieces/box)

Spray, nasal: 0.5 mg/actuation [10 mg/mL (200 actuations)] (10 mL)

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