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Pronunciation:

(nik oh TEEN)

U.S. Brand Names:

Commit™ [OTC]; NicoDerm® CQ® [OTC]; Nicorette® [OTC]; Nicotrol® Inhaler; Nicotrol® NS; Nicotrol® Patch [OTC]

Synonyms:

Habitrol®

Generic Available:

Yes: Transdermal patch and gum

Canadian Brand Names:

Habitrol®; Nicoderm®; Nicorette®; Nicorette® Plus; Nicotrol®

Use:

Treatment to aid smoking cessation for the relief of nicotine withdrawal symptoms (including nicotine craving)

Use - Unlabeled/Investigational:

Management of ulcerative colitis (transdermal)

Pregnancy Risk Factor:

D (transdermal); X (chewing gum)

Lactation:

Excretion in breast milk unknown/contraindicated

Contraindications:

Hypersensitivity to nicotine or any component of the formulation; patients who are smoking during the postmyocardial infarction period; patients with life-threatening arrhythmias, or severe or worsening angina pectoris; active temporomandibular joint disease (gum); pregnancy; not for use in nonsmokers

Warnings/Precautions:

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. Use with caution in oropharyngeal inflammation and in patients with history of esophagitis, peptic ulcer, coronary artery disease, vasospastic disease, angina, hypertension, hyperthyroidism, pheochromocytoma, diabetes, severe renal dysfunction, and hepatic dysfunction. The inhaler should be used with caution in patients with bronchospastic disease (other forms of nicotine replacement may be preferred). Transdermal patch may contain conducting metal (eg, aluminum); remove patch prior to MRI. 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. Safety and efficacy have not been established in pediatric patients.

Adverse Reactions:

Chewing gum/lozenge:

>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%: Atrial fibrillation, erythema, hypersensitivity reactions, itching

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%: Atrial fibrillation, hypersensitivity reactions, itching, nervousness, taste perversion, thirst, tremor

Overdosage/Toxicology:

Symptoms of overdose include nausea, vomiting, abdominal pain, mental confusion, diarrhea, salivation, tachycardia, respiratory and cardiovascular collapse. Treatment is symptomatic and supportive. Remove patch, rinse area with water, and dry. Do not use soap as this may increase absorption.

Drug Interactions:

Substrate (minor) of CYP1A2, 2A6, 2B6, 2C8/9, 2C19, 2D6, 2E1, 3A4; Inhibits CYP2A6 (weak), 2E1 (weak)

Adenosine: Nicotine increases the hemodynamic and AV blocking effects of adenosine; monitor

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

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

Ethanol/Nutrition/Herb Interactions:

Food: Lozenge: Acidic foods/beverages decrease absorption of nicotine.

Stability:

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

Mechanism of Action:

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.

Pharmacodynamics/Kinetics:

Onset of action: Intranasal: More closely approximate the time course of plasma nicotine levels observed after cigarette smoking than other dosage forms

Duration: Transdermal: 24 hours

Absorption: Transdermal: Slow

Metabolism: Hepatic, primarily to cotinine (¹/5 as active)

Half-life elimination: 4 hours

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

Excretion: Urine

Clearance: Renal: pH dependent

Dosage:

Smoking deterrent: Patients should be advised to completely stop smoking upon initiation of therapy.

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

Inhaler: Usually 6 to 16 cartridges per day; best effect was achieved by frequent continuous puffing (20 minutes); recommended duration of treatment is 3 months, after which patients may be weaned from the inhaler by gradual reduction of the daily dose over 6-12 weeks

Lozenge: Patients who smoke their first cigarette within 30 minutes of waking should use the 4 mg strength; otherwise the 2 mg strength is recommended.

Weeks 1-6: One lozenge every 1-2 hours

Weeks 7-9: One lozenge every 2-4 hours

Weeks 10-12: One lozenge every 4-8 hours

Note: Use at least 9 lozenges/day during first 6 weeks to improve chances of quitting; do not use more than one lozenge at a time (maximum: 5 lozenges every 6 hours, 20 lozenges/day)

Transdermal patch: 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. Note: Adjustment may be required during initial treatment (move to higher dose if experiencing withdrawal symptoms; lower dose if side effects are experienced).

Habitrol®, NicoDerm CQ®:

Patients smoking 10 cigarettes/day: Begin with step 1 (21 mg/day) for 4-6 weeks, followed by step 2 (14 mg/day) for 2 weeks; finish with step 3 (7 mg/day) for 2 weeks

Patients smoking <10 cigarettes/day: Begin with step 2 (14 mg/day) for 6 weeks, followed by step 3 (7 mg/day) for 2 weeks

Note: Initial starting dose for patients <100 pounds, history of cardiovascular disease: 14 mg/day for 4-6 weeks, followed by 7 mg/day for 2-4 weeks

Note: Patients receiving >600 mg/day of cimetidine: Decrease to the next lower patch size

Nicotrol®: One patch daily for 6 weeks

Note: 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.

Ulcerative colitis (unlabeled use): Transdermal: Titrated to 22-25 mg/day

Administration:

Gum: Should be chewed slowly to avoid jaw ache and to maximize benefit.

Lozenge: Should not be chewed or swallowed.

Transdermal patch: Do not cut patch; causes rapid evaporation, rendering the patch useless

Monitoring Parameters:

Heart rate and blood pressure periodically during therapy; discontinue therapy if signs of nicotine toxicity occur (eg, severe headache, dizziness, mental confusion, disturbed hearing and vision, abdominal pain; rapid, weak and irregular pulse; salivation, nausea, vomiting, diarrhea, cold sweat, weakness); therapy should be discontinued if rash develops; discontinuation may be considered if other adverse effects of patch occur such as myalgia, arthralgia, abnormal dreams, insomnia, nervousness, dry mouth, sweating

Dietary Considerations:

Each lozenge contains phenylalanine 3.4 mg.

Patient Education:

Use exactly as directed; do not use more often than prescribed. Stop smoking completely during therapy. Do not smoke, chew tobacco, use snuff, nicotine gum, or any other form of nicotine. Nicotine overdose could occur.

Gum: Chew slowly for 30 minutes. Discard chewed gum away from access by children.

Lozenge: Allow to dissolve slowly in the mouth. Do not chew or swallow lozenge whole. Avoid food or drink 15 minutes prior to, during, or after lozenge.

Transdermal patch: Follow directions in package for dosing schedule and use. Do not cut patches or wear more than one patch at a time. Remove backing from patch and press immediately on skin. Hold for 10 seconds. Apply to clean, dry skin in different site each day. Do not touch eyes; wash hands after application. You may experience vivid dreams and sleep disturbances, 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, and 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 contraceptive measures. This drug may cause severe fetal defects. Do not breast-feed.

Additional Information:

A cigarette has 10-25 mg nicotine. Use of an aerosol corticosteroid may diminish local irritation under patches.

Dental Health: Effects on Dental Treatment:

Key adverse event(s) related to dental treatment: Chewing gum: Excessive salivation, mouth/throat soreness, jaw muscle ache, hiccups, tachycardia, headache (mild), vomiting, belching, nausea, xerostomia (normal salivary flow resumes upon discontinuation), dizziness, nervousness, GI distress, hoarseness, hiccups, and muscle pain.

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

No information available to require special precautions

Dosage Forms:

Gum, chewing, as polacrilex (Nicorette®): 2 mg/square (48s, 108s, 168s); 4 mg/square (48s, 108s, 168s) [mint, orange, and original flavors]

Lozenge, as polacrilex (Commit™): 2 mg, 4 mg [contains phenylalanine 3.4 mg/lozenge; mint flavor]

Oral inhalation system (Nicotrol® Inhaler): 10 mg cartridge [delivering 4 mg nicotine] (42s) [each unit consists of 1 mouthpiece, 7 storage trays each containing 6 cartridges, and 1 storage case]

Patch, transdermal: 7 mg/24 (7s, 30s); 14 mg/24 hours (7s, 14s, 30s); 21 mg/24 hours (7s, 14s, 30s)

Kit: Step 1: 21 mg/24 hours (28s); Step 2: 14 mg/24 hours (14s); Step 3: 7 mg/24 hours (14s) [kit also contains support material]

NicoDerm® CQ® [clear patch]: 7 mg/24 hours (14s); 14 mg/24 hours (14s); 21 mg/24 hours (14s)

NicoDerm® CQ® [tan patch]: 7 mg/24 hours (14s); 14 mg/24 hours (14s); 21 mg/24 hours (7s, 14s)

Nicotrol®: 15 mg/16 hours (7s)

Solution, intranasal spray (Nicotrol® NS): 10 mg/mL (10 mL) [delivers 0.5 mg/spray; 200 sprays]

International Brand Names:

Habitrol® (CA); Nicabate® (AU); Nicoderm® (CA); Nicodon® (NL); Nicogum® (FR); Nicolan® (AT, BR); Nicomax® (ES); Nicopatch® (FR); Nicorette® (AR, AT, AU, BE, BG, CA, CH, CL, CZ, DE, DK, ES, FI, FR, GB, GR, IE, IL, IT, LU, NL, NO, NZ, PL, PT, RO, RU, SE, SG); Nicorette® Plus (CA); Nicotinell® (AT, AU, BE, BG, CH, DE, DK, FI, FR, GB, HU, IE, IL, NL, NO, NZ, PL, SE); Nicotinell TTS® (AR, AT, BE, BR, CL, EG, ES, FR, HK, HU, IL, IN, IT, JO, KW, LB, LU, MT, MX, PL, PT, SG, SI, TH, TR); Nicotrol® (AT, CA, ES, NZ); Nikofrenon® (DE); Niquitin® (BE); Niquitinclear® (FR); NiQuitin CQ® (GB, IE); NiQuitin® (DK); Niquitin® (FR, IL, PL, SE)

References

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Benowitz NL, Jacob P 3rd, and Sachs DP, "Deficient C-oxidation of Nicotine,"Clin Pharmacol Ther, 1995, 57(5):590-4.

Blanchard J, "Nicotine,"Clin Toxicol Rev, 1993, 15:11-2.

Guslandi M, "Long-Term Effects of a Single Course of Nicotine Treatment in Acute Ulcerative Colitis: Remission Maintenance in a 12-month Follow-up Study,"Int J Colorectal Dis, 1999, 14(4-5):261-2.

Harchelroad F, Potts K, Burdick J, et al, "Oral Absorption of Nicotine From Transdermal Therapeutic Systems,"Vet Hum Toxicol, 1992, 34:332.

Landesman-Dwyer S and Emanuel I, "Smoking During Pregnancy,"Teratology, 1979, 19(1):119-26.

Li Wan Po A, "Transdermal Nicotine in Smoking Cessation. A Meta-Analysis,"Eur J Clin Pharmacol, 1993, 45(6):519-28.

Luck W and Nau H, "Nicotine and Cotinine Concentrations in Serum and Urine of Infants Exposed Via Passive Smoking or Milk From Smoking Mothers,"J Pediatr, 1985, 107(5):816-20.

McGee D, Brabson T, McCarthy J, et al, "Four-Year Review of Cigarette Ingestions in Children,"Pediatr Emerg Care, 1995, 11(1):13-6.

Ottervanger JP, Festen JM, de Vries AG, et al, "Acute Myocardial Infarction While Using The Nicotine,"Chest, 1995, 107(6):1765-6.

Pattishall EN, Strope GL, Etzel RA, et al, "Serum Cotinine as a Measure of Tobacco Smoke Exposure in Children,"Am J Dis Child, 1985, 139(11):1101-4.

Ross MP, Revolinski D, and Taurman L, "Green Tobacco Sickness Among Adults in Kentucky,"Vet Hum Toxicol, 1994, 36:360.

Sandborn WJ, "Nicotine Therapy for Ulcerative Colitis: A Review of Rationale, Mechanisms, Pharmacology, and Clinical Results,"Am J Gastroenterol, 1999, 94(5):1161-71.

Sandborn WJ, Tremaine WJ, Offord KP, et al, "Transdermal Nicotine for Mildly to Moderately Active Ulcerative Colitis. A Randomized, Double-blind, Placebo-Controlled Trial,"Ann Intern Med, 1997, 126(5):364-71.

Smolinske SC, Spoerke DG, Spiller SK, et al, "Cigarette and Nicotine Chewing Gum Toxicity in Children,"Hum Toxicol, 1988, 7(1):27-31.

Svensson CK, "Clinical Pharmacokinetics of Nicotine,"Clin Pharmacokinet, 1987, 12(1):30-40.

Thomas GA, Rhodes J, Mani V, et al, "Transdermal Nicotine as Maintenance Therapy for Ulcerative Colitis,"N Engl J Med, 1995, 332(15):988-92.

Transdermal Nicotine Study Group, "Transdermal Nicotine for Smoking Cessation. Six-month Results from Two Multicenter Controlled Clinical Trials,"JAMA, 1991, 266(22):3133-8.

Westman EC, Levin ED, and Rose JE, "The Nicotine Patch in Smoking Cessation,"Arch Intern Med, 1993, 153(16):1917-23.

Wynn RL, "Nicotine Patches in Smoking Cessation,"AGD Impact, 1994, 22:14.

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