|
This information has been developed and provided by an independent third-party source. Merck & Co., Inc. does not endorse and is not responsible for the accuracy of the content, or for practices or
standards of non-Merck sources.
Medication Safety Issues
Sound-alike/look-alike issues:
NicoDerm® may be confused with Nitroderm
Nicorette® may be confused with Nordette®
Transdermal patch may contain conducting metal (eg, aluminum); remove patch prior to MRI.
Pronunciation
(nik oh TEEN)
U.S. Brand Names
Index Terms
Generic Available
Yes: Transdermal patch and gum
Canadian Brand Names
Pharmacologic Category
Use: Labeled Indications
Treatment to aid smoking cessation for the relief of nicotine withdrawal symptoms (including nicotine craving)
Use: Dental
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 (nasal)
Pregnancy Considerations
Nicotine is teratogenic in animal studies. Nicotine exposure via cigarette smoke may cause increased ectopic pregnancy, low birth weight, increased risk of spontaneous abortion, increased perinatal mortality; increased aortic blood flow, increased heart rate, decreased uterine blood flow, and decreased breathing have been reported in the fetus. Smoking during pregnancy is associated with sudden infant death syndrome (SIDS), an increased risk of asthma, infantile colic, and childhood obesity. Women who are pregnant should be encouraged not to smoke. The use of nicotine replacement products to aid in smoking cessation has not been adequately studied in pregnant women (amount of nicotine exposure is varied). Nonpharmacologic treatments are recommended. If the benefits of nicotine replacement therapy outweigh the unknown risks, products with intermittent dosing are suggested to be tried first. If a patch is used, it is suggested to remove it overnight while sleeping to decrease fetal exposure.
Lactation
Excretion in breast milk unknown/use caution
Breast-Feeding Considerations
Nicotine from cigarette smoke is found in breast milk at 1.5-3 times the maternal plasma concentrations. The amount from nicotine replacement products is not known. Women who are breastfeeding are encouraged not to smoke.
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
Disease-related concerns:
• Cardiovascular disease: The risk versus the benefits should be weighed in patients with CAD, serious cardiac arrhythmias, or vasospastic disease; use caution in patients with angina or hypertension.
• Diabetes: Use with caution in patients with insulin-dependent diabetes.
• Gastrointestinal disease: Use with caution in patients with oropharyngeal inflammation, history of esophagitis, or peptic ulcer disease; healing may be delayed.
• Hepatic impairment: Use with caution in patients with severe hepatic impairment; effects on metabolism unknown.
• Hyperthyroidism: Use with caution in patients with hyperthyroidism.
• Pheochromocytoma: Use with caution in patients with pheochromocytoma.
• Renal impairment: Use with caution in patients with severe renal impairment; effects on elimination unknown.
Special populations:
• Pediatrics: Safety and efficacy have not been established in children.
Dosage form specific issues:
• Chewing gum: Dental problems may be worsened by chewing gum.
• Inhaler: Use with caution in patients with bronchospastic disease due to potential airway irritation (other forms of nicotine replacement may be preferred).
• Nasal products: Use of nasal product is not recommended with chronic nasal disorders (eg, allergy, rhinitis, nasal polyps, and sinusitis).
• Topical products: Cautious use of topical nicotine in patients with certain skin diseases. Hypersensitivity to the topical products can occur.
• Transdermal patch: May contain conducting metal (eg, aluminum); remove patch prior to MRI.
Other warnings/precautions:
• Appropriate use: Urge patients to stop smoking completely when initiating therapy.
Adverse Reactions
Nasal spray/inhaler:
>10%:
Central nervous system: Headache (18% to 26%)
Gastrointestinal: Inhaler: Mouth/throat irritation (66%), dyspepsia (18%)
Respiratory: Inhaler: Cough (32%), rhinitis (23%)
1% to 10%:
Dermatologic: Acne (3%)
Endocrine & metabolic: Dysmenorrhea (3%)
Gastrointestinal: Flatulence (4%), gum problems (4%), diarrhea, hiccup, nausea, taste disturbance, tooth disorder
Neuromuscular & skeletal: Back pain (6%), arthralgia (5%), jaw/neck pain
Respiratory: Sinusitis
Miscellaneous: Withdrawal symptoms
<1%: Allergy, amnesia, aphasia, bronchitis, bronchospasm, edema, migraine, numbness, pain, purpura, rash, sputum increased, vision abnormalities, xerostomia
Adverse events previously reported in prescription labeling for chewing gum, lozenge and/or transdermal systems. Frequency not defined; may be product or dose specific:
Central nervous system: Concentration impaired, depression, dizziness, headache, insomnia, nervousness, pain
Gastrointestinal: Aphthous stomatitis, constipation, cough, diarrhea, dyspepsia, flatulence, gingival bleeding, glossitis, hiccups, jaw pain, nausea, salivation increased, stomatitis, taste perversion, tooth disorder, ulcerative stomatitis, xerostomia
Dermatologic: Rash
Local: Application site reaction, local edema, local erythema
Neuromuscular & skeletal: Arthralgia, myalgia, paresthesia
Respiratory: Cough, sinusitis
Miscellaneous: Allergic reaction, diaphoresis
Metabolism/Transport Effects
Substrate (minor) of CYP1A2, 2A6, 2B6, 2C9, 2C19, 2D6, 2E1, 3A4; Inhibits CYP2A6 (weak), 2E1 (weak)
Drug Interactions
Adenosine: Nicotine may enhance the AV-blocking effect of Adenosine. Nicotine may enhance the tachycardic effect of Adenosine. Risk C: Monitor therapy
Cimetidine: May decrease the metabolism of Nicotine. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Food: Lozenge: Acidic foods/beverages decrease absorption of nicotine.
Storage
Nicotrol®: 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.
Oral:
Gum: Chew 1 piece of gum when urge to smoke, up to 24 pieces/day. Patients who smoke <25 cigarettes/day should start with 2-mg strength; patients smoking ?25 cigarettes/day should start with the 4-mg strength. Use according to the following 12-week dosing schedule:
Weeks 1-6: Chew 1 piece of gum every 1-2 hours; to increase chances of quitting, chew at least 9 pieces/day during the first 6 weeks
Weeks 7-9: Chew 1 piece of gum every 2-4 hours
Weeks 10-12: Chew 1 piece of gum every 4-8 hours
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. Use according to the following 12-week dosing schedule:
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)
Topical:
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).
NicoDerm CQ®:
Patients smoking ?10 cigarettes/day: Begin with step 1 (21 mg/day) for 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: Patients receiving >600 mg/day of cimetidine: Decrease to the next lower patch size
Note: Benefits of use of nicotine transdermal patches beyond 3 months have not been demonstrated.
Ulcerative colitis (unlabeled use): Transdermal: Titrated to 22-25 mg/day
Nasal: Spray: 1-2 sprays/hour; do not exceed more than 5 doses (10 sprays) per hour [maximum: 40 doses/day (80 sprays); each dose (2 sprays) contains 1 mg of nicotine]
Dental Usual Dosing
Tobacco cessation (patients should be advised to completely stop smoking upon initiation of therapy): Adults:
Gum: Chew 1 piece of gum when urge to smoke, up to 24 pieces/day. Patients who smoke <25 cigarettes/day should start with 2-mg strength; patients smoking ?25 cigarettes/day should start with the 4-mg strength. Use according to the following 12-week dosing schedule:
Weeks 1-6: Chew 1 piece of gum every 1-2 hours; to increase chances of quitting, chew at least 9 pieces/day during the first 6 weeks
Weeks 7-9: Chew 1 piece of gum every 2-4 hours
Weeks 10-12: Chew 1 piece of gum every 4-8 hours
Inhaler: Oral: 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: Oral: Patients who smoke their first cigarette within 30 minutes of waking should use the 4 mg strength; otherwise the 2 mg strength is recommended. Use according to the following 12-week dosing schedule:
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)
Spray: Nasal: 1-2 sprays/hour; do not exceed more than 5 doses (10 sprays) per hour [maximum: 40 doses/day (80 sprays); each dose (2 sprays) contains 1 mg of nicotine]
Transdermal patch: Topical: 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).
NicoDerm CQ®:
Patients smoking ?10 cigarettes/day: Begin with step 1 (21 mg/day) for 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: 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
Administration: Oral
Gum: Should be chewed slowly to avoid jaw ache and to maximize benefit. Chew slowly until it tingles, then park gum between cheek and gum until tingle is gone; repeat process until most of tingle is gone (~30 minutes).
Lozenge: Should not be chewed or swallowed; allow to dissolve slowly (~20-30 minutes)
Administration: Topical
Do not cut patch; causes rapid evaporation, rendering the patch useless. Use of an aerosol corticosteroid may diminish local irritation under patches.
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
Commit®: Each lozenge contains phenylalanine 3.4 mg and sodium 18 mg.
Nicorette®: Fresh mint and fruit chill flavors: The 2-mg strength contains calcium 94 mg/gum and sodium 11 mg/gum. The 4-mg strength contains calcium 94 mg/gum and sodium 13 mg/gum.
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. Consult prescriber for instruction on appropriate contraceptive measures.
Geriatric Considerations
Must evaluate benefit in the elderly who may have chronic diseases mentioned in Warning and Contraindications. The transdermal systems are as effective in the elderly as they are in younger adults; however, complaints of body aches, dizziness, and asthenia were reported more often in the elderly.
Additional Information
A cigarette has 10-25 mg nicotine.
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, and muscle pain.
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Nursing: Physical Assessment/Monitoring
Monitor cardiac status and vital signs prior to, when beginning, and periodically during therapy. Monitor effectiveness of therapy (according to rationale for therapy), and adverse reactions at beginning and periodically during therapy. Assess knowledge/teach patient appropriate use, interventions to reduce side effects, and adverse symptoms to report for prescribed form of drug.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Gum, chewing, as polacrilex: 2 mg (20s, 50s, 110s); 4 mg (20s, 50s, 110s)
Nicorette®:
2 mg (48s, 50s, 108s, 110s, 168s, 170s, 192s, 200s, 216s) [original and mint flavors]; (48s, 108s, 110s) [orange flavor]; (40s, 100s) [contains calcium 94 mg/gum and sodium 11 mg/gum; fresh mint and fruit chill flavors]
4 mg (48s, 50s, 108s, 110s, 168s, 170s, 192s, 200s, 216s) [original and mint flavors]; (48s, 108s, 110s) [orange flavor]; (40s, 100s) [contains calcium 94 mg/gum and sodium 13 mg/gum; fresh mint and fruit chill flavors]
Thrive™:
2 mg (40s) [gluten free, sucrose free; mint flavor]
4 mg (40s) [gluten free, sucrose free; mint flavor]
Lozenge, as polacrilex:
Commit®:
2 mg (48s, 72s, 84s, 168s) [contains phenylalanine 3.4 mg/lozenge, sodium 18 mg/lozenge; mint flavor]; (108s) [contains phenylalanine 3.4 mg/lozenge, sodium 18 mg/lozenge; original flavor]
4 mg (48s, 72s, 84s, 168s, 192s) [contains phenylalanine 3.4 mg/lozenge, sodium 18 mg/lozenge; mint flavor]; (108s) [contains phenylalanine 3.4 mg/lozenge, sodium 18 mg/lozenge; original flavor]
Oral inhalation system:
Nicotrol® Inhaler: 10 mg cartridge (168s) [cartridge delivers nicotine 4 mg; each unit consists of 5 mouthpieces, 28 storage trays each containing 6 cartridges, and 1 storage case]
Solution, intranasal [spray]:
Nicotrol® NS: 10 mg/mL (10 mL) [delivers 0.5 mg/spray; 200 sprays]
Transdermal system, topical: 7 mg/24 (30s); 14 mg/24 hours (30s); 21 mg/24 hours (30s)
NicoDerm® CQ®: 7 mg/24 hours (14s) [step 3; available in tan or clear patch]; 14 mg/24 hours (14s) [step 2; available in tan or clear patch]; 21 mg/24 hours (7s, 14s) [step 1; available in tan or clear patch]
Pricing: U.S. (www.drugstore.com)
Gum (Nicorette Starter Kit)
4 mg (110): $52.76
Patch, 24-hour (Nicotine)
14 mg/24 hrs (30): $179.98
21 mg/24 hrs (30): $168.99
References
ACOG Committee Opinion, Number 316, October 2005, “Smoking Cessation During Pregnancy,” Obstet Gynecol, 2005, 106(4):883-8.
“American Academy of Pediatrics Committee on Drugs. The Transfer of Drugs and Other Chemicals Into Human Milk,” Pediatrics, 2001, 108(3):776-89.
Benowitz NL, “Pharmacologic Aspects of Cigarette Smoking and Nicotine Addiction,” N Engl J Med, 1988, 319(20):1318-30.
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.
International Brand Names
Lexi-Comp.com
Last full review/revision September 2008
|
