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nicotine patch; nicotine transdermal (Habitrol, Nicoderm, Nicotrol, ProStep)
Tradenames: Habitrol, Nicoderm, Nicotrol, ProStep.
Indications:
-> smoking cessation
- patch is the form of nicotine with best compliance, least adverse effects [5]
- not effective [7]
Contraindications:
Caution:
1) esophagitis
2) peptic ulcer
3) coronary artery disease
4) vasospastic disease
5) angina
6) hypertension
7) hyperthyroidism
8) diabetes
9) hepatic dysfunction
not effective in pregnant women [6]
Dosage:
Patch:
1) 14 mg patch (< 10 cigarettes/day, or < 100 lbs, or significant heart disease)
2) step 1: 21 mg patch QD weeks 1-3 step 2: 14 mg patch QD weeks 4-6 step 3: 7 mg patch QD weeks 7-9
3) weekly step intervals may vary patient to patient
4) 8 weeks of use is just as effective as longer use
Habitrol & Nicoderm: 7,14, 21 mg/patch ( 30 systems box).
Nicotrol: 5, 10, 15 mg/patch.
ProStep: 11 & 22 mg/patch.
Pharmacokinetics:
1) 70% of nicotine in patch enters systemic circulation
2) peak concentrations are reached in 2-4 hours
3) steady state levels are achieved on the 2nd day of application
4) obese patients maintain lower concentrations than thin patients
5) elimination: liver & kidney.
Adverse effects:
1) common (> 10%)
- erythema, burning or pruritus at site of application, tachycardia, headache (mild), increased appetite, pruritus, erythema
2) less common (1-10%)
- insomnia, dysmenorrhea, myalgia, nervousness, dry mouth, dizziness, rash, hypertension, cutaneous hypersensitivity, chest pain
3) uncommon (< 1%)
- atrial fibrillation
4) other
- mucosal burning
- light-headedness, dizziness
- stomach ache, indigestion
- hiccups
- hypertension
- use of patch with continued smoking aggravates cardiac problems
Drug interactions:
1) smoking cessation with or without nicotine patches may alter drug metabolism
2) smoking generally increases drug metabolism
3) the following agents may need to be reduced with smoking cessation
a) acetaminophen
b) caffeine
c) propoxyphene
d) imipramine
e) benzodiazepines
f) propranolol
g) theophylline
4) increased insulin absorption may occur with smoking cessation
5) catecholamine & cortisol levels are increased by smoking & by nicotine
Mechanism of action:
1) CNS stimulation in the cortex via the locus ceruleus producing alertness & increased cognitive performance,
2) reward effect in the limbic system
3) at low doses, stimulation occurs; at higher doses, reward effects predominate
General
pharmacologic combination
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Medical Knowledge Self Assessment Program (MKSAP) 11, American
College of Physicians, Philadelphia 1998
- Geriatrics Review Syllabus, American Geriatrics Society,
5th edition, 2002-2004; 7th edition 2010
- Coleman T et al.
A randomized trial of nicotine-replacement therapy patches
in pregnancy.
N Engl J Med 2012 Mar 1; 366:808
PMID: 22375972
http://www.nejm.org/doi/full/10.1056/NEJMoa1109582
- Oncken C.
Nicotine replacement for smoking cessation during pregnancy.
N Engl J Med 2012 Mar 1; 366:846.
PMID: 22375978
http://www.nejm.org/doi/full/10.1056/NEJMe1200136
- Berlin I et al
Nicotine patches in pregnant smokers: randomised, placebo controlled,
multicentre trial of efficacy.
BMJ 2014;348:g1622
PMID: 24627552
http://www.bmj.com/content/348/bmj.g1622
- Brose LS
Helping pregnant smokers to quit
BMJ 2014;348:g1808
PMID: 24620362
http://www.bmj.com/content/348/bmj.g1808
- Alpert HR et al
A prospective cohort study challenging the effectiveness of
population-based medical intervention for smoking cessation
Tob Control doi:10.1136/tobaccocontrol-2011-050129
http://tobaccocontrol.bmj.com/content/early/2012/01/10/tobaccocontrol-2011-050129.abstract
Components
nicotine