Nicotrol NS, Nicotrol Inhaler, Commit
Nicorette Gum, Nicorette DS
NICOTINE TRANSDERMAL SYSTEM
Habitrol, Nicoderm, Nicotrol, ProStep
Classifications: smoking deterrent; cholinergic; Therapeutic: smoking deterrent
Pregnancy Category: D (nasal spray, transdermal system); C (gum)
2 mg, 4 mg gum; 2 mg, 4 mg lozenges; 0.5 mg spray; 4 mg inhaler; 7 mg/d, 14 mg/d, 21 mg/d, 5 mg/d, 10 mg/d, 15 mg/d, 11 mg/d, 22 mg/d transdermal patch
Ganglionic cholinergic receptor antagonist that has both adrenergic and cholinergic effects. Include stimulant and depressant
effects on the peripheral nervous system and CNS; respiratory stimulation; peripheral vasoconstriction; increased heart rate,
contractile force cardiac output, and stroke volume; increased tone and motor activity of GI smooth muscles; increased bronchial
secretions (initially); antidiuretic activity. Heavy smokers are tolerant of these effects.
Rationale for use of nicotine is to reduce withdrawal symptoms accompanying cessation of smoking. Success rate appears to
be greatest in smokers with high "physical" type of nicotine dependence.
In conjunction with a medically supervised behavior modification program, as a temporary and alternate source of nicotine
by the nicotine-dependent smoker who is withdrawing from cigarette smoking.
Nonsmokers, immediate post-MI period; life-threatening arrhythmias; active temporomandibular joint disease; severe angina
pectoris; women with childbearing potential (unless effective contraception is used). Nicotine Gum: pregnancy (category C); Nicotine Transdermal, Inhaler System: pregnancy (category D). Safety in children and adolescents is not established.
Vasospastic disease (e.g., Buerger's disease, Prinzmetal's variant angina), cardiac arrhythmias, hyperthyroidism, type 1
diabetes, pheochromocytoma, esophagitis, oral and pharyngeal inflammation; patient with dentures, denture caps, or partial
bridges; hypertension and peptic ulcer disease (active or inactive); GERD. During lactation, only if benefit of a smoking
cessation program outweighs risks.
Route & Dosage
Adult: PO Chew 1 piece of gum whenever have urge to smoke, may be repeated as needed (max: 30 pieces of gum/d) Intranasal 1 dose = 2 sprays, 1 in each nostril, start with 12 doses (24 sprays) each hour (max: 5 doses/h, 40 doses/d),
may continue for 3 mo Topical Apply 1 transdermal patch q24h by the following schedule: Habitrol, Nicoderm: 21 mg/d x 6 wk, 14 mg/d x 2 wk, 7 mg/d x 2 wk; weight <45 kg (100 lb), smoke pack/d, or have cardiovascular disease, 14 mg/d x 6 wk, 7 mg/d x 24 wk ProStep: 22 mg/d x 48 wk, 11 mg/d x 24 wk; weight <45 kg (100 lb), smoke pack/d, or have cardiovascular disease, 11 mg/d x 48 wk. Nicotrol: Apply 1 transdermal patch 16 h/d by the following schedule: 15 mg/d x 412 wk, 10 mg/d x
24 wk, 5 mg/d x 24 wk
- Note: Most adverse local effects (irritation of tongue, mouth, and throat, jaw-muscle aches, dislike of taste) are transient and
subside in a few days. Modification of the chewing technique may help.
- Remove the old patch before applying the next new patch.
- Apply patch to nonhairy, clean, dry skin site; immediately remove from protective container.
- Store at or below 30° C (86° F); patches are sensitive to heat.
Adverse Effects (≥1%)CNS: Headache, dizziness, light-headedness, insomnia
, irritability, dependence on nicotine. CV:
Arrhythmias, tachycardia, palpitations, hypertension. GI:
Air swallowing, jaw ache, nausea,
belching, salivation, anorexia, dry mouth, laxative effects, constipation
diarrhea, dyspepsia, vomiting, sialorrhea, abdominal pain, diarrhea. Respiratory: Sore mouth or throat, cough, hiccups,
hoarseness; injury to mouth, teeth, temporomandibular joint pain, irritation/tingling of tongue. Skin: Erythema, pruritus, local edema, rash;
skin reactions may be delayed, occurring after 3 wk of patch use. Special Senses: Runny nose, nasal irritation, throat irritation, watering eyes,
minor epistaxis, nasal ulceration. Body as a Whole:
Acute overdose/nicotine intoxication (perspiration; severe headache; dizziness; disturbed hearing and vision; mental confusion;
severe weakness; fainting; hypotension; dyspnea; weak, rapid, irregular pulse; seizures); death
(from respiratory failure
secondary to drug-induced respiratory muscle paralysis
May increase metabolism of caffeine, theophylline, acetaminophen, insulin, oxazepam, pentazocine propranolol. Food:
Coffee, cola may decrease nicotine absorption from nicotine gum.
Approximately 90% of the nicotine in a piece of gum is released slowly over 1530 min; rate of release is controlled
by vigor and duration of chewing; readily absorbed from buccal mucosa; transdermal 7590% absorbed through skin;
5358% of nasal spray is absorbed. Peak:
Transdermal 89 h; nasal spray 415 min. Distribution:
Crosses placenta; distributed into breast milk. Metabolism:
In liver, primarily to cotinine. Elimination:
In urine. Half-Life:
Assessment & Drug Effects
- Be aware that transient erythema, pruritus, or burning is common with transdermal patch and usually disappears 24 h after
- Differentiate cutaneous hypersensitivity (contact sensitization) that does not resolve in 24 h from a transient local reaction.
The former is an indication to discontinue the transdermal patch.
Patient & Family Education
- Review carefully specific written instructions packaged with the chewing gum.
- Chew a piece of gum for approximately 30 min to get the full dose of nicotine.
- Chew only one piece of gum at a time. Chewing gum too rapidly can cause excessive buccal absorption and lead to adverse
effects: nausea, hiccups, throat irritation.
- Gradually decrease number of pieces of gum chewed in 24 h. Usually, a period of 3 mo is allowed before tapering use of gum.
- Promptly discontinue use of transdermal patch and notify physician if a severe or persistent local or generalized skin reaction
- Be aware that smoking while using the transdermal nicotine patch increases the risk of adverse reactions.