NICOTINE
(nik'o-teen)
Nicotrol NS, Nicotrol Inhaler, Commit
NICOTINE POLACRILEX
Nicorette Gum, Nicorette DS
NICOTINE TRANSDERMAL SYSTEM
Habitrol, Nicoderm, Nicotrol, ProStep
Classifications: central nervous system and autonomic nervous system agent; smoking deterrent; cholinergic (parasympathomimetic)
Pregnancy Category: X (polacrilex); D (nasal spray, transdermal system)

Availability

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.

Actions

Ganglionic cholinergic receptor antagonist, which 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.

Therapeutic 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.

Uses

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.

Contraindications

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 Polacrilex: pregnancy (category X); Nicotine Transdermal System: pregnancy (category D). Safety in children and adolescents is not established.

Cautious Use

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). During lactation, only if benefit of a smoking cessation program outweighs risks.

Route & Dosage

Smoking Cessation
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 1–2 doses (2–4 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 <½ pack/d, or have cardiovascular disease, 14 mg/d x 6 wk, 7 mg/d x 2–4 wk. ProStep: 22 mg/d x 4–8 wk, 11 mg/d x 2–4 wk; weight <45 kg (100 lb), smoke <½ pack/d, or have cardiovascular disease, 11 mg/d x 4–8 wk. Nicotrol: Apply 1 transdermal patch 16 h/d by the following schedule: 15 mg/d x 4–12 wk, 10 mg/d x 2–4 wk, 5 mg/d x 2–4 wk

Administration

Oral

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.

Transdermal

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, indigestion, 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).

Interactions

Drug: May increase metabolism of caffeine, theophylline, acetaminophen, insulin, oxazepam, pentazocine propranolol. Food: Coffee, cola may decrease nicotine absorption from nicotine gum.

Pharmacokinetics

Absorption: Approximately 90% of the nicotine in a piece of gum is released slowly over 15–30 min; rate of release is controlled by vigor and duration of chewing; readily absorbed from buccal mucosa; transdermal 75–90% absorbed through skin; 53–58% of nasal spray is absorbed. Peak: Transdermal 8–9 h; nasal spray 4–15 min. Distribution: Crosses placenta; distributed into breast milk. Metabolism: Metabolized in liver, primarily to cotinine. Elimination: Excreted in urine. Half-Life: 30–120 min.

Nursing Implications

Assessment & Drug Effects

Be aware that transient erythema, pruritus, or burning is common with transdermal patch and usually disappears 24 h after patch removal.
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 occurs.
Be aware that smoking while using the transdermal nicotine patch increases the risk of adverse reactions.
Do not breast feed while taking this drug without consulting physician.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug