Nicotine

Action

Supplies nicotine during controlled withdrawal from cigarette smoking. Binds selectively to nicotinic-choliner-gic receptors in central and peripheral nervous systems, autonomic ganglia, adrenal medulla, and neuromuscular junction. At low doses, has a stimulating effect; at high doses, a reward effect.

Availability

Chewing gum: 2 mg, 4 mg

Inhalation: 42 cartridges/system, each containing 10 mg nicotine (delivers 4 mg)

Nasal spray: 10 mg/ml (0.5 mg/spray) in 10-ml bottles (100 doses)

Transdermal patch: 7 mg/day, 11 mg/day, 14 mg/day, 15 mg/day, 21 mg/day, 22 mg/day

Indications and dosages

➣ Adjunctive therapy (with behavior modification) for nicotine withdrawal Transdermal system-

Adults: 21 mg/day transdermally (Habitrol) for 4 to 8 weeks, then 14 mg/day for 2 to 4 weeks, then 7 mg/day for 2 to 4 weeks, for a total of 8 to 16 weeks; patient must wear system 24 hours/day. Or 21 mg/day transdermally (Nicoderm CQ) for 6 weeks, then 14 mg/day for 2 weeks, then 7 mg/day for 2 weeks, for a total of 10 weeks; patient must wear system 24 hours/day. Or 15 mg/day transdermally (one Nicotrol patch) for 6 weeks; patient must wear system 16 hours/day, removing it at bedtime.

Adults, adolescents, and children weighing less than 45 kg (100 lb) who smoke fewer than 10 cigarettes daily or have underlying cardiovascular disease: 14 mg/day transdermally (Habitrol) for 4 to 8 weeks, then 7 mg/day for 2 to 4 weeks, for a total of 6 to 8 weeks; patient must wear system 24 hours/day. Or 14 mg/day transdermally (Nicoderm CQ) for 6 weeks, then 7 mg/day for 2 weeks, for a total of 8 weeks; patient must wear system 24 hours/day. Nasal spray-

Adults: One spray intranasally in each nostril once or twice per hour, up to five times per hour or 40 times per day, for no longer than 6 months Inhalation-

Adults: For optimal response, at least six cartridges inhaled daily for first 3 to 6 weeks, to a maximum of 16 cartridges daily for up to 12 weeks. Patient self-titrates dosage to required nicotine level (usually 6 to 16 cartridges daily), followed by gradual withdrawal over 6 to 12 weeks.

Chewing gum-

Adults: Use as needed depending on smoking urge or chewing rate, or use on fixed schedule q 1 to 2 hours. Initial requirement may range from 18 to 48 mg/day, not to exceed 60 mg/day.

Contraindications

• Hypersensitivity to drug or its components or to menthol (inhaler only)

• Allergy to adhesive (transdermal forms only)

Precautions

Use cautiously in:

• cardiovascular disease, hypertension, bronchospastic disease, diabetes mellitus, pheochromocytoma, peripheral vascular disease, hyperthyroidism, peptic ulcer disease, hepatic disease

• immediately after myocardial infarction, severe arrhythmia, or severe or worsening angina (use not recommended)

• skin disorders (transdermal form)

• dental disorders, esophagitis, pharyngitis, stomatitis (gum form)

• females of childbearing age

• pregnant or breastfeeding patients.

• children under age 18 (safety and efficacy not established).

Administration

• Apply patch when patient awakens and remove patch (as prescribed) at same time each day.

• Administer nasal spray regularly during first week, to help patient get used to irritant effects.

• With inhalation use, give at least six cartridges daily for first 3 to 6 weeks.

• Encourage patient to titrate dosage to level required, followed by gradual withdrawal.

Adverse reactions

CNS: headache, dizziness, drowsiness, poor concentration, nervousness, weakness, paresthesia, insomnia, abnormal dreams

CV: chest pain, hypertension, tachycardia, atrial fibrillation

EENT: sinusitis; pharyngitis (with gum); mouth and throat irritation (with inhaler); nasopharyngeal irritation, rhinitis, sneezing, watering eyes, eye irritation (with nasal spray)

GI: nausea, vomiting, diarrhea, constipation, abdominal pain, dry mouth, dyspepsia; increased salivation, sore mouth (with gum)

GU: dysmenorrhea

Musculoskeletal: joint pain, back pain, myalgia; jaw ache (with gum)

Respiratory: increased cough (with nasal spray or inhaler), bronchospasm

Skin: burning at patch site, erythema, pruritus, cutaneous hypersensitivity, rash, sweating (all with transdermal patch)

Other: abnormal taste, increased appetite (with gum), allergy, hiccups

Interactions

Drug-drug. Acetaminophen, adrenergic antagonists (such as prazosin, labetalol), clozapine, furosemide, imipramine, oxazepam, pentazocine, propranolol and other beta-adrenergic blockers, theophylline: increased effects of these drugs

Bupropion: treatment-emergent hypertension

Insulin: decreased insulin requirement

Isoproterenol, phenylephrine: increased requirements for these drugs

Propoxyphene: decreased nicotine metabolism

Drug-food. Caffeine-containing foods and beverages: increased nicotine effects

Drug-behaviors. Cigarette smoking: increased nicotine metabolism and effects

Patient monitoring

• Assess for signs and symptoms of nicotine withdrawal (irritability, drowsiness, fatigue, headache).

Watch for bronchospasm and evidence of nicotine toxicity (nausea, vomiting, diarrhea, increased salivation, headache, dizziness, visual disturbances).

Patient teaching

Caution patient against any type of smoking during therapy. Urge him to immediately report chest tightness or difficulty breathing.

• If patient uses gum, advise him to chew one piece whenever nicotine craving occurs. Instruct him to chew it slowly until he feels a tingling sensation, then store it between cheek and gum until tingling disappears.

• Instruct patient to apply transdermal patch to clean, dry skin of upper arm or torso when he awakens; to keep it in place when showering, bathing, or swimming; and to remove it at same time each day.

• If patient uses nasal spray, instruct him to tilt head back slightly when spraying. Remind him not to sniff, swallow, or inhale through nose.

• If patient uses inhalation form, teach him to puff continuously for 20 minutes and to use at least six cartridges daily for first 3 to 6 weeks.

• As appropriate, review all significant and life-threatening adverse reactions and interactions, especially those related to the drugs, foods, and behaviors mentioned above.