nicotine
Habitrol, Nicoderm CQ, Nicotrol, Nicotrol Inhaler, Nicotrol NS

Available forms
Available without a prescription
Transdermal system: Designed to release nicotine at a fixed rate
Habitrol: 21 mg daily, 14 mg daily, and 7 mg daily
Nicoderm CQ: 21 mg daily, 14 mg daily, 7 mg daily
Nicotrol: 15 mg daily
Available by prescription only
Nasal spray: Metered spray pump
Nicotrol NS: 10 mg/ml, supplying 0.5 mg of nicotine/actuation
Oral inhaler: Nicotrol inhaler-10 mg cartridge, supplying 4 mg of nicotine

Indications and dosages
 Relief of nicotine withdrawal symptoms in patients trying to stop smoking. Adults: One transdermal system applied to a nonhairy part of the upper trunk or upper outer arm. Dosage varies slightly with product selected.
Habitrol, Nicoderm  
Initially, one 21-mg daily system applied daily for 6 weeks. After 24 hours, system removed and a new system applied to a different site. Then, dosage tapered to 14 mg daily for 2 to 4 weeks. Finally, dosage tapered to 7 mg daily if needed. Nicotine substitution and gradual withdrawal should take 8 to 12 weeks. If patient experiences vivid dreams or sleep disturbances, remove patch h.s. and apply a new patch in a.m.
≡ Dosage adjustment. Patients who weigh less than 45 kg (99 lb), have CV disease, or smoke less than half a pack of cigarettes daily should start therapy with the 14-mg daily system.
Nicotrol
Adults: One 15-mg system applied daily for 6 weeks. System applied upon waking and removed h.s. because patch provides systemic delivery over 16 hours.
Nicotrol Inhaler
Adults: Initial dose is 6 to 16 cartridges daily. Best effect is achieved with continuous puffing. Recommended treatment is up to 3 months and, if needed, gradual reduction over the next 6 to 12 weeks.
Nicotrol NS
Adults: Initially, 1 or 2 doses/hour (1 dose = 1 spray in each nostril for a total of 1 mg). Encourage patient to use at least the recommended minimum of eight doses daily. Maximum recommended dose is five 1-mg doses per hour or 40 mg (80 sprays) daily. Treatment shouldn’t exceed 3 months, with dosage reduced gradually during those 3 months. Safety beyond 6 months hasn’t been established.

Pharmacodynamics
Nicotinic cholinergic action: Nicotine transdermal system and nasal spray provide nicotine, the chief stimulant alkaloid found in tobacco products, which stimulates nicotinic acetylcholine receptors in the CNS, neuromuscular junction, autonomic ganglia, and adrenal medulla.

Pharmacokinetics
Absorption: Rapidly absorbed.
Distribution: Plasma protein-binding of drug is below 5%.
Metabolism: Metabolized by the liver, kidney, and lungs. Over 20 metabolites have been identified. Primary metabolites are cotinine (15%) and trans-3-hydroxycotinine (45%).
Excretion: Excreted primarily in urine as metabolites; about 10% is excreted unchanged. With high urine flow rates or acidified urine, up to 30% can be excreted unchanged.

Contraindications and precautions
Contraindicated in patients hypersensitive to nicotine or its components. Also contraindicated in nonsmokers and in patients with recent MI, life-threatening arrhythmias, and severe or worsening angina pectoris.
  Use cautiously in patients with hyperthyroidism, pheochromocytoma, insulin-dependent diabetes, or peptic ulcer disease.

Interactions
Drug-drug. Acetaminophen, caffeine, imipramine, oxazepam, pentazocine, propranolol, theophylline: Cessation of smoking may decrease induction of hepatic enzymes responsible for metabolizing certain drugs. Dosage reduction of these drugs may be needed.
Adrenergic agonists, such as isoproterenol and phenylephrine; adrenergic antagonists, such as labetalol and prazosin: Cessation of smoking may decrease levels of circulating catecholamines. Dosage adjustment of these drugs may be needed.
Insulin: Cessation of smoking may increase the amount of S.C. insulin absorbed. Adjust insulin dosage.
Propoxyphene: Cessation of smoking may increase first-pass metabolism of propoxyphene. Dose adjustments may be needed.
Drug-herb. Blue cohosh: Increases nicotine effects. Tell patient not to use together.
Drug-food. Caffeine: May decrease induction of hepatic enzymes that help metabolize certain drugs. Dosage reductions may be needed.

Adverse reactions
CNS: somnolence, dizziness, headache, insomnia, paresthesia, abnormal dreams, nervousness.
CV: hypertension.
EENT: pharyngitis, sinusitis.
GI: abdominal pain, constipation, dyspepsia, nausea, diarrhea, vomiting, dry mouth.
GU: dysmenorrhea.
Musculoskeletal: back pain, myalgia.
Respiratory: increased cough.
Skin: local or systemic erythema, pruritus, burning at application site, cutaneous hypersensitivity, rash, diaphoresis.

Effects on lab test results
None reported.

Overdose and treatment
Overdose could produce symptoms caused by acute nicotine poisoning, including nausea, vomiting, diarrhea, weakness, respiratory failure, hypotension, and seizures.
 Treat symptomatically. Barbiturates or benzodiazepines may be used to treat seizures, and atropine may attenuate excessive salivation or diarrhea. Administer fluids for hypotension; increase urine flow to enhance elimination of drug.

Special considerations
• Transdermal nicotine has been used investigationally to manage ulcerative colitis.
• Discourage use of transdermal system for longer than 3 months. Chronic nicotine consumption by any route can be dangerous and habit-forming.
• Patients who can’t stop cigarette smoking during the first 4 weeks of therapy probably won’t benefit from continued use of drug. They may benefit from counseling to identify factors that helped to prevent cessation. Encourage patient to minimize or eliminate factors that contributed to treatment failure and to try again, possibly after some interval.
• Health care workers’ exposure to the nicotine in the transdermal systems should be minimal; however, avoid unnecessary contact with the system. After contact, wash hands with water alone because soap can enhance absorption.
• Nicotrol NS isn’t recommended for patients with chronic nasal disorders or severe reactive airway disease.
• Increased cough is a common occurrence in patients using the inhaler.
• Although use of nicotine replacement therapy isn’t recommended in patients with recent MI, it may be preferable to cigarette smoking in patients experiencing withdrawal.
Breast-feeding patients
• Nicotine passes freely into breast milk and is readily absorbed after oral use. Weigh the infant’s risk of exposure to nicotine against the risk of exposure from continued smoking by the mother.
Pediatric patients
• Safety and efficacy in children haven’t been established.
• The amount of nicotine in a patch could prove fatal to a child if ingested; even used patches contain a substantial amount of residual nicotine.

Patient education
• Tell patient to remove patch and to immediately report a generalized rash or persistent or severe local skin reactions, such as pruritus, edema, or erythema.
• Make sure patient understands that nicotine can evaporate from the transdermal system once it’s removed from its protective packaging. Explain that patch should be applied promptly after removing protective packaging.
• Caution patient not to alter the patch (by folding or cutting, for example) before applying it.
• Tell patient not to store patch at temperatures above 86° F (30° C).
• Teach patient how to dispose of transdermal system by removing it and folding it in half by bringing the adhesive sides together. If the system comes in a protective pouch, tell patient to dispose of used patch in the pouch that contained the new system. Stress that careful disposal is needed to prevent accidental poisoning of children or pets.
• Make sure patient reads and understands the information dispensed with drug.
• Urge patient not to smoke while using the system because increased nicotine levels could cause adverse effects.
• Explain that patient is likely to experience nasal irritation, which may become less bothersome with continued use of Nicotrol NS.
• Warn patient to keep used and unused transdermal systems and metered spray bottles safely out of the reach of children and pets.

Reactions may be common, uncommon, life-threatening, or COMMON AND LIFE THREATENING.
◆ Canada only
◇ Unlabeled clinical use