Habitrol (Nicotine)

HABITROL®

Novartis Consumer Health

Nicotine

Smoking Cessation Aid

Action And Clinical Pharmacology: Habitrol delivers S(-)-nicotine, the active component of tobacco smoke, transdermally into the systemic circulation, continuously over 24 hours. Habitrol releases S(-)-nicotine in controlled amounts at a rate sufficient to produce plasma nicotine concentrations comparable to trough levels observed in smokers before smoking a cigarette. Because of the low, continuous delivery of S(-)-nicotine through the skin, Habitrol does not produce the rapid increases in plasma nicotine concentrations that occur with cigarette smoking and which are primarily responsible for smoking’s addictive effects. Habitrol has been shown to increase rates of cessation in smokers who are motivated to quit.

Indications And Clinical Uses: As a temporary aid used to facilitate smoking cessation in smokers who strongly desire to give up their smoking habit. Habitrol is intended to be used as part of a smoking cessation strategy and should, whenever possible, be combined with behavior modification therapy.

Contra-Indications: In nonsmokers, occasional smokers and children under 18 years of age (see Warnings).

Known hypersensitivity of the skin, allergy to nicotine or Habitrol components; generalized skin disorders; recovery phase of acute myocardial infarction, unstable or worsening angina pectoris, severe cardiac arrhythmias and recent cerebrovascular accident.

Pregnancy and Lactation: Any form of nicotine administration is contraindicated in pregnant and breast-feeding women.

Manufacturers’ Warnings In Clinical States: In view of its pharmacological effects, S(-)-nicotine should not be used in smokers with the following conditions unless there has been careful consideration of the risks and benefits of therapy: hypertension, stable angina pectoris, variant (Prinzmetal’s) angina, cerebrovascular disease, occlusive peripheral arterial and vasospastic diseases, heart failure, hyperthyroidism, diabetes mellitus, renal and hepatic insufficiency, peptic ulcer. Use of Habitrol in these smokers should only be considered if tobacco withdrawal with psychological support alone has been unsuccessful. If these smokers continue to smoke while wearing Habitrol, excessive nicotine levels could be produced that can exacerbate pre-existing diseases and can cause serious adverse reactions (see Adverse Effects).

Adult smokers tolerate doses of nicotine that can be poisonous or fatal to children and pets. Both new and used Habitrol systems contain enough nicotine to cause serious harm if applied or ingested. Therefore, it is important that smokers keep both new and used systems out of the reach of children and pets (see Information for the Patient for the recommended disposal procedure).

Treatment with Habitrol should be discontinued in cases of severe or persistent skin reactions.

No experience is available on treatment with Habitrol in smokers under 18 years of age and is limited in ages 65 years and above.

Precautions: Continued Smoking and Adverse Reactions: If the user continues to smoke while wearing Habitrol, adverse reactions consistent with excessive nicotine exposure, including cardiovascular effects, may be more frequent and more pronounced.

Strenuous Exercise: Preliminary evidence suggests that wearing a nicotine transdermal patch during periods of strenuous exercise may lead to nicotine toxicity as a result of increased absorption of nicotine from the depot of nicotine in the skin under the patch, due to increased skin temperature and increased cutaneous vasodilation and perfusion from exercising. Three cases illustrating this phenomenon were described in Health Canada Adverse Reaction Newsletter, Volume 6, No. 1, Jan. 1996. Advice to remove the nicotine patch before engaging in strenuous exercise was recommended by: W. Dafoe and P. Huston, Current Trends in Cardiac Rehabilitation, Canadian Medical Association Journal, Feb 15, 1997; 156 (14): 527-532. Until definitive studies have been undertaken to clarify this hazard, it is advisable to remove the nicotine patch prior to engaging in strenuous activity.

Occupational Hazards: Effects on Ability to Drive or Use Machines: Nicotine acts as a central nervous stimulant agent. While no direct effect on reaction time is to be expected, the smoker should be cautioned that sleep disturbance, irritability and nervousness may occur during smoking cessation, and could affect performance.

Drug Interactions: To date, no information is available on interactions between S(-)-nicotine and any other drugs. Experience with other forms of nicotine replacement therapy has shown that there are no pharmacodynamic or pharmacokinetic interactions of clinical relevance with various concomitant treatments.

Tobacco withdrawal, with or without nicotine substitution, may alter the response to concomitant medication in ex-smokers. Through enzyme induction, smoking is thought to increase the metabolism – and thus lower the blood levels – of drugs such as antipyrine, caffeine, phenacetin, imipramine, lidocaine, pentazocine, warfarin, theophylline, oxazepam, lorazepam, desmethyldiazepam and estrogens. Smoking cessation may result in increased blood levels of these drugs, therefore requiring appropriate adaptation of dose. Smoking reduces the analgesic efficacy of propoxyphene. Absorption of s.c. insulin may be increased upon cessation of smoking.

Although the relevance to transdermal nicotine therapy is unknown, reported drug interactions with smoking which do not involve alteration of pharmacokinetics (e.g., enzyme induction) include: increased cortisol concentrations; increased circulating levels of catecholamines necessitating dose adjustments for adrenergic agonists (e.g., phenylephrine, isoproterenol), adrenergic a and b receptor antagonists, (e.g., prazosin and propranolol, respectively) and calcium channel blockers (e.g., nifedipine); reduced diuretic response to furosemide, and reduced clinical efficacy of H2-antagonists.

Cessation of smoking may reverse these actions.

Contact Sensitization to Nicotine: Contact sensitization to nicotine has been reported in transdermal nicotine users. Smokers developing this contact sensitization should be cautioned against using nicotine-containing products. Delayed type hypersensitivity reactions (e.g., generalized urticaria, edema) or severe allergic reactions could result.

Adverse Reactions: In principle, S(-)-nicotine can cause adverse reactions similar to those associated with nicotine administered by smoking, or those that accompany tobacco withdrawal, especially in the gastrointestinal and CNS systems. However, since the plasma S(-)-nicotine concentrations reached with Habitrol are substantially lower and fluctuate less than those produced by smoking, nicotine related adverse reactions occurring during treatment with Habitrol can be expected to be less marked. If the user continues to smoke while wearing Habitrol, adverse reactions consistent with excessive nicotine exposure may be more frequent and more pronounced. Severe and fatal adverse reactions have occurred in smokers who continued to smoke while using nicotine transdermal systems. Smokers are strongly advised to stop smoking during Habitrol therapy, especially high-risk smokers, as described in Warnings.

The most commonly reported adverse effect associated with Habitrol in clinical trials was skin reaction at the application site. This was responsible for about 6% of premature discontinuations and included symptoms such as erythema, pruritus, edema, burning sensation, blisters, rash and pinching. Most cases were mild in severity, usually resolving within 48 hours, but in more severe cases erythema and infiltration lasted 1 to 3 weeks. The majority of cases with notable symptoms of erythema (severity: well-defined, moderate or severe) and edema (severity: very slight, slight or moderate) occurred within 3 to 8 weeks. There have been isolated reports of skin reactions beyond the application site. The incidence of cutaneous hypersensitivity is 1.5 to 2.0%.

Symptoms And Treatment Of Overdose: Symptoms and Treatment: The toxicity of nicotine cannot be directly compared to that of smoking, since tobacco smoke contains additional toxic substances (e.g., carbon monoxide and tar).

Acute Toxic Effects: The acute lethal oral dose of nicotine in nonsmoking adults is about 40 to 60 mg. In children the following signs and symptoms have been reported after ingestion of tobacco products: vomiting, agitation, nausea, diarrhea, pallor, weakness, absence of reaction and twitching of the extremities. In nonsmoking adults the following signs and symptoms have been reported in cases of severe nicotine poisoning: pallor, sweating, nausea, salivation, vomiting, abdominal cramps, diarrhea, headache, dizziness, tremor, mental confusion, hearing and visual disturbances, muscular weakness, convulsions, prostration, absence of neurological reaction and respiratory failure. Lethal doses quickly produce convulsions, and death follows as a result of cardiac failure or (more frequently) peripheral or central respiratory paralysis.

Chronic smoking causes the development of tolerance, which means that chronic smokers can tolerate acute, highly toxic doses of nicotine.

The application of several Habitrol systems simultaneously, could result in serious overdosage. The effects of chewing and swallowing Habitrol are unknown.

Chronic Toxic Effects: No experience has been obtained with S(-)-nicotine treatment longer than 3 months’ duration.

Management of Excessive Topical Exposure: If the smoker shows signs of overdosage, Habitrol should be removed immediately. The skin may be washed with water only, as soap may facilitate absorption. Owing to a depot of nicotine in the skin, delivery of nicotine to the bloodstream will continue for several hours afterward.

Management of Nicotine Poisoning: In cases of severe poisoning, the following measures are recommended: supportive measures for seizure control, warming the body to normal temperature, artificial respiration in the case of respiratory failure, atropine for excessive bronchial secretions and vigorous fluid support for pronounced hypotension or cardiovascular collapse.

Dosage And Administration: When starting treatment with Habitrol, the smoker should stop smoking completely.

One Habitrol system should be applied daily and left on the skin for 24 hours.

If the smoker has been unable to maintain or otherwise re-establish initial abstinence with the aid of Habitrol after 1 month, the treatment should be discontinued.

Prolonged continuous use of Habitrol should not exceed 3 months.

Treatment is divided into 3 components: selection and evaluation of an initial dosage strength, a maintenance phase and a weaning phase. Treatment may be completed in as little as 7 weeks, but more typically lasts 9 to a maximum of 12 weeks. The dosage strengths employed, and the duration of use of each, depend upon the individual smoker’s response. Tobacco withdrawal must be accompanied by behavioral support at all times.

Selection and Evaluation: Treatment is initiated with Habitrol 21 mg/day or 14 mg/day, depending on the number of cigarettes smoked per day. Habitrol 21 mg/day is usually recommended for smokers with a consumption of more than 20 cigarettes a day. Habitrol 14 mg/day is usually sufficient for smokers with a consumption of up to 20 cigarettes daily. The dosage strength may be adjusted early in the maintenance phase in response to either the appearance of side effects or difficulty in maintaining abstinence.

Maintenance: The intial dosage strength selected should generally be worn for 3 to 4 weeks, but this period may be extended. Consideration may be given to an extension of this period to 6 to 8 weeks if Habitrol 14 mg/day was selected as the initial dosage strength.

Weaning: The goal of a stepwise reduction from Habitrol 21 mg/day to the lowest dosage strength is accomplished by an intermediate step employing Habitrol 14 mg/day, typically worn for 3 to 4 weeks, whereas Habitrol 7 mg/day is employed directly after maintenance on Habitrol 14 mg/day. Habitrol 7 mg/day, designed to reduce nicotine substitution toward the end of therapy and consolidate abstinence, should typically be worn for 3 to 4 weeks. The weaning phase may be compressed if the maintenance phase has been extended.

After completing treatment with Habitrol it is advisable for behavioral therapy to be continued.

No experience is available on treatment with Habitrol in smokers below the age of 18 and is limited in ages 65 years and above (see Warnings).

Administration: To avoid evaporative loss of nicotine, and as a matter of safety concerning accidental exposure of children and pets, the system should be applied promptly after its removal from the protective pouch. After removing the release liner (first the smaller strip and then the larger portion), the Habitrol system should be applied to a clean, oil-free, non-hairy, dry, intact area of skin on the trunk, or the upper outer arm. A different site of application should be chosen each day, and no site should be re-used within 1 week. The smoker should be advised that the system not be worn for longer than 24 hours, and to dispose of used systems out of the reach of children and pets. For detailed instructions see Information for the Patient.

Note: Dosage adjustment cannot be achieved by cutting a transdermal system. This will cause the nicotine to evaporate rapidly, and render the pieces ineffective.

Safety Note Concerning Children: Nicotine is a highly toxic substance. Doses of nicotine which are tolerated by adults during treatment with Habitrol can produce severe symptoms of poisoning in small children (see Warnings). Even after use, Habitrol contains more than half its initial nicotine content. Therefore smokers must be cautioned that new and used systems must not be handled casually or left where they may be misused (by application) or ingested.

Similarly, care must also be taken when disposing of used systems (for detailed instructions see Information for the Patient).

Availability And Storage: Nonmedicinal ingredients: acrylate vinylacetate, copolymers, fractionated coconut oil and methacrylic acid esters copolymers

The total amount of S(-)-nicotine in the reservoir is needed to maintain the delivery pattern as required while the system is being worn.

Since the amount of S(-)-nicotine released from Habitrol per cmis constant, the dose administered is determined solely by the size of the contact area of the system.

Boxes of 7 patches. Store below 25°C. Do not store unpouched. Apply immediately upon removal from the protective pouch. (Shown in Product Recognition Section)

HABITROL® Novartis Consumer Health S(-)-Nicotine Smoking Cessation Aid

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