Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2019 Publisher: McNeil Products Limited, Foundation Park, Roxborough Way, Maidenhead, Berkshire, SL6 3UG, UK
Pharmacotherapeutic Group: Drug for treatment of addiction.
ATC Code: N07BA01
Nicorette Inhalator facilitates uptake of nicotine through the buccal mucosa into the venous circulation. The amount taken up alleviates the craving symptoms caused by the absence of nicotine from smoking.
Increased appetite is a recognised symptom of nicotine withdrawal and post-cessation weight gain is common. Clinical trials have demonstrated that Nicotine Replacement Therapy can help control weight following a quit attempt.
The following information is based on data derived from Nicorette 10mg Inhalator:
Nicotine given i.v. has a volume of the distribution of 2 or 3 l/kg with a half life of 1-2 hours. Average plasma clearance is about 1-2 l/min mainly in the liver. More than 20 metabolites are known, all less active than nicotine: cotinine, with a half life of 15-20 hours and concentrations ten times that of nicotine is the main one.
Plasma binding of nicotine below 5% means significant displacement of drugs or nicotine is unlikely. Nicotine is excreted in the urine principally as cotinine (15%), 3-hydroxycotinine (45%), nicotine (10%).
Most inhaled nicotine is absorbed via the buccal mucosa. Forced rapid inhalation over 20 minutes, results in a wide range of nicotine doses (1.3-6.2 mg). On average 2 mg of nicotine is released during 20 minutes of intensive use. Uptake is slow and free of the peaks resultant from cigarette smoking. In normal use, plasma levels of 6-8ng/ml nicotine are obtained – about one third that from smoking, which is equivalent to an hourly 2mg nicotine chewing gum.
When used like a cigarette the inhalator on average delivers 1mg in 80 puffs (e.g. 8 puffs per minute for 10 minutes). When used in this way this results in, a degree of nicotine substitution of about 50% compared to hourly smoking. Peak plasma levels occur within 15 minutes after the end of inhalation. Forced rapid inhalation for 20 minutes per hour for 12 hours achieved steady state plasma levels of 20-25ng/ml.
Ambient temperature affects volatilisation of nicotine, the biologically available dose rising by 35% for each 10°C above 20°C. Use below 15°C is not recommended.
Because the pattern of use if decided by the patient up to a limit of 6 cartridges per day to relieve craving, therapeutic levels of nicotine are individual, dictated by the level of dependence.
None stated.
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