Nicorette® Inhalator / Boots NicAssist 10 mg Inhalator

Nicotine 10mg per cartridge.

For excipients see section 6.1

Inhalation cartridge for oromucosal use.

Nicorette Inhalator relieves and/or prevents craving and nicotine withdrawal symptoms associated with tobacco dependence. It is indicated to aid smokers wishing to quit or reduce prior to quitting, to assist smokers who are unwilling or unable to smoke, and as a safer alternative to smoking for smokers and those around them.

Nicorette Inhalator is indicated in pregnant and lactating women making a quit attempt.

Adults and Children over 12 years of age

Nicorette Inhalator should be used whenever the urge to smoke is felt or to prevent cravings in situations where these are likely to occur.

Smokers willing or able to stop smoking immediately should initially replace all their cigarettes with the Inhalator and as soon as they are able, reduce the number of cartridges used until they have stopped completely.

Smokers aiming to reduce cigarettes should use the Inhalator, as needed, between smoking episodes to prolong smoke-free intervals and with the intention to reduce smoking as much as possible.

As soon as they are ready smokers should aim to quit smoking completely.

Maximum daily dose: 12 cartridges.

When making a quit attempt behavioural therapy, advice and support will normally improve the success rate. Those who have quit smoking, but are having difficulty discontinuing their Inhalator are recommended to contact their pharmacist or doctor for advice.

Each cartridge can be used for approximately 4 sessions, with each cartridge lasting approximately 20 minutes of intense use. The more the subject is able to use the inhalator, the easier it will be to achieve maximum reduction of cigarettes and/or quit smoking completely.

Method of administration

The cartridge is inserted into the mouthpiece according to the instructions.

When a patient draws air into the mouth through the mouthpiece, nicotine is vaporised and absorbed by the buccal mucosa. Minimal nicotine reaches the lungs. The amount of nicotine from a puff is less than that from a cigarette. To compensate for less nicotine delivery from a puff it is necessary to inhale more often than when smoking a cigarette.

The number of cartridges, frequency, puffing/inhalation time and technique does vary between individuals.

The actual time that the cartridge is active depends on the intensity of use. After about 20 minutes of intense use the maximal dose is achieved and it is about then that the nicotine amounts released from the cartridge begin to fall away, such that the cartridge is rejected by the user.

Hypersensitivity to any component of the inhalator.

Nicorette Inhalator is contraindicated in children under the age of 12 years.

Any risks that may be associated with NRT are substantially outweighed by the well established dangers of continued smoking.

Underlying cardiovascular disease: In stable cardiovascular disease Nicorette Inhalator presents a lesser hazard than continuing to smoke. However dependent smokers currently hospitalised as a result of myocardial infarction, severe dysrhythmia or CVA and who are considered to be haemodynamically unstable should be encouraged to stop smoking with non-pharmacological interventions. If this fails, Nicorette Inhalator may be considered, but as data on safety in this patient group are limited, initiation should only be under medical supervision.

Diabetes mellitus: Patients with diabetes mellitus should be advised to monitor their blood sugar levels more closely than usual when NRT is initiated as catecholamines released by nicotine can affect carbohydrate metabolism.

GI disease: Swallowed nicotine may exacerbate symptoms in patients suffering from oesophagitis, gastritis or peptic ulcers and oral NRT preparations should be used with caution in these conditions. Ulcerative stomatitis has been reported.

Renal or hepatic impairment: Nicorette Inhalator should be used with caution in patients with moderate to severe hepatic impairment and/or severe renal impairment as the clearance of nicotine or its metabolites may be decreased with the potential for increased adverse effects.

Danger in small children: Doses of nicotine tolerated by adult and adolescent smokers can produce severe toxicity in small children that may be fatal. Products containing nicotine should not be left where they may be misused, handled or ingested by children.

Phaeochromocytoma and uncontrolled hyperthyroidism: As nicotine causes release of catecholamines, Nicorette Inhalator should be used with caution in patients with uncontrolled hyperthyroidism or phaeochromocytoma.

Transferred dependence: Transferred dependence is rare and is both less harmful and easier to break than smoking dependence.

Stopping smoking: Polycyclic aromatic hydrocarbons in tobacco smoke induce the metabolism of drugs metabolised by CYP 1A2 (and possibly by CYP 1A1). When a smoker stops smoking, this may result in slower metabolism and a consequent rise in blood levels of such drugs. This is of potential clinical importance for products with a narrow therapeutic window, e.g. theophylline, clozapine and ropinirole.

Lung Disease

Patients with obstructive lung disease may find use of the Inhalator difficult. Nicotine Gum, Patch, Nasal Spray or Sublingual tablet may be preferred in such cases. Nicorette Inhalator should be used with caution in patients with chronic throat disease and bronchospastic disease.

Potential choking hazard: This product contains some small parts. Any unused cartridges should remain in the cartridge tray to minimise the risk of swallowing.

No clinically relevant interactions between nicotine replacement therapy and other drugs has definitely been established. However nicotine may possibly enhance the haemodynamic effects of adenosine i.e. increase in blood pressure and heart rate and also increase pain response (angina-pectoris type chest pain) provoked by adenosine administration.

Pregnancy

Stopping smoking is the single most effective intervention for improving the health of both the pregnant smoker and her baby, and the earlier abstinence is achieved the better. Ideally smoking cessation during pregnancy should be achieved without NRT. However, if the mother cannot (or is considered unlikely to) quit without pharmacological support, NRT may be used as the risk to the fetus is lower than that expected with smoking tobacco. Stopping completely is by far the best option but if this is not achievable Nicorette Inhalator may be used in pregnancy as a safer alternative to smoking. Because of the potential for nicotine-free periods, intermittent dose forms are preferable, but patches may be necessary if there is significant nausea and/or vomiting. If patches are used they should, if possible, be removed at night when the fetus would not normally be exposed to nicotine.

Lactation

The relatively small amounts of nicotine found in breast milk during NRT use are less hazardous to the infant than second-hand smoke. Intermittent dose forms would minimize the amount of nicotine in breast milk and permit feeding when levels were at their lowest.

Not applicable.

Some symptoms may be related to nicotine withdrawal associated with stopping smoking. These can include; irritability/aggression, dysphoria/depressed mood, anxiety, restlessness, poor concentration, increased appetite/weight gain, urges to smoke (cravings), night-time awakenings/sleep disturbance and decreased heart rate.

Increased frequency of aphthous ulcer may occur after abstinence from smoking. The causality is unclear.

Nicorette Inhalator may cause adverse reactions similar to those associated with nicotine given by other means, including smoking, and these are mainly dose-dependent. At recommended doses Nicorette Inhalator has not been found to cause any serious adverse effects. Excessive use of Nicorette Inhalator by those who have not been in the habit of inhaling tobacco smoke could possibly lead to nausea, faintness or headaches.

Most of the undesirable effects reported by the patient occur during the first weeks after starting treatment. About 40% of users experience mild local reactions such as cough and irritation in the mouth and throat.

Reported adverse events associated with Nicorette Inhalator include:

* Very common (>1/10); common (>1/100, <1/10); uncommon (>1/1 000, <1/100); rare (>1/10 000, <1/1 000); very rare (<1/10 000), including isolated reports.

Symptoms: The minimum lethal dose of nicotine in a non-tolerant man has been estimated to be 40 to 60mg. Symptoms of acute nicotine poisoning include nausea, salivation, abdominal pain, diarrhoea, sweating headache, dizziness, disturbed hearing and marked weakness. In extreme cases, these symptoms may be followed by hypotension, rapid or weak or irregular pulse, breathing difficulties, prostration, circulatory collapse and terminal convulsions.

Management of an overdose: All nicotine intake should stop immediately and the patient should be treated symptomatically. Artificial respiration should be instituted if necessary. Activated charcoal reduces the gastro-intestinal absorption of nicotine

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.

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 are 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 will remove 40% of the nicotine from the cartridge. 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, and equivalent to an hourly 2mg nicotine chewing gum.

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 12 cartridges per day to relieve craving, therapeutic levels of nicotine are individual, dictated by the level of dependence.

None stated.

Levomenthol

None relevant.

Two years.

Store below 30°C.

This product works best at room temperature. In cold conditions (below 15°C) the nicotine evaporates less readily and it will be necessary to inhale more frequently, whilst in warm conditions (above 30°C) nicotine will evaporate more readily and inhalation should be less frequent to avoid overdose.

Polypropylene mouthpiece with acrylonitril / methacrylate copolymer cartridges containing polyethylene porous plugs with polyester / aluminium 60μm foil seals.

The cartridges are provided in a PVC tray which is sealed with 20μm aluminium foil.

All packs contain 1 inhalator mouthpiece with either 6, 18 or 42 inhalation cartridges.

Potential choking hazard: This product contains some small parts. Any unused cartridges should remain in the cartridge tray to minimise the risk of swallowing.

Because of residual nicotine, used cartridges may be a hazard to children, animals and fish and so should never be thrown away or left lying around. They should be kept in the case and disposed of with household rubbish.

McNeil Products Limited

Foundation Park

Roxborough Way

Maidenhead

Berkshire

SL6 3UG

UK

PL 15513/0179

01 February 2008

13 January 2010