1. Name Of The Medicinal Product
Nicorette Freshmint 2 mg Lozenge.
2. Qualitative And Quantitative Composition
Each lozenge contains 2 mg nicotine (as nicotine bitartrate dihydrate).
For a full list of excipients, see section 6.1.
3. Pharmaceutical Form
Compressed lozenge.
White to off white, oval, with mint flavour, one side marked with a 3-sided figure containing the letter “n”.
4. Clinical Particulars
4.1 Therapeutic Indications
Nicorette Freshmint 2mg Lozenge 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 Freshmint 2mg Lozenge is indicated in pregnant and lactating women making a quit attempt.
4.2 Posology And Method Of Administration
Nicorette Freshmint Lozenge is suitable for smokers who smoke 20 or fewer cigarettes per day.
Adults and Children over 12 years of age
Nicorette Freshmint 2mg Lozenge 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 lozenge and as soon as they are able, reduce the number of lozenges used until they have stopped completely.
Smokers aiming to reduce cigarettes should take the lozenge, 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.
Most smokers require 8 to 12 lozenges per day, not to exceed 15 lozenges.
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 with the lozenge are recommended to contact their pharmacist or doctor for advice.
Method of administration
One lozenge should be placed in the mouth and allowed to dissolve. Periodically, the lozenge should be moved from one side of the mouth to the other, and repeated, until the lozenge is completely dissolved. You should not chew or swallow the lozenge. You should not eat or drink while a lozenge is in the mouth.
4.3 Contraindications
Hypersensitivity to any of components of the lozenge.
Nicorette Freshmint Lozenge is contraindicated in children under the age of 12 years.
4.4 Special Warnings And Precautions For Use
Any risks which may be associated with the use of NRT are substantially outweighed in virtually all circumstances by the well established dangers of continued smoking.
Underlying cardiovascular disease: In stable cardiovascular disease Nicorette Freshmint Lozenge presents a lesser hazard than continuing to smoke. However dependent smokers currently hospitalised as a result of myocardial infarction, severe dysrhythmia or cerebrovascular accident and who are considered to be haemodynamically unstable should be encouraged to stop smoking with non-pharmacological interventions. If this fails, Nicorette Freshmint Lozenge 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.
Allergic reactions: susceptibility to angioedema and urticaria.
Renal and hepatic impairment: Use 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.
Phaeochromocytoma and uncontrolled hyperthyroidism: Use with caution in patients with uncontrolled hyperthyroidism or phaeochromocytoma as nicotine causes release of catecholamines.
Gastrointestinal Disease: Swallowed nicotine may exacerbate symptoms in patients suffering from oesophagitis, gastric or peptic ulcers and oral NRT preparations should be used with caution in these conditions. Ulcerative stomatitis has been reported.
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, see section 4.9 Overdose.
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.
4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction
No clinically relevant interactions between nicotine replacement therapy and other drugs have 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.
4.6 Pregnancy And Lactation
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 foetus is lower than that expected with smoking tobacco. Stopping completely is by far the best option but if this is not achievable Nicorette Freshmint 2mg Lozenge 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 foetus 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.
4.7 Effects On Ability To Drive And Use Machines
Not applicable.
4.8 Undesirable Effects
Nicorette Freshmint Lozenge 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 Freshmint Lozenge has not been found to cause any serious adverse effects. Excessive consumption of Nicorette Freshmint Lozenge by those who have not been in the habit of inhaling tobacco smoke could possibly lead to nausea, faintness or headaches.
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 stopping smoking. The causality is unclear.
Most of the undesirable effects reported by the patient occur during the first 3-4 weeks after start of treatment. During the first few days of treatment irritation in the mouth and throat may be experienced. Most patients will get used to this sensation after the first few days.
Very common (
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4.9 Overdose
Symptoms: The minimum lethal dose of nicotine in a non-tolerant man has been estimated to be 40 to 60 mg. 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.
5. Pharmacological Properties
5.1 Pharmacodynamic Properties
Pharmacotherapeutic group: Drug used in nicotine dependence.
ATC code: N07B A01
Nicotine is an agonist at nicotine receptors in the peripheral and central nervous system and has pronounced CNS and cardiovascular effects.
Abrupt cessation of the use of tobacco-containing products following a prolonged period of daily use results in a characteristic withdrawal syndrome that includes four or more of the following: dysphoria or depressed mood; insomnia; irritability, frustration or anger; anxiety; difficulty concentrating, restlessness or impatience; decreased heart rate; and increased appetite or weight gain. Nicotine craving is an important element in the withdrawal syndrome after smoking cessation.
Clinical studies have shown that nicotine replacement products can help smokers abstain from smoking by relieving these withdrawal symptoms.
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.
5.2 Pharmacokinetic Properties
Absorption
The amount of nicotine released from a nicotine lozenge that is absorbed depends on the amount of nicotine released in the oral cavity and the amount thereof that is swallowed. Most of the nicotine released in the oral cavity is absorbed through the oral mucosa. Systemic bioavailability of swallowed nicotine is lowered due to first-pass metabolism.
A maximum nicotine plasma concentration of 3-4 ng/mL is achieved after a single dose of the 2 mg lozenge. The total nicotine intake during the day (indicated by AUC) is at least as much as that provided from the Nicorette® Gum 2 mg . AUCafter one single dose of 2 mg lozenge is between 14 and 15 ng/mLxh.
Distribution
The volume of distribution following intravenous administration of nicotine is about 2 to 3 l/kg.
Plasma protein binding of nicotine is less than 5%. Therefore, changes in nicotine binding from use of concomitant drugs or alterations of plasma proteins by disease states would not be expected to have any significant effects on the nicotine pharmacokinetics.
Biotransformation
The average plasma clearance of nicotine is about 70 l/hour and the half-life is approximately 2-3 hours.
Renal Impairment
Progressive severity of renal impairment is associated with decreased total clearance of nicotine. Nicotine clearance was decreased by 50% on average in subjects with severe renal impairment. Raised nicotine levels have been seen in smokers undergoing haemodialysis.
Hepatic Impairment
The pharmacokinetics of nicotine is unaffected in cirrhotic users with mild liver impairment (Child-Pugh score 5) and decreased by 40-50% in cirrhotic users with moderate liver impairment (Child-Pugh score 7). There is no information available in subjects with a Child-Pugh score> 7.
A minor reduction in total clearance of nicotine has been demonstrated in healthy elderly users, however this does not justify adjustment of dosage.
Metabolism
The major eliminating organ is the liver, although the kidney and lung also metabolise nicotine. More than 20 metabolites of nicotine have been identified, all of which are believed to be less active than the parent compound.
The primary metabolite of nicotine in plasma, cotinine, has a half-life of 15 to 20 hours and concentrations that exceed nicotine by 10-fold.
Excretion
The primary urinary metabolites are cotinine (12% of the dose) and trans-3-hydroxy-cotinine (37% of the dose). About 10% of nicotine is excreted unchanged in the urine. As much as 30% of nicotine may be excreted unchanged in the urine with high flow rates and acidification of the urine below pH 5.
5.3 Preclinical Safety Data
Preclinical data indicate that nicotine is neither mutagenic nor genotoxic.
There are no other findings derived from preclinical testing of relevance to the prescriber in determining the safety of the product which have not been considered in other relevant sections of this Summary of Product Characteristics.
6. Pharmaceutical Particulars
6.1 List Of Excipients
Mannitol (E421)
Xanthan gum (E415)
Sucralose (E955)
Acesulfame-K (E950)
Magnesium stearate (E470b)
Peppermint Flavour including Gum Arabic (E414)
6.2 Incompatibilities
Not applicable.
6.3 Shelf Life
2 years.
6.4 Special Precautions For Storage
Do not store above 25ºC.
6.5 Nature And Contents Of Container
Pack sizes:
Aluminium/polyvinylidenechloride/polyvinylchloride blister containing 12 lozenges. Cardboard boxes in pack sizes of 24 or 96 lozenges.
Not all pack sizes may be marketed.
6.6 Special Precautions For Disposal And Other Handling
Any unused product or waste material should be disposed of in accordance with local requirements.
7. Marketing Authorisation Holder
McNeil Products Limited
Foundation Park
Roxborough Way
Maidenhead
Berkshire SL6 3UG
United Kingdom
8. Marketing Authorisation Number(S)
PL 15513/0362
9. Date Of First Authorisation/Renewal Of The Authorisation
9 December 2010
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