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NICABATE A 2 MG MINT LOZENGES
Active substance(s): NICOTINE POLACRILEX
NAME OF THE MEDICINAL PRODUCT
Nicabate A 2 mg Mint Lozenges
QUALITATIVE AND QUANTITATIVE COMPOSITION
Each lozenge contains 2 mg nicotine (as 11.1 mg nicotine polacrilex) as the
Each lozenge includes the excipients aspartame (E951), sodium alginate and
sodium carbonate anhydrous.
For full list of excipients see Section 6.1.
White, round lozenge with convex surfaces, debossed NL2S on one side.
Nicabate A Mint Lozenges are indicated for the relief of nicotine withdrawal
symptoms including cravings. Permanent cessation of tobacco use is the
eventual objective. Nicabate A Mint Lozenges can be used:
for smoking cessation (abrupt and gradual)
as an aid for smokers during temporary abstinence.
Nicabate A Mint Lozenges should preferably be used in conjunction with a
behavioural support programme.
Posology and method of administration
Directions for use:
Nicabate A 2 mg Mint Lozenges are suitable for smokers who have their first
cigarette of the day more than 30 minutes after waking up.
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 (approximately 20 – 30 minutes). The lozenge
should not be chewed or swallowed whole.
Users should not eat or drink while a lozenge is in the mouth.
Behavioural therapy, advice and support will normally improve the success rate.
Adults (18 years and over):
Abrupt cessation of smoking:
Users should make every effort to stop smoking completely during treatment with
Nicabate A Mint Lozenges.
Recommended treatment schedule:
Weeks 1 to 6
Initial treatment period
1 lozenge every 1 to
Weeks 7 to 9
Step down treatment
1 lozenge every 2 to
Weeks 10 to 12
Step down treatment
1 lozenge every 4 to
During weeks 1 to 6 it is recommended that users take a minimum of 9 lozenges per
day. Users should not exceed 15 lozenges per day.
To help stay smoke free beyond 12 weeks, users may take 1-2 lozenges per day only
on occasions when they are strongly tempted to smoke
Those who use the lozenges beyond 9 months are recommended to seek additional
help and advice from a healthcare professional.
Gradual cessation of smoking:
Use a lozenge whenever there is a strong urge to smoke in order to reduce the number
of cigarettes smoked as far as possible and to refrain from smoking as long as
The number of lozenges a day is variable and depends on the patients needs.
If a reduction in cigarette consumption has not been achieved after 6 weeks of
treatment, a healthcare professional should be consulted.
Reduced tobacco consumption should lead to complete cessation of smoking. This
should be attempted as soon as possible. When the number of cigarettes has been
reduced to a level from which the user feels able to quit completely, then start on the
If an attempt to stop smoking completely has not been started within 6 months after
the beginning of treatment, it is recommended to consult a healthcare professional.
Use a lozenge every 1-2 hours to control troublesome withdrawal symptoms
including cravings. Users should not take more than 15 lozenges per day.
Users should be encouraged to stop smoking completely as soon as possible.
If users are still feeling the need to use lozenges on a regular basis 6 months after the
start of treatment and have still been unable to undertake a permanent quit attempt,
then it is recommended to seek additional help and advice from a healthcare
Adolescents and children:
Adolescents (12-17 years) should follow the schedule of treatment for abrupt
cessation of smoking as given above, but as data are limited, duration of NRT in this
age group is restricted to 12 weeks. If longer treatment is required, or where
adolescents are unwilling or unable to quit smoking abruptly, advice from a
healthcare professional should be sought.
Nicabate A Mint Lozenges are not recommended for use in children under 12 years
Nicabate A Mint Lozenges are contraindicated in:
those with hypersensitivity to nicotine or any of the excipients;
those allergic to soya;
children under the age of 12 years and non-smokers.
Special warnings and precautions for use
The risks associated with the use of NRT are substantially outweighed in
virtually all circumstances by the well established dangers of continued
Patients hospitalised for MI, severe dysrhythmia or CVA who are considered
to be haemodynamically unstable should be encouraged to stop smoking with
non-pharmacological interventions. If this fails, Nicabate A Mint Lozenges
may be considered, but as data on safety in this patient group are limited,
initiation should only be under medical supervision. Once patients are
discharged from hospital they can use NRT as normal.
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
A risk-benefit assessment should be made by an appropriate healthcare
professional for patients with the following conditions:
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
Phaeochromocytoma and uncontrolled hyperthyroidism: Use with caution in
patients with uncontrolled hyperthyroidism or phaeochromocytoma as nicotine
causes release of catecholamines.
GI 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
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.
Stopping smoking: Polycyclic aromatic hydrocarbons in tobacco smoke induce
the metabolism of drugs catalysed by CYP 1A2 (and possibly by CYP 1A1).
When a smoker stops this may result in a slower metabolism and a consequent
rise in blood levels of such drugs.
Transferred dependence: Transferred dependence is rare and is both less
harmful and easier to break than smoking dependence.
Phenylketonuria: Nicabate A Mint Lozenges contain a source of
phenylalanine equivalent to 3mg/dose. May be harmful for people with
Sodium content: Each Nicabate A Mint Lozenge contains 15 mg of sodium.
People on a low sodium diet should take this into account.
Patients with rare hereditary problems of galactose intolerance, the Lapp
lactase deficiency or glucose-galactose malabsorption should not take this
Interactions with other Medicaments 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. Smoking cessation itself may require the
adjustment of some drug therapy.
Pregnancy and lactation
Smoking during pregnancy is associated with risks such as intra-uterine
growth retardation, premature birth or stillbirth. Stopping smoking is the
single most effective intervention for improving the health of both pregnant
smoker and her baby. The earlier abstinence is achieved the better.
Ideally smoking cessation during pregnancy should be achieved without NRT.
However for women unable to quit on their own, NRT may be recommended
to assist a quit attempt. The risk of using NRT to the fetus is lower than that
expected with tobacco smoking, due to lower maximal plasma nicotine
concentration and no additional exposure to polycyclic hydrocarbons and
However, as nicotine passes to the fetus affecting breathing movements and
has a dose dependent effect on placental/fetal circulation, the decision to use
NRT should be made as early on in the pregnancy as possible. The aim should
be to use NRT for only 2-3 months.
Intermittent dosing products may be preferable as these usually provide a lower
daily dose of nicotine than patches. However patches may be preferred if the
woman is suffering from nausea during pregnancy. If patches are used they
should be removed before going to bed.
Nicotine from smoking and NRT is found in breast milk. However the amount of
nicotine the infant is exposed to from NRT is relatively small and less
hazardous than the second-hand smoke they would otherwise be exposed to.
Using intermittent dose NRT preparations, compared with patches, may minimize
the amount of nicotine in the breast milk as the time between
administrations of NRT and feeding can be more easily prolonged.
Effects on ability to drive and use machines
NRT can cause adverse reactions similar to those associated with nicotine
administered in other ways including smoking. These may be attributed to the
pharmacological effects of nicotine, some of which are dose dependent. At
recommended doses Nicabate A Mint Lozenges have not been found to cause
any serious adverse effects. Excessive consumption of Nicabate A Mint
Lozenges by those who have not been in the habit of inhaling tobacco smoke
could possibly lead to nausea, faintness or headaches.
Certain symptoms which have been reported such as depression, irritability,
anxiety and insomnia may be related to withdrawal symptoms associated with
smoking cessation. Subjects quitting smoking by any means could expect to
suffer from headache, dizziness, sleep disturbance, increased coughing or a
Related adverse events with excess in active compared to placebo group in
a controlled study.
Immune system disorders
Very rare <1/10000: anaphylactic reactions
Platelet bleeding and clotting disorders
Uncommon >1/1000; <1/100: gingival bleeding; nosebleed
Common >1/100; <1/10: insomnia; anxiety; irritability; increased appetite
Uncommon >1/1000; <1/100: anger; aggravated anxiety; abnormal
dreaming; abnormal hunger; mood swings; wakefulness
Central and peripheral nervous system disorders
Common >1/100; <1/10: headache
Uncommon >1/1000; <1/100: lightheaded feeling; localised numbness
Heart rate and rhythm disorders
Uncommon >1/1000; <1/100: aggravated palpitations; palpitations;
Vascular (extracardiac) disorders
Uncommon >1/1000; <1/100: vascular disorder; flushing; skin flushed
Respiratory system disorders
Common >1/100; <1/10: pharyngitis
Uncommon >1/1000; <1/100: laryngismus; aggravated asthma; lower
respiratory tract infection; coughing; nasal irritation; throat irritation; nasal
Gastrointestinal system disorders
Very common >1/10: nausea
Common >1/100; <1/10: vomiting; dyspepsia, heartburn, indigestion;
hiccup; mouth irritation, mouth ulceration; tongue ulceration; diarrhoea;
Uncommon >1/1000; <1/100: peptic ucler; dysphagia; aggravated
dyspepsia; gastroesophageal reflux; hiatus hernia; oesophagitis; eructation;
buccal mucosa ulceration; borborygmus; dry lips; dry throat; tongue
disorder; tooth ache
Special senses other, disorders
Uncommon >1/1000; <1/100: parageusia, metallic taste; taste perversion
Skin and appendages disorders
Uncommon >1/1000; <1/100: erythema; itching; rash; skin reaction
localised; increased sweating
Musculoskeletal system disorders
Uncommon >1/1000; <1/100: jaw pain
Urinary system disorders
Uncommon >1/1000; <1/100: nocturia
Body as a whole - general disorders
Uncommon >1/1000; <1/100: overdose effect; pain; leg pain; oedema legs
The minimum lethal dose of nicotine in a non tolerant man has been estimated to be
40 to 60 mg. Even small quantities of nicotine may be dangerous in children and may
prove fatal. Suspected nicotine poisoning in a child should be considered a medical
emergency and treated immediately.
Signs and symptoms of an overdose from nicotine lozenges would be expected to be
the same as those of acute nicotine poisoning, including pallor, cold sweat, salivation,
nausea, vomiting, abdominal pain, diarrhoea, headache, dizziness, disturbed hearing
and vision, tremor, mental confusion and weakness. Prostration, hypotension,
respiratory failure, rapid or weak or irregular pulse, circulatory collapse and
convulsions (including terminal convulsions) may ensue with large overdoses.
In the event of an overdose (e.g. too many lozenges ingested) the user should seek
medical attention immediately. All nicotine intake should cease immediately and the
patient be treated symptomatically. Artificial respiration with oxygen should be
instituted if necessary. Activated charcoal reduces the gastrointestinal absorption of
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. When
consumed in tobacco products, it has been shown to be addictive and
abstinence is linked to craving and withdrawal symptoms. These craving and
withdrawal symptoms include urge to smoke, depressed mood, insomnia,
irritability, frustration or anger, anxiety, difficulty in concentrating,
restlessness and increased appetite or weight gain. The lozenges replace some
of the nicotine provided by tobacco and help reduce the severity of these
nicotine craving and withdrawal symptoms.
Nicabate A Mint Lozenges completely dissolve in the oral cavity, and the
entire amount of nicotine contained in the lozenge becomes available for
buccal absorption or ingestion (swallowing). The complete dissolution of
Nicabate A Mint Lozenge is typically achieved in 20-30 minutes. The peak
plasma concentrations of nicotine achieved after a single dose are
4.4 ng/ml. When dosed every 1.5 hours, the steady state
peak and trough concentrations are 12.7 and 9.4 ng/ml respectively. Ingestion
of Nicabate A Mint Lozenges not following dosing instructions (chewed,
retained in the mouth, and swallowed; chewed and immediately swallowed)
does not result in faster or higher absorption, but a substantial amount of
nicotine (80-93%) is still absorbed.
As the plasma protein binding of nicotine is low (4.9% - 20%), the volume of
distribution of nicotine is large (2.5 l/kg). The distribution of nicotine to tissue
is pH dependent, with the highest concentrations of nicotine found in the
brain, stomach, kidney and liver.
Nicotine is extensively metabolized to a number of metabolites, all of which
are less active than the parent compound. The metabolism of nicotine
primarily occurs in the liver, but also in the lung and kidney. Nicotine is
metabolized primarily to cotinine but is also metabolized to nicotine N′-oxide.
Cotinine has a half-life of 15-20 hours and its blood levels are 10 times higher
than nicotine. Cotinine is further oxidized to trans-3′-hydroxycotinine, which
is the most abundant metabolite of nicotine in the urine. Both nicotine and
cotinine undergo glucuronidation.
The elimination half-life of nicotine is approximately 2 hours (range 1 - 4
hours). Total clearance for nicotine ranges from approximately 62 to 89 l/hr.
Non-renal clearance for nicotine is estimated to be about 75% of total
clearance. Nicotine and its metabolites are excreted almost exclusively in the
urine. The renal excretion of unchanged nicotine is highly dependent on
urinary pH, with greater excretion occurring at acidic pH.
Preclinical safety data
The general toxicity of nicotine is well known and taken into account in the
recommended posology. Nicotine was not mutagenic in appropriate assays.
The results of carcinogenicity assays did not provide any clear evidence of a
tumorigenic effect of nicotine. In studies in pregnant animals, nicotine
showed maternal toxicity, and consequential mild fetal toxicity. Additional
effects included pre- and postnatal growth retardation and delays and changes
in postnatal CNS development.
Effects were only noted following exposure to nicotine at levels in excess of
those which will result from recommended use of Nicabate A Mint Lozenges.
Effects on fertility have not been established.
Comparison of the systemic exposure necessary to elicit these adverse
responses from preclinical test systems with that associated with the
recommended use of Nicabate A Mint Lozenges indicate that the potential risk
is low and outweighed by the demonstrable benefit of nicotine therapy in
smoking cessation. However, Nicabate A Mint Lozenges should only be used
by pregnant women on medical advice if other forms of treatment have failed.
List of excipients
Sodium carbonate anhydrous
Mint flavour powder 57581 (contains lactose and soya protein)
Special precautions for storage
Do not store above 25°C. Store in the original package.
Nature and contents of container
Clear or opaque Polyvinyl Chloride/Polyethylene/Polyvinylidene Chloride/Al
blisters in packs of 12, 24, 36, 48, 72, 96, 108 and 144.
Not all pack sizes may be marketed.
Special precautions for disposal
MARKETING AUTHORISATION HOLDER
Beecham Group plc
980 Great West Road
T/A GlaxoSmithKline Consumer Healthcare
Brentford TW8 9GS, UK.
MARKETING AUTHORISATION NUMBER(S)
DATE OF FIRST AUTHORISATION/RENEWAL OF THE
DATE OF REVISION OF THE TEXT
Source: Medicines and Healthcare Products Regulatory Agency
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