Medication Guide App

BOOTS NICASSIST 2MG COMPRESSED LOZENGE

Active substance: NICOTINE BITARTRATE DIHYDRATE

View full screen / Print PDF » Download PDF ⇩

Transcript
SUMMARY OF PRODUCT CHARACTERISTICS

1

NAME OF THE MEDICINAL PRODUCT
Boots NicAssist 2mg compressed lozenges

2

QUALITATIVE AND QUANTITATIVE COMPOSITION
Each piece of lozenge contains:
Active substance: 2 mg nicotine (corresponding to 6.144 mg nicotine bitartrate
dihydrate).
Excipient(s): aspartame (0.01 g), maltitol (0.9 g) and sodium (9.8 mg).
For a full list of excipients, see section 6.1.

3

PHARMACEUTICAL FORM
Compressed lozenge
White, mint flavoured, round biconvex lozenge

4

CLINICAL PARTICULARS

4.1

Therapeutic indications
Relief of nicotine withdrawal symptoms, in nicotine dependency as an aid to smoking
cessation.
The 2 mg strength is used when severe withdrawal symptoms are experienced.
Patient counselling and support normally improve the success rate.

4.2

Posology and method of administration
Adults and elderly
Users should stop smoking completely during treatment with Boots NicAssist
lozenge.
Boots NicAssist 2 mg lozenge is intended to be used by smokers with a strong or very
strong nicotine dependency and those who have previously failed to stop smoking
with the aid of nicotine replacement therapy.
The optimal dosage form is selected according to the following table:

Low to moderate
dependency

Moderate to strong dependency

Strong to very strong
dependency

Low dosage forms acceptable

High dosage forms acceptable

Less than 20 cigarettes /
day

From 20 to 30 cigarettes / day

Over 30 cigarettes / day

Low dose forms are
preferable

Low (1 mg lozenge) or high (2 mg
lozenge) dose forms are acceptable
depending on patient characteristics
and preference.

High dose forms are
preferable

(1 mg lozenge)

(2 mg lozenge)

If an adverse event occurs with the use of the high dose form (2 mg lozenge), use of
the low dose form (1 mg lozenge) should be considered.
The initial dosage should be individualised on the basis of the patients nicotine
dependence. One piece of lozenge to suck when the user feels the urge to smoke.
Initially, 1 lozenge should be taken every 1-2 hours. The usual dosage is 8-12
lozenges per day. The maximum daily dose is 15 lozenges.
Directions for use:
1

One lozenge to be sucked until the taste becomes strong.

2

The lozenge should then be lodged between the gum and cheek.

3

When the taste fades, sucking of the lozenge should commence again.

4

The sucking routine will be adapted individually and should be repeated until
the lozenge dissolves completely (about 30 minutes).

The treatment duration is individual. Normally, treatment should continue for at least
3 months. After 3 months, the user should gradually reduce the number of lozenges or
alternatively the user should switch to nicotine 1 mg lozenges and then gradually
reduce the number of lozenges per day.
Treatment should be discontinued when the dose has been reduced to 1-2 lozenges
per day. Use of nicotine medicinal products like Boots NicAssist 2 mg lozenge
beyond 6 months is generally not recommended. Some ex-smokers may need
treatment with the lozenge longer to avoid returning to smoking. Patients who have
been using oral nicotine replacement therapy beyond 9 months are advised to seek
additional help and information from health care professionals.
Counselling may help smokers to quit.
Concomitant use of acidic beverages such as coffee or soda may decrease the buccal
absorption of nicotine. Acidic beverages should be avoided for 15 minutes prior to
sucking the lozenge.

Children and adolescents (< 18 years)
Boots NicAssist lozenge should not be used by people under 18 years of age without
recommendation from a physician. There is no experience in treating adolescents
under the age of 18 with Boots NicAssist lozenge.

4.3

Contraindications
Hypersensitivity to nicotine or to any of the excipients.
Boots NicAssist lozenge should not be used by non-smokers.

4.4

Special warnings and precautions for use
Dependent smokers with a recent myocardial infarction, unstable or worsening angina
including Prinzmetal’s angina, severe cardiac arrhythmias, uncontrolled
hypertensions or recent cerebrovascular accident should be encouraged to stop
smoking with non-pharmacological interventions (such as counselling). If this fails,
Boots NicAssist lozenges may be considered but as data on safety in this patient
group are limited, initiation should only be under close medical supervision.
Boots NicAssist lozenges should be used with caution in patients with hypertension,
stable angina pectoris, cerebrovascular disease, occlusive peripheral arterial disease,
heart failure, diabetes mellitus, hyperthyroidism or pheochromocytoma and severe
hepatic and/or renal impairment.
Patients should initially be encouraged to stop smoking with non-pharmacological
interventions (such as counselling).
Swallowed nicotine may exacerbate symptoms in subjects suffering from active
oesophagitis, oral and pharyngeal inflammation, gastritis or peptic ulcer.
Doses of nicotine that are tolerated by adult smokers during treatment may produce
severe symptoms of poisoning in small children and may prove fatal (please see
Section 4.9).
Special warnings about excipients
Boots NicAssist lozenges contain sweeteners, including aspartame and maltitol.
Each Boots NicAssist 2 mg lozenge contains aspartame (E951), a source of
phenylalanine equivalent to 5 mg/dose and may be harmful for people with
phenylketonuria.
Because Boots NicAssist 2 mg lozenge contains maltitol (E965), a source of fructose:
- patients with rare hereditary conditions of fructose intolerance should not take this
medicine,
- patients may experience a mild laxative effect.
Calorific value 2.3 kcal/g maltitol.
Boots NicAssist 2 mg lozenge contains 9.8 mg of sodium per piece

4.5

Interaction with other medicinal products and other forms of interaction
Drug Interactions: No information is available on interactions between Boots
NicAssist lozenge and other medicinal products.
Smoking Cessation: Smoking but not nicotine is associated with increased CYP1A2
activity. After stopping smoking there may be reduced clearance of substrates for this
enzyme and increased plasma levels of some medicinal products of potential clinical
importance because of their narrow therapeutic window e.g. theophylline, tacrine,
olanzapine and clozapine.
The plasma concentrations of other active substances metabolised by CYP1A2 e.g.
caffeine, paracetamol, phenazone, phenylbutazone, pentazocine, lidocaine,
benzodiazepines, warfarin, oestrogen and vitamin B12 may also increase. However
the clinical significance of this effect for these active substances is unknown.

Smoking may lead to reduced analgesic effects of propoxyphene, reduced diuretic
response to furosemide (frusemide), reduced effect of propranolol on blood pressure
and heart rate and reduced responder rates in ulcer healing with H2-antagonists.
Smoking and nicotine may raise the blood levels of cortisol and catecholamines, i.e.
may lead to a reduced effect of nifedipine or adrenergic antagonists and to an
increased effect of adrenergic agonists.
Increased subcutaneous absorption of insulin which occurs upon smoking cessation
may necessitate a reduction in insulin dose.

4.6

Pregnancy and lactation
Pregnancy
In pregnant women, complete cessation of tobacco smoking should always be
recommended without nicotine replacement therapy.
Nevertheless, in the case of failure in highly dependent pregnant smokers, tobacco
withdrawal via nicotine replacement therapy may be recommended. Indeed, foetal
risk is probably lower than that expected with tobacco smoking, due to:
- lower maximal plasma nicotine concentration than with inhaled nicotine
- no additional exposure to polycyclic hydrocarbons and carbon monoxide
- improved chances of quitting smoking by the third trimester.
Smoking continued during the third trimester may lead to intra-uterine growth
retardation or even premature birth or stillbirth, depending on the daily amount of
tobacco.
Tobacco withdrawal with or without nicotine replacement therapy should not be
undertaken alone but as part of a medically supervised smoking cessation program.
In the third trimester nicotine has haemodynamic effects (e.g. changes in foetal heart
rate) which could affect the foetus close to delivery. Therefore, after the sixth month
of pregnancy, the lozenge should only be used under medical supervision in pregnant
smokers who have failed to stop smoking by the third trimester.
Lactation
Nicotine is excreted in breast milk in quantities that may affect the child even in
therapeutic doses. The lozenge, like smoking itself, should therefore be avoided
during breast-feeding. Should smoking withdrawal not be achieved, use of the
lozenge by breast feeding smokers should only be initiated after advice from a
physician. Where nicotine replacement therapy is used whilst breast-feeding, the
lozenge should be taken just after breast-feeding and not during the two hours before
breast-feeding.

4.7

Effects on ability to drive and use machines
There is no evidence of any risks associated with driving or operating machinery
when the gum is used following the recommended dose. Nevertheless one should take
into consideration that smoking cessation can cause behavioural changes.

4.8

Undesirable effects
Boots NicAssist lozenge can cause adverse reactions similar to those associated with
nicotine administered by smoking. These can be attributed to the pharmacological
effects of nicotine, which are dose-dependent. Non dose-dependent adverse reactions
are as follows: hypersensitivity, angioneurotic oedema and anaphylactic reactions.
Most of the adverse reactions which are reported by patients occur generally during
the first 3-4 weeks after initiation of therapy.
Nicotine from lozenges may sometimes cause a slight irritation of the throat and
increased salivation at the start of the treatment. Excessive swallowing of nicotine
which is released in the saliva may, at first, cause hiccups. Those who are prone to
indigestion may suffer initially from minor degrees of dyspepsia or heartburn; slower
sucking will usually overcome this problem.
Excessive consumption of lozenges by subjects who have not been in the habit of
inhaling tobacco smoke, could possibly lead to nausea, faintness and headache.
Increased frequency of aphthous ulcer may occur after abstinence from smoking.
Adverse reactions are listed below, by system organ class and frequency.
Frequencies are defined as: very common (≥1/10), common (≥1/100 to <1/10),
uncommon (≥1/1,000 to <1/100), rare (≥1/10,000, <1/1,000) or very rare
(<1/10,000).
Nervous system disorders:
Common: dizziness, headache
Gastrointestinal disorders:
Common: nausea, flatulence, hiccups, gastritis, dry mouth, stomatitis and
oesophagitis.
Cardiac disorders:
Uncommon: palpitations
Rare: atrial arrhythmia
Immune system disorders:
Rare: hypersensitivity, angioneurotic oedema and anaphylactic reactions.
Certain symptoms which have been reported such as dizziness, headache and
insomnia may be ascribed to withdrawal symptoms in connection with smoking
cessation and may be due to insufficient administration of nicotine.
Cold sores may develop in connection with smoking cessation, but any relation with
the nicotine treatment is unclear.
The patient may still experience nicotine dependence after smoking cessation.

4.9

Overdose
In overdose, symptoms corresponding to heavy smoking may be seen.

The acute lethal oral dose of nicotine is about 0.5 – 0.75 mg per kg body weight,
corresponding in an adult to 40 – 60 mg. Even small quantities of nicotine are
dangerous in children, and may result in severe symptoms of poisoning which may
prove fatal. If poisoning is suspected in a child, a doctor must be consulted
immediately.
Overdose with Boots NicAssist 2 mg lozenge may only occur if many pieces are
sucked simultaneously. Nicotine toxicity after ingestion will most likely be
minimised as a result of early nausea and vomiting that occur following excessive
nicotine exposure.
General symptoms of nicotine poisoning include: weakness, perspiration, salivation,
throat burn, nausea, vomiting, diarrhoea, abdominal pain, hearing and visual
disturbances, headache, tachycardia and cardiac arrhythmia, dyspnoea, prostration,
circulatory collapse, coma and terminal convulsions.
Treatment of overdose:
Treatment of overdose should be immediate as symptoms may develop rapidly.
Emesis is usually spontaneous. Administration of oral activated charcoal and gastric
lavage should be considered as soon as possible and within 1 hour of ingestion.
Monitor vital signs and treat symptomatically.

5

PHARMACOLOGICAL PROPERTIES

5.1

Pharmacodynamic properties
ATC Code: N07B A01
Pharmacotherapeutic group: Drugs used in nicotine dependence
Nicotine, the primary alkaloid in tobacco products and a naturally occurring
autonomous substance, is a nicotine receptor agonist in the peripheral and central
nervous systems and has pronounced CNS and cardiovascular effects. On
consumption of tobacco products, nicotine has proven to be addictive, resulting in
craving and other withdrawal symptoms when administration is stopped. This craving
and these withdrawal symptoms include a strong urge to smoke, dysphoria, insomnia,
irritability, frustration or anger, anxiety, concentration difficulties, agitation and
increased appetite or weight gain. The lozenge replaces part of the nicotine that would
have been administrated via tobacco and reduces the intensity of the withdrawal
symptoms and smoking urge.

5.2

Pharmacokinetic properties
The absorbed amount of nicotine depends on the amount released into the mouth and
absorbed through the buccal mucosa.
The main part of nicotine in Boots NicAssist 2 mg lozenge is absorbed through the
buccal mucosa. A proportion, by the swallowing of nicotine containing saliva,
reaches the stomach and intestine where it is inactivated. Due to the first-pass effect
in the liver, the systemic bioavailability of nicotine is low. Consequently, in the
treatment with Boots NicAssist 2 mg lozenge the high and quick systemic nicotine
concentration, as seen when smoking, is rarely obtained.

Distribution volume after intravenous administration of nicotine is approximately 2-3
1/kg and the half-life is 2 hours. Nicotine is metabolised principally in the liver and
the plasma clearance is approximately 1.2 l/min; nicotine also metabolises in the
kidney and lungs. Nicotine crosses the blood-brain barrier.
More than 20 metabolites have been identified, all believed to be less active than
nicotine. The main metabolite is cotinine which has a half-life of 15-20 hours and
with approximately 10 times higher plasma concentration than nicotine. Nicotine’s
plasma-protein binding is less than 5%. Changes in nicotine binding from the use of
concomitant medicinal products or due to altered disease state are not expected to
have significant effect on nicotine kinetics. The main metabolite in urine is cotinine
(15% of the dose) and trans-3-hydroxy cotinine (45% of the dose).
About 10% of the nicotine is excreted unchanged. Up to 30% may be excreted with
urine in increased diuresis and the acidity under pH 5.
The peak value for the plasma concentration of Boots NicAssist 2 mg lozenge after a
single dose is approximately 7.0 ng per ml and the maximal concentration at steady
state (one 2 mg lozenge/hour for 12 hours) is approximately 22.5 ng per ml (average
plasma concentration of nicotine after smoking one cigarette is 15-30 ng per ml).
Peak plasma concentration is reached after about 48 minutes following sucking of a
single lozenge and after about 30 minutes at steady state.
Studies have demonstrated that there is a linear dose-concentration proportionality
between the 1 mg and 2 mg Boots NicAssist lozenges for both Cmax and AUC. The
Tmax are similar for both strengths.

5.3

Preclinical safety data
Nicotine was positive in some in vitro genotoxicity tests but there are also negative
results with the same test systems. Nicotine was negative in standard in-vivo tests.
Animal experiments have shown that nicotine induces post-implantation loss and
reduces the growth of foetuses.
The results of carcinogenicity assays did not provide any clear evidence of a
tumorigenic effect of nicotine.

6

PHARMACEUTICAL PARTICULARS

6.1

List of excipients
Maltitol (E965)
Sodium carbonate anhydrous
Sodium hydrogen carbonate
Polyacrylate dispersion 30 per cent
Xanthan gum
Colloidal anhydrous silica
Levomenthol
Peppermint oil
Aspartame (E951)
Magnesium stearate

6.2

Incompatibilities
Not applicable.

6.3

Shelf life
3 years

6.4

Special precautions for storage
Do not store above 25°C.

6.5

Nature and contents of container
12, 36, 72, 96, 144 or 204 lozenges in opaque blisters consisting of aluminium foil
and PVC/PE/PVDC/PE/PVC-film. Not all pack sizes may be marketed.

6.6

Special precautions for disposal
No special requirements.

7

MARKETING AUTHORISATION HOLDER

Novartis Consumer Health UK Limited
Park View, Riverside Way
Watchmoor Park, Camberley
Surrey
GU15 3YL
UK
Trading as: Novartis Consumer Health.

8

MARKETING AUTHORISATION NUMBER(S)
PL 00030/0203

9

DATE OF FIRST AUTHORISATION/RENEWAL OF THE
AUTHORISATION
09/04/2009 / 25/03/2009

10

DATE OF REVISION OF THE TEXT
06/01/2015

Expand view ⇕

Source: Medicines and Healthcare Products Regulatory Agency

Disclaimer: Every effort has been made to ensure that the information provided here is accurate, up-to-date and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. This information has been compiled for use by healthcare practitioners and consumers in the United States. The absence of a warning for a given drug or combination thereof in no way should be construed to indicate that the drug or combination is safe, effective or appropriate for any given patient. If you have questions about the substances you are taking, check with your doctor, nurse or pharmacist.

Hide
(web3)