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Active substance(s): NICOTINE RESINATE

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NiQuitin Mint 4mg Lozenges


Each compressed lozenge contains 4mg Nicotine (as 26.66mg Nicotine Resinate)
Excipients with known effect
Aspartame [E951] 6.10 mg
Mannitol [E421]
Each lozenge contains 15 mg of Sodium
For the full list of excipients, see section 6.1.


Compressed Lozenge
Cream/white, biconvex round lozenge, embossed ‘L873’




Therapeutic indications
Nicotine Perrigo 4mg Lozenges are indicated for the treatment of tobacco dependence by
nicotine withdrawal symptoms including cravings, associated with smoking cessation.
cessation of tobacco use is the eventual objective.
Nicotine Perrigo 4mg Lozenges should preferably be used in conjunction with a behavioural
support programme.


Posology and method of administration
Adults (18 years and over):
Users should make every effort to stop smoking completely during treatment with
NiQuitin Mint 4mg Lozenges

Recommended treatment schedule:
Step 1
Step 2
Weeks 1 to 6
Weeks 7 to 9
Initial treatment period Step down treatment
1 lozenge every 1 to 2
1 lozenge every 2 to 4

Step 3
Weeks 10 to 12
Step down treatment
1 lozenge every 4 to
8 hours

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.
Lozenges should not be used for more than 6 months. If users still feel the need for
treatment, a healthcare professional should be consulted.
Behavioural therapy, advice and support will normally improve the success rate.
Paediatric population
NiQuitin Mint 4mg Lozenges should only be used in adolescents (12-17 years) with the

advice of a healthcare professional.
NiQuitin Mint 4mg Lozenges are contraindicated in children under the age of 12 years

in the indication of treatment of nicotine dependence (see section 4.3).
Method of Administration
NiQuitin Mint 4mg Lozenges are suitable for smokers who have their first cigarette of
the day less 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. Liquids which lower the
pH in the mouth such as coffee, juices and soft drinks, can decrease the absorption of
nicotine in the mouth. To obtain maximum absorption of nicotine these liquids should
be avoided for up to 15 minutes before the lozenge is used.


NiQuitin Mint 4mg Lozenges are contraindicated in:

• hypersensitivity to the active substance (nicotine) or to any of the excipients listed in
section 6.1
• children under the age of 12 years and
• non smokers
• those with phenylketonuria
• those with unstable or worsening angina pectoris, Prinzmetals angina or severe
• those who have recently suffered myocardial infarction or cerebrovascular accident.


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 smoking.
The following patients should be treated only after advice from a doctor: those with
cardiovascular disease (also not hospitalized), with uncontrolled hypertension, with
insulin dependent diabetes.
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 adverse events
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 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.
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: NiQuitin Mint 4mg Lozenges are sugar free, but do contain
aspartame which metabolises to phenylalanine, which is of relevance for those with
Sodium content: Each Lozenge contains 15 mg of sodium. People on a low sodium
diet should take this into account.
Mannitol: May have a mild laxative effect.


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.
Paediatric population
Interaction studies have only been performed in adults.


Fertility, 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 by a healthcare professional to assist a quit attempt. The
risk of using NRT to the foetus is lower than that expected with tobacco smoking, due
to lower maximal plasma nicotine concentration and no additional exposure to
polycyclic hydrocarbons and carbon monoxide.
However, as nicotine passes to the foetus affecting breathing movements and has a
dose dependent effect on placental/foetalcirculation, 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.
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. Ideally smoking


cessation during pregnancy should be achieved without NRT. However for women
unable to quit on their own, NRT may be recommended by a healthcare professional
to assist a quit attempt. 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 made as long as possible. Women should
try to breastfeed just before they take the product.
Effects on ability to drive and use machines
NiQuitin Mint 4mg Lozenges has no or negligible influence on the ability to drive and

use machines.


Undesirable effects
NRT can cause adverse reactions similar to those associated with nicotine
administered in other way, including smoking. These may be attributed to the
pharmacological effects of nicotine, which are dose dependent. At recommended
doses NiQuitin Mint 4mg Lozenges
have not been found to cause any serious adverse effects. Excessive consumption of
Nicotine Perrigo 4mg 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 cold.
Description of selected adverse reactions
Immune system disorders
Very rare (<1/10,000)>: anaphylactic reactions Platelet bleeding and clotting disorders
Uncommon (≥1/1,000 to <1/100)>: gingival bleeding; nosebleed

Psychiatric disorders
Common (≥1/100 to <1/10)>: insomnia; anxiety; irritability; increased appetite
Uncommon (≥1/1,000 to <1/100)>: anger; aggravated anxiety;
dreaming;abnormal hunger; mood swings; wakefulness


Nervous system disorders
Common (≥1/100 to <1/10)>: headache
Uncommon (≥1/1,000 to <1/100)>: lightheaded feeling; localised numbness, parageusia,
metallic taste; taste perversion

Cardiac disorders
Uncommon (≥1/1,000 to <1/100)>: aggravated palpitations; palpitations; tachycardia

Vascular disorders
Uncommon (≥1/1,000 to <1/100)>: vascular disorder; flushing; skin flushed

Respiratory, thoracic and mediastinal disorders
Common (≥1/100 to <1/10)>: pharyngitis
Uncommon (≥1/1,000 to <1/100)>: laryngismus; aggravated asthma; lower respiratory tract
infection; coughing; nasal irritation; throat irritation; nasal congestion

Gastrointestinal disorders
Very common (≥1/10)>: nausea
Common (≥1/100 to <1/10)>: vomiting; dyspepsia, heartburn, indigestion; hiccup; mouth
irritation, mouth ulceration; tongue ulceration; diarrhoea; belching; flatulence
Uncommon (≥1/1,000 to <1/100)>: peptic ulcer; dysphagia; aggravated dyspepsia;
gastroesophageal reflux; hiatus hernia; oesophagitis; eructation; buccal mucosa ulceration;
borborygmus; dry lips; dry throat; tongue disorder; tooth ache

Skin and subcutaneous tissue disorders
Uncommon (≥1/1,000 to <1/100)>: erythema; itching; rash; skin reaction localised; increased

Musculoskeletal and connective tissue disorders
Uncommon (≥1/1,000 to <1/100)>: jaw pain

Renal and urinary disorders
Uncommon (≥1/1,000 to <1/100)>: nocturia

General disorders and administration site conditions
Uncommon (≥1/1,000 to <1/100)>: overdose effect; pain; leg pain; oedema legs

Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is
important. It allows continued monitoring of the risk/benefit balance of the medicinal
product. Healthcare professionals are asked to report any suspected adverse reactions
via the Yellow Card Scheme at:

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.




Pharmacodynamic properties
Pharmacotherapeutic group: Drug in nicotine dependence, ATC Code: NO 7B 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.
Pharmacokinetic properties
NiQuitin Mint 4mg 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 NiQuitin Mint 4mg Lozenges
is typically achieved in 20-30 minutes. The peak plasma concentrations of nicotine
achieved after a single dose are approximately 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 Nicotine Perrigo 4mg 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 foetal 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 Nicotine Perrigo 4mg 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 Nicotine Perrigo
4mg Lozenges indicate that the potential risk is low and outweighed by the demonstrable
benefit of nicotine therapy in smoking cessation. However, Nicotine Perrigo 4mg Lozenges
should only be used by pregnant women on medical advice if other forms of treatment have
Environmental Risk Assessment (ERA)
It is not the intention of the applicant to increase the overall usage of this drug substance as a
result of this application, since the product is not being brought to market to address a new




List of excipients
Magnesium stearate
Sodium alginate
Xanthan gum
Potassium bicarbonate
Sodium carbonate anhydrous
Peppermint flavour


Not applicable.


Shelf life
24 months in ACLAR/PVC/AL blisters
21 months in COC/PVdC/AL blisters


Special precautions for storage
Do not store above 25°C. Store in the original packaging in order to protect from light.


Nature and contents of container
Clear, Colourless Laminate comprising: 76 micron UltRx3000 ACLAR / Adhesive / 254
micron PVC blister pack comprising of 20 micron Aluminium Foil with heat seal lacquer.
Clear, Colourless Laminate comprising: 60 micron PVC/240 micron COC (Cyclic Olefin
Copolymer) / 90gsm PVdC blister pack comprising of 20 micron Aluminium Foil with heat
seal lacquer.
Each pack contains 36 or 72 lozenges in a cardboard carton.


Special precautions for disposal
No special requirements.


Wrafton Laboratories Limited
Trading as Perrigo

EX33 2DL
United Kingdom


PL 12063/0114







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Further information

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