NIQUITIN 7MG TRANSDERMAL PATCHES

Active substance: NICOTINE

View full screen / Print PDF » Download PDF ⇩

Transcript
SUMMARY OF PRODUCT CHARACTERISTICS

1

NAME OF THE MEDICINAL PRODUCT
NiQuitin 7 mg transdermal patches

2

QUALITATIVE AND QUANTITATIVE COMPOSITION
Each 7 cm2 transdermal patch contains 36 mg nicotine, equivalent to 5.1
mg/cm2 of nicotine and delivering 7 mg over 24 hours.
For excipients, see section 6.1.

3

PHARMACEUTICAL FORM
Transdermal patch.
Each patch is rectangular and is comprised of an outer matt pinkish tancoloured layer, a middle silver layer and an outer clear layer which is removed
prior to use.

4

CLINICAL PARTICULARS

4.1

Therapeutic indications
NiQuitin patches relieve and/or prevent craving and nicotine withdrawal
symptoms associated with tobacco dependence. They are 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.
NiQuitin patches are indicated in pregnant and lactating women making a quit
attempt.
If possible, when stopping smoking, NiQuitin patches should be used in
conjunction with a behavioural support programme.

4.2

Posology and method of administration
NiQuitin patches should be applied once a day, at the same time each day and
preferably soon after waking, to a non-hairy, clean, dry skin site and worn

continuously for 24 hours. The NiQuitin patch should be applied promptly on
removal from its protective sachet.
Avoid applying to any skin which is broken, red or irritated. After 24 hours
the used patch should be removed and a new patch applied to a fresh skin site.
The patch should not be left on for longer than 24 hours. Skin sites should not
be reused for at least seven days. Only one patch should be worn at a time.
Patches may be removed before going to bed if desired. However use for
24 hours is recommended to optimise the effect against morning cravings.
Concurrent behavioural support is recommended, as such programmes have
been shown to be beneficial for smoking cessation.
Adults 18 years and over
Abrupt cessation of smoking:
During a quit attempt every effort should be made to stop smoking with
NiQuitin patches.
NiQuitin therapy should usually begin with NiQuitin 21 mg and be reduced
according to the following dosing schedule:Dose

Duration

Step 1 NiQuitin 21 mg

First 6 weeks

Step 2 NiQuitin 14 mg

Next 2 weeks

Step 3 NiQuitin 7 mg

Last 2 weeks

Light smokers (e.g. those who smoke less than 10 cigarettes per day) are
recommended to start at Step 2 (14 mg) for 6 weeks and decrease the dose to
NiQuitin 7 mg for the final 2 weeks.
Patients on NiQuitin 21 mg who experience excessive side-effects (please
refer to precautions), which do not resolve within a few days, should change to
NiQuitin 14mg. This strength should then be continued for the remainder of
the 6 week course before stepping down to NiQuitin 7mg for two weeks. If
the symptoms persist the patient should be advised to seek the advice of a
healthcare professional.
For optimum results, the 10 week treatment course (8 weeks for light smokers
or patients who have reduced strength as above), should be completed in full.
Treatment with NiQuitin patch may be continued beyond 10 weeks if needed
to stay cigarette free, however, those who have quit smoking but are having
difficulty discontinuing using the patches recommended to seek additional
help and advice from a healthcare professional.
Further courses may be used at a later time, for NiQuitin patch users who
continue or resume smoking.

Gradual Cessation:
For smokers who are unwilling or unable to quit abruptly.
The 21 mg patch can be used daily for 2-4 weeks while the user continues to
smoke as needed. At the end of the 2-4 weeks the user should quit completely
and continue using Step 1 21 mg patch for 6 weeks daily without smoking.
Thereafter following the Step 2 and 3 directions for abrupt cessation above.
Should the patient feel able to quit completely before their designated quit date
they can do so.
Reduction in smoking:
For smokers who wish to cut down with no immediate plans to quit.
A patch can be used while the user continues to smoke as needed. The user
should reduce the number of cigarettes smoked as far as possible and to refrain
from smoking as long as possible. Users should be encouraged to stop
smoking completely as soon as possible.
If users are still feeling the need to use the patches 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 professional.
Temporary Abstinence
Apply a patch to control troublesome withdrawal symptoms including craving
during the period when smoking is being avoided. Users should be encouraged
to stop smoking completely as soon as possible.
If users are still feeling the need to use the patches 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 professional.
Adolescents and children
Adolescents (12 to 17 years) should follow the schedule of treatment for
abrupt cessation of smoking as given above. Where adolescents are not ready
or not able to stop smoking abruptly, advice from a healthcare professional
should be sought.
Safety and effectiveness in children who smoke has not been evaluated.
NiQuitin is not recommended for use in children under 12 years of age.

4.3

Contraindications
NiQuitin is contraindicated in patients with hypersensitivity to the system, the
active substance, or any of the excipients.
NiQuitin patches should not be used by non-smokers, occasional smokers or
children under 12 years.

4.4

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.
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, NiQuitin patches 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.
Atopic or eczematous dermatitis (due to localised patch sensitivity): In the
case of severe or persistent local reactions at the site of application (e.g. severe
erythema, pruritus or oedema) or a generalised skin reaction (e.g. urticaria,
hives or generalised skin rashes), users should be instructed to discontinue use
of NiQuitin and contact their physician.
Contact sensitisation: Patients with contact sensitisation should be cautioned
that a serious reaction could occur from exposure to other nicotine-containing
products or smoking.
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 effects.
Phaeochromocytoma and uncontrolled hyperthyroidism: Use with caution in
patients with uncontrolled hyperthyroidism or phaeochromocytoma as nicotine
causes release of catecholamines.
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. The patches should be folded in half with the
adhesive side innermost and disposed of with care.
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.
Safety on handling: NiQuitin is potentially a dermal irritant and can cause
contact sensitisation. Care should be taken during handling and in particular
contact with the eyes and nose avoided. After handling, wash hands with
water alone as soap may increase nicotine absorption.

4.5.

Interaction with other medicinal products and other forms of interaction
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.
Healthcare professionals are reminded that smoking cessation itself may
require the adjustment of some drug therapy.

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. 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 NRT 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
NRT may cause adverse reactions similar to those associated with nicotine
administered by other means, including smoking. These may be attributable to
the pharmacological effects of nicotine, some of which are dose dependent. At

recommended doses, NiQuitin patches have not been found to cause any
serious adverse effects. Excessive use of NiQuitin patches by those who have
not been in the habit of inhaling tobacco smoke could possibly lead to nausea,
faintness or headaches.
Subjects quitting smoking by any means could expect to suffer from asthenia,
headache, dizziness, sleep disturbance, coughing or influenza-like illness.
Certain symptoms which have been reported such as depression, irritability,
nervousness, restlessness, mood lability, anxiety, drowsiness, impaired
concentration and insomnia may be related to withdrawal symptoms
associated with smoking cessation.
Application site reactions are the most frequent adverse reaction associated
with NiQuitin. NiQuitin can cause other adverse reactions related to the
pharmacological effect of nicotine or withdrawal effects related to smoking.
The following undesirable effects have been reported in clinical trials or
spontaneously post-marketing.
Certain symptoms which have been reported such as depression, irritability,
nervousness, restlessness, mood lability, anxiety, drowsiness, impaired
concentration, insomnia and sleep disturbances may be related to withdrawal
symptoms associated with smoking cessation. Subjects quitting smoking by
any means could expect to suffer from asthenia, headache, dizziness, coughing
or influenza-like illness.
Immune System Disorders
Uncommon>1/1000; <1/100: hypersensitivity NOS*
Very rare <1/10000: anaphylactic reactions
Psychiatric
Very common >1/10: sleep disorders including abnormal dreams and
insomnia
Common >1/100; <1/10: nervousness
Nervous system disorders
Very Common >1/10: headache, dizziness
Common >1/100; <1/10: tremor
Cardiac disorders
Common >1/100; <1/10: palpitations
Uncommon >1/1000; <1/100: tachycardia NOS
Respiratory, Thoracic and Mediastinal Disorders
Common >1/100; <1/10: dyspnoea, pharyngitis, cough
Gastrointestinal Disorders
Very Common >1/10: nausea, vomiting

Common >1/100; <1/10: dyspepsia, abdominal pain upper, diarrhea NOS,
dry mouth, constipation
Skin and Subcutaneous Tissue Disorders
Common >1/100; <1/10: sweating increased
Very rare > 1/100000; <1/10000: dermatitis allergic*, dermatitis contact*,
photosensitivity
Musculoskeletal and Connective Tissue Disorders
Common >1/100; <1/10: arthralgia, myalgia
General Disorders and Administration Site Conditions
Very Common >1/10: application site reactions NOS*
Common >1/100; <1/10: chest pain, pain in limb, pain NOS, asthenia, fatigue
Uncommon >1/1000; <1/100 malaise, influenza-like illness
*see below
Application site reactions, including transient rash, itching, burning, tingling,
numbness, swelling, pain and urticaria are the most frequent undesirable
effects of NiQuitin patch. The majority of these topical reactions are minor
and resolve quickly following removal of the patch. Pain or sensation of
heaviness in the limb or area around which the patch is applied (e.g. chest)
may be reported.
Hypersensitivity reactions, including contact dermatitis and allergic dermatitis
have also been reported. In the case of severe or persistent local reactions at
the application site (e.g. severe erythema, pruritus or oedema) or a generalized
skin reaction (e.g. urticaria, hives or generalised skin rashes) users should be
instructed to discontinue use of NiQuitin and contact their physician.
If there is a clinically significant increase in cardiovascular or other effects
attributable to nicotine, the NiQuitin dose should be reduced or discontinued.
4.9

Overdose

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.

Symptoms

Signs and symptoms of an overdose from a nicotine patch 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.

Management

Overdose from Topical Exposure

The nicotine patch(es) should be removed immediately in the event of an
overdose or if the patient shows signs of overdosage. The user should seek
medical attention immediately. The skin surface may be flushed with water
and dried. No soap should be used since it may increase nicotine absorption.
Nicotine will continue to be delivered into the bloodstream for several hours
after removal of the system because of a depot of nicotine in the skin.

Overdose from Ingestion

All nicotine intake should stop immediately. The patient should seek medical
attention immediately and be treated symptomatically.

Artificial respiration with oxygen should be instituted if necessary. Activated
charcoal reduces the gastrointestinal absorption of nicotine.

5

PHARMACOLOGICAL PROPERTIES

5.1

Pharmacodynamic properties
Pharmacotherapeutic classification: N07B A01
(Anti-smoking agents: N07BA, Nicotine 01)

Nicotine, the chief alkaloid in tobacco products and a naturally occurring
autonomic drug, is an agonist at nicotine receptors in the peripheral and central
nervous system and has pronounced CNS and cardiovascular effects.
Withdrawal from nicotine in addicted individuals is characterised by craving,
nervousness, restlessness, irritability, mood lability, anxiety, drowsiness, sleep
disturbances, impaired concentration, increased appetite, minor somatic
complaints (headache, myalgia, constipation, fatigue) and weight gain.
Withdrawal symptoms, such as cigarette craving, may be controlled in some
individuals by steady-state plasma levels lower than those for smoking.
In clinically controlled trials, NiQuitin was shown to alleviate nicotine
withdrawal symptoms as well as craving. NiQuitin reduced the severity of
cravings by at least 35% at all times of day during the first two weeks of
abstinence, compared to placebo (p<0.05).

5.2

Pharmacokinetic properties
Absorption
Following transdermal application, the skin rapidly absorbs nicotine released
initially from the patch adhesive. The plasma concentrations of nicotine reach
a plateau within 2-4 hours after initial application of NiQuitin with relatively
constant plasma concentrations persisting for 24 hours or until the patch is
removed. Approximately 68% of the nicotine released from the patch enters
systemic circulation and the remainder of the released nicotine is lost via
vaporisation from the edge of the patch.
With continuous daily application of NiQuitin (worn for 24 hours), dosedependent steady state plasma nicotine concentrations are achieved following
the second NiQuitin application and are maintained throughout the day. These
steady state maximum concentrations are approximately 30% higher than
those following a single application of NiQuitin.
Plasma concentrations of nicotine are proportional to dose for the three dosage
forms of NiQuitin. The mean plasma steady state concentrations of nicotine
are approximately 17 ng/ml for the 21 mg/day patch, 12 ng/ml for the 14 mg
/day patch and 6 ng/ml for the 7 mg/day patch. For comparison, half-hourly
smoking of cigarettes produces average plasma concentrations of
approximately 44 ng/ml.
The pronounced early peak in nicotine blood levels seen with inhalation of
cigarette smoke is not observed with NiQuitin.
Distribution

Following removal of NiQuitin, plasma nicotine concentrations decline with
an apparent mean half-life of 3 hours, compared with 2 hours for IV
administration due to continued absorption of nicotine from the skin depot. If
NiQuitin is removed most non-smoking patients will have non-detectable
nicotine concentrations in 10 to 12 hours.
A dose of radiolabelled nicotine given intravenously showed a distribution of
radioactivity corresponding to the blood supply with no organ selectively
taking up nicotine. The volume of distribution of nicotine is approximately
2.5 l/kg.
Metabolism
The major elimination organ is the liver and average plasma clearance is about
1.2 l/min; the kidney and the lung also metabolise nicotine. More than 20
metabolites of nicotine have been identified, all of which are believed to be
pharmacologically inactive. The principal metabolites are cotinine and trans3-hydroxycotinine. Steady state plasma cotinine concentrations exceed
nicotine by 10-fold. The half-life of nicotine ranges from 1 to 2 hours and
cotinine’s between 15 and 20 hours.
Excretion
Both nicotine and its metabolites are excreted through the kidneys and about
10% of nicotine is excreted unchanged in the urine. As much as 30% may be
excreted in the urine with maximum flow rates and extreme urine acidification
(pH≤5).
There were no differences in nicotine kinetics between men and women using
NiQuitin. Obese men using NiQuitin had significantly lower AUC and Cmax
values compared with normal weight men. Linear regression of AUC vs total
body weight showed the expected inverse relationship (AUC decreases as
weight increases). Nicotine kinetics were similar for all sites of application on
the upper body and upper outer arm.

5.3

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 NiQuitin. 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 NiQuitin indicate that the potential risk is low and
outweighed by the demonstrable benefit of nicotine therapy in smoking
cessation. However, NiQuitin should only be used by pregnant women on
medical advice if other forms of treatment have failed.

6.

PHARMACEUTICAL PROPERTIES

6.1.

List of excipients
Drug Reservoir:
Occlusive Backing:
Rate Controlling Membrane:
Contact Adhesive and
Protective Layer:
Printing Ink:

6.2

Incompatibilities
Not applicable.

6.3

Shelf life
3 years

6.4

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

Ethylene Vinyl Acetate Copolymer
Polyethylene/Aluminium/Polyethylene
Terephthalate/ Ethylene vinyl acetate
Polyethylene Film
Polyisobutylene Adhesive Laminate
PMS 465 Brown Ink

6.5

Nature and contents of container
7 or 14 patches in a carton. Each patch is contained in a laminate sachet.

6.6

Special precautions for disposal
No special requirements.

7

MARKETING AUTHORISATION HOLDER
Beecham Group PLC
980 Great West Road
Brentford
Middlesex
TW8 9GS
United Kingdom
T/A GlaxoSmithKline Consumer Healthcare
Brentford
TW8 9GS

8

MARKETING AUTHORISATION NUMBER(S)
PL 00079/0366

9

DATE OF FIRST AUTHORISATION/RENEWAL OF THE
AUTHORISATION
22/04/2009

10

DATE OF REVISION OF THE TEXT
28/03/2013

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
(web2)