QuitX Patches
Nicotine
PRODUCT INFORMATION
NAME OF THE MEDICINE
Active ingredient: Nicotine
Chemical name:
S-3-(1-methyl-2-pyrrolidinyl) pyridine
Structural formula:
Molecular formula:
C14H16N2
Molecular weight:
162.26
CAS Registry no.:
54-11-5
DESCRIPTION
QuitX Patches are round, punched out matrix patches with yellow-ochre backing foil. They consist of
a release liner which protects the patch during storage; an adhesive layer, which is necessary for
contact between the transdermal patch and the skin during application; several matrix layers; a pad
with the active ingredient solution and a backing foil for protection of the patch during wearing. Each
patch is packaged in a heat sealed multilaminate sachet.
Nicotine penetrates the skin by diffusion and thus becomes directly bioavailable to the systemic
circulation. The following 3 systems are available as shown in the table below:
Average dose (mg) of nicotine delivered in vivo
during 24 hours
Content of nicotine (mg)
Drug releasing area (cm²).
Printed code (on backing film)
QuitX
Patch Step 3
QuitX
Patch Step 2
QuitX
Patch Step 1
7
14
21
17.5
35.0
52.5
10
20
30
CWC
FEF
EME
To sustain the concentration gradients for diffusion, more nicotine is contained in the QuitX Patch
than is actually delivered over 24 hours. The QuitX Patch releases approximately 0.7 mg/cm2/24 hours
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of nicotine.
Therefore, the average daily dose administered is determined largely by the size of the contact area of
the system.
PHARMACOLOGY
Pharmacodynamics
Nicotine acts primarily on cholinergic receptors of the nicotine type in the peripheral and in the central
nervous system. For many effects, low doses of nicotine have a stimulant action. Conversely, high
doses have a depressant effect. Intermittent administration of nicotine affects neurohormonal
pathways, and results in the release of acetylcholine, noradrenaline, dopamine, serotonin, vasopressin,
beta-endorphin, growth hormone, cortisol, and ACTH.
These neuroregulators may be involved in the reported behavioural and subjective effects of smoking.
Improved performance with some parameters such as finger tapping has been shown following
nicotine administration in smokers who have been abstinent overnight. The actions of nicotine in man
are complex, depending on dose, rate of delivery, prevalent autonomic tone, individual variation, and
prior exposure (tolerance).
The cardiovascular effects of nicotine are due to stimulation of the central and the peripheral
sympathetic nervous system. For example nicotine at the concentrations achieved during smoking
causes increases in heart rate, systolic and diastolic pressure, and also cutaneous vasoconstriction.
Partial or complete tolerance to some effects of nicotine develops rapidly: a second infusion after 60 or
120 minutes results in lesser heart rate acceleration and subjective effects than the initial infusion in
spite of higher venous nicotine concentrations. When the second infusion is given after 210 minutes,
the response is the same as that after the initial infusion.
Application of QuitX Patch 14 mg/day (Step 2) to smokers abstinent overnight resulted in small
increases in mean heart rate (up to 6 beats per minute) and systolic blood pressure and a decrease in
stroke volume. The changes in heart rate and stroke volume were still present at day 10 after repeated
application suggesting that development of complete tolerance to the effects of nicotine did not occur.
The effects were smaller in magnitude than those produced by cigarette smoking, whereas no changes
in skin temperature or blood flow were observed compared with placebo control.
During tobacco withdrawal, symptoms such as nicotine craving, irritability, frustration, anger,
restlessness, nervousness, anxiety, mood lability, drowsiness, increased appetite, minor somatic
complaints (headache, myalgia, constipation, and fatigue), weight gain, difficulties with concentration,
and sleep disturbances have been observed. During placebo-controlled double-blind clinical studies,
nicotine replacement with QuitX Patches in the first few weeks or months after stopping smoking
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increased the chances of successful abstinence with or without group support. There was also a strong
trend towards reduction of withdrawal symptoms.
Pharmacokinetics
Nicotine is readily absorbed through the skin into the systemic circulation. The absorption profile after
single application of a QuitX Patch to healthy abstinent smokers (subjects undergoing a course of
smoking cessation therapy with the patch) shows an initial 1-2 hours delay followed by a progressive
rise in plasma concentrations, plateaus being attained at about 8-10 hours after application. After the
system is removed, plasma concentrations decline more slowly than would be predicted by the 2-hour
elimination half-life for this agent after an intravenous infusion.
About 10% of the total amount of nicotine that reaches the circulation is delivered from the skin after
QuitX Patch 21mg/day (Step 1) is removed. The area under the plasma concentration time curve
(AUC0-24h) varied in proportion to the dose delivered by the QuitX Patch, which in turn depends on the
size of the patch. In comparison with an IV infusion, 76.8% ± 17.8% of the nicotine released from the
QuitX Patch is systemically available. With repeated applications of QuitX Patches 21 mg/day (Step
1) and 14 mg/day (Step 2), mean minimum and maximum plasma concentrations at steady state were
7.1 nanogram/mL and 12.0 nanogram/mL for the 14 mg/day patch (Step 2) and 10.3 nanogram/mL
and 17.7 nanogram/mL for the 21mg/day patch (Step 1). These plasma concentrations were within the
range observed during moderate cigarette smoking.
Analysis of residual nicotine content in systems worn for 24 hours indicates that total nicotine delivery
into the circulation varies by a factor of two between individuals. However, within-individual
variability in the amount of nicotine delivered is small, indicating a high level of consistency in the
performance of the system during once-daily application of the QuitX Patch.
No data are available on the influence of gender on the pharmacokinetic parameters of nicotine
following administration. AUC values do not seem to be related to body weight within the range 50 to
110kg. No pharmacokinetic data exist for subjects outside this weight range.
Nicotine is distributed widely in the body with a volume of distribution of approximately 180 L. It
crosses the blood-brain barrier, the placenta, and is also found in breast milk. Plasma protein binding
of nicotine is negligible, with less than 5%. Therefore, changes in nicotine binding from use of
concomitant drugs or alternations of plasma proteins by disease states would not be expected to have
significant consequences.
Total plasma clearance of nicotine ranges from 0.92 to 2.43 L/min. It is eliminated mainly via hepatic
metabolism, and the primary metabolites are cotinine and nicotine-1'-N-oxide. Cotinine is to a large
extent further metabolised. However, some of the metabolites of nicotine are unidentified to date.
Only small amounts of nicotine are eliminated in unchanged form via the kidneys. There is
considerable individual variability in distribution, metabolism, and bioavailability of nicotine from
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cigarettes, capsules, and nicotine gum. Renal excretion of unchanged nicotine is pH-dependent, being
negligible under alkaline conditions.
INDICATIONS
QuitX Patches are indicated for the treatment of nicotine dependence, as an aid to smoking cessation.
QuitX Patches are intended to be used as part of an effective behavioural therapy program in an
overall strategy for smoking cessation. Therapy should be confined to short term usage (3 months).
CONTRAINDICATIONS
QuitX Patches should not be used by:
•
Non-smokers, children under 12 years of age or occasional smokers (see Precautions)
•
People who are hypersensitive to the system or any component, including nicotine
•
People with diseases of the skin that may complicate patch therapy
PRECAUTIONS
Nicotine from any source can be toxic and addictive. Smoking causes lung cancer, heart disease and
emphysema, and may adversely affect the foetus and the pregnant woman. For any smoker, with or
without concomitant disease or pregnancy, the risk of nicotine replacement in a smoking cessation
program should be weighed against the hazard of continued smoking while using QuitX Patch
systems, and the likelihood of achieving cessation of smoking without nicotine replacement therapy
(see Overdosage).
QuitX Patches contain a thin aluminium lining which serves as a heat conducting foil. The patch
should be removed prior to undergoing any MRI (Magnetic Resonance Imaging) procedures.
Occasional smokers are not expected to benefit from the use of QuitX Patches.
Subjects should be informed that if they continue to smoke while using QuitX Patches, they may
experience increased adverse effects, including cardiovascular events (e.g. angina) due to peak
nicotine levels higher than those experienced from smoking alone.
The use of QuitX Patches beyond three months by patients who stop smoking should be discouraged,
because the chronic consumption of nicotine by any route can be harmful and addictive.
Patients should be instructed to promptly discontinue the use of QuitX Patches and contact their
doctors if they experience severe or persistent local skin reactions (e.g. severe erythema, pruritus or
oedema) at the site of application or a generalised skin reaction (e.g. urticaria, hives or generalised
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rash) (see Adverse Effects). Patients with contact sensitisation should be cautioned that a serious
reaction could occur from exposure to other nicotine containing products or smoking.
Underlying cardiovascular disease. In patients with stable cardiovascular disease, QuitX Patches
present a lesser hazard than continuing to smoke. However dependent smokers currently hospitalised
as a result of a recent myocardial infarction, severe dysrhythmia or recent cerebrovascular accident
and who are considered to be haemodynamically unstable should be encouraged to stop smoking with
non-pharmacological interventions. If this fails, QuitX Patches may be considered but as data on
safety in this patient group is 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 nicotine replacement therapy is initiated as catecholamines
released by nicotine can affect carbohydrate metabolism.
Allergic reactions. Discontinuation of treatment may be advisable in cases of severe or persistent
allergic reactions. Angioedema and urticaria have been reported. Contact sensitisation was reported in
a few patients using transdermal nicotine in clinical trials. Patients who develop contact sensitisation
to nicotine should be cautioned that a severe reaction could occur from smoking or exposure to other
nicotine containing products.
Renal and/or hepatic impairment. Should be used with caution in patients with moderate to severe
hepatic impairment as the clearance of nicotine or its metabolites may be decreased with the potential
for increased adverse effects.
Gastro-Intestinal disease. QuitX Patches should be used with caution in patients with peptic ulcers.
Pheochromocytoma and uncontrolled hyperthyroidism. QuitX Patches should be used with caution in
patients with uncontrolled hyperthyroidism or pheochromocytoma as nicotine causes release of
catecholamines.
Transferred dependence. Transferred dependence is rare and is both less harmful and easier to break
than smoking dependence.
Danger in small children. Doses of nicotine that are tolerated by adult and adolescent smokers can
produce severe toxicity in small children that may be fatal. Both before and after use, the patch
contains a significant amount of nicotine. Subjects must be cautioned that the patches must not be
handled casually or left where they might be inadvertently misused or consumed by children or pets.
Used patches must be disposed of with care by folding them in half with the adhesive sides inwards,
and ensuring that they do not fall into the hands of children under any circumstances (see
Precautions, Instructions to Patients).
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
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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.
Note: Precautions for the combination use of QuitX Patches with QuitX 2mg Coated Chewing Gum
are the same as those for each treatment alone.
Carcinogenicity and Mutagenicity
Nicotine itself does not appear to be a carcinogen in laboratory animals. However, nicotine and its
metabolites increased the incidence of tumours in the cheek pouches of hamsters and forestomach of
F344 rats, respectively, when given in combination with tumour initiators. One study, which could not
be replicated, suggested that cotinine, the primary metabolite of nicotine, may cause lymphoreticular
sarcoma in the large intestine in rats.
Nicotine and cotinine were not mutagenic in the Ames Salmonella test. Nicotine induced repairable
DNA damage in an Escherichia coli test system. Nicotine was shown to be genotoxic in a test system
using Chinese hamster ovary cells. In rats and rabbits, implantation can be delayed or inhibited by a
reduction in DNA synthesis that appears to be caused by nicotine. Studies have shown a decrease in
litter size in rats treated with nicotine during gestation.
Impairment of Fertility
Teratogenicity studies with nicotine in several animal species have demonstrated non-specific
retardation of foetal growth. In the mouse, the unborn offspring of dams treated with nicotine 25mg/kg
subcutaneously (SC), corresponding to approximately 120 times the human transdermal dose, showed
some skeletal defects in the peripheral parts of the limbs. Chronic SC administration of 1.5 or 3mg/kg
in pregnant rats caused some behavioural disorders in the offspring. In rats and rabbits, implantation of
the blastocyst in the uterine epithelium may be inhibited or delayed to a certain extent by a reduction
in DNA synthesis, which appears to be caused by nicotine.
Overall, there are no clear grounds for believing that nicotine has any teratogenic potential and/or
inhibitory effects on fertility at concentrations reached by the use of QuitX Patches.
Use in Pregnancy (Category D)
Nicotine is harmful to the foetus. Smoking during pregnancy is associated with risks such as intrauterine growth retardation, premature birth or still birth. Stopping smoking is the single most effective
intervention for improving the health of both the pregnant smoker and her baby. The earlier abstinence
is achieved, the better. Ideally, smoking cessation during pregnancy should be achieved without
nicotine replacement therapy. For women unable to quit on their own, nicotine replacement therapy
may be recommended to assist a quit attempt. The risk of using nicotine replacement therapy to the
foetus is lower than that expected with tobacco smoking, due to lower maximal plasma nicotine
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concentrations and no additional exposure to polycyclic hydrocarbons and carbon monoxide.
As nicotine passes to the foetus affecting breathing movements and has a dose-dependent effect on the
placental/foetal circulation, the decision to use nicotine replacement therapy should be made on a riskbenefit assessment as early on in pregnancy as possible with the aim of discontinuing use after 2 – 3
months.
Intermittent dose products, such as QuitX Coated Chewing Gums, 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 to avoid exposure overnight, when the foetus would not normally be subjected to smoke-derived
nicotine.
Use in Lactation
Nicotine from smoke and nicotine replacement therapy is found in breast milk. However the amounts
of nicotine the infant is exposed to is relatively small and less hazardous than the second-hand smoke
they would otherwise be exposed to.
Using intermittent dose products, such as QuitX Coated Chewing Gums, compared to patches, may
minimise the amount of nicotine in the breast milk as the time between administrations of nicotine
replacement therapy and feeding can be more easily prolonged. Women should breastfeed just before
using the product.
Effect on Ability to Drive or Operate Machinery
When used as recommended, there are minimal risks associated with the use of QuitX Patches in
driving vehicles or operating machinery.
Instructions to Patients
Safety note. QuitX Patches can be dermal irritants and can cause contact sensitisation. Although
exposure of healthcare workers to nicotine from QuitX Patches should be minimal, care should be
taken to avoid unnecessary contact with active systems. When the used patch is removed from the
skin, it should be folded over and placed in the protective patch that contained the new patch. The used
patch should be immediately disposed of in such a way as to prevent its access by children or pets.
Because QuitX Patches contain residual nicotine after use, they must therefore be kept out of reach of
children at all times. As with other nicotine containing transdermal patches, accidental application by
small children could produce severe symptoms of poisoning, and may prove fatal (see Precautions,
Danger in small children).
Interactions with Other Medicines
No clinically relevant interactions between nicotine replacement therapy and other drugs have
definitely been established, however nicotine may possibly enhance the haemodynamic effects of
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adenosine.
Smoking cessation, with or without nicotine replacement, may alter the individual’s response to
concomitant medication and may require adjustment of dose. In particular, anticonvulsants may
require special monitoring and/or dosage adjustment. Smoking is thought to increase the metabolism
through enzyme induction and thus to lower the blood concentrations of agents such as antipyrine,
caffeine, oestrogens, desmethyldiazepam, imipramine, lidocaine, oxazepam, pentazocine, phenacetin,
theophylline, and warfarin.
Cessation of smoking may result in increased concentrations of these agents.
Other reported effects of smoking include reduced analgesic efficacy of propoxyphene, reduced
diuretic response to frusemide, and altered pharmacological response to propranolol, as well as altered
rates of ulcer healing with H2-antagonists. Both smoking and nicotine can increase levels of circulating
cortisol and catecholamines.
Dosages of nifedipine, adrenergic agonists, or adrenergic blocking agents may need to be adjusted.
ADVERSE EFFECTS
In principle, QuitX Patches can cause adverse effects similar to those associated with nicotine
administered by other means (including smoking) and these are mainly dose dependent. Some
symptoms such as dizziness, headache, and sleep disturbance may be related to the withdrawal of
nicotine associated with stopping smoking. Since the maximum plasma concentrations of nicotine that
are produced by the patch are lower than those produced by smoking and fluctuate less, nicotinerelated adverse effects occurring during treatment with the patch can be expected to be less marked
than during smoking.
At recommended doses, QuitX Patches have not been found to cause any serious adverse effects.
Excessive use of QuitX Patches by those who have not been in the habit of inhaling tobacco smoke
could possibly lead to nausea, faintness or headaches.
Some of the symptoms listed below are hard to differentiate from recognised tobacco withdrawal
symptoms when comparison with placebo is made. The placebo used contained about 13% of the
nicotine of a matching QuitX Patch (to match colour and odour for blinding purposes).
The main unwanted effect of the QuitX Patch is local reaction at the application site. This led to
premature discontinuation of patches in about 6% of clinical trial participants. Skin reactions consisted
of erythema or pruritus at the patch site. Oedema, burning sensation, blisters, rash, or pinching
sensation at the application site was also noted. The majority of these reactions were mild. Most of the
skin reactions resolved within 48 hours, but in more severe cases the erythema and infiltration lasted
from 1 to 3 weeks. The time of onset of important skin reactions was between 3 and 8 weeks from the
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start of therapy. In isolated cases the skin reactions extended beyond the application sites. Isolated
cases of urticaria, angioneurotic oedema and dyspnoea were reported.
The following are the adverse events/withdrawal symptoms most commonly reported in three doubleblind clinical trials irrespective of causal association to study drug.
Nicotine transdermal patch
(N=401)
Placebo
(N=391)
Application site reaction
34.9%
17.6%
Headache
29.7%
29.2%
Cold and flu-like symptoms
12.0%
8.4%
Dysmenorrhoea
6.6% **
8.8% **
Insomnia
6.5%
5.4%
Nausea
6.2%
4.6%
Myalgia
6.0%
4.1%
Dizziness
6.0%
5.9%
** % of female subjects
The following unwanted experiences were also reported, irrespective of causal association with QuitX
Patch, at incidences of < 6%:
Incidence ≥ 2%, and greater than placebo (by at least 0.5%)
Abdominal pain, dyspepsia, allergy, motor dysfunction, coughing, abnormal dreaming, arthritis.
Incidence ≥ 2%, and similar to or less than placebo
Anxiety, emotional lability, irritability, constipation, diarrhoea, toothache, Arthralgia, back pain,
pharyngitis, rhinitis, sinusitis, upper respiratory symptoms.
Incidence between 1 and 2%
Somnolence, impaired concentration, vomiting, chest pain, fatigue, pain, changes in blood pressure,
bronchitis, rash, herpetic rash, earache.
Incidence ≤ 1%*
Hot flushes, local oedema, weight increase, extrasystoles, hypertension, palpitation, gastric ulcer, dry
mouth, flatulence, gingivitis, dysphagia, abnormal stool, thyroid disorders, lymph gland tenderness,
taste perversion, abnormal vision, dyspnoea, cystitis, paraesthesias, memory impairment, twitching,
confusion, agitation, increased appetite, leg cramps, migraine, pruritus, increased sweating, urticaria,
acne.
*Only events considered by the investigator to be possibly related to QuitX Patch are included in this
list, but the overall incidence was ≤ 1% irrespective of relationship to study agents. A similar profile
has also been observed in previous clinical trials.
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DOSAGE AND ADMINISTRATION
Patients should be instructed to stop smoking completely as they begin using QuitX Patch therapy.
The patient should read the package insert on QuitX Patch therapy and be encouraged to ask any
questions. Treatment should be initiated with QuitX Patches 21 mg/day (Step 1) for patients who
smoke more than 20 cigarettes a day; or 14 mg/day (Step 2) for those who smoke less. The size of the
patch may be adjusted according to individual response, maintaining or increasing the dose if
abstinence is not achieved or if withdrawal symptoms are experienced.
Once the appropriate dosage is selected the patient should begin four weeks of therapy at that dosage.
The patient should stop smoking cigarettes completely during this period. The size of the patch may be
adjusted according to individual response, maintaining or increasing the dose if abstinence is not
achieved or if withdrawal symptoms are experienced. The dosage cannot be adjusted by cutting a
transdermal patch. If the patient is unable to stop cigarette smoking within four weeks, professional
help should be sought.
Patients who have cardiovascular disease (see Precautions), weigh less than 45 kg or smoke less than
half a pack of cigarettes per day should start their therapy with QuitX Patch 14 mg/day (Step 2) for
four weeks and look at decreasing the dose to QuitX Patch 7 mg/day (Step 3) for the last eight weeks,
depending on the individual response. An overall 12 week plan still applies.
Patients who have successfully abstained from smoking should have their dose of QuitX Patches
reduced after each four weeks of treatment until the 7 mg/day (Step 3) dose has been used for four
weeks. The entire course of nicotine substitution and gradual withdrawal should take no more than 12
weeks. Total treatment periods of more than three months and daily doses above 30 cm2 have not been
evaluated.
The QuitX Patch system is contained in a child-resistant sachet. The sachet should be cut along the
dotted line to facilitate removal of the QuitX Patch contents. Following removal of the metallic
backing, the patch should be applied to a non-hairy, clean, dry skin site on the upper body or upper
outer arm and held in position for 10-20 seconds with the palm of the hand. After 24 hours, the used
QuitX Patch should be removed and a new patch applied to an alternate skin site. Skin sites should not
be reused for at least three days.
Patients should be cautioned not to continue to use the same patch for more than 24 hours. The patch
is recommended to be worn for 24 hours to minimise the chance of morning cravings. However, if the
user experiences any vivid dreams or other disruptions of sleep while wearing the patch for 24 hours,
it is recommended that the patch be removed at bed time (after 16 hours) and a new one put on upon
waking the next day. In pregnant patients, it is also recommended that the patch be removed before
going to bed (see Precautions; Use in Pregnancy).
QuitX Patches should be applied promptly upon its removal from the protective pouch to prevent
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evaporative loss of nicotine from the patch. QuitX Patches should only be used when the pouch is
intact to assure than the product has not been tampered with.
Drug Abuse and Dependence
QuitX Patch therapy is likely to have a low abuse potential (see Precautions, Transferred
dependence) based on differences between it and cigarettes in four characteristics commonly
considered important in contributing to abuse: slower absorption rate; smaller fluctuations in blood
concentrations; lower blood levels of nicotine; and less frequent use (i.e. once daily).
Moreover, gradual weaning from the patches is instituted within the treatment schedule, and the risk of
dependence after therapy is minimal. The effects of abrupt withdrawal from QuitX Patches are likely
to be similar to those observed with tobacco withdrawal from comparable nicotine concentrations.
Use in Children and Young Adults
The above recommendation can be used for adolescents between 12 and 18 years of age. As data is
limited in this age group, medical advice should be obtained should it be found necessary to use the
patch beyond 12 weeks. Nicotine Replacement therapy should only be used in adolescents in
conjunction with a counseling program.
QuitX Patches should not be used in children under 12 years of age (see Contraindications).
In Combination with QuitX Coated Chewing Gums
The use of combination therapy may be appropriate for smokers who have previously relapsed or
experienced cravings using NRT monotherapy, or who experience breakthrough craving or have
difficulty in controlling cravings for cigarettes with NRT monotherapy.
Initial treatment:
The treatment should begin with one 21 mg/day patch (Step 1) daily applied to an intact area of the
skin upon waking up in the morning and removed the next morning, combined with the 2mg gum. Use
a minimum of 4 x 2mg gums/day with a maximum recommended dose of 12 gums/day. Usually 5 to 6
gums will be adequate for effect.
This full dose should be used for 12 weeks. Gradual weaning from the products should then be
initiated.
Weaning from combination use:
This can be done in two ways:
-
By using lower strength patches i.e. 3 to 4 weeks on 14mg/day patches (Step 2) and then 3 to
4 weeks on 7 mg/day (Step 3), using the same amount of QuitX 2mg coated chewing gum as
per the initial treatment period, and then gradually reduce the amount of gums until only 1 – 2
gums are required each day, at which the therapy should be stopped, or alternatively,
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-
12
Stop using the patch and gradually reduce the number of gums up to 9 months. Those who use
nicotine replacement therapy beyond 9 months are recommended to seek additional help and
advice from a healthcare professional.
Recommended dosage:
Initial treatment
Time period
QuitX Patch
QuitX 2mg Coated Chewing Gum
12 weeks
1 x 21mg/day (Step 1) patch per day Minimum 4 gums per day and
maximum 12 gums per day. To be used
as needed.
Weaning – alternative 1
Next 3 to 4 weeks
1 x 14mg/day (Step 2) patch per day Continue to use gum as needed
Following 3 to 4
1 x 7mg/day (Step 3) patch per day Continue to use gum as needed
weeks
Up to 9 months
------------------------------Gradually wean from gum use
Weaning – alternative 2
Up to 9 months
------------------------------Continue to gradually wean from gum
use
Use in the Elderly
Experience in the use of QuitX Patches in smokers over the age of 65 years is limited. QuitX Patches
does not appear to pose safety problems in this age group.
OVERDOSAGE
The effects of applying several QuitX Patches simultaneously or swallowing QuitX Patches are
unknown (see Precautions).
The oral LD50 for nicotine in rodents varies with species but is in excess of 24mg/kg; death is due to
respiratory paralysis. The oral minimum acute lethal dose for nicotine in human adults is reported to
be 40 to 60mg (< 1mg/kg).
The toxicity of nicotine cannot be directly compared with that of smoking because tobacco smoke
contains additional toxic substances such as carbon monoxide, and tar.
Whilst chronic smokers can tolerate doses of nicotine that may be toxic to non-smokers, application of
several patches can result in overdosage symptoms.
Slower absorption after cutaneous exposure to nicotine favours the development of tolerance to toxic
effects. Rapid systemic delivery of nicotine from QuitX Patches would not be expected on chewing
and swallowing, owing to the slow release of nicotine from the patch and first-pass metabolism.
Acute Toxic Effects
Signs and symptoms of an overdose from QuitX Patches would be expected to be the same as those of
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acute nicotine poisoning, including pallor, cold sweat, nausea, salivation, vomiting, abdominal pain,
diarrhoea, headache, dizziness, disturbed hearing and vision, tremor, mental confusion and marked
weakness. Prostration, hypotension, irregular pulse, and respiratory failure may ensue with large
overdoses. Lethal doses produce convulsions quickly and death follows as a result of peripheral or
central respiratory paralysis or, less frequently, cardiac failure.
Management of Overdose
Overdose from topical exposure. QuitX Patches should be removed immediately if the patient shows
signs of overdosage, and immediate medical care should be sought. 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 blood stream for several hours (see Pharmacokinetics) after removal
of the system because of a depot of nicotine in the skin. Artificial respiration with oxygen should be
substituted if necessary.
Overdose from ingestion. People ingesting QuitX Patches should be referred to a healthcare facility for
management. Due to the possibility of nicotine induced seizures, activated charcoal should be
administered. In unconscious patients with a secure airway, instil activated charcoal via a nasogastric
tube. A saline cathartic or sorbitol added to the first dose of activated charcoal may speed
gastrointestinal passage of the system. Repeated doses of activated charcoal should be administered as
long as the patch remains in the gastrointestinal tract since it will continue to release nicotine for many
hours.
Management of nicotine poisoning
Other supportive measures include diazepam for seizures, atropine for excessive bronchial secretions
or diarrhoea, respiratory support for respiratory failure, and vigorous fluid support for hypotension and
cardiovascular collapse.
Contact the Poisons Information Centre on 13 11 26 (Australia) for further advice on management of
overdosage.
PRESENTATION AND STORAGE CONDITIONS
QuitX Patches. Transdermal nicotine patches:
Step 1: 21 mg/day (equiv. nicotine 52.5 mg, 30 cm2 release area)
Step 2: 14 mg/day (equiv. nicotine 35 mg, 20 cm2 release area)
Step 3: 7 mg/day (equiv. nicotine 17.5 mg, 10 cm2 release area)
Each box contains 7 patches. All presentations contain information on QuitX Patches and how to use
them.
QuitX Patches – Product Information
Store below 30°C. Do not refrigerate. Keep the patch sealed in the pouch until needed.
POISON SCHEDULE OF THE MEDICINE
Unscheduled.
NAME AND ADDRESS OF THE SPONSOR
Alphapharm Pty Limited
Chase Building 2
Wentworth Park Road
Glebe NSW 2037
ABN 93 002 359 739
www.alphapharm.com.au
DATE OF APPROVAL
Approved by the Therapeutic Goods Administration on 15 September 2008.
Date of most recent amendment: 13 May 2009.
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