Consumer medicine information

Nicabate Minis Mint

Nicotine

BRAND INFORMATION

Brand name

Nicabate Mini Lozenges

Active ingredient

Nicotine

Schedule

Unscheduled

 

Consumer medicine information (CMI) leaflet

Please read this leaflet carefully before you start using Nicabate Minis Mint.

What is in this leaflet?

This leaflet answers some common questions about NICABATE Minis. It does not contain all the available information.

It does not take the place of talking to your pharmacist or doctor.

All medicines have risks and benefits. Your doctor or pharmacist has weighed the risks of you using NICABATE Minis against the benefits this medicine is expected to have for you.

If you have any concerns about using this medicine, ask your pharmacist or doctor.

Keep this information with the medicine. You may need to read it again.

What are NICABATE Minis used for?

NICABATE Minis are a stop smoking aid. They can help you stop smoking over a few months. You can also use them to help you stop smoking more gradually over a longer period of time.

They help you to give up smoking by replacing some of the nicotine you are used to getting from cigarettes. It is the nicotine in cigarettes that can make you physically addicted to them. This type of treatment is called Nicotine Replacement Therapy (NRT).

NICABATE Minis contain a nicotine resin and, when used, nicotine is released slowly from the resin and absorbed through the lining of the mouth. This medicine can reduce your urge to smoke by providing some of the nicotine previously inhaled from cigarettes and helps you resist cigarettes. You may feel the following withdrawal symptoms when you stop smoking; anger, irritability, frustration; anxiety; difficulty concentrating; restlessness; increased appetite and or weight gain; insomnia; depression. The nicotine in NICABATE Minis may help relieve some or many of these symptoms.

There are no health benefits to smoking. It is always better to give up smoking and using NRT can help. In general any possible side effects associated with NRT are far outweighed by the well-established dangers of continuing to smoke.

If possible, when giving up smoking, NICABATE Minis should be used with a stop smoking behavioural support programme such as the NICABATE Quit Smoking Support Programme.

NICABATE 1.5 mg Minis are suitable for smokers who smoke 20 cigarettes or less a day.

NICABATE 4 mg Minis are suitable for smokers who smoke more than 20 cigarettes a day.

Your pharmacist or doctor may have given you this medicine for another reason.

If you need more information ask your pharmacist or doctor.

Before you use NICABATE Minis

When you must not use them

You should not use NICABATE Minis if:

  • You are allergic to nicotine or any of the ingredients listed at the end of this leaflet.
  • You are a non-smoker.
  • You are under 12 years of age.

If you are in hospital because of a heart attack, severe heart rhythm disturbances or a stroke, you should try to quit smoking without using NRT unless your doctor tells you to use it. Once you are discharged from hospital, you may use NRT in consultation with your doctor.

If you have diabetes you should monitor your blood sugar levels more often than usual when starting NICABATE Minis as you may find your insulin or other medication requirements alter.

If you have had allergic reactions that involve swelling of the lips, face and throat (angioedema) or itchy skin rash (urticaria), using NRT can sometimes trigger this type of reaction.

If you have epilepsy or are taking medicine for seizures, you should not use NICABATE Minis unless your doctor has told you to.

Do not use NICABATE Minis if you are under 12 years of age. The levels of nicotine in NRT are suitable for people who are giving up smoking but not for children under 12. Children are more likely to be affected by nicotine and it could cause severe toxicity which can be fatal. Make sure you keep nicotine containing products out of the reach and sight of children at all times.

Do not use the medicine after the expiry date (EXP) printed on the pack. If you take it after the expiry has passed, it may not work as well.

Do not use NICABATE Minis if the packaging is torn or shows signs of tampering.

Do not use this medicine to treat any other complaint unless your doctor or pharmacist says it is safe.

Do not give this medicine to anyone else even if they have the same symptoms as you.

Before you start to use it

You must tell your pharmacist or doctor if:

  • You have an uncontrolled, overactive thyroid gland. Nicotine may make your symptoms worse.
  • You have a stomach or duodenal ulcer or inflammation of the oesophagus. Swallowing nicotine can make your symptoms worse. Some people have reported getting mouth ulcers. If your symptoms do get worse you should talk to your doctor and you might want to use a non-oral type of NRT such as patches.
  • You have heart or circulation problems including heart failure or stable angina or high blood pressure.
  • You have had a stroke.
  • You have any serious liver or kidney disease. You may be more prone to side effects.
  • You are a diabetic.
  • You have been diagnosed as having a tumour of the adrenal glands (phaeochromocytoma). Nicotine may make your symptoms worse.
  • You have any allergies to any other medicines.
  • You are pregnant or intend to become pregnant.
  • You are breastfeeding or planning to breastfeed.
  • You have ever experienced seizures.

If you have not told your pharmacist or doctor about any of the above, tell them before you use NICABATE Minis.

If you are pregnant or breastfeeding then you should try to quit smoking without the use of NICABATE Minis if possible. However it is better to stop smoking using NRT than to continue smoking.

If you are pregnant
Smoking during pregnancy has risks such as poor growth of your baby before birth, premature birth or still birth. Stopping smoking is the best way to improve both your health and that of your baby. The earlier you stop smoking, the better.

Ideally, if you are pregnant, you should stop smoking without using NRT. However, if you have tried and this hasn’t worked, NRT may be recommended to help you stop smoking. This is because it is better for your developing baby than if you carry on smoking. The decision to use NRT should be made as early on in your pregnancy as possible and you should aim to use it for only 2-3 months. Remember, the most important thing is to stop smoking.

Products that are taken intermittently, such as lozenges or Gum, are preferable to nicotine patches. However, patches may be preferred if you have nausea or sickness.

If you are breastfeeding
Tobacco smoke causes breathing difficulties and other problems in babies and children. If you need to use NRT to help you quit, the amount of nicotine your baby may receive is much smaller and less harmful than breathing in second hand smoke. Do not use patches if you are breastfeeding. You should use NRT products that are taken intermittently (e.g. Gum or lozenges rather than patches) and breastfeed just before you take the product. This allows as long a time as possible between NRT use and feeding and will help your baby to get the smallest amount of nicotine possible.

Using other medicines

Tell your pharmacist or doctor if you are using any other medicines, including any that you buy without a prescription from your pharmacy, supermarket or health food shop.

Stopping smoking, with or without nicotine replacement products such as NICABATE Minis may alter the absorption of some medicines. The doses of the other medicines that you are using may need to be changed.

Other medicines may be affected by NICABATE Minis or affect how well NICABATE Minis work.

Your pharmacist or doctor can tell you what to do if you are taking any of these medicines.

If you have not told your pharmacist or doctor about any of these things, tell him/her before you take any NICABATE Minis

How to use NICABATE Minis

During any attempt to give up smoking using NICABATE Minis, it is important that you make every effort to stop smoking completely. However, if you do smoke a cigarette while you are using NRT, you should continue your quit attempt. Talking to your pharmacist or doctor may help.

For some people, the use of more than one NRT product may help them to identify the combination most appropriate for their individual quit attempt.

NICABATE 1.5 mg Minis are suitable for smokers who smoke 20 cigarettes or less a day.

NICABATE 4 mg Minis are suitable for smokers who smoke more than 20 cigarettes a day.

One lozenge should be placed in the mouth and be allowed to dissolve to be effective. From time to time the lozenge should be moved from one side of the mouth to the other. The lozenge should not be chewed, sucked or swallowed whole.

You should not eat or drink while a lozenge is in your mouth as this may reduce the absorption of nicotine. Avoid drinking acidic beverages such as coffee, juices and fizzy drinks for 15 minutes before sucking the lozenge as this may also reduce the absorption of nicotine.

Adults (18 years and over)

For smokers who want to stop smoking abruptly.

NICABATE Minis should be used according to the following schedule:

Weeks 1 to 6
1 lozenge every 1 to 2 hours

Weeks 7 to 9
1 lozenge every 2 to 4 hours

Weeks 10 to 12
1 lozenge every 4 to 8 hours

To help you stay smoke free over the next 12 weeks, take 1 lozenge in situations where you are strongly tempted to smoke.

Do not use more than 1 NICABATE Mini at a time and do not use more than 15 of the 4 mg NICABATE Minis or 20 of the 1.5 mg NICABATE Minis per day during weeks 1 to 6.

Do not use more than 1 NICABATE Mini per hour.

Adults aged 18 years and over should use at least nine NICABATE Minis a day for the first 6 weeks.

For adult smokers who want to stop over several months.

Use a lozenge whenever you have a strong urge to smoke instead of smoking a cigarette. Do not use more than 15 of the 4 mg NICABATE Minis a day or 20 of the 1.5 mg NICABATE Minis a day.

Do not use more than 1 NICABATE Mini per hour.

When you have reduced the number of cigarettes you smoke each day to a level you feel you can quit completely then use the schedule in the section above for smokers who want to quit smoking abruptly

If you have not reduced the number of cigarettes you smoke each day after 6 weeks, then see your pharmacist or doctor.

If you still need to use NICABATE Minis on a regular basis 6 months after the start of treatment and haven’t started a permanent quit attempt, you should seek help and advice from your pharmacist or doctor.

Using NICABATE combination therapy

Combination therapy can be used by smokers who have been unsuccessful giving up smoking when they have used just one type of NRT.

Do not use in young people aged 12 to 17 years.

If you want to use NICABATE Patches together with NICABATE 2 mg Gum, 2 mg Lozenges or 1.5 mg Minis, you should start with the 21 mg patch and you should use at least 4 pieces of Gum, Lozenges or Minis a day. Most people use 4 to 5 pieces a day. Do not use more than 12 pieces of Gum, Lozenges or Minis a day when using in addition to the patch.

If you are using NICABATE Patches together with Gum, Lozenges or Minis, the combination treatment should be used for 12 weeks. After this time you should begin weaning yourself off NRT. You can do this by:

  1. Using the 14 mg patch for 2 weeks and then the 7 mg patch for 2 weeks while continuing to take the same number of NICABATE Minis you routinely use. Once you are not using any patches, you can gradually reduce the number of Lozenges, Minis or pieces of Gum until you are not using any.

OR

  1. Stop using the 21 mg patch and then gradually reduce the number of Lozenges, Minis or pieces of Gum you are using.

Use in adolescents (12-17 years)

Young people aged 12 to 17 years old should only use NICABATE Minis for 10 weeks in total. If you think you may need to use NICABATE Minis for longer than 10 weeks, talk to your pharmacist or doctor.

NRT should only be used by those aged 12 to 17 years if a counselling programme is used at the same time. NRT is not likely to work in this age group if there is no counselling with it.

Use in children

Children under 12 years of age should not use NICABATE Minis.

How long to use it

Adults (over 18 years): NICABATE Minis should not be used after 9 months. If you find it difficult to give up NICABATE Minis or you are worried that you may start smoking again than speak to your pharmacist or doctor.

To give you the best chance for success, it is important you complete the step down programme in full. This is because the urge to smoke and withdrawal symptoms can occur for weeks after stopping smoking.

Young people aged 12 to 17 years old should only use NICABATE Minis for 10 weeks in total (see Use in adolescents (12-17 years) above).

If you do start smoking again, you may want to talk to your pharmacist about how to get the best results from further courses of NICABATE Minis.

The directions given to you by your pharmacist or doctor may be different from the information in this leaflet. If you are unsure how to use this medicine, ask your pharmacist or doctor for advice.

If you use too much (Overdose)

If you smoke or use any other nicotine containing product while you are using NICABATE Minis, you may suffer an overdose of nicotine. However, if used correctly, nicotine overdose is unlikely.

Symptoms of nicotine overdosage include:

  • Headache
  • Dizziness
  • Stomach upset
  • Drooling
  • Vomiting
  • Diarrhoea
  • Cold sweat
  • Blurred vision
  • Hearing distortion
  • Confusion
  • Weakness
  • Fainting

If it is a large overdose, you may collapse and experience breathing difficulty.

Immediately telephone your doctor or Poisons Information Centre (Australia telephone 13 11 26, New Zealand telephone 0800 764 766) for advice or go to Accident and Emergency at your nearest hospital, if you think that you or anyone else may have used too many NICABATE Minis.

Do this even if there are no signs of discomfort or poisoning. You may need urgent medical attention. Keep telephone numbers of these places handy.

NICABATE Minis are not suitable for children under 12 or for non-smokers. They may develop signs of nicotine overdose including headache, sickness, stomach pains and diarrhoea. Even small amounts of nicotine can be dangerous to children. If you think a child has used any NICABATE Minis, you must contact a doctor immediately.

While you are using NICABATE Minis

Things you must do

Use NICABATE Minis exactly as your pharmacist or doctor has told you to.

Tell all your doctors, dentists and pharmacists that you are using NICABATE Minis.

Tell your doctor or pharmacist if you become pregnant while using NICABATE Minis.

Side Effects

Tell your doctor or pharmacist as soon as possible if you do not feel well while taking NICABATE Minis.

NICABATE Minis help most people but they may have unwanted side effects in a few people.

All medicines can have side effects. Sometimes they are serious, most of the time they are not. You may need medical treatment if you get some of the side effects.

Stopping smoking itself can cause some symptoms such as dizziness, headache, sleep disturbance, cough and cold-like symptoms. Symptoms such as depression, irritability, anxiety and insomnia may also be related to withdrawal symptoms associated with giving up smoking.

Ask your doctor or pharmacist to answer any questions you may have.

Tell your pharmacist or doctor if you notice any of the following and they worry you:

  • Sore or swollen throat
  • Slightly sore or irritated mouth or tongue
  • Nausea
  • Hiccups
  • Stomach upsets
  • Vomiting
  • Diarrhoea
  • Indigestion/heartburn
  • Flatulence
  • Constipation
  • Dry mouth
  • Insomnia
  • Cough
  • Excess saliva
  • Dizziness
  • Headache
  • Palpitations (feeling your heart beat)

These are the more common side effects of NICABATE Minis. Mostly these are mild and short-lived. You may experience these side effects as you decrease the number of lozenges that you use.

If any of the following happen, stop using NICABATE Minis and tell your doctor immediately or go to accident and emergency at your nearest hospital:

  • Fast or very irregular heartbeat
  • Severe allergic reaction, symptoms of which include sudden wheeziness or tightness of the chest, rash and feeling faint.

These are very serious side effects. You may need urgent medical attention or hospitalisation.

Other side effects not listed above may also occur in some people. Tell your pharmacist or doctor if you notice anything else that is making you feel unwell. Do not be alarmed by this list of possible side effects. You may not experience any of them.

Transferred dependence
Some people worry that they will quit smoking but become dependent on NICABATE Minis. This is very rare and, if it did happen, it is less harmful to you than continuing to smoke and an easier habit to break.

After using NICABATE Minis

Storage

Keep your NICABATE Minis in their container until it is time to use them. If you keep the lozenges out of their container, they will not keep well.

Keep NICABATE Minis in a cool dry place Heat and dampness can destroy some medicines. Do not leave NICABATE Minis in the car on hot days.

Store Mint lozenges below 30°C

Do not store NICABATE Minis or any other medicine in the bathroom or near a sink. Keep NICABATE Minis where children and pets cannot reach them. A locked cupboard at least one and a half metres above the ground is a good place to store medicines.

Disposal

If your pharmacist or doctor tells you to stop using NICABATE Minis, ask your pharmacist what to do with any lozenges that are left over.

This is not all the information that is available on NICABATE Minis. If you have any more questions or are not sure about anything, ask your pharmacist or doctor.

Product Description

NICABATE Minis come in two strengths.

Active ingredient
Each NICABATE Minis lozenge contains either 1.5 mg or 4 mg of nicotine in the form of a resin complex called nicotine polacrilex. Nicotine polacrilex is also known as nicotine resinate.

Other ingredients:

  • Mannitol
  • Sodium alginate
  • Xanthan gum
  • Potassium bicarbonate
  • Polacrilin
  • Calcium polycarbophil
  • Sodium carbonate anhydrous
  • Magnesium stearate
  • Acesulfame potassium
  • Flavours
  • Water purified

Each strength comes in a container containing 20 lozenges.

Manufactured by

GlaxoSmithKline Consumer Healthcare
82 Hughes Avenue
ERMINGTON NSW 2115
ACN: 008 399 415

NICABATE Minis have the following Australian Registration numbers for:

Mint flavoured:

  • AUST R 156603 (1.5 mg)
  • AUST R 156604 (4 mg)

Date of preparation: March 2019

NICABATE and the MINIs device are trade mark of the GlaxoSmithKline group of companies.

Free NICABATE Quit Smoking Support Programme

Stopping smoking is a major decision that marks a turning point in your life. We are pleased that you have chosen to use NICABATE to help you quit.

Becoming an ex-smoker is not just about overcoming the cravings and urges for a cigarette, it is also about modifying your lifestyle to overcome the habits of smoking, like having a cigarette with your coffee or on the phone.

With NICABATE you don’t have to go it alone. Using NICABATE Minis will help you reduce the cravings for a cigarette and by joining our free stop smoking programme you can also receive help with the behavioural aspects of quitting.

This programme is FREE to anyone who has bought NICABATE. It is a programme designed to help you break the behavioural aspects of your smoking habit.

To join the programme, go to www.NICABATE.com.au

Published by MIMS November 2020

BRAND INFORMATION

Brand name

Nicabate Mini Lozenges

Active ingredient

Nicotine

Schedule

Unscheduled

 

1 Name of Medicine

Nicotine.

2 Qualitative and Quantitative Composition

Active ingredient.

Nicotine.
Nicotine 1.5 mg lozenge.
Nicotine 4 mg lozenge.

Excipients.

For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Nicabate Mini Lozenges nicotine 1.5 mg mint flavour lozenges.

White to off white oval tablet with convex surfaces; one surface bearing a debossed "L" logo.

Nicabate Mini Lozenges nicotine 4 mg mint flavour lozenges.

White to off white oval tablet with convex surfaces; one surface bearing a debossed "F" logo.

4 Clinical Particulars

4.1 Therapeutic Indications

For the relief of nicotine withdrawal symptoms including cravings associated with smoking cessation. It may also be used as part of a smoking reduction strategy by smokers who are unable or not ready to stop smoking abruptly as a step towards stopping smoking. It should be used as part of a behavioural support programme.

4.2 Dose and Method of Administration

Directions for use.

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 10-13 minutes). The lozenge should not be chewed or swallowed whole.
Users should not eat or drink while a lozenge is in the mouth.

Adults (18 years and over including the elderly).

Abrupt cessation of smoking.

Nicabate Mini Lozenges 1.5 mg are suitable for smokers who smoke 20 cigarettes or less a day.
Nicabate Mini Lozenges 4 mg are suitable for smokers who smoke more than 20 cigarettes a day.
Users should make every effort to stop smoking completely during treatment with Nicabate Mini Lozenges.
Behavioural therapy, advice and support will normally improve the success rate.
Users should follow the schedule of treatment in Table 1.
During weeks 1 to 6 it is recommended that users take at least nine lozenges per day.
Users should not exceed 15 of the 4 mg Minis per day or 20 of the 1.5 mg Minis per day during weeks 1 to 6.
Users should not use more than 1 lozenge per hour.
Those who use the lozenges beyond 9 months are recommended to seek additional help and advice from a healthcare professional who may consider alternate quit strategies such as combination therapy.

Gradual cessation of smoking (reduce to quit).

For smokers who are unwilling or unable to quit abruptly. 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 possible. The number of lozenges a day is variable and depends on the patient's needs. Nonetheless it should not exceed 15 of the 4 mg lozenges per day or 20 of the 1.5 mg lozenges per day.
If a reduction in cigarette consumption has not been achieved after 6 weeks of treatment, a healthcare professional should be consulted. Reduced tobacco consumption may help to 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 schedule for "abrupt cessation" as given above.
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.

Combination therapy.

In some instances, it may be beneficial to utilize more than one form of NRT concurrently. For example, combination therapy could be used by smokers who have relapsed with NRT monotherapy in the past, who experience breakthrough cravings or have difficulty controlling cravings for cigarettes using single therapy. This would allow users to identify the combination most appropriate for their individual quit attempt. If required, Nicabate gum 2 mg, Nicabate lozenges 2 mg or Nicabate Mini Lozenges 1.5 mg may be combined with Nicabate 21 mg patches. Nicabate 4 mg lozenges and/or Nicabate 4 mg Minis and/or Nicabate 4 mg gum should not be used with Nicabate patches.
When using Nicabate 21 mg patches in addition to Nicabate 2 mg gums, 2 mg lozenges or 1.5 mg Minis, it is recommended that a minimum of 4 pieces of gum/4 lozenges/4 Minis are used daily. Most people will use 4-5 pieces. The maximum number of gum, lozenges or Minis used in conjunction with the patch is 12 pieces per day.
Combination treatment should be used for 12 weeks after which weaning may be initiated. If required, weaning may be done by either:
1. Using Nicabate 14 mg patch for 2 weeks and then Nicabate 7 mg patch for 2 weeks while maintaining the number of pieces of 2 mg gum/lozenges or 1.5 mg Minis that have been routinely used. Then, when a patch is no longer used, the number of pieces of gum/lozenges or 1.5 mg Minis can be gradually reduced; or
2. Stopping use of Nicabate 21 mg patch and then gradually reducing the number of pieces of 2 mg gum/lozenges or 1.5 mg Minis that are being used.
Users should stop smoking completely during treatment with Nicabate 2 mg gum/lozenge or 1.5 mg Minis in combination with Nicabate 21 mg patches.

Children and adolescents.

The use of NRT in adolescents should only be used when the benefits of abstinence outweigh the risks of continued smoking.
Data are limited in relation to the value of NRT use in young people where the demand for cessation products and the motivation to quit is low. Nevertheless NRT is safe in this group. NRT should only be used by adolescents in conjunction with a counselling programme. Counselling is needed in this age group because NRT is likely to be ineffective in the absence of counselling.
Adolescents (12-17 years) should follow the schedule of treatment for adults in the table above for steps 1, 2 and 3 but, as data are limited, duration of NRT in this age group is restricted to 10 weeks. If longer treatment is required, advice from a healthcare professional should be sought who can then reassess the patient for their commitment to quitting and the benefits of continued treatment. If treatment is continued, it should not be extended for more than another four weeks.
Nicabate Mini Lozenges should not be used by adolescents for gradual cessation of smoking.
Adolescents should not quit with a combination NRT regimen.
Nicabate Mini Lozenges should not be used in children under 12 years of age.

4.3 Contraindications

Nicabate should not be used by:
Non-smokers;
Children under 12 years of age;
Those with hypersensitivity to nicotine or any of the excipients.

4.4 Special Warnings and Precautions for Use

The risks associated with the use of NRT (nicotine replacement therapy) are substantially outweighed in virtually all circumstances by the well established dangers of continued smoking.

Patients hospitalised for myocardial infarction, severe dysrhythmia or CVA.

Patients hospitalised for myocardial infarction, severe dysrhythmia or CVA (cerebrovascular accident) who are considered to be haemodynamically unstable should be encouraged to stop smoking with non-pharmacological interventions. If this fails, Nicabate Mini 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. If there is a clinically significant increase in cardiovascular or other effects attributable to nicotine, the mini lozenges should be reduced or discontinued. Use with caution in patients with recent or unstable cardiovascular disease. In patients with unstable cardiovascular disease, do not continue NRT if patient continues to smoke.
The combination NRT regimen should not be used in people with known cardiovascular disease without evaluation of the risk/benefit by a health care professional.

Diabetes mellitus.

Blood glucose levels may be more variable when stopping smoking, with or without NRT, so it is important for patients with diabetes mellitus to monitor their blood glucose levels more closely than usual when NRT is initiated as catecholamines released by nicotine can affect carbohydrate metabolism and vasoconstriction may delay/reduce insulin absorption.

Seizures.

Potential risk and benefits of nicotine should be carefully evaluated before use in subjects taking anti-convulsant therapy or with a history of epilepsy as cases of convulsions have been reported in association with nicotine.

Allergic reactions.

Susceptibility to angioedema and urticaria. NRT should be used with caution by patients who are susceptible to angioedema and/or urticaria.

Phaeochromocytoma and uncontrolled hyperthyroidism.

Use with caution in patients with uncontrolled hyperthyroidism or phaeochromocytoma as nicotine causes release of catecholamines. A risk-benefit assessment should be made by an appropriate healthcare professional.

GI disease.

Swallowed nicotine may exacerbate symptoms in patients suffering from active oesophagitis, oral or pharyngeal inflammation, gastritis and gastric or peptic ulcers. Oral NRT preparations should be used with caution in these conditions. Ulcerative stomatitis has been reported. A risk-benefit assessment should be made by an appropriate healthcare professional.

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.

Transferred dependence.

Transferred dependence is rare and is both less harmful and easier to break than smoking dependence.
Combination Nicabate therapy should not be used in people with known cardiovascular disease without evaluation of the risk/benefit by a health professional.
Nicabate products should be kept out of the sight and reach of children.

Use in hepatic impairment.

Use 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. A risk-benefit assessment should be made by an appropriate healthcare professional.

Use in renal impairment.

Use with caution in patients with severe renal impairment as the clearance of nicotine or its metabolites may be decreased with the potential for increased adverse effects. A risk-benefit assessment should be made by an appropriate healthcare professional.

Use in the elderly.

No data available.

Paediatric use.

Do not use in children under 12 years of age.

Effects on laboratory tests.

No data available.

4.5 Interactions with Other Medicines and Other Forms of Interactions

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, with or without nicotine replacement, may alter the individual's response to concomitant medication and may require adjustment of dose.
Polycyclic aromatic hydrocarbons in tobacco smoke induce the metabolism of drugs metabolised by CYP1A2 (and possibly by CYP1A1). When a smoker stops this may result in a slower metabolism and a consequent rise in blood levels of such drugs.
The following drugs may require adjustment in dose at cessation of smoking: caffeine, theophylline, imipramine, pentazocine, tacrine, clomipramine, insulin, clozapine, olanzapine and fluvoxamine. In particular, anticonvulsants may require special monitoring and/or dosage adjustment.
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.

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

In rats and rabbits, implantation can be delayed or inhibited by a reduction DNA synthesis that appears to be caused by nicotine. Studies have shown a decrease in litter size in rats treated with nicotine during gestation.
(Category D)
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 should only be used on the advice of a health care professional. Nicotine is harmful to the foetus. However, 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/foetal 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.
While no data exist to support one form of NRT over another, it may be prudent to use intermittent dosing products 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. Nicabate patches should not be used while breastfeeding. Intermittent dosing products such as Nicabate gums, lozenges or mini lozenges, should be used while breastfeeding and women should breast feed just before they use the product to allow as long a time as possible between NRT use and feeding.

4.7 Effects on Ability to Drive and Use Machines

Used as recommended there are minimal risks associated with the use of Nicabate Mini Lozenges in driving vehicles or operating machinery. Nevertheless, one should take into consideration that smoking cessation can cause behavioural changes.

4.8 Adverse Effects (Undesirable Effects)

Nicotine lozenges can cause adverse reactions similar to those associated with nicotine from tobacco. Many of the observed adverse reactions are consistent with the pharmacological effects of nicotine, which are dose dependent.

Clinical trial data.

The following undesirable effects detailed in Tables 2 and 3 are nicotine related adverse events for all oral dosage forms.
Table 2 shows events which were identified from a double-blind, randomised, placebo-controlled lozenge clinical study involving 1818 patients. Adverse events reported in this study have been considered for inclusion, where the incidence in the 2 mg or 4 mg nicotine arm was higher than the corresponding placebo arm. Frequencies calculated from the study safety data.

Post marketing.

Table 3 shows events which have been identified from post-marketing experience of oral nicotine products. Frequencies for these events cannot be estimated for oral nicotine dosage forms from the available data.

Reporting suspected adverse effects.

Reporting suspected adverse reactions after registration of the medicinal product is important. It allows continued monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions at www.tga.gov.au/reporting-problems.

4.9 Overdose

Nicotine doses that are tolerated by adult smokers during treatment may produce severe symptoms of poisoning in small children and may be fatal.
Signs and symptoms of an overdose from nicotine mini 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 and convulsions may ensue with large overdoses.

Treatment of overdose.

For information on the management of overdose, contact the Poison Information Centre on 13 11 26 (Australia).
All nicotine intake should stop immediately and the patient should be treated symptomatically. Activated charcoal may reduce absorption of the medicine if given within one or two hours after ingestion. In patients who are not fully conscious or have impaired gag reflex, consideration should be given to administering activated charcoal via a nasogastric tube, once the airway is protected.

5 Pharmacological Properties

Nicotine, the chief alkaloid in tobacco products, binds stereoselectively to acetylcholine receptors at the autonomic ganglia, in the adrenal medulla, at neuromuscular junctions and in the brain. Two types of central nervous system effects are believed to be the basis of nicotine's positively reinforcing properties. A stimulating effect exerted mainly in the cortex via the locus ceruleus, produces increased alertness and cognitive performance. A "reward" effect via the "pleasure system" in the brain is exerted in the limbic system. At low doses the stimulant effects predominate, while at high doses the reward effects predominate. Intermittent intravenous administration of nicotine activates neurohormonal pathways, releasing acetylcholine, noradrenaline, dopamine, serotonin, vasopressin, beta-endorphin, growth hormone, and ACTH.

5.1 Pharmacodynamic Properties

Mechanism of action.

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 include peripheral vasoconstriction, tachycardia, and elevated blood pressure. Acute and chronic tolerance to nicotine develops from smoking tobacco or ingesting nicotine preparations. Acute tolerance (a reduction in response for a given dose) develops rapidly (less than 1 hour), but at distinct rates for different physiological effects (skin temperature, heart rate, subjective effects). Withdrawal symptoms, such as cigarette craving, can be reduced in some individuals by plasma nicotine levels lower than those for smoking.
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. Nicotine toxicity is characterised by nausea, abdominal pain, vomiting, diarrhoea, diaphoresis, flushing, dizziness, disturbed hearing and vision, confusion, weakness, palpitations, altered respiration and hypotension.

Clinical trials.

A multicentre, double blind, placebo controlled, randomised, parallel group study assessed the efficacy of nicotine lozenges 2 mg and 4 mg in smokers wanting to quit. These lozenges had a different formulation to that of the Nicabate Mini Lozenges. Treatment allocation was based on time to first cigarette (TTFC). Those smoking within 30 minutes of waking were allocated to the 4 mg group (or matching placebo) and those smoking more than 30 minutes after waking were allocated to the 2 mg group (or matching placebo).
The study was undertaken in both the USA and the UK. A total of 1,818 smokers motivated to stop and aged over 18 years were randomised; 459 in the 2 mg active group, 458 in the 2 mg placebo, 450 in the 4 mg active and 451 in the 4 mg placebo.
Subjects were given clear instructions on how to suck the lozenge. Treatment instructions were to use one lozenge every 1-2 hours for the first 6 weeks, one lozenge every 2-4 hours for weeks 7-9, and one lozenge every 4-8 hours for weeks 10-12. Thereafter subjects were advised to use 1-2 lozenges per day as needed to remain abstinent. During the first six weeks, subjects were advised to use a minimum of 9 lozenges daily. At the end of 6 months subjects were told to abstain from taking the lozenge.
Six week, 3 month and 6 month, continuous, biochemically confirmed smoking cessation rates presented by treatment group are tabulated in Table 4.
In a single clinical study, Nicabate 4 mg lozenge has been shown to attenuate cessation related weight gain in high dependency smokers during the 12 weeks treatment period. Weight gain was reduced from a mean of 2.30 kg (range -3.6 to 7.3 kg) in placebo lozenge users to 1.27 kg (range -3.7 to 9.9 kg) in 4 mg lozenge users after 6 weeks lozenge use, and reduced from 3.40 kg (range -2.2 to 10.9 kg) in placebo users to 2.67 kg (range -4.2 to 14.5 kg) in 4 mg lozenge users after 3 months lozenge use. Weight gain rebounded to at least placebo levels after cessation of use of the lozenges in subjects continuing to abstain from smoking.

5.2 Pharmacokinetic Properties

Absorption.

Nicabate Mini Lozenges dissolve completely 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 Mini Lozenges is typically achieved in approximately 10-13 minutes. The mean peak plasma concentrations of nicotine achieved after a single 4 mg dose are approximately 9.1 nanogram/mL.

Distribution.

The plasma protein binding of nicotine is low (4.9%), and 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.

Metabolism.

Nicotine is extensively metabolised 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 metabolised primarily to cotinine but is also metabolised 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 oxidised to trans-3'-hydroxycotinine, which is the most abundant metabolite of nicotine in the urine. Both nicotine and cotinine undergo glucuronidation.

Excretion.

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/hour. 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.
A multiple dose pharmacokinetic study, comparing the 1.5 mg Nicabate Mini Lozenges with commercially available 2 mg nicotine gum, that the products were not bioequivalent - Cmax was 18.5% higher and AUC 17% higher for the 1.5 mg Nicabate Mini Lozenges compared with the 2 mg gum.
A single dose pharmacokinetic study, comparing the 4 mg Nicabate Mini Lozenges with commercially available 4 mg nicotine gum, demonstrated the products were not bioequivalent - Cmax was 23% higher and AUC 44% higher for the Nicabate Mini Lozenges compared with the gum. A single dose pharmacokinetic study, comparing the 4 mg Nicabate Mini Lozenges with the standard Nicabate 4 mg lozenge, demonstrated the 4 mg Nicabate Mini Lozenges to be bioequivalent with the standard 4 mg lozenge.

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

Genotoxicity.

Nicotine and cotinine were not mutagenic in the Ames Salmonella test. Nicotine induced repairable DNA damage in an E. coli test system. Nicotine was shown to be genotoxic in a test system using Chinese hamster ovary cells.

Carcinogenicity.

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.

6 Pharmaceutical Particulars

6.1 List of Excipients

Mannitol, Sodium alginate, Xanthan gum, Potassium bicarbonate, Calcium polycarbophil, Sodium carbonate anhydrous, Acesulfame potassium, Magnesium stearate, Micron Artificial Menthol Flavor TAK-02084, Micron Intensates Natural and Artificial Flavor Blend Masking Type TAK-031431, Micron Natural and Artificial Peppermint Flavor TAK-022173, Polacrilin and Water-purified.

6.2 Incompatibilities

Incompatibilities were either not assessed or not identified as part of the registration of this medicine.

6.3 Shelf Life

In Australia, information on the shelf life can be found on the public summary of the Australian Register of Therapeutic Goods (ARTG). The expiry date can be found on the packaging.

6.4 Special Precautions for Storage

Store below 30°C.

6.5 Nature and Contents of Container

Nicabate Mini Lozenges are presented in a polypropylene tube containing 20 lozenges with a reclosable flip top lid.
Pack sizes include 20, 60 and 120 lozenges.
Not all pack sizes may be marketed.
All presentations contain information on Nicabate and how to use it.

6.6 Special Precautions for Disposal

In Australia, any unused medicine or waste material should be disposed of in accordance with local requirements.

6.7 Physicochemical Properties

Chemical structure.


CAS number.

54-11-5.

7 Medicine Schedule (Poisons Standard)

Unscheduled.

Summary Table of Changes