Pharmacotherapy

Pharmacotherapy 1 v2

This section provides a brief summary of information on pharmacotherapy options to assist with smoking cessation.

The information sources included the British National Formulary (BNF), individual Specific Product Characteristics, Medicines and Healthcare products Regulatory Authority (MHRA) and WeMeReC Bulletin on smoking cessation (2009).

Clinicians are advised to refer to the latest updates of individual Specific Product Characteristics for full prescribing information (e-medicines compendium website), and the latest edition of the BNF (BNF website) and MHRA advice (MHRA website) for guidance.

Click here to view the WeMeReC Bulletin on smoking cessation (2009)

NOTE: Stop Smoking Wales Advisors do not prescribe or supply stop smoking medication to clients, nor do they have access to patients’ medical records.

Nicotine Replacement Therapy (NRT)

NRT can be used in place of cigarettes after abrupt cessation of smoking, or alternatively to reduce the amount of cigarettes used in advance of a quit attempt (BNF Number 61, 2011).

NRT can also be used to minimise second-hand smoking and to treat cravings and reduce compensatory smoking after enforced abstinence in smoke-free environments (BNF Number 61, 2011).

Nicotine delivery from NRT is at a lower dose and slower rate compared with smoking. There are many different NRT preparations available in a range of strengths. This offers a variety of approaches to tailoring NRT for individuals.

NRT preparations currently available include: transdermal patches, gums, a nasal spray, an inhalator, sublingual tablets and lozenges. Patches provide slower, sustained release of nicotine whilst oral and nasal forms provide fast release of nicotine. NRT can be bought over the counter or it can be prescribed.

Advantages and disadvantages of different NRT preparations

NRT preparation Advantages and disadvantages
Patch
  • Discreet and easy to use
  • Sustained release can provide extended coverage
  • May help with early morning cravings
  • 24 hour patches may disturb sleep
  • Does not mimic the highs and lows associated with nicotine
Gum
  • Allows good control of nicotine dose
  • Some people do not like the taste
  • Unsuitable for people with dentures
Nasal spray
  • Fast acting, rapid delivery of nicotine similar to cigarettes
  • Good for heavy smokers
  • Can cause nose and throat irritation, coughing, and watering eyes
Inhalator
  • Good for people who miss the ritual of smoking
Sublingual tablet
  • Discreet and flexible, good control
  • Nicotine is absorbed through the lining of the mouth, offering good control
Lozenge
  • Discreet and flexible, good control
  • Nicotine is absorbed through the lining of the mouth, offering good control

Combination NRT therapy

A combination of NRT products has been shown to have a moderate advantage over using a single product. For example, patches may be combined with one of the oral products (gum, sublingual tablet or inhalator). Use of combination therapy may be considered for patients with a high level of nicotine dependence or who have found single forms of NRT inadequate in the past. Combination therapy should not be offered as routine practice to all smokers.

Special population groups

NRT is licensed for use by the following population groups, but should be discussed with the GP/pharmacist before starting treatment:

  • Pregnant women
  • Breast feeding mothers
  • Young people aged 12 – 18 years

NOTE: Stop Smoking Wales clients interested in using NRT to assist them in their quit attempt are advised to consult their GP or pharmacist.

Varenicline

Varenicline is a selective nicotine-receptor partial agonist used to assist with smoking cessation. It may reduce the craving and reward of smoking, and may also decrease nicotine withdrawal symptoms when attempting to stop smoking.

Varenicline was launched in the UK in December 2006 and is a prescription-only medicine. As it is relatively new; information about the use of varenicline in the general population is limited. Clinicians and patients are encouraged to report any side effects thought to be associated with varenicline use to the MHRA via the Yellow Card scheme.

The combination of varenicline with NRT or bupropion is unlicensed and is not recommended.

NOTE: Stop Smoking Wales clients interested in using varenicline to assist them in their quit attempt are advised to consult their GP.

Bupropion

Bupropion has been used as an antidepressant but its mode of action in smoking cessation is not clear. It may involve an effect on noradrenaline and dopamine neurotransmission resulting in a reduction in craving and withdrawal symptoms.

The combination of bupropion with NRT or varenicline is unlicensed and is not recommended.

NOTE: Stop Smoking Wales clients interested in using bupropion to assist them in their quit attempt are advised to consult their GP.

Comparison of pharmacotherapy treatment options for smoking cessation

Pharmacotherapy treatment options for smoking cessation
 

NRT

Varenicline

Bupropion

Pharmaceutical form

 

Transdermal patches

Gum

Nasal spray

Inhalator

Tablet

Lozenges

Film-coated tablets

Prolonged-release film coated tablets

Treatment duration

10 to 12 weeks

Transdermal patches

12 weeks

7 to 9 weeks

Licensed age groups(s)

Adults and children over 12 years

Adults over 18 years

Adults over 18 years

Use in pregnancy

  • Use only if smoking cessation without NRT fails
  • Intermittent NRT is preferable over patches but avoid liquorice-flavoured NRT products
  • Patches may be useful in pregnancy-related nausea and vomiting
  • If patches are used they should be removed before going to bed

Not licensed – avoid

Not licensed – avoid

Use in breast-feeding

Intermittent NRT is preferred

Not licensed – avoid

  • Not licensed – avoid
  • Present in breast-milk

Contraindications

Known hypersensitivity to nicotine or any component of the formulation

Known hypersensitivity to varenicline or any component of the formulation

  • Known hypersensitivity to bupropion or any component of the formulation
  • Acute alcohol or benzodiazepine withdrawal
  • Severe hepatic cirrhosis
  • CNS tumour
  • History of seizure, eating disorders, or bipolar disorder

Cautions

  • Haemodynamically unstable patients hospitalised with severe arrhythmias, MI or CVA
  • Phaeochromocytoma
  • Uncontrolled hyperthyroidism
  • Diabetes: monitor blood-glucose concentration closely when starting treatment
  • Specific cautions for particular forms of NRT are usually related to the local effect of nicotine
  • Risk of relapse, irritability, depression, and insomnia on discontinuation (Consider dose tapering on completion of 12 week course)
  • History of psychiatric illness (may exacerbate underlying illness including depression)
  • Elderly
  • Predisposition to seizures including concomitant use of medicines that lower seizure threshold
  • Alcohol misuse
  • History of head trauma or diabetes
  • Measure blood pressure before and during treatment

Adverse effects

  • Not generally serious and often similar to some of those caused by smoking. Usually improve over time.
  • Effects include nausea, indigestion, dizziness, headache, cold and flu-like symptoms, dry mouth rash and less frequently, palpitations.
  • Specific effects observed with different presentations, for example, sleep disturbance and skin reactions with 24 hour patches, mucosal irritation with nasal or oral preparations.
  • The most commonly reported side-effect is nausea. It is generally mild to moderate in severity and occurs early in treatment.
  • Also commonly reported are headaches, abnormal dreams and insomnia.
  • Depression, suicidal ideation and behaviour, and suicide attempts have been reported with varenicline.
  • Clinicians should be aware of the possible development of these symptoms in patients attempting to stop smoking.
  • Varenicline should be stopped immediately if agitation, depressed mood, or changes in behaviour are observed.
  • Care should be taken in patients with a history of psychiatric illness.
  • Stopping varenicline is associated with an increase in irritability, urge to smoke, depression, and/or insomnia. Dose tapering at the end of treatment may help to prevent this.
  • Bupropion is associated with a dose-related risk of seizures.
  • Bupropion commonly causes insomnia.
  • Hypertension has been reported in patients taking bupropion.
  • Cases of suicidal ideation and behaviour have been reported with bupropion.
  • Clinicians should be aware of the possible development of these symptoms in patients attempting to stop smoking.

Interactions

No clinically relevant interactions between NRT and other medication.

However nicotine may possibly enhance the effects of the antiarrhythmic adenosine.

No clinically relevant interactions between varenicline and other medication.

Bupropion inhibits the cytochrome P450 CYP2DB6 enzyme pathway and so certain antidepressants, antipsychotics, beta-blockers, and antiarrhythmics should be prescribed at the lower end of the recommended dose ranges in patients taking bupropion.

If a patient is already taking such a medicine, then the need to reduce the dose of that medicine should be considered if bupropion is to be started. The expected benefits must be weighed against potential risks.

Bupropion is metabolised by CYP2B6 . Medication that affects CYP2B6 may result in altered levels of bupropion and its metabolites (e.g. cyclophosphamide, orphenadrine, clopidogrel). Clinical effects not known but monitoring advised.

Clinical effects of bupropion may be altered by medication that inhibit (for example, valproate) or induce (for example, carbamazepine, phenytoin) it metabolism.

Nicotine withdrawal

Stopping smoking (with or without the use of smoking cessation aids) may cause symptoms of depression, irritability, anger, insomnia, anxiety, difficulty concentrating, restlessness and weight gain.

Whilst any of these symptoms may be experienced during a quit attempt assisted by pharmacotherapy, it is important to remember that they may not have been caused by that particular medicine. They may relate to other factors such as nicotine withdrawal from stopping smoking, other illnesses, or other medication taken at the same time (MHRA, 2011).

Smoking and concomitant medication

Cigarette smoking increases the metabolism of some medicines by stimulating the hepatic enzyme CYP1A2. When smoking is discontinued, the dose of these drugs, in particular theophyllinecinacalcetropinirole, and some antipsychotics (including clozapine,olanzapinechlorpromazine, and haloperidol), may need to be reduced. Regular monitoring for adverse effects is advised (BNF Number 61, 2011; North West Medicines Information Centre, 2010).


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