Nicotine

Registered South African indications:

• Treatment of tobacco dependence in adults by relief of nicotine withdrawal symptoms, including cravings, during a quit attempt (Permanent cessation of tobacco use is the eventual objective)
  - Should preferably be used in conjunction with a behavioural support program

Registered South African contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Children under the age of 18 years
• Those who have never smoked

Caution recommended in the following patient groups

• Pregnancy
• Breastfeeding
• Severe renal impairment
• Moderate to severe hepatic impairment

Non-smokers

• Nicotine oromucosal spray should not be used by individuals who do not currently smoke

Cardiovascular disease

• Use with caution and under medical supervision in patients with recent myocardial infarction, unstable angina, Prinzmetal’s angina, severe dysrhythmias, recent stroke, or uncontrolled hypertension
• These patients should be encouraged to stop smoking with non-pharmacological interventions (such as counselling). If this fails, nicotine oromucosal spray may be considered, but as data on safety in this patient group are limited, initiation should only be under close medical supervision

Diabetes mellitus

• Monitor blood glucose levels more frequently upon initiation as reduced nicotine-induced catecholamine release can affect carbohydrate metabolism

Allergic reactions

• Caution is advised for individuals susceptible to angioedema and urticaria

Renal and hepatic impairment

• Use with caution in patients with moderate to severe hepatic impairment or severe renal impairment due to potential decreased clearance of nicotine and its metabolites

Pheochromocytoma and uncontrolled hyperthyroidism

• Caution is required as nicotine-induced catecholamine release may exacerbate these conditions

Gastrointestinal (GI) disease

• Swallowed nicotine may worsen symptoms of oesophagitis, gastritis, or peptic ulcers

Seizures

• The risk-benefit ratio should be carefully evaluated in patients with a history of epilepsy, as convulsions have been reported in association with nicotine

Danger in children

• Nicotine doses tolerated by adults can cause fatal toxicity in small children; ensure the product is stored out of their reach and sight to prevent accidental ingestion or misuse

Transferred dependence

• There is a minor risk of transferred dependence, though it is generally less harmful and easier to break than smoking tobacco

Stopping smoking (drug metabolism)

• Cessation may slow the metabolism of drugs processed by CYP1A2 (e.g., clozapine, theophylline, ropinirole), leading to increased plasma concentrations and potential toxicity

Excipients and Administration

• Contains butylated hydroxytoluene, which may cause local skin or mucosal irritation
• Care must be taken to avoid contact with the eyes during administration

Effects on ability to drive and use machines

• Nicotine oromucosal spray has no or negligible influence on the ability to drive and use machines

Forms avail. in SA and covered in this monograph: spo

South African registered indications and dosages

Treatment of tobacco dependence in adults by relief of nicotine withdrawal symptoms, including cravings, during a quit attempt
(Permanent cessation of tobacco use is the eventual objective)
- Should preferably be used in conjunction with a behavioural support program

Dosing Summary

• Oral (spo): Recommended usage schedule Step 1 (during full treatment) and Step 2-3 (during tapering) is highlighted below; Up to 4 sprays/hr may be used; Max. sprays: 2 sprays per dose episode AND 64 sprays (4 sprays/hr, over 16hrs)/24hrs

Step 1: Weeks 1-6

• Oral (spo): 1-2 sprays at times when cigarettes normally would have been smoked or if cravings emerge; If after a single spray, cravings are not controlled within a few minutes: A second spray should be used; If 2 sprays are required, future doses may be delivered as 2 consecutive sprays; Most smokers will require 1-2 sprays, every 30mins to 1hr

Step 2: Weeks 7-9

• Oral (spo): Start reducing the number of sprays per day; By the end of week 9, patients should be using HALF the average number of sprays per day that was used in Step 1

Step 3: Weeks 10-12

• Oral (spo): Continue reducing the number of sprays per day so that patients are not using more than 4 sprays/day during week 12. When patients have reduced to 2-4 sprays per day, oromucosal spray use should be discontinued

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Patients should stop smoking completely during the course of treatment with nicotine oromucosal spray

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Example: If an average of 15 cigarettes per day are usually smoked, 1-2 sprays should be used at least 15 times during the day

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To help stay smoke-free after Step 3, patients may continue to use the nicotine oromucosal spray in situations when they are strongly tempted to smoke. One spray may be used in situations where there is an urge to smoke, with a second spray if one spray does not help within a few minutes. No more than 4 sprays per day should be used during this period. Regular use of nicotine oromucosal spray beyond 6 months is generally not recommended

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Some ex-smokers may need treatment with nicotine oromucosal spray longer to avoid returning to smoking. Any remaining nicotine spray should be retained to be used in the event of sudden cravings

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Patients should not eat or drink when administering the nicotine oromucosal spray

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Behavioural therapy advice and support will normally improve the success rate

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See Additional Prescribing Points for method of administration

Not established for use in children below 18 years (see Contraindications)

Pregnancy

South African recommendations

• Caution; not recommended
• 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
• Nicotine passes to the foetus and affects its breathing movements and circulation. The effect on the circulation is dose dependent. Therefore, the pregnant smoker should always be advised to stop smoking completely without use of nicotine replacement therapy
• The risk of continued smoking may pose greater hazard to the foetus as compared with the use of nicotine replacement products in a supervised smoking cessation programme. The use of a nicotine oromucosal spray by the pregnant smoker should only be initiated after advice from a health care provider

Women of childbearing potential/ contraception in males and females

• In contrast to the well-known adverse effects of tobacco smoking on human conception and pregnancy, the effects of therapeutic nicotine treatment are unknown
• Thus, whilst to date no specific advice regarding the need for female contraception has been found to be necessary, the most prudent state for women intending to become pregnant is to be both non-smoking, and not using NRT
• Whilst smoking may have adverse effects on male fertility, no evidence exists that particular contraceptive measures are required during NRT treatment by males

Breastfeeding

South African recommendations

• Caution; not recommended
• Nicotine passes freely into breast milk in quantities that may affect the child even with therapeutic doses. Nicotine oromucosal spray should therefore be avoided during breastfeeding
• Should smoking cessation not be achieved, use of a nicotine oromucosal spray by breastfeeding smokers should only be initiated after advice from a healthcare professional
• Women should take the product just after having breastfed and leave as long a time as is possible (2 hours is suggested) between taking the mouth spray and the next feed

Fertility

South African recommendations

• Smoking increases the risk for infertility in women and men. In vitro studies have shown that nicotine can adversely affect human sperm quality. In rats, impaired sperm quality and reduced fertility has been shown

South African recommendations

• Mild to moderate: No dose adjustment recommended
• Severe: Caution; no dose adjustment recommended

South African recommendations

• Mild: No dose adjustment recommended
• Moderate to severe: Caution; no dose adjustment recommended

South African recommendations

• No dose adjustment recommended

Immune System Disorders

Frequent

• Hypersensitivity

Frequency unknown

• Allergic reactions including angioedema and anaphylaxis

Psychiatric Disorders

Less frequent

• Abnormal dreams

Nervous System Disorders

Frequent

• Headache
• Dysgeusia
• Paraesthesia

Frequency unknown

• Seizure

Eye Disorders

Less frequent

• Blurred vision
• Increased lacrimation

Cardiac Disorders

Less frequent

• Palpitations
• Tachycardia

Frequency unknown

• Atrial fibrillation

Vascular disorders

Less frequent

• Flushing
• Hypertension

Respiratory, Thoracic and Mediastinal Disorders

Frequent

• Hiccups
• Throat irritation

Less frequent

• Bronchospasm
• Rhinorrhoea
• Dysphonia
• Dyspnoea
• Nasal congestion
• Oropharyngeal pain
• Sneezing
• Throat tightness

Gastrointestinal Disorders

Frequent

• Nausea
• Abdominal pain
• Diarrhoea
• Dry mouth
• Dyspepsia
• Flatulence
• Salivary hypersecretion
• Stomatitis
• Vomiting

Less frequent

• Eructation
• Gingivitis
• Glossitis
• Oral mucosal blistering and exfoliation
• Oral paraesthesia
• Dysphagia
• Oral hypoesthesia
• Retching

Frequency unknown

• Dry throat
• Gastrointestinal discomfort
• Lip pain

Skin and Subcutaneous Tissue Disorders

Less frequent

• Hyperhidrosis
• Pruritus
• Rash
• Urticaria

Frequency unknown

• Erythema

General Disorders and Administration Site Conditions

Frequent

• Burning sensation
• Fatigue

Less frequent

• Asthenia
• Chest discomfort and pain
• Malaise

No significant interactions (see Additional Prescribing Points)

None routine. Specific cases may require

• Blood glucose (patients with diabetes mellitus)

Method of administration

• After priming, point the spray nozzle as close to the open mouth as possible
• Press firmly the top of the dispenser and release one spray into the mouth, avoiding the lips
• Subjects should not inhale while spraying to avoid getting spray into the respiratory tract
• For best results, do not swallow for a few seconds after spraying

Interaction with other medicines and other forms of interaction

• No clinically relevant interactions between nicotine replacement therapy and other medicines has definitely been established
• However, nicotine may possibly enhance the haemodynamic effects of adenosine, i.e. increase in blood pressure and heart rate and also increase pain response (angina-pectoris type chest pain) provoked by adenosine administration

Nicotine is an agonist at nicotine receptors in the peripheral and central nervous system and has pronounced CNS and cardiovascular effects. Abrupt cessation of the established, regular use of tobacco-containing products results in the characteristic syndrome, with withdrawal symptoms including cravings (urges to smoke). Clinical studies have shown that nicotine replacement products can help smokers abstain from smoking by raising blood nicotine levels and relieving these withdrawal symptoms.

Gum 2mg

• Nicorette (Johnson & Johnson) originator
• Nicorette Mint (Johnson & Johnson) originator

Gum 4mg

• Nicorette (Johnson & Johnson) originator
• Nicorette Mint (Johnson & Johnson) originator

Tablet sublingual 2mg

• Nicorette Microtab (Johnson & Johnson) originator

Patch 5mg

• Nicorette Transdermal Patch  (Johnson & Johnson) originator 

Patch 10mg

• Nicorette Transdermal Patch (Johnson & Johnson) originator 

Patch 15mg

• Nicorette Transdermal Patch  (Johnson & Johnson) originator

Patch 17,5mg/10cm²

• Nicotinell TTS 10 (GSK) originator

Patch 35mg/20cm²

• Nicotinell TTS 20  (GSK) originator

Patch 52.5mg/30cm²

• Nicotinell TTS 30  (Novartis) originator

Spray (per spray) 1:1.0mg, 2:0.66mg, 3:0.33mg, 4:0mg

• Quit 1/2/3/4 (Pharmacare)