Nicotine

Indications
Buccal
Smoking cessation
Adult: Chewing gum: Smokers of > 20 cigarettes/day: Start with 4 mg gum (chewed slowly and parked on the gum)over 30 min when the urge to smoke occurs; reduce to 2 mg gum when able. Smokers of ≤ 20 cigarettes/day: Start with 2 mg gum. Not more than 15 pieces of either strength daily. Lozenges: Initially, 1 every 1-2 hr; max daily dose 30 mg (i.e. 15 x 2 mg lozenges or 30 x 1 mg lozenges). Sublingual tablets (each tab is equivalent to 2 mg of nicotine as β-cyclodextrin complex): 1-2 tab/hr, max 40 tab daily if necessary. Reduce usage of nicotine replacement therapy gradually until no longer needed.
Buccal
Smoking cessation
Adult: 2 mg or 4 mg gum: Chew (and park on the gum) one piece when urge to smoke occurs between smoking episodes; reduce smoking within 6 wk and attempt smoking cessation within 6 mth.
Nasal
Smoking cessation
Adult: Nasal spray: 1 spray of 500 mcg administered into each nostril as required. Max use twice hrly and 64 sprays daily. Reduce usage gradually until no longer needed.
Transdermal
Smoking cessation
Adult: 1 patch for 16 or 24 hr daily applied to dry, hair free skin on the hip, trunk or upper arm. Site patch on a different area each day, leaving several days before using area again. Start with the highest strength (21 mg/24 hr or 15 mg/16 hr) and reduce gradually over several wk to lower strengths (14 mg/24 hr or 10 mg/16 hr then 7 mg/24 hr or 5 mg/16 hr). Lighter smokers may start with the lower strength patches.
Inhalation
Smoking cessation
Adult: Inhalator with 10 mg/cartridge nicotine: Inhale when urge to smoke occurs. Initial use of 6-12 cartridges daily, reduced gradually until no longer needed.
Inhalation
Smoking cessation
Adult: Inhalator with 10 mg/cartridge nicotine: Inhale when urge to smoke occurs between smoking episodes; reduce smoking within 6 wk and attempt smoking cessation within 6 mth.
Contraindications
Nonsmokers, children and occasional smokers. Recent cerebrovascular accident, acute MI, unstable or worsening angina pectoris, severe cardiac arrhythmias, active temporomandibular joint disease (gum).
Warnings / Precautions
Use with caution in oropharyngeal inflammation and in patients with cerebrovascular disease, heart failure and renal impairment. History of oesophagitis, peptic ulcer, CV disease, hyperthyroidism, hepatic dysfunction; myasthenia gravis; DM (monitor blood glucose concentrations); pregnancy, lactation; peripheral vascular disease; skin disease (should not be applied on broken skin).
Adverse Reactions
Headache, cold and flu-like symptoms; insomnia; nausea; myalgia and dizziness; palpitations; dyspepsia, hiccups; vivid dreams; chest pain; anxiety and irritability; somnolence and impaired concentration; abnormal hunger; dysmenorrhoea; rash. Patches: Skin reactions (discontinue if severe), vasculitis. Spray: Nasal irritation, nose bleeds, watery eyes, ear sensations. Gum, lozenges, SL tab or inhalator: Apthous ulceration, throat irritation. Inhalator: Cough, rhinitis, pharyngitis, stomatitis, sinusitis, dry mouth.
Overdose Reactions
Characterised by initial stimulation followed by depression of the autonomic nervous system. Symptoms include burning of mouth and throat, nausea and salivation, abdominal pain, vomiting, diarrhoea, hypertension or hypotension, headache, convulsions, dizziness, confusion, dyspnoea, faintness and sweating. Severe overdose may result in respiratory failure and death. If nicotine was taken orally, gastric lavage and activated charcoal may be used. Treatment is supportive; atropine may be used to reduce features of parasympathomimetic stimulation.
Drug Interactions
Nicotine increases the haemodynamic and AV blocking effects of adenosine. Monitor for treatment-emergent hypertension in patients treated with combination of nicotine patch and bupropion. Smoking cessation may increase response to various drugs e.g. theophylline, imipramine, oxazepam, pentazocine, some β-blockers; monitor for increased toxicity.
See Below for More nicotine Drug Interactions
Food Interactions
Acidic foods/beverages decrease absorption of nicotine.
Mechanism of Actions
Nicotine is a potent ganglionic and CNS stimulant. It paralyses all autonomic ganglia after stimulation of the respiratory system (a central effect of small doses). Larger doses produce medullary-type convulsions then paralysis. The actions of nicotine are mediated via nicotine-specific receptors.
Onset: Formulation specific.
Duration: Formulation specific.
Distribution: Crosses the placenta and present in breast milk.
Metabolism: Metabolised principally in the liver via oxidation.
Excretion: Excreted in the urine (10-20% as unchanged drug). Excretion is pH dependant with increased excretion in acidic urine.
Administration
Loz: May be taken with or without food. (Suck until the taste becomes strong. Then, lodge the loz between the gum & cheek. When the taste fades, start sucking it again. Repeat until the loz completely dissolves (about 30 min). Do not swallow. Avoid coffee, acidic drinks or soft drinks for 15 min prior to sucking the loz.)
Gum: May be taken with or without food. (Chew gum until the taste becomes strong, then rest it between the gums & the cheek. When the taste fades, start chewing it again. Repeat the chewing routine for 30 min.)
ATC Classification
N07BA01 - nicotine ; Belongs to the class of drugs used in the management of nicotine dependence.
Available As
  • Nicotine 1 mg
  • Nicotine 2 mg
  • Nicotine 4 mg
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