Nicotine information from DrugsUpdate
P - Caution when used during pregnancy
L - Caution when used during lactation
FI - Food *
Nicotine is an alkaloid found in the nightshade family of plants (Solanaceae) which constitutes approximately 0.6–3.0% of dry weight of tobacco, with biosynthesis taking place in the roots, and accumulating in the leaves. Nicotine, a main ingredient of tobacco products are mainly used for smoking cessation in adults. Nicotine is used either as Nicotine gums or lozenges. Using controlled levels of Nicotine can be helpful to lower Nicotine withdrawal symptoms while quitting cigarette smoking.
Pharmacodynamics
Nicotine exerts peripheral vasoconstriction, hypertension and tachycardia. Acute and chronic tolerance is reported with Nicotine use. Abrupt discontinuation of Nicotine products results in withdrawal symptoms including cigarette craving and behavioural changes.
Pharmacokinetics
Nicotine is mostly absorbed via the buccal mucosa, and the absorption rate depends on the route of administration such as cigarette smoking and inhalation. After IV administration, the Vss is approximately 3 L/kg, and the plasma protein binding rate is less than 5%. The drug is metabolized by liver, lungs and kidneys. More than 20 metabolites are identified and are biological less active. About 10% is excreted via the urine as unchanged drug. The terminal half-life of Nicotine is 1-2 hours.
Nicotine Indications / Nicotine Uses
Information Not Available
Nicotine Adverse Reactions / Nicotine Side Effects
Headache, cold & flu- like symptoms; insomnia; nausea; myalgia & dizziness; palpitations; dyspecia, hiccups; vivid dreams; chest pain; anxiety & irritability; somnolence & impaired concentration; abnormal hunger; dysmenorrhoea; rash.
Patches
Skin reactions (discontinue if severe vasculities)
Spray
Nasal irritations. nose bleeds, watery eyes, ear sensations.
Gum
Lozenges, SL tab or inhalator: Apthous ulceration, Throat irritation.
Inhalator
Cough, Rhintis, pharyngtis, stomatitis, dry mouth.
Precautions
Nicotine is contraindicated in patients with COPD, asthma, GI ulcer, Raynaud’s syndrome, CAD, MI, arrhythmia, stroke, uncontrolled BP, thyroid disorders, oral problems, liver or renal disorders and pheochromocytoma.
Special Precautions
Use with caution in oropharyngeal inflammation & in patients with cerebrovascular disease, heart failure & renal impairment. History of oesophagitis, peptic ulcer, CV disease, hyperthyroidism, hepatic dysfunction, myasthenia gravis; DM (monitor blood glucose concentrations); peripheral vascular disease; skin disease (should not be applied on broken skin)
Other Drug Interactions
Nicotine increases the haemodynamic & AV blockig effects of adenosine. Monitor for treatment- emergent HTN in patients treated with combination of nicotine patch & bupropion. Smoking cessation may increase to various drugs e.g theophyllines, imipramine, oxazepam, pentazocine, some ß- blockers; monitor for increased toxicity. Nicotine can interact with propranolol, anti-histamines, imipramine, insulin, labetalol, oxazepam, isoproterenol, pentazocine, theophylline, varenicline and imipramine.
Other Interactions
Avoid smoking cigarettes while using Nicotine.
Contraindications
Dosage
Transdermal
Smoking Cessation
Adult: One patch for 16 or 24 hours hours 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 that area again. Start with the highest strength (21 mg/24 hours or 15 mg/16 hours) and reduce gradually over several weeks to lower strenghts (14mg/24 hours or 10 mg/16 hours then 7 mg/24 hours or 5mg/16 hours). Lighter smokers may start with the lower strength patches.
Nasal
Smoking Cessation
Adult: Nasal spray: 1 spray of 500 mcg administered into each nostril as required. Max use twice daily hourly or 64 sprays daily. Reduce usage gradually until no longer needed.
Inhalation
Smoking Cessation
Adult: Inhalator with 10 mg/catridge nicotine: Inhale when urge to smoke occurs. Initial use of 6-12 catridges daily, reduced gradually until no longer needed.
Reduction of smoking:
Adult: Inhalator with 10 mg/catridge nicotine: Inhale when urge to smoke occurs between smoking within 6 weeks & attempt smoking cessation with 6 months.
Buccal
Smoking Cessation
Adult: Chewing gum: Smokers of > 20 cigarrettes/day: Start with 4mg gum (chewed slowly and parked on the gum) over 30 minutes when the urge to smoke occurs; reduce to 2mg gum when able. Smokers of ≤ 20 cigarettes/ day: Start with 2mg gum. Not more than 15 pieces of either strength. Lozenges: Initially 1 every 1-2 hours; max daily dose 30mg (i.e 15 x 2 mg loz or 30 x 1 mg lozenges)
Sublingual tab (each tab is equiv to 2 mg of nicotine as ß- cyclodextrin complex)
1-2 tab/hr, max 40 tab daily if necesary. Reduce usage of NRT gradually until no longer needed.
Reduction of smoking:
Adult 2mg or 4mg gum: Chew (and park on the gum) one piece when urge to smoke occurs between smoking episodes; reduce smoking within 6 weeks and attempt smoking cessation within six months.
Food(before/after)
Information Not Available
List of Contraindications
Nicotine and Pregnancy
Contraindicated in pregnancy
USFDA pregnancy category D. Nicotine can harm the unborn fetus. Perform pregnancy tests before using Nicotine. Use effective contraceptive modes to prevent unintended pregnancies while taking Nicotine. Cigarette smoking during gestation can cause low birth weight, stillbirth or abortion.
Nicotine and Lactation
Nicotine alternatives should be considered while breastfeeding a baby. Nursing mothers should consult a physician before using Nicotine. However, Nicotine lozenges should not be used as it contains phenylalanine.
Nicotine and Children
Safety and efficacy not established
Nicotine and Geriatic
May be more susceptible to adverse reactions
Nicotine and Other Contraindications
Non- smokers, child & occasional smokers. Recent cerebrovascular accident, acute MI, unstable or worsening angina pectoris, severe cardiac arrhythmias, active temporomandibular joint disease (gum)
Storage
Inhalation System
Store cartridge at 77°F or below. Protect from light.
Lozenge
Store at controlled room temperature (68° to 77°F). Protect from light.
Nicotine Chewing Gum
Store at controlled room temperature (68° to 77°F). Protect from light.
Transdermal System
Store at controlled room temperature (68° to 77°F). Do not store out of pouch.
Lab interference
Inhalation System
Store cartridge at 77°F or below. Protect from light.
Lozenge
Store at controlled room temperature (68° to 77°F). Protect from light.
Nicotine Chewing Gum
Store at controlled room temperature (68° to 77°F). Protect from light.
Transdermal System
Store at controlled room temperature (68° to 77°F). Do not store out of pouch.
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