Nicotine


Thông tin thuốc gốc
Chỉ định và Liều dùng
Buccal
Smoking cessation aid
Adult: As chewing gum containing 2mg or 4 mg nicotine polacrilex: Smokers of ≤20 cigarettes daily: Start w/ 2 mg chewed slowly and parked between cheek and gum over 30 min when urge to smoke occurs. Smokers of >20 cigarettes daily: Start w/ 4 mg. Max: 15 gums daily. As lozenge containing 1, 1.5, 2 or 4 mg nicotine polacrilex or tartrate: Initially, 1 loz 1-2 hrly allowing to slowly dissolve for 20-30 min. Usual dose: 8-12 loz daily. Max: 30 loz (1-mg strength) or 15 loz (higher strengths) daily. Continue treatment for up to 3 mth, then withdraw gradually.
Child: 12-18 yr Same as adult dose.

Inhalation/Respiratory
Smoking cessation aid
Adult: As cartridge containing 10 mg: Initially, 6-16 cartridges daily for 12 wk and reduced gradually over a further 4-12 wk.
Child: 12-18 yr Same as adult dose.

Nasal
Smoking cessation aid
Adult: As soln containing 0.5 mg/spray: 1 spray into each nostril 2 times hrly. Max: 32 mg (64 sprays) daily for first 8 wk and reduced gradually. Treatment should be limited to 3 mth.
Child: 12-18 yr Same as adult dose.

Sublingual
Smoking cessation aid
Adult: As tab containing 2 mg nicotine β-cyclodextrin complex: 1-2 tab hrly, increased as necessary. Max: 40 tab daily. Continue treatment for up to 3 mth, then withdraw gradually.
Child: 12-18 yr Same as adult dose.

Transdermal
Smoking cessation aid
Adult: Smokers of ≤10 cigarettes daily: Start w/ 14 mg daily for 6 wk, then reduce to 7 mg daily for 2 wk. Smokers of >10 cigarettes daily: Start w/ 21 mg daily for 6 wk, then reduce to 14 mg daily for 2 wk; finish w/ 7 mg daily for 2 wk. Apply patch for 16 or 24 hr daily to dry, clean, and hairless skin on the hip, trunk, or upper arm. Place patch on different area each day allowing several days to elapse before using the same area.
Child: 12-18 yr Same as adult dose.
Cách dùng
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.
Chống chỉ định
Recent cerebrovascular accident. Self-medication in patients who will continue to smoke, chew tobacco, or use snuff or other nicotine-containing preparations. Non-smokers and occasional smokers.
Thận trọng
Patient w/ CV disease (e.g. MI, severe arrhythmia, unstable angina pectoris, CVA, uncontrolled HTN), peripheral vascular disease, endocrine disorder (e.g. phaeochromocytoma, hyperthyroidism, DM), peptic ulcer, and skin disease (patch). Hepatic and renal impairment. Childn. Pregnancy and Lactation.
Phản ứng phụ
Nausea, vomiting, abdominal pain, diarrhoea, headache, dizziness, hiccups, flu-like symptoms, palpitations, insomnia, vivid dreams, myalgia, chest pain, anxiety, irritability, somnolence, dysmenorrhoea; mouth (e.g. aphthous ulceration) and throat irritation; nasal irritation, epistaxis, lachrymation, salivation, swelling of the tongue (gum); unpleasant taste (loz); cough, rhinitis, stomatitis, sinusitis, dry mouth (inhalator); ear sensations (nasal spray); skin reactions (patch).
Inhalation/Respiratory/Nasal/SL/Transdermal: D
MonitoringParameters
Monitor cardiac status, vital signs and blood sugar levels.
Quá liều
Symptoms: Burning of the mouth and throat, nausea, vomiting, salivation, abdominal pain, diarrhoea, sweating, headache, dizziness, hearing and visual disturbances, weakness, confusion, syncope, prostration, dyspnoea, tachycardia, hypotension, rapid or weak or irregular pulse, seizure, resp failure, circulatory collapse, coma. Management: Symptomatic and supportive treatment. Artificial respiration is instituted if necessary. Employ activated charcoal to reduce GI absorption. For TTS, the skin should be washed w/ water w/o using soap and dried.
Tương tác
May enhance the haemodynamic effects of adenosine. Decreased metabolism leading to increased plasma concentrations w/ methoxsalen.
Food Interaction
Acidic beverages (e.g. coffee, juices, carbonated soft drinks) may inhibit buccal absorption of nicotine.
Tác dụng
Description: Nicotine, a pyridine alkaloid, is a stereo-selective nicotinic-cholinergic receptor agonist. Low doses cause an initial stimulation of autonomic ganglia, adrenal medulla, neuromuscular junction, and brain. High doses produce initial ganglionic stimulation followed by inhibition of neurotransmission leading to subsequent persistent depression of receptor activity.
Pharmacokinetics:
Absorption: Readily absorbed through mucous membranes and the skin. Time to peak plasma concentration: 4-15 min (intranasal); 15-30 min (oral inhalation); 25-30 min (gum); 2-10 hr (TTS).
Distribution: Widely distributed into most body tissues and fluids. Crosses blood-brain barrier and placenta; enters breast milk. Volume of distribution: Approx 2-3 L/kg. Plasma protein binding: 5-20%.
Metabolism: Metabolised mainly in the liver via CYP2A6 isoenzyme into cotinine and nicotine-N-oxide. Undergoes extensive first-pass metabolism.
Excretion: Via urine (approx 10-20% as unchanged drug). Elimination half-life: 1-2 hr (intranasal and oral inhalation); approx 4 hr (TTS).
Đặc tính

Chemical Structure Image
Nicotine

Source: National Center for Biotechnology Information. PubChem Database. Nicotine, CID=89594, https://pubchem.ncbi.nlm.nih.gov/compound/Nicotine (accessed on Jan. 22, 2020)

Bảo quản
Store below 25˚C. Protect from light and moisture.
Phân loại ATC
N07BA01 - nicotine ; Belongs to the class of drugs used in the management of nicotine dependence.
References
American Fare Nicotine Transdermal System - Nicotine Patch, Extended Release (Novartis Consumer Health, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 28/06/2016.

Anon. Nicotine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 28/06/2016.

Berkley and Jensen Nicotine Polacrilex Gum, Chewing (BJWC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 28/06/2016.

Berkley and Jensen Nicotine Polacrilex Lozenge (BJWC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 28/06/2016.

Buckingham R (ed). Nicotine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com . Accessed 28/06/2016.

Joint Formulary Committee. Nicotine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 12/08/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Nicotine. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 28/06/2016.

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