Pharmacology of nicotine: addiction and therapeutics

Annu Rev Pharmacol Toxicol. 1996:36:597-613. doi: 10.1146/


Nicotine maintains tobacco addiction and has therapeutic utility to aid smoking cessation and possibly to treat other medical diseases. Nicotine acts on nicotinic cholinergic receptors, which demonstrate diversity in subunit structure, function, and distribution within the nervous system, presumably mediating the complex actions of nicotine described in tobacco users. The effects of nicotine in people are influenced by the rate and route of dosing and by the development of tolerance. The metabolism of nicotine is now well characterized in humans. A few individuals with deficient C-oxidation of nicotine, unusually slow metabolism of nicotine, and little generation of cotinine have been described. Nicotine affects most organ systems in the body, although its contribution to smoking-related disease is still unclear. Nicotine as a medication is currently available as a gum, a transdermal delivery device, and a nasal spray, all of which are used for smoking cessation. Nicotine is also being investigated for therapy of ulcerative colitis, Alzheimer's disease, Parkinson's disease, Tourette's syndrome, sleep apnea, and attention deficit disorder.

Publication types

  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • Administration, Cutaneous
  • Administration, Intranasal
  • Animals
  • Cotinine / metabolism
  • Dose-Response Relationship, Drug
  • Drug Tolerance
  • Ganglionic Stimulants / administration & dosage
  • Ganglionic Stimulants / adverse effects*
  • Ganglionic Stimulants / pharmacokinetics
  • Ganglionic Stimulants / therapeutic use
  • Humans
  • Nicotine / administration & dosage
  • Nicotine / adverse effects*
  • Nicotine / pharmacokinetics
  • Nicotine / therapeutic use
  • Smoking / adverse effects
  • Smoking / physiopathology
  • Substance-Related Disorders / drug therapy*
  • Substance-Related Disorders / therapy


  • Ganglionic Stimulants
  • Nicotine
  • Cotinine