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Pharmacology of Nicotine

Pharmacology of Nicotine. Colleen Miller Lesley-Ann Giddings. What is nicotine?. plant alkaloid derived from nicotinic acid. http://www.scs.leeds.ac.uk/cgi-bin/pfaf/arr_html?Nicotiana+tabacum. How does nicotine act on receptors?. nicotinic acetylcholine receptors

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Pharmacology of Nicotine

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  1. Pharmacology of Nicotine Colleen Miller Lesley-Ann Giddings Downloaded from www.pharmacy123.blogfa.com

  2. What is nicotine? • plant alkaloid • derived from nicotinic acid Downloaded from www.pharmacy123.blogfa.com http://www.scs.leeds.ac.uk/cgi-bin/pfaf/arr_html?Nicotiana+tabacum

  3. How does nicotine act on receptors? • nicotinic acetylcholine receptors • mimics acetylcholine (agonist) • opens ion channel • depolarizes Downloaded from www.pharmacy123.blogfa.com

  4. Nicotine and Acetylcholine Downloaded from www.pharmacy123.blogfa.com http://www.biomedcentral.com/1472-6807/2/1

  5. Releases ACh, NE, DA, S, glutamate, and GABA Downloaded from www.pharmacy123.blogfa.com

  6. Effects of Nicotine Positive: Anxiolysis Cognitive Enhancement Cerebro-vasodilation Neuroprotection Analgesia Anti-psychotic Negative: Gastrointestinal Distress Hypothermia Emesis Hypertension Seizures Respiratory Distress Downloaded from www.pharmacy123.blogfa.com

  7. Nicotine Administration • Inhalation • Cigarettes (~1.0 mg) • Inhaler • Nasal • Nasal spray • Oral • Gum • Lozenges • Tablets • Transdermal • Patch Downloaded from www.pharmacy123.blogfa.com

  8. Chemistry of Nicotine • basic compound • water soluble • lipophilic • environments: • no absorption in acidic environments • functions at blood pH = 7.4 (31%) • absorption occurs readily in basic environments Downloaded from www.pharmacy123.blogfa.com

  9. Pharmacokinetics • Inhalation of nicotine is the most addictive Downloaded from www.pharmacy123.blogfa.com

  10. Addiction via smoking • cigarettes have additives that cause addiction • sensory cues (heat, sight, and smell) • smokers have greater number of nicotinic receptors • inhalation from cigarettes causes nicotine to cross blood brain barrier more rapidly Downloaded from www.pharmacy123.blogfa.com

  11. Nicotine absorption from cigarettes • Readily absorbed through oral and nasal mucous membrane • basic pipe or cigar smoke leads to rapid increases in nicotine without inhalation • flue-cured cigarettes are acidic • little buccal absorption • need to absorb nicotine through inhalation Downloaded from www.pharmacy123.blogfa.com

  12. Absorption through Inhalation • absorption through the surface of alveolar capillary interface • absorption into the pulmonary capillary blood flow • circulates throughout entire blood volume Downloaded from www.pharmacy123.blogfa.com http://sln.fi.edu/biosci/systems/pulmonary.html

  13. Buccal Absorption • Absorbed in small intestine • Carried to blood • Undergoes pre-systemic metabolism by liver • 30-40% bioavailability Downloaded from www.pharmacy123.blogfa.com

  14. Elimination • First order • Half-life averages 2 hours • Metabolized in liver, lung and kidney Downloaded from www.pharmacy123.blogfa.com

  15. How is nicotine eliminated? • P-450 and aldehyde oxidase enzymes in liver Downloaded from www.pharmacy123.blogfa.com

  16. Therapeutic Opportunities • Cognitive Dysfunction/ Attention Disorders • Neurodegenerative disorders (Alzheimers, Parkinsons) • Pain • Schizophrenia • Depression Downloaded from www.pharmacy123.blogfa.com

  17. Epilepsy • Tourette’s Syndrome • ADHD • Anxiety • Vestibular Function • Gastric Disorders Downloaded from www.pharmacy123.blogfa.com

  18. And the take home message is… • The pharmacokinetics are important for determining addictive potential of nicotine • Inhalation of nicotine is the most addictive form of uptake • There are many therapeutic opportunities to be developed Downloaded from www.pharmacy123.blogfa.com

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