Neuropharmacology: Caffeine

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Lecture 13 from a college level neuropharmacology course taught in the spring 2012 semester by Brian J. Piper, Ph.D. (psy391@gmail.com) at Willamette University. Includes pharmacokinetics and pharmacodynamics.

Text of Neuropharmacology: Caffeine

  • 1. CaffeineBrian J. Piper, Ph.D.
  • 2. Goals Structure of different xanthines Pharmacokinetics Psychological and Physiological Effects Pharmacodynamicshttp://en.wikipedia.org/wiki/Caffeine
  • 3. Coffea aribica Coffea robusta Botany Coffea aribica: grown in Brazil, 10 m tall, 7 years to mature Coffea robusta (Coffea canephora): grown in Vietnam, < 1 year to mature, 2 x caffeine Camellia sinensis: grown in China, 2 m tall, leaves = 4% caffeine Theobroma cacoa: grown in Mexico, 6 m tall, contains theobromine, dogs Theobroma cacao Camellia sinensis http://en.wikipedia.org/wiki/Camellia_sinensis http://www.ico.org/botanical.asp
  • 4. Structure Xanthine: group of mild stimulants, Xanthine forms backbone Methly Group: a Carbon & 3 Hydrogens (CH3) Theobromine: Xanthine + two methyl groups (3,7) Theophylline: Xanthine + two methyl groups (1,3) Caffeine: Xanthine + three methyl groups (1,3,7)
  • 5. Structure Caffeine: Xanthine + three methyl groups (1,3,7) CYP1A2: removes methyl groups
  • 6. Energy Drinks Serving Size Caffeine (mg) (oz.)Spike Shooter 8.4 300Cocaine 8.4 280Monster Energy 16 160Full Throttle 16 144Rip It, all varieties 8 100Enviga 12 100Tab Energy 10.5 95SoBe 8 83Red Bull Sugarfree 8.3 80Rockstar Energy Drink 8 80SoBe Adrenaline Rush 8.3 79Amp 8.4 74Glaceau Vitamin Water Energy Citrus 20 50SoBe Essential Energy, Berry or Orange 8 48 http://www.cspinet.org/new/cafchart.htm Accessed 3/15/08
  • 7. http://anrcatalog.ucdavis.edu/pdf/8265.pdf
  • 8. Seizures? Rats that were genetically prone to convulsions received different doses (umol/kg) of methylxanthines. Behavior was rated for 6 hours: 0 = no response 2 = tremor 4 = forelimb clonus 6 = falling down 8 = tonic-clonic seizures/death *Clonus (Gr: violent, confused motion), large involontary movementsDe Sarro et al. (1997) Naunyn-Schmiedebergs Arch Pharmacol, 356, 48-55.
  • 9. Seizures? Rats that were genetically prone to convulsions received different doses (umol/kg) of methylxanthines. *Clonus (Gr: violent, confused motion), large involontary movementsDe Sarro et al. (1997) Naunyn-Schmiedebergs Arch Pharmacol, 356, 48-55.
  • 10. Sex Differences in Caffeine PK