Common Psychostimulants: Caffeine and Nicotine Sources Pharmacokinetics Pharmacodynamics Side effects
Pharmacology Xanthine derivatives or  methylxanthines Caffeine Theophylline Divine Leaf
Caffeine Most popular drug in the world “ Caffeine is useless since it serveth neither Nourishment nor Debauchery.” --Anonymous, 1650 Plants of 28 genera in 17 families Most common sources are coffee, tea, chocolate, and kola Coffea arabica  and  Coffea robusta
Pharmacokinetics Oral administration  Beverages: Coffee, tea, cocoa, chocolate milk, cola (fortified) Chocolate Complete absorption from GIT in 30-60 minutes Elimination half-life ranges from 3 to 10 hrs Accumulation Dosing  Longer late in pregnancy,  in utero , elderly  Concentrated in breast milk Shorter in smokers
Pharmacodynamics: Effects Cortex at normal doses (100-200 mg): Rewarding effect: Feel competent Alertness, sustained attention, faster thought Reduced fatigue, lower need for sleep Fine motor coordination, timing accuracy, and arithmetic may be impaired Heavy dosing (1.5 grams a day) may produce agitation, anxiety, tremors, panting, and insomnia
Medicinal Effects  OTC  Stimulants No-Doz 100mg/tab Vivarin 200mg/tab Analgesics Caffeine synergizes ASA Anacin 32 mg/tab Excedrin 64.8 mg/tab Diuretics and cold preparations Asthma products Bronchodilation
Cardiac Effects Indirect Stimulation of Catecholamines Epinephrine Elevated BP, HR Spinal cord stimulated at toxic doses (2 - 5 grams); cardiac arrhythmias at 10 - 20 grams Dilates coronary arteries; constricts cerebral arteries
Pharmacodynamic Mechanisms Caffeine and Theophylline  Block GABA receptors Stimulate calcium release with in the cells Blockade of adenosine receptors results in caffeine induced behavioral stimulation A normal dose blockades 50% of receptors Adenosine–  neuromodulator Adenosine is linked to sleep inducing effects Adenosine, and thus caffeine, act on NE, DA, ACh , glutamate, and GABA
Caffeinism Caffeine-induced disorders from DSM-IV Tolerance and Dependence Withdrawal effects due to increased adenosine receptor density and thus increased adenosine sensitivity High doses >1000mg/day Psychiatric effects
Conflicting data on reproductive effects May slow growth  in utero , especially high dose Caffeine may be harmful prior to conception May increase the risk of spontaneous abortion
How much caffeine? 5oz 5oz 5oz 1oz  1oz  12oz  Tab-  Anal-  Diur- Coffee Tea  Cocoa  Choc.  C.Milk  Cola  lets  gesics  etics
The REAL Thing – Coca-Cola Active ingredient is phosphoric acid.  pH of 2.8 Dissolves a nail in 4 days. Dissolves a tooth in 24-48 hours. Trucks carrying Coca Cola syrup (the concentrate) must use Hazardous Material placards. The distributor of Coke use it to clean the engines of their trucks.

Caffeine

  • 1.
    Common Psychostimulants: Caffeineand Nicotine Sources Pharmacokinetics Pharmacodynamics Side effects
  • 2.
    Pharmacology Xanthine derivativesor methylxanthines Caffeine Theophylline Divine Leaf
  • 3.
    Caffeine Most populardrug in the world “ Caffeine is useless since it serveth neither Nourishment nor Debauchery.” --Anonymous, 1650 Plants of 28 genera in 17 families Most common sources are coffee, tea, chocolate, and kola Coffea arabica and Coffea robusta
  • 4.
    Pharmacokinetics Oral administration Beverages: Coffee, tea, cocoa, chocolate milk, cola (fortified) Chocolate Complete absorption from GIT in 30-60 minutes Elimination half-life ranges from 3 to 10 hrs Accumulation Dosing Longer late in pregnancy, in utero , elderly Concentrated in breast milk Shorter in smokers
  • 5.
    Pharmacodynamics: Effects Cortexat normal doses (100-200 mg): Rewarding effect: Feel competent Alertness, sustained attention, faster thought Reduced fatigue, lower need for sleep Fine motor coordination, timing accuracy, and arithmetic may be impaired Heavy dosing (1.5 grams a day) may produce agitation, anxiety, tremors, panting, and insomnia
  • 6.
    Medicinal Effects OTC Stimulants No-Doz 100mg/tab Vivarin 200mg/tab Analgesics Caffeine synergizes ASA Anacin 32 mg/tab Excedrin 64.8 mg/tab Diuretics and cold preparations Asthma products Bronchodilation
  • 7.
    Cardiac Effects IndirectStimulation of Catecholamines Epinephrine Elevated BP, HR Spinal cord stimulated at toxic doses (2 - 5 grams); cardiac arrhythmias at 10 - 20 grams Dilates coronary arteries; constricts cerebral arteries
  • 8.
    Pharmacodynamic Mechanisms Caffeineand Theophylline Block GABA receptors Stimulate calcium release with in the cells Blockade of adenosine receptors results in caffeine induced behavioral stimulation A normal dose blockades 50% of receptors Adenosine– neuromodulator Adenosine is linked to sleep inducing effects Adenosine, and thus caffeine, act on NE, DA, ACh , glutamate, and GABA
  • 9.
    Caffeinism Caffeine-induced disordersfrom DSM-IV Tolerance and Dependence Withdrawal effects due to increased adenosine receptor density and thus increased adenosine sensitivity High doses >1000mg/day Psychiatric effects
  • 10.
    Conflicting data onreproductive effects May slow growth in utero , especially high dose Caffeine may be harmful prior to conception May increase the risk of spontaneous abortion
  • 11.
    How much caffeine?5oz 5oz 5oz 1oz 1oz 12oz Tab- Anal- Diur- Coffee Tea Cocoa Choc. C.Milk Cola lets gesics etics
  • 12.
    The REAL Thing– Coca-Cola Active ingredient is phosphoric acid. pH of 2.8 Dissolves a nail in 4 days. Dissolves a tooth in 24-48 hours. Trucks carrying Coca Cola syrup (the concentrate) must use Hazardous Material placards. The distributor of Coke use it to clean the engines of their trucks.