Stimulants_2009

Stimulants_2009 - MEDC 417/502 Dr. McCurdy CNS STIMULANTS...

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MEDC 417/502 Dr. McCurdy CNS STIMULANTS AND OTHER DRUGS OF ABUSE Medicinal Chemistry of Psychostimulants CNS STIMULANTS Analeptics o Agents that have a stimulant effect primarily on autonomic centers involved in the regulation of respiration and circulation Generally concerned with control of respiration - hypoventilation which may be caused by: o CO 2 accumulation cause by respiratory disease o Post-anesthetic respiratory depression o Circulatory failure causing low blood pressure o Intoxication of overdoses of CNS depressants These drugs generally possess low therapeutic indexes Overdoses can cause ________________________ Sometimes classified as: o Reflex stimulants (lobeline) o Spinal Cord stimulants (strychnine) o Psychic stimulants (CNS) o Medullary stimulants (doxapram) OLDER AGENTS Lobeline Cholinomimetic Strychnine Glycine antagonist Pentylemetetrazole (Metrazole®) Convulsant Doxapram (Dopram®) MOA: Unclear
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MEDC 417/502 Dr. McCurdy XANTHINE ALKALOIDS Purine derivatives - Methylxanthines o Caffeine (coffee, tea, cola) o Theophylline (tea) o Theobromine (cocoa) o Classified as psychic stimulants NOTE: 0.5 g caffeine IV will induce convulsions! Mildly habituating o Some withdrawal in users of > 600 mg/day (6 cups of coffee) Xanthines also have diuretic properties Theophylline widely used as a bronchodilator in asthma N N N N O O HN N N N O O N N N H N O O caffeine theophylline theobromine Methylxanthines – MOA Previously thought to work as Phosphodiesterase (PDE) inhibitors o Increase cAMP levels resulting in: Increased glycogenolysis and gluconeogenesis o Increases Brain glucose thus stimulation
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Stimulants_2009 - MEDC 417/502 Dr. McCurdy CNS STIMULANTS...

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