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CNS stimulant

CNS stimulant. Used in treatment of depression and as analeptics. I. Analeptics. Drugs enhance the response to sensory stimulation Respiratory stimulant. 1. Nikethimide. 2. Ethamivan. 3. Methylxanthines. Caffeine Theophylline Theobromine. II. Antidepressants. MAO inhibitors TCAs

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CNS stimulant

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  1. CNS stimulant Used in treatment of depression and as analeptics.

  2. I. Analeptics • Drugs enhance the response to sensory stimulation • Respiratory stimulant

  3. 1. Nikethimide

  4. 2. Ethamivan

  5. 3. Methylxanthines • Caffeine • Theophylline • Theobromine

  6. II. Antidepressants • MAO inhibitors • TCAs • Miscellaneous

  7. A. MAO Inhibitors • Elevate biogenic amine by inhibiting MAO. Nonhydrazine hydrazine Iproniazide Tranycypromine phenelzine

  8. 1. Iproniazide Hydrazine derivative • S.E

  9. 2. phenelzine

  10. Non hydrazine derivatives • Less SE Tranylcypromine

  11. B. Tricyclic antidepressants (TCAs) • SAR • Side effects anticholinergic effects

  12. 1. Imipramine hydrochloride (tofranil) • Close relative to antipsychotic phenothiazines • SE: anticholinergic and sedative efffects

  13. 2. Desipramine hydrochloride

  14. 3. Amitriptyline hydrochloride 4. Nortriptyline

  15. 5. Doxepin hydrochloride • Oxacongener.

  16. C. Miscellaneous • Effects on cardiovascular system. 1. Maprotiline hydrochloride

  17. 2.Trazodone hydrochloride • Similar to fluorobutyrophenone • 5HT • SE: sedation

  18. 3. Fluoxetine • Serotonin reuptake inhibitor

  19. III. psychadelics

  20. Local anesthesia • Characteristics for an ideal local anaesthetics - reversible blockade of sensory nerve fibers with a minimal effect on the motor nerve activation

  21. Toxicity and side effects • Effects on excitable membranes such as in the heart, the neuromuscular junctions, and the CNS. With more effect on neuromuscular junctions and the CNS. • convulsions, followed by severe CNS depression, (particularly of the respiratory and cardiovascular centers). Due to inhibtion of inhibtory neurons as GABA system.

  22. amide-type local anesthetics likely to produce CNS side effects than the ester- type compounds • SE depend on route and site of administration, the lipid solubility and metabolic stability of local anesthetics. • allergic reactions rare More with p-amino-benzoic ester-type • amide- type: antiarhythmic (parenterally and at a subanesthetic dosage) effect on Na channel.

  23. SAR • Lipophilic portion

  24. Intermediate chain • Short alkyl (1-3) carbons • Nature of chain determine stability and duration (amide more resistant) • Branching increase the duration

  25. hydrophilic portion • Tertiary alkyl amine form water soluble

  26. Classification • Ester type • Amide type

  27. Ester type • procaine

  28. benzocaine

  29. Tetracaine

  30. benoxinate

  31. Amide type • Lidocaine Mepvacaine

  32. Synthesis of lidocaine

  33. Metabolism • Ester type esterase interaction with anticholinesterase increase toxicity Antagonize the antibacterial activity of sulfonamide Amide type:

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