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. hydrazine Non hydrazine Iproniazide Tranycypromine phenelzine

8. 1. Iproniazide  S.E Hydrazine derivative

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: