1. Cholinergic drugs

2. Nervous system CENTRAL NERVOUS SYSTEM PERIPHERAL NERVOUS SYSTEMS
Sensory fiber motor fiber
involuntary voluntary
sympathetic parasympathetic

3. function Sympathetic and parasympathetic are complemantary
Composition: pre,ganglion and post
Chemicals are Ach and NA

4. Drugs produce similar effects to acetylcholine
Cholinergic drugs
Drugs produce similar effects to acetylcholine

5. Classification Direct cholinergic agents Indirect
Cholinestrase reactivator

6. Effects of acetylcholine
Muscarinic effects
Contaraction of smooth muscle
Peripheral vasodilation
Increase secretion of saliva, exocrine
Dcrease the contraction of the heart
B. Nicotinic
Stimulation of skeletal muscle tone

7. Trans acetylcholine active on muscarinic and nicotinic receptors

8. A. Direct cholinergic agents
Mode of action
Cholinomimetic alkaloid
Choline esters
Pilocarpine
Methacholine
Carbachol
[Cholinomimetics & parasympathomimetics]

9. SAR
Acetyl choline

10. Metacholine CH3 on beta carbon increase muscarinic Long duration
Uses: Mythenia gravis, paroxysmal tachycardia

11. Synthesis

12. Carbachol
Long duration
Uses: glucoma
Synthesis

13. Bethanicol Bioisoster of methacholine Long duration Mainly muscarinic
Uses:abdominal distention,urinary distention

14. 2. Cholinomimetic alkaloid
pilocarpine
Uses: glucoma, antagonises mydriatics

15. cevimeline For treatment of dry mouth in Sjogren’s syndrome
Similar to pilocarpin

16. B.Indirect acting [anticholinesterase]
Organophosphorus
Carbamates
Physostigmine
Neostigmine methyl sulphate
Pyridostigmine
Neostigmine bromide(prostigmin)
Edrophonium

17. Physostigmine acts by interfering with the metabolism of acetylcholine
Physostigmine acts by interfering with the metabolism of acetylcholine. It is an inhibitor of acetylcholinesterase, the enzyme responsible for the breakdown of acetylcholine in the synaptic cleft of the neuromuscular junction. It indirectly stimulates both nicotinic and muscarinic receptors. (Find the structure and uses).

18. Neostigmine bromide(prostigmin)

19. Synthesis

20. Neostigmine methyl sulphate
Uses
Contraindication
Bradycardia, cardiac disease, hypotension, parkinsonism.

21. Pyridostigmine bromide(mestinon)

22. Synthesis
Uses: Mysthenia gravis

23. Edrophonium Chloride Short and rapid-acting cholinergic drug.
Uses:myasthenia gravis , emergency treatment (short action)
Side effects: bradycardiaa, hypotension,increase saliva

24. Cholinesterase reactivators
2-[(Hydroxyimino)methyl]-1-methylpyridinium chloride

25. Synthesis

26. Cholinergic blocking agents [Anticholinergic]
Act at different sites
Postganglionic of parasympathetic
(Antimuscurinic)
At ganglionia of sympathetic and parasympathetic
(ganglion blockers)
Neuromuscular junction of voluntry system
(neuromuscular blocking agents)

27. I. Antimuscarinics [similar to Ach & alkaloid]
There effects will be :
Mydriatic
Antispasmodic
antisecretory

28. Antimuscarinics similar to Acetyl choline
Antimuscarinic:aminoalcohol,aminoamides,papaverine derivatives.
Aminoalcohols:esters,ethers,carbamates.
Esters:solaneceous alk.,synthetic analouges,esters of other alc.

29. 2. Alkaloid antimuscarinics
Atropine, Hyoscin
Uses of Antimuscarinics:
Antispasmodic
Antisecretory
Antiparkinsonism
mydriatics

30. Esters of other aminoalcohol
Cyclopentolate
Uses: mydriatic ,cycloplegic

31. Aminoalcohol ethers Orphenadrine
Uses: Antihistaminic,antiparki-nsonism.
N,N-dimethyl-2-(phenyl(o-tolyl)methoxy)ethanamine

32. Oxybutynin
used to relieve urinary and bladder difficulties, including frequent urination and inability to control urination
Homework : find the structure and mechanism of action

33. Papaverine and related compounds.
Vasodilator relax smooth muscle.(GIT,bronchi,uretures,biliary system).

34. Trihexyphenidyl
Uses
Parkinson’s disease

35. Ipratropium bromide
Uses Bronchodilator

36. Ganglionic blocking agent
Hexamethonium

37. Neuromuscular bloking agents
Decamethonium bromide
Assay :volhard

38. Neuromuscular blocking agents
Uses