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Cholinergic drugs

Cholinergic drugs. Nervous system. CENTRAL NERVOUS SYSTEM PERIPHERAL NERVOUS SYSTEMS Sensory fiber motor fiber involuntary voluntary sympathetic parasympathetic. function.

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Cholinergic drugs

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  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. 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. 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 5 A 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

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