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Cholinomimetics

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Cholinomimetics

  1. 1. www.company.com CHOLINOMIMETICS Dr Igor Khalin
  2. 2. www.company.com Druds acting on ANS • Parasympathomimetics Sympathomimetics (cholinomimetics) (adrenomimetics) • Parasyimpatholythics Sympatholythics (cholinoblockers) (adrenoblockers)
  3. 3. www.company.com Drugs acting on ANS • Parasympathomimetics (cholinomimetics) • Sympatholythics (adrenoblockers)
  4. 4. www.company.com Drugs acting on ANS • Sympathomimetics (adrenomimetics) • Parasympatholythics (cholinoblockers)
  5. 5. www.company.com Cholinomimetics • Eye  accommodation for near vision, miosis, IOP • Saliva  copious, liquid • Bronchi  constriction, secretion • Heart  rate, blood pressure • GIT  secretion, peristalsis sphincter tone • Bladder  detrusor sphincter tone
  6. 6. www.company.com Cholinergic neuron ATP ATP negative feedback
  7. 7. www.company.com Cholinergic receptors MUSCARINIC NICOTINIC M1 M2 M3 M4 M5 NM NN Eye Heart Smooth muscles Exocrine glands CNS Ganglions Carotid sinus Skeletal muscles Adrenal glands CNS
  8. 8. www.company.com Muscarinic receptors • High affinity for muscarine • M1 – gastric parietal cells, saliva, CNS • M2 - cardiac cells, smooth muscle, CNS • M3 - bladder, exocrine glands, smooth muscle, eye, CNS • M1&M3 – Gq • M2 - Gi Amanita muscaria
  9. 9. www.company.com Muscarinic receptors M1 M3
  10. 10. www.company.com Cholinergic Agonists Direct acting Indirect acting Acetylcholine Bethanecol Carbachol Pilocarpine Edrophonium Physostigmine Neostigmine
  11. 11. Direct acting cholinergic agonists www.company.com ACETYLCHOLINE - Pharmakokinetics
  12. 12. Direct acting cholinergic agonists 1. Decrease in heart rate and cardiac output 2. Decrease in blood pressure www.company.com ACETYLCHOLINE - Effects
  13. 13. www.company.com Organ system effects ACETYLCHOLINE • 3. Eye – Contraction of sphincter (Miosis) – Contraction of cilliary muscle (Myopia)
  14. 14. Direct acting cholinergic agonists www.company.com ACETYLCHOLINE 4. Other actions diarrhea sweating nausea 4. Clinical use very rare: eye drops to obtain miosis
  15. 15. Direct acting cholinergic agonists www.company.com 1. Stimulation of atonic bladder 2. Nonobstructive urinary retention 3. Neurogenic atony 4. Megacolon Ophthalmology -glaucoma -surgery
  16. 16. Direct acting cholinergic agonists www.company.com PILOCARPINE - PK 1. Tertiary nitrogen 2. Good adsorbtion 3. Penetrate BBB
  17. 17. Direct acting cholinergic agonists Jaborandi (Pilocarpus pennatifolius) www.company.com PILOCARPINE - Effects 1. Secretagoge (sweat, tears, saliva) • Jaborandi - what causes slobbering PILOCARPINE – Clinical usage 1. Sjögren’s syndrome • Dry mouth, lack tears 2. Glaucoma
  18. 18. Direct acting cholinergic agonists PILOCARPINE open-angle vs. closed angle glaucoma www.company.com posterior synechiae anterior synechiae
  19. 19. www.company.com Mushroom poisoning  Miosis  Hyper salivation  Excessive sweating, lacrimation  Cold, wet skin  Bradycardia  Polyuria  Diarrhea  Convulsions
  20. 20. www.company.com Nicotinic receptors • High affinity to nicotine • NM- neuro-muscular junction • NN – ganglion, adrenal gland CNS, carotid sinus
  21. 21. Indirect acting cholinergic agonists Reversible Irreversible www.company.com Edrophonium Neostigmine Physostigmine Rivastigmine Galantamine Echothiophate Organophosphates
  22. 22. www.company.com Mechanism of action
  23. 23. www.company.com Mechanism of action
  24. 24. www.company.com Mechanism of action
  25. 25. www.company.com Reversible Physostigmine Calabar Bean 1. Tertiary nitrogen 2. Good adsorbtion 3. Penetrate BBB
  26. 26. www.company.com Reversible Physostigmine 1. Atony of intestine 2. Atony of bladder 3. Glaucoma 4. Overdose of ATROPINE, ANTIPSYCOTICS, ANTIDEPRESSANTS
  27. 27. www.company.com Reversible Physostigmine 1. Convulsions 2. Bradycardia 3. Paralysis of skeletal muscle
  28. 28. www.company.com Reversible Neostigmine 1. Quatenary nitrogen 2. Poor adsorbtion 3. Not penetrate BBB
  29. 29. www.company.com Reversible Neostigmine 1. Paralyzes 2. Myastenia gravis 3. Antidote of neuro-muscular blocker TUBOCURARINE
  30. 30. www.company.com Reversible Neostigmine 1. Salivation 2. Flushing 3. Decreased BP 4. Abdominal pain 5. Diarrhea 6. Bronchospasm
  31. 31. www.company.com Reversible Neostigmine 1. Bronchial asthma 2. Intestinal inflammation, obstruction 3. Bladder obstruction 4. Peritonitis
  32. 32. www.company.com Reversible Edrophonium 1. Quatenary nitrogen 2. Poor adsorbtion 3. Not penetrate BBB 4. Fast elimination 5. Duration 10-20 min
  33. 33. www.company.com Reversible Edrophonium 1. Diagnosis of myasthenia gravis 2. Antidote of neuro-muscular blocker
  34. 34. www.company.com Reversible Rivastigmine 1. Tertiary nitrogen 2. Good adsorbtion 3. Penetrate BBB
  35. 35. www.company.com Reversible Rivastigmine Alzheimer disease
  36. 36. www.company.com Irreversible Echothiophate Glaucoma
  37. 37. www.company.com Toxicology Organophosphates
  38. 38. www.company.com Toxicology Salivation Lacrimation Urination Defecation Gastrointestinal motility Emesis Miosis
  39. 39. www.company.com Toxicology 1. Reactivation of acetylcholinesterase • PRALIDOXIME  Not enter BBB 2. M-cholinoblocker • ATROPINE  Antimuscarinic only 3. Anticonvulsant • DIAZEPAM
  40. 40. www.company.com SUMMARY

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