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Cholinomimetics
This document discusses cholinergic drugs and their effects in the body. It describes two main types of cholinergic drugs: direct-acting cholinomimetics like acetylcholine and indirect-acting drugs like physostigmine and neostigmine. Direct-acting drugs mimic acetylcholine and bind nicotinic and muscarinic receptors. Indirect drugs inhibit acetylcholinesterase to increase the level and duration of acetylcholine at receptors. Side effects of cholinergic stimulation include increased salivation, sweating, lacrimation, gastrointestinal motility, urination, and bradycardia. These drugs find clinical use in glaucoma, urinary retention, and as antidotes to
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Cholinomimetics
- 1. www.company.com CHOLINOMIMETICS DrIgor Khalin
- 2. www.company.com Druds actingon ANS • Parasympathomimetics Sympathomimetics (cholinomimetics) (adrenomimetics) • Parasyimpatholythics Sympatholythics (cholinoblockers) (adrenoblockers)
- 3. www.company.com Drugs actingon ANS • Parasympathomimetics (cholinomimetics) • Sympatholythics (adrenoblockers)
- 4. www.company.com Drugs actingon ANS • Sympathomimetics (adrenomimetics) • Parasympatholythics (cholinoblockers)
- 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. www.company.com Cholinergic neuron ATP ATP negative feedback
- 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. 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
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- 10. www.company.com Cholinergic Agonists Direct acting Indirect acting Acetylcholine Bethanecol Carbachol Pilocarpine Edrophonium Physostigmine Neostigmine
- 11. Direct acting cholinergicagonists www.company.com ACETYLCHOLINE - Pharmakokinetics
- 12. Direct acting cholinergicagonists 1. Decrease in heart rate and cardiac output 2. Decrease in blood pressure www.company.com ACETYLCHOLINE - Effects
- 13. www.company.com Organ systemeffects ACETYLCHOLINE • 3. Eye – Contraction of sphincter (Miosis) – Contraction of cilliary muscle (Myopia)
- 14. Direct acting cholinergicagonists www.company.com ACETYLCHOLINE 4. Other actions diarrhea sweating nausea 4. Clinical use very rare: eye drops to obtain miosis
- 15. Direct acting cholinergicagonists www.company.com 1. Stimulation of atonic bladder 2. Nonobstructive urinary retention 3. Neurogenic atony 4. Megacolon Ophthalmology -glaucoma -surgery
- 16. Direct acting cholinergicagonists www.company.com PILOCARPINE - PK 1. Tertiary nitrogen 2. Good adsorbtion 3. Penetrate BBB
- 17. Direct acting cholinergicagonists 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. Direct acting cholinergicagonists PILOCARPINE open-angle vs. closed angle glaucoma www.company.com posterior synechiae anterior synechiae
- 19. www.company.com Mushroom poisoning Miosis Hyper salivation Excessive sweating, lacrimation Cold, wet skin Bradycardia Polyuria Diarrhea Convulsions
- 20. www.company.com Nicotinic receptors • High affinity to nicotine • NM- neuro-muscular junction • NN – ganglion, adrenal gland CNS, carotid sinus
- 21. Indirect acting cholinergicagonists Reversible Irreversible www.company.com Edrophonium Neostigmine Physostigmine Rivastigmine Galantamine Echothiophate Organophosphates
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- 25. www.company.com Reversible Physostigmine Calabar Bean 1. Tertiary nitrogen 2. Good adsorbtion 3. Penetrate BBB
- 26. www.company.com Reversible Physostigmine 1. Atony of intestine 2. Atony of bladder 3. Glaucoma 4. Overdose of ATROPINE, ANTIPSYCOTICS, ANTIDEPRESSANTS
- 27. www.company.com Reversible Physostigmine 1. Convulsions 2. Bradycardia 3. Paralysis of skeletal muscle
- 28. www.company.com Reversible Neostigmine 1. Quatenary nitrogen 2. Poor adsorbtion 3. Not penetrate BBB
- 29. www.company.com Reversible Neostigmine 1. Paralyzes 2. Myastenia gravis 3. Antidote of neuro-muscular blocker TUBOCURARINE
- 30. www.company.com Reversible Neostigmine 1. Salivation 2. Flushing 3. Decreased BP 4. Abdominal pain 5. Diarrhea 6. Bronchospasm
- 31. www.company.com Reversible Neostigmine 1. Bronchial asthma 2. Intestinal inflammation, obstruction 3. Bladder obstruction 4. Peritonitis
- 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. www.company.com Reversible Edrophonium 1. Diagnosis of myasthenia gravis 2. Antidote of neuro-muscular blocker
- 34. www.company.com Reversible Rivastigmine 1. Tertiary nitrogen 2. Good adsorbtion 3. Penetrate BBB
- 35. www.company.com Reversible Rivastigmine Alzheimer disease
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- 38. www.company.com Toxicology Salivation Lacrimation Urination Defecation Gastrointestinal motility Emesis Miosis
- 39. www.company.com Toxicology 1.Reactivation of acetylcholinesterase • PRALIDOXIME Not enter BBB 2. M-cholinoblocker • ATROPINE Antimuscarinic only 3. Anticonvulsant • DIAZEPAM
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