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Introduction of Parasympathomimetics Acetylcholine biosynthesis Acetylcholine receptors

Introduction of Parasympathomimetics Acetylcholine biosynthesis Acetylcholine receptors ACT on M receptors: Bethanechol , Carbachol , Pilocarpine Reversable inhibitor of cholinestrase enzyme: Edrophonium , Neostigmine , Physostigmine

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Introduction of Parasympathomimetics Acetylcholine biosynthesis Acetylcholine receptors

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  1. Introduction of Parasympathomimetics • Acetylcholine biosynthesis • Acetylcholine receptors • ACT on M receptors: Bethanechol, Carbachol,Pilocarpine • Reversable inhibitor of cholinestrase enzyme: Edrophonium, Neostigmine, Physostigmine • Irreversable inhibitor of cholinestrase enzyme IICE: Echothiophate. • Antidote of IICE: Pralidoxime • Anti- Alzheimer.

  2. Acetylcholine biosynthesis Acetylcholine

  3. Acetylcholine receptors are: • M.....M1(CNS), M2(Heart), M3(glands &GI), M4(lung), M5 (?). • N1........NMJ • N2

  4. Parasympathomimetics • Bethanechol (Urivoid) • Pharmaceutical chemistry • Possible Origin • Physiochemical Properties • Idea of Retro-synthesis • Molecular pharmacology • Mechanism of action: Direct cholinergic • Structure-based explanation of Therapeutic uses: Atonic bladder before surgery, neurogenic atony of colon. • Structure-based explanation of Side effects: sweating, salivation, decreased blood pressure, abdominal pain, diarrhoea, miosis and bronchospasm • Analysis

  5. Parasympathomimetics • Carbachol (Optichol) • Pharmaceutical chemistry • Possible Origin • Physiochemical Properties • Idea of Retro-synthesis • Molecular pharmacology • Mechanism of action: Direct cholinergic • Structure-based explanation of Therapeutic uses: rarely because of receptor non-selectivity. • Structure-based explanation of Side effects: • Analysis

  6. Parasympathomimetics • Pilocarpine (isopto carpine) • Pharmaceutical chemistry • Possible Origin • Physiochemical Properties • Idea of Retro-synthesis • Molecular pharmacology • Mechanism of action: Direct cholinergic • Structure-based explanation of Therapeutic uses: emergency of open and closed angle glaucoma. • Structure-based explanation of Side effects: Reverse CNS effect of atropine and TCA. • Analysis

  7. Parasympathomimetics • Edrophonium (Enlon) • Pharmaceutical chemistry • Possible Origin • Physiochemical Properties • Idea of Retro-synthesis • Molecular pharmacology • Mechanism of action: Anti-cholinesterase • Structure-based explanation of Therapeutic uses: diagnosis of myasthenia gravis (short duration of action) • Structure-based explanation of Side effects • Analysis

  8. Parasympathomimetics • Neostigmine (stigmin) • Pharmaceutical chemistry • Possible Origin • Physiochemical Properties • Idea of Retro-synthesis • Molecular pharmacology • Mechanism of action: Anti-cholinesterase (potent) • Structure-based explanation of Therapeutic uses: Txt of myasthenia gravis • Structure-based explanation of Side effects: • Analysis

  9. Parasympathomimetics • Physostigmine • Pharmaceutical chemistry • Possible Origin • Physiochemical Properties • Idea of Retro-synthesis • Molecular pharmacology • Mechanism of action: Anti-cholinesterase • Structure-based explanation of Therapeutic uses: for atony muscles before surgery, glaucoma (pilocarpine is more effective). • Structure-based explanation of Side effects: reverse CNS effect of atropine and TCA. • Analysis

  10. Irreversible Parasympathomimetics • Echothiophate • Pharmaceutical chemistry • Possible Origin • Physiochemical Properties • Idea of Retro-synthesis • Molecular pharmacology • Mechanism of action: Irreversible Anti-cholinesterase • Structure-based explanation of Therapeutic uses: Rarely used. • Structure-based explanation of Side effects: • Analysis

  11. Anti-dote of organophosphates • Pralidoxime • Pharmaceutical chemistry • Possible Origin • Physiochemical Properties • Idea of Retro-synthesis • Molecular pharmacology • Mechanism of action: De-alkylation of cholinesterase enzyme. • Structure-based explanation of Therapeutic uses: antidote of organophosphates. • Structure-based explanation of Side effects • Analysis

  12. centrally acting cholinesterase inhibitor • Donepezil (aricept) • Pharmaceutical chemistry • Possible Origin • Physiochemical Properties • Idea of Retro-synthesis • Molecular pharmacology • Mechanism of action: centrally acting reversible cholinesterase inhibitor • Structure-based explanation of Therapeutic uses: Txt of Alzheimer • Structure-based explanation of Side effects • Analysis

  13. Galantamine • Pharmaceutical chemistry • Possible Origin • Physiochemical Properties • Idea of Retro-synthesis • Molecular pharmacology • Mechanism of action: Increasing the acetylcholine concentration in the brain?! • Structure-based explanation of Therapeutic uses: Txt of Alzheimer • Structure-based explanation of Side effects • Analysis

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