Cholinergic Drugs

Description

Lebanese American University - Medical Chemistry 1
Majd Fawaz
Flashcards by Majd Fawaz, updated more than 1 year ago
Majd Fawaz
Created by Majd Fawaz over 3 years ago
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Resource summary

Question Answer
State the effects of ACh on - Vasculature - Eye - Salivary and Lacrimal Glands - Bronchi - Heart - GI Tract - Urinary Blander - Sweat Glands - Male Reproductive Tract - Uterus - Vasculature: Indirect Vasodilation (NO) - Eye: Miosis+Accommodation (Near) - Salivary Glands: Inc. Watery Secretions - Bronchi: Constrition - Heart: Bradycardia+Dec. Conductivity (AV node) - GI Tract: Inc. Tone, Secretions+Relax Sphincter - Urinary Blander: Detrusor Muscle Contraction+Relax Sphincter - Sweat Glands: Diaphorisis - Male Reproductive Tract: Erection - Uterus: Variable
- Muscarine - Isolated from Amanita Muscaria (Mushroom) - Epi-Allo-Epiallo Isomers
- Nicotine
- Acetylcholine - Non Selective Cholinergic Agonist - pH Independent - Not Used Clinically
- Methacholine - Muscarinic Agonist - (+) is Equipotent to ACh - More Resistance to AChE
- Carbachol - Similar Potency to ACh - Non Selective - More Resistance to AChE
- Bethanechol - Potent Selective Muscarinic Agonist - (+) > (-) - More Resistance to AChE
- Choline Ethyl Ether - Muscarinic Agonist - Exception to the SAR
- Pilocarpine - Alkaloid (Pilocarpus Jaborandi) - Potant Muscarinic Agonist - Hydrolisis and Epimerization Give 2 Inactive Products (Pilocarpic Acid, Isopilocarpine)
- Physostigmine - Reversible AChEI - Alkaloid (Physostigma venenosum/Calanbar Bean) - Exhibits High Affinity to AChE Compared to Carbachol - Used To Treat Glaucoma and Overdoses of Anticholinergics - Light Sensitive - Undegoes Hydrolysis in Aqeuous Sol.
- Eseroline - Inactive product of Physostigmine Degradation
- Rubreserine - Inactive product of Physostigmine Degradation - Red in Color - Used to Identify Shelf Life of Physostigmine
- Neostigmine - Reversible AChEI – Synthetic compounds – Ionized – Indicated for Myastenia Gravis
- Pyridostigmine - Reversible AChEI – Synthetic compounds – Ionized – Indicated for Myastenia Gravis
- Rivastigmine - Reversible AChEI - Used for Alzheimer’s Disease
- Carbaryl - Reversible AChEI
- Donepezil - Reversible AChEI - Used for Alzheimer’s Disease - Lacks Hepatotoxicity
- Tacrine - Reversible AChEI - Used for Alzheimer’s Disease - Reported Hepatotoxicity
- Edrophonium - Reversible AChEI - Class: Bisquaternery amonium - Myastenia Graves VS Cholinergic Criss - Rapid Renal Excretion - No Medicinal Use
- Demecarium bromide - Reversible AChEI - Class: Bisquaternery amonium
- Galantamine - Reversible AChEI - Class: Bisquaternery amonium
- Ambenonium Cholride - Reversible AChEI - Class: Bisquaternery amonium
- Sarin - Irreversible AChEI (Organophosphate) - Very Lipophilic - Deadly Nerve Gas - Faster Aging
- Diisopropylflourophosphate (DFP) - Irreversible AChEI - Very Lipophilic - Deadly Nerve Gas
- Echothiophate iodide - Irreversible AChEI - Very Lipophilic - Used as Eye Drops for Glaucoma
- Malathion - Irreversible AChEI - Very Lipophilic - Poor AChE Inhibitor (Malathionic Acid as well)
- Malaoxone - x10000 > inhibition than Malathion
- Parathion - Irreversible AChEI - Very Lipophilic - Poor AChE Inhibitor
- Paraoxon - Irreversible AChEI - Very Lipophilic - Good AChE Inhibitor
- Schradan - Irreversible AChEI - Very Lipophilic
- Dichlofenthion - Irreversible AChEI - Very Lipophilic
- Obidoxime - Organophosphate Antidote (Give within 30 min) - Ionized (Periphery) - Should be given in combination
- Diacetyl monoxime (DAM) - Organophosphate Antidote (Give within 30 min) - Centrally - Should be given in combination
- 2-Pyridyl Acetyl Monooxime (2-PAM) - Organophosphate Antidote (Give within 30 min) - Ionized (Periphery) - Should be given in combination
- Atropine - Nonselective Muscarinic Antagonist - Alkaloid (Atropa Belladonna/Datura Stramonium)
- Scopolamin - Nonselective Muscarinic Antagonist - Alkaloid (Hyoscyamus niger)
- Glycopyrrolate - Competitive Antagonist - Antispasmodic Effects - Produce mydriasis - Antisecretory - Main Use: Anti-Ulcer Othe Use: Anti-Diarrhea, Anti-Asthmatic
- Propantheline - Competitive Antagonist - Antispasmodic Effects - Produce Mydriasis - Antisecretory - Main Use: Anti-Ulcer Othe Use: Anti-Diarrhea, Anti-Asthmatic
- Clidinium - Competitive Antagonist - Antispasmodic Effects - Produce Mydriasis - Antisecretory - Main Use: Anti-Ulcer Othe Use: Anti-Diarrhea, Anti-Asthmatic
- Ipratropium - Competitive Antagonist - Antispasmodic Effects - Produce Mydriasis - Antisecretory - Main Use: Anti-Asthmatic
- Flavoxate - Competitive Antagonist - Antispasmodic Effects - Produce Mydriasis - Antisecretory - pH Dependent
- Oxyphencyclimine - Competitive Antagonist - Antispasmodic Effects - Produce Mydriasis - Antisecretory - Use: Parkinson
- Procyclidine - Competitive Antagonist - Antispasmodic Effects - Produce Mydriasis - Antisecretory - pH Dependent - Central/Peripheral Effect
- Trihexyphenidyl - Competitive Antagonist - Antispasmodic Effects - Produce Mydriasis - Antisecretory - pH Dependent - Central/Peripheral Effect
- Benzatropine - Competitive Antagonist - Antispasmodic Effects - Produce Mydriasis - Antisecretory - Use: Parkinson
- Orphenadrine - Competitive Antagonist - Anticholinergic > Antihistaminic - Antispasmodic Effects - Produce Mydriasis - Antisecretory - Use: Parkinson
- Diphenhydramine - Competitive Antagonist - Anticholinergic < Antihistaminic - Antispasmodic Effects - Produce Mydriasis - Antisecretory - Use: Parkinson
- Pirenzepine - Selective M1 antagonist - Class: 1,5 BDZ - Use: Peptic Ulcer
- Telenzepine - Selective M1 antagonist - Class: 1,5 BDZ - Use: Peptic Ulcer
- Hexamethonium - Ganglionic blockers - Class: Bis-quaternaryamonium - Local Effect
- Trimetaphan - Ganglionic blockers - Class: Sulfonium - Local Effect
- Pentolinium - Ganglionic blockers - Class: Bis-quaternaryamonium - Local Effect
- Mecamylamine - Ganglionic blockers - Class: 2nd Amine - Systemic Effect
- Pempidine - Ganglionic blockers - Class: 3rd Amine - Systemic Effect
- Succinylcholine - DNMJ Blockers - Low DOA
- Tubocurarine - NDNMJ Blockers - Use: Muscle Relaxtion
- Pancuronium - Competitive Antagonists (Treatable) - Lack CNS Effect - Given IV - Class: Ammonium Steroids - Use: Muscle Relaxtion
- Vecuronium - Competitive Antagonists (Treatable) - Lack CNS Effect - Given IV - Class: Ammonium Steroids - Use: Muscle Relaxtion
- Pipecuronium - Competitive Antagonists (Treatable) - Lack CNS Effect - Given IV - Class: Ammonium Steroids - Use: Muscle Relaxtion
- Rocuronium - Competitive Antagonists (Treatable) - Lack CNS Effect - Given IV - Class: Ammonium Steroids - Use: Muscle Relaxtion
- Atracurium - Competitive Antagonists (Treatable) - CNS Effect - Given IV - Class: Benzylisoquinoline - Use: Muscle Relaxtion
- Mivacurium - Competitive Antagonists (Treatable) - Lack CNS Effect - Given IV - Class: Benzylisoquinoline - Shortest DOA - Use: Muscle Relaxtion
- Doxacurium - Competitive Antagonists (Treatable) - Lack CNS Effect - Given IV - Class: Benzylisoquinoline - Use: Muscle Relaxtion
- Laudanosine
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