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Holinergic Drugs
2/24/2023
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ACETYLCHOLINE CHOLINE NA* 6 RECYCLING OF CHOLINE Ca²+ S DEGRADA- Pr TION OF ACETYLCHOLINE +Cast CHOLINE Na* ACETYLCHOLINE CHOLINE ACETATE SYNAPTIC VECICLE 1 SYNTHESIS 20276 OF ACETYLCHOLINE 2 UPTAKE INTO STORAGE VESICLES PREZYNAPTIC RECEPTOR 3 RELEASE OF NEURO- TRANSMITTER 4 BINDING TO THE RECEPTOR Thank ACETYLCHOLINESTERASE → degrades acetylcholine CHOLINERGIC AGONIST →1acetylcholine CHOLINOMIMETIC DRUG → mimics cholinergic system SYMPATHOLYTIC DRUG → sympathetic response PRASYMPATHOMIMETIC M receptors, parasympathetic D CHOLINOMIMETIC (CHOLINERGIC) DRUGS 7 DIRECT-ACTING MUSCARINIC NICOTINIC INDIRECT-ACTING ORGANOPHOSPHATE CARBAMATES/ CHOLINE ESTERS ALKALOIDS EDROPHONIUM DIRECT-ACTING activates muscarinic and micotinic receptors ★IN DIRECT-ACTING → ↑acetylcholine by inhibiting acetylcholinesterase inhibitors CHOLINE ESTERS (DIRECT-ACTING) AT TAMANNAS ACETYLCHOLINE → prototype • BETANECHOL→ treatment for urinary retention CARBACHOL for glaucoma ( intraocular pressure) METHACHOLINE -diagnosis of asthma ALKALOIDS (DIRECT - ACTING) PILOCARPINE DOC for emergency lowering of Intraocular pressure CACUTE ANGLE CLOSURE GLAUCOMA) ● · · ARECHOLINE •MUSCARINE INDIRECT-ACTING (QUATERNARY AMINE) RAS EDROPHONIUM diagnosis of myes thenia gravis. → Tensilon. →Tensilon Test weakness MY ESTHENIA GRAVIS - muscle severe • Ach Ach Receptor 37061430 TRADERO SAM 30 damaged acetylcholine receptors → autoimmune (genetic) Nm (Nicotinic receptor muscular) = muscle contraction Nn Ng (Nicotinic receptor neural) = neurotransmission CARBAMATES (INDIRECT-ACTING; INTERMEDIATE DURATION) •PHYSOSTIGMINE 1 acetylcholine → aka eserine → antidote for anticholinergic poisoning CATROPINE, PHENOTHIAZINE, TRICYCLIC ANTIDEPRESSANT) NEOSTIGMINE-DOC) for the treatment of myesthenia gravis •PYRIDOSTIGMINE (MESTINON) treatment of myesthenia gravis •CARBAMATE INSECTICIDES ORGANOPHOSPHATES (INDIRECT ACTING; LONG DURATION) ISOFLUOROPHATE, ECHOTHIOPHATE →glaucoma MALATHION, PARATHION → insecticides, pesticides (Malathion-scabicide) , SOMAN →nerve gases; chemical warfare •TABUN, SARIN, S ANTIDOTE: PRALIDOXIME (PAM) * ATROPINE CHOLINERGIC ANTAGONIST CHOLINERGIC RECEPTORS ANTICHOLINERGIC MUSCARINIC (M1-M5) muscle contraction Nm (NEUROMUSCULAR BLOCKERS) Nn CGANGLION BLOCKERS) SANT MUSCARINIC BLOCKERS ATROPINE (anticholinergic) m →L-hyoscyamine (G) antispasmodic) prototype ● ● ● HYOSCINE (Buscopan, Transderm-Scop) - hyoscine → prevent motion sickness (transdermal patch) → S/E constipation, urinary retention NITROGLYCERINE PATCH NICOTINE PATCH SCOPOLAMINE PATCH To TOOS "1 ANTICHOLINERGIC EFFECTS "DRY as a bone" "BLIND as a bat" "HOT as a hare" + BEQ alice in Wonderland" BLIND...
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Alternative transcript:
as a Bar тао ORY as a Bone HOT as a hare ReD as a BeeT 7 HOMATROPINE, CYCLOPENTOLATE, TROPICAMIDE opthalmoscopic examination IPRATROPIUM, TOTROPIUM 3 blockers (for bronchodilation) → Quaternary derivative of atropine → More peripheral effects (lungs), less CNS effects • Asthma t PIRENZEPINE peptic ulcer • BENZTROPINE,TRIHEYYLPHENIDYL, BIPERIDEN→Parkinson's Disease а на пер DARIFENACIN, PESOTERIDINE, OXYBUTYNIN, SOLIFENACIN, TOLTERODINE, TROSPIUM CHLORIDE Overactive bladder blocks Nn/g GANGLIONIC BLOCKERSONEUROTRANSMISSION •NICOTINE · HEXAMETHONIUM, MECANULAMINE, TRIMETHAPMAN (HMT)* BEQ LOBELINE from Indian tobacco ↓ Ganglionic blockers • T NEUROMUSCULAR BLOCKERS • NON- DEPOLARIZING, COMPETITIVE REVERSIBLE → muscle relaxants Tubouurarine Cis- a tracurium ISOQUINOLINE: Atracurium, Tubocurarine STEROIDAL: Pancuronium, Rocuronium •●Fastest) metabolism (Vant-Hoff reaction) DEPOLARIZING IRREVERSIBLE, NON-COMPETITIVE SUCUNYLCHOLINE only depolarizing muscle relaxant used) causes MALIGNANT HYPERTHERMIA • SEIZURES SPASM .PARALYSIS • ] LIFE THREATENING! excessive release of calcium due to overactivation RYANODINE receptor +2 TX DANTROLENE Ca Channel blocker 1 : Ryanodine receptor blocker