Cardio 1 Med Chem Cholinergics

Pregunta	Respuesta
Image: Carbachol (binary/octet-stream)	Cholinergic agonist Carbachol (isopto-carbachol) C -->N (carbamate) More resistant to hydrolysis mAChRs and nAChRs Topical, glaucoma
Image: Methacholine (binary/octet-stream)	Cholinergic agonist Methacholine (provocholine) Add methyl to B carbon Selective for mAChR S is more potent Asthma diagnosis
Image: Bethanechol (binary/octet-stream)	Cholinergic agonist Bethanechol (Urecholine) Carbamate and methyl Selective mAChRs Postsurgical and postpartum urinary retention and abdominal distention
Image: Pilocarpine (binary/octet-stream)	(Muscarinic agonist) - non classical Pilocarpine (Isopto, Carpine, Salogen) N is in ring Top left C is chiral Easily degraded Glaucoma, dry mouth, sjogren's syndrome
Image: Cavimeline (binary/octet-stream)	(Muscarinic agonist) - non classical Cevimeline (Exovaac) Quinuclidine ring M3 selective Dry mouth, Sjogren's syndrome
Image: Physostigmime (binary/octet-stream)	AChE inhibitors -reversible Physostigmine Carbamate More resistant to hydrolysis (increase half-life) Glaucoma, anticholinergic drug overdsoe
Image: Neostigmine (binary/octet-stream)	AChE inhibitors -reversible Neostigmine Quaternary amine No CNS activity Myasthenia gravis, reverse nerve block, urinary retention
Image: Pyridostigmine Br (binary/octet-stream)	AChE inhibitors -reversible Pyridostigmine Bromide (Mestinon) N is in pyrimidine ring N is positive Oral Myasthenia gravis
Image: Carbaryl (binary/octet-stream)	AChE inhibitors -reversible Carbaryl (Servin) Carbamate NO N!! Toxic to insects
Image: Donepezil (binary/octet-stream)	AChE inhibitor - non classical , reversible Donepezil (Aricept) No carbamate CNS activity, no hepatoxicity, affinity AChE > BChE, Alzheimer's
Image: Rivastigmine (binary/octet-stream)	AChE inhibitor - non classical , reversible Rivastgmine (exelon) Carbamate CNS activity, reversible inhibitor, affinity AChE=BChE, Alzheimer's
Image: Galatmine (binary/octet-stream)	AChE inhibitor - non classical , reversible Galatamine (Razadyne) Phenanthrene derivative Tertiary amine Reversible inhibitor (NO BChE affinity)
Image: Echothiophate (binary/octet-stream)	AChE inhibitor - non classical , irrreversible Echothiophate Iodide (Phospholine) Phosphate = serine target = aging Effective for 4 weeks Glaucoma eye drops
Image: Malathion (binary/octet-stream)	AChE inhibitor - non classical , irreversible Malathion (insecticide) P=S bond Altered to P=O in insects (NOT humans) Kill bugs not hoomans
Image: Pralidoxim (binary/octet-stream)	AChE inhibitor reversal Pralidoxime chloride (2-PAM) Hydroxylamine (N-OH) STRONG nucleophile to cleave phosphate esters in site Reverse irreversible AChE inhibitors BEFORE aging happens
Image: Atropine (binary/octet-stream)	Muscarinic antagonist (anticholinergics) Atropine Bulky side chains Antagonists activity Bradycardia, decrease secretions, ophthalmology, AChE inhibitor poisoning
Image: Scopolamine (binary/octet-stream)	Muscarinic antagonist (anticholinergics) Scopolamine Bulky side chains Antagonist activity Motion sickness
Image: Methscopolamine (binary/octet-stream)	Muscarinic antagonist (anticholinergics) Methscopolamine Quaternary amine NO CNS activity
Image: Tiotropium (binary/octet-stream)	Muscarinic antagonist - synthetic Tiotropium (Spiriva) Ester linkage 2 rings + -OH Bronchodilator for COPD
Image: Ipatropium (binary/octet-stream)	Muscarinic antagonist - synthetic Ipratropium (Atrovet) Ester linkage 1 ring, CH2OH and H Less potent? Bronchodilator for COPD
Image: Trospium (binary/octet-stream)	Muscarinic antagonist - synthetic Trospium (Sanctura) Ester linkage 2rings + OH Bulky on N Overactive bladder
Image: Oxybutynin (binary/octet-stream)	Muscarinic antagonist - synthetic Oxybutynin (Ditropan) Ester linkage 2 rings and OH CΞC Can cross the BBB Overactive bladder
Image: Glycopyrrolate (binary/octet-stream)	Muscarinic antagonist - synthetic Glycopyrrolate (Robinul) Ester linkage 2 rings + OH Preop dec secretions, hyperhidrosis
Image: Trihexyphenidyl (binary/octet-stream)	Muscarinic antagonist - synthetic Trihexyphenidyl (Artane) Amino-alcohol 2 rings and OH Parkinson's syndrome, EPS of antipsychotics
Image: Tolterodine (binary/octet-stream)	Muscarinic antagonist - synthetic Tolterodine (Detrol) Amino-alcohol Urinary incontinence/overactive bladder
Image: Fesoterodine (binary/octet-stream)	Muscarinic antagonist - synthetic Fesoterodine (Toviaz) Amino alcohol + ester Nonselective M activity ** lyse ester to get active drug Urinary incontinence/overactive bladder
Image: Orphenadrine (binary/octet-stream)	Muscarinic antagonist - synthetic Orphenadrine (Norflex) Amino-ether2 rings and H Non-selective anticholinergic and antihistamine activity Muscle pain, and improve muscle control for Parkinson's
Image: Benztropin (binary/octet-stream)	Muscarinic antagonist - synthetic Benztropin (Cogentin) 2 rings and H Some antihistamine Parkinson's and dec EPS
Image: Umeclidine 1 (binary/octet-stream)	Muscarinic antagonist - synthetic Umeclidinium Long lipophilic tail Increase action time/long acting COPD
Image: Aclindinium (binary/octet-stream)	Muscarinic antagonist - synthetic Aclidinium Long lipophilic tail Increase action time/long acting COPD

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