Cholinergic Drugs Flashcards
Actylcholine
Direct Acting Agonist
Chemical: Esters of Choline(poor CNS absorb)
Receptors: N&M
Effects: Low dose: Tachycardia, High Dose: Bradycardia. With Atropine Symp. like effect on N receptors
Uses: rapid miosis after cataracts surgery
AE: Muscarinic Syndrome, DUMBBELLS
Bethanechol
Direct Acting Agonist
Chemical: Ester of Choline(poor CNS absorb)
Receptors: M
Effects:activates bowel and bladder
Uses: Post op urinary retention, atony of bladder, congenital megacolon
AE:AE: Muscarinic Syndrome, DUMBBELLS
Carbachol
Direct Acting Agonist
Chemical: Ester of Choline ( poor CNS absorb)
Receptors: M/N
Effects: Miosis and contraction of ciliary mm.
Uses: Miosis during surgery,. decrease intraocular pressure, Glaucoma( after Pilocarpine)
AE: Muscarinic Syndrome, DUMBBELLS
Methacholine
Direct Acting Agonist
Chemical: Ester of Choline
Receptors: M and little N
Effects:
Uses: Diagnosis of bronchial airway hyperreactivity
AE: Muscarinic Syndrome, DUMBBELLS
Muscarine
Direct Acting Agonist
Chemical: Natural Alkaloid
Receptor:M
Effects: no clinical use
Pilocarpine
Direct Acting Agonist
Chemical: Natural Alkaloid
Receptor: Partial M, Tertiary amine(cross BBB)
Effects: contraction of ciliary mm, Secretions from glands
Uses: Glaucoma after Timol, dry mouth d/t radiotherapy or Sjogren’s
AE:CNS disturbances, Sweating, Salivations
Nicotine
Direct Acting Action
Chemical: Ganglion Stim.
Receptor: Nn> NM, Tertiary amine can cross BBB
Effects: CVS- Sympathomimetic, GI/UG- Parasymp.
Uses: smoking cessations
AE: Nicotinic Poisoning, Hypotension with weak rapid, irregular phase
Erdophonium
AChE inhibitors
Chemical: Simple Alcohol(QAC), poor CNS absorb
MOA: reversible binding to active site of AChE and butycholinesterase
Effects: CVS- predominate PNS action, NMJ- increase contraction
Uses: Diag. MG , reverse neuromuscular blockage
AE: CNS- coma, Resp Arrest,
Physostigmine
AChE inhibitors
Chemical: Carbamates, Tertiary Amine(crosses BBB)
MOA: forms covalent bond w/ AChE
Effects: CVS- predominate PNS action (predominate), NMJ- increase contraction
Uses: TXT for anticholinergic overdose
AE: High dose- paralysis, CNS effects, Contraindicated in TCA overdose
Neostigmine
AChE inhibitors
Chemical: Carbamates-QAC
MOA:Forms covalent bond with AChE
Effects:CVS- predominate PNS action (predominate), NMJ- increase contraction
Uses: Reverses the neuromuscular blockade caused by blocker like Tubocurarine, 2nd like for MG. TXT urinary retention
AE:Salivation, Flushing, hypotension, nausea, brochospasm
Pyridostigmine
AChE inhibitors
Chemical: Carbamates-QAC
MOA:Forms covalent bond with AChE
Effects:CVS- predominate PNS action (predominate), NMJ- increase contraction
Uses: MG (most common)
AE:AE:Salivation, Flushing, hypotension, nausea, brochospasm
Echothiophate
AChE inhibitors
Chemical: organophosphates synthetic
MOA: phos. active site making extremely stable covalent bond
Effects:
Uses: chronic open-angle glaucoma.
AE:
Sarin
Chemical: organophosphates synthetic
MOA: phos. active site making extremely stable covalent bond, can cross BBB
Effects: Nerve agent(most potent synthetic toxic agent know)
Uses: Terrorism
AE: CNS toxicity, Organophosphate overdose
Sarin
AChE inhibitors
Chemical: organophosphates synthetic
MOA: phos. active site making extremely stable covalent bond, can cross BBB
Effects: Nerve agent(most potent synthetic toxic agent know)
Uses: Terrorism
AE: CNS toxicity, Organophosphate overdose
Donepezil
AChE inhibitors
MOA: Centrally acting AChE inhibitor
Uses: Alzheimer’s