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
Rivastigmine
AChE inhibitors
MOA: Centrally acting AChE inhibitor
Uses: Alzheimer’s
Galantamine
AChE inhibitors
MOA: Centrally acting AChE inhibitor
Uses: Alzheimer’s
Pralidoxime
Reactivator of AChE
Chemical: Synthetic compound
Effects: Reactivate inhibited AChe after organophosphate poisoning (before ageing) ,short lived spontaneously reversible. Postively charged( doesn’t enter CNS)
Uses: carbamate intox.
Atropine
Muscarinic Agonist
Chemical: Belladonna Alkaloids, Tertiary Amine can cross BBB
Effects: mydriasis, decreases GI motility, decreases bladder, Low dose: bradycardia High dose: tachycardia, decreases salivary secreations
Uses: Antisialogogue, OD of cholinergic, Mushroom poisoning
AE:Atropine flush, dry mouth, blurry vision, constipation, confusion, delirium.
Scopolamine
Muscarinic Antagonist
Chemical: Belladonna Alkaloids, Tertiary Amine can cross BBB
Effects; greater actin on CNS than Atropine,Sedation but at high doses: excitement
Uses: DOC for motion sickness
AE:Blocks short term memory, Atropine flush, dry mouth, blurry vision, constipation, confusion, delirium.
Ipratropium/Tiotropium
Muscarinic Antagonist
Chemical: QAC
Effects: Bronchodilation(M3)
Uses: COPD, Asthma
AE:Atropine flush, dry mouth, blurry vision, constipation, confusion, delirium.
Glycopyrrolate
Muscarinic Antagonist
Chemical:QA
Uses: Orally inhibit GI motility, prevent bradycardia during surgery
AE:Atropine flush, dry mouth, blurry vision, constipation, confusion, delirium.
Homatropine
Muscarinic Antagonist
Chemical: Tertiary amine(can cross BBB)
Effects: Mydriasis and cycloplegia
Uses:
AE:Atropine flush, dry mouth, blurry vision, constipation, confusion, delirium.
Tropicamide
Muscarinic Antagonist
Chemical: Tertiary amine(can cross BBB)
Effects: Mydriasis and cycloplegia
Uses:
AE:Atropine flush, dry mouth, blurry vision, constipation, confusion, delirium.
Benztropine
Muscarinic Antagonist
Chemical: Tertiary amine(can cross BBB)
Effects: Restore, balance input after loss of dopaminergic neurons in nigrostriatal pathway
Uses: Parkinsonism, Extrapyramidal effects of antiphysch.
AE:Atropine flush, dry mouth, blurry vision, constipation, confusion, delirium.
Trihexyphenidzyl
Muscarinic Antagonist
Chemical: Tertiary amine(can cross BBB)
Effects: Restore, balance input after loss of dopaminergic neurons in nigrostriatal pathway
Uses: Parkinsonism, Extrapyramidal effects of antiphysch.
AE:Atropine flush, dry mouth, blurry vision, constipation, confusion, delirium.
Tolterodine
Muscarinic Antagonist
Chemical: Tertiary amine(can cross BBB)
Effects: relaxes smooth mm.
Uses: overactive bladder
AE:Atropine flush, dry mouth, blurry vision, constipation, confusion, delirium.
Tubocurarine
Nicotinic Receptor Antagonist
MOA: Non-depol., competitive antagonist bind to Nm
Effects: muscle weakness
Uses: Anesthesia
AE: block M receptors, increase Histamine release
Succinylcholine
Nicotinic receptor Antagonist
MOA: depol. binds to NM, desensitization
Uses: rapid endotracheal intubation, ECT
AE: Malignant hyperthermia TXT Dantrolene ( blocks Ca releases decreasing heat produce and tone of mm)
Hemicholinium-3
Presynaptic Cholinergic Antagonist
MOA: blocks CHT1-prevents uptake and scythe of ACh
uses: research
Vesamicol
Presynaptic Cholinergic Antagonist
MOA: blocks vesicular ACh-H+ anti transporter (VAChT)-prevents storage of ACh
Uses:Research
Botulinum Toxin
Presynaptic Cholinergic Antagonist
MOA: Neurotoxin produced by C. botulinum prevents synaptic fusion of the vesicle with axon terminal(via synaptobrevin)- inhibits ACh release
Uses: local injection TXT condtion w/XS mm tone, Wrinkles
