Cholinergic Drugs Flashcards

1
Q

Actylcholine

A

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

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2
Q

Bethanechol

A

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

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3
Q

Carbachol

A

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

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4
Q

Methacholine

A

Direct Acting Agonist

Chemical: Ester of Choline

Receptors: M and little N

Effects:

Uses: Diagnosis of bronchial airway hyperreactivity

AE: Muscarinic Syndrome, DUMBBELLS

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5
Q

Muscarine

A

Direct Acting Agonist

Chemical: Natural Alkaloid

Receptor:M

Effects: no clinical use

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6
Q

Pilocarpine

A

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

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7
Q

Nicotine

A

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

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8
Q

Erdophonium

A

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,

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9
Q

Physostigmine

A

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

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10
Q

Neostigmine

A

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

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11
Q

Pyridostigmine

A

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

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12
Q

Echothiophate

A

AChE inhibitors

Chemical: organophosphates synthetic

MOA: phos. active site making extremely stable covalent bond

Effects:

Uses: chronic open-angle glaucoma.

AE:

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13
Q

Sarin

A

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

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14
Q

Sarin

A

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

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15
Q

Donepezil

A

AChE inhibitors

MOA: Centrally acting AChE inhibitor

Uses: Alzheimer’s

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16
Q

Rivastigmine

A

AChE inhibitors

MOA: Centrally acting AChE inhibitor

Uses: Alzheimer’s

17
Q

Galantamine

A

AChE inhibitors

MOA: Centrally acting AChE inhibitor

Uses: Alzheimer’s

18
Q

Pralidoxime

A

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.

19
Q

Atropine

A

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.

20
Q

Scopolamine

A

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.

21
Q

Ipratropium/Tiotropium

A

Muscarinic Antagonist

Chemical: QAC

Effects: Bronchodilation(M3)

Uses: COPD, Asthma

AE:Atropine flush, dry mouth, blurry vision, constipation, confusion, delirium.

22
Q

Glycopyrrolate

A

Muscarinic Antagonist

Chemical:QA

Uses: Orally inhibit GI motility, prevent bradycardia during surgery

AE:Atropine flush, dry mouth, blurry vision, constipation, confusion, delirium.

23
Q

Homatropine

A

Muscarinic Antagonist

Chemical: Tertiary amine(can cross BBB)

Effects: Mydriasis and cycloplegia

Uses:

AE:Atropine flush, dry mouth, blurry vision, constipation, confusion, delirium.

24
Q

Tropicamide

A

Muscarinic Antagonist

Chemical: Tertiary amine(can cross BBB)

Effects: Mydriasis and cycloplegia

Uses:

AE:Atropine flush, dry mouth, blurry vision, constipation, confusion, delirium.

25
Q

Benztropine

A

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.

26
Q

Trihexyphenidzyl

A

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.

27
Q

Tolterodine

A

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.

28
Q

Tubocurarine

A

Nicotinic Receptor Antagonist

MOA: Non-depol., competitive antagonist bind to Nm

Effects: muscle weakness

Uses: Anesthesia

AE: block M receptors, increase Histamine release

29
Q

Succinylcholine

A

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)
30
Q

Hemicholinium-3

A

Presynaptic Cholinergic Antagonist

MOA: blocks CHT1-prevents uptake and scythe of ACh

uses: research

31
Q

Vesamicol

A

Presynaptic Cholinergic Antagonist

MOA: blocks vesicular ACh-H+ anti transporter (VAChT)-prevents storage of ACh

Uses:Research

32
Q

Botulinum Toxin

A

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