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FTM2 > Cholinergic Agonist/Antagonists > Flashcards

Cholinergic Agonist/Antagonists Flashcards

1
Q

Acetylcholine

Coline Ester

A

*Muscarinic and nicotinic agonist

Use: obtain miosis after delivery of the lens in cataract Sx

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2
Q

Metacholine

Choline Ester

A

Muscarinic Agonist

Use: Dx of bronchial airway hyperactivity in subjects who do not have clinically apparent asthma

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3
Q

Bethanechol

Choline Ester

A

Muscarnic agonist

Use: Post-OP urinary retention, and atony of the urinary bladder

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4
Q

Carbachol

Choline Ester

A

Muscarnic and nictotinic agonist
Uses:
1. Miosis during surgery
2. Reduce intraocular pressure after cataract Sx

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5
Q

Pilocarpine

Natural Alkaloids

A

Partial muscarnic agonist
Tertiary amine
Stable to hydrolysis by AChE

Use:
1. Second line of open angle glaucoma
2. Management of acute angle-closure glaucoma
3. Tx of dry mouth by radiotherapy or Sjogren’s Syndrome

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6
Q

Nicotine

Natural Alkaloids

A

Selective Nicotinic Agonist
Tertiary amine

Action:
Low dose: ganglionic stimulation-resembles simultaneous para/sympathetic nervous system

High dose: ganglionic blockade and neuromuscular blockade

Uses: Smoking Cessation Therapy

Can depolarize autonomic ganglia-resulting first in stimulation and then paralysis

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7
Q

Edrophonium

Anticholinesterase

A

binds reversilby to the active site of the enzyme (no covalent bond)
-inhibition is short lived

Uses:
1. To Dx myasthenia gravis-leads to rapid increase in muscle strength.
2. Reverse neuromuscular blocks produced by non-depolarizing muscular blockers

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8
Q

What is the effect on the CVS of Anticholinesterases?

A

Minimal-due to vascular beds that lack cholinergic innervation

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9
Q

Physostigmine

Anticholinesterase

A

Tertiary amine (can enter and stimulate CNS)

Uses: Tx of overdoses of anticholinergic drugs

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10
Q

Neostigmine

Anticholinesterase

A

Quaternary ammonium

Uses:
1. Post-Op Urinary retention
2. Reversal of effects of non-depolarizing neuromuscular blockers after surgery
3. Tx of myasthenia gravis

Off label use of Tx of non-obstructive ileus

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11
Q

Pyridostigmine

Anticholinesterase

A

Quaternary Ammonium-does not enter CNS

Uses: Myasthenia Gravis treatment

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12
Q

Echothiophate

Organophosphate

A

Rarely used for glaucoma

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13
Q

What are the 3 acetylcholinesterase inhibitors used in the treatment of ALzheimer’s Disease?

A
  1. Donepezil
  2. Rivastigmine
  3. Galantamine

Tertiary amines–> cross BBB

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14
Q

What are the two natural Alkaloids?

A
  1. Atropine
  2. Scopolamine
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15
Q

Atropine action

Muscarinic Receptor Antagonists: Belladone Alkaloids

A

**Reversible competitive antagonist **
Tertiary amine: both central and peripheral muscarinic blocker

Action: M3 blockade
Eye: Mydriasis & cycloplegia
GI: reduce gastric motility
Urinary: decrease hypermotility of urinary bladder
Secrections: block (sweat, salivary…)
M2 blockade: moderate to high doses cause tachycardia

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16
Q

What are the 3 uses for Atropine?

A
  1. Antidote for cholinergic agonists (organophosphate poisoning)
  2. Block respiratory secretions prior to surgery
  3. Antispasmodic: relax GI tract/bladder
17
Q

What are the adverse effects of Atropine?

A

Dry mouth, tachy, blurred vision, constipation, tachycardia, urinary retention, sandy eyes

CNS effects: restlessness, confusion, hallucinations, delirium-similar to hallucinigens

18
Q

Pralidoxime

Reactivator of AChE

A

Split phosphorous-enzyme bond

Adjunct therapy in organophosphate poisoning

19
Q

Scopolamine uses and mechanism of action

Belladona Alkaloid

A

Used to treat motion sickness-enters vomiting center (M1), mydriasis and cycloplegia in diagnositc procedures
* Tertiary amine
* Blocks short-term memory
* Longer duration of action compared to atropine

Produces sedation in contrast to atropine

20
Q

Ipratropium/Tiotropium

Quaternary Ammonium Muscarinic Antagonist

A

Uses: Tx of COPD, Asthma
Bronchodilator

21
Q

Tropicamide, Cyclopentolate, Homatropine

Tertiary Amine Muscarinic Antagonist

A

Uses: Mydriatics for fundoscopy
Produce mydriases w/ cycloplegia

Short half life compared to atropine (preferred)

22
Q

Glycopyrrolate

A

Quaternary ammonium compound

Uses:
1. Prevention of bradycardia in Sx
2. COPD
3. Adjunctive therapy of peptic ulcer
4. Severe drooling in neuro cases

23
Q

Contraindications of Antimuscarinic Agents? (2)

A
  1. Angle-closue glaucoma
  2. BPH/elderly patients
  • Elderly are very sensitive to cholinergic blockade-causes acute encephalopathy, falls, urinary retention, exacerbation of functional/behavior/cognitive deficits
24
Q

Benztropine, Trihexyphenidyl

Treatment only

A

Treatment of Parkinson’s Disease and Extrapyramidal Symptoms associated w/ antipsychotic meds

Tertiary Amine Muscarinic Antagonist

25
Q

Oxybutynin, Tolterodine

Treatment only

A

Overactive bladder

Tertiary amine

Muscarinic Antagonist

26
Q

Hexamethonium

Ganglion Blocker

A

Previously used for HTN but d/t A/E replaced by other anti HTN
Pharm properties: remove dominant control of the ANS

27
Q

Tubocurarine

Competitive Antagonist (Non-depolarizing blocker)

A

Uses: adjuvant drugs in anaesthesia during surgery to relax skeletal muscle

28
Q

Name the 5 Non-depolarizing NMJ blockers

A
  1. Tubocurarine-prototype
  2. Pancuronium
  3. Rocuronium
  4. Vecuronium
  5. Mivacurium-short acting (hydrolysis by plasma butyrylcholinestrase
29
Q

What is the action of NMJ non depolarizing blockers?

A

First cause motor weakness–>skeletal muscles become totally flaccid and inexcitable to stimulation

Action can be overcome by increasing concentration of ACh-Edrophonium and Neostigmine

30
Q

Succinylcholine

Agonist (Depolarizing Blocker)

A

Uses: Endotracheal intubation
ECT

Rapid blockade (<1 min onset, lasts 5 min)
Fasciculations
Not metabolized by AChE leading to flaccid paralysis

31
Q

What happens to patients with low-activity geneetic polymorphism of the enzyme butyrlcholinesterase?

A

Longer time to metabolise Succinylcholine-mechanical ventilation until muscle function returns to normal

32
Q

What are the adverse effects of Succinylcholine?

(4)

A
  1. Muscle pain
  2. Hyperkalemia-loss of tissue potassium d/t depolarizaqtion
  3. Increased intraocular pressure
  4. Malignant hyperthermia-excessive release of Ca2+ from SR. Defect in Ryanidine Receptor gene (RYR1)
33
Q

Treatment for Malignant Hyperthermia?

A

Dantrolene

34
Q

Inhibitor of ACh Release

A

Botulinum Toxin
Uses:
1. Cosmetic Tx of facial wrinkles
2. Severe muscle spasms (Ex: Blepharospasm-inability to open eyes)

Acts presynaptically

35
Q

Inhibitor of ACh Synthesis

A

Hemicholinium-3

Prevents uptake of choline to make ACh
Research tool

36
Q

Inhibitor of ACh Storage

A

Vesamicol

Blocks ACh-H+ antiporter using transport ACh into vesicles
Research tool

37
Q

Mecamylamine

A

Ganglion Blocker used as an antihypertensive agent

38
Q

General properties of Neuromuscular blockers (4)

A
  1. Block at Nm receptor on skeletal muscle
  2. Highly polar-poorly soluble in lipid
  3. Do not cross BBB or enter cells
  4. Always given IV/IM-inactivated if given PO

FTM2 (10 decks)

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