Cholinergic Pharmacology II Flashcards

1
Q

Types of cholinoceptor-blocking drugs (3)

A
  1. Muscarinic Receptor antagonists
  2. Nicotinic receptor antagonists (NN and NM)
  3. Neuromuscular blocking drugs (NM only)
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2
Q

Muscarinic Receptor antagonists (3)

A
  1. Atropine
  2. Ipratropium
  3. Benztropine
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3
Q
Pharmacologic effects of atropine
Secretory
Vision
Temperature
Cardiovascular
Behavioral
GU
Vascular effects
BP effects
A
  1. decreased secretions (salivary, bronchiolar, sweat)
    mydriasis, and cycloplegia
    hyperthermia
    tachycardia
    sedation
    urinary retention & constipation
    behavioral excitation & hallucinations
  2. Completely counteracts peripheral vasodilation caused by choline esters
  3. Does not affect blood pressure when given alone
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4
Q

Clinical uses of atropine

A
  1. Management of AChE inhibitor overdose
  2. Antispasmodic in GI tract
  3. Prevention of vagal reaction
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5
Q

Antidote for atropine overdose

A

Physostigmine

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6
Q

Ipratropium properties (2)

A
  1. Non-selective muscarinic antagonist

2. Acts on M3

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7
Q

Ipratropium effects and clinical uses

A
  1. Decreases bronchoconstriction and bronchosecretion

2. Used in COPD and asthma

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8
Q

Benztropine (Cogentin) uses (2)

A
  1. Re-establish dopaminergic-cholinergic balance in patients with Parkinson’s Disease
  2. Decrease GI/GU secretions, decrease motility, INCREASE heart rate
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9
Q

Nicotinic Receptor Antagonists (2)

A

Hemamethonium and Mecamylamine

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10
Q

Effects of nicotinic receptor antagonists

A

Reduces the predominant autonomic tone

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11
Q

Non-depolarizing NM blocker? Depolarizing NM blocker?

A

D-Tubocurarine

Succinylcholine

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12
Q

Why do the NM blockers not enter the CNS?

A

Because they are quaternary amines and highly ionized

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13
Q

3 mechanisms by which D-Tubocurarine blocks the NMJ?

A
  1. Binds to receptor (competes with ACh in low doses)
  2. Blocks channel (higher doses)
  3. Blocks pre-junctional Na+ channels which decreases ACh relsease
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14
Q

Prototype drug for depolarizing NM blocker?

A

Succinylcholine

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15
Q

Phase 1 blockade for succinylcholine

A

Binds to the NM causing strong, persistent depolarization. This leads to paralysis due to chronic activation

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16
Q

Phase 2 blockade for succinylcholine

A

End plate finally repolarized but does not depolarize again easily. Known as desensitization

17
Q
Side effects of NM blockers (depolarizing or non-depolarizing)
Cardiovascular
Potassium
Intraocular pressure
Gastric pressure
Muscles
A
Hypotension due to histamine release. Severe hypotension occurs with high doses
Hyperkalemia
Increased intraocular pressure
Increased gastric pressure
Muscle pain