Cholinergic Receptor Inhibitors Flashcards

1
Q

Cholinergic Receptor MOA

A

Drugs that bind to cholinergic receptors, but do not trigger usual receptor mediated response

Types:

  1. Muscarinic receptor antagonists
  2. Ganglionic antagonists
  3. Neuromuscular blockers
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2
Q

Muscarinic Receptor Antagonist MOA

A
  1. Inhibits muscarinic functions
  2. Primarily affects the parasympathetic NS
    excp. salivary and sweat glands
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3
Q

Ganglionic Blockers MOA

A

Block nicotinic receptors for both the sympathetic and parasympathetic ganglia. Rarely used clinically bc response is wide and unpredictable

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4
Q

Neuromuscular Junction Blockers MOA

A
  1. Block cholinergic transmission between motor nerve endings and nicotinic receptors on the neuromuscular end plate of skeletal muscle
  2. May be an agonist or antagonist
  3. Clinically useful during surgery as a muscle relaxant
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5
Q

Common Side Effects of Muscarinic Receptor Antagonists

A
  1. Blurred vision
  2. Confusion
  3. Constipation
  4. Urinary Retention
  5. Mydriasis
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6
Q

Atropine MOA

A

Muscarinic receptor antagonist via competitive inhibition

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7
Q

Atropine Clinical Indications

A
  1. Bradycardia
  2. AV Block
  3. IBS
  4. Antisecretory agent
  5. Ocular inflammation
  6. Antidote for AChesterase inhibitor poisoning
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8
Q

Atropine Effects on the Eye

A
  1. Eye exam relaxant
  2. Blocks all cholinergic activity in the eye
  3. Results in mydriasis, unresponsiveness to light and cycloplegia (inability to focus near vision)
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9
Q

Atropine Effects on the GI System

A
  1. Used as an antispasmodic to reduce activity of GI tract (relax GI)
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10
Q

Atropine Effects on the Urinary System

A
  1. Reduces hypermotility states of the bladder (relaxes bladder)
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11
Q

Atropine Effects on the Cardiovascular System

A
  1. Increase heart rate and conduction velocity

2. Causes smooth muscle relaxation

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12
Q

Atropine Effects on Secretory Activity

A
  1. Blocks salivary glands, decreasing secretion (used to dry secretions in upper and lower respiratory tracts prior to surgery)
  2. Produces xerostomia: dryness of mucous membranes
  3. Decreases activity of sweat and lacrimal glands
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13
Q

Atropine Overdose Mnemonic

A
  1. Dry as a bone: decreased secretions, sweat, and tears
  2. Blind as a bat: blockade of pupillary accommodation, and excessive dilation
  3. Red as a beet: Dilation of cutaneous vessels in upper body
  4. Mad as a Hatter: Inhibition of CNS muscarinic receptors with confusion and hallucinations
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14
Q

Benzetropine (Cogentin) MOA

A

Muscarinic receptor antagonist

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15
Q

Benzetropine (Cogentin) Treatments

A
  1. Parkinson’s Disease: blockage of muscarinic receptors may restore neurotransmitter balance in basal ganglia
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16
Q

Benzetropine (Cogentin) Side Effects

A
  1. Mood Changes
  2. Xerostomia: dryness of mucous membranes
  3. Visual problems
17
Q

Scopalamine MOA

A

Muscarinic receptor antagonist

18
Q

Scopalamine Treatments

A

Motion sickness prophylaxis. Blocks short term memory

19
Q

Ipatropium (Atrovent) MOA

A

Muscarinic receptor antagonist, causes bronchodilation and dries respiratory secretions

20
Q

Ipatropium (Atrovent) Treatments

A

Asthma and COPD: Causes bronchodilation and dries respiratory secretions

21
Q

Titropium (Spiriva) MOA

A

Muscarinic receptor antagonist, causes bronchodilation and dries respiratory secretions

22
Q

Titropium (Spiriva) Treatments

A

Asthma and COPD: Causes bronchodilation and dries respiratory secretions

23
Q

Dicyclomine (Bentyl) MOA

A

Muscarinic Receptor Antagonist

Blocks parasympathetic stimulation of enteric nervous system

24
Q

Dicyclomine Treatments

A
  1. IBS. Reduces GI motility and tone, and relaxes smooth muscle
25
Q

Tolterodine (Detrol)

A

Muscarinic Receptor Antagonist

26
Q

Tolterodine (Detrol) Treatments

A
  1. Transient cystitis
  2. Post-operative bladder spasms
  3. Incontinence
27
Q

Tropicamide (Mydriacyl) MOA

A

Muscarinis Receptor Antagonist

28
Q

Tropicamide (Mydriacyl) Treatments

A
  1. Eye exam relaxant
  2. Blocks all cholinergic activity in the eye
  3. Results in mydriasis, unresponsiveness to light and cycloplegia (inability to focus near vision)
29
Q

Tubocarine (Curare) MOA

A

Non-depolarizing Neuromuscular (Nicotinic) antagonist. Competitive inhibitor

30
Q

Tubocarine (Curare) Treatments

A
  1. Paralytic agent that lasts for 30-60 minutes

2. Used as a surgical muscle relaxant w/o deep anesthesia

31
Q

Succinylcholine (Anectine) MOA

A
  1. Super-agonist: Overstimulation of nicotinic receptor, leading to desensitization of muscle unit to further ACh stimulation
32
Q

Succinylcholine (Anectine) Treatments

A
  1. Paralytic agent that lasts for 5-10 minutes

2. Used as muscle relaxant for short procedures such as trachial intubation

33
Q

Mivacurium (Mivacron) MOA

A

Non-depolarizing Neuromuscular (Nicotinic) antagonist. Competitive inhibitor

34
Q

Mivacurium (Mivacron) Treatments

A
  1. Used as a surgical muscle relaxant w/o deep anesthesia
35
Q

Botulism Toxin A MOA

A
  1. Blocks release of ACh at the synapse by inhibiting/degrading SNAP 25. SNAP 25 mediates the fusion of the synaptic vesicle with the presynaptic membrane
36
Q

Botulism Toxin A Treatments

A
  1. Can affect both voluntary and involuntary muscles
  2. Cosmetic surgery: reduce frown lines and wrinkles
  3. Reduce misalignment of eyes in strabismus
  4. Achalasia: Improve esophageal contractions
  5. Oromandibular dystonia (spasms of face, jaw, and neck)
37
Q

Tolterodine (Detrol) MOA

A

Blocks muscarinic receptors

38
Q

Tolterodine (Detrol) Therapeutics

A
  1. Transient Cystitis

2. Postoperative bladder spasms and incontinence

39
Q

Tolterodine (Detrol) SE

A

General block of muscarinic functions