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Pharmacology: Exam 3 > Cholinergics and Anti Cholinergics > Flashcards

Cholinergics and Anti Cholinergics Flashcards

1
Q

Non Depolarizing Neuromuscular Blockers (NMBs)

A

Antagonists at muscular nicotinic receptors:
Competitively binds to nicotinic receptors on motor end plate (skeletal muscle) to antagonize ACh, resulting in blockade of neuromuscular transmission

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2
Q

Result of Non Depolarizing NMBs

A

Skeletal Muscle Relaxation

eyes, then head and neck, to torso and limbs

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3
Q

Non Depolarizing NMBs Drugs

A 
Atracurium
Cisatracurium
Rocuronium
Vecuronium
Pancuronium
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4
Q

Non depolarizing NMBs ADE

A

-Prolonged apnea via diaphragm paralysis (prevent by immediately terminating NMB effect when procedure ends)

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5
Q

Succinylcholine

A

“Depolarizing” NMB- mimics ACh and depolarize (Ca influx) motor end plate- Skeletal muscle relaxation (paralysis)

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6
Q

Succinylcholine ADR

A

Malignant Hyperthermia: an uncontrolled release of calcium from sarcoplasmic reticulum
-Generalized rigidity, increased oxygen demand, lactic acidosis, hyperthermia, tachycardia, fever, arrhythmia

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7
Q

Dantrolene

A

Treats Malignant Hyperthermia (from Succinylcholine)

  • directly interferes with calcium channel ion release from SR in skeletal muscle cells
  • “uncouples” excitation-contraction process
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8
Q

Anti Cholinergic Toxidrome

A 
Hyperthermia
Dry mucous membranes
Skin flushed
Confusion, delirium
Mydriasis, blurred vision
Seizures
Urinary retention
tachycardia
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9
Q

Onabotulinumtoxin A (Botox) MOA

A
  • Inhibits exocytosis of ACh: binds pre synaptic proteins (VAMPs and SNAPs) which impairs vesicle fusion (which normally would permit ACh release)
  • Result in muscle denervation and a local reduction in muscle activity
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10
Q

Onabotulinumtoxin A Therapeutic Use

A

RELIEVES MUSCLE ACTIVITY

  • Strabismus, blepharospasm, wrinkles, hyperhidrosis
  • Migraine prophylaxis; neurogenic/overactive bladder
  • Spasticity; urinary incontinence;sialorrhea
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11
Q

Natural Substance: Muscarine

A
  • Mimics the effects of ACh at the post ganglionic receptor
  • Has NO effect on skeletal muscle or autonomic ganglia (nicotinic receptors)
  • Natural Antagonist: Belladonna
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12
Q

Natural Substance: Nicotine

A
  • Mimics effects of ACh on Skeletal muscle and autonomic ganglia
  • Can potentially stimulate both SANS and PANS ganglia
  • Has NO effect on post ganglionic (muscarinic) receptors
  • Natural antagonist: Curare
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13
Q

Cholinergic Receptors: Muscarinic

A

M1-M5

  • smooth muscle, heart, exocrine glands
  • G protein coupled receptor (GPCR)
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14
Q

Cholinergic Receptors: Nicotinic

A

Neuronal (Nn)/Muscular (Nm)

  • autonomic ganglia (n; neuronal)
  • skeletal muscle (m; muscular)
  • ion channel receptor
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15
Q

What is the muscarinic agonist effect on the heart?

A

Decreases HR and CV force; treats Tachycardia

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16
Q

What is the muscarinic antagonist effect on the heart?

A

Increases HR/CV force; treats Bradycardia

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17
Q

What is the muscarinic agonist effect on the bronchial smooth muscle?

A

Bronchoconstriction; used in asthma diagnosis

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18
Q

What is the muscarinic antagonist effect on the bronchial smooth muscle?

A

Bronchodilation; used for Asthma or COPD

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19
Q

What is the muscarinic agonist effect on the eyes?

A

Miosis to drain aqueous humor; used for Glaucoma

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20
Q

What is the muscarinic antagonist effect on the eye?

A

Mydriasis; used in Retinal exams

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21
Q

What is the muscarinic agonist effect on the glands?

A

increases secretions; treats xerostomia and sjoren’s

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22
Q

What is the muscarinic antagonist effect on the glands?

A

decreases secretions; treats COPD, Pre Op, Rhinorrhea

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23
Q

What is the muscarinic agonist effect on the GI tract?

A

increases GI motility; used for Gastric Atony

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24
Q

What is the muscarinic antagonist effect on the GI tract

A

decrease GI motility; used for GI spasms

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25
Q

What is the muscarinic agonist effect on the Bladder?

A

Increases urination; treats post op urinary retention

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26
Q

What is the muscarinic antagonist effect on the Bladder?

A

Decreases urination; treats overactive bladder

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27
Q

What is the muscarinic agonist effect on vessels?

A

Vasodilation; treats HTN

28
Q

What is the muscarinic antagonist effect on vessels?

A

vasoconstriction; treats hypotension

29
Q

What is the muscarinic agonist effect on CNS?

A

Increase cognition/tremor; treats Alzheimers (only AChI)

30
Q

What is the muscarinic antagonist effect on CNS?

A

CNS depression, decreases tremors; treats Motion sickness and Parkinson’s

31
Q

Muscarinic Agonist: Pilocarpine & Carbachol

A

Helps Glaucoma; reduces IOP by enhancing drainage of aqueous humor

32
Q

Muscarinic Agonist: Pilocarpine; Cevimeline

A

Helps Xerostomia associated with Sjogren’s syndrome or radiation from head and neck cancers

33
Q

Muscarinic Agonist: Bethanechol

A

Post Op/ Postpartum non obstructive urinary retention; atonic neurogenic bladder; gastric atony

34
Q

Muscarinic Agonist: Methacholine

A

Asthma diagnosis

35
Q

Nicotine

A
  • Complex effects as a drug due to non specific activation of autonomic ganglia and skeletal muscle
  • Stimulates mesolimbic DA system (reward pathway)
  • Smoking cessation typically requires gradual reduction in nicotine exposure to prevent withdrawal syndrome
36
Q

Nicotine Toxicity effects

A

Acute Toxicity is Rare

  • Central: convulsions, progression to coma and respiratory paralysis
  • Skeletal: depolarization, rigidity
  • Muscarinic excess resulting from stimulating parasympathetic ganglia
37
Q

Nicotinic Replacement Therapy (NRT)

A
  • Agonist on the Alpha 4 Beta 2 receptors; reduces withdrawal symptoms
  • Types: Gum, Patch, Lozenge, Nasal Spray, Inhaler
  • NRT delivers nicotine slower than smoking
  • Patient should not actively smoke on NRT
38
Q

Varenicline (Chantix) MOA

A

Partial Agonist at the alpha 4 beta 2 neuronal nicotinic receptors

  • “High affinity”; competes with nicotine
  • Suppresses nicotine withdrawal symptoms
39
Q

Varenicline Therapeutic Effects

A
  • Smoking cessation

- can smoke initially during therapy but must set quit date

40
Q

Varenicline ADEs

A
  • Vivid/abnormal dreams; insomnia, N/V; Constipation
  • Neuropsychiatric disorders?
  • cardiovascular disorders?
41
Q

Bupropion

A
  • Primarily used as an anti depressant: inhibits reuptake of dopamine and norepinephrine
  • Increased NE may reduce nicotine withdrawal symptoms
  • Increased DA may reduce nicotine cravings and urge to smoke
42
Q

Bupropion ADE

A
  • Agitation, Insomnia, Irritability, dry mouth, nausea, tachycardia
  • Can lower seizure threshold (dose limit)
  • Weight loss
43
Q

Role of Acetylcholinesterase (AChE)

A

Inactivation of ACh by AChE

44
Q

Cholinesterase Inhibitors (AChI) MOA

A

Reversible inhibition of AChE: increased [local ACh] at receptors

45
Q

AChI Therapeutic Uses

A

Alzheimer’s Disease; Myasthenia Gravis
Neuromuscular Blockade reversal
Anticholinergic toxidrome

46
Q

Alzheimer’s Disease (AD)

A

Cholinergic neurons are predominantly lost

  • drugs aim to increase ACh activity/ concentration
  • AD patients especially sensitive to anti ACh drugs
47
Q

AChI Therapy in Alzheimer’s Disease

A
  • Drugs must cross BBB (lipophilic)

- AChI’s in AD are more selective for AChE in the brain

48
Q

AChI Drugs for Alzheimers

A

Tacrine (off market)
Rivastigmine
Galantamine
Donepezil

49
Q

AChI for Alzheimers ADE

A 
Mostly Muscarinic:
-Bradycardia (dose limiting)
-Dizziness, lightheadedness
-Increased urinary frequency
-GI: nausea, diarrhea, potential GI bleed
To use with food
50
Q

Myasthenia Gravis

A

Autoimmune disease affecting skeletal muscle at neuromuscular junction (NMJ; muscular nicotinic receptors) which diminishes ACh activity

51
Q

AChI’s in Myasthenia Gravis

A

Diagnose with short acting AChI (edrophonium)

  • treatment with neostigmine, pyridostigmine, or ambenonium
  • Don’t cross BBB
52
Q

Non Alzheimer’s AChI Drugs

A

Used for Myasthenia Gravis and NMB reverse

  • Edrophonium
  • Neostigmine
  • Pyridostigmine
  • Physostigmine
  • Ambenonium
53
Q

Non AD AChI: ADEs for muscarinic

A

salivation, urination, bradycardia, bronchoconstriction, abdominal cramping

54
Q

Non AD AChI: ADEs for nicotinic

A

Muscle Fasciculation/Cramping

55
Q

“Cholinergic Crisis”

A

Too much ACh in NMJ (need less)

  • continuous stimulation: permanent depolarization
  • concern for respiratory paralysis
56
Q

“Myasthenic Crisis”

A

Not enough ACh in NMJ (need more)

-similar to non depolarizing neuromuscular blockade

57
Q

Organophosphates: Irreversible AChIs Drugs

A
  • Pesticides: Malathion, Parathion
  • Nerve Gas: Sarin
  • Herbicides
58
Q

Irreversible AChI MOA

A

Covalent binding to enzyme active site leading to irreversible inhibition of AChE

  • Leads to non specific increase in ACh at peripheral and central muscarinic and nicotinic receptor site
  • Cholinergic Toxidrome
59
Q

Cholinergic Toxidrome: Muscarinic SLUDGE/BBB

A

Salivation, Lacrimation, Urination, Diaphoresis, GI upset (diarrhea), Emesis
Bronchorrhea, Bronchospasm, Bradycardia

60
Q

Cholinergic Toxidrome: Muscarinic DUMBELS

A

Defecation/Diarrhea, Urination, Miosis, Bronchorrhea,/Bronchospasm/Bradycardia, Emesis/Excitation, Lacrimation, Salivation/Sweating

61
Q

Side effects of increased stimulation of nicotinic receptors

A
  • Muscle fasciculation, weakness, diaphragm failure

- CNS effects: anxiety, labile affect, ataxia, tremors, seizures

62
Q

Primary Treatment of Organophosphate Toxicity

A
  • Airway control, adequate oxygenation
  • Decontamination, removal of all clothing
  • Management of seizure: diazepam
63
Q

Pralidoxime (2-PAM)

A
  • Enzyme reactivation prior to “aging” of enzyme
  • “cholinesterase regenerator”-breaks phosphorus enzyme bond if given in an appropriate time window based on particular organophosphate and aging rate
64
Q

Atropine

A
  • muscarinic receptor antagonist

- Blocks ACh to stop effects of increased ACh in synapse: reduces SLUDGE/DUMBELS

65
Q

Anti-Cholinergic Therapeutic uses

A
  • Nicotinic receptor antagonism
  • Neuromuscular blocker (NMB; muscular nicotinic)
  • Muscarinic receptor antagonism (Asthma/COPD, Overactive Bladder, Parkinson’s)

Pharmacology: Exam 3 (5 decks)

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