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Pharmacology: Exam 3 > Cholinergics and Anti Cholinergics > Flashcards

Cholinergics and Anti Cholinergics Flashcards

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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
What is the muscarinic agonist effect on the Bladder?
Increases urination; treats post op urinary retention
26
What is the muscarinic antagonist effect on the Bladder?
Decreases urination; treats overactive bladder
27
What is the muscarinic agonist effect on vessels?
Vasodilation; treats HTN
28
What is the muscarinic antagonist effect on vessels?
vasoconstriction; treats hypotension
29
What is the muscarinic agonist effect on CNS?
Increase cognition/tremor; treats Alzheimers (only AChI)
30
What is the muscarinic antagonist effect on CNS?
CNS depression, decreases tremors; treats Motion sickness and Parkinson's
31
Muscarinic Agonist: Pilocarpine & Carbachol
Helps Glaucoma; reduces IOP by enhancing drainage of aqueous humor
32
Muscarinic Agonist: Pilocarpine; Cevimeline
Helps Xerostomia associated with Sjogren's syndrome or radiation from head and neck cancers
33
Muscarinic Agonist: Bethanechol
Post Op/ Postpartum non obstructive urinary retention; atonic neurogenic bladder; gastric atony
34
Muscarinic Agonist: Methacholine
Asthma diagnosis
35
Nicotine
- 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
Nicotine Toxicity effects
Acute Toxicity is Rare - Central: convulsions, progression to coma and respiratory paralysis - Skeletal: depolarization, rigidity - Muscarinic excess resulting from stimulating parasympathetic ganglia
37
Nicotinic Replacement Therapy (NRT)
- 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
Varenicline (Chantix) MOA
Partial Agonist at the alpha 4 beta 2 neuronal nicotinic receptors - "High affinity"; competes with nicotine - Suppresses nicotine withdrawal symptoms
39
Varenicline Therapeutic Effects
- Smoking cessation | - can smoke initially during therapy but must set quit date
40
Varenicline ADEs
- Vivid/abnormal dreams; insomnia, N/V; Constipation - Neuropsychiatric disorders? - cardiovascular disorders?
41
Bupropion
- 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
Bupropion ADE
- Agitation, Insomnia, Irritability, dry mouth, nausea, tachycardia - Can lower seizure threshold (dose limit) - Weight loss
43
Role of Acetylcholinesterase (AChE)
Inactivation of ACh by AChE
44
Cholinesterase Inhibitors (AChI) MOA
Reversible inhibition of AChE: increased [local ACh] at receptors
45
AChI Therapeutic Uses
Alzheimer's Disease; Myasthenia Gravis Neuromuscular Blockade reversal Anticholinergic toxidrome
46
Alzheimer's Disease (AD)
Cholinergic neurons are predominantly lost - drugs aim to increase ACh activity/ concentration - AD patients especially sensitive to anti ACh drugs
47
AChI Therapy in Alzheimer's Disease
- Drugs must cross BBB (lipophilic) | - AChI's in AD are more selective for AChE in the brain
48
AChI Drugs for Alzheimers
Tacrine (off market) Rivastigmine Galantamine Donepezil
49
AChI for Alzheimers ADE
``` Mostly Muscarinic: -Bradycardia (dose limiting) -Dizziness, lightheadedness -Increased urinary frequency -GI: nausea, diarrhea, potential GI bleed To use with food ```
50
Myasthenia Gravis
Autoimmune disease affecting skeletal muscle at neuromuscular junction (NMJ; muscular nicotinic receptors) which diminishes ACh activity
51
AChI's in Myasthenia Gravis
Diagnose with short acting AChI (edrophonium) - treatment with neostigmine, pyridostigmine, or ambenonium - Don't cross BBB
52
Non Alzheimer's AChI Drugs
Used for Myasthenia Gravis and NMB reverse - Edrophonium - Neostigmine - Pyridostigmine - Physostigmine - Ambenonium
53
Non AD AChI: ADEs for muscarinic
salivation, urination, bradycardia, bronchoconstriction, abdominal cramping
54
Non AD AChI: ADEs for nicotinic
Muscle Fasciculation/Cramping
55
"Cholinergic Crisis"
Too much ACh in NMJ (need less) - continuous stimulation: permanent depolarization - concern for respiratory paralysis
56
"Myasthenic Crisis"
Not enough ACh in NMJ (need more) | -similar to non depolarizing neuromuscular blockade
57
Organophosphates: Irreversible AChIs Drugs
- Pesticides: Malathion, Parathion - Nerve Gas: Sarin - Herbicides
58
Irreversible AChI MOA
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
Cholinergic Toxidrome: Muscarinic SLUDGE/BBB
Salivation, Lacrimation, Urination, Diaphoresis, GI upset (diarrhea), Emesis Bronchorrhea, Bronchospasm, Bradycardia
60
Cholinergic Toxidrome: Muscarinic DUMBELS
Defecation/Diarrhea, Urination, Miosis, Bronchorrhea,/Bronchospasm/Bradycardia, Emesis/Excitation, Lacrimation, Salivation/Sweating
61
Side effects of increased stimulation of nicotinic receptors
- Muscle fasciculation, weakness, diaphragm failure | - CNS effects: anxiety, labile affect, ataxia, tremors, seizures
62
Primary Treatment of Organophosphate Toxicity
- Airway control, adequate oxygenation - Decontamination, removal of all clothing - Management of seizure: diazepam
63
Pralidoxime (2-PAM)
- 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
Atropine
- muscarinic receptor antagonist | - Blocks ACh to stop effects of increased ACh in synapse: reduces SLUDGE/DUMBELS
65
Anti-Cholinergic Therapeutic uses
- 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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