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PDA Block 1 > Cholinergics > Flashcards

Cholinergics Flashcards

1
Q

Parasympathomimetic

A

Muscarinic receptor agonists

  • direct agonists of muscarinic receptors
  • produce effects similar to those obsered during the stimulation of post-ganglionic PS nerves
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2
Q

parasympatholytic

A

Muscarinic receptor antagonists

Interfere with responses that result from PS stimulation

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3
Q

Cholinergic

Receptors types

A

Acetyl CoA +Choline–> AcH
AcH acts on
- muscarinic R (PS)
- nicotinic R

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4
Q

Muscarinic R effects

Eye
Heart
Lung
GI
Sweat glands
BV
A

Eye: contraction of ciliary m.= accomodation, contraction of iris= miosis

Decrease HR
Bronchoconstriction
bladder voiding
Salivation, increase gastric secretion, intestinal tone and motility
generalized sweating
Vasodilation
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5
Q

anti-muscarinic

A

parasympatholytics

muscarinic receptor antagonists

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6
Q

nicotinic

Nicotinic (muscle m)
Nicotinic (neural)

A

skeletal m: end plate depolarization

Autonomic ganglia: depolarization of post-ganglionic neurons

Adrenal Medulla: depolarization and secretion of catecholamines

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7
Q

Bethanechol

A

choline ester- muscarinic receptor agonist
Quaternary amine
- primary effect of GI/GU tracts
- orally or SQ injection for urinary retention in absence of obstruction

  • Not administered thru IV- cause hypotension
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8
Q

Pilocarpine

A 
Alkaloid- muscarinic receptor agonist
Tertiary amine 
muscarinic effects
Uses:
- orally to treat xerostomia
- miotic agent ophthalmically to treat wide- angle glaucoma & emergency treatment for narrow angle glaucoma
  • not administered thru IV- will cause hypotension
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9
Q

Edrophonium

A

Reversible competitive AcHE inhibitor

  • rapid onset and short duration of action
  • not orally active: IV admistration

Uses

  • diagnosis of myasthenia gravis
  • distinguish cholinergic crisis from myasthenic crisis
  • reversal of paralysis by competitive neuromuscular blocking drugs
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10
Q

Physostigmine

A

Reversible non-substrate AcHE inhibitor

  • alkaloid
  • slowly reversible
  • tertiary amine–> CNS effects

Uses:

  • treatment of wide-angle glaucoma
  • treat toxicity by anti-muscarinic drug poisoning ( IV penetrates into CNS)
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11
Q

Neostigmine

A

Reversible non-substrate AcHE inhibitor

  • slow reversible
  • quaternary amine: no CNS effects

Use:

  • treat myasthenia gravis (oral)
  • prevention and treatment of post-operatirve atony of gut and bladder
  • reversal of anesthesia
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12
Q

Sarin

A

Irreversible Organophosphate inhibitors of AcHE

  • irreversibly phosphorylate the serine in the substrate binding domain of AcHE
  • regeneration of enzyme is slow
  • return of activity depends on synthesis of new enzyme
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13
Q

Atropine

A

muscarinic receptor antagonist

  • treat AcHE or muscarinic toxicity
  • treat bradyarrhythmia (acute MI)
  • produce mydriasis (dilation) and cycloplegia (paralysis of accomodation)
  • long duration of action (7-10 days)
  • treat acute iritis or choroiditis
  • use as anethesia to block vagal reflex
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14
Q

Scopolamine

A

Muscarinic Antagonist

  • CNS penetration
  • used as a transdermal patch
  • used to treat motion sickness
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15
Q

Ipratropium

A

Derivative of alkaloids

  • muscarinic receptor antagonist
  • used to treat COPD
  • administered by inhalation
  • no CNS penetration
  • reduce brochosecretions and constriction
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16
Q

Tropicamide

A

Synthetic muscarinic antagonist

  • used to produce mydriasis and cycloplegia
  • fast onset (20-40 min) and short duration (4-6 hrs)
17
Q

Oxybutynin

A

Synthetic muscarinic antagonist

  • Use to treat overactive bladder and incontinence
  • high incidence of anti-muscarinic side effects
  • treat xerostomia mainly but also blurred vision, GI and antimuscarinic effects
18
Q

Darifenacin

A

Synthetic muscarinic antagonist

  • used to treat overactive bladder and incontinence
  • selective for M3 receptors
19
Q

Glycopyrrolate

A

Synthetic muscarinic antagonist

  • used to block PS effects during reversal of anesthesia with ACHE
  • no CNS penetration
20
Q

Rocuronium

A

Competitive Neuromuscular blocking agent

  • aminosteroid
  • intermediate duration (30-60 min)
  • rapid onset of action (intubation)
  • liver metabolism
21
Q

Atracurium

A

Competitive Neuromuscular blocking agent

  • benzylioquinoline
  • intermediate duration (30-60 min)
  • spontaneously degrades ( inactive)
  • minimal CV effects
22
Q

Vecuronium

A

Competitive Neuromuscular blocking agent

  • aminosteroid
  • intermediate duration of action (30-60 min)
  • onset 2-4 min
  • liver metabolism
  • no CV effects
23
Q

Pancuronium

A

Competitive Neuromuscular blocking agent

  • aminosteroid
  • onset 2-4 min
  • long duration of action (120-180 min)
  • liver metabolism
  • no CV effects
24
Q

Succinylcholine

A

Depolarizing Neuromuscular blocking agent
agonist of nicotinic receptors at NMJ–> opening of cation channels
- activate nicotinic receptors at NMJ maintains motor end plate depolarization ( prevent transmission of another AP)
- muscle fasciculations followed by flaccid paralysis
- metabolized by pseudocholinesterase
- ultra short duration of action (5-8 min): tracheal intubation
-genetic variation in pseudocholinesterase activity

25
Q

Pralidoxime

A 
Reactivates AcHE ( need to treat quickly 2-3 hours)
- used for poisoning
26
Q

Anti-cholinesterase

A

agents that enhance the effects of endogenously released AcH by blocking natural breakdown of ACH by AcHE

27
Q

Ganglionic blocking agents

A

neural nicotinic receptor antagonists

  • competitive antagonists for Nn at autonomic ganglia
  • interferes with ganglionic transmission of both PS and S nerves
28
Q

Side effects of choline esters

what blocks toxicity?

Use with caution in which groups?

A 
SLUDGE
Salivation
Lacrimation
Urination
Defecation
GI upset
Emesis

Atropine blocks toxicity

Use w/ caution:

  • Asthma & COPD
  • Urinary or GI obstruction
  • CV disease (bradycardia, hypotension)
29
Q

Malathion

A

Irreversible Organophosphate inhibitors of AcHE

  • irreversibly phosphorylate the serine in the substrate binding domain of AcHE
  • regeneration of enzyme is slow
  • return of activity depends on synthesis of new enzyme

-insecticide

30
Q

Side effects of AcHE inhibitors

Treatment

A

SLUDGE
- death due to respiratory failure

Treatment
- atropine: muscarinic receptor antagonist- blocks muscarinic effects

  • pralidoxime- reactivates AcHE ( need to treat quickly 2-3 hours)
31
Q

Muscarinic R antagonists

Effects

A

competitively block muscarinic receptors

Effects:

  • relax iris sphincter and ciliary muscles
  • relax non-vascular smooth muscle
  • inhibit exocrine gland secretion
  • increase HR
  • CNS effects
  • low dose: sedation
  • high dose: excitement, delirium, agitation
32
Q

Side effects of muscarinic antagonist

Use with caution

A 
Hot as a hare (no sweating)
Dry as a bone (dry mouth)
Red as beet ( excessive heat)
Blind as a bat (mydriasis, cycloplegia, blurred vision)
Drowsiness- CNS

Toxic: mad as a hatter- hallucinations, delirium, coma

Use with caution

  • Glaucoma: increase intraocular pressure
  • Prostatic Hypertrophy
  • tachycardia

Poisoning: Treat with physostigmine

33
Q

Neuromuscular blocking agent

A

block neurotransmission at NMJ producing muscle paralysis

  • use as adjuvant in anesthesia to obtain relaxation
  • use to facilitate intubation with tracheal tube
  • 2 classes ( non-depolarizing/ competitive or depolarizing)
34
Q

Adverse effects/ Toxicity of neuromuscular blocking agents

A

Competitive: prolonged apnea and analphylaxis

  • toxicity can be reversed with neostigmine or edrophonium
  • if treating with ACHE for reversal, co-administer with muscarinic antagonist (glycopyrrolate) to reduce muscarinic actions

Depolarizing:

  • prolonged apnea
  • not treatable with ACHE
  • Malignant hyperthermia: triggered by administration of depolarizing agents–> cause uncontrolled Ca release (due to mutation in ryanodine receptor) –> treat with ca release blocker
  • post- operative muscle pain due to muscle fasciculation
  • hyperkalemia: release potassium from intracellular sites

PDA Block 1 (3 decks)

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