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Quarter 3 > Pharmacology Local and MR > Flashcards

Pharmacology Local and MR Flashcards

1
Q

Ester-linked Local Anesthetic drugs

A
  • cocaine
  • procaine
  • benzocaine
  • tetracaine
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2
Q

local anesthetic mechanism of action

A

votalge-gated Na+ channel blocker

  • decrease rate of depolarization
  • increase threshold for electrical excitability
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3
Q

Nociception

A
  • opioids = morphine
  • voltage-gated = local anesthetics
  • a2 agonists = dexmedetomidine
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4
Q

Susceptibility factors of local anesthetics

A
  • fiber diameter
  • myelination
  • fiber position
  • firing frequency
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5
Q

Myelination and local anesthetics

A

myelinated nerves are blocked before unmyelinated

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6
Q

fiber position and local anesthetics

A

outer nerves in a bundle are blocked more readily than inner nerves

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7
Q

Firing frequency and local anesthetics

A

LA have a higher affinity for the active Na+ channels compared to resting

  • Rapidly firing neurons are more readily blocked by local anesthetics when compared to slowly firing neurons
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8
Q

Ionizable group of local anesthetics

A

most LA are weak bases

  • LA must be unpronated and neutral to permeate cellular membranes
  • Protonated LA are more potent than their unprotonated counterpart
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9
Q

Ester-Linked Local Anesthetics

A

rapidly hydrolyzed

  • have a shorter half life
  • have a lower Vd
  • are less likely to elicit systemic side effects
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10
Q

“local” adverse effects of LA

A

tissue damage

  • stinging sensation due to acidic nature
  • hypoxia due to co-administration of vasoconstrictor
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11
Q

Large doses of which 3 LA may cause metheglobinemia?

A

prilocaine, benzocaine, lidocaine

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12
Q

Vasoconstrictors and LA

A

epinephrine or Levonordefrin

  • limits escape of LA from site of administration
  • decreases the potential for systemic toxicity
  • increases the duration of action at target site
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13
Q

3 classifications of muscle relaxants

A
  • neuromuscular blockers
  • spasmolytics
  • antispasmodics
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14
Q

Neuromuscular blockers

A
  • exert effects on periphery
  • do not cross the BBB
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15
Q

Spasmolytics

A

used to reduce spasticity assoicated with neuromuscular disorders

  • mostly exert effects within the CNS
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16
Q

Antispasmodics

A

Used to treat musculoskeletal conditions such as back bain and fibromyalgia

  • exert their effect within the CNS
17
Q

Neuromuscular blocker mechanism of action

A

bidns to and blocks nicotinic cholinergic receptors (NM) located at the NMJ

  • interferes with acetylcholine action
18
Q
A
19
Q

Nicotinic cholinergic receptors are ____ and ____

A

ligand-gated receptors and sodium channels

20
Q

Structure of Nicotinic receptors

A
  • Made from 5 types of homologous subunits
  • NN located at ganglia
21
Q

Acetylcholine binding sites on nicotinic receptors

A

2 (alpha2)

22
Q

Describe the “pore” of nicotinic receptors

A

M2 region within each of the 5 subunits forms the pore that is selective for Na+

  • 3 negatively charged amino acid rings pull Na+ through
  • Leucine ring is important in channel desensitization
23
Q

Succinylcholine

A

Depolarizing MR

  • at low concentrations, acts like ACh and depolarizes membrane
    • large doses cause muscle paralysis
  • rapid onset (1-1.5 min)
  • short duration (5-10 minutes)
24
Q

Black box warning on Succinylcholine

A

acute rhabdomylosis with hyperkalemia in children with undiagonsed musclar dystrophies

25
Q

Malignant Hyperthermia

A

drugs induce massive Ca2+ discharge through a defective mucle cell ryanodine receptor (RyR)

26
Q

Dantrolene

A

RYR-1 calcium channel antagonist

  • prevents Ca2+ release from the SR
  • blocks movement of myosin and actin
27
Q

Isoquinolone NDMR

A

atracurium, cisatracurium, tubocurarine

28
Q

Steroid NDMR

A

rocuronium, vecuronium, pancuronium

29
Q

NDMR

A

competitive antagonist at NM

30
Q

AChE inhibitors for MR reversal

A

neostigmine or pyridosigmine

31
Q

Sugammadex

A

selective relaxant binding drug

  • chelates steroid-derived NMB and facilitates urinary excretion

Quarter 3 (12 decks)

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