neuromuscular blocking agents Flashcards

1
Q

Neuromuscular blocking agents

A

drugs used to immobilize patients for surgery, certain procedures and paralyze skeletal muscle and are high alert

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

effects of IV competitive blocking agent

A

motor weakness progresses to total flaccid paralysis, small moving muscels relax before larger until paralysis - recovery moves in the opposite direction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

___ is the NT involved in skeletal muscle activation

A

ach

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

process of skeletal muscle action

A

ach released from a somatic neuron and activates Nm receptors - allowing for the influx of sodium depolarizing the t-tubule and promotes an increase in intracellular calcium contraction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Nm belongs to a family of _____

A

ligand-gated ion channels which also include GABA, 5HT, glycine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

the general structure of Nm receptor

A

pentamer composed of 5 subunits, 2 ACh molecules are required to open the cahnnel and the binding site for ach is on the ALPHA (when it binds it opens), each subunit has a single peptide chain with with 4 membrane spanning units

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

how many configurations of neuronal nicotinic receptors

A

16

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

drugs that interact with the Nm receptor

A

they usually have two portions of the molecule which resemble ach. (N + ester) bc the molecule will bind to both sides to block it

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

succinylcholine

A

Nm receptor blocker depolarizing unit, resistant to AChE, rapidly metabolized by cholinesterase resulting in a short half-life

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

atracurium

A

non-depolarizing unit, more rigid in structure, Nm receptor blocker

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

the only depolarizing NMBA

A

succinylcholine - causes a muscle fasiculations because the cell membrane becomes depolarized, ion chanels on the membrane become refractory and the muscle become resistant to further stimulation (flaccid paralysis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

phase 1 block

A

depolarizing agent immediately after admin- muscle becomes resistant to flaccid paralysis because the cell membrane becomes refractory
(depolarized to -55mV, immediate, lower dose dependent, rapid recovery, no fade, augments (inc) ach inhibition, fasiculations to paralysis)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

phase 2 block

A

due to high doses of depolarizing NM agents, resembles non-polarizng NMBA (replarization towards -80mV, slow transition, usually higher or follows prolonged infusion, more prolonged, fade, reverse ach inhib, flaccid paralysis)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

how would admin of AChE inhibitor effect the actions of succinyl choline

A

inch ach, turn off the receptor, one agent not reversed by cholinesterase inhibitor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

amino steroids

A

drugs end in -uronium (rocuronium, vecuronium, pncuronium)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

benzylisoquinolines

A

drugs end in -cruium (mivacruium, (cis)aracurium)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

all _____ are competitive antagonists at the Nm receptor

A

non-depolarizing

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

would non-depolarizing cause muscle fasiculation

A

no, not depolarizing

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

would non-depolarizing be reversed by AChE inhibitor

A

yes, inc in Ach, compete off the drug

20
Q

which non-depolarizing drugs have the shortest half life

A

succinylcholine, mivacurium both by BchE

21
Q

what non-depolarizing drugs should be does independ

A

succ, atra, cis atra

22
Q

where would non-depolarizing drugs primarily distribute throughout the body

A

total body water

23
Q

mivacurium

A

met - renal, BuChE, short duration

24
Q

cisatracurium / atracurium

A

met- hofman degration (except atra also has ester hydrolysis)
intermediate duration

25
Q

panuronium

A

met- renal, some hepatic

long duration

26
Q

rocuronium

A

met- hepatic (bile), renal

intermediate duration

27
Q

succinylcholine

A

met- BuChE

short duration

28
Q

vecuronium

A

met- hepatic, some renal

intermediate duration

29
Q

hofmann degradation

A

atracurium/cisatracurim both undergo spontaneous degradation without any enzymes!

30
Q

incresed fluid volume leads to

A

inc fluid volume bc of hepatic or renal disease will have a higher vd and will need a higher dose

31
Q

t 1/2 =

A

0.693 x vd / Cl

32
Q

hyperkalemia

A

concern with NMBA admin, associated with succinylcholine, prolonged depolarization of the membrane results in the efflux of potassium from within the muscle cells

33
Q

depolarization =

A

cell trying to repolarize and k+ goes into the plasma

34
Q

increased intragastric pressure

A

succinyl choline- abdomen contracts and stomach muscle contracts, may result in vomiting and issues with the airway

35
Q

histamine release

A

succinylcholine and atracurium are most associated with a decrease in BP

36
Q

myalgias

A

muscle pain caused by succinylcholine

37
Q

all agents

A

combinded admin with inhaled anesthetic may make the pt more sensitive to the medications and reduce the dose of the NMBA

38
Q

reversal of non-depolarizing block

A

neostigmine- Ach inhibitor- reverse paralysis

39
Q

what is the rational for admin neostigmine? why not work for succinylcholine reversal

A

inc ach- compete with neuromuscular blocker

40
Q

what is the rationale for administering neostigmine -

A

increase ach and compete with a NM blocker

41
Q

what is the rationale for admin of a musc ADR from neostig -

A

getting ach - GI discomfort and bladder loss salivary increased

42
Q

if the patient is bradycardia why should anti-muscurinic agent always be admin first

A

HR would be too low just with neostigmine, give anti muscurinic first then give the other

43
Q

aged enzyme

A

resistant to hydrolysis- permentantly phosphorylated ser-o-p, isopropyl leaves - hardly any electrophilicity,

44
Q

definition of depolarizing

A

Depolarizing muscle relaxants acts as ACh receptor agonists. They bind to the ACh receptors and generate an action potential. However, because they are not metabolized by acetylcholinesterase, the binding of this drug to the receptor is prolonged resulting in an extended depolarization of the muscle end-plate. As the muscle relaxant continues to bind to the ACh receptor, the end plate cannot repolarize, resulting in a phase I block. The ACh receptor can also undergo conformational and ionic changes after a period of time, resulting in a phase II block.

45
Q

definition of non-depolarizing

A

competitive antagonists. They bind to the ACh receptors but unable to induce ion channel openings. They prevent ACh from binding and thus end plate potentials do not develop.