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Summer Pharmacology > Neuromuscular relaxants > Flashcards

Neuromuscular relaxants Flashcards

1
Q

What do NMB produce?

A

paralysis

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2
Q

Do NMB produce amnesia or analgesia?

A

NO

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3
Q

What are the pharm effects of NMB?

A

-interrupt nerve impulses at the NMJ -similar structure to the endogenous neurotransmitter acetylcholine (Ach) - provides muscle relaxation

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4
Q

Ca channels and nicotinic receptors are embedded where?

A

lipid bilayer

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5
Q

Are nicotinic receptors presynapic or postsynaptic?

A

POSTsynaptic

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6
Q

Describe the neuromuscular transmission release of Ach from nerve terminal…

A

AP and depolarizing of nerve terminal Ca channels open ca diffuses down gradient to nerve terminal Ach spills out into synaptic cleft Presynaptic nicotinic receptor responds to Ach by increasing in the synthesis and release of Ache

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7
Q

Describe the events at postsynaptic membrane

A

Ach combines with nicotinic receptors Both nicotinic receptors occupied. Channels open Na, Ca diffuse into cell and K diffuse out. Motor end plate depolarizes AP potentiated Skeletal muscle contracts

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8
Q

What is terminated by neurotransmitter action?

A

acetylcholinesterase (AChe) The choline is transported back to the nerve terminal and reconverted to Ach

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9
Q

Acetylcholine receptor _ protein subunits Central core for _ channeling Ach must bind to both _ subunits to open the core A subunits are the site of agonism and antagonism

A

Acetylochline receptor 5 protein subunits central core for cation channeling Ach must bind to both A subunits to open the core “A” subunits are the site of agonism and antagonism

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10
Q

Nondepolarizing BLOCK Nondepolarizing agents are competitive _. _ can not attach to the receptor Channels can not _ _ _ effect on the channel

A

inhibitors Ach open no direct

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11
Q

Depolarizing BLOCK _ binds to _ receptors, channel opens, motor endplate depolarizes _ contraction occurs Sch not metabolized by _ _ _ cannot be initiated

A

Succs, nicotinic single true acetylcholinesterases - channels stay open until Sch diffuses back into the circulation AP

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12
Q

What is a depolarizing muscle relaxant?

A

Succinylcholine

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13
Q

What are nondepolarizing muscle relaxants? (acd mpp rrv)

A

Mivacurium Rapacuronium Rocuronium Vecuronium Atracurium Cisatracurium Pipecuronium Pancuronium Doxacurium (ACD MPP RRV)

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14
Q

Succs: is there a reversal agent?

A

no

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15
Q

Succs: metabolism: rapid hydrolysis by _

A

pseudocholinesterase = plasma cholinesterase = an enzyme of the liver and plasma

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16
Q

How is a Sch block terminated?

A

by diffusion of Sch away from the neuromuscular junction

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17
Q

What are the Sch side effects for pediatrics?

A

contraindicated in routine mgmt d/t side effects MHAUS strongly advises against Sch use in children IV atropine 0.02mg/kg

18
Q

What does the black box warning about Sch say for pediatrics?

A

-IV bolus admin may result in Malignant ventricular arrythmias and cardiac arrest 2 to actue rhado with HYPERkalemia. - IV bolus may result in profound bradycardia/asystole. Bradycardia is higher following a 2nd dose of succs. The occurrence of bradyarrhythmias may be reduced by pretreatment with atropine.

19
Q

What are the side effects of Sch?

A

HYPERkalemia = increased with burns, trauma, nerve damage, neuromuscular disease, renal failure Muscle pains (fasciculations) INCREASED ICP, IOP, IGP =intragastric pressure (IGP) Massester spasm =jaw muscle rigidity in assoc with limb flaccidity Potent MH trigger agent

20
Q

Dibucaine is a _ _ inhibits normal _ # indicates _ makeup of a person with regard to _ # is _ NOT _

A

Dibucaine is a local anesthetic inhibits normal pseudocholinesterase genetic makeup of a person with regard to pseduocholinesterase is qualitative NOT quanitative

21
Q

Describe the incidence, dibucaine number, duration of homozygous typical…

A

incidence: normal Dibucaine #: 70-80 duration: 4-6 minutes

22
Q

Describe the incidence, dibucaine number, duration of heterozygous atypical…

A

incidence: 1/50 patients Dibucaine #: 50-60 duration: 20-30 minutes

23
Q

Describe the incidence, dibucaine number, duration of homozygous atypical…

A

incidence: 1/3000 Dibucaine #: 20-30 duration: 4-8 hours

24
Q

Chemical properties of NonDepolarMR __ ammonium Steroid derivatives of _ Benzylisoquinolines are _ soluble Principle route of elimination is __ excretion

A

quaternary ammonium steroid derivatives of benzylisquinolines Benzylisoquinolines are water soluble = inhibits uptake into hepatocytes leads to lack of liver elimination = exception is steroid based relaxants Priniciple route of elimination is urinary excretion

25
Q

DOA if NDMRs Short acting onset duration Route of elimination

A

Rapacuronium Mivacuronium - metabolism, plasma cholinesterase Rocuronium - biliary excretion (MRR) onset 1 minutes duration < 30 minutes

26
Q

DOA if NDMRs Intermediate acting onset duration Route of elimination

A

Vecuronium -biliary excretion Atracurium -metabolism = 2/3 nonspec ester hydrolysis and 1/3 hoffman elimination Cisatracurium - metabolism =hoffman elimination Rocuronium -biliary excretion (Carv) onset: 2 minutes duration: 60 minutes

27
Q

DOA if NDMRs LONg acting onset duration route of elimination

A

Alcuronium Doxacurium - renal d-tubocurarine -renal Gallamine -renal Metocurine -renal Pancuronium -renal Pipecuronium -renal Onset: 2-6 minutes Duration: 120 minutes

28
Q

Agent Histamine HR BP

sux small brady

mivacurium small tachy (rapid)

atracurium small tachy

vecuronium none None

rocuronium none None

D-tubo mod reflex tachy

pancuronium none tachy

A

Agent Histamine HR BP

sux small brady decrease

mivacurium small tachy (rapid) decrease

atracurium small tachy none

vecuronium none None none

rocuronium none None none

D-tubo mod reflex tachy decrease

pancuronium none tachy increase

29
Q

Agent Histamine HR BP

sux small decrease

mivacurium small decrease

atracurium small none

vecuronium none none

rocuronium none none

D-tubo mod decrease

pancuronium none increase

A

Agent Histamine HR BP

sux small brady decrease

mivacurium small tachy (rapid) decrease

atracurium small tachy none

vecuronium none None none

rocuronium none None none

D-tubo mod reflex tachy decrease

pancuronium none tachy increase

30
Q

Agent Histamine HR BP

sux brady decrease

mivacurium tachy (rapid) decrease

atracurium tachy none

vecuronium None none

rocuronium None none

D-tubo reflex tachy decrease

pancuronium tachy increase

A

Agent Histamine HR BP

sux small brady decrease

mivacurium small tachy (rapid) decrease

atracurium small tachy none

vecuronium none None none

rocuronium none None none

D-tubo mod reflex tachy decrease

pancuronium none tachy increase

31
Q

What are the factors effecting degree of muscle relaxation?

A

antiHTN

renal/hepatic disease

cholineseterase inhibitors

ketamine

lithium

32
Q

Drug Efct: depol block Efct:nondepol block

Antibiotic +

Cholinesterase inh -

Antidysrhythmics +

Dantrolene +

Inhalational anes +

Ketamine +

Locals +

A

Drug Efct: depol block Efct:nondepol block

Antibiotic + +

Cholinesterase inh + -

Antidysrhythmics + +

Dantrolene ? +

Inhalational anes + +

Ketamine ? +

Locals + +

33
Q

Drug : Effect on the nondepol block

Antibiotic Cholinesterase inhibitor

Antidysrhythmics

Dantrolene

Inhalational anes

Ketamine

Locals

A

Drug Efct: depol block Efct:nondepol block

Antibiotic + +

Cholinesterase inh + -

Antidysrhythmics + +

Dantrolene ? +

Inhalational anes + +

Ketamine ? +

Locals + +

34
Q

Causes of altered responses to NDMR:

A

Hypothermia

=Prolongs block esp intermed acting NDMR

Acidosis

=Decrease pH prolongs action of atracurium by inhibiting Hoffman elimination

Hypokalemia

=Prolongs effect (diuretics)

Burns

=3rd degree burns > 30% of body resistance to NDMR (40-60 days post injury)

35
Q

Long acting muscle relaxants

Produce paralysis in __ minutes

Mainteance of anesthesia for operations > _ hours

Recovery __ minutes

Primarily exreted via __ unchanged

A

3-5 minutes

2 hours

40-70 minutes

kidney unchanged

36
Q

Intermediate acting relaxants

Useful for _

half DOA of long acting relaxants

onset time varies

minimal _ events

A

intubation

circulatory effects

37
Q

Short acting relaxant

SCh

  • _ drip

_ of Ns or D5W

_ mg/min

Micacurium

Alternative to __ (avoid _)

Onset longer than _

_ DOA, _ shorter than intermediates

useful for brief _ surgery when used just for _

A

Sch

-continuous drip

1gm/500ml of NS or D5W

2-4 mg/min

Mivacurium

  • Alternative to succs (avoid myalgia)
  • onset longer than SCh
  • short doa, 30-40% SHORTER THAN INTERMIEDIATES

useful for brief outpatient surgery when used just for intubation

38
Q

How do you speed the onset of NDMR?

A

Administer 10% of intubating dose followed in 5 minutes before induction

Initial small dose primes spare receptors without producing paralysis the time

Onset of larger dose faciliated

ALWAYS have emergency airway equipment available

39
Q

Defasciculating dose

describe it and the dose of vecuronium and rocuronium

A

10% of intubating dose of NDMR to prevent Sux induced fasciculation.

= Fasciculations increase risk of hyperkalemia, muscle pain, increases introgastric pressure adn aspiration

=Temporary increase in ICP with succs

=-= Traditionally we still give defasciculating agents when Sch used in head injury patients

Vecuronium = .01 mg/kg

Rocuronium = .1 mg/kg

40
Q

Doses

NMB can be used to _ (full bolus) and to __ __ (reduced bolus after initial bolus and with return of twitces on PNS)

A

intubate and maintain anesthesia

41
Q
A

Summer Pharmacology (4 decks)

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