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Pharmacology 1, 680 > Nondepolarizing Neuromuscular Blockade > Flashcards

Nondepolarizing Neuromuscular Blockade Flashcards

1
Q

Chemical Characteristics- 8

A

*Structurally similar to Ach
*Have one or two quaternary nitrogens
*Highly polar, highly ionized
*Making them lipid insoluble
*Prevents crossing lipid barriers
*Blood brain barrier – no CNS effects
*Placental membrane – maternal effects only
*Gastroepithelium – poor oral absorption

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2
Q

Benzylisoquinoline Class- drug name ending

A

curium
ex. d-Tubocurarine (Curare)
Atracurium (Tracrium)
Cisatracurium (Nimbex)
Doxacurium (Nuromax)
Mivacurium (Mivacron

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3
Q

Steroidal Class- drug name ending

A

Curonium
ex. Pancuronium (Pavulon)
Vecuronium (Norcuron)
Pipecuronium (Arduan)
Rocuronium (Zemuron)
Rapacuronium (Raplon

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4
Q

Mechanism of Action- Nondepolarizing Neuromuscular Blocks

A

Compete with acetylcholine to bind with the 2 alpha subunits on the postjunctional AChR = thus, prevent the ion channel from opening and prevent the muscle cell membrane from depolarizing.

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5
Q

Sequence of Relaxation

A

Small, rapidly contracting muscles
Eyes, fingers and toes
Larynx
Small muscles of the inner ear

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6
Q

Muscles composed of slow fibers

A

Adductor pollicis
Intercostal, abdomen

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7
Q

Organ that is the first to recover but last to be paralyzed

A

Diaphragm

The dose of a given NMB to produce blockade at the diaphragm is about twice the dose required to produce a similar block at the adductor pollicis.

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8
Q

Characteristics of Nondepolarizing NMB- (5)

A

*Decreased twitch response to a single stimulus
*Fade with tetanus, TOF
*Posttetanic potentiation
*Enhanced by other nondepolarizing NMB
*Antagonized by anticholinesterase drugs

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9
Q

Characteristics of NMB that determine its selection(5)

A

*Onset of agent
*Duration of agent
*Side effects of agent
*Metabolism and clearance
*Cost

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10
Q

Characteristics of the patient that determine which NMB to use (3)

A

*Co-existing diseases (renal, hepatic, cardiac, neuromuscular)
*Current medical therapy
*Surgical procedure

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11
Q

Onset-The less potent the drug the _____ the ED95 & more _____ the onset

A

higher& rapid

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12
Q

Drug Order of Onset Time(fast to slow)

A

SCh<) Rocuronium<Atracurium, Vecuronium, Mivacurium<Cisatracurium

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13
Q

ED95- Rocuronium

A

0.3

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14
Q

ED95 Atracurium

A

0.2

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15
Q

ED95 Vecuronium

A

0.05

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16
Q

ED95 -Mivacurium

A

0.08

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17
Q

ED95 Cisatracurium

A

0.05

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18
Q

Least potent drug and has highest ED

A

Rocuronium (same as Sux)

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19
Q

Priming Principle

A

To facilitate rapid intubating conditions with nondepolarizing agents, a small dose (1/10th the intubating dose or 1/3 the ED95) of the NMB is given prior to the induction to allow some receptors to be occupied and minimize the time required for the remaining receptors to be blocked by remainder of the intubating dose.

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20
Q

Disadvantage of increasing dose of NMB to speed onset is ?

A

also increases side effects and prolongs duration
ex. Vecuronium
Increased dose 0.2 mg/kg - Onset 1.5 min - Duration 60-80 min
Normal dose 0.1 mg/kg - Onset 2.3 min - Duration 45-60 min

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21
Q

Short-acting non-depolarizing NMB drug

A

Mivacurium (Mivacron)

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22
Q

Intermediate - acting non depolarizing NMB drugs

A

Atracurium (Tracrium)
Cisatracurium (Nimbex)
Vecuronium (Norcuron)
Rocuronium (Zemuron)

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23
Q

Long- acting non depolarizing NMB drugs

A

Pancuronium (Pavulon)
Doxacurium (Nuromax)
Pipecuronium (Arduan)

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24
Q

Termination of drug is when it ______ not when it is _______

A

when drug diffuses away from alpha subunit receptors=when the plasma level is low, not when it is eliminated from the body

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25
Q

2 parts of Duration

A

Distribution (rapid) and Clearance (slower)

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26
Q

The _____ of elimination affects the duration of action

A

route

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27
Q

Excreted by the kidneys =

A

longer half-lives and longer duration > 60 minutes

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28
Q

Metabolism and clearance by the liver =

A

shorter half-lives and durations; steroid family

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29
Q

Atracurium elimination is achieved by

A

Hofmann elimination primarily, some hepatic

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30
Q

Mivacurium is eliminated by

A

plasma cholinesterase

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31
Q

Long acting non depoloarizing NMB- d- Tubocurarine (Curare)

A

naturally occurring benzylisoquinoline obtained from Chondodendrum plant in Amazon jungle

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32
Q

Long acting non depoloarizing NMB- d- Tubocurarine (Curare) duration and elimination:

A

Long-acting – eliminated both by renal and hepatic

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33
Q

Long acting non depoloarizing NMB- d- Tubocurarine (Curare) adverse reaction

A

Massive Histamine Release

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34
Q

Dose of d-Tubocurarine (Curare) needed for defasciculation

A

3 mg

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35
Q

precurarization=

A

a small dose of a non-depolarizing NMBD is given 2–3 min before the administration of succinylcholine which reduces the potency of succinylcholine, requiring a larger dose to produce the same effect.

36
Q

Pancuronium (Pavulon) (most commonly used long acting NMB), ED95=

A

0.07 mg/kg= potent

37
Q

Pancuronium (Pavulon) intubating dose:

A

0.1 mg/kg

38
Q

Pancuronium (Pavulon) onset and duration=

A

onset 3-5 minutes, duration= 60-90 minutes

39
Q

Pancuronium (Pavulon) elimination=

A

80% unchanged in urine (renal failure slows clearance 2-3X); 10 to 40% metabolized in the liver

40
Q

Pancuronium cardiovascular effect=

A

vagolytic effects due to 1)vagal blockade at cardiac muscarinic receptors and 2)stimulation of the sympathetic nervous system (theory - by causing release of norepinephrine and preventing its uptake back into nerve endings)

41
Q

Vagolytic effects on cardiovascular system=

A

*increased HR (10-15%), BP, CO, and MAP, dysrhythmias, and AV conduction
*Increase is HR inversely related to baseline HR, not dose or rate of administration of pancuronium

42
Q

Doxacurium (Nuromax) is what class of non depolarizing NMB

A

Benzylisoquinolone, long-acting
*no cardiovascular effects

43
Q

Doxacurium (Nuromax) ED95 & intubating dose:

A

ED95= 0.030= potent
intubating dose= 0.05-0.08

44
Q

Doxacurium (Nuromax) onset and duration

A

Onset= 4 to 6 minutes
duration= 60-90 minutes

45
Q

Doxacurium (Nuromax) elimination

A

mostly unchanged via the kidneys and some unchanged via the liver

46
Q

Pipecuronium (Arduan) drug class

A

Long-acting, steroid family
* no cardiovascular or histamine effects

47
Q

Pipecuronium (Arduan) ED95 and intubation dose

A

ED95=0.050mg/kg- potent
Intubation dose= 0.085 mg/kg

48
Q

Pipecuronium (Arduan) onset and duration

A

onset= 3-5 minutes
duration= 60-90 minutes

49
Q

Pipecuronium (Arduan) Elimination

A

unchanged in the urine (ess. no metabolism); unlike pancuronium, no prolonged effect with liver disease.
Prolonged duration in renal failure.

50
Q

Vecuronium (Norcuron) drug class

A

Intermediate ating NMB
*Monoquaternary analog of steroid class pancuronium
*rarely a histamine release and n vagolytic effect

51
Q

Vecuronium ED95 and intubating dose=

A

ED95= 0.05mg/kg- potent
intubation dose 0.1mg/kg, same as pancuronium

52
Q

Vecuronium onset and duration

A

onset= 2.3 minutes
duration= 45- 60 minutes

53
Q

Vecuronium elimination

A

hepatic metabolism and 40% excreted unchanged in the bile, 30% unchanged in urine (both in the first 24 hours)

54
Q

Vecuronium is ____ ____ soluble than pancuronum which allows greater:

A

more lipid soluble
*passage into the hepatocytes for clearance (shorter duration)

55
Q

Vecuronium doesn’t release histamine but interferes with the ____ of histamine causing more to ____ _____

A

*catabolism
*remain active (inhibits histamine -N- methyl-transferase

56
Q

Vecuronium has a prolonged duration of action in what patients?

A

*renal failure and hepatic dysfunction
* and infants less than 1 yr old

57
Q

Rocuronium drug class

A

Intermediate acting derivative of steroidal vecuronium

58
Q

Rocuronium ED95 and intubating dose

A

ED95= 0.3 mg/kg- least potent
intubating dose= 0.6 mg/kg

59
Q

Rocuronium onset and duration

A

onset = 1 to 2 min
duration = 20-35 minutes
*sugammadex made by same company to offset duration

60
Q

Rocuronium elimination

A

unchanged in the bile (50%) and in the urine (>30%)

61
Q

Rocuronium has a prolonged duration in what patients?

A

liver disease- especially with infusions or repeated doses
*renal failure
*elderly

62
Q

Rocuronium Drug Effects

A

Anaphylactoid reactions but no histamine release (also seen with SUX)
*slight vagolytic effect

63
Q

Rocuronium is indicated for a ____ but not patients with a _____ because of its _____

A

*rapid sequence
*difficult airway
*duration

64
Q

Atracurium (Tracrium) drug class

A

Intermediate-acting, benzylisoquinoline diester

65
Q

Atracurium (Tracrium) ED95 and intubating dose

A

ED95- 0.2 mg/kg- least potent & rapid onset
intubating dose= 0.5 mg/kg

66
Q

Atracurium (Tracrium) onset and duration

A

onset= 2 to 3 minutes
duration 20-35 minutes

67
Q

Atracurium (Tracrium) Elimination

A

Hofmann elimination
*metabolism by plasma esterases not plasma cholinesterases, good for renal failure pts

68
Q

Hofmann elimination

A

(spontaneous breakdown) at normal temperature and pH;

69
Q

Laudanosine

A

the metabolite of both routes is a CNS stimulant (cause seizures and cerebral excitation in animals).
*Clinically increased levels not reached in humans
*Prolonged elimination in renal failure patients

70
Q

Atracurium CV effects

A

Histamine release
Increased HR, decreased MAP, decreased SVR, decreased BP, flushing (3x ED95)
(bigger and more rapid the dose= increased effects)

71
Q

How to avoid histamine release effect of Atracurium

A

slow administration 30 to 75 seconds and/or *pretreatment with H1 (Benadryl)
and H2(Pepcid or zantac) blockers- prevents effects
*give low doses of drug

72
Q

Cisatracurium (Nimbex) drug class

A

Isomer of atracurium, intermediate-acting benzylisoquinoline

73
Q

Cisatracurium (Nimbex) ED95 and intubating dose

A

ED95= 0.05 more potent and not for rapid onset
intubating dose= 0.2 mg/kg

74
Q

Cisatracurium (Nimbex) onset and duration

A

onset= 2 to 3 minutes
duration= 20- 35 minutes

75
Q

Cisatracurium (Nimbex) elimination

A

Hofmann elimination(organ independent) (spon. breakdown), but no ester hydrolysis

76
Q

Cisatracurium indications:

A

organ failure, intermediate-length case, need to avoid histamine effects (CV or pulmonary), infusion.

77
Q

Cisatracurium effects

A

No cumulative effects – good for infusions.
*Production of laudanosine is less due to only one pathway.
*Unlike atracurium, histamine release is MINIMAL, thus minimal CV effects.

78
Q

Mivacurium (Mivacron) drug class

A

Short-acting benzylisoquinoline

79
Q

Mivacurium (Mivacron) ED95 and intubating dose

A

ED95= 0.08 mg/kg- potent no fast onset
intubating dose= 0.15- 0.2 mg/kg

80
Q

Mivacurium (Mivacron) onset and duration

A

onset= 1.5 to 3 minutes- NOT INDICATED FOR RAPID SEQUENCE
duration 12-20 minutes

81
Q

Mivacurium (Mivacron) elimination

A

metabolism by plasma cholinesterase at 70-80% the rate of SCh metabolism

82
Q

Mivacurium consists of what 3 stereoisomers

A

– cis-trans, trans-trans (1/2 lives of 2 minutes), cis-cis (1/2 life of 53 minutes)

83
Q

Mivacurium causes histamine release ____ ED95, avoid by giving the dose in ____ doses

A

*2x-histamine release from mast cells causes hypotension and tachycardia
-Prophylaxis: low doses, slow administration, pretreat

*divided

84
Q

What drug slows the recovery of Mivacurium? and how?

A

Neostigmine (anticholinesterase) - 20- 60 minutes
*it inhibits the activity of plasma cholinesterase which is what metabolizes mivacurium.
Establish that recovery is already occurring prior to giving anticholinesterase (edrophonium)

85
Q

Mivacurium causes a prolonged blockage in patients with ____ ____ ____ due to metabolism by ___ _____

A

*atypical plasma cholinesterase
*plasma cholinesterase

86
Q

Mivacurium may cause prolonged duration in what other patients?

A

renal and hepatic failure

Pharmacology 1, 680 (3 decks)

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