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Pharmacology- Muscle Relaxant SAQ

Pharmacology- Muscle Relaxant SAQ

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Published by anaeshkl

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Published by: anaeshkl on Feb 26, 2011
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12/24/2012

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Q. Compare and contrast atracurium and cisatracuriumatracurium cisatracurium
y
 
I
ntermediate acting non-depolarizingmuscle relaxant
y
 
intermediate acting non-depolarisingagent from the Bissquaternarybenzylisoquinolone
y
 
intermediate acting non-depolarizing musclerelaxant
y
 
intermediate acting non-depolarising agentfrom the benzylquinolone groupphysicochemical propertiesPresentation
y
 
clear,
y
 
colourless
y
 
or faint yellow,
y
 
PCYpreparation
y
 
sterile solution containing atracuriumbesylate 10 mg, in each mL of Waterfor
I
njections.pH of solution
y
 
T
he solution also containsbenzenesulfonic acid to adjust the pHto 3.2 to 3.7.Storage condition
y
 
stored at 2 to 8
y
 
D
o not freeze.
y
 
Protect from lightpresentation
y
 
pale
y
 
yellow
y
 
greenish solution
y
 
PYGadditive
y
 
no antimicrobial preservativepH of solution
y
 
solubilized in benzenesulfonic acid
y
 
therefore, both is available for use but has to be kept in refrigeratorstructure activity relationship
 
y
 
bisquartenary benzylquinolone group
y
 
mixture of ten isomers
y
 
15% by weight is cistracurium
y
 
Constitute 15% of the mixture of 10isomers of atracurium
y
 
50% of the relaxant axtivity of atracuriumis from cis-atracurium
y
 
R
-cis isomer of atracurium , where
R
istetrahydropapavarine rings and cis is thedimethoxy and 2 alkyl ester group at C1and N2
D
ose and administrationintubating dose0.4-0.5 0.1E
D9
50.25 0.05cis- atracurium is more potent than atracurium because it need less drug to block
9
5%contraction on single twitch stimulation
T
he E
D9
0 (dose required to produce
9
0% depression of the twitch response of the thumb tostimulation of the ulnar nerve) during intravenous anaesthesiaOnset of actionslow onset3-5slow onset3- 5Atracurium has similar onset of action as atracurium
D
uration of action
 
20-35 20-35?
D
uration of action - similar? Mentioned recovery timeatracurium and cisatracurium are intermediate acting muscle relaxantVolume of distribution0.2Both compound are distributed mainly in ECFElimination
y
 
eliminated in in plasma via twononoxidative pathways:
y
 
1. ester hydrolysis, catalysed bynonspecific esterases; 67%
y
 
2. Hofmann elimination, anonenzymatic chemical process whichoccurs at physiological pH and bodytemperature. 33%
y
 
Atracurium eliminated mainly byester hydrolysis 2/3
y
 
Hoffman degradation= 1/3
y
 
T
he rate of Hofmann elimination,principal route of elimination foratracurium, is increased at a higherpH or at higher temperatures, andreduced at a lower pH or lowertemperatures
y
 
I
n vivo degradation and biologicalmetabolism
y
 
R
apidly broken by spontaneouschemical reaction ie hoffmanelimination
y
 
Eliminate mainly by hoffman elimination 77% and16% by renal excretion

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