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DEPOLARISING
NON-DEPOLARISING
SUXAMETHONIUM
SHORT ACTING INTERMEDIATE ACTING LONG ACTING
SUXAMETHONIUM
PRESENTATION
Injection solution: a clear, colourless, particle-free solution containing 50 mg/mL suxamethonium chloride.
DOSE
Traditional dose to facilitate intubation is IV 1mg/kg. If unsuitable IV access, IM up to 2.5mg/kg can be given (total not exceed 150mg) According to Smith et al 1988, the ED90 for SCh as determined by the administration of thiopental while breathing nitrous oxide is 0.27mg/kg Thus the dose 1mg/kg represents 3.5-4 x the ED95
What is ED??
ED = effective dose, dose required to produce an effect ED50 50% effect ED95 95% effect
SEQUENCE 0F PARALYSIS
Thumb Orbicularis oculis limbs Trunk
laryngeal muscle
Intercostal muscles diaphragm
RECOVERY
Conceptually..
administration of 1mg/kg Sch to a preO2 patient : results a return of spontaneous breath within 5 minutes YET, the average duration to 90% twitch height recovery following 1mg/kg is greater than 10minutes the diaphragm recovers before the adductor pollicis muscle
MECHANISM OF ACTION
PHASE 1 BLOCKADE
PHASE II BLOCKADE
Sch
Duration of Action?
Brief duration of action (3 - 5minutes) d/t hydroysis by plasma cholinesterase (pseudocholinesterase) enzyme Vs acetylcholinesterases enzyme??
- Synthesized by the liver -A tetrameric glycoprotein containing 4 identicals subunits each have active catalytic site - enormous capacity to hydrolyze Sch at a rapid rate , so that only a small fraction of the original IV dose actually reach the NMJ
METABOLISM
SUCCINYLCHOLINE
PLASMA CHOLINESTERASE
SUCCINYLMONOCHOLINE
+ +
CHOLINE
SUCCINIC ACID
CHOLINE
(PROLONGED BLOCK)
(SHORTER BLOCK)
1) Decrease in hepatic production 1) obese patient - liver disease must be severe b4 2) Myasthenia gravis (ED95 is X 2.6 decrease is sufficent to prolong block normal) 2) Drug interaction 3) juvenile hyaline fibromatosis - neostigmine (> edrophonium), - potent anticholinesterase drugs in insecticides/Rx of MG/glaucoma/cyclophosphamide/nitr ogen mustard) - after IV metoclpromide 10mg 3) Presence of atypical plasma cholinesterase 4) High eostrogen levels
Enzyme deficiency
ACQUIRED
INHERITED
a. the newborn, until 2-6 months Atypical plasma cholinesterase b. acute or chronic liver diseases c. malnutrition d. pregnancy e. collagen diseases f. chronic anaemia g. uraemia h. myxedema i. other chronic debilitating diseases j. severe burns k. chronic pesticide exposure & accidental poisoning l. drugs
DIBUCAINE
An LA with an amide linkage , inhibits activity of normal plasma cholinesterase enzyme by approximately 80% (Dibucaine 80) In atypical homozygous enzyme inhibits approx. 20% of enzyme activity (Dibucaine 20)
EaEa
EuEa
20
60
20
45
EuEf EfEa
75 45
50 35
1 in 3200
1 in 480
1 in 200 1 in 20000
DIBUCAINE NUMBER
A dibucaine number of 80, which reflects 80% inhibition of enzyme xtvt normal response A dibucaine number of 20, reflects the presence of atypical homozygous enzymes, where blockade persist for > 3hours Heterozygous atypical enzyme manifest prolonged blockade up to 30minutes
Absorption
rapid onset and a short duration of action. complete muscle relaxation occurs within to 1 minute, persists for about 2-3 minutes, and gradually dissipates within 10 minutes. Following IM administration the onset of action occurs in about 2-3 minutes, with a duration ranging from 10-30 minutes.
Distribution
Initial rapid redistribution SUXAMETHONIUM crosses the placenta, generally in small amounts.
Metabolism
- By plasma pseudocholinesterases to succinylmonocholine and choline. - Succinylmonocholine further hydolyzed to succinic acid and choline
Elimination
- Approximately 10% of drug is excreted unchanged in the urine. - Patients with impaired renal function may occasionally experience prolonged apnoea due to accumulation of succinylmonocholine.
EFFECT
- Fasciculation followed by phase I block - with repeated dose or administration of a large dose, results a phase II block -- ICP and IOP raised - Repeated doses might results bradycardia and slight increase in MAP - Apneoa occurs subsequently after paralysis -Increase in intragastric pressure - lower oesophageal sphincter tone decrease - Salivation & gastric secretions are increased - Serum potassium briefly increased by 0.2-0.4mmol/L
CVS Respiratory GI
metabolic
ADVERSE EFFECT
Cardiac dysrhythmias Hyperkalemia Myalgia Myoglobinuria Increased intragastric pressure Increased IOP/ICP Sustained skeletal muscle contraction
CONTRAINDICATIONS OF USE
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