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GOOD BYE SUXAMETHONIUM. Prof. Dr. I. CHANDRASEKARAN, MD.,DA., DIRECTOR i/c INSTITUTE OF ANAESTHESIOLOGY MADURAI MEDICAL COLLEGE & GOVT. RAJAJI HOSPITAL, MADURAI. INTRODUCTION. WHY? IS IT POSSIBLE? HOW?. HISTORY.
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Prof. Dr. I. CHANDRASEKARAN, MD.,DA.,
INSTITUTE OF ANAESTHESIOLOGY
MADURAI MEDICAL COLLEGE
GOVT. RAJAJI HOSPITAL, MADURAI
IS IT POSSIBLE?
It was introduced in clinical practice around 1951 by various people in different parts of the world
PHASE 2 BLOCK
RAISE IN ICT , IOT
THESE DRUGS WERE THOUGHT TO BE INDISPENSIBLE IN ANAESTHESIA PRACTICE…
SO COULD BE SUXAMETHONIUM !
ALL THESE AGENTS WERE TRIED BUT NONE COULD REPLACE SUXAMETHONIUM
Intubation Conditions Provided by Rapacuronium (ORG 9487) or Succinylcholine in Humans during Anesthesia with Fentanyl and Propofol Fleming, Neal W. M.D., Ph.D.; Chung, Frances M.D.; Glass, Peter S
THIS IS COMPARABLE TO SUXAMETHONIUM
• Decrease in NMBA concentration
• Increase in acetylcholine
ALONG WITH IT (PROBLEMS OF ANTICHOLINERGIC DRUGS)
and completely reverse NMB, irrespective
of the depth of blockade and without the
need to manage the side effects of currently
available reversal drugs
• The properties of an improved reversal drug
will offer real and important patient benefits
They have been tried as solubilising agents for various drugs like Propofol, bupivacaine, sufentanil
Szejtli J. (1988). "Cyclodextrin Technology"vol 1. Springer, New York
Eight sugar side chains are added to make the gamma cyclodextrin bigger to accommodate the rocuronium molecule
Bom A, Bradley M, Cameron K, et al. A novel concept of reversing neuromuscular block: chemical encapsulation of rocuronium bromide by a cyclodextrin-based synthetic host. Angew Chem IntEd Engl 2002;41:266 –70.
SELECTIVE RELAXANT BINDING AGENT (SRBA)
Sugammadex: Another Milestone in Clinical Neuromuscular Pharmacology , Mohamed Naquib, MB, BCh, MSc, FFARCSI, MD
ROCURONIUM > VECURONIUM > PANCURONIUM
• Volume of distribution ≈ 12-15 L
• Plasma half-life ≈ 2.2 h
• Clearance ≈91 mL/min (≈ GFR)
• No metabolism
• Blood-brain barrier penetration
(< 3% in rat)
• Placental transfer (< 2-6%) in rat and rabbit)
TWO TYPES OF BINDING INTERACTIONS
Another drug binding to sugammadex,
causing rise in free NMBA concentration
Sugammadex binding another drug, decreasing its free concentrations
• Drugs used in anesthesia
• Drugs / hormones with steroidal nucleus
• Drugs acting on steroidal receptors
• Drugs most commonly prescribed
The highest affinity constant - for REMIFENTANIL ( 0.2% of the affinity constant of sugammadex with rocuronium)
But no clinical evidence of interactions was found during clinical trials in approximately 2000 patients
ANTON BOM.,MD., PhD, SENIOR RESEARCH FELLOW, PHARMACOLOGY
NONE WERE SERIOUS
Sorgenfrei IF, Norrild K, Larsen PB, et al. Reversal of rocuronium-induced neuromuscular block by the selective relaxant binding agent sugammadex: a dose-finding and safety study. Anesthesiology 2006;104:667–74.
In one study, PROLONGATION OF THE CORRECTED QT interval was noted in five subjects who received placebo and in three subjects who received sugammadex
suggest risk for adverse effects on any target organ for all life stages
2.0 – 4.0 mg/kg -Reverses rocuronium-induced neuromuscular blockade within 3 min
8.0 mg/kg - 3 min after the administration of 0.6 mg/kg rocuronium results in the recovery of the TOF ratio to 0.9 within 2 min
16 mg/kg -Reverses 1.2mg/kg of rocuronium within 3 mins
• Rapid and complete recovery from rocuronium-induced NMB in normal and RENALLY Impaired patients
• Both doses (2 AND 4 MG/KG ) were efficacious in pulmonary and cardiac patients
• No clinical evidence of residual NMB
• Reversal of profound rocuronium-induced (1.2mg/kg) neuromuscular block with sugammadex was significantly
FASTER THAN SPONTANEOUS RECOVERY FROM SUCCINYLCHOLINE
Sugammadex offers the possibility of IMMEDIATE REVERSAL of rocuronium-induced block in a possible scenario of
FAILED VENTILATION / FAILED INTUBATION
Studies using succinylcholine have indicated that the risk of desaturation in the immediate postinduction period is much greater than initially recognized in “cannot intubate, cannot ventilate” situations.
The use of extrinsically administered cysteine to deliberately accelerate reversal of gantacurium is being investigated currently.
Provides complete and rapid reversal of profound neuromuscular blockade
With Sugammadex it is now possible to achieve rapid onset and fast recovery from neuromuscular block
ROCURONIUM SUGAMMADEX COMBINATION IS PROMISING US A SAFER FUTURE IN ANAESTHESIA
GOOD BYE TO
ARE NOT FAR OFF