Emerging horizons in anaesthetic practice: a pharmacological update
Keywords:Gantacurium, Methoxy carbonyl carboetomidate, Remimazolam, Sugammadex, Tapentadol
Anesthesiologists are in search for new drugs possessing properties like rapid onset of action, minimal residual effects, better hemodynamic stability, organ independent metabolism and cost effective. Structural alterations of the currently available compounds or newer formulations of the older ones or newer anaesthetic drug delivery system will be an useful alternative to newer discovery by reducing the cost and time. Tapentadol is a centrally acting µ opioid receptor (MOR) agonist with selective norepinephrine reuptake inhibition, approved by US FDA for treating moderate to severe acute pain in adults more than 18 years of age. Sugammadex, a novel selective relaxant binding agent to reverse steroidal neuromuscular blockers is recently approved by the European Union. Gantacurium, a rapid and ultra short acting non depolarizing neuromuscular blocker, inactivated rapidly by the adduction of non essential amino acid cysteine to the gantacurium molecule is in clinical trials. Remimazolam is a new drug in clinical trials that has a rapid onset of action like midazolam and is metabolized by non specific tissue esterases like remifentanil and expected to have a promising future. Liposomal Bupivacaine is approved by FDA in October 2011 that uses bupivacaine in liposomal vesicles to extend the duration of analgesia upto 72 hours and reduces the opioid use in the post operative period. Methoxy carbonyl carboetomidate is in clinical trials that combines the advantages of MOC etomidate and carboetomidate. Hence anaesthesiology is marching towards a bright pathway with new soft drugs coming up making not only anaesthesiology soft but also pharmacology.
Heitz JW, Witkowski T, Viscusi ER. New and emerging analgesics and analgesic technologies for acute pain management. Current Opinion in Anesthesiology. 2009;22(5):608-17.
Afilalo M, Stegmann JU, Upmalis D. Tapentadol immediate release: A new treatment option for acute pain management. J Pain Res. 2010;3:1-9.
Power. An update on analgesics. Br J Anaesth. 2011;107(1):19-24.
Wade WE, Spruill WJ. Tapentadol hydrochloride: a centrally acting oral analgesic. Clin Ther. 2009;31(12):2804-18.
Singh DR, Nag K, Shetti AN, Krishnaveni N. Tapentadol hydrochloride: A novel analgesic. Saudi J Anaesth. 2013 Jul-Sep;7(3):322-6.
Tayal G, Kundra S, Grewal A. Sugammadex - New Neuromuscular Block Reversal. J Anaesth Clin Pharmacol. 2008;24(2):211-4.
Sorgenfrei IF, Norrild K, Larsen PB, Stensballe J, Ostergaard D, Prins ME, et al. Reversal of Rocuronium-induced Neuromuscular Block by the Selective Relaxant Binding Agent Sugammadex A Dose-finding and Safety Study. The Journal of the American Society of Anesthesiologists. 2006 Apr 1;104(4):667-74.
Bom A, Bradley M, Cameron K, Clark JK, van Egmond J, Feilden H, et al. A novel concept of reversing neuromuscular block: chemical encapsulation of rocuronium bromide by a cyclodextrin‐based synthetic host. Angewandte Chemie. 2002 Jan 18;114(2):275-80.
Sparr HJ, Vermeyen KM, Beaufort AM, Rietbergen H, Proost JH, Saldien V, et al. Early reversal of profound rocuronium-induced neuromuscular blockade by sugammadex in a randomized multicenter study. Anesthesiology. 2007 May;106(5):935-43.
Lien CA. Development and potential clinical impact of ultra-short acting neuromuscular blocking agents. Br J Anaesth 2011;107(1):60-71.
Belmont MR, Lien CA, Tjan J, Bradley E, Stein B, Patel SS, et al. Clinical pharmacology of GW280430A in humans. Anesthesiology: The Journal of the American Society of Anesthesiologists. 2004 Apr 1;100(4):768-73.
Sneyd JR, Wright PCM, Cross M, Thompson P, Voortman G, Weideman MM, et al. Administration to man of ORG 21465 a water soluble steroid intravenous anaesthetic agent. British Journal of Anaesthesia. 1997;79:427-32.
Kilpatrick GJ, McIntyre MS, Lovell GG, Wiard RP, Feldman PL, Tilbrook GS. CNS 7056: A Novel Ultra-Short-Acting Benzodiazepine. Anesthesiology. 2007;107:60-6.
Rogers WK, McDowell TS. Remimazolam, a short-acting GABA(A) receptor agonist for intravenous sedation and/or anesthesia in day-case surgical and non-surgical procedures. I Drugs. 2010;13:929-37.
Praveen C, Kennneth CC. Liposomal bupivacaine: a review of a new bupivacaine formulation. J Pain Res. 2012;5:257-64.
Grant GJ, Barenholz Y, Bolotin EM. A novel liposomal bupivacaine formulation to produce ultra-long acting analgesia. Anesthesiology. 2004;101(1):133-7.
Boogaerts. JG, Lafont. ND, Declercq AG. Epidural administration of liposome-associated bupivacaine for the management of postsurgical pain: a first study, Journal of Clinical Anesthesia. 1994;6(4):315-20.
Cotten JF, Hussain SS, Forman SA, Miller KW, Kelly EW, Nguyen HH, et al. A Novel Rapidly Metabolized and Ultra-short-acting Etomidate Analogue that does not produce prolonged Adrenocortical Suppression. Anesthesiology. 2009;111:240-9.
Forman SA. Clinical and Molecular Pharmacology of Etomidate. Anesthesiology. 2011;114:695-707.