New skeletal muscle relaxants. 1995

J E Caldwell
University of California, San Francisco, School of Medicine, USA.

In a little over 10 years, six new muscle relaxants have been introduced in clinical practice. The first two, intermediate-duration vecuronium and atracurium, were outstanding drugs and clearly an advance over the earlier, longer-acting drugs. With their introduction, the phenomenon of "recurarization" largely disappeared. The next two, long-acting doxacurium and pipecuronium, were relics of an earlier era and have made little clinical impact. Mivacurium created a new class, the short-acting nondepolarizing relaxant, and caused succinylcholine to be reclassified as an ultra-short-acting drug. However, mivacurium has neither the rapid onset nor the ultra-short duration of succinylcholine. Rocuronium is the first nondepolarizing relaxant with an onset approaching that of succinylcholine. It is likely that we will see the introduction of at least two more drugs, Org 9487 and 51W89, by the end of this decade, and the goal of developing a nondepolarizing relaxant that is a complete replacement for succinylcholine may not be too far in the future.

UI MeSH Term Description Entries
D007546 Isoquinolines A group of compounds with the heterocyclic ring structure of benzo(c)pyridine. The ring structure is characteristic of the group of opium alkaloids such as papaverine. (From Stedman, 25th ed)
D003473 Neuromuscular Nondepolarizing Agents Drugs that interrupt transmission at the skeletal neuromuscular junction without causing depolarization of the motor end plate. They prevent acetylcholine from triggering muscle contraction and are used as muscle relaxants during electroshock treatments, in convulsive states, and as anesthesia adjuvants. Curare-Like Agents,Curariform Drugs,Muscle Relaxants, Non-Depolarizing,Neuromuscular Blocking Agents, Competitive,Nondepolarizing Blockers,Agents, Curare-Like,Agents, Neuromuscular Nondepolarizing,Blockers, Nondepolarizing,Curare Like Agents,Drugs, Curariform,Muscle Relaxants, Non Depolarizing,Non-Depolarizing Muscle Relaxants,Nondepolarizing Agents, Neuromuscular
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000077123 Rocuronium An androstanol non-depolarizing neuromuscular blocking agent. It has a mono-quaternary structure and is a weaker nicotinic antagonist than PANCURONIUM. Androstane-3,17-diol, 2-(4-morpholinyl)-16-(1-(2-propen-1-yl)-1-pyrrolidiniumyl)-, 17-acetate, (2beta,3alpha,5alpha,16beta,17beta)-,1-(17-(Acetoyl)-3-hydroxy-2-(4-morpholinyl)androstan-16-yl)-1-(2-propenyl)pyrrolidinium,Esmeron,Esmerone,ORG 9426,ORG-9426,Pyrrolidinium, 1-((2beta,3alpha,5alpha,16beta,17beta)-17-(acetyloxy)-3-hydroxy-2-(4-morpholinyl)androstan-16-yl)-1-(2-propenyl)-, bromide,Rocuronium Bromide,Zemuron,ORG9426
D000077590 Mivacurium An isoquinoline derivative that is used as a short-acting non-depolarizing agent. BW B1090U,BW-B 1090U,BW-B-1090U,BW-B1090U,Mivacron,Mivacurium Chloride,BW B 1090U,BWB 1090U,BWB1090U
D000732 Androstanols Androstanes and androstane derivatives which are substituted in any position with one or more hydroxyl groups. Hydroxyandrostanes
D001279 Atracurium A non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents. Atracurium Besylate,Atracurium Dibesylate,33 A 74,Atracurium Besilate,BW-33A,Relatrac,Tracrium,A 74, 33,BW 33A,BW33A,Besilate, Atracurium
D013390 Succinylcholine A quaternary skeletal muscle relaxant usually used in the form of its bromide, chloride, or iodide. It is a depolarizing relaxant, acting in about 30 seconds and with a duration of effect averaging three to five minutes. Succinylcholine is used in surgical, anesthetic, and other procedures in which a brief period of muscle relaxation is called for. Succinyldicholine,Suxamethonium,Anectine,Celocurine,Dicholine Succinate,Ditilin,Listenon,Lysthenon,Myorelaxin,Quelicin,Succicuran,Succinylcholine Chloride,Succinylcholine Dibromide,Succinylcholine Dichloride,Succinylcholine Dichloride, Di-H2O,Succinylcholine Diiodide,Succinylcholine Diperchlorate,Succinylcholine Iodide,Suxamethonium Bromide,Suxamethonium Chloride,Bromide, Suxamethonium,Dibromide, Succinylcholine,Dichloride, Succinylcholine,Diiodide, Succinylcholine,Diperchlorate, Succinylcholine,Succinate, Dicholine,Succinylcholine Dichloride, Di H2O
D014673 Vecuronium Bromide Monoquaternary homolog of PANCURONIUM. A non-depolarizing neuromuscular blocking agent with shorter duration of action than pancuronium. Its lack of significant cardiovascular effects and lack of dependence on good kidney function for elimination as well as its short duration of action and easy reversibility provide advantages over, or alternatives to, other established neuromuscular blocking agents. NC-45,Norcuron,ORG-NC 45,ORG-NC-45,ORG-NC45,Vecuronium,Vecuronium Bromide, Quaternary Ion,Vecuronium Citrate,Vecuronium Hydrobromide,Vecuronium Hydrochloride,Vecuronium Maleate,Vecuronium Phosphate,Bromide, Vecuronium,Citrate, Vecuronium,Hydrobromide, Vecuronium,Hydrochloride, Vecuronium,Maleate, Vecuronium,NC 45,NC45,ORG NC 45,ORG NC45,ORGNC 45,ORGNC45,Phosphate, Vecuronium
D017300 Pipecuronium A piperazinyl androstane derivative which is a non-depolarizing neuromuscular blocking agent (NEUROMUSCULAR NONDEPOLARIZING AGENTS). It is used as a muscle relaxant during ANESTHESIA and surgical procedures. Pipecurium,Arduan,Pipecurium Bromide,Pipecuronium Bromide,Pipecuronium Dibromide, (16 alpha)-Isomer,Pipecuronium Dibromide, (17 alpha)-Isomer,Pipecuronium Dibromide, (3 beta)-Isomer,Pipecuronium Dibromide, Dihydrate,Pipecuronium, Dibromide,RGH-1106,Bromide, Pipecurium,Bromide, Pipecuronium,Dibromide Pipecuronium,Dibromide, Dihydrate Pipecuronium,Dihydrate Pipecuronium Dibromide,RGH 1106,RGH1106

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