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A Journal on Anesthesiology, Resuscitation, Analgesia and Intensive Care

Official Journal of the Italian Society of Anesthesiology, Analgesia, Resuscitation and Intensive Care
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Minerva Anestesiologica 2000 May;66(5):414-6

language: English

Drug development in anaesthesia: the Remi-fentanil

Haigh C. G.

Metabolic, Cardiovascular and Oncology Therapeutic Development Group Glaxo Wellcome - Greenford (UK)

Drug devel­op­ment in anaesthe­sia pos­es spe­cif­ic chal­leng­es. Describing the devel­op­ment of remi­fen­ta­nil high­lights ­some of ­these. A new ­drug in anaesthe­sia ­must ­achieve its clin­i­cal ­goals in all ­patients and sig­nif­i­cant lev­els of tox­ic­ity are unac­cept­able. Rather ­than ask­ing, “What new ­drugs ­does the anaesthe­tist ­need?” it may be ­more rel­e­vant to ­pose the ques­tion, “How can we ­design ­drugs to do ­things bet­ter?”. Recent ­trends in anaesthe­sia ­have led to the devel­op­ment of ­short act­ing ­agents - one of ­these ­agents, remi­fen­ta­nil, has ­been ­designed to pro­vide a µ-opi­oid recep­tor ago­nist ­with a rap­id and pre­dict­able off­set of ­action. The inser­tion of an ­alkyl ­ester ­group ­into ­this 4-anil­i­dop­i­per­i­dine mole­cule has result­ed in a com­pound ­which, ­whilst retain­ing the ­desired µ-opi­oid recep­tor phar­ma­col­o­gy, is sus­cep­ti­ble to metab­olism by non-spe­cif­ic este­ras­es in the ­blood and tis­sues. The rap­id ­onset and off­set of ­action ­means ­that the anaesthe­tist can deliv­er ­high dos­es of opi­oid result­ing in ­stable anaesthe­sia and the ­lack of accu­mu­la­tion ­ensures ­that ­even ­after pro­longed infu­sion remi­fen­ta­nil ­does not com­pro­mise recov­ery. This abil­ity to con­trol the anaesthet­ic pro­cess has rel­e­vance in ­both ­short and ­long pro­ce­dures and the ­unique char­ac­ter­is­tics of remi­fen­ta­nil may ­also in the ­future ­prove to ­have util­ity in the inten­sive ­care set­ting.

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