Remifentanil up2date – Teil 1

Zusammenfassung

Remifentanil ist ein kurzwirksames, potentes Opioid mit guter Steuerbarkeit – und vor allem in der ambulanten Anästhesiologie nahezu unverzichtbar. Umso härter trifft uns die seit 2016 eingeschränkte Verfügbarkeit und Kontingentierung. Dieser Beitrag liefert einen Überblick über die Substanz, ihre Geschichte und pharmakologischen Eigenschaften.

Abstract

Remifentanil is a short-acting opioid of high analgetic potency and superior controllability. It is widely used in day-case surgery, procedural sedation, for reduction of recovery-times and obstetrics and whenever excellent controllability of opioid effects is needed. Especially in combination with Propofol it is used for target-controlled infusion (TCI). The first part of the article provides readers with information about historical aspects, pharmacological characteristics, effects and side effects of remifentanil.

Kernaussagen

• Remifentanil ist mittlerweile seit 20 Jahren im klinischen Einsatz.

• Die Substanz zeigt aufgrund ihrer starken Aktivierung von MOR-1 und MOR-2 alle bekannten Opioideffekte und entsprechende unerwünschte Wirkungen.

• Vor allem die Thoraxrigidität sowie die vagale Stimulation sind im Gegensatz zu anderen Opioiden von anästhesiologischer Relevanz. Da sich diese vor allem bei Bolusgabe zeigen, sollte diese mit Vorsicht eingesetzt werden.

• Bei Patienten mit Erkrankungen des kardialen Reizleitungssystems sollte Remifentanil ebenfalls sehr vorsichtig eingesetzt werden.

• Pharmazeutisch ist weiterhin die Lagerung des rekonstituierten Konzentrats sowie der Verdünnungslösungen von Interesse.

• Ökologisch spielt die Substanz anscheinend eine untergeordnete Rolle.

Schlüsselwörter

Remifentanil - Pharmakologie - unerwünschte Wirkungen - Lagerung

Key words

Remifentanil - pharmacology - side effects - storage

• Literatur

• 1 James MK, Feldman PL, Schuster SV. et al. Opioid receptor activity of GI 87084B, a novel ultra-short acting analgesic, in isolated tissues. J pharmacol Exp Ther 1991; 259: 712-718
• 2 Eger II, Saidman LawrenceJ, Westhorpe RodN. eds. The wondrous Story of Anesthesia. New York: Springer; 2014
• 3 GlaxoSmithKline GmbH & Co KG. Fachinformationen Ultiva. In: Webpage Rote Liste Service GmbH. Frankfurt: Glaxo Smith Kline; 2015
• 4 Mercier FJ, Benhamou D. Promising non-narcotic analgesic techniques for labour. Baillieres Clin Obstet Gynaecol 1998; 12: 397-407
• 5 Bjorksten AR, Chan C, Crankshaw DP. Determination of remifentanil in human blood by capillary gas chromatography with nitrogen-selective detection. J Chromatogr B Analyt Technol Biomed Life Sci 2002; 775: 97-101
• 6 Remifentanil PD. Remifentanil 2015.
• 7 KRINKO. Anforderungen an die Hygiene bei Punktionen und Injektionen. Bundesgesundheitsbl 2011; 54: 1135-1144
• 8 Bevans T, Deering-Rice C, Stockmann C. et al. Inhaled remifentanil in rodents. Anesth Analg 2016; 122: 1831-1838
• 9 Hermann DJ, Egan TD, Muir KT. Influence of arteriovenous sampling on remifentanil pharmacokinetics and pharmacodynamics. Clin Pharmacol Ther 1999; 65: 511-518
• 10 Duthie DJ, Stevens JJ, Doyle AR. et al. Remifentanil and pulmonary extraction during and after cardiac anesthesia. Anesth Analg 1997; 84: 740-744
• 11 Lee CW, Ho IK. Sex differences in opioid analgesia and addiction: interactions among opioid receptors and estrogen receptors. Mol Pain 2013; 9: 45
• 12 Liu XY, Liu ZC, Sun YG. et al. Unidirectional cross-activation of GRPR by MOR1D uncouples itch and analgesia induced by opioids. Cell 2011; 147: 447-458
• 13 Watanabe K, Kashiwagi K, Kamiyama T. et al. High-dose remifentanil suppresses stress response associated with pneumoperitoneum during laparoscopic colectomy. J Anesth 2014; 28: 334-340
• 14 Myre K, Raeder J, Rostrup M. et al. Catecholamine release during laparoscopic fundoplication with high and low doses of remifentanil. Acta Anaesthesiol Scand 2003; 47: 267-273
• 15 Watanabe M, Shimizu H, Kikuchi C. [Anesthetic management with remifentanil infusion during laparoscopic cholecystectomy]. Masui 2009; 58: 1232-1235
• 16 Minto CF, Schnider TW, Egan TD. et al. Influence of age and gender on the pharmacokinetics and pharmacodynamics of remifentanil. I. Model development. Anesthesiology 1997; 86: 10-23
• 17 Egan TD, Minto CF, Hermann DJ. et al. Remifentanil versus alfentanil: comparative pharmacokinetics and pharmacodynamics in healthy adult male volunteers. Anesthesiology 1996; 84: 821-833
• 18 Drover DR, Lemmens HJ. Population pharmacodynamics and pharmacokinetics of remifentanil as a supplement to nitrous oxide anesthesia for elective abdominal surgery. Anesthesiology 1998; 89: 869-877
• 19 Mertens MJ, Engbers FH, Burm AG. et al. Predictive performance of computer-controlled infusion of remifentanil during propofol/remifentanil anaesthesia. Br J Anaesth 2003; 90: 132-141
• 20 Anderson BJ. Pediatric models for adult target-controlled infusion pumps. Paediatr Anaesth 2010; 20: 223-232
• 21 Yeganeh N, Roshani B, Yari M. et al. Target-controlled infusion anesthesia with propofol and remifentanil compared with manually controlled infusion anesthesia in mastoidectomy surgeries. Middle East J Anaesthesiol 2010; 20: 785-793
• 22 Moerman AT, Herregods LL, De Vos MM. et al. Manual versus target-controlled infusion remifentanil administration in spontaneously breathing patients. Anesth Analg 2009; 108: 828-834
• 23 Short TG, Hannam JA, Laurent S. et al. Refining target-controlled infusion: an assessment of pharmacodynamic target-controlled infusion of propofol and remifentanil using a response surface model of their combined effects on bispectral index. Anesth Analg 2016; 122: 90-97
• 24 Liu Y, Li M, Yang D. et al. Closed-loop control better than open-loop control of profofol TCI guided by BIS: a randomized, controlled, multicenter clinical trial to evaluate the CONCERT-CL closed-loop system. PloS One 2015; 10: e0123862
• 25 Choe S, Choi BM, Lee YH. et al. Response-surface modelling of the pharmacodynamic interaction between propofol and remifentanil in patients undergoing anaesthesia. Clin Exper Pharmacol Physiol 2017; 44: 30-40
• 26 Manyam SC, Gupta DK, Johnson KB. et al. Opioid-volatile anesthetic synergy: a response surface model with remifentanil and sevoflurane as prototypes. Anesthesiology 2006; 105: 267-278
• 27 Heyse B, Proost JH, Schumacher PM. et al. Sevoflurane remifentanil interaction: comparison of different response surface models. Anesthesiology 2012; 116: 311-323
• 28 Alsina E, Matute E, Ruiz-Huerta AD. et al. The effects of sevoflurane or remifentanil on the stress response to surgical stimulus. Curr Pharm Des 2014; 20: 5449-5468
• 29 Davis JJ, Buck NS, Swenson JD. et al. Serotonin syndrome manifesting as patient movement during total intravenous anesthesia with propofol and remifentanil. J Clin Anesth 2013; 25: 52-54
• 30 Loyd DR, Murphy AZ. The neuroanatomy of sexual dimorphism in opioid analgesia. Exp Neurol 2014; 259: 57-63
• 31 Kim SY, Song MK, Kim MS. et al. Sex-related differences in the effect-site concentration of remifentanil for preventing QTc interval prolongation following intubation in elderly patients with a normal QTc interval. Drugs Aging 2014; 31: 695-702
• 32 Soh S, Park WK, Kang SW. et al. Sex differences in remifentanil requirements for preventing cough during anesthetic emergence. Yonsei Med J 2014; 55: 807-814
• 33 Lee BW, Kim SH, So KY. The effect of gender on EC(50) of remifentanil to prevent pain during injection of microemulsion propofol. Korean J Anesthesiol 2012; 63: 504-509
• 34 Joe HB, Kim JY, Kwak HJ. et al. Effect of sex differences in remifentanil requirements for the insertion of a laryngeal mask airway during propofol anesthesia: A prospective randomized trial. Medicine 2016; 95: e5032
• 35 Park SJ, Park HJ, Choi JY. et al. The influence of age and gender on remifentanil EC(50) for preventing rocuronium induced withdrawal movements. Korean J Anesthesiol 2010; 58: 244-248
• 36 Hossain A, Sullivan P. The effects of age and sex on electroconvulsive therapy using remifentanil as the sole anesthetic agent. J ECT 2008; 24: 232-235
• 37 Freye E. Opioids in Medicine. Monographie 2008. Dordrecht: Springer; 2008: 90-233
• 38 Min SK, Kim DH, Cho HB. et al. Limited maximal flow rate of target-controlled remifentanil infusion and induced cough. Anaesthesia 2012; 67: 145-148
• 39 Kim H, Choi SH, Choi YS. et al. Comparison of the antitussive effect of remifentanil during recovery from propofol and sevoflurane anaesthesia. Anaesthesia 2012; 67: 765-770
• 40 Lee JH, Koo BN, Jeong JJ. et al. Differential effects of lidocaine and remifentanil on response to the tracheal tube during emergence from general anaesthesia. Br J Anaesth 2011; 106: 410-415
• 41 Del Blanco Narciso BB, Jimeno Fernandez C, Almendral Garrote J. et al. Effects of remifentanil on the cardiac conduction system. Our experience in the study of remifentanil electrophysiological properties. Curr Pharm Des 2014; 20: 5489-5496
• 42 Jung HS, Joo JD, Jeon YS. et al. Comparison of an intraoperative infusion of dexmedetomidine or remifentanil on perioperative haemodynamics, hypnosis and sedation, and postoperative pain control. J Int Med Res 2011; 39: 1890-1899
• 43 Mireskandari SM, Abulahrar N, Darabi ME. et al. Comparison of the effect of fentanyl, sufentanil, alfentanil and remifentanil on cardiovascular response to tracheal intubation in children. Iran J Pediatr 2011; 21: 173-180
• 44 Bilgin H, Basagan Mogol E, Bekar A. et al. A comparison of effects of alfentanil, fentanyl, and remifentanil on hemodynamic and respiratory parameters during stereotactic brain biopsy. J Neurosurg Anesthesiol 2006; 18: 179-184
• 45 Guo X, Yi J, Ye T. et al. Comparison of remifentanil and fentanyl in patients undergoing modified radical mastectomy or total hysterectomy. Chin Med J (Engl) 2003; 116: 1386-1390
• 46 Joo HS, Salasidis GC, Kataoka MT. et al. Comparison of bolus remifentanil versus bolus fentanyl for induction of anesthesia and tracheal intubation in patients with cardiac disease. J Cardiothorac Vasc Anesth 2004; 18: 263-268
• 47 Doyle PW, Coles JP, Leary TM. et al. A comparison of remifentanil and fentanyl in patients undergoing carotid endarterectomy. Eur J Anaesthesiol 2001; 18: 13-19
• 48 Schuttler J, Albrecht S, Breivik H. et al. A comparison of remifentanil and alfentanil in patients undergoing major abdominal surgery. Anaesthesia 1997; 52: 307-317
• 49 Rollins MD, Feiner JR, Lee JM. et al. Pupillary effects of high-dose opioid quantified with infrared pupillometry. Anesthesiology 2014; 121: 1037-1044
• 50 Neidhart P, Burgener MC, Schwieger I. et al. Chest wall rigidity during fentanyl- and midazolam-fentanyl induction: ventilatory and haemodynamic effects. Acta Anaesthesiol Scand 1989; 33: 1-5
• 51 Vacanti CA, Silbert BS, Vacanti FX. The effects of thiopental sodium on fentanyl-induced muscle rigidity in a human model. J Clin Anesth 1991; 3: 395-398
• 52 Nakada J, Nishira M, Hosoda R. et al. Priming with rocuronium or vecuronium prevents remifentanil-mediated muscle rigidity and difficult ventilation. J Anesth 2009; 23: 323-328
• 53 Vacanti CA, Silbert BS, Vacanti FX. Fentanyl-induced muscle rigidity as affected by pretreatment with amantadine hydrochloride. J Clin Anesth 1992; 4: 282-284
• 54 Yu EH, Tran DH, Lam SW. et al. Remifentanil tolerance and hyperalgesia: short-term gain, long-term pain?. Anaesthesia 2016; 71: 1347-1362
• 55 Lee M, Silverman SM, Hansen H. et al. A comprehensive review of opioid-induced hyperalgesia. Pain Physician 2011; 14: 145-161
• 56 Chu LF, Dairmont J, Zamora AK. et al. The endogenous opioid system is not involved in modulation of opioid-induced hyperalgesia. J Pain 2011; 12: 108-115
• 57 Rivosecchi RM, Rice MJ, Smithburger PL. et al. An evidence based systematic review of remifentanil associated opioid-induced hyperalgesia. Expert Opin Drug Saf 2014; 13: 587-603
• 58 Zhang W, Liu Y, Hou B. et al. Activation of spinal alpha-7 nicotinic acetylcholine receptor attenuates remifentanil-induced postoperative hyperalgesia. Int J Clin Exp Med 2015; 8: 1871-1879
• 59 Liu M, Zhang H, Du BX. et al. Neurokinin-1 receptor antagonists in preventing postoperative nausea and vomiting: a systematic review and meta-analysis. Medicine 2015; 94: e762
• 60 Rama-Maceiras P, Ferreira TA, Molins N. et al. Less postoperative nausea and vomiting after propofol + remifentanil versus propofol + fentanyl anaesthesia during plastic surgery. Acta Anaesthesiol Scand 2005; 49: 305-311
• 61 Hara R, Hirota K, Sato M. et al. The impact of remifentanil on incidence and severity of postoperative nausea and vomiting in a university hospital-based ambulatory surgery center: a retrospective observation study. Korean J Anesthesiol 2013; 65: 142-146
• 62 Jang JS, Lee JH, Lee JJ. et al. Postoperative nausea and vomiting after myringoplasty under continuous sedation using midazolam with or without remifentanil. Yonsei Med J 2012; 53: 1010-1013
• 63 Kim SH, Oh CS, Yoon TG. et al. Total intravenous anaesthesia with high-dose remifentanil does not aggravate postoperative nausea and vomiting and pain, compared with low-dose remifentanil: a double-blind and randomized trial. ScientificWorldJournal 2014; 2014: 724753
• 64 Savilampi J, Magnuson A, Ahlstrand R. Effects of remifentanil on esophageal motility: a double-blind, randomized, cross-over study in healthy volunteers. Acta Anaesthesiol Scand 2015; 59: 1126-1136
• 65 Wallden J, Thorn SE, Lindberg G. et al. Effects of remifentanil on gastric tone. Acta Anaesthesiol Scand 2008; 52: 969-976
• 66 Fragen RJ, Vilich F, Spies SM. et al. The effect of remifentanil on biliary tract drainage into the duodenum. Anesth Analg 1999; 89: 1561-1564
• 67 Nomura Y, Funai Y, Fujimoto Y. et al. Remifentanil increases the incidence of mesenteric traction syndrome: preliminary randomized controlled trial. J Anesth 2010; 24: 669-674
• 68 Rosow CE, Gomery P, Chen TY. et al. Reversal of opioid-induced bladder dysfunction by intravenous naloxone and methylnaltrexone. Clin Pharmacol Ther 2007; 82: 48-53
• 69 Levine AI, Bryson EO. Intranasal self-administration of remifentanil as the foray into opioid abuse by an anesthesia resident. Anesth Analg 2010; 110: 524-525
• 70 McLeod S, Ball DR. Remifentanil and seizures. Anaesthesia 2000; 55: 1038-1039
• 71 Blair JM, Hill DA. Probable seizure after remifentanil in a 4-year-old boy. Anaesthesia 2000; 55: 501
• 72 Nielsen J, Kroigaard M. Seizures in a 77-year-old-woman after a bolus dose of remifentanil. Acta Anaesthesiol Scand 2004; 48: 253-254
• 73 Haber GW, Litman RS. Generalized tonic-clonic activity after remifentanil administration. Anesth Analg 2001; 93: 1532-1533
• 74 Bousselmi R, Anis Lebbi M, Ben Romdhane M. et al. [Generalised tonic-clonic seizures with sudden decrease in bispectral index values after remifentanil infusion]. Ann Fr Anesth Reanim 2013; 32: 882-883
• 75 Fodale V, Schifilliti D, Pratico C. et al. Remifentanil and the brain. Acta Anaesthesiol Scand 2008; 52: 319-326
• 76 Fa. GlaxoSmithKline, Safety Data Sheet, 2013;. Im Internet: http://www.msds-gsk.com/GetSdsFile.ashx?fileId=2229 Stand: 11.01.2013
• 77 Egan TD, Lemmens HJ, Fiset P. et al. The pharmacokinetics of the new short-acting opioid remifentanil (GI87084B) in healthy adult male volunteers. Anesthesiology 1993; 79: 881-892
• 78 Shafer SL, Varvel JR. Pharmacokinetics, pharmacodynamics, and rational opioid selection. Anesthesiology 1991; 74: 1136-1138
• 79 Eleveld D, Proost JH, Vereecke H. et al. An Allometric Model of Remifentanil Pharmacokinetics and Pharmacodynamics. Anesthesiology 2017; 126: 1005-1018
• 80 Kim TK, Obara S, Egan TD. et al. and the Remifentanil Pharmacokinetics in Obesity Investigators. Disposition of Remifentanil in Obesity: A New Pharmacokinetic Model Incorporating the Influence of Body Mass. Anesthesiology 2017; 126: 1019-1032