Dose comparison of Remifentanil and Alfentanil for loss of consciousness

被引:66
作者
Jhaveri, R [1 ]
Joshi, P [1 ]
Batenhorst, R [1 ]
Baughman, V [1 ]
Glass, PSA [1 ]
机构
[1] DUKE UNIV,MED CTR,DEPT ANESTHESIA,DURHAM,NC 27710
关键词
anesthetics; intravenous; remifentanil; alfentanil; analgesics; potency; anesthetic; median effective dose (ED50); median effective concentration (EC50);
D O I
10.1097/00000542-199708000-00011
中图分类号
R614 [麻醉学];
学科分类号
100217 ;
摘要
Background: This study evaluated the efficacy and safety of remifentanil, a potent mu agonist opioid with a rapid onset and offset of effect, as a sole induction agent for loss of consciousness (LOC) and compared it with alfentanil. Methods: Remifentanil and alfentanil were administered intravenously over 2 min in ascending doses (remifentanil 2, 3, 4, 5, 6, 8, 10, 15, 20 mu g/kg; alfentanil 40, 60, 80, 100, 120, 160, 200 mu g/kg) to unpremedicated healthy patients, Patients were observed for rigidity and LOC for 30 s after the end of infusion. if patients had not lost consciousness, 2 mg.kg(-1).min(-1) thiopental was administered until LOC was achieved. Arterial blood samples, obtained at specified time intervals, were analyzed for remifentanil and alfentanil whole-blood concentration. Blood pressure and heart rate were also recorded at preset time intervals. Results: Neither drug could reliably produce LOC. With both drugs, there was a dose-dependent decrease in thiopental requirements and a dose-dependent increase in the incidence and severity of rigidity (P < 0.05). The median effective dose (ED50) for LOC with remifentanil was 12 mu g/kg, and for alfentanil it was 176 mu g/kg. The median effective concentration (EC50; whole-blood concentration) of remifentanil was 53.8 ng/ml and for alfentanil it was 1,012 ng/ml. Minimal hemodynamic changes were observed after either drug was given. Conclusions: Remifentanil is 15 times more potent than alfentanil, based on the ED50 to achieve loss of response to a verbal command and 20 times more potent than alfentanil based on the EC50. Neither opioid is suitable as a sole induction agent.
引用
收藏
页码:253 / 259
页数:7
相关论文
共 16 条
[1]   PHYSIOLOGY OF ALFENTANIL-INDUCED RIGIDITY [J].
BENTHUYSEN, JL ;
SMITH, NT ;
SANFORD, TJ ;
HEAD, N ;
DECSILVER, H .
ANESTHESIOLOGY, 1986, 64 (04) :440-446
[2]   THE PHARMACOKINETICS OF THE NEW SHORT-ACTING OPIOID REMIFENTANIL (GI87084B) IN HEALTHY ADULT MALE-VOLUNTEERS [J].
EGAN, TD ;
LEMMENS, HJM ;
FISET, P ;
HERMANN, DJ ;
MUIR, KT ;
STANSKI, DR ;
SHAFER, SL .
ANESTHESIOLOGY, 1993, 79 (05) :881-892
[3]   REMIFENTANIL VERSUS ALFENTANIL - COMPARATIVE PHARMACODYNAMICS [J].
EGAN, TD ;
MINTO, C ;
LEMMENS, HJM ;
MUIR, KT ;
HERMANN, DJ ;
SHAFER, SL .
ANESTHESIOLOGY, 1994, 81 (3A) :A374-A374
[4]   DESIGN, SYNTHESIS, AND PHARMACOLOGICAL EVALUATION OF ULTRASHORT-ACTING TO LONG-ACTING OPIOID ANALGESICS [J].
FELDMAN, PL ;
JAMES, MK ;
BRACKEEN, MF ;
BILOTTA, JM ;
SCHUSTER, SV ;
LAHEY, AP ;
LUTZ, MW ;
JOHNSON, MR ;
LEIGHTON, HJ .
JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (07) :2202-2208
[5]  
GLASS PSA, 1993, ANESTH ANALG, V77, P1031
[6]   DETERMINATION OF REMIFENTANIL IN HUMAN BLOOD BY LIQUID-LIQUID-EXTRACTION AND CAPILLARY GC-HRMS-SIM USING A DEUTERATED INTERNAL STANDARD [J].
GROSSE, CM ;
DAVIS, IM ;
ARRENDALE, RF ;
JERSEY, J ;
AMIN, J .
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, 1994, 12 (02) :195-203
[7]  
HALL RI, 1987, ANESTH ANALG, V66, pS76
[8]   Reduction of isoflurane minimal alveolar concentration by remifentanil [J].
Lang, E ;
Kapila, A ;
Shlugman, D ;
Hoke, JF ;
Sebel, PS ;
Glass, PSA .
ANESTHESIOLOGY, 1996, 85 (04) :721-728
[9]   DETERMINATION OF ALFENTANIL AND NORALFENTANIL IN HUMAN PLASMA BY GAS-CHROMATOGRAPHY MASS-SPECTROMETRY [J].
MAUTZ, DS ;
LABROO, R ;
KHARASCH, ED .
JOURNAL OF CHROMATOGRAPHY B-BIOMEDICAL APPLICATIONS, 1994, 658 (01) :149-153
[10]   ED50 OF ALFENTANIL FOR INDUCTION OF ANESTHESIA IN UNPREMEDICATED YOUNG-ADULTS [J].
MCDONNELL, TE ;
BARTKOWSKI, RR ;
WILLIAMS, JJ .
ANESTHESIOLOGY, 1984, 60 (02) :136-140