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Comparative Opioid Pharmacology: Evidence Based Rationale Steven L. Shafer, M.D. Palo Alto VA Health Care System Stanford University School of Medicine University of California at San Francisco Please Fasten Safety Belts Prior to Take Off Pharmacokinetics: Volume of Distribution
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Steven L. Shafer, M.D.
Palo Alto VA Health Care System
Stanford University School of Medicine
University of California at San Francisco
100
Rapid
10
Concentration
Intermediate
Slow
1
0
120
240
360
480
600
Minutes since bolus injection
100
10
Percent of peak plasma opioid concentration
fentanyl
1
sufentanil
alfentanil
0.1
360
480
600
240
0
120
Minutes since bolus injection
120
fentanyl
90
alfentanil
Minutes required
60
sufentanil
30
0
240
360
480
600
0
120
Minutes since beginning of infusion
60
fentanyl
40
Minutes required
alfentanil
20
sufentanil
0
240
360
480
600
0
120
Minutes since beginning of infusion
300
fentanyl
240
alfentanil
180
Minutes required
120
sufentanil
60
0
240
360
480
600
0
120
Minutes since beginning of infusion
Gregg K, Varvel JR, Shafer SL. J Pharmacokinet Biopharm 20, 611-635, 1992
Gregg K, Varvel JR, Shafer SL. J Pharmacokinet Biopharm 20, 611-635, 1992
Scott J, Ponganis KV, Stanski DR. Anesthesiology 62:234-241, 1985
Scott J, Ponganis KV, Stanski DR. Anesthesiology 62:234-241, 1985
Comparison of sufentanil - O2 and Fentanyl - O2 for coronary artery surgery
de Lange S, Boscoe MJ, Stanley TH, Pace N.
Anesthesiology 56:112-118, 1982
long half-life!
Lang et al, Anesthesiology 85, 721-728, 1996
400
Intubation
300
Maintenance
200
Alfentanil Concentration (ng/ml)
Emergence
100
0
0
2
4
6
8
10
Propofol Concentration (mg/ml)
Propofol Anesthesia and Rational Opioid Selection
Determination of Optimal EC50-EC95 Propofol-Opioid
Concentrations that Assure Adequate Anesthesia and a Rapid
Return on Consciousness
Jaap Vuyk, M.D., Ph.D., Martijn J. Mertens, M.D., Erik Olofsen, M.Sc., Anton G.L. Burm, M.Sc, Ph.D.
James G. Bovill, M.D., Ph.D., F.F.A.R.C.S.I.
Anesthesiology 1997; 87:1549-62
Optimal Maintenance Propofol / Opioid Concentrations
Sufentanil (ng/ml)
40
35
30
25
Fentanyl
Minutes for Recovery
20
Alfentanil
15
Sufentanil
10
5
Remifentanil
0
0
120
240
360
480
600
Infusion Duration (minutes)
Presentation can be downloaded from:
http//:anesthesia.stanford.edu
1. Navigate to “Online Lectures” 2. Navigate to “Pharmacology” 3. Download “Comparative Opioid Pharmacology” 4. Use broadband connection: presentation is 6 MB
