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Vol. 38. Issue 1.
Pages 68-83 (February - April 2010)
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Vol. 38. Issue 1.
Pages 68-83 (February - April 2010)
Artículo de Reflexión
Open Access
Fentanilo PK/PD, un medicamento vigente
Phentanyl PK/PD, a valid drug
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Luis Alberto Tafur*, Ana Milena Serna**, Eduardo Lema***
* Médico anestesiólogo, Universidad del Valle, Hospital Universitario del Valle; Clínica Visual y Auditiva, Instituto para Niños Ciegos y Sordos del Valle del Cauca, Cali, Colombia
** Médica anestesióloga, Universidad del Valle, Hospital Universitario del Valle, Cali, Colombia
*** Médico anestesiólogo, Universidad del Valle, Hospital Universitario del Valle; Clínica Visual y Auditiva, Instituto para Niños Ciegos y Sordos del Valle del Cauca; docente, Departamento de Anestesiología, Universidad del Valle, Cali, Colombia
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RESUMEN

Con la aparición de nuevos medicamentos opioides en el mercado de los fármacos anestésicos, podríamos pensar que disponemos de moléculas capaces de reemplazar al legendario fentanilo. Sin embargo, el estudio de sus propiedades farmacocinéticas y farmacodinámicas, nos permite utilizarlo de una manera adecuada, aprovechando su potencia, su excelente analgesia y su seguridad, comparable esta última con los demás opioides cuando se administra con la guía de modelos farmacocinéticos.

Para esto, es necesario tener en cuenta que varios de los medicamentos utilizados con frecuencia durante el acto anestésico (midazolam, dexametasona, prednisolona, ketamina, etc.), pueden influenciar su metabolismo por la enzima citocromo P4503A4.

El conocimiento y la aplicación juiciosa de los modelos farmacocinéticos nos permiten estimar las concentraciones plasmáticas, de modo que nos brinde las mejores condiciones analgésicas, asociadas a un destacado sinergismo con los hipnóticos de uso frecuente, como el propofol y el desfluorano. Su aprovechamiento es máximo cuando se utiliza con una indicación específica, como en cirugía prolongada (mayor de 120 minutos) o que represente un estímulo de percepción del dolor importante para el paciente.

Palabras clave:
fentanilo
farmacocinética
farmacología
nomogramas
anestesia intravenosa (Fuente: DeCS, Bireme)
ABSTRACT

With the advent of the new opioids in the anesthetic drug market, we may think that we have molecules available to replace the legendary fentanyl. However, studying its pharmacodynamic and pharmacokinetic properties, fentanyl can still be appropriately used to take advantage of its excellent analgesia and safety, comparable to that of other opioids when administered in accordance with pharmacokinetic models.

We must not forget however that several drugs frequently used during anesthesia (midazolam, dexametasone, prednisolone, ketamin, etc.), may impact the metabolism of fentanyl on account of the cytochrome P450 3A4 enzyme.

The knowledge and judicious application of pharmacokinetic models serve to estimate plasma concentrations in order to ensure the best analgesic conditions associated to synergies with the frequent use of hypnotics such as propofol and desfluorane. Fentanyl is best used for specific indications such as extended surgical procedures (over 120 minutes) or procedures that stimulate the patient's pain perception.

Key words:
fentanyl
pharmacokinetics
pharmacology
nomograms
intravenous anesthesia (Source: MeSH, NLM)
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REFERENCES
[1.]
H.B. Gutstein, H. Akil.
Opioid Analgesics. En Goodman & Gilman`s.
The Pharmacological Basis of Therapeutics, 11th Ed, pp. 547-590
[2.]
Coda B. Opioids, P.G. En Barash.
Clinical Anesthesia, Fifth edition, pp. 353-383
[3.]
H. Wang, E.Y. Li, G.W. Xu, C.S. Wang, Y.L. Gong, P. Li.
Intravenous fentanyl is exhaled and the concentration fluctuates with time.
J Int Med Res., 37 (2009), pp. 1158-1166
[4.]
I.S. Coral, A.R. Moore, L. Strunin.
Plasma concentrations of fentanyl in normal surgical patients with severe renal failure.
Br J Anaesth., 52 (1980), pp. 101
[5.]
P. Fine, R.K. Portenoy.
Opioid analgesia.
2nd Edition, McGraw Hill, (2007),
[6.]
R.B. Labroo, M.F. Paine, K.E. Thummel, E.D. Kharasch.
Fentanyl metabolism by human hepatic and intestinal cytochrome P450 3A4: implications for interindividual variability in disposition, efficacy, and drug interactions.
Drug Metab Dispos., 25 (1997), pp. 1072-1080
[7.]
H. Stoeckel, J.H. Hengstmann, J. Schüttler.
Pharmacokinetics of fentanyl as a possible explanation for recurrence of respiratory depression.
Br J Anaesth., 51 (1979), pp. 741-745
[8.]
A. Adams, D. Pybus.
Delayed respiratory depression after use of fentanyl during anaesthesia.
Br Med J., 1 (1978), pp. 278-279
[9.]
J.H. Williams.
Delayed respiratory depression after use of fentanyl.
Br Medical J., 1 (1978), pp. 441
[10.]
S. Shafer, J. Varvel.
Pharmacokinetics, Pharmacodynamics, and Rational Opioid Selection.
Anesthesiology., 74 (1991), pp. 53-63
[11.]
A. Yassen, E. Olofsen, R. Romberg, E. Sarton, L. Teppema, M. Danhof.
Mechanism-based PK/PD modeling of the respiratory depressant effect of buprenorphine and fentanyl in healthy volunteers.
Clin Pharmacol Ther., 81 (2007), pp. 50-58
[12.]
E. Magosso, M. Ursino, J.H. van Oostrom.
Opioid-induced respiratory depression: a mathematical model for fentanyl.
IEEE Trans Biomed Eng., 51 (2004), pp. 1115-1128
[13.]
J.E. Sternlo, R.H. Sandin.
Recurrent respiratory depression after total intravenous anaesthesia with propofol and alfentanil.
Anaesthesia., 53 (1998), pp. 378-381
[14.]
B.D. Krane, J.M. Kreutz, D.L. Johnson, J.E. Mazuzan Jr..
Alfentanil and delayed respiratory depression: case studies and review.
Anesth Analg., 70 (1990), pp. 557-561
[15.]
J. Scholz, M. Steinfath, M. Schulz.
Clinical pharmacokinetics of alfentanil, fentanyl and sufentanil.
An update. Clin Pharmacokinet., 31 (1996), pp. 275-292
[16.]
P. Glass, J. Jacobs, R. Smith, B. Ginsberg, T. Quill, S. Bai.
Pharmacokinetic Model-driven Infusion of Fentanyl: Assesment of Accuracy.
Anesthesiology., 73 (1990), pp. 1082-1090
[17.]
S. Shafer, J. Varvel, N. Aziz, J. Scott.
Pharmacokinetics of Fentanyl Administered by Computer – controlled Infusion Pump.
Anesthesiology., 73 (1990), pp. 1091-1102
[18.]
E. Youngs, S. Shafer.
Pharmacokinetic Parameters Relevant to Recovery from Opioids.
Anesthesiology, 81 (1994), pp. 833-842
[19.]
J.C. Scott, D.R. Stanski.
Decreased fentanyl and alfentanil dose requirements with age. A simultaneous pharmacokinetic and pharmacodynamic evaluation..
J Pharmacol Exp Ther., 240 (1987), pp. 159-166
[20.]
K. Shibutani, M. Inchiosa, K. Sawada, M. Bairamian.
Accuracy of Pharmacokinetic Models for Predicting Plasma Fentanyl Concentrations in Lean and Obese Surgical Patients.
Derivation of Dosing Weight (“Pharmacokinetic Mass”). Anesthesiology., 101 (2004), pp. 603-613
[21.]
J. Vuyk, M. Mertens, E. Olofsen, A. Burm, J. Bovill.
Propofol Anesthesia and Rational Opioid Selection: Determination of Optimal EC sub 50 -EC sub 95 Propofol-Opioid Concentrations that Assure Adequate Anesthesia and a Rapid Return of Consciousness.
Anesthesiology., 87 (1997), pp. 1549-1562
[22.]
C. Smith, A. McEwan, R. Jhaveri, M. Wilkinson, D. Goodman, R. Smith.
The Interaction of Fentanyl onthe Cp50 of Propofol for Loss of Conciousness and Skin Incision.
Anethesiology, 81 (1994), pp. 820-828
[23.]
L.H. Mildh, H. Scheinin, O.A. Kirvela.
The concentration-effect relationship of the respiratory depressant effects of alfentanil and fentanyl.
Anesth Analg., 93 (2001), pp. 939-946
[24.]
P. Cartwright, C. Prys-Roberts, K. Gill, A. Dye, M. Stafford, A. Gray.
Ventilatory depression related to plasma fentanyl concentrations during and after anesthesia in humans.
Anesth Analg., 62 (1983), pp. 966-974
[25.]
K. Kaneda, T.H. Han.
Comparative population pharmacokinetics of fentanyl using non-linear mixed effect modeling: burns vs. non-burns..
[26.]
D.E. Koehntop, J.H. Rodman.
Fentanyl pharmacokinetics in patients undergoing renal transplantation.
Pharmacotherapy, 17 (1997), pp. 746-752
[27.]
T. Han, D. Kim, H. Kil, Y. Inagaki.
The effects of plasma fentanyl concentrations on propofol requirement, emergence from anesthesia, and postoperative analgesia in propofol-nitrous oxide anesthesia.
Anesth Analg., 90 (2000), pp. 1365-1371
[28.]
H. Iwakiri, O. Nagata, T. Matsukawa, M. Ozaki, D. Sessler.
Effect-Site Concentration of Propofol for Recovery of Consciousness Is Virtually Independent of Fentanyl Effect-Site Concentration.
Anesth Analg, 96 (2003), pp. 1651-1655
[29.]
T. Ledowski, A. Manopas, S. Lauer.
Bronchial mucus transport velocity in patients receiving desflurane and fentanyl vs. sevoflurane and fentanyl..
Eur J Anaesthesiol., 25 (2008), pp. 752-755
[30.]
J. Feld, W. Hoffman, C. Paisansathan, H. Park, R.C. Ananda.
Autonomic activity during dexmedetomidine or fentanyl infusion with desflurane anesthesia.
J Clin Anesth, 19 (2007), pp. 30-36
[31.]
M. Watcha, P. White.
Postoperative Nausea and Vomiting Its Etiology, Treatment and Prevention.
Anesthesiology, 77 (1992), pp. 162-184
[32.]
H. Yang, P. Choi, McChesney, N. Buckley.
Induction with sevoflurane-remifentanil is comparable to propofol-fentanyl-rocuronium in PONV after laparoscopic surgery..
Can J Anesth, 51 (2004), pp. 660-667
[33.]
P. Phitayakorn, B.M. Melnick, A.F. Vicine 3rd.
Comparison of sufentanil and fentanyl infusions for outpatient anaesthesia.
Can J Anaesth., 34 (1987), pp. 242-245
[34.]
J.W. Flacke, B.C. Bloor, B.J. Kripke, W.E. Flacke, C.M. Warneck, A.P. Van Etten.
Comparison of morphine, meperidine, fentanyl and sufentanil in balanced anesthesia: a double blind study.
Anesth Analg., 64 (1985), pp. 897-910
[35.]
J. Schuttler, S. Albrecht, H. Breivik, S. Osnes, C. Prys-Roberts, K. Holder.
A comparison of remifentanil and alfentanil in patients undergoing major abdominal surgery.
Anaesthesia., 52 (1997), pp. 307-317
[36.]
W.S. Jellish, J.P. Leonetti, A. Avramov, E. Fluder, J. Murdoch.
Remifentanil-based anesthesia versus a propofol technique for otologic surgical procedure.
Otolaryngol Head Neck Surg., 122 (2000), pp. 222-227
[37.]
P. Michalowski, DershwitzM, C.E. Rosow, L.A. Conlay, Y.C. Chang.
Total intravenous anesthesia with remifentanil or alfentanil in ambulatory orthopedic surgery carries minimal risk of postoperative nausea and vomiting.
Anesthesiology, 89 (1998), pp. A34
[38.]
P.J. Davis, J.C. Finkel, R.J. Orr, L. Fazi, J.J. Mulroy, S.K. Woelfel.
A randomised, doble-blind study of remifentanil versus fentanyl for tonsillectomy and adenoidectomy surgery in pediatric ambulatory surgical patients.
Anesth Analg, 90 (2000), pp. 863-871
[39.]
T. Gaszynski, J. Strzelczyk, W. Gaszynski.
Post-anesthesia Recovery after Infusion of Propofol with Remifentanil or Alfentanil or Fentanyl in Morbidly Obese Patients.
Obes Surg., 14 (2004), pp. 498-504
[40.]
S. Langevin, M.R. Lessard, C.A. Trépanier, J.P. Baribault.
Alfentanil causes less postoperative nausea and vomiting than equipotent doses of fentanyl or sufentanil in outpatients.
Anesthesiology., 91 (1999), pp. 1666-1673
[41.]
E.L. Bloomfield.
The incidence of postoperative nausea and vomiting: a retrospective comparison of alfentanil versus sufentanil.
Mil Med., 157 (1992), pp. 59-61
[42.]
P. Rama-Maceiras, T. Ferreira, N. Molins, Y. Sanduende, A. Bautista, T. Rey.
Less postoperative nausea and vomiting after propofol + remifentanil versus propofol + fentanyl anaesthesia during plastic surgery.
Acta Anaesthesiol Scand., 49 (2005), pp. 305-311
[43.]
A. Bowdle.
Adverse Effects of Opioid Agonists and Agonist-Antagonists in Anaesthesia.
Drug Saf., 19 (1998), pp. 173-189
[44.]
J. Streisand, P. Bailey, L. LeMaire, M. Ashburn, S. Tarver, J. Varvel.
Fentanyl-induced rigidity and Unconsciousness in Human Volunteers. Incidence, Duration and Plasma Concentrations.
Anesthesiology, 78 (1993), pp. 629-634
[45.]
T. Bowdle, G. Rooke.
Postoperative Myoclonus and Rigidity After Anesthesia with Opioids.
Anesth Analg, 78 (1994), pp. 783-786
[46.]
S. Roy, L. Fortier.
[Fentanyl-induced rigidity during emergence from general anesthesia potentiated by venlafexine] La rigidité induite par le fentanyl, pendant le retour á la conscience qui suit l'anesthésie générale, est potentialisée par la venlafexine.
Can J Anesth, 50 (2003), pp. 32-35
[47.]
N.T. Smith, J.L. Benthuysen, R.G. Bickford, T.J. Sanford, T. Blasco, P.C. Duke.
Seizures during opioid anesthetic induction-are they opioid-induced rigidity?.
Anesthesiology, 71 (1989), pp. 85242
[48.]
H. Fahnenstich, J. Steffan, N. Kau, P. Bartmann.
Fentanyl-induced chest wall rigidity and laryngospasm in preterm and term infants.
Crit Care Med., 28 (2000), pp. 836-839
[49.]
P. Bailey, J. Wilbrink, P. Zwanikken, N. Pace, T. Stanley.
Anesthetic Induction with Fentanyl.
Anesth Analg., 64 (1985), pp. 48-53
[50.]
P.W. Lui.
Involvement of spinal adenosine A1 and A2 receptors in fentanyl-induced muscular rigidity in the rat.
Neurosci Lett., 224 (1997), pp. 189-192
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