ACTUALIZACION EN FORMULACIONES DE PROPOFOL

(especial para SIIC © Derechos reservados)
Para evitar los efectos adversos asociados con la administración de propofol en su formulación original se han logrado grandes avances en su farmacología. No obstante, es preciso conocer las diferencias farmacológicas entre las distintas formulaciones antes de utilizarlas en la práctica clínica.
telletxea9.jpg Autor:
Sorkunde Telletxea
Columnista Experto de SIIC

Institución:
Hospital de Galdakao-Usansolo


Artículos publicados por Sorkunde Telletxea
Recepción del artículo
29 de Mayo, 2008
Aprobación
15 de Julio, 2008
Primera edición
9 de Abril, 2009
Segunda edición, ampliada y corregida
7 de Junio, 2021

Resumen
En los últimos años se han logrado grandes avances en la farmacología del propofol. Estos avances se han producido con el fin de evitar los efectos adversos colaterales asociados con la administración de propofol en su formulación original. Estos efectos no deseados son: el dolor a la inyección intravenosa, la hiperlipidemia y la contaminación bacteriana. La industria farmacéutica ha introducido formulaciones como el propofol con EDTA, metabisulfito o bencilalcohol para evitar la contaminación bacteriana. También se ha utilizado lipuro para evitar el aumento de los niveles de triglicéridos. Existen formulaciones más avanzadas de propofol en ciclodextrina o en nanopartículas (IDD-propofol). Por último, conoceremos los profármacos del propofol. Es preciso conocer las diferencias farmacológicas entre las distintas formulaciones antes de utilizarlas en la práctica clínica.

Palabras clave
propofol, formulaciones, farmacocinética, farmacodinamia


Artículo completo

(castellano)
Extensión:  +/-5.82 páginas impresas en papel A4
Exclusivo para suscriptores/assinantes

Abstract
Great progress has been made in the pharmacology of propofol in recent years. These progress have been developed to avoid adverse side effects associated with the original formulation. The unwanted effects are: pain upon intravenous injection of the drug, hyperlipidemia, and bacterial contamination. Pharmaceutical industries has developed new formulations like propofol-EDTA, metabisulfite or bencyl-alcohol to avoid bacterial contamination. Other formulations use Lipuro to avoid elevated concentrations of triglycerides. More advanced formulations are propofol in Ciclodextrine or in Nanoemulsions. Finally, we will know propofol prodrugs. It is necessary to know the pharmacological differences between formulations before use them in ordinary practice.

Key words
propofol, formulations, pharmacokinetics, pharmacodinamics


Clasificación en siicsalud
Artículos originales > Expertos de Iberoamérica >
página   www.siicsalud.com/des/expertocompleto.php/

Especialidades
Principal: Anestesiología
Relacionadas: Cirugía, Cuidados Intensivos, Educación Médica, Farmacología, Medicina Farmacéutica



Comprar este artículo
Extensión: 5.82 páginas impresas en papel A4

file05.gif (1491 bytes) Artículos seleccionados para su compra



Enviar correspondencia a:
Sorkunde Telletxea, Hospital de Galdakao-Usansolo, 48960, Barrio Labeaga s/n Usansolo, Usansolo, España
Bibliografía del artículo

1. Hurle M. Fármacos anestésicos generales en: Florez ed. Farmacología humana. 3ª ed. Barcelona, Masson, pp. 477-488, 1997.
2. Schnider T, Minto C, Shafer S, Gambus P, Andresen C, Goodale D et al. The influence of age on propofol pharmacodynamics. Anesthesiology 90:1502-1516, 1999.
3. Vuyk J, Oostwouder CJ, Vletter A, Burm AGL, Bovill JG. Gender differences in the pharmacokinetics of propofol in elderly patients during and after continous infusion. Br J Anaesth 86:183-188, 2001.
4. Stokes DN, Hutton P. Rate-dependent induction phenomena with propofol: implications for the relative potency of intravenous anesthetics. Anesth Analg 72:578-583, 1991.
5. Short TG, Chui PT. Propofol and midazolam act synergistically in combination. Br J Anaesth 67:539-545, 1991.
6. Lind L, Johansson S, Ekman K. The influence of obesity and fat distribution and maintenance doses of propofol. Ups J Med Sci 98:187-188, 1993.
7. Hirota K, Ebina T, Sato T, Ishihara H, Matsuki A. Is total body weight appropriate predictor for propofol maintenance dose? Acta Anaesthesiol Scand 43:842-844, 1999.
8. Schuttler J, Ihmsen H. Population pharmacokinetics of propofol. Anesthesiology 92:727-738, 2000.
9. Schnider T, Minto C, , Gambus P, Andresen C, Goodale D, Shafer S et al. The influence of method of administration and covariates on the pharmacokinetics of propofol in adult volunteers. Anesthesiology 88:1170-1182, 1998.
10. Gepts E, Camu F, Cockshott ID, Douglas EJ. Disposition of propofol administered as constant rate intravenous infusions in humans. Anesth Analg 66:1256-1263, 1987.
11. Kataria BK, Ved SA, Nicodemus HF, Hoy GR, Lea D, Dubois MY et al. The pharmacokinetics of propofol in children using three different data aproaches. Anesthesiology 80:104-122, 1994.
12. Kirkpatrick T, Cockshott ID, Douglas EJ, Nimmo WS. Pharmacokinetics of propofol in elderly patients. Br J Anaesth 60:146-150, 1988.
13. Jones RDM, Chan K, Andrew IJ. Pharmacokinetics of propofol in children. Br J Anaesth 65:661-667, 1990.
14. Smith I, White PF. Pharmacokinetics and pharmacodynamics of drugs used in total intravenous anaesthesia en: Smith and White ed. Total intravenous anaesthesia. 1st ed. London, Hahn and Adams, pp. 29-81, 1998.
15. Scheepstra GL, Booij LHDJ, Rutten CLG, Coenen LGJ. Propofol for induction and maintenance of anaesthesia: Comparison between younger and older patients. Br J Anaesth 62:54-60, 1989.
16. Andrade J, Sapsford DJ, Jeevaratnum D. The coherent frequency in the electroencephalogram as an objetive measure sedation function during propofol sedation. Anesth Analg 83:1279-1284, 1996.
17. Glass P, Bloom M, Kearse L, Rosow C, Sebel P, Manberg P. Bispectral analysis measures sedation and memory effects of propofol, midazolam, isoflurane, and alfentanil in healthy volunteers. Anesthesiology 86:836-847, 1997.
18. Martin G. Gender differences: Hype or fact? Semin Anesth 19:76-82, 2000.
19. Servin F, Farinotti R, Haberer JP, Desmonts JM. Propofol infusion for mantenance of anaesthesia in morbidly obese patients receiving nitrous oxide. A clinical and pharmacokinetic study. Anesthesiology 78:657-665, 1993.
20. Ayuso MA, Luis M, Sala X, Fernandez J, Gomar C. Estudio de la incidencia de dolor a la inyección de una nueva preparación de propofol en emulsión grasa conteniendo triglicéridos de cadena media y larga. Rev Esp Anestesiol Reanim 51:531-536, 2004.
21. Dutta S, Matsumoto Y, Ebling WF. Propofol pharmacokinetics and pharmacodynamics assessed a cremophor-EL formulation. J Pharm Sci 86:967-969, 1997.
22. Dutta S, Ebling WF. Formulation-dependent brain and lung distribution kinetics of propofol in rats. Anesthesiology 89:678-685, 1998.
23. Calvo R, Telletxea S, Leal N, Aguilera L, Suárez, De la Fuente L et al. Influence of formulation on propofol pharmacokinetics and pharmacodynamics in anesthetized patients. Act Anaesth Scand 48:1038-1048, 2004.
24. Diprivan. Wilmington, DF: Stuart Pharmaceuticals, 1993.
25. Baker MT, Naguib M. Propofol. The challenges of formulation. Anesthesiology 103:860-876, 2005.
26. Jansson JR, Fukada T, Ozaki M, Kimura S. Propofol EDTA and reduced incidente of infection. Anaesth Intensive Care 34:362-368, 2006.
27. Shafer SL. Propofol formulations. Seminars in Anesthesia 21:248-2257, 2002.
28. Beaumont A, Marmarou A, Dunbar J. EEG burst suppression in the rat: propofol with EDTA versus sulfite-containing propofol for induction. American J Anaesth 27:22-29, 2000.
29. Lewis T, Janicki P, Higgins M, Szmyd-Hogan K, Beattie C. Anesthetic potency of propofol with disodium edetate versus sulfite-containing propofol in patients undergoing magnetic resonance imaging: a retrospective analysis. American J Anaesth 27:30-32, 2000.
30. Rieschke P, Lafleur B, Janicki P. Effects of EDTA-and sulfite-containing formulations of propofol on repiratory system resistance after tracheal intubation in smokers. Anesthesiology 98:323-328, 2003.
31. Sneyd JR. Recent advances in intravenous anaesthesia Br J Anaesth 93(5):725-36, 2004.
32. Wang H, Cork R, Rao A. Development of a new generation of propofol. Curr Opinion in Anesth 20:311-315, 2007.
33. Rau J, Roizen MF, Doenicke AW, O'Connor MF, Strohschnider U. Propofol in an emulsion of long- and medium-chain triglycerides: the effect on pain. Anesth Analg 93(2):382-384, 2001.
34. Telletxea S, Pérez P, Gómez C, Makua P, Arizaga A. Propofol: nuevas formulaciones. Rev Esp Anestesiol Reanim 53:426-436, 2006.
35. Morey TE, Modell JH, Shekhamat D, Shah DO, Klatt B, Thomas GP. Preparation and anesthetic properties of propofol microemulsions in rats. Anesthesiology 104:1184.1190, 2006.
36. Morey TE, Modell JH, Shekhamat D, Shah DO, Klatt B, Thomas GP. Anesthetic properties of a propofol microemulsion in dogs. Anesth Analg 103:882-887, 2006.
37. Kim K, Choi B, Park S, Lee S, Christensen L, Zhou J. Pharmacokinetics and Pharmacidynamics of propofol microemulsion and lipid emulsion after en intravenous bolus and variable rate infusion. Anesthesiology 106:924-934, 2007.
38. Ward D, Norton R, Guivarch P, Litman R, Bailey P. Phamarcodynamics and pharmacokinetics of propofol a medium-chain triglyceride emulsion. Anesthesiology 97:1401-1408, 2002.
39. Sikharam S, Egan TD, Kern SE. Cyclodextrins as new formulation entities and therapeutic agents. Current Opinion in Anesthesiology 18:392-395, 2005.
40. Egan T, Kern S, Johnson K y Pace N. The pharmacokinetics and pharmacodynamics of propofol in a modified Ciclodextrin formulation (Captisol) versus propofol in a lipid formulation (Diprivan): an electroencephalographic and hemodynamic study in a porcine model. Anesth Analg 97:72-79, 2003.
41. Song D, Hamza M, White P, Byerly S, Jones S, Macaluso A. Comparison of a lower lipid propofol emulsion with the standard emulsion for sedation during monitored anesthesia care. Anesthesiology 100:1072-1075, 2004.
42. Song D, Hamza M, White P, Klein K, Recat A, Khodaparast O. The pharmacodynamic effects of a lower-lipid emulsion of propofol: A comparison with the standard propofol emulsion. Anesth Analg 98:687-691, 2004.
43. Paul M, Dueck M, Kampe S, Fruendt H, Kasper SM. Pharmacological characteristics and side effects of a new galenic formulation of propofol without soyabean oil. Anaesthesia 58:1056-1062, 2003.
44. Munjal M, Sood D, Gupta VK, Singh A, kaul TK. Use of vegetarian propofol in Jain community of India. Anaesthesia 58:1137, 2003.
45. Subramani K. Use of vegetarian propofol in Jain community of India. Anaesthesia 60:521, 2005.
46. Sood D, Tewari A, Katyal S, Narula N, Garg S, Kaul TK. Pain on inyection of cleofol. Anaesthesia 60:521-522, 2005.
47. Schywalsky M, Ihmsen H, Tzabaris A, Fechner J, Burak E, Vornov J et al. Phamacokinetics and pharmacodynamics of the new propofol prodrug GPI 15715 in rats. Eur J Anaesth 20:182-190, 2003.
48. Fechner J, Imhsen H, Hatterscheid D, Schiessl C, Vornov J, Burak E et al. Pharmacokinetic and clinical pharmacodynamics of the new propofol prodrug GPI 15715 in volunteers. Anesthesiology 99:303-313, 2003.
49. Gibiansky E, Struys M, Gibiansky L, Vanluchene A, Vornov J, Mortier E et al. Aquavan injection, a water-soluble prodrug of propofol, as a bolus injection: a phase I dose-escalation comparison with Diprivan (part 1). Pharmacokinetics. Anesthesiology 103:718-729, 2005.
50. Struys M, Vanluchene A, Gibiansky E, Gibiansky L, Vornov J, Mortier E et al. Aquavan injection, a water-soluble prodrug of propofol, as a bolus injection: a phase I dose-escalation comparison with Diprivan (part 2). Pharmacodynamics and safety. Anesthesiology 103:718-72, 2005.
51. Telletxea S. Importancia de los parámetros FC/FD en anestesia total intravenosa en: Luciano Aguilera ed. Anestesia total intravenosa: principios básicos. 1ª ed. Francia, Springer-Verlag, pp. 1-15, 2002.

 
 
 
 
 
 
 
 
 
 
 
 
Está expresamente prohibida la redistribución y la redifusión de todo o parte de los contenidos de la Sociedad Iberoamericana de Información Científica (SIIC) S.A. sin previo y expreso consentimiento de SIIC.
ua31618
Home

Copyright siicsalud © 1997-2024 ISSN siicsalud: 1667-9008