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Chemical Compound Review

Alfenta     N-[1-[2-(4-ethyl-5-oxo- tetrazol-1...

Synonyms: ALFENTANIL, Alfentanyl, Alfentanilum, CHEMBL634, Rapifen (TN), ...
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Disease relevance of ALFENTANIL

  • 58 temporal lobe epilepsy (TLE) patients were studied with alfentanil activation during electrocorticography, at the Epilepsy Surgery Unit (ING, Brazil) [1].
  • Dose-dependent alfentanil disposition was mirrored by commensurate changes in clinical effect, although miosis was variable and not detectable in all subjects at the lowest dose [2].
  • Significant and marked reductions of hyperalgesia to cold (visual analogue score at threshold value) were seen following both alfentanil (4.5 before, 1.4 after, median value) and ketamine (6.8 before, 0.4 after, median value) [3].
  • Of the newer analgesic agents, alfentanil is an ideal agent for infusion, and may be the agent of choice in renal failure [4].
  • The difficulties in accurately predicting the response of an individual critically ill patient necessitate careful and continuous dose titration of alfentanil according to the clinical response [5].

Psychiatry related information on ALFENTANIL


High impact information on ALFENTANIL


Chemical compound and disease context of ALFENTANIL


Biological context of ALFENTANIL


Anatomical context of ALFENTANIL


Associations of ALFENTANIL with other chemical compounds


Gene context of ALFENTANIL

  • Alfentanil undergoes extensive metabolism by cytochrome P4503A4 (CYP3A4) [24].
  • There was a poor correlation between alfentanil metabolism and CYP3A4 content but an excellent correlation when CYP3A5 (i.e., total CYP3A content) was considered (r = 0.81, P < 0.0001) [24].
  • Pharmacogenetic determinants of human liver microsomal alfentanil metabolism and the role of cytochrome P450 3A5 [24].
  • There was a significant correlation (r = 0.97, P < 0.001) between alfentanil systemic clearance and P450 3A4 activity [25].
  • Alfentanil is a selective CYP3A probe but not a P-gp substrate [26].

Analytical, diagnostic and therapeutic context of ALFENTANIL


  1. Alfentanil-induced activation: a promising tool in the presurgical evaluation of temporal lobe epilepsy patients. Ragazzo, P.C., Galanopoulou, A.S. Brain Res. Brain Res. Rev. (2000) [Pubmed]
  2. Disposition and miotic effects of oral alfentanil: a potential noninvasive probe for first-pass cytochrome P4503A activity. Kharasch, E.D., Hoffer, C., Walker, A., Sheffels, P. Clin. Pharmacol. Ther. (2003) [Pubmed]
  3. Cold allodynia and hyperalgesia in neuropathic pain: the effect of N-methyl-D-aspartate (NMDA) receptor antagonist ketamine--a double-blind, cross-over comparison with alfentanil and placebo. Jørum, E., Warncke, T., Stubhaug, A. Pain (2003) [Pubmed]
  4. The use of sedative agents in critically ill patients. Burns, A.M., Shelly, M.P., Park, G.R. Drugs (1992) [Pubmed]
  5. Alfentanil infusions in patients requiring intensive care. Bodenham, A., Park, G.R. Clinical pharmacokinetics. (1988) [Pubmed]
  6. Concentration-effect relationship of intravenous alfentanil and ketamine on peripheral neurosensory thresholds, allodynia and hyperalgesia of neuropathic pain. Leung, A., Wallace, M.S., Ridgeway, B., Yaksh, T. Pain (2001) [Pubmed]
  7. Profiles of opioid analgesia in humans after intravenous bolus administration: alfentanil, fentanyl and morphine compared on experimental pain. Chapman, C.R., Hill, H.F., Saeger, L., Gavrin, J. Pain (1990) [Pubmed]
  8. Alcohol consumption alters the pharmacodynamics of alfentanil. Lemmens, H.J., Bovill, J.G., Hennis, P.J., Gladines, M.P., Burm, A.G. Anesthesiology (1989) [Pubmed]
  9. Reinforcing effect of alfentanil is mediated by mu opioid receptors: apparent pA2 analysis. Bertalmio, A.J., Woods, J.H. J. Pharmacol. Exp. Ther. (1989) [Pubmed]
  10. Opioids, cocaine, and food change runtime distribution in a rat runway procedure. Wakonigg, G., Sturm, K., Saria, A., Zernig, G. Psychopharmacology (Berl.) (2003) [Pubmed]
  11. Voriconazole, but not terbinafine, markedly reduces alfentanil clearance and prolongs its half-life. Saari, T.I., Laine, K., Leino, K., Valtonen, M., Neuvonen, P.J., Olkkola, K.T. Clin. Pharmacol. Ther. (2006) [Pubmed]
  12. Single-point sampling for assessment of constitutive, induced, and inhibited cytochrome P450 3A activity with alfentanil or midazolam. Chaobal, H.N., Kharasch, E.D. Clin. Pharmacol. Ther. (2005) [Pubmed]
  13. Pharmacodynamic interaction between propofol and alfentanil when given for induction of anesthesia. Vuyk, J., Engbers, F.H., Burm, A.G., Vletter, A.A., Griever, G.E., Olofsen, E., Bovill, J.G. Anesthesiology (1996) [Pubmed]
  14. The influence of cryogenic brain injury on nociception in the rat. Archer, D.P., Samanani, N. Anesthesiology (1993) [Pubmed]
  15. Naloxone-induced and spontaneous reversal of depressed ventilatory responses to hypoxia during and after continuous infusion of remifentanil or alfentanil. Amin, H.M., Sopchak, A.M., Esposito, B.F., Henson, L.G., Batenhorst, R.L., Fox, A.W., Camporesi, E.M. J. Pharmacol. Exp. Ther. (1995) [Pubmed]
  16. The relationship between alfentanil distribution kinetics and cardiac output. Henthorn, T.K., Krejcie, T.C., Avram, M.J. Clin. Pharmacol. Ther. (1992) [Pubmed]
  17. Patient-controlled analgesic infusions: alfentanil versus morphine. Hill, H.F., Coda, B.A., Mackie, A.M., Iverson, K. Pain (1992) [Pubmed]
  18. Patient controlled analgesia for extracorporeal shock wave lithotripsy of gallstones. Schelling, G., Mendl, G., Weber, W., Pauletzki, J., Sackmann, M., Pöppel, E., Peter, K. Pain (1992) [Pubmed]
  19. Effect of diltiazem on midazolam and alfentanil disposition in patients undergoing coronary artery bypass grafting. Ahonen, J., Olkkola, K.T., Salmenperä, M., Hynynen, M., Neuvonen, P.J. Anesthesiology (1996) [Pubmed]
  20. Liposome encapsulation prolongs alfentanil spinal analgesia and alters systemic redistribution in the rat. Bernards, C.M., Luger, T.J., Malmberg, A.B., Hill, H.F., Yaksh, T.L. Anesthesiology (1992) [Pubmed]
  21. Metabolism of cytochrome P4503A substrates in vivo administered by the same route: lack of correlation between alfentanil clearance and erythromycin breath test. Krivoruk, Y., Kinirons, M.T., Wood, A.J., Wood, M. Clin. Pharmacol. Ther. (1994) [Pubmed]
  22. Cerebral blood flow response to increases in arterial CO2 tension during alfentanil anesthesia in the rabbit. Ludbrook, G.L., Helps, S.C., Gorman, D.F. J. Cereb. Blood Flow Metab. (1992) [Pubmed]
  23. Pharmacokinetic-pharmacodynamic modeling in drug development: application to the investigational opioid trefentanil. Lemmens, H.J., Dyck, J.B., Shafer, S.L., Stanski, D.R. Clin. Pharmacol. Ther. (1994) [Pubmed]
  24. Pharmacogenetic determinants of human liver microsomal alfentanil metabolism and the role of cytochrome P450 3A5. Klees, T.M., Sheffels, P., Thummel, K.E., Kharasch, E.D. Anesthesiology (2005) [Pubmed]
  25. The role of cytochrome P450 3A4 in alfentanil clearance. Implications for interindividual variability in disposition and perioperative drug interactions. Kharasch, E.D., Russell, M., Mautz, D., Thummel, K.E., Kunze, K.L., Bowdle, A., Cox, K. Anesthesiology (1997) [Pubmed]
  26. Evaluation of first-pass cytochrome P4503A (CYP3A) and P-glycoprotein activities using alfentanil and fexofenadine in combination. Kharasch, E.D., Walker, A., Hoffer, C., Sheffels, P. Journal of clinical pharmacology. (2005) [Pubmed]
  27. Postoperative analgesia with intravenous infusion of alfentanil. Andrews, C.J., Robertson, J.A., Chapman, J.M. Lancet (1985) [Pubmed]
  28. Alfentanil infusion for sedation and analgesia in intensive care. Yate, P.M., Thomas, D., Sebel, P.S. Lancet (1984) [Pubmed]
  29. Dose effects of alfentanil in human analgesia. Hill, H., Walter, M.H., Saeger, L., Sargur, M., Sizemore, W., Chapman, C.R. Clin. Pharmacol. Ther. (1986) [Pubmed]
  30. A comparison of spectral edge, delta power, and bispectral index as EEG measures of alfentanil, propofol, and midazolam drug effect. Billard, V., Gambus, P.L., Chamoun, N., Stanski, D.R., Shafer, S.L. Clin. Pharmacol. Ther. (1997) [Pubmed]
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