Skip to main content
SpringerLink
Log in

Histamine-releasing properties of Polysorbate 80in vitro andin vivo: correlation with its hypotensive action in the dog

  • Histamine and Kinins
  • Published:
Agents and Actions Aims and scope Submit manuscript

Abstract

The solvent of commercial amiodarone (Polysorbate 80) has been reported to produce haemodynamic responses in humans and in dogs similar to those produced by histamine infusion. We therefore evaluated the correlation between hypotension induced by the solvent of amiodarone and its histamine-releasing properties in the awake dog.

The solvent of amiodarone administered to a dog, over 5 min in a dose of 10 mg/kg of Polysorbate 80, produced severe hypotension after the first administration; the second injection (24 h later) caused fewer hypotensive effects.

Histamine release in the peripheral tissues was demonstrated by a marked increase in plasma histamine concentrations, with the maximum value 10 min after the solvent administration. H1- and H2-receptor blockade with mepyramine (5 mg/kg) and cimetidine (10 mg/kg) significantly reduced the cardiovascular effects of the solvent.

Isolated peritoneal mast cells from rats also released histamine in response to Polysorbate 80. These studies show that Polysorbate 80 releases histamine bothin vitro and in isolated mast cells from rats andin vivo in the dog, and that the plasma concentrations are correlated with the haemodynamic responses.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Similar content being viewed by others

References

  1. M. Alam, G.V. Anrep, G.S. Barsoum, M. Talaat andE. Wieninger,Liberation of histamine from skeletal muscle by curare, J. Physiol., Lond.95, 148–158 (1939).

    Google Scholar 

  2. P.L. Smith, A. Kagey-Sobotka, E.R. Bleecker, R. Traystman, A.P. Kaplan, H. Gralnick, M.D. Valentine, S. Permutt andL.M. Lichtenstein,Physiological manifestations of human anaphylaxis, J. clin. Invest.66, 1072–1080 (1980).

    PubMed  Google Scholar 

  3. J. Moss, N. Fahmy, N. Sunder andM.A. Beaven,Hormonal and hemodynamic profile of anaphylactic reaction in man, Circulation63, 210–213 (1981).

    PubMed  Google Scholar 

  4. K. Pavek, A. Wegmann, L. Nordström andD. Schwander,Cardiovascular and respiratory mechanisms in anaphylactic and anaphylactoid shock reactions, Klin. Wschr.60, 941–947 (1982).

    Article  PubMed  Google Scholar 

  5. C. Meyer-Burgdorff, G. Seidel andF.J. Schlüter,Freisetzung von Histamin und Serotonin bei extrakorporaler Zirkulation, Anaesthesist22, 212–216 (1973).

    PubMed  Google Scholar 

  6. H.G. Beger andD. Stopix,Histamine release and hepatic elimination of histamine following abdominal surgery, Klin. Wschr.60, 935–938 (1982).

    Article  PubMed  Google Scholar 

  7. W. Lorenz, A. Doenicke, B. Schöning andE. Neugebauer, The role of histamine in adverse reactions to intravenous agents. InAdverse Reactions to Anaesthetic Drugs, pp. 169–238 (Ed.J.A. Thornton) Elsevier, North-Holland Biomedical Press, Amsterdam 1981.

    Google Scholar 

  8. C. Meyer-Burgdorff, G. Seidel andI. Wolf,Histaminfreistzung durch Narkosemittel, Anaesthesist25, 1–5 (1976).

    PubMed  Google Scholar 

  9. J. Moss, C.D. Rosow, J.J. Savarese, D.M. Philbin andK.F. Kniffen,Role of histamine in the hypotensive action of d-tubocuranine in humans, Anaesthesiology55, 19–25 (1981).

    Google Scholar 

  10. D.M. Philbin, J. Moss, C.W. Akins, C.E. Rosow, K.,R.C. Schneider, T.R. Verlee andJ.J. Savarese,The use of H 1-and H 2-histamine antagonists with morphine anaesthesia: a double blind study, Anaesthesiology55, 292–296 (1981).

    Google Scholar 

  11. C.E. Rosow, J. Moss, D.M. Philbin andJ.J. Savarese, Histamine release during morphine and fentanyl anesthesia. Anaesthesiology56, 93–96 (1982).

    Google Scholar 

  12. S.D., Rockoff andU.T. Aker,Contrast media as histamine liberators: VI. Arterial plasma histamine and hemodynamic responses following angiocardiography in man with 75% hypaque, Invest. Radiol.7, 403–406 (1972).

    PubMed  Google Scholar 

  13. W. Lorenz, A. Doenicke, B. Schöning, C.H. Ohmann, B. Grote andE. Neugebauer,Definition and classification of histamine-release response to drugs in anaesthesia and surgery: studies in the conscious human subject, Klin. Wschr.60, 896–913 (1982).

    Article  PubMed  Google Scholar 

  14. M.R. Bristow, W.S. Sageman, R.H. Scott, M.E. Billingham, R.E. Bowder, R.S. Kernoff, G.H. Snidow andJ.R. Daniels,Acute and chronic cardiovascular effects of Doxorubicin in dog: the cardiovascular pharmacology of drug-induced histamine release, J. Cardiovasc. Pharmac.2, 487–515 (1980).

    Google Scholar 

  15. A. Eschalier, M. Rodriguez, C. Burtin andJ. Lavarenne,Acute cardiovascular effects of several antitumor agents in the dog: involvement of histamine, Naunyn-Schmiedeberg's Arch. Pharmak. Supplement 324, Abs.256 (1983).

  16. W. Lorenz, A. Schmal, H. Schult, S. Lang, C.H. Ohmann, D. Weber, B. Kappa, L. Luben andA. Doenicke,Histamine release and hypotensive reactions in dogs by solubilizing agents and fatty acids: analysis of various components of Cremophor El ® and development of a component with reduced toxicity, Agents and Actions12, 64–81 (1982).

    Article  PubMed  Google Scholar 

  17. W. Lorenz, A. Doenicke, R. Meyer, H.J. Reimann, J. Kusche, H. Barth, H. Geesing, M. Hutzel andB. Weissenbacher,Histamine release in man by Propanidid and Thiopentone: pharmacological effects and clinical consequences, Br. J. Anaesth.44, 355–369 (1972).

    PubMed  Google Scholar 

  18. W. Lorenz, A. Doenicke, R. Meyer, H.J. Reimann, J. Kusche, H. Barth, H. Geesing, M. Hutzel andB. Weissenbacher,An improved method for the determination of histamine release in man: its application in studies with propanidid and thiopentone, Eur. J. Pharmac.19, 180–190 (1972).

    Article  Google Scholar 

  19. A. Doenicke, W. Lorenz, R. Beigl, H. Bezecny, G. Uhlig, L. Kalmar, B. Praetorius andG. Mann,Histamine release after intravenous application of short-acting hypnotics: a comparison of etomidate, althesin (CT 1314) and propanidid, Br. J. Anaesth.45, 1097–1104 (1973).

    PubMed  Google Scholar 

  20. P. Cote, M.G. Bourassa, J. Delaye, A. Janin, R. Froment andP. David,Effects of amiodarone on cardiac and coronary hemodynamic and on myocardial metabolism in patients with coronary artery disease, Circulation59, 1165–1172 (1979).

    PubMed  Google Scholar 

  21. R. Charlier, G. Deltour, A. Baudine andF. Chaillet,Pharmacology of Amiodarone, an antianginal drug with a new biological profile, Arzneimittel-Forsch.18, 1408–1417 (1968).

    Google Scholar 

  22. N. El-Sherif, R.R. Hope, B.J. Sherlag andR. Lazzara,Reentrant ventricular arrhythmias in the late myocardial infarction period. 1. Conduction characteristics in the infarction zone, Circulation55, 686–701 (1977).

    PubMed  Google Scholar 

  23. N. El-Sherif, R.R. Hope, B.J. Sherlag andR. Lazzara,Reetrant arrhythmias in the late myocardial infarction period. 2. Patterns of initiation and termination of reentry, Circulation55, 702–719 (1977b).

    PubMed  Google Scholar 

  24. J.T. Bigger, A.L. Basseit andB.F. Hoffman,Electrophysiological effects of diphenylhydantoin on canine Purkinje fibers, Circulation Res.22, 221–236 (1968).

    PubMed  Google Scholar 

  25. W.B. Gough, R.H. Zeiler, P. Barreca andN. El-Sherif,Hypotensive action of commercial intravenous amiodarone and polysorbate 80 in dogs, J. Cardiovasc. Pharmac.4, 375–380 (1982).

    Google Scholar 

  26. W. Lorenz, H.J. Reimann, A. Schmal, P. Dormann, B. Schwarz andE. Neugebauer,Histamine release in dogs by Cremophor El ® and its derivatives: oxethylated oleic acid is the most effective constituent, Agents and Actions7, 63–67 (1977).

    PubMed  Google Scholar 

  27. R.S.J. Clarke, J.W. Dundee, T. Garrett, G.K. McArdle andJ.S. Sutton,Adverse reactions to intravenous anaesthetics. Br. J. Anaesth.47, 575–585 (1975).

    PubMed  Google Scholar 

  28. B. Unväs andI.L. Thon,Evidence for enzymatic histamine release from isolated rat mast cells, Expl. Cell. Res.23, 45–57 (1961).

    Article  Google Scholar 

  29. P.A. Shore, A. Burkhalter andV.H. Cohn,A method for the fluorimetric assay of histamine in tissue, J. Pharmac. exp. Ther.127, 182–186 (1959).

    Google Scholar 

  30. L.T. Kremzner andI.R. Wilson,A procedure for the determination of histamine, Biochim. biophys. Acta50, 364–367 (1961).

    Article  Google Scholar 

  31. H.U. Bergmeyer andE. Bernt, Lactate dehydrogenase. UV-Assay with pyruvate and NADH. InMethods of Enzymatic Analysis, vol. 2, pp. 574–579 (Ed.H.U. Bergmeyer) Verlag Chemic Academic Press, New York, 1974.

    Google Scholar 

  32. W. Lorenz,Histamine release in man, Agents and Actions,5, 402–416 (1975).

    PubMed  Google Scholar 

  33. R.T. Garrett, The clinical manifestations of adverse reactions following althesin and thiopentane. InAdverse Response to Intravenous Drugs, pp. 34–40 (EdsJ. Watkins andA.M. Ward) Academic Press, London 1978.

    Google Scholar 

  34. A. Doenicke, Pseudoallergic reactions due to histamine release during intravenous anaesthesia. InPseudoallergic Reactions: Genetic Aspects and Anaphylactoid Reactions, pp. 224–250 (EdsP. Dukor, P. Kallos, H.D. Schlumberger andG.B. West) S. Karger, Basel 1980.

    Google Scholar 

  35. J. Watkins,Anaphylactoid reactions to i.v. substances, Br. J. Anaesth.51, 51–60 (1979).

    PubMed  Google Scholar 

  36. W. Lorenz andA. Doenicke, Anaphylactoid reactions and histamine release by intravenous drugs used in surgery and anaesthesia. InAdverse response to Intravenous Drugs, pp. 83–112 (Eds.J. Watkins andA.M. Ward) Academic Press, London 1978.

    Google Scholar 

  37. J.B. Glen, G.E. Davies, D.S. Thomson, S.C. Scarth andA.V. Thompson, Adverse reaction to intravenous anaesthetics in animals. InAdverse Response to Intravenous Drugs, pp. 129–135 (Eds.J. Watkin andA.M. Ward) Academic Press, London 1978.

    Google Scholar 

  38. J.B. Glen, G.E. Davies, D.S. Thomson, S.C. Scarth andA.V. Thompson,An animal model for the investigation of adverse response to i.v. anaesthetic agents and their solvents, Br. J. Anaesth.51, 819–827 (1978).

    Google Scholar 

  39. W. Schmutzler,Histamine release from human adenoidal mast cells induced by anti-human IgE, acetylcholine Epontol ®,Chremophor El ® and 12-hydroxystearic acid, Allergologie, in press.

  40. M. Werner andE. Wolff, Klinisch-experimentelle Untersuchungen zur Frage der Propanidid-Allergie. In (EdsM. Zindler, H. Yamamura, W. Wirth) Springer-Verlag, Heidelberg, New York 1973).

    Google Scholar 

  41. M. Thermann, W. Lorenz, A. Schmal, F. Schingale, P. Dormann andH. Hamelmann Alterations in the circulatory system of anaesthetized dogs following administration of histamine and histamine H 1-and H 2-receptor antagonists in relation to plasma histamine levels, Agents and Actions5, 450–455 (1975).

    PubMed  Google Scholar 

  42. S.C. Verma andJ.H. McNeill Cardiac histamine receptors: differences between right and left atria and right ventricle, J. Pharmac. exp. Ther.200, 352–362 (1977).

    Google Scholar 

  43. R. Ginsburg, M.R. Bristow andE.B. Stinson,Histamine receptors in the human heart, Life Sci.26, 2245–2249 (1980).

    Article  PubMed  Google Scholar 

  44. J. Moss, N.R. Fahmy, N. Sunder andM.A. Beaven,Hormonal and hemodynamic profile of an anaphylactic reaction in man, Circulation63, 210–213 (1981).

    PubMed  Google Scholar 

  45. W. Lorenz, R. Meyer, A. Doenicke, A. Schmal, H.J. Reimann, M. Hutzel andE. Werle,On the species specificity of the histamine release from mast cell stores by Cremophor El ®, Naunyn-Schmiedeberg's Arch. Pharmak.269, 417–421 (1971).

    Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Department of Preclinical and Clinical Pharmacology, University of Florence, Viale G.B. Morgagni 65, 50134, Firenze, Italy

    Emanuela Masini

  2. Sanofi-Centre de Recherches Clin-Midy, Rue de Prof. Blayac, 34082, Montpellier Cedex, France

    Jaques Planchenault, Francis Pezziardi, Patrick Gautier & Jean Pierre Gagnol

Authors
  1. Emanuela Masini
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Jaques Planchenault
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Francis Pezziardi
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. Patrick Gautier
    View author publications

    You can also search for this author in PubMed Google Scholar

  5. Jean Pierre Gagnol
    View author publications

    You can also search for this author in PubMed Google Scholar

Rights and permissions

Reprints and permissions

About this article

Cite this article

Masini, E., Planchenault, J., Pezziardi, F. et al. Histamine-releasing properties of Polysorbate 80in vitro andin vivo: correlation with its hypotensive action in the dog. Agents and Actions 16, 470–477 (1985). https://doi.org/10.1007/BF01983649

Download citation

  • Received:

  • Accepted:

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF01983649

Keywords

Search

Navigation