Skip to main content

Pharmakologie von Pentamidin

  • Conference paper
  • 18 Accesses

Zusammenfassung

Pentamidin ist eine aromatische Diamidinoverbindung, die in den 30er Jahren erstmalig innerhalb einer Reihe von Diamidinoverbindungen synthetisiert (Stilba-midin, Propamidin, Pentamidin) und in den 40er Jahren erfolgreich in der Behandlung der afrikanischen Schlafkrankheit (Trypanosoma rhodiense und gambiense) sowie der Leishmaniose eingesetzt wurde (Schoenbach u. Greenspan 1948). Das antiparasitäre pharmakologische Spektrum der Substanz wurde in den 60er Jahren um die nach neueren Untersuchungen möglicherweise zu den Pilzen zu zählende Pneumocystis carinii erweitert, die bei ätiologisch völlig unterschiedlich immunsupprimierten Patienten eine diffuse interstitielle Pneumonie hervorgerufen hatten (Ivady et al. 1963). Trotz bekannter klinischer Toxizität hat diese antiprotozoale Eigenschaft dem Pentamidin seit Bekanntwerden der Aids-Krank-heit einen bedeutenden Stellenwert in der Therapie der Pneumocystis carinii Pneumonie eingeräumt. Im folgenden soll daher versucht werden, die Pharmakologie dieser Substanz vor dem Hintergrund der neueren Erkenntnisse über eine Inhalationstherapie im Vergleich mit der i.v.-Applikation aufzuzeigen. Hierbei wird ausschließlich das Isethionatsalz von Pentamidin Berücksichtigung finden — eine zweite pharmazeutische Zubereitung, das Methansulfonat von Pentamidin (Lomidine) scheint toxischer zu sein und ist inzwischen aus dem Handel genommen worden.

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

Buying options

Chapter
USD   29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD   54.99
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD   69.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Learn about institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

reference

  • Belehu A, Naafs B (1982) Diabetes mellitus associated with pentamidine mesylate. Lancet 1: 1463–1464

    Article  PubMed  CAS  Google Scholar 

  • Bernard EM, Donnelly HJ, Maher MP, Armstrong D (1985) Use of a bioassay to study pentamidine pharmacokinetics. J Infect Dis 152: 750–754

    Article  PubMed  CAS  Google Scholar 

  • Bornstein RS, Yarbo JW (1970) An evaluation of the mechanism of action of pentamidine isethionate. J Surg Oncol 2: 393–398

    Article  PubMed  CAS  Google Scholar 

  • Bouchard P, Sai P, Reach G, Caubarrere I, Ganeval D, Assan R (1982) Diabetes mellitus following pentamidine-induced hypoglycemia in humans. Diabetes 31: 40–45

    Article  PubMed  CAS  Google Scholar 

  • Conte JE, Upton RA, Phelps RT, Wofsy CB, Zurlinden E, Lin ET (1986) Use of a specific and sensitive assay to determine pentamidine pharmacokinetics in patients with Aids. J Infect Dis 154: 923–929

    Article  PubMed  Google Scholar 

  • Conte JE, Upton RA, Lin ET (1987 a) Pentamidine pharmacokinetics in patients with Aids with impaired renal function. J Infect Dis 156: 885–890

    Article  PubMed  Google Scholar 

  • Conte JE, Hollander H, Golden JA (1987b) Inhaled or reduceddose intravenous pentamidine for Pneumocystis carinii pneumonia. Ann Intern Med 107: 495–498

    PubMed  Google Scholar 

  • Cushion MT, Stanforth D, Linke MJ, Walzer PD (1985) Methods of testing the susceptibility of Pneumocystis carinii to antimicrobial agents in vitro. Antimicrob Agents Chemother 28: 796–801

    PubMed  CAS  Google Scholar 

  • Debs RJ, Blumenfeld W, Brunette EN et al. (1987) Successful treatment with aerosolized pentamidine of Pneumocystis carinii pneumonia in rats. Antimicrob Agents Chemother 31: 37–41

    PubMed  CAS  Google Scholar 

  • Ivady G, Paldy L, Unger G (1963) Weitere Erfahrungen bei der Behandlung der interstitiellen plasmacellulären Pneumonie mit Pentamidin. Monatsschr Kinderheilkd 111: 279–299

    Google Scholar 

  • Jakob GM, Green GM (1973) Effects of pneumonia on intrapulmonary distribution of inhaled particles. Am Rev Respir Dis 107: 675–678

    Google Scholar 

  • Launoy L, Guillot M, Jonchere H (1960) Study on the storage and elimination of pentamidie in the mouse and white rat. Ann Pharm Fr 18: 424–439

    PubMed  CAS  Google Scholar 

  • Lin JM, Shi RJ, Lin ET (1986) High performance liquid chromatographic determination of pentamidine in plasma. J Liqu Chromatogr 9: 2035–2046

    Article  CAS  Google Scholar 

  • Makulu DR, Waalkes TP (1975) Interaction between aromatic diamidines and nucleic acids: Possible implications for chemotherapy. J Natl Cancer Inst 54: 305–309

    PubMed  CAS  Google Scholar 

  • Montgomery AB, Debs RJ, Luce JM et al. (1988) Selective delivery of pentamidine to the lung by aerosol. Am Rev Respir Dis 137: 477–478

    PubMed  CAS  Google Scholar 

  • Osei K, Falko JM, Nelson KP, Stephens R (1984) Diabetogenic effect of pentamidine. In vitro and in vivo studies in a patient with malignant insulinoma. Am J Med 77: 41–46

    Article  PubMed  CAS  Google Scholar 

  • Pearson RD, Hewlett EL (1985) Pentamidine for the treatment of Pneumocystis carinii pneumonia and other protozoal diseases. Ann Intern Med 103: 782–786

    PubMed  CAS  Google Scholar 

  • Pesanti EL, Cox C (1981) Metabolie and synthetic activities of pneumoncystis carinii in vitro,. Infect Immun 34: 908–914

    PubMed  CAS  Google Scholar 

  • Pifer LL, Pifer DD, Woods DR (1983) Biological profile and response to anti-pneumoeystis agents of Pneumocystis carinii in cell culture. Antimicrob Agents Chemother 24: 674–678

    CAS  Google Scholar 

  • Robbins JB (1967) Pneumocystis carinii pneumonitis - a review. Pediatr Res 1:131–138

    Article  PubMed  CAS  Google Scholar 

  • Salamone FR, Cunha BA (1988) Update of pentamidine for the treatment of Pneumocystis carinii pneumonia. Clin Pharm 7: 501–510

    PubMed  CAS  Google Scholar 

  • Sands M, Kron MA, Brown RB (1985) Pentamidine: a review. Rev Infect Dis 7: 625–634

    Article  PubMed  CAS  Google Scholar 

  • Sattler FR, Cowan R, Nielsen DM, Ruskin J (1988) Trimethoprim-sulfamethoxazole compared with pentamidine for treatment of Pneumocystis carinii pneumonia in the acquired immunodeficiency syndrome. Ann Intern Med 109: 280–287

    PubMed  CAS  Google Scholar 

  • Schoenbach EB, Greenspan EM (1984) The pharmacology, mode of action and therapeutic potentialities of stilbamidine, pentamidine, propamidine and other aromatic diamidines - a review. Medicine (Baltimore) 27: 327–377

    Google Scholar 

  • Waalkes TP, Denham C, De Vita VT (1970) Pentamidine: Clinical pharmacologic correlations in man and mice. Clin Pharmacol Ther 11: 505–512

    PubMed  CAS  Google Scholar 

  • Waalkes TP, Makulu DR (1976) Pharmacologic aspects of pentamidine. Natl Cancer Inst Monogr 43: 171–176

    PubMed  CAS  Google Scholar 

  • Wallace JM, Barbers RG, Oishi JS, Prince H (1984) Cellular and T-lymphocyte subpopulation profiles in bronchoalveolar lavage fluid from patients with acquired immunodeficiency syndrome and pneumonitis. Am Rev Respir Dis 130: 786–790

    PubMed  CAS  Google Scholar 

  • Wallis OC (1966) The effect of pentamidine on ribosomes of the parasitic flagellate crithidia (strigomonas) oncopelti. J Protozool 13: 234–239

    PubMed  CAS  Google Scholar 

  • Waring MJ (1965) The effects of antimicrobial agents on ribonucleic acid polymerase. Mol Pharmacol 1:1–13

    PubMed  CAS  Google Scholar 

  • Williamson J (1979) Effects of trypanocides on the fine structure of target organisms. Pharmacol Ther 7: 445–512

    Article  PubMed  CAS  Google Scholar 

Download references

Authors

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 2011 Springer Verlag

About this paper

Cite this paper

Vöhringer, HF., Arasteh, K., Hornscheidt, M., L’age, M. (2011). Pharmakologie von Pentamidin. In: Dietrich, M. (eds) Die Pneumocystis carinii Pneumonie. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-74771-7_8

Download citation

  • DOI: https://doi.org/10.1007/978-3-642-74771-7_8

  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-540-51177-9

  • Online ISBN: 978-3-642-74771-7

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics