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Pharmacy World & Science

, Volume 29, Issue 3, pp 190–198 | Cite as

Effect of Fascioliasis on the pharmacokinetic parameters of triclabendazole in human subjects

  • Walid H. El-Tantawy
  • Heba F. Salem
  • Nirmeen A. S. Mohammed SafwatEmail author
Original Paper

Abstract

Objectives

To study the clinical efficacy of Triclabendazole (TCBZ) on Egyptian patients infected with Fasciola and understand the effect of Fascioliasis on the pharmacokinetics of TCBZ.

Methods

The pharmacokinetics of TCBZ administered as a single oral dose (10 mg/kg) was investigated in both infected and parasite––free Egyptian subjects. After oral administration, TCBZ is metabolized to a sulphone and sulfoxide derivatives. The latter is responsible for the fasciolicidal activity of TCBZ, and it could be used as a marker of drug bioavailability. Blood samples were collected following the oral administration, and TCBZ sulfoxide plasma concentrations were determined by a sensitive and specific HPLC method.

Results

Pharmacokinetic parameters (C max, AUC0–48, t 1/2 and t max) for TCBZ sulfoxide were calculated. In patients; the mean C max was 9.11 ± 1.3 μg/ml, the mean AUC (0–48) was 91 ± 10.5 μg h ml−1, the mean t 1/2 was 7.4 ± 0.6 h, and the t max was 3.0 ± 0.4 h. In normal subjects, the mean C max was 8.48 ± 0.92 μg/ml, the mean AUC(0–48) was 85 ± 6.55 μg h ml−1, the mean t 1/2 was 6.2 ± 0.357 h, and the t max was 3 ± 0.4 h. No significant difference could be detected in the patients as compared to normal subjects, which would suggest that Fascioliasis does not affect any of the studied parameters.

No eggs in faeces could be detected following TCBZ treatment. Also, most of the clinical investigations showed significant decline back to the normal ranges post-treatment which indicates complete curing and high TCBZ efficacy.

Conclusion

Fasioliasis as an infective condition widely spread in Egypt has no significant effect on the pharmacokinetic parameters of the orally administered TCBZ and at the same time it is very effective against the parasite which strongly and safely suggests the use of this medication for the treatment of this infection.

Keywords

Triclabendazole sulfoxide Clinical investigation Eggs Pharmacokinetics Fascioliasis 

Notes

Acknowledgments

The authors are thankful to Prof. Dr. Salah El-Banawy, Internal Medicine Department, Medical Research Institute, Alexandria for his medical supervision during the period of this self funded study.

References

  1. 1.
    Laburte C, Mott KE, Hull R, Severne Y. Triclabendazole for fascioliasis: efficacy and tolerability of a single treatment. Infectious diseases and public health. A research and clinical update. In: Angelico M, Rocchi G, editors. Italy: Balaban Publishers; p. 325–333.Google Scholar
  2. 2.
    Lecaillon JB, Godbillon J, Campestrini J, Naquira C, Miranda L, Pacheco R, Mull R Effect of food on the bioavailability of triclabendazole in patients with fascioliasis. Br J Clin Pharmacol 1998; 45:601–4.PubMedCrossRefGoogle Scholar
  3. 3.
    Keiser J, Engels D, Büscher G, Utzinger J Triclabendazole for the treatment of fascioliasis and paragonimiasis. Expert Opin Investig Drugs 2005; 14(12):1513–26.PubMedCrossRefGoogle Scholar
  4. 4.
    El-Shazly A, El-Desouky I, El-Feky A A case of ectopic fascioliasis in a farmer from Mansoura City. Dakahlia, Egypt. J Egypt Soc Parasitol 1991; 21:333–5.PubMedGoogle Scholar
  5. 5.
    Haseeb AN, El-Shazly AM, Arafa MA, Morsy AT A review on Fascioliasis in Egypt. J Egypt Soc Parasitol 2002; 32(1):317–54.PubMedGoogle Scholar
  6. 6.
    Robert W, Tolan RW Fascioliasis, http://www.emedicine.com/ped/topic760.htm. Cited 14-5-2006 Google Scholar
  7. 7.
    Fairweather I Triclabendazole: new skills to unravel an old(ish) enigma. J Helminthol 2005; 79(3):227–34.PubMedCrossRefGoogle Scholar
  8. 8.
    Sanyal PK, Gupta AC The efficacy and pharmacokinetics of long––term low––level intraruminal administration of triclabendazole in buffalo with induced fasciolosis. Vet Res Commun 1996; 20:461–8.PubMedCrossRefGoogle Scholar
  9. 9.
    Sanyal PK, Gupta AC The efficacy and pharmacokinetics of long-term low- level intraruminal administration of triclabendazole in urea molasses blocks against induced bovine and bubaline fascioliasis. Vet Parasitol 1998; 76(8):57–64.PubMedCrossRefGoogle Scholar
  10. 10.
    Sanyal PK, Gupta AC The efficacy and pharmacokinetics of triclabendazole in buffalo with induced fasciolosis. Vet Parasitol 1996; 63(1–2):75–82.PubMedCrossRefGoogle Scholar
  11. 11.
    Sanyal PK Pharmacokinetic behaviour of triclabendazole in domestic Ruminants follows single and divided dose administration. J Vet Parasitol 1998; 12(2):89–93.Google Scholar
  12. 12.
    Boray JC, Crowfoot PD, Strong MB, Allison JR, Schelenbaum M, Von Ornelli M, et al. Treatment of immature and mature Fasciola Hepatica infections in sheep and cattle. Vet Rec 1983; 113:315–7.PubMedGoogle Scholar
  13. 13.
    Negro A, Alvarez-Bujidos ML, Ortiz AI, Cubria JC, Menedez R, Ordonez D Reversed––phase ion––pair high performance liquid chromatographic determination of triclabendazole metabolites in serum and urine. J Chromatogr 1992; 576:135–141.PubMedCrossRefGoogle Scholar
  14. 14.
    Martin LK, Beaver PC Evaluation of Kato-Katz thick smear technique for quantitative diagnosis of helminthes infection. Am J Trop Med Hyg 1968; 17:382.PubMedGoogle Scholar
  15. 15.
    Hennessy DR, Lacey E, Steel JW, Prichard RK The kinetics of triclabendazole disposition in sheep. J Vet Pharmacol Ther 1987; 10(1):64–72.PubMedGoogle Scholar
  16. 16.
    Alvinerie M, Galter P Assay of triclabendazole and its main metabolites in plasma by high performance liquid chromatography. J Chromatogr 1986; 374:409–414.PubMedCrossRefGoogle Scholar
  17. 17.
    Abd Elbary A, Foda N, El-Gazayerly O, El Khatib M Reversed phase liquid chromatographic determination of vinpocetine in human plasma and its pharmacokinetic application. Anal Letters 2002; 35(6):1041–54.CrossRefGoogle Scholar
  18. 18.
    Lancaster R 1980 Pharmacology in clinical practice. Butterworth – Williams Heinenmann Medical books Ltd, London (UK), p. 44. ISBN 0433190523.Google Scholar
  19. 19.
    Chen MG, Mott KE Progress in assessment of morbidity due to Fasciola Hepatica infection: a review of recent literature. Trop Dis Bull 1990; 87:1–26.Google Scholar
  20. 20.
    Kinabo LDB, Bogan JA Pharmacokinetics and efficacy of triclabendazole in goats with induced fasciolosis. J Vet Pharmacol Ther 1988; 11:254–59.PubMedGoogle Scholar
  21. 21.
    Yadegari D, Talaie H, Massoud J Clinical trial of triclabendazole on human fascioliasis: long term follow-up. Med J Islam Rep Iran 1999; 13:89–91.Google Scholar
  22. 22.
    Farid Z, Trabbolsi B, Boctor F, Hafez A Unsuccessful use of praziquantel to treat fascioliasis in children. J Infect Dis 1986; 154:920–921.PubMedGoogle Scholar
  23. 23.
    Farid Z, Kamal M, Waodly J Treatment of acute toxaemic fascioliasis. Trans R Soc Trop Med Hyg 1988; 82:299.PubMedCrossRefGoogle Scholar
  24. 24.
    Farid Z, Kamal M, Mansour N Praziquantel and Fasciola Hepatica infection. Trans R Soc Trop Med Hyg 1989; 83:813.PubMedCrossRefGoogle Scholar
  25. 25.
    Apt W, Aguilera X, Vega F, Miranda C, Zulantay I, Perez C, Gabor M, Apt P Treatment of human chronic fasciolosis with triclabendazole: drug efficacy and serologic response. Am J Trop Med Hyg 1995; 52(6):532–5.PubMedGoogle Scholar

Copyright information

© Springer Science+Business Media, LLC 2007

Authors and Affiliations

  • Walid H. El-Tantawy
    • 1
  • Heba F. Salem
    • 2
  • Nirmeen A. S. Mohammed Safwat
    • 3
    Email author
  1. 1.Drug Bioavailability CentreNational Organization For Drug Control &Research, Ministry of HealthCairoEgypt
  2. 2.Department of Pharmaceutics, School of PharmacyBeni-sueif UniversityBeni SueifEgypt
  3. 3.Department of Pharmaceutics and Industrial Pharmacy, Faculty of PharmacyCairo UniversityAl-Orman 12612, CairoEgypt

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