Zeitschrift für Parasitenkunde

, Volume 52, Issue 2, pp 129–150 | Cite as

Praziquantel, a new broad-spectrum antischistosomal agent

  • R. Gönnert
  • P. Andrews
Praziquantel-Data On The Efficacy Against Schistosoma Mansoni, S. Haematobium, And S. Japonicum In Experimentally Infected Animals


Praziquantel, (2-cyclohexylcarbonyl)-1,2,3,6,7,11b-hexa-hydro-2H pyrazino[2,1a]isoquinolin-4-one, belongs to a new series of antischistosomal compounds. The results of a detailed study of the efficacy of praziquantel on Schistosoma mansoni in mice, Mastomys and Syrian hamsters are described.

Praziquantel is effective after oral and all parenteral routes of administration tested. The amount of praziquantel required to achieve parasite reductions of at least 95% depends on the host species and on the routes and schedules of administration. Total doses range from 200–1,000 mg/kg in mice and from 100–500 mg/kg for Mastomys and hamsters.

In all three species, splitting of the total dose into 3 or more fractional doses given within 1 day approximately doubles the efficacy over that achieved after a single oral administration of the same total dose. A single subcutaneous dose is only slightly more effective, whilst a single intramuscular injection in olive oil is about twice as effective as a single oral administration.

Praziquantel is very effective against the invading stages and slightly less against schistosomules up to an age of 7 days. It is less effective against 2- to 4-week-old juveniles, but is effective again against 5-week-old and older schistosomes.

Praziquantel is equally effective against both sexes of S. mansoni. It is less effective against unpaired and therefore juvenile female worms, but fully effective against single male worms.

The efficacy of praziquantel on S. mansoni in mice is not influenced by the strain or the sex of the host, the worm burden or the age of the infection.

Considering all data available, praziquantel promises to be a very potent antischistosomal drug.


Praziquantel Syrian Hamster Worm Burden Schistosoma Mansoni Female Worm 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


Praziquantel, (2-Cyclohexylcarbonyl)-1,2,3,6,7,11b-hexa-hydro-2H-pyrazino[2,1a]isochinolin-4-on), gehört zu einer neuen Reihe von Schistosomenmitteln. Die Arbeit beschreibt eingehend Versuche zur Wirksamkeit von Praziquantel gegen Schistosoma mansoni in Maus, Mastomys und Goldhamster.

Praziquantel ist nach oraler und allen geprüften parenteralen Verabreichungsweisen wirksam. Die für eine 95%ige Parasitenreduktion benötigte Dosis hängt von der Art des Wirtes und der Applikationsweise ab. Sie beträgt 200–1,000 mg/kg bei der Maus und 100–500 mg/kg bei Mastomys und Goldhamstern.

Bei allen drei Wirten bewirkt die Aufteilung der Gesamtdosis auf mehrere im Laufe eines Tages gegebene Teildosen eine Verdoppelung der Wirksamkeit im Vergleich zur einmaligen oralen Gabe. Die einmalige subcutane Gabe ist nur geringfügig wirksamer als die einmalige orale Gabe, aber eine intramuskuläre Gabe in Olivenöl ist wiederum etwa doppelt so wirksam.

Praziquantel ist gegen die jüngsten Schistosomulae in der Haut hoch wirksam und etwas geringer wirksam gegen Schistosomulae bis zum Alter von 7 Tagen. Gegen 2–4 Wochen alte Jugendliche ist es weniger wirksam. Ab einem Alter von 5 Wochen werden S. mansoni wieder voll erfaßt.

Praziquantel ist gegen gepaarte S. mansoni beider Geschlechter und gegen ungepaarte Männchen gleich gut wirksam. Gegen ungepaarte und daher juvenile Weibchen ist es weniger wirksam.

Die Wirksamkeit von Praziquantel gegen S. mansoni wird nicht beeinflußt von Stamm oder Geschlecht des Wirtstieres und auch nicht von der Anzahl oder dem Alter der Parasiten.

Unter Berücksichtigung aller Ergebnisse verspricht Praziquantel ein hoch wirksames Schistosomenmittel zu sein.


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  1. Andrews, P.: Pharmacokinetic studies with Droncit® in animals using a biological assay. Vet.-med. Nachr. 154–165 (1976)Google Scholar
  2. Andrews, P.: Untersuchungen zur Wirkungsweise von Praziquantel. (in preparation, 1977a)Google Scholar
  3. Andrews, P.: In vitro-Wirkung von Praziquantel auf adulte Schistosoma mansoni und Schistosomulae. (In preparation, 1977b)Google Scholar
  4. Andrews, P.: Wirkung von Praziquantel auf die freilebenden Entwicklungsstadien von Schistosoma mansoni. (In preparation, 1977c)Google Scholar
  5. Andrews, P.: Wirkung von Praziquantel auf Biomphalaria glabrata und die Entwickungsstadien von Schistosoma mansoni in der Schnecke. (In preparation, 1977d)Google Scholar
  6. Andrews, P., and Frank, G.: Tests for liver damage and haematologic changes in healthy and schistosome-infected mice after treatment with praziquantel. (In preparation, 1977)Google Scholar
  7. Bruckner, D.A.: Susceptibility of Schistosoma mansoni from Liberia and Puerto Rico to antischistosomal drugs. Amer. J. trop. Med. Hyg. 23, 634–638 (1974)Google Scholar
  8. Campbell, W., and Cuckler, A.C.: Efficacy of a 2-phenyl-quinoline against experimental Schistosoma mansoni infections in mice and monkeys. J. Parasit. 49, 528 (1963)PubMedGoogle Scholar
  9. Diekmann, H.W., and Bühring, K.U.: The fate of praziquantel in the organism. III. Metabolism in rat, beagle dog and rhesus monkey. Europ. J. Drug. Metab. Pharmacokinetics 1, 107–112 (1976)Google Scholar
  10. Duvall, R.H., and De Witt, W.B.: An improved perfusion technique for recovering adult schistosomes from laboratory animals. Amer. J. trop. Med. Hyg. 16, 483–486 (1967)Google Scholar
  11. Eckert, J., and Wolff, K.: The efficacy of Droncit against the lancet fluke Dicrocoelium dendriticum in sheep. Vet. Parasit. (in press 1977)Google Scholar
  12. Ercoli, N., and Payares, G.: Schistosoma mansoni: Early antimonial treatment of infected mice. Exp. Parasit. 35, 171–178 (1974)CrossRefPubMedGoogle Scholar
  13. Fink, H., Hund, G. and Meysing, D.: Vergleich biologischer Wirkungen mittels programmierter Probitanalyse. Meth. Inform. Med. 5, 19–25 (1966)PubMedGoogle Scholar
  14. Foster, R.: The preclinical development of oxaminquine. Rev. Inst. Med. trop. St Paulo 15 (Suppl. 1), 1–6 (1973)Google Scholar
  15. Foster, R., and Cheetham, B.L.: Studies with the schistosomicide oxamniquine (UK-4271). I. Activity in rodents and in vitro. Trans. roy. Soc. trop. Med. Hyg. 67, 674–684 (1973)CrossRefPubMedGoogle Scholar
  16. Foster, R., Cheetham, B.L., Messmer, E.T. and King, D.F.: Comparative studies of the action of mirasan, lucanthone, hycanthone and niridazole against Schistosoma mansoni in mice. Ann. trop. Med. Parasit. 65, 45–58 (1970)Google Scholar
  17. Foster, R., Messmer, E.T., Cheetham, B.L., and King, D.F.: The control of immature Schistosoma mansoni in mice by UK 3883. Ann. trop. Med. Parasit. 65, 221–232 (1971)PubMedGoogle Scholar
  18. Freireich, E.J., Gehan, E.A., Rall, D.P., Schmidt, L.H., and Skipper, H.E.: Quantitative comparison of toxicity of anticancer agents in mouse, rat, hamster, dog, monkey and man. Cancer Chemother. Rep. 50, 219–244 (1966)PubMedGoogle Scholar
  19. Goble, R.C., and Konopka, E.A.: Sex as a factor in infectious diseases. Trans. N.Y. Acad. Soc. 35, 325–346 (1973)Google Scholar
  20. Gönnert, R.: The structure activity relationship in several schistosomicidal compounds. Bull. Wld Hlth Org. 25, 702–706 (1961)Google Scholar
  21. Gönnert, R., and Vogel, H.: Über die Abhängigkeit des Therapieerfolges von Wirts- und Parasitenstamm bei der experimentellen Schistosomiasis. Z. Tropenmed. Parasit. 6, 193–198 (1955)Google Scholar
  22. Gönnert, R., and Wegner, D.: Clinical and experimental experiences with Bilarcil against Schistosoma haematobium. Meeting Port. Soc. trop. Med., Lisbon, 26.2.–1.3. 1973Google Scholar
  23. James, C., Webbe, G., and Nelson, G.S.: The susceptibility to praziquantel of Schistosoma haematobium in the baboon (Papio anubis) and of S. japonicum in the vervet monkey (Cercopithecus aethiops). Z. Parasitenk. 52, 179–195 (1977)PubMedGoogle Scholar
  24. Jewsbury, J.M.: Experimental chemoprophylaxis against schistosomiasis. I. Introduction and rationale. Ann. trop. Med. Parasit. 66, 409–419 (1972)PubMedGoogle Scholar
  25. Jewsbury, J.M.: Experimental chemoprophylaxis against schistosomiasis. II. Stage I comparison of lucanthone, hycanthone, niridazole and oxamniquine (UK 4271). Ann. trop. Med. Parasit. 67, 431–438 (1973)PubMedGoogle Scholar
  26. Kikuth, W., and Gönnert, R.: Experimentelle Untersuchungen und Erfahrungen mit dem neuen Schistosomenmittel Miracil. Z. Tropenmed. Parasit. 1, 234–258 (1949)Google Scholar
  27. Kikuth, W., Gönnert, R., and Mauss, H.: Miracil, ein neues Chemotherapeutikum gegen Darmbilharziose. Naturwissenschaften 33, 253 (1946)Google Scholar
  28. Lapierre, J., Holler, C., Lebas-Saisson, E., Le Prioux, B., and Roose, A.: Action de l'hycanthone aux divers stades évolutifs de l'infection expérimentale de la souris par Schistosoma mansoni. C.R. Soc. Biol. (Paris) 168, 452–454 (1974)Google Scholar
  29. Lee, H.G., Cheever, A.W., and Fairweather, W.R.: Influence of parasite strain on the chemotherapy of murine infections with Schistosoma mansoni. Bull. 45, 147–155 (1971)Google Scholar
  30. Lennox, R.W., and Bueding, E.: The relative chemotherapeutic efficacy of a nitrovinylfuran (SQ 18,506) against immature and mature stages of Schistosoma mansoni. Amer. J. trop. Med. Hyg. 21, 302–306 (1972)Google Scholar
  31. Mürmann, P., Eberstein, M.v., and Frohberg, H.: Zur Verträglichkeit von Droncit. Zusammenfassung der Versuchsergebnisse. Vet.-med. Nachr. 5, 142–153 (1976)Google Scholar
  32. Mauss, H., Kölling, H., and Gönnert, R.: Studien zur Chemotherapie der Schistosomiasis. Med. u. Chem. 5, 185–205 (1956)Google Scholar
  33. Pellegrino, J.: Protection against human schistosome cercariae. Exp. Parasit. 21, 112–131 (1967)CrossRefPubMedGoogle Scholar
  34. Pellegrino, H., Lima-Costa, F.F., Carlos, M.A., Mello, R.T.: Experimental chemotherapy of schistosomiasis mansoni. XIII. Activity of praziquantel, an isoquinoline-pyrazino derivative, on mice, hamsters and Cebus monkeys. Z. Parasitenk. 52, 151–168 (1977)PubMedGoogle Scholar
  35. Rosi, D., Peruzzoti, G., Dennis, E. W., Berberian, D. A., Freele, H. and Archer, S.: A new active metabolite of Miracil D. Nature 208, 1005–1006 (1965)Google Scholar
  36. Steiner, K., Garbe, A., Diekmann, H. W., Nowak, H.: The fate of praziquantel in the organism. I. Pharmacokinetics in animals. Europ. J. Drug. Metab. Pharmacokinetics 1, 85–96 (1976)Google Scholar
  37. Steiner, K., and Garbe, A.: The fate of praziquantel in the organism. II. Distribution in rats. Europ. J. Drug. Metab. Pharmacokinetics 1, 97–106 (1976)Google Scholar
  38. Stohler, H.R., and Frey, J.R. Chemotherapy of experimental schistosomiasis mansoni: Prophylactic and protective activity of clinically active compounds in mice and hamsters. Ann. trop. Med. Parasit. 57, 466–480 (1963)PubMedGoogle Scholar
  39. Stohler, H.R., and Frey, J.R.: Chemotherapy of experimental schistosomiasis mansoni: Prophylactic, protective and therapeutic activity of sodium antimony dimercaptosuccinate and antimony dimercaptosuccinic acid in mice and hamsters. Ann. trop. Med. Parasit. 58, 280–291 (1964)PubMedGoogle Scholar
  40. Thomas, H., Gönnert, R.: The efficacy of praziquantel against cestodes in animals. Z. Parasitenk. 52, 117–127 (1977a)PubMedGoogle Scholar
  41. Thomas, H., and Gönnert, R.: The efficacy of Droncit® against cestodes in cats, dogs and sheep. Res. Vet. Sci. (in press 1977b)Google Scholar
  42. Thomas, H., Gönnert, R., Pohlke, R. and Seubert, J.: Experience with a new compound against larval cestodes. 2nd Europ. Multicoll. Parasit. Trogir, September 1975Google Scholar
  43. Webbe, G., and James, C.: A comparison of the susceptibility to praziquantel of Schistosoma haematobium, S. japonicum, S. mansoni, S. intercalatum and S. mattheei in hamsters. Z. Parasitenk. 52, 169–177 (1977)PubMedGoogle Scholar
  44. Wegner, D.H.G.: Clinical and experimental experiences with Bilarcil® against Schistosoma haematobium. 9th Int. Congr. trop. Med. Malaria, Athens 2, 92 (1973)Google Scholar

Copyright information

© Springer-Verlag 1977

Authors and Affiliations

  • R. Gönnert
    • 1
  • P. Andrews
    • 1
  1. 1.Institute of ChemotherapyBayer AGWuppertalGermany

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