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Chemical Compound Review

Samorin     3-[2-(3-amino-5-ethyl-6- phenyl...

Synonyms: ISMM, Isometamidium, SureCN913500, AG-K-45657, SureCN7550257, ...
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Disease relevance of Isometamidium chloride


High impact information on Isometamidium chloride


Chemical compound and disease context of Isometamidium chloride


Biological context of Isometamidium chloride

  • A mathematical model has been developed which was able to predict theoretical lines representing the uptake kinetics in trypanosomes which were sensitive to isometamidium, as well as for resistant trypanosomes in which reduced accumulation was a result of either reduced uptake or enhanced efflux of the drug [14].
  • The overall absolute bioavailability of intramuscular-administered isometamidium was 65.7% [15].
  • Pharmacokinetics of the chemoprophylactic and chemotherapeutic trypanocidal drug isometamidium chloride (Samorin) in cattle [15].
  • The presence of the insertion, specifying an extra codon was found to always be present in the genomes of T. congolense clones that were resistant to isometamidium chloride [16].
  • Only 6 (2.8%) of 212 serum samples from trypanosome-infected cattle had serum levels of the drug above 0.4 ng isometamidium per ml serum which is indicative for drug resistance in the infecting parasite population [17].

Anatomical context of Isometamidium chloride


Associations of Isometamidium chloride with other chemical compounds


Gene context of Isometamidium chloride


Analytical, diagnostic and therapeutic context of Isometamidium chloride

  • Evaluation and improvement of an enzyme-linked immunosorbent assay for the detection of isometamidium in bovine serum [4].
  • These findings were consistent with extensive tissue binding at the intramuscular injection site to form a primary depot responsible for most of the prolonged chemoprophylactic effect of isometamidium, and an additional role for significant secondary drug depots formed by tissue binding elsewhere, particularly after intravenous administration [15].
  • A simple competitive enzyme immunoassay for the detection of the trypanocidal drug isometamidium [30].
  • Although there was no clear indication of underestimation of the weight of the animals and although farmers had adequate knowledge of the correct usage of isometamidium, the results suggest frequent underdosing when considering isometamidium serum concentrations 1 week after treatment [31].
  • Solid-phase extraction and ion-pair reversed-phase HPLC of isometamidium in bovine serum and tissues [32].


  1. Effects of ethidium and isometamidium on adenosine triphosphate catabolism and purine nucleotide synthesis in Ehrlich ascites tumor cells in vitro. Henderson, J.F., Battell, M.L., Zombor, G., Khoo, M.K. Cancer Res. (1977) [Pubmed]
  2. Modulation of mitochondrial electrical potential: a candidate mechanism for drug resistance in African trypanosomes. Wilkes, J.M., Mulugeta, W., Wells, C., Peregrine, A.S. Biochem. J. (1997) [Pubmed]
  3. Field evaluation of the prophylactic effect of an isometamidium sustained-release device against trypanosomiasis in cattle. Diarra, B., Diall, O., Geerts, S., Kageruka, P., Lemmouchi, Y., Schacht, E., Eisler, M.C., Holmes, P. Antimicrob. Agents Chemother. (1998) [Pubmed]
  4. Evaluation and improvement of an enzyme-linked immunosorbent assay for the detection of isometamidium in bovine serum. Eisler, M.C., Gault, E.A., Smith, H.V., Peregrine, A.S., Holmes, P.H. Therapeutic drug monitoring. (1993) [Pubmed]
  5. Therapeutic and prophylactic effects of isometamidium chloride (Samorin) against the hemoflagellate Cryptobia salmositica in chinook salmon (Oncorhynchus tshawytscha) and the effects of the drug on uninfected rainbow trout (O. mykiss). Ardelli, B.F., Woo, P.T. Parasitol. Res. (2001) [Pubmed]
  6. Selective cleavage of kinetoplast DNA minicircles promoted by antitrypanosomal drugs. Shapiro, T.A., Englund, P.T. Proc. Natl. Acad. Sci. U.S.A. (1990) [Pubmed]
  7. The accumulation and compartmentalization of isometamidium chloride in Trypanosoma congolense, monitored by its intrinsic fluorescence. Wilkes, J.M., Peregrine, A.S., Zilberstein, D. Biochem. J. (1995) [Pubmed]
  8. Fluorescence analysis of the interaction of isometamidium with Trypanosoma congolense. Zilberstein, D., Wilkes, J., Hirumi, H., Peregrine, A.S. Biochem. J. (1993) [Pubmed]
  9. Inhibitors of histamine metabolism in vitro and in vivo. Correlations with antitrypanosomal activity. Duch, D.S., Bacchi, C.J., Edelstein, M.P., Nichol, C.A. Biochem. Pharmacol. (1984) [Pubmed]
  10. Point mutations in mitochondrial topoisomerase enzymes of Trypanosoma congolense are not involved in isometamidium resistance. Delespaux, V., Geysen, D., Geerts, A.S. Mol. Biochem. Parasitol. (2007) [Pubmed]
  11. Concentrations of isometamidium chloride (Samorin) in sera of Zebu cattle which showed evidence of hepatotoxicity following frequent trypanocidal treatments. Eisler, M.C., Stevenson, P., Munga, L., Smyth, J.B. J. Vet. Pharmacol. Ther. (1997) [Pubmed]
  12. Influence of atropine on the acute toxicity of isometamidium. Gimbi, A.A., Kinabo, L.D. Veterinary and human toxicology. (1992) [Pubmed]
  13. The protection of 80 Nigerian trade cattle from trypanosomiasis and liver flukes using Samorin 1 and Trodax 2. Na'isa, B.K., Nyinya, R. Bulletin of animal health and production in Africa. Bulletin des santé et production animales en Afrique. (1976) [Pubmed]
  14. Kinetic modelling of isometamidium chloride (Samorin) uptake by Trypanosoma congolense. Sutherland, I.A., Mounsey, A., Eisler, M., Holmes, P.H. Parasitology (1992) [Pubmed]
  15. Pharmacokinetics of the chemoprophylactic and chemotherapeutic trypanocidal drug isometamidium chloride (Samorin) in cattle. Eisler, M.C. Drug Metab. Dispos. (1996) [Pubmed]
  16. Identification of a genetic marker for isometamidium chloride resistance in Trypanosoma congolense. Delespaux, V., Geysen, D., Majiwa, P.A., Geerts, S. Int. J. Parasitol. (2005) [Pubmed]
  17. Trypanocidal drug resistance in eastern province of Zambia. Sinyangwe, L., Delespaux, V., Brandt, J., Geerts, S., Mubanga, J., Machila, N., Holmes, P.H., Eisler, M.C. Vet. Parasitol. (2004) [Pubmed]
  18. Some effects of the trypanocidal drug isometamidium on encapsulation in bovine carrier erythrocytes. DeLoach, J.R., Wagner, G.G. Biotechnol. Appl. Biochem. (1988) [Pubmed]
  19. The in vitro effects of isometamidium chloride (Samorin) on the piscine hemoflagellate Cryptobia salmositica (Kinetoplastida, Bodonina). Ardelli, B.F., Woo, P.T. J. Parasitol. (2001) [Pubmed]
  20. A preliminary study on the absorption of isometamidium chloride (Samorin) in the stomach and small intestine of rat. Ogun, C.O., Eghianruwa, K.I. Journal of chemotherapy (Florence, Italy) (1993) [Pubmed]
  21. Metabolism of isometamidium in hepatocytes isolated from control and inducer-treated rats. Boibessot, I., Tettey, J.N., Skellern, G.G., Watson, D.G., Grant, M.H. J. Vet. Pharmacol. Ther. (2006) [Pubmed]
  22. Binding of isometamidium to calf thymus DNA and lipids: pharmacological implications. Kinabo, L.D., Bogan, J.A. J. Vet. Pharmacol. Ther. (1987) [Pubmed]
  23. Susceptibility of a rodent-adapted strain of Trypanosoma vivax to Berenil, Samorin and Novidium. Arowolo, R.O., Ikede, B.O. Acta Trop. (1977) [Pubmed]
  24. Comparison of isometamidium chloride and homidium bromide as prophylactic drugs for trypanosomiasis in cattle at Nguruman, Kenya. Stevenson, P., Sones, K.R., Gicheru, M.M., Mwangi, E.K. Acta Trop. (1995) [Pubmed]
  25. Rapid identification of isometamidium-resistant stocks of Trypanosoma b. brucei by PCR-RFLP. Afework, Y., Mäser, P., Etschmann, B., von Samson-Himmelstjerna, G., Zessin, K.H., Clausen, P.H. Parasitol. Res. (2006) [Pubmed]
  26. In vivo and in vitro sensitivity of Trypanosoma evansi and T. equiperdum to diminazene, suramin, MelCy, quinapyramine and isometamidium. Zhang, Z.Q., Giroud, C., Baltz, T. Acta Trop. (1991) [Pubmed]
  27. Susceptibility of Ugandan Trypanosoma brucei rhodesiense isolated from man and animal reservoirs to diminazene, isometamidium and melarsoprol. Matovu, E., Iten, M., Enyaru, J.C., Schmid, C., Lubega, G.W., Brun, R., Kaminsky, R. Trop. Med. Int. Health (1997) [Pubmed]
  28. Trypanosoma congolense: drug resistance during cyclical transmissions in tsetse flies and syringe passages in mice. Nyeko, J.H., Golder, T.K., Otieno, L.H., Ssenyonga, G.S. Exp. Parasitol. (1989) [Pubmed]
  29. Drug sensitivity of Trypanosoma evansi and the use of immunoassays in diagnosing infections with T. evansi in buffaloes in Vietnam. Le, N.M., Wuyts, N., Luckins, A.G., Nguyen, A.D., Nguyen, T.G. Ann. N. Y. Acad. Sci. (1998) [Pubmed]
  30. A simple competitive enzyme immunoassay for the detection of the trypanocidal drug isometamidium. Eisler, M.C., Elliott, C.T., Holmes, P.H. Therapeutic drug monitoring. (1996) [Pubmed]
  31. Monitoring the correct use of isometamidium by farmers and veterinary assistants in Eastern Province of Zambia using the isometamidium-ELISA. Delespaux, V., Geerts, S., Brandt, J., Elyn, R., Eisler, M.C. Vet. Parasitol. (2002) [Pubmed]
  32. Solid-phase extraction and ion-pair reversed-phase HPLC of isometamidium in bovine serum and tissues. Kinabo, L.D., Bogan, J.A. Acta Trop. (1988) [Pubmed]
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