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The pharmacokinetics of primaquine in calves after subcutaneous and intravenous administration

  • Pharmacology
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Abstract

The pharmacokinetics of primaquine was studied in calves of 180–300 kg live weight. Primaquine was injected at 0.29 mg/kg (0.51 mg/kg as primaquine diphosphate) intravenously (IV) or subcutaneously (SC) and the plasma concentrations of primaquine and its metabolite carboxyprimaquine were determined by high-performance liquid chromatography. The extrapolated concentration of primaquine at zero time after IV administration was 0.50±0.48 µg/ml (mean ±SD) which decreased with an elimination half-life of 0.16±0.07 h. Primaquine was rapidly converted to carboxyprimaquine after either route of administration. The peak concentration of carboxyprimaquine was 0.50±0.08 µg/ml at 1.67±0.15 h after IV administration. The corresponding value was 0.47±0.07 µg/ml at 5.05±1.20 h after SC administration. The elimination half-lives of carboxyprimaquine after IV and SC administration were 15.06±0.99 and 12.26±3.06 h, respectively. The areas under the concentration-time curve for carboxyprimaquine were similar following either IV or SC administration of primaquine; the values were 11.85±2.62 µg.h/ml after the former and 10.95±2.65 µg.h/ml after the latter. The mean area under the concentration-time curve for primaquine was less than 0.1 µg.h/ml after either route of administration.

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Abbreviations

AUC:

area under the concentration-time curve

CPRQ:

carboxyprimaquine

IV:

intravenous

6M8AQ:

6-methoxy-8-aminoquinoline

PRQ:

primaquine

SC:

subcutaneous

References

  • Baker, J.K., McChesney, J.D., Hufford, C.D. and Clark, A.M., 1982. High-performance liquid chromatographic analysis of the metabolism of primaquine and the identification of a new mammalian metabolite.Journal of Chromatography,230, 69–77

    PubMed  Google Scholar 

  • Baker, J.K., Bedford, J.A., Clark, A.M. and McChesney, J.D., 1984. Metabolism and distribution of primaquine in monkeys.Pharmaceutical Research,1, 98–100

    Google Scholar 

  • Bates, M.D., Meshnick, S.R., Sigler, C.I., Leland, P. and Hollingdale, M.R., 1990. In vitro effects of primaquine and primaquine metabolites on exoerythrocytic stages ofPlasmodium berghei.American Journal of Tropical Medicine and Hygiene,42, 532–537

    Google Scholar 

  • Baty, J.D., Price-Evans, D.A. and Robinson, P.A., 1975. The identification of 6-methyoxy-8-aminoquinoline as a metabolite of primaquine in man.Mass Spectrometry,2, 304–306

    Google Scholar 

  • Brossi, A., Millet, P., Landau, I., Bembenek, M.E. and Abell, C.W., 1987. Antimalarial activity and inhibition of monoamine oxidases A and B by exoerythrocytic antimalarials.FEBS Letters,214, 291–294

    PubMed  Google Scholar 

  • Clark, A.M., Baker, J.K. and McChesney, J.D., 1984. Excretion, distribution and metabolism of primaquine in rats.Journal of Pharmaceutical Sciences,73, 502–506

    PubMed  Google Scholar 

  • Endoh, Y.S., Yoshimura, H., Sasaki, N., Ishihara, Y., Sasaki, H., Nakamura, S., Inoue, Y. and Nishikawa, M., 1992. High-performance liquid chromatographic determination of pamaquin, primaquine and carboxyprimaquine in calf plasma using electrochemical detection.Journal of Chromatography,579, 123–129

    PubMed  Google Scholar 

  • Lee, C.C., Kinter, L.D. and Heiffer, M.H., 1981. Subacute toxicity of primaquine in dogs, monkeys and rats.Bulletin of the World Health Organization,59, 439–448

    PubMed  Google Scholar 

  • Link, C.M., Theoharides, A.D., Anders, J.C., Chung, H. and Canfield, C.J., 1985. Structure-activity relationships of putative primaquine metabolites causing methemoglobin formation in canine hemolysates.Toxicology and Applied Pharmacology,81, 192–202

    PubMed  Google Scholar 

  • Mihaly, G.W., Ward, S.A., Edwards, G., Orme, M.L'E. and Breckenridge, A.M., 1984. Pharmacokinetics of primaquine in man: Identification of the carboxylic acid derivative as a major plasma metabolite.British Journal of Clinical Pharmacology,17, 441–446

    PubMed  Google Scholar 

  • Mihaly, G.W., Ward, S.A., Edwards, G., Nicholl, D.D., Orme, M. L'E. and Breckenridge, A.M., 1985. Pharmacokinetics of primaquine in man. I. Studies of the absolute bioavailability and effects of dose size.British Journal of Clinical Pharmacology,19, 745–750

    PubMed  Google Scholar 

  • Nova, M.V., Parkhurst, G.W., Thomas, R.W. and Carson, P.E., 1984. High-performance liquid chromatographic-electrochemical assay method for primaquine in plasma and urine.Journal of Chromatography,307, 451–456

    PubMed  Google Scholar 

  • Parkhurst, G.W., Nova, M.V., Thomas, R.W. and Carson, P.E., 1984. High-performance liquid chromatographic-ultraviolet determination of primaquine and its metabolites in human plasma and urine.Journal of Pharmaceutical Sciences,73, 1329–1331

    PubMed  Google Scholar 

  • Schmidt, I.G. and Schmidt, L.H., 1951. Neurotoxicity of the 8-aminoquinolines. III. The effect of pentaquine, isopentaquine, primaquine and pamaquine on the central nervous system of rhesus monkeys.Journal of Neuropathology and Experimental Neurology,10, 231–256

    PubMed  Google Scholar 

  • Ward, S.A., Mihaly, G.W., Edwards, G., Looareesuwan, S., Phillips, R.E., Chanthavanich, P., Warrell, D.A., Orme, M. L'E. and Breckenridge, A.M., 1985. Pharmacokinetics of primaquine in man. II. Comparison of acute vs chronic dosage in Thai subjects.British Journal of Clinical Pharmacology,19, 751–755

    PubMed  Google Scholar 

  • Yamaoka, K., 1986.Methods for Pharmacokinetic Analysis by Personal Computer, (Nanko-do, Tokyo)

    Google Scholar 

  • Zhang, Z.H., 1987. Elimination of the gametocytes ofTheileria annulata of cattle by primaquine phosphate.Veterinary Pharmacology,23, 11–21

    Google Scholar 

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Yoshimura, H., Endoh, Y.S., Ishihara, Y. et al. The pharmacokinetics of primaquine in calves after subcutaneous and intravenous administration. Vet Res Commun 17, 129–136 (1993). https://doi.org/10.1007/BF01839241

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