Pharmacology and toxicology of artelinic acid: Preclinical investigations on pharmacokinetics, metabolism, protein and red blood cell binding, and acute and anorectic toxicities

Transactions of the Royal Society of Tropical Medicine and Hygiene

Volumn 92, Issue 3, 1998, Pages 332-340

  Li, Q G ^a   Peggins, J O ^a   Lin, A J ^a   Masonic, K J ^a   Trotman, K M ^a   Brewer, T G ^b  

^a WALTER REED ARMY INSTITUTE OF RESEARCH   (United States)

^b ARMED FORCES RESEARCH INSTITUTE OF MEDICAL SCIENCES   (Thailand)

Author keywords

Anorectic toxicity; Artelinic acid; Chemotherapy; Erythrocyte binding; Malaria; Pharmacokinetics; Plasmodium falciparum; Protein binding

Indexed keywords

ANTIMALARIAL AGENT; ARTELINIC ACID; DIHYDROARTEMISININ;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANORECTAL DISEASE; ARTICLE; BINDING AFFINITY; DOG; DRUG ABSORPTION; DRUG BINDING; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG ELIMINATION; DRUG METABOLISM; DRUG STABILITY; DRUG TRANSFORMATION; ERYTHROCYTE; HUMAN; HUMAN CELL; INTRAMUSCULAR DRUG ADMINISTRATION; INTRAVENOUS DRUG ADMINISTRATION; ISOTOPE LABELING; MALARIA; MONKEY; NONHUMAN; ORAL DRUG ADMINISTRATION; RABBIT; RAT;

ANIMALIA; CANIS FAMILIARIS; ORYCTOLAGUS CUNICULUS; PLASMODIUM FALCIPARUM; PROTOZOA;

EID: 0031805447     PISSN: 00359203     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0035-9203(98)91033-1     Document Type: Article

References (46)

1. Basco, L. K. & Le Bras, J. (1993). In vitro activity of artemisinin derivatives against African isolates and clones of Plasmodium falciparum. American Journal of Tropical Medicine and Hygiene, 49, 301-307.
2. Brewer, T. G., Petras, J. M., Peggins, J. O., Li, W.-G., Lin, A. J., Sperry, M., Figueroa, L., Aguilar, A. & Schuster, B. G. (1993). Differential neurotoxicity of artemisinin analogs in an in vivo model. American Journal of Tropical Medicine and Hygiene, 49, supplement, 292.
3. Brewer, T. G., Peggins, J. O., Grate, S. J., Petras, J. M., Levine, B. S., Weina, P. J., Swearengen, J., Heiffer, M. H. & Schuster, B. G. (1994a). Neurotoxicity in animals due to arteether and artemether. Transactions of the Royal Society of Tropical Medicine and Hygiene, 88, supplement 1, S33-S36.
4. Brewer, T. G., Grate, S. J., Peggins, J. O., Weina, P. J., Petras, J. M., Levine, B. S., Heiffer, M. H. & Schuster, B. G. (1994b). Fatal neurotoxicity of arteether and artemether. American Journal of Tropical Medicine and Hygiene, 51, 251-259.
5. Brossi, A., Venugepalan, B., Gerpe, L. D., Yeh, H. J. C., Flippen-Anderson, J. L., Buchs, P., Luo, X. D., Milhous, W. & Peters, W. (1988). Arteether, a new antimalarial drug: synthesis and antimalarial properties. Journal of Medicinal Chemistry, 31, 645-651.
6. China Co-operative Research Group [on Qinghaosu and its Derivatives as Antimalarials] (1982a). Antimalarial efficacy and mode of action of qinghaosu and its derivatives in experimental models. Journal of Traditional Chinese Medicine, 2, 17-24.
7. China Co-operative Research Group [on Qinghaosu and its Derivatives as Antimalarials] (1982b). Studies on the toxicity of qinghaosu and its derivatives. Journal of Traditional Chinese Medicine, 2, 31-38.
8. China Co-operative Research Group [on Qinghaosu and its Derivatives as Antimalarials] (1982c). Clinical studies on the treatment of malaria with qinghaosu and its derivatives. Journal of Traditional Chinese Medicine, 2, 45-50.
9. Dutta, G. P., Bajpai, R. & Vishwakarma, R. A. (1989). Comparison of antimalarial efficacy of artemisinin (qinghaosu) and arteether against Plasmodium cynomolgi B infection in monkeys. Transactions of the Royal Society of Tropical Medicine and Hygiene, 83, 56-57.
10. Edlund, P. O., Westerlund, D., Carlqvist, J., Wu, B. L. & Jin, J. H. (1984). Determination of artesunate and dihydroartemisinin in plasma by liquid chromatography with post-column derivatization and UV detection. Acta Pharmaceutica Suecica, 21, 223-234.
11. Hien, T. T. (1994). An overview of the clinical use of artemisinin and its derivatives in the treatment of falciparum malaria in Viet Nam. Transactions of the Royal Society of Tropical Medicine and Hygiene, 88, supplement 1, S7-S8.
12. Hien, T. T., Arnold, K., Vinh, H., Cuong, B. M., Phu, N. H., Chau, T. T. H., Hoa, N. T. M., Chuong, L. V., Mai, N. T. H., Vinh, N. N. & Trang, T. T. M. (1992a). Comparison of artemesinin suppositories with intravenous artesunate and intravenous quinine in the treatment of cerebral malaria. Transactions of the Royal Society of Tropical Medicine and Hygiene, 86, 582-583.
13. Hien, T. T., Phu, N. H., Mai, N. T. H., Chau, T. T. H., Trang, T. T. M., Loc, P. P., Cuong, B. M., Dung, M. T., Vinh, H., Waller, D. J. & White, N. J. (1992b). An open randomized comparison of intravenous and intramuscular artesunate in severe falciparum malaria. Transactions of the Royal Society of Tropical Medicine and Hygiene, 86, 584-585.
14. Kager, P. A., Schultz, M. J., Zijlstra, E. E., van den Berg, B. & van Boxtel, Ch. J. (1994). Arteether administration in humans: preliminary studies of pharmacokinetics, safety and tolerance. Transactions of the Royal Society of Tropical Medicine and Hygiene, 88, supplement 1, S53-S54.
15. Kar, K., Nath, A., Bajpai, R., Dutta, G. P. & Vishwakarma, R. A. (1989). Pharmacology of α/β arteether - a potential antimalarial drug. Journal of Ethnopharmacology, 27, 297-305.
16. Klayman, D. L. (1985). An antimalarial drug from China. Science, 228, 1049-1055.
17. Klayman, D. L., Ager, A. K., jr, Fleckenstein, L. & Lin, A. J, (1991). Transdermal artelinic acid: an effective treatment for Plasmodium berghei infected mice. American Journal of Tropical Medicine and Hygiene, 45, 602-607.
18. Li, Q.-G. (editor) (1989). Investigations on the Metabolism of Five Progestogens of the 19-Nortestosterone Type in Various Laboratory Animal Species. Berlin: Papyrus-Druck.
19. Li, Q.-G., Guo, X.-B., Fu, L.-C., Jian, H.-X., & Wang, X.-H. (1994). Clinical trials of artemisinin and its derivatives in the treatment of malaria in China. Transactions of the Royal Society of Tropical Medicine and Hygiene, 88, supplement 1, S5-S6.
20. Li, Q.-G., Peggins, J. O., Fleckenstein, L. L., Masonic, K., Heiffer, M. H. & Brewer, T. G. (1998). Pharmacokinetics and bioavailability of dihydroartemisinin, arteether, artemether, artesunic acid and artelinic acid in rats. Journal of Pharmacy and Pharmacology, 50, 173-182.
21. Li, Q.-G., Brewer, T. G. & Peggins, J. O. (in press). Anorectic toxicity of dihydroartemisinin, artemether and arteether in rats following multiple intramuscular doses. International Journal of Toxicology, 17.
22. Lin, A. J., Klayman, D. L. & Milhous, W. K. (1987). Antimalarial activity of new water-soluble dihydroartemisinin derivatives. Journal of Medicinal Chemistry, 30, 2147-2150.
23. Lin, A. J., Klayman, D. L. & Milhous, W. K. (1988). Novel antimalarial dihydroartemisinin derivatives. US patent 4, 791, 135 (13 December 1988).
24. Looareesuwan, S. (1994). Overview of clinical studies on artemismin derivatives in Thailand. Transactions of the Royal Society of Tropical Medicine and Hygiene, 88, supplement 1, S9-S11.
25. Lowry, O. H., Rosebrough, N. J., Farr, A. L. & Randall, R. J. (1951). Protein measurement with the Folin phenol reagent. Journal of Biological Chemistry, 193, 265-275.
26. Melendez, V., Peggins, J. O., Brewer, T. G. & Theoharides, A. D. (1991). Determination of the antimalarial arteether and its deethylated metabolite dihydroartemisinin in plasma by high-performance liquid chromatography with reductive electrochemical detection. Journal of Pharmaceutical Sciences, 80, 132-138.
27. Milhous, W. K., Zalis, M. D., Gerena, L., Pang, L. W., Wirth, D. F. & Kyle, D. E. (1996). Differential in vitro drug susceptibility of Brazilian Plasmodium falciparum isolates to existing and developmental antimalarial drugs. American Journal of Tropical Medicine and Hygiene, 55, 180.
28. Nichols, M. B. & Maickel, R. P. (1989). Amphetamine enantiomers and rat consummatory behaviour: a new perspective. Pharmacology, Biochemistry and Behaviour, 33, 181-188.
29. Panisko, M. D. & Keystone, J. S. (1990). Treatment of malaria - 1990. Drugs, 39, 160-189.
30. Price, R. N., van Vugt, M., Nosten, F., Luxemburger, C. L. & White, N. J. (1997). Adverse effects of artemisinin derivatives studied in 3645 patients. American Journal of Tropical Medicine and Hygiene, 57, supplement, 102.
31. Sakata, T., Fukushima, K., Tsutsui, K., Arase, K. & Fujimoto, K. (1982). Theophylline disrupts diurnal rhythms of humoral factors with loss of meal cyclicity. Physiology and Behaviour, 28, 641-647.
32. Shmuklarsky, M. J., Klayman, D. L., Milhous, W. K., Rossan, R. N., Ager, A. L., Tang, D. B., jr., Heiffer, M. H., Canfield, C. J. & Schuster, B. G. (1993). Comparison of β-artemether and β-arteether against malaria parasites in vivo and in vitro. American Journal of Tropical Medicine and Hygiene, 48, 377-384.
33. Tallarida, R. J. & Murray, R. B. (1981). Manual of Pharmacologic Calculations with Computer Programs. New York: Springer-Verlag, pp. 21-49.
34. Taylor, P. & Insel, P. A. (1990). Molecular basis of pharmacologic selectivity. In: Principles of Drug Action, 3rd edition, Pratt, W. B. & Taylor, P. (editors). New York: Churchill Livingstone, pp. 1-102.
35. Theoharides, A. D., Peggins, J. O., Brewer, T. G., Melendez, V. & Boyd, J. M. (1989). Automated sample deoxygenation and injection in reductive LC-EC with a programmable auto injector and a novel switching apparatus. LG/GC, 7, 925-928.
36. Titulaer, H. A. & Vink-Blijleven, N. (1993). Assay of artelinic acid in serum by high-performance liquid chromatography. Journal of Chromatography, 612, 331-335.
37. Titulaer, H. A. C., Zuidema, J. & Lügt, C. B. (1991). Formulation and pharmacokinetics of artemisinin and its derivatives. International Journal of Pharmaceutics, 69, 83-92.
38. Titulaer, II. A., Eling, W. M. & Zuidema, J. (1993). Pharmacokinetic and pharmacodynamic aspects of artelinic acid in rodents. Journal of Pharmacy and Pharmacology, 45, 830-835.
39. Tripathi, R., Puri, S. K. & Dutta, G. P. (1996). Sodium betaartelinate - a new potential gametocycide. Experimental Parasitology, 82, 251-254.
40. Van Vianen, Ph. H., Klayman, D. L., Lin, A. J., Lugt, C. B., Van Engen, A. L., Van der Kaay, H. J. & Mons, B. (1990). Plasmodium berghei: the antimalarial action of artemisinin and sodium artelinate in vivo and in vitro, studied by flow cytometry. Experimental Parasitology, 70, 115-123.
41. Weder, H. G., Schildknecht, T., Luto, R. A. & Kesselring, P. (1974). Determination of binding parameters from Scatchard plots. European Journal of Biochemistry, 42, 475-481.
42. White, N. J. (1994). Artemisinin: current status. Transactions of the Royal Society of Tropical Medicine and Hygiene, 88, supplement 1, S3-S4.
43. WHO (1993). Arteether Injection. Geneva: World Health Organization, 1993 Investigator's Brochure, annex H, pp. 3-7.
44. Yang, Q., Shi, W., Li, R. & Gan, J. (1982). The antimalarial and toxic effect of artesunate on animal models. Journal of Traditional Chinese Medicine, 2, 99-103.
45. Yoa-Pu, Ha, O. & Carry, S. H. (1986). Calculation of fraction bound in equilibrium dialysis with special reference to drug losses by decomposition and adsorption. Biopharmaceutics and Drug Disposition, 7, 211-214.
46. Zhou, Z. M., Anders, J. C., Chung, H. & Theoharides, A. D. (1987). Analysis of artesunic acid and dihydroqinghaosu in blood by high-performance liquid chromatography with reductive electrochemical detection. Journal of Chromatography, 414, 77-90.