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. 1993 May;37(5):970–974. doi: 10.1128/aac.37.5.970

Efficacy of intramuscular amopyroquin for treatment of Plasmodium falciparum malaria in the Gabon Republic.

C Gaudebout 1, E Pussard 1, F Clavier 1, D Gueret 1, J Le Bras 1, O Brandicourt 1, F Verdier 1
PMCID: PMC187865  PMID: 8517723

Abstract

The efficacy of a 12-mg/kg (of body weight) intramuscular amopyroquin (ApQ) regimen (two successive 6-mg/kg injections at a 24-h interval), previously established from kinetic studies on healthy volunteers and multicenter studies on patients with malaria, was investigated in 152 patients (children and adults) in Gabon with Plasmodium falciparum malaria. All children in the present study (ages, 1 to 14 years) showed higher degrees of parasitemia and temperatures and lower hematocrit values than did adults at the time of admission. No major side effects in the patients were observed. On day 7, all patients were apyretic; clearance of parasites was obtained in 143 of 152 patients (94%); a low level of parasitemia was observed in nine patients, all of whom were children (6%). In vitro chemosusceptibility tests carried out on P. falciparum isolates from patients demonstrated 51% of resistance to chloroquine (Cq). A correlation was found between the in vitro chemosusceptibilities to Cq and ApQ, but no relationship between the in vitro activity and the in vivo efficacy of ApQ could be found. Concentrations of ApQ in blood assayed by high-performance liquid chromatography on day 2 did not differ significantly between the groups in whom therapy was a success or a failure, although the mean ApQ concentration in blood for the group that failed therapy was 31% lower. Concentrations greater than 100 nmol of self-prescribed Cq and amodiaquine per liter, which were assayed simultaneously with ApQ, were observed in 78 patients (51%). They did not correlate with degrees of parasitemia compared with ApQ alone, which did. Successful treatment by day 7 was obtained in 69 of 74 patients (93%) who had no other 4-aminoquinolines in their blood. The results of the present study show that an ApQ regimen of 12 mg/kg over 2 days may be an alternative for the treatment of Cq-resistant malaria, at least in adult patients, in the field.

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Selected References

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  1. Bergqvist Y., Hed C., Funding L., Suther A. Determination of chloroquine and its metabolites in urine: a field method based on ion-pair extraction. Bull World Health Organ. 1985;63(5):893–898. [PMC free article] [PubMed] [Google Scholar]
  2. Bernuau J., Larrey D., Campillo B., Degott C., Verdier F., Rueff B., Pessayre D., Benhamou J. P. Amodiaquine-induced fulminant hepatitis. J Hepatol. 1988 Feb;6(1):109–112. doi: 10.1016/s0168-8278(88)80469-0. [DOI] [PubMed] [Google Scholar]
  3. Godfrey K. Statistics in practice. Comparing the means of several groups. N Engl J Med. 1985 Dec 5;313(23):1450–1456. doi: 10.1056/NEJM198512053132305. [DOI] [PubMed] [Google Scholar]
  4. Guéret D., Migot F., Ringwald P., Thibaut P., Le Bras J. Stabilité de la résistance de P. falciparum à la chloroquine entre 1987 et 1989 à Mounana, Gabon. Bull World Health Organ. 1992;70(5):621–624. [PMC free article] [PubMed] [Google Scholar]
  5. HOEKENGA M. T. Intramuscular amopyroquin for acute malaria. Am J Trop Med Hyg. 1962 Jan;11:1–5. doi: 10.4269/ajtmh.1962.11.1. [DOI] [PubMed] [Google Scholar]
  6. HOEKENGA M. T. Propoquin in treatment of malaria. Am J Trop Med Hyg. 1957 Nov;6(6):987–989. doi: 10.4269/ajtmh.1957.6.987. [DOI] [PubMed] [Google Scholar]
  7. Hatton C. S., Peto T. E., Bunch C., Pasvol G., Russell S. J., Singer C. R., Edwards G., Winstanley P. Frequency of severe neutropenia associated with amodiaquine prophylaxis against malaria. Lancet. 1986 Feb 22;1(8478):411–414. doi: 10.1016/s0140-6736(86)92371-8. [DOI] [PubMed] [Google Scholar]
  8. Landau I., Lepers J. P., Ringwald P., Rabarison P., Ginsburg H., Chabaud A. Chronotherapy of malaria: improved efficacy of timed chloroquine treatment of patients with Plasmodium falciparum infections. Trans R Soc Trop Med Hyg. 1992 Jul-Aug;86(4):374–375. doi: 10.1016/0035-9203(92)90224-z. [DOI] [PubMed] [Google Scholar]
  9. Le Bras J., Deloron P. In vitro study of drug sensitivity of Plasmodium falciparum: evaluation of a new semi-micro test. Am J Trop Med Hyg. 1983 May;32(3):447–451. doi: 10.4269/ajtmh.1983.32.447. [DOI] [PubMed] [Google Scholar]
  10. Pussard E., Clavier F., Verdier F. Liquid chromatographic determination of amopyroquine in rabbit plasma and red blood cells. J Chromatogr. 1987 Oct 9;421(1):192–197. doi: 10.1016/0378-4347(87)80397-3. [DOI] [PubMed] [Google Scholar]
  11. Pussard E., Verdier F., Faurisson F., Clavier F., Simon F., Gaudebout C. Disposition of amopyroquin in rats and rabbits and in vitro activity against Plasmodium falciparum. Antimicrob Agents Chemother. 1988 Apr;32(4):568–572. doi: 10.1128/aac.32.4.568. [DOI] [PMC free article] [PubMed] [Google Scholar]
  12. Verdier F., Pussard E., Clavier F., Le Bras J., Gaudebout C. Pharmacokinetics of intramuscular amopyroquin in healthy subjects and determination of a therapeutic regimen for Plasmodium falciparum malaria. Antimicrob Agents Chemother. 1989 Mar;33(3):316–321. doi: 10.1128/aac.33.3.316. [DOI] [PMC free article] [PubMed] [Google Scholar]
  13. White N. J. Antimalarial pharmacokinetics and treatment regimens. Br J Clin Pharmacol. 1992 Jul;34(1):1–10. doi: 10.1111/j.1365-2125.1992.tb04100.x. [DOI] [PMC free article] [PubMed] [Google Scholar]

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