Volume 71, Issue 3
  • ISSN: 0002-9637
  • E-ISSN: 1476-1645


Amodiaquine (AQ) is currently a major candidate for new antimalarial combinations, although and tests have been rarely simultaneously investigated. The efficacy of AQ was assessed at the dose of 30 mg/kg in treating malaria attacks in 74 children from southeast Gabon, and the activity of monodesethylamodiaquine (MdAQ), the main metabolite of AQ, was measured against parasites isolated from these children. Treatment failures were observed in 40.5% of the children, while 5.4% of the isolates showed resistance to MdAQ. No relationship was observed between and susceptibility. The activities of MdAQ and chloroquine were correlated. The reasons for such disparities between and AQ activities are discussed and the issue of the validity of tests to measure AQ efficacy is raised.


Article metrics loading...

The graphs shown below represent data from March 2017
Loading full text...

Full text loading...



  1. World Health Organization, 1996. Assessment of Therapeutic Efficacy of Antimalarial Drugs for Uncomplicated falciparum Malaria in Areas with Intense Transmission. Geneva: World Health Organization. WHO/MAL/96.1077.
  2. Le Bras J, Ringwald P, 1990. Situation de la chimiorésistance de Plasmodium falciparum en Afrique en 1989. Med Trop (Mars) 50 : 11–16. [Google Scholar]
  3. Aubouy A, Bakary M, Mbomat B, Makita JR, Keundjian A, Migot-Nabias F, Le Bras J, Deloron P, 2003. Combination of drug dosage and parasite genotyping data for a better assessment of amodiaquine and sulfadoxine-pyrimethamine efficacy to treat Plasmodium falciparum malaria in Gabonese children. Antimicrob Agents Chemother 47 : 231–237. [Google Scholar]
  4. World Health Organization, 2002. Monitoring Antimalarial Drug Resistance. Geneva: World Health Organization. WHO/CDS/CSR/EPH/2002,17.
  5. Le Bras J, Deloron P, 1983. In vitro study of drug sensitivity of Plasmodium falciparum: evaluation of a new semi-micro test. Am J Trop Med Hyg 32 : 447–451. [Google Scholar]
  6. Le Bras J, Simon F, Ramanamirija JA, Calmel MB, Hatin I, Deloron P, Porte J, Marchais H, Clausse JL, Biaud JM, Sarrouy J, Guiguemde TR, Carme B, Charmot G, Coulaud JP, Coulanges P, 1987. Sensibilité de Plasmodium falciparum aux quinoléines et stratégies thérapeutiques: comparaison de la situation en Afrique et à Madagascar entre 1983 et 1986. Bull Soc Pathol Exot Filiales 80 : 477–489. [Google Scholar]
  7. Brasseur P, Agnamey P, Same Ekobo A, Samba G, Favennec L, Kouamouo J, 1995. Sensitivity of Plasmodium falciparum to amodiaquine and chloroquine in central Africa: a comparative study in vivo and in vitro. Trans R Soc Trop Med Hyg 89 : 528–530. [Google Scholar]
  8. Trenholme KR, Kum DE, Raiko AK, Gibson N, Narara A, Alpers MP, 1993. Resistance of Plasmodium falciparum to amodiaquine in Papua New Guinea. Trans R Soc Trop Med Hyg 87 : 464–466. [Google Scholar]
  9. Ringwald P, Keundjian A, Same Ekobo A, Basco LK, 2000. Chemoresistance of Plasmodium falciparum in the urban region of Yaounde, Cameroon. Part 2: Evaluation of the efficacy of amodiaquine and sulfadoxine-pyrimethamine combination in the treatment of uncomplicated Plasmodium falciparum malaria in Yaounde, Cameroon. Trop Med Int Health 5 : 620–627. [Google Scholar]
  10. Basco LK, Ndounga M, Keundjian A, Ringwald P, 2002. Molecular epidemiology of malaria in Cameroon. IX. Characteristics of recrudescent and persistent Plasmodium falciparum infections after chloroquine or amodiaquine treatment in children. Am J Trop Med Hyg 66 : 117–123. [Google Scholar]
  11. Hengy C, Garrigue G, Abissegue B, Ghogomu NA, Gazin P, Gelas H, Kouka-Bemba D, Le Bras J, Jambou R, 1989. Surveillance de la chimiosensibilité de Plasmodium falciparum à Yaoundé et ses environs (Cameroun). Etude in vivo et in vitro. Bull Soc Pathol Exot Filiales 82 : 217–223. [Google Scholar]
  12. Carme B, Moudzeo H, Mbitsi A, Ndounga M, Samba G, 1991. Stabilization of drug resistance (chloroquine and amodiaquine) of Plasmodium falciparum in semiimmune populations in the Congo. J Infect Dis 164 : 437–438. [Google Scholar]
  13. Sexton JD, Deloron P, Bugilimfura L, Ntilivamunda A, Neill M, 1988. Parasitologic and clinical efficacy of 25 and 50 mg/kg of chloroquine for treatment of Plasmodium falciparum malaria in Rwandan children. Am J Trop Med Hyg 38 : 237–243. [Google Scholar]
  14. Li XQ, Bjorkman A, Andersson TB, Ridderstrom M, Masimirembwa CM, 2002. Amodiaquine clearance and its metabolism to N-desethylamodiaquine is mediated by CYP2C8: a new high affinity and turnover enzyme-specific probe substrate. J Pharmacol Exp Ther 300 : 399–407. [Google Scholar]
  15. Ong CE, Coulter S, Birkett DJ, Bhasker B, Miners JO, 2000. The xenobiotic inhibitor profile of cytochrome P450 2C8. Br J Clin Pharmacol 50 : 573–580. [Google Scholar]
  16. Goldstein JA, 2001. Clinical relevance of genetic polymorphisms in the human CYP2C subfamily. Br J Clin Pharmacol 52 : 3 49–355. [Google Scholar]
  17. Dai D, 2001. Allelic frequencies of human CYP2C8 and genetic linkage among different ethnic populations. FASEB J 15 : A575. [Google Scholar]
  18. Churchill FC, Mount DL, Patchen LC, Bjorkman A, 1986. Isolation, characterization and standardization of a major metabolite of amodiaquine by chromatographic and spectroscopic methods. J Chromatogr 377 : 307–318. [Google Scholar]
  19. Mount DL, Patchen LC, Nguyen-Dinh P, Barber AM, Schwartz IK, Churchill FC, 1986. Sensitive analysis of blood for amodiaquine and three metabolites by high-performance liquid chromatography with electrochemical detection. J Chromatogr 383 : 375–386. [Google Scholar]
  20. Pussard E, Verdier F, Faurisson F, Scherrmann JM, Le Bras J, Blayo MC, 1987. Disposition of monodesethylamodiaquine after a single oral dose of amodiaquine and three regimens for prophylaxis against Plasmodium falciparum malaria. Eur J Clin Pharmacol 33 : 409–414. [Google Scholar]
  21. Daubersies P, Sallenave-Sales S, Magne S, Trape JF, Contamin H, Fandeur T, Rogier C, Mercereau-Puijalon O, Druilhe P, 1996. Rapid turnover of Plasmodium falciparum populations in asymptomatic individuals living in a high transmission area. Am J Trop Med Hyg 54 : 18–26. [Google Scholar]
  22. Farnert A, Snounou G, Rooth I, Bjorkman A, 1997. Daily dynamics of Plasmodium falciparum subpopulations in asymptomatic children in a holoendemic area. Am J Trop Med Hyg 56 : 538–547. [Google Scholar]

Data & Media loading...

  • Received : 23 Jan 2004
  • Accepted : 09 Apr 2004

Most Cited This Month

This is a required field
Please enter a valid email address
Approval was a Success
Invalid data
An Error Occurred
Approval was partially successful, following selected items could not be processed due to error