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-
1
Li Q, Gerena L, Xie L, Zhang J, Kyle D, Milhous W, 2007. Development and validation of flow cytometric measurement for parasitemia in cultures of P. falciparum vitally stained with YOYO-1. Cytometry A 71A :297–307.
-
2
Li QG, Mog SR, Si YZ, Kyle DE, Gettayacamin M, Milhous WK, 2002. Neurotoxicity and efficacy of artemether related to its exposure times and exposure levels in rodents. Am J Trop Med Hyg 66 :516–525.
-
3
McLean WG, Ward SA, 1998. In vitro neurotoxicity of artemisinin derivatives. Med Trop 58 (3 Suppl):28–31.
-
4
Skinner TS, Manning LS, Johnston WA, Davis TM, 1996. In vitro stage-specific sensitivity of Plasmodium falciparum to quinine and artemisinin drugs. Int J Parasitol 26 :519–525.
-
5
Batty KT, Le AT, Ilett KF, Nguyen PT, Powell SM, Nguyen CH, Truong XM, Vuong VC, Huynh VT, Tran QB, Nguyen VM, Davis TM, 1998. A pharmacokinetic and pharmacodynamic study of artesunate for vivax malaria. Am J Trop Med Hyg 59 :823–827.
-
6
Davis TM, Phuong HL, Ilett KF, Hung NC, Batty KT, Phuong VD, Powell SM, Thien HV, Binh TQ, 2001. Pharmacokinetics and pharmacodynamics of intravenous artesunate in severe falciparum malaria. Antimicrob Agents Chemother 45 :181–186.
-
7
Li QG, Peggins JO, Fleckenstein LL, Masonic K, Heiffer MH, Brewer TG, 1998. The pharmacokinetics and bioavailability of dihydroartemisinin, artemether, artemether, artesunic acid and artelinic acid in rats. J Pharm Pharmacol 50 :173–182.
-
8
Navaratnam V, Mansor SM, Sit NW, Grace J, Li QG, Olliaro P, 2000. Pharmacokinetics of artemisinin-type compounds. Clin Pharmacokinet 39 :255–270.
-
9
Janssens B, van Herp M, Goubert L, Chan S, Uong S, Nong S, Socheat D, Brockman A, Ashley EA, Van Damme W, 2007. A randomized open study to assess the efficacy and tolerability of dihydroartemisinin-piperaquine for the treatment of uncomplicated falciparum malaria in Cambodia. Trop Med Int Health 12 :251–259.
-
10
Malik EM, Mohamed TA, Elmardi KA, Mowien RM, Elhassan AH, Elamin SB, Mannan AA, Ahmed ES, 2006. From chloroquine to artemisinin-based combination therapy: the Sudanese experience. Malar J 5 :65.
-
11
Rosenthal PJ, 2008. Artesunate for the treatment of severe falciparum malaria. N Engl J Med 358 :1829–1836.
-
12
Artemether-Quinine Meta-analysis Study Group, 2001. A meta-analysis using individual patient data of trials comparing artemether with quinine in the treatment of severe falciparum malaria. Trans R Soc Trop Med Hyg 95 :637–650.
-
13
Tran TH, Day NP, Nguyen HP, Nguyen TH, Tran TH, Pham PL, Dinh XS, Ly VC, Ha V, Waller D, Peto TE, White NJ, 1996. A controlled trial of artemether or quinine in Vietnamese adults with severe falciparum malaria. N Engl J Med 335 :76–83.
-
14
Whitty CJ, Ansah E, Reyburn H, 2005. Treating severe malaria. BMJ 330 :317–318.
-
15
Davis TM, Phuong HL, Ilett KF, Hung NC, Batty KT, Phuong VD, Powell SM, Thien HV, Binh TQ, 2001. Pharmacokinetics and pharmacodynamics of intravenous artesunate in severe falciparum malaria. Antimicrob Agents Chemother 45 :181–186.
-
16
Hien TT, Davis TM, Chuong LV, Ilett KF, Sinh DX, Phu NH, Agus C, Chiswell GM, White NJ, Farrar J, 2004. Comparative pharmacokinetics of intramuscular artesunate and artemether in patients with severe falciparum malaria. Antimicrob Agents Chemother 48 :4234–4239.
-
17
Ashley EA, White NJ, 2005. Artemisinin-based combinations. Curr Opin Infect Dis 18 :531–536.
-
18
Dondorp A, Nosten F, Stepniewska K, Day N, White N, 2005. South East Asian Quinine Artesunate Malaria Trial (SEAQUAMAT) group. Artesunate versus quinine for treatment of severe falciparum malaria: a randomised trial. Lancet 366 :717–725.
-
19
Jones KL, Donegan S, Lalloo DG, 2007. Artesunate versus quinine for treating severe malaria. Cochrane Database Syst Rev 17 :CD005967.
-
20
Jelinek T, 2005. Intravenous artesunate recommended for patients with severe malaria: position statement from TropNetEurop. Eurosurveillance 10 :ii-2841.
-
21
Pasvol G, 2006. The treatment of complicated and severe malaria. Br Med Bull 75–76 :29–47.
-
22
Nosten F, Ashley E, McGready R, Price R, 2006. We still need artesunate monotherapy. BMJ 333 :45.
-
23
Jones KL, Donegan S, Lalloo DG, 2008. Treating severe malaria: artesunate or Quinine? Indian Pediatr 45 :41–42.
-
24
Li Q, Weina P, Milhous WK, 2007. Pharmacokinetic and pharmacodynamic profiles of rapid-acting artemisinins in the antimalarial therapy. Curr Drug Ther 2 :210–223.
-
25
Li Q, Milhous WK, Weina PJ, 2007. Antimalarial in Malaria Therapy. New York: Nova Science Publishers.
-
26
Day N, Dondorp AM, 2007. The management of patients with severe malaria. Am J Trop Med Hyg 77 (Suppl):29–35.
-
27
Li Q, Xie LH, Haeberle A, Zhang J, Weina P, 2006. The evaluation of radiolabeled artesunate on tissue distribution in rats and protein binding in humans. Am J Trop Med Hyg 75 :817–826.
-
28
Li QG, Xie LH, Johnson TO, Si YZ, Haeberle AS, Weina PJ, 2007. Toxicity evaluation of artesunate and artelinate in Plasmodium berghei-infected and uninfected rats. Trans R Soc Trop Med Hyg 101 :104–112.
-
29
Gu Y, Li Q, Melendez V, Weina PJ, 2008. Comparison of HPLC with electrochemical detection and LC-MS/MS for the separation and validation of artesunate and dihydroartemisinin in animal and human plasma. J Chromatogr B Analyt Technol Biomed Life Sci 867 :213–218.
-
30
Bourne D, 1995. Mathematical Modeling of Pharmacokinetic Data, vol. 1. Lancaster, PA: Technomic Publishing.
-
31
Gabrielsson J, Weiner D, 2000. Pharmacokinetic and Pharmacodynamic Data Analysis: Concepts and Applications, vol. 3. Stockholm, Sweden: Apotekarsocieteten (Swedish Pharmaceutical Society).
-
32
Navaratnam V, Mansor SM, Sit NW, Grace J, Li QG, Olliaro P, 2000. Pharmacokinetics of artemisinin-type compounds. Clin Pharmacokinet 39 :255–270.
| Past two years | Past Year | Past 30 Days | |
|---|---|---|---|
| Abstract Views | 414 | 363 | 25 |
| Full Text Views | 515 | 7 | 0 |
| PDF Downloads | 151 | 7 | 0 |
Pharmacokinetic Profiles of Artesunate After Single Intravenous Doses at 0.5, 1, 2, 4, and 8 mg/kg in Healthy Volunteers: A Phase I Study
Qigui Li
Qigui Li
Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland; Division of Clinical Pharmacology and Medical Toxicology, Uniformed Services University of the Health Sciences, Bethesda, Maryland
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Louis R. Cantilena
Louis R. Cantilena
Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland; Division of Clinical Pharmacology and Medical Toxicology, Uniformed Services University of the Health Sciences, Bethesda, Maryland
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Kevin J. Leary
Kevin J. Leary
Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland; Division of Clinical Pharmacology and Medical Toxicology, Uniformed Services University of the Health Sciences, Bethesda, Maryland
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George A. Saviolakis
George A. Saviolakis
Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland; Division of Clinical Pharmacology and Medical Toxicology, Uniformed Services University of the Health Sciences, Bethesda, Maryland
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R. Scott Miller
R. Scott Miller
Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland; Division of Clinical Pharmacology and Medical Toxicology, Uniformed Services University of the Health Sciences, Bethesda, Maryland
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Victor Melendez
Victor Melendez
Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland; Division of Clinical Pharmacology and Medical Toxicology, Uniformed Services University of the Health Sciences, Bethesda, Maryland
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Peter J. Weina
Peter J. Weina
Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland; Division of Clinical Pharmacology and Medical Toxicology, Uniformed Services University of the Health Sciences, Bethesda, Maryland
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The pharmacokinetics of good manufacturing process injection of artesunate (AS) were evaluated after single doses at 0.5, 1, 2, 4, and 8 mg/kg with a 2-minute infusion in 40 healthy subjects. Drug concentrations were analyzed by validated liquid chromatography and mass spectrometry system (LC-MS/MS) procedures. The drug was immediately converted to dihydroartemisinin (DHA), with elimination half-lives ranging 0.12–0.24 and 1.15–2.37 hours for AS and DHA, respectively. Pharmacokinetic model-dependent analysis is suitable for AS, whereas DHA fits both model-dependent and -independent methods. Although DHA concentration was superior to that of AS with a 1.12–1.87 ratio of area under the curve (AUC)DHA/AS, peak concentration of AS was much higher than that of DHA, with a 2.80- to 4.51-fold ratio of peak concentration (Cmax AS/DHA). Therefore, AS effectiveness has been attributed not only to its rapid hydrolysis to DHA, but also to itself high initial Cmax.
Author Notes
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-
1
Li Q, Gerena L, Xie L, Zhang J, Kyle D, Milhous W, 2007. Development and validation of flow cytometric measurement for parasitemia in cultures of P. falciparum vitally stained with YOYO-1. Cytometry A 71A :297–307.
-
2
Li QG, Mog SR, Si YZ, Kyle DE, Gettayacamin M, Milhous WK, 2002. Neurotoxicity and efficacy of artemether related to its exposure times and exposure levels in rodents. Am J Trop Med Hyg 66 :516–525.
-
3
McLean WG, Ward SA, 1998. In vitro neurotoxicity of artemisinin derivatives. Med Trop 58 (3 Suppl):28–31.
-
4
Skinner TS, Manning LS, Johnston WA, Davis TM, 1996. In vitro stage-specific sensitivity of Plasmodium falciparum to quinine and artemisinin drugs. Int J Parasitol 26 :519–525.
-
5
Batty KT, Le AT, Ilett KF, Nguyen PT, Powell SM, Nguyen CH, Truong XM, Vuong VC, Huynh VT, Tran QB, Nguyen VM, Davis TM, 1998. A pharmacokinetic and pharmacodynamic study of artesunate for vivax malaria. Am J Trop Med Hyg 59 :823–827.
-
6
Davis TM, Phuong HL, Ilett KF, Hung NC, Batty KT, Phuong VD, Powell SM, Thien HV, Binh TQ, 2001. Pharmacokinetics and pharmacodynamics of intravenous artesunate in severe falciparum malaria. Antimicrob Agents Chemother 45 :181–186.
-
7
Li QG, Peggins JO, Fleckenstein LL, Masonic K, Heiffer MH, Brewer TG, 1998. The pharmacokinetics and bioavailability of dihydroartemisinin, artemether, artemether, artesunic acid and artelinic acid in rats. J Pharm Pharmacol 50 :173–182.
-
8
Navaratnam V, Mansor SM, Sit NW, Grace J, Li QG, Olliaro P, 2000. Pharmacokinetics of artemisinin-type compounds. Clin Pharmacokinet 39 :255–270.
-
9
Janssens B, van Herp M, Goubert L, Chan S, Uong S, Nong S, Socheat D, Brockman A, Ashley EA, Van Damme W, 2007. A randomized open study to assess the efficacy and tolerability of dihydroartemisinin-piperaquine for the treatment of uncomplicated falciparum malaria in Cambodia. Trop Med Int Health 12 :251–259.
-
10
Malik EM, Mohamed TA, Elmardi KA, Mowien RM, Elhassan AH, Elamin SB, Mannan AA, Ahmed ES, 2006. From chloroquine to artemisinin-based combination therapy: the Sudanese experience. Malar J 5 :65.
-
11
Rosenthal PJ, 2008. Artesunate for the treatment of severe falciparum malaria. N Engl J Med 358 :1829–1836.
-
12
Artemether-Quinine Meta-analysis Study Group, 2001. A meta-analysis using individual patient data of trials comparing artemether with quinine in the treatment of severe falciparum malaria. Trans R Soc Trop Med Hyg 95 :637–650.
-
13
Tran TH, Day NP, Nguyen HP, Nguyen TH, Tran TH, Pham PL, Dinh XS, Ly VC, Ha V, Waller D, Peto TE, White NJ, 1996. A controlled trial of artemether or quinine in Vietnamese adults with severe falciparum malaria. N Engl J Med 335 :76–83.
-
14
Whitty CJ, Ansah E, Reyburn H, 2005. Treating severe malaria. BMJ 330 :317–318.
-
15
Davis TM, Phuong HL, Ilett KF, Hung NC, Batty KT, Phuong VD, Powell SM, Thien HV, Binh TQ, 2001. Pharmacokinetics and pharmacodynamics of intravenous artesunate in severe falciparum malaria. Antimicrob Agents Chemother 45 :181–186.
-
16
Hien TT, Davis TM, Chuong LV, Ilett KF, Sinh DX, Phu NH, Agus C, Chiswell GM, White NJ, Farrar J, 2004. Comparative pharmacokinetics of intramuscular artesunate and artemether in patients with severe falciparum malaria. Antimicrob Agents Chemother 48 :4234–4239.
-
17
Ashley EA, White NJ, 2005. Artemisinin-based combinations. Curr Opin Infect Dis 18 :531–536.
-
18
Dondorp A, Nosten F, Stepniewska K, Day N, White N, 2005. South East Asian Quinine Artesunate Malaria Trial (SEAQUAMAT) group. Artesunate versus quinine for treatment of severe falciparum malaria: a randomised trial. Lancet 366 :717–725.
-
19
Jones KL, Donegan S, Lalloo DG, 2007. Artesunate versus quinine for treating severe malaria. Cochrane Database Syst Rev 17 :CD005967.
-
20
Jelinek T, 2005. Intravenous artesunate recommended for patients with severe malaria: position statement from TropNetEurop. Eurosurveillance 10 :ii-2841.
-
21
Pasvol G, 2006. The treatment of complicated and severe malaria. Br Med Bull 75–76 :29–47.
-
22
Nosten F, Ashley E, McGready R, Price R, 2006. We still need artesunate monotherapy. BMJ 333 :45.
-
23
Jones KL, Donegan S, Lalloo DG, 2008. Treating severe malaria: artesunate or Quinine? Indian Pediatr 45 :41–42.
-
24
Li Q, Weina P, Milhous WK, 2007. Pharmacokinetic and pharmacodynamic profiles of rapid-acting artemisinins in the antimalarial therapy. Curr Drug Ther 2 :210–223.
-
25
Li Q, Milhous WK, Weina PJ, 2007. Antimalarial in Malaria Therapy. New York: Nova Science Publishers.
-
26
Day N, Dondorp AM, 2007. The management of patients with severe malaria. Am J Trop Med Hyg 77 (Suppl):29–35.
-
27
Li Q, Xie LH, Haeberle A, Zhang J, Weina P, 2006. The evaluation of radiolabeled artesunate on tissue distribution in rats and protein binding in humans. Am J Trop Med Hyg 75 :817–826.
-
28
Li QG, Xie LH, Johnson TO, Si YZ, Haeberle AS, Weina PJ, 2007. Toxicity evaluation of artesunate and artelinate in Plasmodium berghei-infected and uninfected rats. Trans R Soc Trop Med Hyg 101 :104–112.
-
29
Gu Y, Li Q, Melendez V, Weina PJ, 2008. Comparison of HPLC with electrochemical detection and LC-MS/MS for the separation and validation of artesunate and dihydroartemisinin in animal and human plasma. J Chromatogr B Analyt Technol Biomed Life Sci 867 :213–218.
-
30
Bourne D, 1995. Mathematical Modeling of Pharmacokinetic Data, vol. 1. Lancaster, PA: Technomic Publishing.
-
31
Gabrielsson J, Weiner D, 2000. Pharmacokinetic and Pharmacodynamic Data Analysis: Concepts and Applications, vol. 3. Stockholm, Sweden: Apotekarsocieteten (Swedish Pharmaceutical Society).
-
32
Navaratnam V, Mansor SM, Sit NW, Grace J, Li QG, Olliaro P, 2000. Pharmacokinetics of artemisinin-type compounds. Clin Pharmacokinet 39 :255–270.
| Past two years | Past Year | Past 30 Days | |
|---|---|---|---|
| Abstract Views | 414 | 363 | 25 |
| Full Text Views | 515 | 7 | 0 |
| PDF Downloads | 151 | 7 | 0 |