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Journal articles on the topic 'Pharmacokinetics; Dihydroartemisinin'

Author: Grafiati

Published: 4 June 2021

Last updated: 7 February 2022

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1

Rijken, Marcus J., Rose McGready, Aung Phae Phyo, et al. "Pharmacokinetics of Dihydroartemisinin and Piperaquine in Pregnant and Nonpregnant Women with Uncomplicated Falciparum Malaria." Antimicrobial Agents and Chemotherapy 55, no. 12 (2011): 5500–5506. http://dx.doi.org/10.1128/aac.05067-11.

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ABSTRACTDihydroartemisinin-piperaquine is a fixed-dose artemisinin-based combination treatment. Some antimalarials have altered pharmacokinetics in pregnancy. Pregnant women in the 2nd or 3rd trimester and matched nonpregnant women with uncomplicated falciparum malaria were treated with a total of 6.4 mg/kg of body weight dihydroartemisinin and 51.2 mg/kg piperaquine once daily for 3 days. Venous blood samples were drawn at prespecified time points over 9 weeks. Plasma dihydroartemisinin and piperaquine concentrations were analyzed by liquid chromatography-mass spectrometry. Piperaquine and di

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2

Tarning, Joel, Marcus J. Rijken, Rose McGready, et al. "Population Pharmacokinetics of Dihydroartemisinin and Piperaquine in Pregnant and Nonpregnant Women with Uncomplicated Malaria." Antimicrobial Agents and Chemotherapy 56, no. 4 (2012): 1997–2007. http://dx.doi.org/10.1128/aac.05756-11.

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ABSTRACTPregnant women are particularly vulnerable to malaria. The pharmacokinetic properties of antimalarial drugs are often affected by pregnancy, resulting in lower drug concentrations and a consequently higher risk of treatment failure. The objective of this study was to evaluate the population pharmacokinetic properties of piperaquine and dihydroartemisinin in pregnant and nonpregnant women with uncomplicated malaria. Twenty-four pregnant and 24 matched nonpregnant women on the Thai-Myanmar boarder were treated with a standard fixed oral 3-day treatment, and venous plasma concentrations o

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3

Hanboonkunupakarn, Borimas, Elizabeth A. Ashley, Podjanee Jittamala, et al. "Open-Label Crossover Study of Primaquine and Dihydroartemisinin-Piperaquine Pharmacokinetics in Healthy Adult Thai Subjects." Antimicrobial Agents and Chemotherapy 58, no. 12 (2014): 7340–46. http://dx.doi.org/10.1128/aac.03704-14.

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ABSTRACTDihydroartemisinin-piperaquine is an artemisinin-based combination treatment (ACT) recommended by the WHO for uncomplicatedPlasmodium falciparummalaria, and it is being used increasingly for resistant vivax malaria where combination with primaquine is required for radical cure. The WHO recently reinforced its recommendations to add a single dose of primaquine to ACTs to reduceP. falciparumtransmission in low-transmission settings. The pharmacokinetics of primaquine and dihydroartemisinin-piperaquine were evaluated in 16 healthy Thai adult volunteers in a randomized crossover study. Vol

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4

Nyunt, Myaing M., Vy K. Nguyen, Richard Kajubi, et al. "Artemether-Lumefantrine Pharmacokinetics and Clinical Response Are Minimally Altered in Pregnant Ugandan Women Treated for Uncomplicated Falciparum Malaria." Antimicrobial Agents and Chemotherapy 60, no. 3 (2015): 1274–82. http://dx.doi.org/10.1128/aac.01605-15.

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Artemether-lumefantrine is a first-line regimen for the treatment of uncomplicated malaria during the second and third trimesters of pregnancy. Previous studies have reported changes in the pharmacokinetics and clinical outcomes following treatment with artemether-lumefantrine in pregnant women compared to nonpregnant adults; however, the results are inconclusive. We conducted a study in rural Uganda to compare the pharmacokinetics of artemether-lumefantrine and the treatment responses between 30 pregnant women and 30 nonpregnant adults with uncomplicatedPlasmodium falciparummalaria. All parti

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5

Davis, Timothy M. E., Hoang Lan Phuong, Kenneth F. Ilett, et al. "Pharmacokinetics and Pharmacodynamics of Intravenous Artesunate in Severe Falciparum Malaria." Antimicrobial Agents and Chemotherapy 45, no. 1 (2001): 181–86. http://dx.doi.org/10.1128/aac.45.1.181-186.2001.

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ABSTRACT To provide novel data relating to the dispositions, effects, and toxicities of the artemisinin derivatives in severe malaria, we studied 30 Vietnamese adults with slide-positive falciparum malaria treated with intravenous artesunate. Twelve patients with complications (severe; group 1) and 8 patients without complications but requiring parenteral therapy (moderately severe; group 2) received 120 mg of artesunate by injection, and 10 patients with moderately severe complications (group 3) were given 240 mg by infusion. Serial concentrations of artesunate and its active metabolite dihyd

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6

Birgersson, Sofia, Innocent Valea, Halidou Tinto, et al. "Population pharmacokinetics of artesunate and dihydroartemisinin in pregnant and non-pregnant women with uncomplicated Plasmodium falciparum malaria in Burkina Faso: an open label trial." Wellcome Open Research 4 (March 7, 2019): 45. http://dx.doi.org/10.12688/wellcomeopenres.14849.1.

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Background: Malaria during pregnancy is a major health risk for both the mother and the foetus. Pregnancy has been shown to influence the pharmacokinetics of a number of different antimalarial drugs. This might lead to an under-exposure in these patients which could increase the risk of treatment failure and the development of drug resistance. The study aim was to evaluate the pharmacokinetics of artesunate and dihydroartemisinin in pregnant and non-pregnant patients using a population modelling approach. Methods: Twenty-four women in their second and third trimester of pregnancy and twenty-fo

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7

Birgersson, Sofia, Innocent Valea, Halidou Tinto, et al. "Population pharmacokinetics of artesunate and dihydroartemisinin in pregnant and non-pregnant women with uncomplicated Plasmodium falciparum malaria in Burkina Faso: an open label trial." Wellcome Open Research 4 (January 10, 2020): 45. http://dx.doi.org/10.12688/wellcomeopenres.14849.2.

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Background: Malaria during pregnancy is a major health risk for both the mother and the foetus. Pregnancy has been shown to influence the pharmacokinetics of a number of different antimalarial drugs. This might lead to an under-exposure in these patients which could increase the risk of treatment failure and the development of drug resistance. The study aim was to evaluate the pharmacokinetics of artesunate and dihydroartemisinin in pregnant and non-pregnant patients using a population modelling approach. Methods: Twenty-four women in their second and third trimester of pregnancy and twenty-fo

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8

Hietala, Sofia Friberg, Andreas Mårtensson, Billy Ngasala, et al. "Population Pharmacokinetics and Pharmacodynamics of Artemether and Lumefantrine during Combination Treatment in Children with Uncomplicated Falciparum Malaria in Tanzania." Antimicrobial Agents and Chemotherapy 54, no. 11 (2010): 4780–88. http://dx.doi.org/10.1128/aac.00252-10.

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ABSTRACT The combination of artemether (ARM) and lumefantrine is currently the first-line treatment of uncomplicated falciparum malaria in mainland Tanzania. While the exposure to lumefantrine has been associated with the probability of adequate clinical and parasitological cure, increasing exposure to artemether and the active metabolite dihydroartemisinin (DHA) has been shown to decrease the parasite clearance time. The aim of this analysis was to describe the pharmacokinetics and pharmacodynamics of artemether, dihydroartemisinin, and lumefantrine in African children with uncomplicated mala

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9

Tarning, Joel, Frank Kloprogge, Mehul Dhorda, et al. "Pharmacokinetic Properties of Artemether, Dihydroartemisinin, Lumefantrine, and Quinine in Pregnant Women with Uncomplicated Plasmodium falciparum Malaria in Uganda." Antimicrobial Agents and Chemotherapy 57, no. 10 (2013): 5096–103. http://dx.doi.org/10.1128/aac.00683-13.

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ABSTRACTPregnancy alters the pharmacokinetic properties of many drugs used in the treatment of malaria, usually resulting in lower drug exposures. This increases the risks of treatment failure, adverse outcomes for the fetus, and the development of resistance. The pharmacokinetic properties of artemether and its principal metabolite dihydroartemisinin (n= 21), quinine (n= 21), and lumefantrine (n= 26) in pregnant Ugandan women were studied. Lumefantrine pharmacokinetics in a nonpregnant control group (n= 17) were also studied. Frequently sampled patient data were evaluated with noncompartmenta

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10

Nguyen, Dao Van Hoang, Quoc Phuc Nguyen, Ngoa Dang Nguyen, et al. "Pharmacokinetics and Ex Vivo Pharmacodynamic Antimalarial Activity of Dihydroartemisinin-Piperaquine in Patients with Uncomplicated Falciparum Malaria in Vietnam." Antimicrobial Agents and Chemotherapy 53, no. 8 (2009): 3534–37. http://dx.doi.org/10.1128/aac.01717-08.

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ABSTRACT Compared to healthy subjects, malaria patients show a reduction in the mean oral clearance (1.19 versus 5.87 liters/h/kg of body weight) and apparent volume of distribution (1.47 versus 8.02 liters/kg) of dihydroartemisinin in Vietnamese patients following treatment with dihydroartemisinin-piperaquine (Artekin) for uncomplicated Plasmodium falciparum. Dihydroartemisinin is responsible for most of the ex vivo antimalarial activity of dihydroartemisinin-piperaquine.

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11

Batty, Kevin T., Peter L. Gibbons, Kenneth F. Ilett, and Timothy M. E. Davis. "Pharmacokinetics of Dihydroartemisinin in a Murine Malaria Model." American Journal of Tropical Medicine and Hygiene 78, no. 4 (2008): 641–42. http://dx.doi.org/10.4269/ajtmh.2008.78.641.

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12

Chinh, Nguyen Trong, Nguyen Ngoc Quang, Nguyen Xuan Thanh, et al. "Pharmacokinetics and Bioequivalence Evaluation of Two Fixed-Dose Tablet Formulations of Dihydroartemisinin and Piperaquine in Vietnamese Subjects." Antimicrobial Agents and Chemotherapy 53, no. 2 (2008): 828–31. http://dx.doi.org/10.1128/aac.00927-08.

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ABSTRACT The two fixed-dose combinations of dihydroartemisinin and piperaquine (Artekin and Arterakine) were found to be bioinequivalent in healthy Vietnamese subjects. However, because the peak plasma concentrations and areas under the concentration-time curves of dihydroartemisinin and piperaquine were only marginally different between the two formulations, similar therapeutic efficacies are expected in the treatment of malaria infections.

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13

Reuter, Stephanie E., Allan M. Evans, Sepehr Shakib, et al. "Effect of Food on the Pharmacokinetics of Piperaquine and Dihydroartemisinin." Clinical Drug Investigation 35, no. 9 (2015): 559–67. http://dx.doi.org/10.1007/s40261-015-0312-8.

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14

Chinh, Nguyen Trong, Nguyen Ngoc Quang, Chu Xuan Anh, et al. "Pharmacokinetics andEx VivoAntimalarial Activity of Artesunate-Azithromycin in Healthy Volunteers." Antimicrobial Agents and Chemotherapy 55, no. 9 (2011): 4412–15. http://dx.doi.org/10.1128/aac.00365-11.

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ABSTRACTIn 18 male healthy subjects, artesunate (200 mg)-azithromycin (1,500 mg) daily for 3 days was found to be well tolerated, with only mild gastrointestinal disturbances reported. The pharmacokinetic properties of artesunate-azithromycin given in combination are comparable to those of the drugs given alone. Artesunate and its major active metabolite, dihydroartemisinin, are responsible for most of theex vivoantimalarial activity, with a delayed contribution by azithromycin.

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15

Davis, Timothy M. E., Michelle England, Anne-Marie Dunlop, et al. "Assessment of the Effect of Mefloquine on Artesunate Pharmacokinetics in Healthy Male Volunteers." Antimicrobial Agents and Chemotherapy 51, no. 3 (2006): 1099–101. http://dx.doi.org/10.1128/aac.01253-06.

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ABSTRACT The effect of mefloquine on artesunate pharmacokinetics was assessed in 20 volunteers given artesunate for 3 days, followed ≥21 days later by combination therapy for 3 days. The areas under the concentration-time curve from 0 h to infinity for dihydroartemisinin, the active metabolite of artesunate, were similar on day 3 of the two dosing periods (P = 0.12), implying no interaction.

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16

Chotsiri, Palang, Thanaporn Wattanakul, Richard M. Hoglund, et al. "Population pharmacokinetics and electrocardiographic effects of dihydroartemisinin–piperaquine in healthy volunteers." British Journal of Clinical Pharmacology 83, no. 12 (2017): 2752–66. http://dx.doi.org/10.1111/bcp.13372.

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17

Guo, Wenju, Ning Li, Guolian Ren, et al. "Murine pharmacokinetics and antimalarial pharmacodynamics of dihydroartemisinin trimer self-assembled nanoparticles." Parasitology Research 120, no. 8 (2021): 2827–37. http://dx.doi.org/10.1007/s00436-021-07208-6.

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18

Ren, Guolian, Pei Chen, Jiaqi Tang, et al. "In vivo and in vitro evaluation of dihydroartemisinin prodrug nanocomplexes as a nano-drug delivery system: characterization, pharmacokinetics and pharmacodynamics." RSC Advances 10, no. 29 (2020): 17270–79. http://dx.doi.org/10.1039/d0ra02150d.

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To develop new, more effective and lower toxicity antitumor dihydroartemisinin (DHA) nanocomplexes, a DHA prodrug synthesized in this study was used to prepare DHA prodrug self-assembled nanocomplexes (DHANPs) by molecular self-assembly technology.

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19

Salman, Sam, Madhu Page-Sharp, Susan Griffin, et al. "Population Pharmacokinetics of Artemether, Lumefantrine, and Their Respective Metabolites in Papua New Guinean Children with Uncomplicated Malaria." Antimicrobial Agents and Chemotherapy 55, no. 11 (2011): 5306–13. http://dx.doi.org/10.1128/aac.05136-11.

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ABSTRACTThere are sparse published data relating to the pharmacokinetic properties of artemether, lumefantrine, and their active metabolites in children, especially desbutyl-lumefantrine. We studied 13 Papua New Guinean children aged 5 to 10 years with uncomplicated malaria who received the six recommended doses of artemether (1.7 mg/kg of body weight) plus lumefantrine (10 mg/kg), given with fat over 3 days. Intensive blood sampling was carried out over 42 days. Plasma artemether, dihydroartemisinin, lumefantrine, and desbutyl-lumefantrine were assayed using liquid chromatography-mass spectro

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20

Xie, Lisa H., Qigui Li, Jing Zhang, and Peter J. Weina. "Pharmacokinetics, tissue distribution and mass balance of radiolabeled dihydroartemisinin in male rats." Malaria Journal 8, no. 1 (2009): 112. http://dx.doi.org/10.1186/1475-2875-8-112.

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21

Duan, Shuai, Ruili Wang, Rongrong Wang, et al. "In vivo antimalarial activity and pharmacokinetics of artelinic acid-choline derivative liposomes in rodents." Parasitology 147, no. 1 (2019): 58–64. http://dx.doi.org/10.1017/s0031182019001306.

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AbstractIt is urgent to develop new antimalarial drugs with good therapeutic effects to address the emergence of drug resistance. Here, the artelinic acid-choline derivative (AD) was synthesized by dehydration reaction and esterification reaction, aimed to avoid the emergence of drug resistance by synergistic effect of artemisinins and choline derivative, which could compete with choline for rate-limiting enzymes in the phosphatidylcholine (PC) biosynthetic pathway. AD was formulated into liposomes (ADLs) by the thin-film hydration method. Efficacy of ADLs was evaluated by Peters 4-day suppres

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22

Srinivas, Nuggehally R. "Dihydroartemisinin Pharmacokinetics in Patients with Malaria after Multiple Doses—Assembling Clues and Perspectives." Drug Metabolism and Pharmacokinetics 24, no. 3 (2009): 282–84. http://dx.doi.org/10.2133/dmpk.24.282.

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23

Xing, J., K. H. Bai, T. Liu, R. L. Wang, L. F. Zhang, and S. Q. Zhang. "The multiple-dosing pharmacokinetics of artemether, artesunate, and their metabolite dihydroartemisinin in rats." Xenobiotica 41, no. 3 (2010): 252–58. http://dx.doi.org/10.3109/00498254.2010.542257.

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24

Benjamin, John M., Brioni R. Moore, Sam Salman, et al. "Population Pharmacokinetics, Tolerability, and Safety of Dihydroartemisinin-Piperaquine and Sulfadoxine-Pyrimethamine-Piperaquine in Pregnant and Nonpregnant Papua New Guinean Women." Antimicrobial Agents and Chemotherapy 59, no. 7 (2015): 4260–71. http://dx.doi.org/10.1128/aac.00326-15.

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ABSTRACTThe tolerability, safety, and disposition of dihydroartemisinin (DHA) and piperaquine (PQ) were assessed in 32 pregnant (second/third trimester) and 33 nonpregnant Papua New Guinean women randomized to adult treatment courses of DHA-PQ (three daily doses) or sulfadoxine-pyrimethamine (SP)-PQ (three daily PQ doses, single dose of SP). All dose adminstrations were observed, and subjects fasted for 2 h postdose. Plasma PQ was assayed by using high-performance liquid chromatography, and DHA was assessed by using liquid chromatography-mass spectrometry. Compartmental pharmacokinetic models

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Morris, Carrie A., Marie A. Onyamboko, Edmund Capparelli, et al. "Population pharmacokinetics of artesunate and dihydroartemisinin in pregnant and non-pregnant women with malaria." Malaria Journal 10, no. 1 (2011): 114. http://dx.doi.org/10.1186/1475-2875-10-114.

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26

Ali, Shabana, Muzammil H. Najmi, Joel Tarning, and Niklas Lindegardh. "Pharmacokinetics of artemether and dihydroartemisinin in healthy Pakistani male volunteers treated with artemether-lumefantrine." Malaria Journal 9, no. 1 (2010): 275. http://dx.doi.org/10.1186/1475-2875-9-275.

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27

Osonwa, Uduma E., and Ming Hu. "Bioavailability and Pharmacokinetics of Dihydroartemisinin (DHA) and its Analogs—Mechanistic Studies on its ADME." Current Pharmacology Reports 4, no. 1 (2018): 33–44. http://dx.doi.org/10.1007/s40495-018-0120-y.

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28

Moore, Brioni R., Kevin T. Batty, Christopher Andrzejewski, Jeffrey D. Jago, Madhu Page-Sharp, and Kenneth F. Ilett. "Pharmacokinetics and Pharmacodynamics of Piperaquine in a Murine Malaria Model." Antimicrobial Agents and Chemotherapy 52, no. 1 (2007): 306–11. http://dx.doi.org/10.1128/aac.00878-07.

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ABSTRACT Piperaquine (PQ) is an important partner in antimalarial treatment strategies. However, there is a paucity of detailed preclinical and pharmacokinetic data to link PQ serum concentrations and toxicity or efficacy. The aim of this study was to investigate the pharmacokinetics and pharmacodynamics of PQ in a murine malaria treatment model. The study comprised three arms. (i) PQ pharmacokinetic parameters were determined in healthy and malaria-infected mice (90 mg/kg PQ phosphate [PQP]). (ii) For determination of single-dose pharmacodynamics, Swiss mice were inoculated with Plasmodium be

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29

Olorunfemi, Eseyin A., Igboasoiyi C. Arnold, Igbo Chinenye, Igboasoiyi Adaora, Ekarika Johnson, and Dooka Barido. "Effects of the Leaf Extract of Vernonia amygdalina on the Pharmacokinetics of Dihydroartemisinin in Rat." Pharmacologia 3, no. 12 (2012): 713–18. http://dx.doi.org/10.5567/pharmacologia.2012.713.718.

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30

Le Thi, Diem Thuy, Ngoc Hung Le, Canh Hung Nguyen, Danh Phan Thi, and Kesara Na-Bangchang. "Pharmacokinetics of a Five-day Oral Dihydroartemisinin Monotherapy Regimen in Patients with Uncomplicated Falciparum Malaria." Drug Metabolism and Pharmacokinetics 23, no. 3 (2008): 158–64. http://dx.doi.org/10.2133/dmpk.23.158.

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LI, QI-GUI, JAMES O. PEGGINS, LAWRENCE L. FLECKENSTEIN, KELLY MASONIC, MELVIN H. HEIFFER, and THOMAS G. BREWER. "The Pharmacokinetics and Bioavailability of Dihydroartemisinin, Arteether, Artemether, Artesunic Acid and Artelinic Acid in Rats." Journal of Pharmacy and Pharmacology 50, no. 2 (1998): 173–82. http://dx.doi.org/10.1111/j.2042-7158.1998.tb06173.x.

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32

McGready, Rose, Aung Pyae Phyo, Marcus J. Rijken, et al. "Artesunate/dihydroartemisinin pharmacokinetics in acute falciparum malaria in pregnancy: absorption, bioavailability, disposition and disease effects." British Journal of Clinical Pharmacology 73, no. 3 (2012): 467–77. http://dx.doi.org/10.1111/j.1365-2125.2011.04103.x.

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Sambol, NC, L. Yan, DJ Creek, et al. "Population Pharmacokinetics of Piperaquine in Young Ugandan Children Treated With Dihydroartemisinin-Piperaquine for Uncomplicated Malaria." Clinical Pharmacology & Therapeutics 98, no. 1 (2015): 87–95. http://dx.doi.org/10.1002/cpt.104.

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34

Hong, Xin, Chang-hui Liu, Xiao-tao Huang, et al. "Pharmacokinetics of dihydroartemisinin in Artekin tablets for single and repeated dosing in Chinese healthy volunteers." Biopharmaceutics & Drug Disposition 29, no. 4 (2008): 237–44. http://dx.doi.org/10.1002/bdd.607.

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35

Simpson, Julie A., Tsiri Agbenyega, Karen I. Barnes, et al. "Population Pharmacokinetics of Artesunate and Dihydroartemisinin following Intra-Rectal Dosing of Artesunate in Malaria Patients." PLoS Medicine 3, no. 11 (2006): e444. http://dx.doi.org/10.1371/journal.pmed.0030444.

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36

McGready, R., K. Stepniewska, S. A. Ward, et al. "Pharmacokinetics of dihydroartemisinin following oral artesunate treatment of pregnant women with acute uncomplicated falciparum malaria." European Journal of Clinical Pharmacology 62, no. 5 (2006): 367–71. http://dx.doi.org/10.1007/s00228-006-0118-y.

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Minzi, Omary Mashiku, Rajabu Hussein Mnkugwe, Eliford Ngaimisi, et al. "Effect of Dihydroartemisinin-Piperaquine on the Pharmacokinetics of Praziquantel for Treatment of Schistosoma mansoni Infection." Pharmaceuticals 14, no. 5 (2021): 400. http://dx.doi.org/10.3390/ph14050400.

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Praziquantel (PZQ) and dihydroartemisinin-piperaquine (DHP) combination recently showed superior effectiveness than PZQ alone to treat intestinal schistosomiasis. In this follow-up study, we investigated the effect of DHP co-administration on the pharmacokinetics of PZQ and its enantiomers among 64 Schistosoma mansoni infected children treated with PZQ alone (n = 32) or PZQ + DHP combination (n = 32). Plasma samples collected at 0, 1, 2, 4, 6, and 8 h post-dose were quantified using UPLCMS/MS. The geometric mean (GM) of AUCs for total PZQ, R-PZQ and S-PZQ were significantly higher among childr

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Wang, Rongrong, Guolian Ren, Liqing Chai, et al. "Pharmacokinetics and antimalarial activities of reduction-responsive releasing dihydroartemisinin prodrug self-assembled nanoparticles in rodents." Journal of Drug Delivery Science and Technology 63 (June 2021): 102515. http://dx.doi.org/10.1016/j.jddst.2021.102515.

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39

Tarning, J., E. A. Ashley, N. Lindegardh, et al. "Population Pharmacokinetics of Piperaquine after Two Different Treatment Regimens with Dihydroartemisinin-Piperaquine in Patients with Plasmodium falciparum Malaria in Thailand." Antimicrobial Agents and Chemotherapy 52, no. 3 (2008): 1052–61. http://dx.doi.org/10.1128/aac.00955-07.

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ABSTRACT The population pharmacokinetics of piperaquine in adults and children with uncomplicated Plasmodium falciparum malaria treated with two different dosage regimens of dihydroartemisinin-piperaquine were characterized. Piperaquine pharmacokinetics in 98 Burmese and Karen patients aged 3 to 55 years were described by a two-compartment disposition model with first-order absorption and interindividual random variability on all parameters and were similar with the three- and four-dose regimens. Children had a lower body weight-normalized oral clearance than adults, resulting in longer termin

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Sunitha G N, Satyavati Dulipala D, and Girish Gudi. "Effect of ritonavir on pharmacokinetics of antimalarial drug combinations in rats." International Journal of Research in Pharmaceutical Sciences 10, no. 3 (2019): 2477–86. http://dx.doi.org/10.26452/ijrps.v10i3.1497.

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The current treatment for Human Immunodeficiency Virus (HIV) patients coinfected with malaria involves the coadministration of antimalarial and antiretroviral (ARV) drugs. The World Health Organization (WHO) recommends artemisinin-based therapy for malaria that usually consists of artemether, artesunate or dihydroartemisinin with non-artemisinin derivatives such as amodiaquine, lumefantrine and mefloquine. Protease inhibitors (PI) such as ritonavir contribute to the improved health of HIV-positive individuals, and the inclusion of ritonavir in antiretroviral regimens is common in clinical prac

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Morris, Carrie A., Beesan Tan, Stephan Duparc, et al. "Effects of Body Size and Gender on the Population Pharmacokinetics of Artesunate and Its Active Metabolite Dihydroartemisinin in Pediatric Malaria Patients." Antimicrobial Agents and Chemotherapy 57, no. 12 (2013): 5889–900. http://dx.doi.org/10.1128/aac.00635-13.

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ABSTRACTDespite the important role of the antimalarial artesunate and its active metabolite dihydroartemisinin (DHA) in malaria treatment efforts, there are limited data on the pharmacokinetics of these agents in pediatric patients. This study evaluated the effects of body size and gender on the pharmacokinetics of artesunate-DHA using data from pediatric and adult malaria patients. Nonlinear mixed-effects modeling was used to obtain a base model consisting of first-order artesunate absorption and one-compartment models for artesunate and for DHA. Various methods of incorporating effects of bo

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Annerberg, Anna, Khin Maung Lwin, Niklas Lindegardh, et al. "A Small Amount of Fat Does Not Affect Piperaquine Exposure in Patients with Malaria." Antimicrobial Agents and Chemotherapy 55, no. 9 (2011): 3971–76. http://dx.doi.org/10.1128/aac.00279-11.

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ABSTRACTDihydroartemisinin-piperaquine is a new, highly effective, and well-tolerated combination treatment for uncomplicated falciparum malaria. The lipophilic characteristic of piperaquine suggests that administration together with fat will increase the oral bioavailability of the drug, and this has been reported for healthy volunteers. This pharmacokinetic study monitored 30 adult patients with uncomplicated falciparum malaria for 4.5 months to evaluate the effects of the concomitant intake of fat on the total piperaquine exposure. The fixed-drug combination of dihydroartemisinin-piperaquin

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Chai, Liqing, Rongrong Wang, Yan Wang, et al. "Auto-Induction of Intestinal First-Pass Effect Related Time-Dependent Pharmacokinetics of Artemisinin Rather than Dihydroartemisinin." Journal of Pharmaceutical Sciences 110, no. 1 (2021): 458–66. http://dx.doi.org/10.1016/j.xphs.2020.09.023.

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Smit, Menno R., Eric O. Ochomo, David Waterhouse, et al. "Pharmacokinetics‐Pharmacodynamics of High‐Dose Ivermectin with Dihydroartemisinin‐Piperaquine on Mosquitocidal Activity and QT ‐Prolongation ( IVERMAL )." Clinical Pharmacology & Therapeutics 105, no. 2 (2018): 388–401. http://dx.doi.org/10.1002/cpt.1219.

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Salman, Sam, Daryl Bendel, Toong C. Lee, David Templeton, and Timothy M. E. Davis. "Pharmacokinetics of a Novel Sublingual Spray Formulation of the Antimalarial Drug Artemether in African Children with Malaria." Antimicrobial Agents and Chemotherapy 59, no. 6 (2015): 3208–15. http://dx.doi.org/10.1128/aac.05014-14.

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ABSTRACTThe pharmacokinetics of sublingual artemether (ArTiMist) was investigated in 91 young African children with severe malaria or who could not tolerate oral antimalarial therapy. Each received 3.0 mg/kg of body weight of artemether at 0, 8, 24, 36, 48, and 60 h or until the initiation of oral treatment. Few blood samples were drawn postdose. Plasma artemether and dihydroartemisinin (DHA) levels were measured using liquid chromatography-mass spectrometry, and the data were analyzed using established population compartmental pharmacokinetic models. Parasite clearance was prompt (median para

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Dai, Tianming, Weifan Jiang, Zizheng Guo, Yanxiang Xie, and Renke Dai. "Comparison of in vitro/in vivo blood distribution and pharmacokinetics of artemisinin, artemether and dihydroartemisinin in rats." Journal of Pharmaceutical and Biomedical Analysis 162 (January 2019): 140–48. http://dx.doi.org/10.1016/j.jpba.2018.09.024.

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Tan, Beesan, Himanshu Naik, In-Jin Jang, et al. "Population pharmacokinetics of artesunate and dihydroartemisinin following single- and multiple-dosing of oral artesunate in healthy subjects." Malaria Journal 8, no. 1 (2009): 304. http://dx.doi.org/10.1186/1475-2875-8-304.

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Ittarat, Wanida, Sornchai Looareesuwan, Pensri Pootrakul, Petchmanee Sumpunsirikul, Phantip Vattanavibool та Steven R. Meshnick. "Effects of α-Thalassemia on Pharmacokinetics of the Antimalarial Agent Artesunate". Antimicrobial Agents and Chemotherapy 42, № 9 (1998): 2332–35. http://dx.doi.org/10.1128/aac.42.9.2332.

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ABSTRACT Thalassemia is common in Southeast Asia, where artemisinin derivatives are frequently used in the treatment of malaria. It has been previously reported that artemisinin derivatives can be concentrated by uninfected thalassemic erythrocytes in vitro but not by normal erythrocytes. As a follow-up to this report, we studied the antimalarial kinetics of intravascular artesunate (2.4 mg/kg of body weight) in 10 persons with normal hemoglobins and in 10 patients with thalassemia (2 with α-thalassemia type 1–hemoglobin Constant Spring and 8 with α-thalassemia type 1–α-thalassemia type 2). Co

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Salman, Sam, Daryl Bendel, Toong C. Lee, David Templeton, and Timothy M. E. Davis. "Pharmacokinetics of a Novel Sublingual Spray Formulation of the Antimalarial Drug Artemether in Healthy Adults." Antimicrobial Agents and Chemotherapy 59, no. 6 (2015): 3197–207. http://dx.doi.org/10.1128/aac.05013-14.

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ABSTRACTThe pharmacokinetics of sublingual artemether (ArTiMist) was investigated in two open-label studies. In study 1, 16 healthy males were randomized to each of four single-dose treatments administered in random order: (i) 15.0 mg of sublingual artemether (5 × 3.0 actuations), (ii) 30.0 mg of sublingual artemether (10 × 3.0 mg), (iii) 30.0 mg of sublingual artemether (5 × 6.0 mg), and (iv) 30.0 mg of artemether in tablet form. In study 2, 16 healthy males were randomized to eight 30.0-mg doses of sublingual artemether given over 5 days as either 10 3.0-mg or 5 6.0-mg actuations. Frequent b

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Khemawoot, Phisit, David Saunders, Maneerat Rasameesoraj, et al. "Absolute Bioavailability ofcis-Mirincamycin andtrans-Mirincamycin in Healthy Rhesus Monkeys andEx VivoAntimalarial Activity against Plasmodium falciparum." Antimicrobial Agents and Chemotherapy 55, no. 12 (2011): 5881–86. http://dx.doi.org/10.1128/aac.01619-10.

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ABSTRACTThe pharmacokinetics, oral bioavailability, andex vivoantimalarial activity of mirincamycin isomers in a healthy rhesus monkey model were assessed to support lead optimization of novel nonhemolytic drugs for radical cure and causal prophylaxis of malaria. Fourteen male rhesus monkeys were randomized to four groups, which includedcisandtransisomers by the oral and intravenous routes, with vehicle-only controls for each dosing route. Concentration-time data were collected for 7 days and were analyzed by noncompartmental analysis.cis-Mirincamycin had an absolute oral bioavailability of 13

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