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Pharmacokinetics/pharmacodynamics of chloroquine and artemisinin-based combination therapy with primaquine

September 24, 2019 - 14:59 -- Open Access
André Daher, Ghait Aljayyoussi, David G. Lalloo, et al.
Malaria Journal 2019 18:325, 23 September 2019

Activation of hypnozoites of vivax malaria causes multiple clinical relapses, which contribute to the Plasmodium vivax burden and continuing transmission. Artemisinin-based combination therapy (ACT) is effective against blood-stage P. vivax but requires co-administration with primaquine to achieve radical cure. The therapeutic efficacy of primaquine depends on the generation of a therapeutically active metabolite via cytochrome P450 2D6 (CYP2D6). Impaired CYP2D6 metabolism has been associated with primaquine treatment failure. This study investigated the association between impaired CYP2D6 genotypes, drug-exposure to the long-acting ACT component (schizonticidal drugs) and tolerance and efficacy.

Medical Condition: 

NOT Open Access | Chloroquine Analogues as Leads against Pneumocystis Lung Pathogens

October 30, 2018 - 12:44 -- NOT Open Access
Ana Gomes, Ricardo Ferraz, Lauren Ficker, Margaret S. Collins, Cristina Prudêncio, Melanie T. Cushion, Cátia Teixeira and Paula Gomes
Antimicrob. Agents Chemother. November 2018 62:e00983-18

The impact of Pneumocystis pneumonia (PcP) on morbidity and mortality remains substantial for immunocompromised individuals, including those afflicted by HIV infection, organ transplantation, cancer, autoimmune diseases, or subject to chemotherapy or corticosteroid-based therapies.

Chloroquine efficacy for Plasmodium vivax in Myanmar in populations with high genetic diversity and moderate parasite gene flow

July 11, 2017 - 12:53 -- Open Access
Myo Win Htun, Nan Cho Nwe Mon, Kamala Thriemer, et al.
Malaria Journal 2017 16:281, 10 July 2017

Treatment failures after chloroquine were observed following chloroquine monotherapy, with pvmdr1 amplification present in both Myawaddy and Shwegyin.

Medical Condition: 

Efficacy of Artesunate-mefloquine for Chloroquine-resistant Plasmodium vivax Malaria in Malaysia: An Open-label, Randomized, Controlled Trial

May 26, 2016 - 16:39 -- Open Access
Matthew J. Grigg, Timothy William, Nicholas M. Anstey, et al.
Clin Infect Dis. (2016) 62 (11): 1403-1411

A randomized, controlled trial of CQ vs artesunate-mefloquine (AS-MQ) for uncomplicated vivax malaria was conducted in 3 district hospitals in Sabah, Malaysia. Primaquine was administered on day 28. The primary outcome was the cumulative risk of treatment failure by day 28 by Kaplan–Meier analysis.

A Randomized Comparison of Chloroquine Versus Dihydroartemisinin–Piperaquine for the Treatment of Plasmodium vivax Infection in Vietnam

April 12, 2016 - 16:34 -- Open Access
Phung Duc Thuan, Nguyen Thuy Nha Ca, Tran Tinh Hien, et al.
Am J Trop Med Hyg 2016 vol. 94 no. 4 879-885

All cases of recurrent parasitemia in the chloroquine arm occurred from day 33 onward, with corresponding whole blood chloroquine concentration lower than 100 ng/mL in all patients. Chloroquine thus remains efficacious for the treatment of P. vivax malaria in southern Vietnam, but DHA-PPQ provides more rapid symptomatic and parasitological recovery.

NOT Open Access | Quinoline-based antimalarial hybrid compounds

August 12, 2015 - 14:27 -- NOT Open Access
Stéphanie Vandekerckhove, Matthias D’hooghe
Bioorganic & Medicinal Chemistry, Volume 23, Issue 16, 15 August 2015, Pages 5098–5119

Quinoline-containing compounds, such as quinine and chloroquine, have a long-standing history as potent antimalarial agents.

Medical Treatment: 

Monitoring PfMDR1 transport in Plasmodium falciparum

July 14, 2015 - 09:25 -- Open Access
Sarah J Reiling, Petra Rohrbach
Malaria Journal 2015, 14:270 (15 July 2015)

This study demonstrates that Fluo-4 can be used to investigate PfMDR1 transport dynamics in both drug-sensitive and -resistant parasites.

Medical Treatment: 

Not Open Access | Chloroquine analogues in drug discovery: new directions of uses, mechanisms of actions and toxic manifestations from malaria to multifarious diseases

May 23, 2015 - 10:32 -- NOT Open Access
Abdul Alim Al-Bari
J. Antimicrob. Chemother. (2015) 70 (6): 1608-1621.

This review is concerned with the lysosomotropic, anti-inflammatory and immunomodulatory mechanisms of chloroquine, hydroxychloroquine, quinacrine and related analogues, and the current evidence for both their beneficial effects and potential adverse manifestations in various diseases.

Persistence of chloroquine-resistant haplotypes of Plasmodium falciparum in children with uncomplicated Malaria in Lagos, Nigeria, four years after change of chloroquine as first-line antimalarial medicine

April 28, 2015 - 16:50 -- Open Access
Oladosu O Oladipo, Oyibo A Wellington and Colin J Sutherland
Diagnostic Pathology 2015, 10:41

This study determined the prevalence of pfcrt haplotypes and point mutations in pfmdr1 genes four years after the change in antimalarial treatment policy from CQ to the ACTs in Lagos, a commercial city in South-West, Nigeria.

Efficacy of chloroquine for the treatment of Plasmodium vivax in the Saharan zone in Mauritania

February 25, 2015 - 15:29 -- Open Access
Mohamed Ould Ahmedou Salem, Yeslim Mohamed Lemine, Sidi Lebatt, et al.
Malaria Journal 2015, 14:39 (28 January 2015)

The aim of the present study was to evaluate the clinical efficacy and tolerance of chloroquine to treat P. vivax malaria in Mauritanian patients.


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