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chloroquine

Mechanisms of Resistance: Evidence of Selective Sweeps in Genes Conferring Resistance to Chloroquine and Pyrimethamine in Plasmodium falciparum Isolates in India

February 25, 2010 - 21:28 -- Kabogo Ndegwa
Author(s): 
Tonya Mixson-Hayden, Vidhan Jain, Neeru Singh et al.
Reference: 
Antimicrobial Agents and Chemotherapy, March 2010, Pages 997-1006, Volume 54, No. 3

We tested whether chloroquine- and antifolate drug-resistant genotypes would be more commonly associated with cases of cerebral malaria than with cases of mild malaria in the province of Jabalpur, India, by genotyping the dhps, dhfr, pfmdr-1, and pfcrt genes using pyrosequencing, direct sequencing, and real-time PCR.

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Pharmacology: Pharmacokinetics of Chloroquine and Monodesethylchloroquine in Pregnancy

February 25, 2010 - 20:54 -- Kabogo Ndegwa
Author(s): 
Harin A. Karunajeewa, Sam Salman, Ivo Mueller, Francisca Baiwog, Servina Gomorrai, Irwin Law,1 Madhu Page-Sharp, Stephen Rogerson, Peter Siba, Kenneth F. Ilett, and Timothy M. E. Davis
Reference: 
Antimicrobial Agents and Chemotherapy, March 2010, Pages 1186-1192, Volume 54, No. 3

Reduced plasma concentrations of both CQ and DECQ could compromise both curative efficacy and posttreatment prophylactic properties in pregnant patients. Higher IPTp CQ doses may be desirable but could increase the risk of adverse hemodynamic effects.

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Open Access | Evaluation of chloroquine therapy for vivax and falciparum malaria in southern Sumatra, western Indonesia

February 17, 2010 - 20:26 -- Ingeborg van Schayk
Author(s): 
Inge Sutanto, Dedeh Endawati, Liem Hui Ling, Ferdinand Laihad, Rianto Setiabudy, J Kevin Baird
Reference: 
Malaria Journal 2010, 9:52 (12 February 2010)

Clinical trial of the use of chloroquine for monoinfections of P.falciparum and P. vivax. Although a small study and almost 7 years old, the data provide clear evidence of high grade chloroquine resistance in western Indonesia, a long distance from the known hot spot on the Island of Papua.

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Therapeutic efficacy of chloroquine and chloroquine plus primaquine for the treatment of Plasmodium vivax in Ethiopia

January 21, 2010 - 09:17 -- Kabogo Ndegwa
Author(s): 
Asnakew K. Yeshiwondima, Afework H. Tekleb, 1, Dereje O. Dengelac, 2, Ambachew M. Yohannesa, 3 and Awash Teklehaimanot
Reference: 
Acta Tropica, Volume 113, Issue 2, February 2010, Pages 105-113

We assessed the efficacy of standard chloroquine and chloroquine plus primaquine treatment for P. vivax infections in a randomized open-label comparative study in Debre Zeit and Nazareth in East Shoa, Ethiopia.

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Sensory Neuron-Specific GPCR Mrgprs Are Itch Receptors Mediating Chloroquine-Induced Pruritus

December 29, 2009 - 13:12 -- Patrick Sampao
Author(s): 
Qin Liu, Zongxiang Tang, Lenka Surdenikova, Seungil Kim, Kush N. Patel, Andrew Kim, Fei Ru, Yun Guan, Hao-Jui Weng, Yixun Geng, Bradley J. Undem, Marian Kollarik, Zhou-Feng Chen, David J. Anderson, and Xinzhong Dong
Reference: 
Cell, Volume 139, Issue 7, 24 December 2009, Pages 1353-1365

Itch induced by chloroquine (CQ) is a common side effect of this widely used antimalarial drug. Here, we show that Mrgprs, a family of G protein-coupled receptors expressed exclusively in peripheral sensory neurons, function as itch receptors.

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Open Access | Chloroquine reduces arylsulphatase B activity and increases chondroitin 4-sulphate: implications for mechanisms of action and resistance

December 23, 2009 - 21:42 -- Ingeborg van Schayk
Author(s): 
Sumit Bhattacharyya, Kemal Solakyildirim, Zhenqing Zhang, Robert J Linhardt, Joanne K Tobacman
Reference: 
Malaria Journal 2009, 8:303 (17 December 2009)

If chloroquine reduced ASB activity, leading to increased chondroitin-4-sulphation, it was hypothesized that the anti-malarial mechanism of chloroquine might derive, at least in part, from suppression of ASB.

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Synthesis, antimalarial activity and cytotoxicity of 4-aminoquinoline–triazine conjugates

December 22, 2009 - 12:59 -- Patrick Sampao
Author(s): 
Sunny Manohar, Shabana I. Khan, Diwan S. Rawat
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 20, Issue 1, 1 January 2010, Pages 322-325

A series of 4-aminoquinoline–triazine conjugates with different substitution pattern have been synthesized and evaluated for their in vitro antimalarial activity against chloroquine-sensitive and resistant strains of Plasmodium falciparum.

Short communication: Absence of an impact of resistance to chloroquine on consultations for malaria in Niakhar, Senegal (1992–2004)

November 26, 2009 - 06:50 -- Kabogo Ndegwa
Author(s): 
A. Munier, A. Diallo, J.P. Chippaux
Reference: 
Transactions of the Royal Society of Tropical Medicine and Hygiene, Volume 103, Issue 12, December 2009, Pages 1288-1290, doi:10.1016/j.trstmh.2009.03.017

We retrospectively assessed the impact of chloroquine (CQ) resistance in the rural region of Niakhar, Senegal, where resistance to CQ emerged in 1992, from increases in consultations and returns of patients to the health centre following antimalarial treatment.

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In Vitro Activities of Piperaquine, Lumefantrine, and Dihydroartemisinin in Kenyan Plasmodium falciparum Isolates and Polymorphisms in pfcrt and pfmdr1.

November 18, 2009 - 12:47 -- Patrick Sampao
Author(s): 
Leah Mwai, Steven M. Kiara, Abdi Abdirahman, Lewa Pole, Anja Rippert, Abdi Diriye, Pete Bull, Kevin Marsh, Steffen Borrmann, and Alexis Nzila
Reference: 
Antimicrobial Agents and Chemotherapy, December 2009, p. 5069-5073, Vol. 53, No. 12, doi:10.1128/AAC.00638-09

We have analyzed the in vitro chemosensitivity profiles of 115 Kenyan isolates for chloroquine (CQ), piperaquine, lumefantrine (LM), and dihydroartemisinin in association with polymorphisms in pfcrt at codon 76 and pfmdr1 at codon 86, as well as with variations of the copy number of pfmdr1.

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The dynamics of mutations associated with anti-malarial drug resistance in Plasmodium falciparum.

November 18, 2009 - 12:38 -- Kabogo Ndegwa
Author(s): 
Ananias A. Escalante, David L. Smith, Yuseob Kim.
Reference: 
Trends in Parasitology, Volume 25, Issue 12, December 2009, Pages 557-563, doi:10.1016/j.pt.2009.09.008

The evolution of resistance in Plasmodium falciparum against safe and affordable drugs such as chloroquine (CQ) and sulfadoxine-pyrimethamine (SP) is a major global health threat. Investigating the dynamics of resistance against these antimalarial drugs will lead to approaches for addressing the problem of resistance in malarial parasites that are solidly based in evolutionary genetics and population biology. In this article, we discuss current developments in population biology modeling and evolutionary genetics.

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