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Antimalarial interaction of quinine and quinidine with clarithromycin

Published online by Cambridge University Press:  09 November 2012

SWAROOP KUMAR PANDEY ,
HEMLATA DWIVEDI ,
SARIKA SINGH ,
WASEEM AHMAD SIDDIQUI  and
RENU TRIPATHI
SWAROOP KUMAR PANDEY
Affiliation:
Division of Parasitology, CSIR-CDRI, Lucknow, India-226001 Department of Biochemistry, Jamia Hamdard University, New Delhi, India
HEMLATA DWIVEDI
Affiliation:
Division of Parasitology, CSIR-CDRI, Lucknow, India-226001
SARIKA SINGH
Affiliation:
Division of Toxicology, CSIR-CDRI, Lucknow, India-226001
WASEEM AHMAD SIDDIQUI
Affiliation:
Department of Biochemistry, Jamia Hamdard University, New Delhi, India
RENU TRIPATHI*
Affiliation:
Division of Parasitology, CSIR-CDRI, Lucknow, India-226001
*
*Corresponding author: Division of Parasitology, P.O.Box No. 173, Central Drug Research Institute (CSIR), Chattar Manzil Palace, Lucknow 226001, India. Tel: +91 522 2612411-18 Extn. 4461. Fax: +91 522 2623405/2623938. E-mail: [email protected]
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Summary

Quinine (QN) and quinidine (QND) have been commonly used as effective and affordable antimalarials for over many years. Quinine primarily is used for severe malaria treatment. However, plasmodia resistance to these drugs and poor patient compliance limits their administration to the patients. The declining sensitivity of the parasite to the drugs can thus be dealt with by combining with a suitable partner drug. In the present study QN/QND was assessed in combination with clarithromycin (CLTR), an antibiotic of the macrolide family. In vitro interactions of these drugs with CLTR against Plasmodium falciparum (P. falciparum) have shown a synergistic response with mean sum fractional inhibitory concentrations (ΣFICs) of ⩽1 (0·85 ± 0·11 for QN + CLTR and 0·64 ± 0·09 for QND + CLTR) for all the tested combination ratios. Analysis of this combination of QN/QND with CLTR in mouse model against Plasmodium yoelii nigeriensis multi-drug resistant (P. yoelii nigeriensis MDR) showed that a dose of 200 mg/kg/day for 4 days of QN or QND produces 100% curative effect with 200 mg/kg/day for 7 days and 150 mg/kg/day for 7 days CLTR respectively, while the same dose of individual drugs could produce only up to a maximum 20% cure. It is postulated that CLTR, a CYP3A4 inhibitor, might have caused reduced CYP3A4 activity leading to increased plasma level of the QN/QND to produce enhanced antimalarial activity. Further, parasite apicoplast disruption by CLTR synergies the antimalarial action of QN and QND.

Keywords

malariadrug resistancequininequinidineclarithromycin
Type
Research Article
Information
Parasitology , Volume 140 , Issue 3 , March 2013 , pp. 406 - 413
Copyright
Copyright © Cambridge University Press 2012

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