A sensitive and selective gas-liquid chromatographic method for the determination of plasma levels of mefloquine in human and dog plasma is described. The drug and internal standard were extracted from plasma at pH 9.0 into isopropyl acetate. After evaporation of the solvent, the residue was taken up in toluene and derivatised with heptafluorobutyrylimidazole. The derivative was quantified by gas-liquid chromatography on a 3% GC GE-SE30 column with electron-capture detection. The limit of detection for mefloquine in plasma was 10 ng/ml. The mean overall recovery from plasma was 102.7 +/- 3.3%. The method was shown to be specific for mefloquine without any interference from endogenous compounds in plasma or from the drugs pyrimethamine and sulfadoxine (compounds often administered in combination with mefloquine). The assay described was successfully applied to the determination of plasma levels of mefloquine in man and dog following oral and intravenous administration, respectively.
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http://dx.doi.org/10.1016/0378-4347(85)80006-2 | DOI Listing |
Microorganisms
December 2024
Agents Infectieux, Résistance et Chimiothérapie (AGIR), UR 4294, Université de Picardie Jules Verne, 1 rue des Louvels, 80037 Amiens, France.
Currently, artemisinin-based combination therapy is recommended as first-line treatment of uncomplicated malaria. Arylamino alcohols (AAAs) such as mefloquine (MQ) are the preferred partner drugs due to their longer half-life, reliable absorption and strong antimalarial activity. However, the mode of action of MQ remains poorly understood and its neurotoxicity limits its use.
View Article and Find Full Text PDFPLoS One
December 2024
Laboratory of Biomolecular Research, Paul Scherrer Institute, Villigen, Switzerland.
Gap junction intercellular communication (GJIC) between two adjacent cells involves direct exchange of cytosolic ions and small molecules via connexin gap junction channels (GJCs). Connexin GJCs have emerged as drug targets, with small molecule connexin inhibitors considered a viable therapeutic strategy in several diseases. The molecular mechanisms of GJC inhibition by known small molecule connexin inhibitors remain unknown, preventing the development of more potent and connexin-specific therapeutics.
View Article and Find Full Text PDFCureus
November 2024
Department of Pediatrics, Teikyo University School of Medicine, Tokyo, JPN.
Background Alveolar echinococcosis (AE) is a fatal zoonotic disease distributed mainly in the Northern Hemisphere. At present, its curative treatment relies on surgery, and the development of effective drugs is needed. We previously demonstrated the anti-echinococcal effect of atovaquone (ATV) as a mitochondrial complex III inhibitor in both in vitro and in vivo experiments.
View Article and Find Full Text PDFFront Cell Infect Microbiol
December 2024
School of Public Health, Gansu University of Chinese Medicine, Lanzhou, Gansu, China.
Antimicrobial resistance is among the greatest threats to public health globally, and drug repurposing strategies may be advantageous to addressing this problem. Mefloquine, a drug traditionally used to treat malaria, has emerged as a promising antibiotic adjuvant, due to its ability to enhance the effectiveness of conventional antibiotics against resistant bacterial strains. In this paper, we first outline the enhancement properties of mefloquine and its mechanisms of action as an adjuvant antibiotic against multidrug-resistant bacteria.
View Article and Find Full Text PDFProc Natl Acad Sci U S A
December 2024
Centre for Tropical Medicine and Global Health, Nuffield Department of Medicine, University of Oxford, Oxford OX3 7LF, United Kingdom.
parasites can lie dormant in the liver as hypnozoites, activating weeks to months after sporozoite inoculation to cause relapsing malarial illness. It is not known what biological processes govern hypnozoite activation. We use longitudinal data from the most detailed cohort study ever conducted in an area where both and were endemic to fit a simple within-host mathematical model of hypnozoite activation.
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