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Mefloquine (Mefloquine Hydrochloride) - Summary



Mefloquine hydrochloride is an antimalarial agent available as 250 mg tablets of mefloquine hydrochloride (equivalent to 228.0 mg of the free base) for oral administration. Mefloquine hydrochloride is a 4-quinolinemethanol derivative with the specific chemical name of (R*, S*)-(±)-α-2-piperidinyl-2,8-bis (trifluoromethyl)-4-quinolinemethanol hydrochloride. It is a 2-aryl substituted chemical structural analog of quinine. The drug is a white to almost white crystalline compound, slightly soluble in water.

MEFLOQUINE is indicated for the following:

P. falciparum (both chloroquine-susceptible and resistant strains) or by Plasmodium vivax. There are insufficient clinical data to document the effect of mefloquine in malaria caused by P. ovale or P. malariae.

  Note: Patients with acute P. vivax malaria, treated with mefloquine, are at high risk of relapse because mefloquine does not eliminate exoerythrocytic (hepatic phase) parasites. To avoid relapse, after initial treatment of the acute infection with mefloquine, patients should subsequently be treated with an 8-aminoquinoline derivative (e.g., primaquine). P. falciparum and P. vivax malaria infections, including prophylaxis of chloroquine-resistant strains of P. falciparum.

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Published Studies Related to Mefloquine

Efficacy and effectiveness of mefloquine and artesunate combination therapy for uncomplicated Plasmodium falciparum malaria in the Peruvian Amazon. [2011.09]
We evaluated the efficacy and effectiveness of mefloquine (MQ) plus artesunate (AS) to treat patients with uncomplicated malaria in the Peruvian Amazon Basin in April 2005-March 2006. Patients >/= 1 year of age with fever (axillary temperature >/= 37.5 degrees C) or history of fever and Plasmodium falciparum monoinfection were included...

Effect of artesunate and mefloquine in combination on the Fridericia corrected QT intervals in Plasmodium falciparum infected adults from Thailand. [2011.04]
OBJECTIVE: To ascertain whether mefloquine (MQ) produces electrocardiogram (ECG) changes that could be a risk for Torsades de Pointe (TdP), a potentially malignant, ventricular tachyarrhythmia... CONCLUSIONS: In this small group of patients, slowing heart rates due to malaria resolution best explained the observed increases in the QTcF intervals. (c) 2011 Blackwell Publishing Ltd.

Artesunate/mefloquine paediatric formulation vs. artemether/lumefantrine for the treatment of uncomplicated Plasmodium falciparum in Anonkoua koute, Cote d'Ivoire. [2011.03]
OBJECTIVES: To test the hypothesis that Artesunate-mefloquine paediatric (AS+MEF) is as effective as Artemether-lumefantrine (AL) in treating acute uncomplicated malaria in children... CONCLUSION: AS+MEF is as effective as AL, and both combinations were efficacious and safe. (c) 2011 Blackwell Publishing Ltd.

Efficacy and safety of mefloquine, artesunate, mefloquine-artesunate, tribendimidine, and praziquantel in patients with Opisthorchis viverrini: a randomised, exploratory, open-label, phase 2 trial. [2011.02]
BACKGROUND: Praziquantel is the only drug available for treatment of Opisthorchis viverrini, although in-vivo studies point to activity of mefloquine, artesunate, and tribendimidine against this liver fluke. We aimed to assess the efficacy and safety of these drugs compared with that of praziquantel in patients with O viverrini infection... INTERPRETATION: Tribendimidine seems to be at least as efficacious as the drug of choice, praziquantel, for the treatment of O viverrini infections; both drugs were well tolerated. Mefloquine, artesunate, and mefloquine-artesunate did not show an effect. Tribendimidine should be further investigated with large clinical trials. FUNDING: Swiss National Science Foundation, University of Basel. Copyright (c) 2011 Elsevier Ltd. All rights reserved.

A phase III, randomized, non-inferiority trial to assess the efficacy and safety of dihydroartemisinin-piperaquine in comparison with artesunate-mefloquine in patients with uncomplicated Plasmodium falciparum malaria in southern Laos. [2010.12]
We conducted an open, randomized clinical trial of oral dihydroartemisinin-piperaquine (DP) versus artesunate-mefloquine (AM) in 300 patients in Laos with uncomplicated Plasmodium falciparum malaria as part of a multicentre study in Asia. Survival analysis and adjustment for re-infection showed that the 63-day cure rates (95% confidence interval [CI]) were 100% for AM and 99.5% (96.4-99.8%) for DP...

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Clinical Trials Related to Mefloquine

Study to Investigate the Safety, Tolerability and Pharmacokinetics of AD 452 [(+)-Mefloquine] Compared With Racemic Mefloquine [Completed]
Mefloquine is a quinolinemethanol antimalarial that is effective as therapy and prophylaxis for all species of malaria infecting humans, including multi-drug resistant Plasmodium falciparum. The marketed anti-malaria drug consists of two enantiomers of mefloquine. Mefloquine's clinical utility has been impaired by its association with neuropsychiatric side effects. The pharmacological basis of mefloquine's side effects is not known but two of the most reported hypotheses relate to its action on (i) the adenosine receptor and (ii) its effect on the cholinesterase enzyme. For both of these mechanisms, there is a significant stereoselective activity of the two enantiomers. In vitro studies show that the (-) isomer is 50-100 fold more potent towards adenosine receptors compared with the (+) isomer. In addition, (-)-mefloquine has considerably more anti-cholinesterase activity. It has therefore been hypothesised that (+)-mefloquine may have a better central nervous system (CNS) safety profile compared with either the racemate or (-)-mefloquine. This study is a randomized, ascending dose, double-blind, active and placebo-controlled, parallel group study in healthy male and female volunteers designed to investigate this hypothesis and to describe the comparative pharmacokinetics of the racemate and the single enantiomer.

Phase I Factorial Trial of Temozolomide, Memantine, Mefloquine, and Metformin for Post-Radiation Therapy (RT) Glioblastoma Multiforme (GBM) [Recruiting]
The goal of this clinical research study is to find the highest tolerable dose of temozolomide in combination with memantine, mefloquine, and/or metformin that can be given to patients with glioblastoma who have already been given radiation and chemotherapy in combination. The safety of these drug combinations will also be studied. Temozolomide is designed to kill cancer cells by damaging DNA (the genetic material of cells). The damaged DNA may cause tumor cell death. Memantine is designed to block the activity of a protein found on the surface of cells that may control tumor growth and survival. This may stop further spread of tumor cells. Mefloquine is designed to block a protein that helps to clean the waste in the cells and to destabilize the cell membrane. Blocking this protein may cause tumor cell death. Metformin is designed to block a protein in tumor cells that is important in tumor growth and blood vessel development. This may cause cell death or reduce the spread of the disease.

Study to Explore the Effect of Mefloquine in Participants With Progressive Multifocal Leukoencephalopathy (PML) [Terminated]
The primary objective of the study was to explore whether mefloquine can delay or stop progression of progressive multifocal leukoencephalopathy (PML) as measured by JC virus (human polyomavirus or JCV) deoxyribonucleic acid (DNA) levels in cerebrospinal fluid (CSF). The secondary objective of the study was to explore whether mefloquine can delay or stop progression of PML based on neurological deterioration, magnetic resonance imaging (MRI) measures of brain lesion evolution or the formation of new lesions, and mortality.

Efficacy of Artesunate-Mefloquine Combination Therapy in Trat Province, Thailand [Completed]

Assessment of Artesunate/Mefloquine in the Peruvian Amazon [Not yet recruiting]
There is growing evidence of the emergence of P. falciparum resistance to artesunate (a derivative of artemisin) in Southeast Asia. The emergence and spread of resistant strains to artemisinin would represent an alarming threat to the success of the antimalarial combination therapy in the region. The delayed clearance of parasitemia for more than 24 hours has been taken as an early sign of resistance, a phenomenon seen at the Thai-Cambodia border. The purpose of this research study, is to assess the in vitro and in vivo efficacy of combinated artesunate/mefloquine therapy to treatment of uncomplicated Plasmodium falciparum malaria in the Peruvian Amazon through the analysis of the rate of clearance of parasitemia and other important outcomes.

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Page last updated: 2011-12-09

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