Mefloquine hydrochloride is an antimalarial agent available as 250 mg tablets of mefloquine hydrochloride (equivalent to 228 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- piperidinyI-2,8-bis(trifluoromethyl)-4-quinolinemethanoI 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.
Treatment of Acute Malaria Infections
Mefloquine Hydrochloride Tablets are indicated for the treatment of mild to moderate acute malaria caused by mefloquine-susceptible strains of 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.
Prevention of Malaria
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 (eg, primaquine).
Mefloquine Hydrochloride Tablets are indicated for the prophylaxis of P. falciparum and P. vivax malaria infections, including prophylaxis of chloroquine-resistant strains of P. falciparum.
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...
Clinical Trials Related to Mefloquine
Prevention of Pregnancy-associated Malaria in HIV-infected Women: Cotrimoxazole Prophylaxis Versus Mefloquine [Recruiting]
The purpose of this study is to evaluate the efficacy of cotrimoxazole prophylaxis in
prevention of malaria during pregnancy in HIV-infected women, compared to intermittent
preventive treatment with mefloquine.
Activity of Mefloquine Against Urinary Schistosomiasis [Not yet recruiting]
Urinary schistosomiasis is a debilitating disease in Central Africa and pregnant women are
frequently suffering from this condition. Mefloquine is currently investigated as preventive
treatment against malaria in pregnancy and mefloquine is also known to exert activity
against schistosomiasis. The investigators want to test the hypothesis whether mefloquine
may active against urinary schistosomiasis when used as preventive treatment against malaria
Pharmacokinetics of Mefloquine-Artesunate in Pregnant Women With Uncomplicated Plasmodium Falciparum Infection [Not yet recruiting]
Artemisinin-based combination therapies (ACTs) are now the treatment of choice for malaria
in non-pregnant individuals living in areas with established chloroquine resistance; they
have been shown to be both safe and highly efficacious. There is rapidly increasing
experience with artemisinin derivatives in the 2nd and 3rd trimesters of pregnancy, with
over 1,000 well documented cases with no reported serious adverse effects to mother or fetus
(WHO Malaria Treatment Guidelines, 2006). Many countries in Latin America have abandoned the
previous 1st line regimen of Quinine-Clindamycin for treatment of malaria in pregnancy, a
complex and poorly tolerated regimen with low adherence, in favor of ACTs, despite limited
safety and pharmacokinetic data on the use of these compounds in pregnant women. Lack of
pharmacokinetic data may lead to underdosing of pregnant women, with subsequent reduced
efficacy and increased potential for development of resistance.
One ACT regimen, Artesunate-Mefloquine, has been developed as a fixed-dose combination
(Farmanguinhos Artesunato + Mefloquina), as part of an international collaborative research
effort led by Drugs for Neglected Diseases Initiative (DNDi), and manufactured by
Farmanguinhos, laboratory of the Brazilian Ministry of Health. Initial clinical trials
suggest that it is very well tolerated and efficacious in both pregnant and non-pregnant
individuals. The convenient dosing afforded by a fixed drug combination make this a very
promising candidate for treatment of pregnant women with malaria. Preliminary
pharmacokinetic data from mefloquine monotherapy and prophylaxis suggest that the peak
concentration of mefloquine is lowered in pregnant women. Prior to wide-spread adoption of
the Artesunate-Mefloquine combination, further studies on safety, efficacy, and dose
optimization are imperative. We propose to compare the pharmacokinetics of the fixed
combination of mefloquine-artesunate (MA) for treatment of P. falciparum in 28 pregnant women
in the second and third trimesters to the pharmacokinetics of this regimen in 28 matched
non-pregnant P. falciparum infected women. This will allow us to determine whether the
standard adult dose is sufficient for pregnant women.
Immunization With Plasmodium Falciparum Sporozoites Under Chloroquine Versus Mefloquine Prophylaxis [Not yet recruiting]
Malaria is one of the major infectious diseases in the world with a tremendous impact on the
quality of life, significantly contributing to the ongoing poverty in endemic countries. It
causes 800. 000 deaths per year, the majority of which are children under the age of five.
The malaria parasite enters the human body through the skin, by the bite of an infected
mosquito. Subsequently, it invades the liver and develops and multiplies inside the
hepatocytes. After a week, the hepatocytes burst open and the parasites are released in the
blood stream, causing the clinical phase of the disease.
As a unique opportunity to study malaria immunology and efficacy of immunisation strategies,
a protocol has been developed in the past to conduct controlled human malaria infections
(CHMIs). CHMIs generally involve small groups of malaria-naïve volunteers infected via the
bites of P. falciparum infected laboratory-reared Anopheline mosquitoes. Although
potentially serious or even lethal, P. falciparum malaria can be radically cured at the
earliest stages of blood infection when risks of complications are virtually absent.
The investigators have shown previously that healthy human volunteers can be protected from
a malaria mosquito (sporozoite) challenge by immunization with sporozoites (by mosquito
bites) under chloroquine prophylaxis (CPS immunization). Interestingly, sterile protection
in 100% of the human CPS immunized volunteers was achieved by a relatively miniscule dose,
i. e. a total of 45 infectious mosquito bites, strikingly 20-fold more potent than the 1000
bites needed in a model using irradiated mosquitoes. One possible explanation for this
efficient induction of protective immunity, is the immune modulating effect of chloroquine.
The investigators aim to assess this possible immune modulating effect in CPS immunization
by comparing immunization with P. falciparum sporozoites under chloroquine with immunization
under mefloquine prophylaxis, which has the same antimalarial effect, but not the immune
modulating effects known from chloroquine.
Efficacy of Artemisinin Combination Therapies for the Treatment of Uncomplicated P. Falciparum in Pregnancy in Brazil [Recruiting]
Data on the burden of MIP in low transmission areas, such as Latin America, are very
limited; there is even less information on the efficacy of case management of MiP. The
treatment recommendations for MiP in Latin American countries have been changing rapidly in
recent months; currently, either artemether-lumefantrine (AL) or mefloquine-artesunate (MA)
is the first line treatment for P. falciparum (depending on country); however, no data
exists on the efficacy of these drugs for the treatment of malaria in pregnancy in Latin
America to support their use.
We propose a multi-center 2-arm open-label randomized Phase 4 clinical trial to assess
safety and efficacy of the present therapies, AL and MA. We hypothesize that the drugs will
both be efficacious for use in pregnant women in Brazil.
Page last updated: 2011-12-09