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 23,468 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The pharmacokinetics of the prophylactic dose of mefloquine (Lariam: 500 mg every 4 weeks, with a loading dose of 750 mg on the first week) was studied in six healthy Thai male volunteers. Mefloquine was well tolerated during the study period of 16 weeks. The only side-effects found were nausea and diarrhea in 2 volunteers after the first dose of mefloquine. The mean minimum concentration of mefloquine at steady state ranged from 290 to 460 ng/ml. The maximum concentration on week 16 after the last dose was 1558 +/- 48 ng/ml at the mean time of 38 +/- 19 hours. The other pharmacokinetic parameters obtained were: absorption half life = 6.6 +/- 3.0 hours; distribution = 5.1 +/- 3.1 days; terminal half life = 12.9 +/- 2.2 days; apparent volume of distribution = 10.5 +/- 2.3 l/kg; area under the concentration-time curve = 26.9 +/- 2.2 mg/dl. Although this prophylaxis regimen is ideal when considering the compliance, the minimum concentration obtained was much too low for optimum therapeutic concentration. We therefore suggest that weekly prophylaxis schedule should be a better regimen as the difference between minimum and maximum mefloquine concentration would be smaller.
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PMID:Pharmacokinetics of prophylactic mefloquine. 182 Jun 37

The pharmacokinetics of mefloquine at the therapeutic dose of 750 mg single orally were compared between cured and recrudescent patients with acute uncomplicated falciparum malaria. Mefloquine was well-tolerated during the study. The side-effects found were nausea, vomiting and diarrhea. Five patients showed R-I and two showed R-II types of response. All recrudescent patients came from the eastern border of Thailand. The time taken to clear the parasites (PCT) was significantly longer in patients with recrudescence (99.6 +/- 36.9 and 63.0 +/- 8.9 hours); however, there was no difference regarding fever clearance time (FCT: 39.0 +/- 16.1 and 31.0 +/- 21.3 hours). The maximum concentration (Cmax) and the concentration on the first and second days in cured patients were significantly higher than those of treatment failure patients. Other pharmacokinetic parameters appeared to be similar in both groups. The present study indicates the existence of mefloquine-resistant falciparum malaria in the eastern border of Thailand. Inadequate mefloquine concentration may play an important role in this aspect. In addition, this study also suggests that Cmax or the concentrations on the first or second day of treatment may be used as guidelines to predict the outcome of treatment.
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PMID:Pharmacokinetics of mefloquine in treatment failure. 182 Jun 38

The therapeutic effects and side effects of mefloquine in falciparum malaria were investigated in an open prospective trial involving 20 patients. None of them had a history of neurologic or psychiatric disorders. Mefloquine was given in a total dose of 1500 mg base. The cure rate was 100%, fever and parasitemia subsided within 3 days. Side effects were vomitus and nausea in 25% of the patients. No neurological or psychiatric disorders were observed. Mefloquine was shown to be a safe therapeutic agent in the dosage used. However, regular follow-up examinations should be done in short intervals because of the possibility of late neuropsychiatric side effects; the patients and their relatives should be informed about this fact.
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PMID:[Clinical experiences with mefloquine in tropical malaria--a prospective study]. 191 70

Halofantrine (WR 171,669) hydrochloride was administered orally to 82 patients infected with Plasmodium falciparum malaria on the Thai-Kampuchean border between June 1982 and December 1983 in a randomized double-blind treatment trial which compared the efficacy of halofantrine with that of mefloquine. Halofantrine was curative with oral treatment on a single day in 65% of patients (13/20) who received 1000 mg followed 6 hours later by an additional 500 mg, and in 88% of patients (53/60) who received 500 mg every 6 hours for 3 doses. Mefloquine was curative in 88% of patients (22/25) given a single oral dose of 1000 mg and in 97% of patients (38/39) given a single oral dose of 1500 mg. The difference in cure rates between the 3-dose halofantrine regimen and either of the mefloquine regimens was not significant. The mean parasite clearance time for all regimens ranged from 75 to 84 hours. The mean fever clearance time for all four treatment groups was in the range 50-60 hours, with no significant differences between groups. Post-dosing side-effects in patients treated with halofantrine consisted of nausea, vomiting, abdominal pain and diarrhoea and were not significantly different from those treated with mefloquine. Halofantrine therefore appeared to be of comparable efficacy to mefloquine in the treatment of multidrug-resistant P. falciparum malaria.
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PMID:Malaria: treatment efficacy of halofantrine (WR 171,669) in initial field trials in Thailand. 329 28

A double-blind, randomized, dose-finding, phase II mefloquine trial was carried out in 147 adult male patients suffering from acute, uncomplicated, falciparum malaria and admitted to the Hospital for Tropical Diseases, Bangkok, between January 1980 and April 1981. Mefloquine was administered as a single oral dose of 500, 750, or 1000 mg (base) in the form of the hydrochloride. The clinical and parasitological responses were satisfactory with all three dosage regimens. The cure rates for the 1000-, 750-, and 500-mg doses were 100%, 92.5%, and 95% respectively, over an observation period of 63 days.The side-effects, which were transient and generally mild, included nausea, vomiting, and diarrhoea. No significant changes were noted in haematological or biochemical parameters in any of the three groups. Sinus bradycardia, which started 4-7 days after drug administration and lasted for a few weeks, was seen in 10 patients. It was symptomless and needed no treatment.Acute brain syndrome was observed in one patient on day 21 after receiving a 1000-mg dose of mefloquine.Mefloquine was well tolerated in one case of acute renal failure, in 10 cases of moderately severe malaria with jaundice, in 13 cases with glucose-6-phosphate dehydrogenase deficiency, and in one case of thalassaemia.Mefloquine showed no effect on either gametocytes of Plasmodium falciparum or tissue forms of P. vivax.Mefloquine hydrochloride was found to be an effective drug for the treatment of falciparum malaria and tended to produce a more rapid clinical and parasitological response at the highest tested dose of 1000 mg (base).
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PMID:A phase II clinical trial of mefloquine in patients with chloroquine-resistant falciparum malaria in Thailand. 634 13

Mefloquine was compared with sulfadoxine-pyrimethamine for safety and efficacy in a randomized, double-blind clinical trial in adult males from a malaria-endemic area of Brazil. A total of 99 oligosymptomatic and symptomatic volunteers with Plasmodium falciparum parasitaemia took part in the trial; 49 were given 1000 mg of mefloquine and the remainder received 1500 mg of sulfadoxine plus 75 mg of pyrimethamine, in a single oral dose.Mefloquine was 100% successful in clearing parasitaemia within 7 days; there were no recrudescences. Sulfadoxine-pyrimethamine was less successful; 35 cases showed an S-type response, 8 an RI response, 3 an RII, and 2 an RIII response. The side-effects of mefloquine were mild and transient and included headache, nausea, vomiting, dizziness, and diarrhoea. A satisfactory weight gain and rise in haemoglobin level were seen in both groups.
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PMID:A phase II clinical trial of mefloquine in Brazilian male subjects. 636 Apr 1

Mefloquine is an orally administered blood schizontocide. Initial dose-finding and comparative studies performed between 1977 and 1989 demonstrated efficacy of mefloquine as prophylaxis in nonimmune individuals and in the suppression and treatment of malaria in adults and children caused by multidrug-resistant Plasmodium falciparum. It was also effective against P. vivax infection, while data concerning the treatment of P. ovale and P. malariae infections were limited. In an attempt to delay the emergence of resistance to this promising antimalarial agent, mefloquine was combined with sulfadoxine and pyrimethamine. Although initial clinical trials indicated that this regimen was effective in preventing and treating falciparum malaria, recent treatment failures, the potential for severe dermatological reactions and lack of therapeutic advantage over mefloquine alone has prompted the World Health Organization to recommended that the combination be no longer used for treatment or prophylaxis of malaria. Mefloquine is generally well tolerated in both adults and children, with nausea, vomiting, diarrhoea, headache, dizziness, rash, pruritus and abdominal pain being the most common adverse effects, although it is difficult to distinguish between disease- and treatment-related events. The incidence of these adverse effects is similar to or lower than those observed with other antimalarial agents. Cardiovascular changes, such as bradycardia, occasionally occur. The most notable adverse effects associated with mefloquine are neuropsychiatric disturbances; precipitation of such events should be closely monitored and requires termination of prophylaxis or therapy. The eventual emergence of resistance to mefloquine, as with many other antimalarial agents, was inevitable. Mefloquine resistance is established in certain areas of Thailand and may be becoming a growing problem in other regions of the world. In order to preserve the efficacy of mefloquine in non-resistant areas, this useful agent should be used with care and only prescribed for prophylaxis in travellers and treatment in areas of multidrug-resistant plasmodia. Future options to combat mefloquine resistance may include the combination of mefloquine with other antimalarial agents such as qinghaosu derivatives. Thus, with cautious use and possible combination with other agents, mefloquine is likely to remain an important treatment option for falciparum malaria, a widespread parasitic disease for which an increasing number of drugs have proved inadequate.
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PMID:Mefloquine. A review of its antimalarial activity, pharmacokinetic properties and therapeutic efficacy. 768 11

Plasmodium falciparum in south-east Asia is highly resistant to chloroquine and sulfadoxine-pyrimethamine. Mefloquine used to be the chemosuppressant drug of choice in areas with chloroquine resistance. However, sensitivity to this drug has recently decreased in Thailand, Cambodia and Myanmar, and there is no suitable single alternative drug. We therefore investigated possible alternative combination therapies for multidrug resistant falciparum malaria. 120 male Thai patients at Makarm Malaria Clinic, Chantaburi, in eastern Thailand were allocated at random to receive either oral artemether (group A) or artesunate (group B) at a single dose of 300 mg on day 1, both followed by mefloquine, 750 and 500 mg at 24 and 30 h, respectively. Follow-up was on days 1, 2, 7, 14, 21, 28, 35 and 42. Patients in both groups had a rapid initial response to treatment; in most cases parasitaemia was cleared within 24 h, and fever was cleared within 24 h in 62% and 76.7% of the patients in groups A and B, respectively. 58 patients in group A and 57 in group B completed follow-up and cure rates were 98% and 97%, respectively. Reinfection could not be excluded for the 3 patients with recrudescences; all were cured with a repeated course of treatment. No serious adverse effect was observed in either group, only mild and transient nausea, vomiting and loss of appetite, with no significant difference between the 2 groups. These results suggest that a single oral dose of 300 mg of either artemether or artesunate followed by 1250 mg of mefloquine in 2 divided doses is effective against multiple drug resistant falciparum malaria. Either regimen can be considered as a suitable 'stand-by' in endemic areas of multiple drug resistant falciparum malaria.
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PMID:Artemether or artesunate followed by mefloquine as a possible treatment for multidrug resistant falciparum malaria. 888 93

Poor quality medical care in some countries is an important concern, because of a lack of sterile equipment and lack of screening of blood products The safest time for travel is 18-24 weeks--after the risk of miscarriage and unpleasant nausea, but before problems such as premature labour Women with a previous history of miscarriage or ectopic pregnancy should be advised against travelling to countries where medical care is poor After 28 weeks a doctor's letter may be required before an airline will allow a pregnant woman to fly On board an aircraft, pregnant women should walk around the cabin at least once an hour to minimise the risk of deep vein thrombosis Malaria in pregnancy can be severe for both mother and fetus: chloroquine and proguanil have a long safety record Mefloquine is contraindicated in the first trimester and doxycycline should be avoided during pregnancy.
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PMID:Pregnancy and travel. 945 Apr 66

Mefloquine has been licensed and registered in Japan for chemoprophylaxis against malaria since 2001. Guidelines for the prevention of malaria for Japanese overseas travelers were published by a group of malaria specialists under the auspices of the Japanese Society of Tropical Medicine and the Ministry of Health, Labor and Welfare, but not until March 2005. We implemented these guidelines in our clinic at the International Medical Center of Japan in Tokyo and, to better understand whether these guidelines are optimally useful, we conducted a study of Japanese travelers who visited our clinic seeking pertinent information and prophylaxis against malaria. The study group comprised 52 individuals who visited our clinic during the period October 2004 through June 2005 prior to travel abroad. On the basis of the above-mentioned guidelines, mefloquine was given to 27 of these individuals, 22 of whom were judged to need regular chemoprophylaxis. Mefloquine was not recommended to the other 25 individuals because their stays abroad would have been too long to avoid possible side effects or too short for symptoms to appear. In fact, some were traveling to malaria-free areas. Of the 27 individuals given mefloquine, 7 (26%) reported side effects, such as headache, vertigo, and nausea, 17 (63%) reported no side-effects, and the other 3 (11%) were unable to be followed. The diversity of destinations and accompanying malaria risks makes it very difficult for us to administer chemoprophylaxis to overseas travelers appropriately. The guidelines proved to be somewhat useful, but further experience in malaria chemoprophylaxis is needed for physicians to provide reliable pre-travel consultation.
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PMID:Chemoprophylaxis according to the guidelines on malaria prevention for Japanese overseas travelers. 1754 42


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