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Query: UMLS:C0024530 (malaria)
 44,886 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Malaria is largely preventable, so travelers should be taught general protective measures and given appropriate chemoprophylaxis before they leave on their trip. Chloroquine phosphate (Aralen) is still the drug of choice in locations where malaria remains chloroquine-sensitive. However, chloroquine-resistant areas infested with Plasmodium falciparum are becoming more numerous. In such areas, mefloquine hydrochloride (Lariam), doxycycline, or proguanil (Paludrine) (obtainable outside the United States) may be used. A single dose of pyrimethamine-sulfadoxine (Fansidar) may be used to treat presumptive malarial infection if medical care is not immediately available. For prevention of relapse of Plasmodium vivax and Plasmodium ovale infection, primaquine phosphate is recommended for the final 2 weeks of chemoprophylaxis on return from a malarious area.
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PMID:Prophylaxis for malaria. Helping world travelers come home healthy. 151 52

The A.A. weight present criteria of choice in order to set right a correct and effective anti-malarial prophylaxis. In the last ten years, a progressive increase of tropical diseases has been observed. This is due to the considerable growth of intercontinental traffic and of the number of persons moving to or from tropical areas where such diseases are endemic. Among these, malaria represent the most alarming problem, both because of the incidence cases and the difficulties related to the efficacy of pharmacological remedies for the chemoprophylaxis. In particular, three are now various pharmacological possibilities for malarial prophylaxis. Undoubtedly Chloroquine is the most efficacious even if there are many Plasmodium falciparum species resistant to Chloroquine and to other available medicines (multi-resistance). Most authors recommend to associate Chloroquine to others pharmacological substances to avoid pharmaco-resistance phenomena. Among the most famous pharmacological products used elsewhere are Fansidar, Maloprim, Paludrine and Lapudrine, not all are available in Italy. In China, for the therapy of resistant forms of malaria, the Qinghaosu a "schizont-killer" acting on multiresistant plasmodium falciparum has been utilizing for years. The Qinghaosu is not responsible for the crossing-reactions with other anti-malarial medicines. Various substances with Ca-antagonist action (Verapamil) are being experimented. It is supposed that Verapamil associated with Chloroquine can stop the flow of chlorine from plasmodium cells. The same mechanism is expected to be valid also for Desipramine, an experimental tricyclic anti-depressive when associated to Chloroquine. To the people moving to endemic areas, the A.A., at the end, suggest a series of practical norms to prevent infection and, therefore, the incidence of imported cases, still increasing at the moment, due to the absence of efficacious vaccine.
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PMID:[A current problem: the prevention of malaria]. 248 2

Pharmacokinetic parameters for cycloguanil and chlorcycloguanil, the active metabolites of proguanil (Paludrine] and chlorproguanil (Lapudrine) have been measured in a bioassay which assesses the in-vitro growth inhibition of a cycloguanil- and chlorcycloguanil-sensitive strain of Plasmodium falciparum produced by dilutions of plasma collected after oral administration of the pro-drugs. A single compartment model is applicable for cycloguanil with mean rate constants of elimination of 0.0624 h-1 and availability of 0.2398 h-1. The elimination profile for chlorcycloguanil indicates partition of drug into more than one compartment. In 2 of 10 subjects dosed with proguanil and 1 of 11 subjects dosed with chlorproguanil, the active metabolite levels were significantly lower than the mean for the other subjects. Abnormally low cycloguanil or chlorcycloguanil plasma levels may be of importance in relation to effective prophylaxis against malaria.
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PMID:A preliminary pharmacokinetic study of the antimalarial drugs, proguanil and chlorproguanil. 288 88

In different countries opinions differ as to which chemotherapeutic methods should be used for malaria prophylaxis. It has long been the opinion of the Nordic countries, that WHO should give an official recommendation and the result is reflected now in the publication "Vaccination certificate requirements and health advice for internation travel." The malaria-endemic regions of the world are divided into 3 categories: regions without risk and no need for prophylaxis, low risk regions (A) with predominantly vivax inflections, risk regions (B) with predominantly chloroquine sensitive P. falciparum, and high risk regions (C) with often both chloroquine as well as sulfa/pyrimethamine resistance. Chloroquine is a sufficient prophylaxis for A-regions. For B-regions proguanil should be added and for C-regions only mefloquine is given. Proguanil was reintroduced basically because of Swedish research results in Liberia. An American initiative recommends for all regions, A-C, chemorprophylaxis as an alternative. However, a precondition is an observant traveller and clear instructions for self-treatment. Travellers who fall ill in a B-region should choose between Fansidar, mefloquine and quinine for self-treatment. Mefloquine has the least serious side effects, whereas quinine is therapeutically more safe. Fansidar very seldom gives any side effects. For C-regions only mefloquine is recommended for self-treatment. Nordic colleagues have recommended to double prophylaxis (chloroquine + Paludrine) treatment for the entire African tropical region. For short-time travellers to Kenya, Tanzania and Uganda, 6 tablets Lariam should be added. Only chloroquine is recommended for India and the Amazon region of South America. No chemoprophylaxis can guarantee full protection. Insect protection is therefore more important than ever. Malaria decreases the unspecific immune defense system. Surprisingly, repeated tests have shown that the AIDS frequency is not higher in patients with chronic malaria than for persons without plasmodia in the blood. In WHO's new little yellow booklet, a page concerning prophylaxis against AIDS appears. Equipment that is not new should be steamed or cooked for a least 20 minutes or treated with chemical disinfectants for at least 30 minutes. These measures should be enough to prevent HIV-infection.
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PMID:[Malaria and HIV prevention in WHO's "little gem"]. 338 44

In vitro studies have indicated that the antifolates pyrimethamine [4, 6] and cycloguanil (the active metabolite of proguanil) suppress the proliferation of stimulated human lymphocytes; proguanil has no effect [2]. During the early growth phase of the cells, 14C-thymidine (14C-TdR) incorporation is increased by pyrimethamine and cycloguanil, reflecting blockage of endogenous TdR synthesis [3]. Proguanil (Paludrine) is increasingly being used for malaria prophylaxis. It is considered the most innocuous of the antimalarials currently employed. Since nothing is known about the effect of oral proguanil on human lymphocytes, the present study was undertaken. Little information is available about the serum levels of proguanil and cycloguanil following ingestion of prophylactic doses [8]. Therefore, the serum concentrations of proguanil and cycloguanil were estimated, to allow comparison with previous in vitro studies [2].
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PMID:Effect of oral proguanil on human lymphocyte proliferation. 370 55

Malaria has had an enormous impact on human history, not least in times of war. The disease has been treatable by a natural remedy, quinine, since the 17th century, but the production of synthetic antimalarial agents was first achieved in Germany in the wake of the Great War of 1914-1918, in which malaria had caused immense problems. In the 1920s research workers in the Bayer laboratories of the IG Farbenindustrie consortium developed the 8-aminoquinoline plasmoquine (the forerunner of primaquine). They went on to develop the acridine dye, atebrin (mepacrine) and the 4-aminoquinolines, Resochin (developed at the end of the Second World War in America as chloroquine) and Sontochin. British attempts to match the advances achieved by the Germans were at first unproductive, partly because collaboration between academic and industrial organizations in the UK was beset by concerns over patent rights. However, with the outbreak of World War II, when supplies of antimalarials were scarce, ICI succeeded in the large-scale production of mepacrine (essential to prosecution of the war, particularly in the Far East) and also initiated a programme of collaborative research that eventually led to the discovery of proguanil (Paludrine); this, in its turn led to the diaminopyrimidine, pyrimethamine. A massive cooperative screening programme in the USA during World War II eventually bore fruit in the realization of the therapeutic potential of chloroquine, and in the later development of amodiaquine and primaquine. Some of this work also influenced the subsequent discovery of mefloquine and halofantrine at the Walter Reed Army Institute of Research.
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PMID:Conflicts of interest: the genesis of synthetic antimalarial agents in peace and war. 862 69

In France, 4,000 imported malaria cases are reported each year (7,000 to 8,000 estimated). Chemoprophylaxis is essential for prevention in travelers. When malaria is susceptible to chloroquine, this drug (Nivaquine) has to be used. It is given daily in France (1.5 mg/kg per day), from departure to four weeks after return. When low levels of chloroquino-resistance are reported, French authorities recommend the use of chloroquine + proguanil (Savarine) if the body weight is >50 kg or Nivaquine) + Paludrine), if <50 kg), or atovaquone + proguanil (Malarone). Nivaquine) (1.5 mg/kg per day) and Paludrine) (3 mg/kg per day) have to be pursued for one month after return, although Malarone) (1 pediatric tablet/10 kg per day, in children >10 kg weight) may be disrupted after one single week. Adverse events are rarer with atovaquone + proguanil, than with chloroquine + proguanil. When chloroquino-resistance is high, Malarone) or mefloquine (Lariam) are used. Weekly drug regimen is recommended with mefloquine (5 mg/kg per weight) for the travel duration and four weeks after return and the drug tolerance is good in pediatric prophylaxis. Doxycycline is used under conditions in children >8 years of age. New drugs as for tafenoquine, an amino-8 quinoleine, might enhance patients compliance if given monthly.
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PMID:[Malaria chemoprophylaxis in traveling children]. 1565 56