Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0024530 (malaria)
44,886 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The clinical and parasitological response of adult male patients to mefloquine and to a combination of quinine and sulfadoxine-pyrimethamine during the treatment of falciparum malaria was compared. These patients were from an area in Brazil where Plasmodium falciparum is showing increasing resistance to quinine and to sulfadoxine-pyrimethamine. The drugs were administered to 100 patients (50 in each group), based on a randomized study design.The rates of clearance of parasitaemia and fever were similar in both groups. However, the parasitological cure rate ("S" response) was 100% for mefloquine but only 92% for quinine plus sulfadoxine-pyrimethamine. Tolerance was good in both groups. The main side-effects (nausea, vomiting, abdominal pain, and dizziness) were mild, transient and required no specific treatment. Nausea and vomiting were more frequent in patients who received quinine plus sulfadoxine-pyrimethamine, while abdominal pain and loose stools or mild diarrhoea were more frequent in the mefloquine group. Tinnitus and hearing difficulty were observed following the administration of quinine plus sulfadoxine-pyrimethamine, but not after mefloquine treatment. Laboratory tests of various haematological and biochemical parameters were not adversely affected in either group after drug administration.It can be concluded that mefloquine, given in a single oral dose of 1000 mg, is highly effective, well tolerated, and safe for the treatment of falciparum malaria in adult males in Brazil.
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PMID:An open, randomized, phase III clinical trial of mefloquine and of quinine plus sulfadoxine-pyrimethamine in the treatment of symptomatic falciparum malaria in Brazil. 389 97

A double-blind, randomized phase I clinical trial was carried out to compare Fansimef (a fixed-dose combination of mefloquine, sulfadoxine, and pyrimethamine) with sulfadoxine and pyrimethamine (Fansidar) for safety and tolerance. Twenty adult male Brazilian subjects from malaria endemic areas were studied for a period of 66 days, which included 2 days before and 63 days after drug administration.Both drugs were well tolerated and safe, as seen from the absence of drug-induced changes in the various laboratory, haematological, and biochemical parameters measured. Fansimef produced a complete clearance of parasites on day 3, with an "S" type response in one subject who had blood smears which were positive for Plasmodium falciparum on day 0. Two subjects in the sufladoxine-pyrimethamine group also had P. falciparum infections on day 0; the parasitaemia was cleared on day 2 in one of these subjects and on day 3 in the other, but an early RI response (recrudescence) was observed in the former case. Relapses due to P. vivax occurred in both groups.Side-effects due to Fansimef included mild dizziness, nausea, and vomiting. The incidence of dizziness and nausea was similar in the sulfadoxine-pyrimethamine group. In both groups, these side-effects were mild, short-lived and did not require specific treatment. Thus, Fansimef in an oral dose of three tablets (total of 750 mg mefloquine (base) plus 1500 mg sulfadoxine plus 75 mg pyrimethamine) was found to be well tolerated and safe.
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PMID:A phase I clinical trial of Fansimef (mefloquine plus sulfadoxine-pyrimethamine) in Brazilian male subjects. 389 98

Halofantrine is a 9-phenanthrene-methanol effective against multiresistant strains of Plasmodium falciparum. It is extremely effective and well-tolerated in treating cases of malaria imported into France. 1,500 mg in 3 doses at 8 hour intervals produced 100% cure rate in semi-immune patients. This dosage could be repeated after 14 days in order to obtain the same cure rate in non-immune patients. Side-effects are minor and include epigastric pain, nausea and one case of skin rash.
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PMID:[Treatment with halofantrine of Plasmodium falciparum malaria imported into France]. 391 50

The antimalarials, chloroquine, hydroxychloroquine, and quinacrine, are used primarily for malaria; but they can be beneficial for cutaneous lupus erythematosus (LE), polymorphous light eruption, solar urticaria, and porphyria cutanea tarda. Antimalarials bind to deoxyribonucleic acid (DNA) which prevents DNA and ribonucleic acid (RNA) polymerase reactions and DNA heat inactivation; and they inhibit the LE cell phenomenon, antinuclear antibody reactions, and suppress lymphocyte transformation. By competing with calcium ion, they stabilize membranes and have an anesthetic effect. Their anti-inflammatory potential is due to their inhibition of hydrolytic enzymes, stabilization of lysosomes, interference with prostaglandin synthesis, blocking of chemotaxis, and antagonism of histamine responses. The antimalarials have no sunscreening properties. The most common toxic effects are cutaneous pigmentation, nausea, vomiting, diarrhea, mild ileus, and cycloplegia. There has been a reluctance to use chloroquine and hydroxychloroquine because of the possibility of retinopathy. However, if the "safe" daily dose limit of chloroquine, 2 mg per pound of body weight, and of hydroxychloroquine, 3.5 mg per pound of body weight, is followed, the chance of retinopathy is slight. Quinacrine does not cause retinopathy, but it has more cutaneous side effects than the other two agents.
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PMID:Antimalarials. 616 44

Different doses of mefloquine (20 and 30 mg/kg of body weight in children, and 750 and 1000 mg in adults) were tested in controlled clinical trials in 89 children and 60 adults who were semi-immune carriers of Plasmodium falciparum. There was no significant difference in the efficacy of the two doses, either in the children or in the adults. An RI-type resistance was found in 1 adult, when recrudescence occurred on day 7, and in 4 children, who showed recrudescence on day 14. In all 5 patients, spontaneous disappearance of parasites was observed at further parasitological checks, thus indicating that mefloquine has a prolonged action. One patient who vomited after taking the drug was successfully retreated with mefloquine on day 14.Nausea, giddiness, and vomiting are the three symptoms most frequently attributed to mefloquine. The incidence of nausea and giddiness was similar in both dosage groups, but the adults in the higher dosage group had a significantly higher frequency of vomiting than those in the low-dose group.In view of the rapid and reliable action of a single dose, mefloquine seems to be the drug of choice for treatment of cases of falciparum malaria that are resistant to 4-aminoquinolines and to sulfonamide-pyrimethamine combinations. A dose of 20 mg per kg of body weight for children and 750 mg for adults is sufficient for treatment of semi-immune persons.
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PMID:Single-dose treatment of falciparum malaria with mefloquine: field studies with different doses in semi-immune adults and children in Burma. 621 27

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

A combination of the drugs amodiaquine and tetracycline was used in a clinical trial at Phrabuddhabat Hospital in Central Thailand for treating Plasmodium falciparum malaria. Of the 51 patients who completed the 28-day follow-up, 49 (96%) were cured; in two cases the parasitaemia was cleared within seven days of initial therapy but returned within 28 days (RI response). Only one patient experienced a mild and transient side effect of nausea. The treatment regimen was cheap and the drugs are readily available commercially. Results of this study suggest that amodiaquine-tetracycline combination offers a practical, safe and highly effective method for treating uncomplicated falciparum malaria.
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PMID:Treatment of Plasmodium falciparum malaria with a combination of amodiaquine and tetracycline in Central Thailand. 635 87

A total of 99 male Zambian patients with symptomatic falciparum malaria were treated in a double-blind randomized manner with either mefloquine (1000 mg given in one day) or chloroquine (1500 mg given over 3 days). An S-type response was seen in all the chloroquine patients and 98% of the mefloquine group; one patient in the latter group (2%) showed an RI-type response, but the parasites obtained during the recrudescence were sensitive to both chloroquine and mefloquine in the in vitro microtest, and the patient responded satisfactorily to oral chloroquine. The rate of clearance of parasitaemia was marginally faster in the chloroquine-treated group. The rate of clearance of fever was similar in the two groups. Both drugs were well tolerated and side-effects such as nausea, vomiting, dizziness, loose stools, and pruritus were mild and transient. Pruritus was more common after chloroquine administration and dizziness more common in the mefloquine group. There were no drug-induced alterations in the haematological and biochemical profiles.
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PMID:A double-blind comparative clinical trial of mefloquine and chloroquine in symptomatic falciparum malaria. 635 7

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


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