Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: KEGG:D02448 (Fansidar)
 243 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Between 1980 and 1985 falciparum malaria was diagnosed in 28 and tertian malaria in 17 patients. Only three of the 35 non-immune patients complied with the appropriate chemoprophylaxis; these three patients nevertheless developed tertian malaria (recurrences caused by "dormant" merozoites). The main drawbacks of chemoprophylaxis were lack of patient compliance (26 out of 35 patients) and inappropriate medical advice (14 out of 35 patients). Initial symptoms developed within one month after the end of exposition in 21 out of 23 patients infected by Plasmodium falciparum, but only in three out of twelve cases of tertian malaria. Risk of infection by Plasmodium falciparum is highest in Africa, while most of the malaria cases in India are caused by Plasmodium vivax. Long-term prophylaxis using pyrimethamine-sulfadoxine (Fansidar) is not advisable as there is a risk of life-threatening side effects.
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PMID:[Malaria prevention. Risk of infection in relation to preventive measures]. 352 80

Seven patients (one black African and six white Europeans) developed chloroquine-resistant falciparum malaria in East Africa. In vitro studies confirmed chloroquine resistance in three patients, but the parasites failed to grow in the other four patients. Six patients were cured by sequential quinine and Fansidar, one by sequential quinine and mefloquine.
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PMID:Chloroquine-resistant falciparum malaria from East Africa. 354 85

Sixty-eight cases of vivax and 30 cases of falciparum malaria patients were treated with a combination of sulfamonomethoxine-pyrimethamine (MP tablet with 500 mg of sulfamonomethoxine and 25 mg of pyrimethamine) and the results were compared with those with chloroquine, Fansidar and quinine. Vivax malaria: Fever and parasites were cleared by the 4th day of treatment in 94 and 92% of the patients, respectively. Chloroquine was the most effective drug and Fansidar and MP tablets shared the next position. Falciparum malaria: Fever and asexual parasites were cleared by the 4th day of treatment in 67 and 78% of the patients, respectively. MP tablets were effective in chloroquine-resistant falciparum malaria contracted in Kalimantan (Indonesia) and Oceanian countries (Vanuatu etc.). Fever and parasite clearance times were shorter with chloroquine or with Fansidar than with MP tablets. Defective preschizonts used to appear following administration of MP tablets both in vivax and falciparum malarias. They were the premonitory laboratory indications that the asexual parasites will be soon eradicated.
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PMID:A combination of sulfamonomethoxine and pyrimethamine versus other drugs for the treatment of malaria. 354 42

The protective effect of malaria chemoprophylaxis with either Fansidar (pyrimethamine-sulfadoxine) or chloroquine was estimated by determining the attack rates of Plasmodium falciparum infections acquired in Kenya and imported by U.S. and Swiss travelers who had used no chemoprophylaxis, who had used only chloroquine for prophylaxis, and who had used Fansidar weekly, either alone or in combination with chloroquine. The estimated attack rates were almost identical in U.S. and Swiss travelers. The attack rate per 100,000 travelers averaged 280 in those who did not use chemoprophylaxis, 162 in those who took 4-aminoquinolines (P greater than .05), and 27 in those who used Fansidar for prophylaxis (P less than .001). Non-immune travelers to Kenya have an appreciable risk of acquiring a P. falciparum infection and need to be informed of current guidelines for chemoprophylaxis. The changing drug susceptibility patterns in Africa require continuous evaluation of the efficacy of recommended drug regimens for malaria prophylaxis.
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PMID:Efficacy of malaria prophylaxis in American and Swiss travelers to Kenya. 355 47

We report on a 72-year-old man suffering from transient acantholytic dermatosis (TAD). The histologic pattern resembled that of Darier's disease. The disorder first set on after an episode of intensive exposure to sunlight and persisted for 6 years. The only drug the patient took during this period was the prophylactic antimaterial preparation, Fansidar. His sensitivity to UVB radiation was markedly increased. After Fansidar was replaced by Resochin, the skin cleared up. After one year the sensitivity to UVB had normalized.
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PMID:[Persistent acantholytic dermatosis with increased light sensitivity]. 359 Sep 11

The pharmacokinetics of sulfadoxine (SULF) and pyrimethamine (PYR) were studied in 7 healthy volunteers after a single oral dose of Fansidar. A comparison was made between the pharmacokinetics of the components of Fansidar calculated from whole blood and plasma data. The mean whole blood to plasma concentration ratios of SULF and PYR were 0.62 and 0.87, respectively. The elimination half-lives of SULF and PYR were similar in whole blood and plasma. The apparent volume of distribution and clearance of SULF and PYR in whole blood were significantly higher (p less than 0.01) than the corresponding plasma values. Because malaria-infected erythrocytes appear to concentrate SULF, it may be more relevant to measure drug concentrations in whole blood rather than in plasma in assessing the antimalarial efficacy of Fansidar.
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PMID:Pharmacokinetics of sulfadoxine and pyrimethamine after Fansidar administration in man. 360 21

Fansimef is a new oral schizonticide which contains pyrimethamine (P), sulfadoxine (S) and mefloquine (M) in a weight ratio of 1:20:10. This antimalarial combination is highly active against multi-resistant Plasmodium falciparum and in vitro studies showed that the resistance development by plasmodia against this combination is considerably delayed. The single-dose pharmacokinetics of the three Fansimef components were investigated in 10 Caucasian volunteers with special emphasis on possible mutual kinetic interactions. For this reason the same subjects received successively tablets of Fansimef (P + S + M), Fansidar (P + S) and mefloquine alone. Following administration of Fansimef all three components revealed long elimination half-lives (P = 88 h, S = 183 h, M = 437 h) and high binding to plasma proteins (P = 92.5%, S = 87.6%, M = 97.6%). The apparent volume of distribution in the postdistributive phase (VD beta/F) was small for S (0.13 l/kg) but amounted to 2.1 l/kg for P and reached even 11.8 l/kg in the case of M. The systemic clearance (ClTS/F) showed almost identical values for P and M, namely approximately equal to 19 ml/h/kg, while sulfadoxine reached only a value of 0.5 ml/h/kg. Almost identical pharmacokinetic parameters (p greater than 0.05) were found after administration of Fansidar or M alone. Therefore one can exclude any significant interaction between the single components of the Fansimef combination. In addition, animal studies showed that synergism of the toxicity of the three combination partners can be excluded.
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PMID:Single-dose investigation of possible interactions between the components of the antimalarial combination Fansimef. 360 26

We report a subject who had Fansidar prescribed to him for the purpose of malaria prophylaxis. This agent is a combination of pyrimethamine and sulphadoxine. He subsequently developed severe hypersensitivity pneumonia and required mechanical ventilation. We believe that sulphadoxine was responsible for his illness.
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PMID:Fansidar hypersensitivity pneumonitis. 365 13

A fatal case of Stevens-Johnson syndrome associated with Fansidar and chloroquine is reported in a 5-year-old boy.
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PMID:Fatal Stevens-Johnson syndrome associated with Fansidar and chloroquine. 373 64

The in vitro effect of pyrimethamine (PYR) on human blood mononuclear cells stimulated with phytohaemagglutinin (PHA), pokeweed mitogen (PWM) and purified protein derivative of tuberculin (PPD) was studied by 14C-thymidine incorporation, by cell counting and by total DNA estimation. PYR in concentrations 10 times higher than serum values obtained in clinical practice inhibited lymphocyte proliferation irreversibly. PYR in concentrations corresponding to clinical practice quickly and irreversibly suppressed the proliferation of PWM-stimulated cells, and more slowly the proliferation of PPD-stimulated cells. The suppression of PHA-stimulated cells was reversed after one week. The increased 14C-thymidine incorporation observed in stimulated cells exposed to PYR in vitro in the early phase of proliferation did not reflect immunopotentiation but rather blocked endogenous thymidine synthesis. Sulphadoxine (SDX), added in vitro, had no effect on the lymphocytes, while SDX plus PYR had the same effect as PYR alone. Oral intake of SDX plus PYR (Fansidar) also blocked the thymidine synthesis of mitogen-stimulated lymphocytes. The possible consequences of the findings for the use of PYR in malaria prophylaxis and therapy are discussed.
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PMID:Effect of pyrimethamine and sulphadoxine on human lymphocyte proliferation. 378 90


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