Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0027497 (nausea)
 23,468 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Halofantrine has been given to 14 children and 15 adults suffering from an acute attack of P. falciparum malaria and living in Dakar (Senegal) to a total dose of 24 mg/kg/body weight for the first group and 1,500 mg for the second in 3 times at 6-hourly intervals. This treatment has allowed the fever to clear in all cases within 36.3 +/- 19.9 hours and headache to disappear at D3 in 93.1% of cases. A reduction by 93.6% of the average parasite density which amounted before treatment to 27,710 trophozoites/mm3 of blood has been recorded from the day following the beginning of treatment and the parasite clearance obtained in all the patients of whom had chloroquine-resistant P. falciparum strains in mean time of 58.0 +/- 14.7 hours. In 3 cases (10.7%) a recrudescence of parasitemia has been noticed in D14. Only 1 of them was treated again with halofantrine which proved efficient from D2. The only adverse reactions have been nausea, vomiting, a slight diarrhoea and dizziness which affected only 13.8% of the patients. No abnormality has been noticed at a biological level. These results confirm the efficacy and good tolerance of halofantrine and allow to list it among the resource drugs used for the treatment of chloroquine-resistant P. falciparum malaria in our area.
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PMID:[Trial of halofantrine in the treatment of malaria attacks by Plasmodium falciparum in Dakar (Senegal)]. 176 59

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

Halofantrine is a 9-phenanthrenemethanol which is effective against multi-drug resistant strains of Plasmodium falciparum. It has been shown to be highly effective and extremely well tolerated in the treatment of imported cases of falciparum malaria in France. A total of 1,500 mg administered in three 500 mg doses at six-hour intervals results in a 100% cure rate in semi-immune subjects. This dosage should be repeated after 14 days to obtain the same cure rate in non-immune patients. Minor clinical side effects included epigastric pains, nausea and, in one case, a skin rash.
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PMID:Treatment of imported cases of falciparum malaria in France with halofantrine. 354 61

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

Halofantrine is a phenanthrenemethanol antimalarial that is effective against asexual forms of multidrug-resistant Plasmodium falciparum malaria. It has no action on gametocytes or hypnozoites in the liver. The drug is administered as a racemic mixture but the (+)- and (-)-enantiomers show no difference in activity in vitro. Three formulations for oral administration are available for human use, i.e. tablets, capsules and suspension. Toxicity studies in animals suggest that halofantrine has very low toxicity both in short term and long term animal studies, and there has been no evidence of mutagenicity in these studies. Phase I, II and III clinical trials of halofantrine conducted in several tropical countries found the drug to be well tolerated and effective against multidrug-resistant P. falciparum malaria when 500mg was administered every 6 hours for 3 doses. The majority of clinical adverse effects reported, including nausea, vomiting, abdominal pain, diarrhoea, orthostatic hypotension, prolongation of QTc interval, pruritus and rash, have been mild and transient. There is wide interindividual variation in halofantrine absorption. The maximal plasma concentration (Cmax) is achieved approximately 6 hours after oral administration. Bioavailability is not dose-proportional for doses over 500mg, but there is a dose-proportional increase in Cmax and area under the plasma concentration-time curve (AUC) for doses between 250 and 500mg. In patients with malaria the bioavailability of halofantrine is decreased. The mean half-life of absorption is 4 hours and Cmax is significantly lower than that obtained in healthy individuals. Furthermore, halofantrine absorption is enhanced when the drug is taken with fatty food. Therefore, halofantrine should be taken with food to ensure optimal absorption in patients with malaria. The terminal elimination half-life is 5 days in patients with malaria. Halofantrine is biotransformed in the liver to its major metabolite N-debutyl-halofantrine. Plasma concentrations of this metabolite are observed soon after administration of halofantrine, but in much lower concentrations. The elimination half-life is similar to that of halofantrine. There have been increasing reports of halofantrine treatment failure, particularly in the eastern part of Thailand. The majority of treatment failures have been associated with incomplete drug absorption. The dose-dependent cardiotoxic effects (e.g. cardiac arrhythmia) are a major concern, particularly when the bioavailability of the drug cannot be predicted. Ongoing and future studies should aim at developing more appropriate drug formulation(s) and/or optimising dosage regimens. This will allow therapeutic concentrations to be achieved with minimum adverse effects, particularly cardiotoxicity.
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PMID:Clinical pharmacokinetics of halofantrine. 795 74

The standard first-line treatment for malaria in adults in Papua New Guinea is chloroquine; for severe and treatment-failure malaria standard therapy is a combination of quinine and Fansidar (sulphadoxine-pyrimethamine). These standard treatments are currently under revision. The present study evaluated the effect of halofantrine in treatment-failure falciparum malaria in adults in Port Moresby compared to standard therapy. In the halofantrine group all parasites were cleared by day 5 after starting therapy, in the quinine-Fansidar group by day 7. There was no evidence of recurrence of parasitaemia during the 21-day follow-up in either group. Nausea was associated with halofantrine use in 68% of patients. In the quinine-Fansidar group 79% had muffled deafness, 32% tinnitus and 26% dizziness; 32% of patients withdrew from treatment on day 2 because of intolerance to quinine. Halofantrine in this study population provided an efficacy against treatment-failure falciparum malaria similar to that of quinine-Fansidar, with a more favourable profile of adverse effects.
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PMID:Halofantrine versus quinine-Fansidar combination in the treatment of post-chloroquine falciparum parasitaemia. 1093 52