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

Halofantrine is an orally administered blood schizontocide which is active against both chloroquine-sensitive and chloroquine-resistant plasmodia. Dose-finding and noncomparative clinical trials have confirmed the efficacy of halofantrine in the treatment of falciparum malaria in areas of chloroquine- and sulfonamide/pyrimethamine-resistant malaria and vivax malaria. However, poor results obtained in patients who failed mefloquine prophylaxis suggest that the efficacy of halofantrine may not extend to mefloquine-resistant P. falciparum, although more studies are needed to confirm this. Data concerning halofantrine in the treatment of P. ovale and P. malariae infections are still limited. One comparative study indicates that halofantrine has an efficacy equivalent to that of mefloquine and may be better tolerated. Halofantrine is generally well tolerated in both adults and children, the most common drug-associated effects being abdominal pain, pruritus, vomiting, diarrhoea, headache and rash, although it is difficult to distinguish between disease- and treatment-related events. The development of parasite resistance to halofantrine, like other blood schizontocides, is inevitable. Poor absorption resulting in variable peak plasma halofantrine concentrations, and possible cross-resistance with mefloquine, may accelerate the emergence of resistance to halofantrine. Thus, it is of primary importance that halofantrine is used only in areas where chloroquine- and sulfonamide/pyrimethamine-resistance are established in order to preserve and sustain its efficacy. If used with care, halofantrine will provide an important treatment option for falciparum malaria, a widespread parasitic disease associated with considerable morbidity against which the number of effective drugs available is being increasingly compromised by the spread of resistance.
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PMID:Halofantrine. A review of its antimalarial activity, pharmacokinetic properties and therapeutic potential. 137 21

Halofantrine chlorhydrate 2 per cent suspension was given to 50 children (mean age 6.2 years in a dose of 8 mg/kg three times a day as a single day treatment. The children were born and lived in Gabon, where malaria transmission is continuous. They all had acute Plasmodium falciparum malaria. The children were kept in hospital for 5 days, and regularly followed over a 15-day period. The 50 children were cured and efficacy was evaluated as good in 44 cases, and excellent in six cases, as judged by improvement in their clinical signs and parasitaemia. Two criterias were considered in the evaluation of efficacy: clearance of parasitaemia (mean day 4), fever clearance (mean hour 24). There were two cases of persistences of parasites at day 15 with a very low parasitaemia rate. Tolerance to halofantrine was good from a clinical and biological point of view. Acceptability was excellent in all cases. Halofantrine 2 per cent suspension is a good alternative in the treatment of acute Plasmodium falciparum malaria in children, especially with the present situation of multidrug-resistant strains in Central Africa.
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PMID:Efficacy, safety and acceptability of halofantrine in the treatment of acute Plasmodium falciparum malaria in African children (Gabon). 157 96

Halofantrine is a new blood schizontocidal drug used for the treatment of multidrug-resistant falciparum malaria. The pharmacokinetics of halofantrine (HAL) and its principal metabolite, N-desbutylhalofantrine (BHAL), was investigated in 6 adult male patients of Melanesian origin with uncomplicated falciparum malaria. The patients received 500 mg of halofantrine hydrochloride at times 0, 6 and 12 h (total 1.5 g). All patients responded to treatment with a mean parasite clearance time of 52.7 h and a mean fever clearance time of 33.8 h. The following kinetic parameters (mean values) were determined for HAL and BHAL, respectively: maximum plasma concentration (Cmax) = 896 and 491 ng.ml-1; time to reach the Cmax (tmax) = 15 and 56 h; elimination half-life (t1/2) = 91 and 79 h and the mean residence time (MRT) = 71 and 102 h. Based on the clinical response the plasma concentrations of HAL and BHAL were adequate for the treatment of uncomplicated falciparum malaria in the 6 patients.
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PMID:Pharmacokinetics of halofantrine and n-desbutylhalofantrine in patients with falciparum malaria following a multiple dose regimen of halofantrine. 174 49

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

According to the new strategy of the WHO for malaria prophylaxis, the use of stand-by drugs should be recommended when feasible. Because of its favourable safety/efficacy profile, I recommend Halofantrine to be used as the drug for stand-by treatment with the precautions expressed here.
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PMID:Expert opinion on presumptive treatment with halofantrine (Halfan). 179 Jan 36

Paludism can occur quite easily in pregnant women in endemic zones, above all those who are primiparous or in their 2nd or 3rd terms. The onset of paludal attacks can be serious for both the mother and the child. That is to say, besides the obviously imperative therapeutic action, a prophylaxis is also a necessity. The use of antipaludial substances at our disposal has been complicated during the last few years as a result of chloroquine-resistance extension. Besides a few nuances of kinetic nature observed in pregnant women, a good knowledge of teratogenous or embryotoxic effects is necessary. But this remains fragmentary. Among the principal antipaludial medications is quinine (Q), reported to be abortifacient but in reality it is not: it is often poorly tolerated by the mother (hypoglycemia), but is not responsible for abnormalities in children, except under large doses. Chloroquine (CQ), considered to be without harmful effects, can be used in women without large restrictions, even if toxic effects have been observed in animals. The pyrimethamine-sulfanilamide (P-S) combination contains two substances which are a potential risk. Nevertheless, experiments have never showed harmful effects in pregnant women, particularly when under cover of a joint prescription of folinic acid. Proguanil is without doubt the only molecule which can be used without restriction. Two new medications, quinoline methanol, Mefloquine (MQ) and Halofantrine (HF) are contra-indicated for lack of experimentation and because of some abnormalities observed at high doses in animals. Artemisinine and amino-8-quinoline are contra-indicated, and cyclines are strongly inadvised. From the practical point of view, the present use of antipaludial medication in pregnancy should take into account the surrounding risk, namely that of paludism and of treatments. Curatively, Q remains a serious treatment in any form. In CQ-sensitive zones CQ is usable unreservedly in simple attacks. In CQ resistance zones the use of Q seems preferable to that of Fansidar proposed by certain people. MQ and HF, although contra-indicated, have already been employed without inconvenience. By way of prevention, it is important first of all to avoid all leisure stays in endemic zones. If travel is unavoidable or for indigenous people, a chemoprophylaxis, judged according to the local risk of impaludation, is desirable: CQ in sensitive zones, PG+CQ in resistant zones, P-S, as proposed by some people, is normally contra-indicated; MQ and HF are contra-indicated. Protection against nocturnal mosquito bites is still strongly applied (Mosquito net, repellents, insecticides).
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PMID:[Antimalarials and pregnancy]. 181 22

Mefloquine and halofantrine are quinine-related aminoalcohols recently introduced for the oral treatment (both drugs) and oral chemoprophylaxis (mefloquine) of malaria. Soon after these new drugs were launched the volume of sales testified to the need for alternative treatments in view of the resistance of Plasmodium falciparum to a variety of drugs, including chloroquine, amodiaquine and sulfadoxine-pyrimethamine. Quinine remains effective but it is difficult to handle. Both mefloquine and halofantrine are remarkably effective against the intraerythrocytic pathogenic forms of malaria; they also have a rapid and prolonged action and a low toxicity. Halofantrine is sometimes incompletely absorbed. Neurological side-effects, usually moderate, have been reported with mefloquinone. Partial cross-resistance has been demonstrated within each class of antimalarials: aminoalcohols, amino-4-quinoleins (chloroquine, amodiaquine) and antifolics-antifolinics (sulfamides, pyrimethamine, proguanil), but not between the classes. Further studies are necessary concerning the absorption and tolerability of mefloquine and halofantrine, as well as the regional level of P. falciparum sensitivity to these new drugs.
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PMID:[Mefloquine and halofantrine, new therapeutic drugs of malaria]. 204 18

Twelve patients with acute uncomplicated falciparum malaria were admitted to the Hospital for Tropical Diseases for 42 days. The patients were treated with halofantrine 500 mg 6 hourly for three doses and halofantrine and its desbutyl metabolite were analysed in plasma by h.p.l.c. Cmax values of halofantrine and desbutylhalofantrine (n = 12) were 1192 +/- 410 (mean +/- s.d.) and 397 +/- 160 ng ml-1 with tmax values of 16 +/- 2 and 55 +/- 26 h, respectively. AUC was 60.6 +/- 23.9 and 48.5 +/- 22.2 mg l-1 h, respectively, for halofantrine and its metabolite. Halofantrine cured 83% of the patients but in two patients a reduction only in asexual parasitaemia was seen and no overall parasite clearance occurred. One of these, however had relatively low plasma concentrations of both halofantrine and its desbutyl metabolite and it appeared to be a case of inadequate treatment rather than true resistance. We suggest that the large intersubject variability in plasma drug concentrations may relate in part to its poor and inconsistent bioavailability and this rather than true resistance might be responsible for some of the treatment failures.
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PMID:Pharmacokinetics of halofantrine in Thai patients with acute uncomplicated falciparum malaria. 204 60

59 cases of Plasmodium falciparum malaria fever occurring in non-immune Caucasian subjects having got a correct chemoprophylaxis by chloroquine were treated by halofantrine (HALFAN). They were given 1500 mg divided in 3 doses of 500 mg every 6 hours from D1 to D8. All them were back from a malarial highly endemic zone with chloroquine resistance. Analysis of the main biological and clinical efficiency parameters displayed very satisfactory results: disappearances of fever (mean 22 H) and parasitemia (mean 36 H) are short. After two months of monitoring, no malaria recrudescence was noted. With an efficacy of 10 p.c. associated to a noticeable clinical and biological tolerance Halofantrine is a first-class treatment of chloroquine resistant malaria fever.
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PMID:[The treatment of imported Plasmodium falciparum malaria with halofantrine. Apropos of 59 case reports (corrected and republished article orginally printed in Med Trop (Mars) 1990 Jan-Mar;50(1):113-7)]. 210 May 12

Chloroquine is currently the drug of choice for treatment of acute attacks of Plasmodium falciparum malaria in chloroquine-sensitive areas. In areas of low level resistance, this drug may still be used (25 mg/kg of body weight in three days) in semi-immune patients. In case of failure, or in areas of high level resistance, quinine (25 mg/kg/day for 3 to 5 days) or, in spite of increasing resistance, Fansidar should be prescribed. Mefloquine, Fansimef and Halofantrine ought to be strictly prescribed to delay occurrence of resistance. Severe attacks require quinine by continuous intravenous infusion. Spleen enlargement does not usually require specific treatment unless poor tolerance is observed. Blood transfusions present a considerable risk of HIV transmission. Appropriate malaria treatment may avoid blood transfusions thus preventing HIV dissemination in Africa.
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PMID:[Treatment of Plasmodium falciparum malaria in Africa (except cerebral malaria)]. 219 75


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