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1.
Am J Trop Med Hyg ; 110(4): 677-680, 2024 Apr 03.
Artigo em Inglês | MEDLINE | ID: mdl-38460198

RESUMO

Unlike praziquantel, artemisinin derivatives are effective against juvenile schistosome worms. We assessed the efficacy and safety of a single oral dose of artesunate plus sulfalene-pyrimethamine versus praziquantel in the treatment of Schistosoma mansoni. Seventy-three schoolchildren (aged 9-15 years) with confirmed S. mansoni infection in Rarieda, western Kenya, were randomly assigned to receive either a single oral dose of artesunate plus sulfalene-pyrimethamine (n = 39) or a single dose of praziquantel (n = 34). The cure and egg reduction rates at 4 weeks posttreatment were 69.4% (25/36) versus 80.6% (25/31) (P = 0.297) and 99.1% versus 97.5% (P = 0.607) in the artesunate plus sulfalene-pyrimethamine group versus praziquantel group, respectively. Fourteen children developed adverse events, and there were no serious adverse events. A single oral dose of artesunate plus sulfalene-pyrimethamine has efficacy comparable to that of praziquantel in the treatment of S. mansoni, but these results should be confirmed in larger randomized controlled trials.


Assuntos
Anti-Helmínticos , Artemisininas , Esquistossomose mansoni , Sulfaleno , Adolescente , Animais , Criança , Humanos , Anti-Helmínticos/uso terapêutico , Artemisininas/efeitos adversos , Artesunato/uso terapêutico , Quimioterapia Combinada , População da África Oriental , Quênia , Praziquantel/efeitos adversos , Pirimetamina/uso terapêutico , Schistosoma mansoni , Esquistossomose mansoni/tratamento farmacológico , Sulfaleno/farmacologia , Sulfaleno/uso terapêutico , Resultado do Tratamento
2.
Parasitol Res ; 100(3): 511-7, 2007 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-17013650

RESUMO

An open randomized controlled study of artemether-lumefantrine (AL) and amodiaquine-sulfalene-pyrimethamine (ASP) for the treatment of uncomplicated Plasmodium falciparum malaria was carried out in 181 children. In 79 children, the hepatomegaly reduction ratios (HRR) and the speed of resolution of hepatomegaly, the hepatomegaly resolution rates (HRSR), were calculated and compared between the two treatment groups. HRR and HRSR were similar in the two treatment groups. HRSR was 71% and 62% in AL- and ASP-treated children, respectively, 14 days after commencing treatment. There was no significant correlation between HRR and parasite reduction ratio in the same patient. In children in whom parasitaemia cleared and hepatomegaly resolved within 14 days, recurrence of parasitaemia was associated with reoccurrence of hepatomegaly, suggesting that the propensity for recurrence of infection drives the malaria-attributable hepatomegaly in children from this endemic area. Combination therapy may provide additional beneficial effects on pathophysiological processes and changes associated with falciparum malaria by rapid clearing of asexual parasitaemia and reducing the propensity for recurrence of infection.


Assuntos
Amodiaquina/uso terapêutico , Antimaláricos/uso terapêutico , Artemisininas/uso terapêutico , Etanolaminas/uso terapêutico , Fluorenos/uso terapêutico , Hepatomegalia/complicações , Malária Falciparum/complicações , Pirimetamina/uso terapêutico , Sulfaleno/uso terapêutico , Amodiaquina/administração & dosagem , Amodiaquina/farmacologia , Animais , Antimaláricos/administração & dosagem , Antimaláricos/farmacologia , Combinação Arteméter e Lumefantrina , Artemisininas/administração & dosagem , Artemisininas/farmacologia , Criança , Pré-Escolar , Combinação de Medicamentos , Quimioterapia Combinada , Etanolaminas/administração & dosagem , Etanolaminas/farmacologia , Feminino , Fluorenos/administração & dosagem , Fluorenos/farmacologia , Hepatomegalia/tratamento farmacológico , Humanos , Malária Falciparum/tratamento farmacológico , Malária Falciparum/patologia , Masculino , Pirimetamina/administração & dosagem , Pirimetamina/farmacologia , Sulfaleno/administração & dosagem , Sulfaleno/farmacologia , Fatores de Tempo , Resultado do Tratamento
3.
Pak J Biol Sci ; 10(1): 156-9, 2007 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-19070005

RESUMO

The effects of sulphamethoxypyridazine: Pyrimethamine (Metakelfin) a combination antimalarial drug on mouse sperm head morphology were evaluated in University of Ibadan Veterinary F1 mice. Five different dose levels of 3.85:0.19; 7.7:0.38; 15.4:0.76; 23.1:1.13 and 30.8:1.54 mg kg(-1) body weight of sulphamethoxypridazine:pyrimetamine, respectively were administered to the animals by a schedule of 5 consecutive daily intraperitoneal (i.p.) injections. The sperm of the mice from the cauda epididymis were examined 5 weeks after treatment. Metakelfin induced sperm head abnormalities; however, of the 5 doses sampled; only the 7.7:0.38 mg kg(-1) dose, corresponding to 0.5x the human therapeutic dose (HTD0), gave a statistically significant (p > 0.05) increase over the negative control value of 2.53% abnormality. All the other dose level treatments did not yield statistically significant increase over the negative control value. The 15.4:0.77 mg kg(-1) dose showed 3.5% abnormality and fewer abnormalities than the preceding lower dose. The drug is probably not mutagenic as induction of sperm head abnormality was not dose dependent.


Assuntos
Antimaláricos/farmacologia , Pirimetamina/farmacologia , Cabeça do Espermatozoide/efeitos dos fármacos , Espermatozoides/efeitos dos fármacos , Sulfaleno/farmacologia , Animais , Combinação de Medicamentos , Humanos , Masculino , Camundongos , Nigéria , Cabeça do Espermatozoide/ultraestrutura , Espermatozoides/anormalidades , Espermatozoides/citologia
4.
Exp Parasitol ; 93(1): 33-7, 1999 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-10464036

RESUMO

The present communication deals with drug-resistant Plasmodium falciparum malaria complicating hematologic malignancies (leukemias, n = 24, and lymphomas, n = 7) in children. Of 50 cases of hematologic malignancies, 31 patients were microscopically diagnosed as having P. falciparum infection (MP +). Initially, all the patients were treated with chloroquine. The results of primary treatment showed chloroquine resistance in 16 (51. 62%) cases. Of these 16 chloroquine-resistant cases, 13 were secondarily treated with a combination of pyrimethamine plus sulfamethopyrazine. The results of secondary treatment also revealed resistance to pyrimethamine plus sulfamethopyrazine in 6 of 13 (46. 10%) cases. The 6 pyrimethamine plus sulfamethopyrazine-resistant P. falciparum cases were finally cured by quinine therapy, against which no resistance was encountered. Conversely, in the control group comprising 38 cases of P. falciparum without malignancy, the incidence of chloroquine resistance was found in only 9 cases, which is rather low (23.70%). Of these 7 chloroquine-resistant cases, 5 were found to be sensitive to pyrimethamine plus sulfamethopyrazine treatment, while the 2 nonresponders were finally cured with quinine. The overall results of this study show a high prevalence of chloroquine resistance among clinical cases of falciparum malaria (25/69; 30.6%). Among the nonresponders (n = 20) 40% of cases were also resistant to the pyrimethamine plus sulfamethopyrazine combination. There was no resistance to quinine.


Assuntos
Antimaláricos/farmacologia , Doença de Hodgkin/complicações , Leucemia Mieloide Aguda/complicações , Linfoma não Hodgkin/complicações , Malária Falciparum/complicações , Leucemia-Linfoma Linfoblástico de Células Precursoras/complicações , Adolescente , Animais , Antimaláricos/uso terapêutico , Criança , Pré-Escolar , Cloroquina/farmacologia , Cloroquina/uso terapêutico , Resistência a Medicamentos , Quimioterapia Combinada , Feminino , Humanos , Lactente , Malária Falciparum/tratamento farmacológico , Masculino , Plasmodium falciparum/efeitos dos fármacos , Pirimetamina/farmacologia , Pirimetamina/uso terapêutico , Quinina/uso terapêutico , Sulfaleno/farmacologia , Sulfaleno/uso terapêutico
5.
Antibiot Khimioter ; 36(11): 26-7, 1991 Nov.
Artigo em Russo | MEDLINE | ID: mdl-1793291

RESUMO

The effect of sulfalen on the weight and structure of the thymus, spleen and adrenal glands was studied. The findings were compared with the results observed in control rats. It was shown that after administration of sulfalen, the weight of the adrenal glands markedly decreased while their structure did not change. Thymus specimens showed a large number of hypertrophic epitheliocytes, in the medulla which was accompanied by a decrease in its weight.


Assuntos
Glândulas Suprarrenais/efeitos dos fármacos , Baço/efeitos dos fármacos , Sulfaleno/farmacologia , Timo/efeitos dos fármacos , Glândulas Suprarrenais/anatomia & histologia , Animais , Masculino , Tamanho do Órgão/efeitos dos fármacos , Ratos , Baço/anatomia & histologia , Timo/anatomia & histologia
6.
Antibiot Khimioter ; 33(12): 917-21, 1988 Dec.
Artigo em Russo | MEDLINE | ID: mdl-3245708

RESUMO

The effect of sulfalen and furosemide on benzylpenicillin kinetics in blood serum, intact tissues and aseptic inflammation foci was studied on rats. It was shown that under the action of sulfalen and furosemide protein binding of benzylpenicillin lowered by 30 per cent. The changes in the antibiotic kinetics after combined use with sulfalen and furosemide were of the same type: markedly increased concentrations in blood serum and tissues and retarded elimination.


Assuntos
Dermatite Atópica/tratamento farmacológico , Furosemida/farmacologia , Penicilina G/farmacocinética , Sulfaleno/farmacologia , Sulfanilamidas/farmacologia , Animais , Dermatite Atópica/metabolismo , Sinergismo Farmacológico , Furosemida/administração & dosagem , Penicilina G/metabolismo , Penicilina G/uso terapêutico , Ligação Proteica/efeitos dos fármacos , Ratos , Sulfaleno/administração & dosagem
8.
Antibiot Med Biotekhnol ; 30(2): 103-6, 1985 Feb.
Artigo em Russo | MEDLINE | ID: mdl-4004182

RESUMO

Interaction of erythromycin and oleandomycin with isolated subcellular fractions of rat liver homogenates and intracellular distribution of the antibiotics were studied. It was found that the macrolides were bound by the cell organoids. The binding was partially reversible. The intracellular distribution was characterized by accumulation of erythromycin and oleandomycin in the mitochondrial fraction while erythromycin preserved higher activity in cytosol as compared to oleandomycin. Sulfalen induced redistribution of the macrolides. It decreased absorption of the macrolides by the organoids and increased the concentration of free erythromycin and especially oleandomycin in cytosol.


Assuntos
Eritromicina/metabolismo , Fígado/metabolismo , Oleandomicina/metabolismo , Animais , Sítios de Ligação , Permeabilidade da Membrana Celular , Núcleo Celular/metabolismo , Citosol/metabolismo , Feminino , Técnicas In Vitro , Membranas Intracelulares/metabolismo , Cinética , Lisossomos/metabolismo , Masculino , Microssomos Hepáticos/metabolismo , Mitocôndrias Hepáticas/metabolismo , Organoides/metabolismo , Ratos , Sulfaleno/farmacologia
9.
Antibiotiki ; 29(11): 823-5, 1984 Nov.
Artigo em Russo | MEDLINE | ID: mdl-6524880

RESUMO

The combined use of cephaloridin and cephalothin with sulfalen resulted in decreased binding of the cephalosporins by serum proteins and decreased rate of drug elimination in rabbits. It might be suggested that these two processes were interrelated. The decreased binding of the antibiotics by proteins in rabbits promoted an increase in the volume distribution of the drugs at the expense of a rise in the level of their penetration from the blood into the peripheral tissues.


Assuntos
Cefaloridina/metabolismo , Cefalotina/metabolismo , Sulfaleno/metabolismo , Sulfanilamidas/metabolismo , Animais , Cefaloridina/administração & dosagem , Cefalotina/administração & dosagem , Humanos , Cinética , Taxa de Depuração Metabólica/efeitos dos fármacos , Ligação Proteica/efeitos dos fármacos , Coelhos , Sulfaleno/administração & dosagem , Sulfaleno/farmacologia
17.
Zentralbl Bakteriol Orig A ; 238(3): 419-29, 1977 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-910581

RESUMO

Two month old chronically infected Mastomys natalensis, which had been treated for ten days with sulfomethoxypyrazine-pyrimethamine, were utilized for testing the effect of chemotherapy on the fine structure of Toxoplasma cysts (strain ALT). After completion of the therapy, cysts were examined from the brains of killed animals in scanning and transmission electron microscopes. The scanning electron microscopic experiments revealed no or only slight morphological differences between the cysts of the untreated controls (Fig. 1) and the treated animals (Fig 2). In transmission electron microscopic studies the cyst membrane appeared less rugged (see Fig. 3,7 and the untreated control Fig. 6). The cyst basic substance often produces an optically empty space (Fig. 3,4). The pellicle of individual parasites display an unusual affinity for the pellicle of neighboring parasites (Fig. 3,5,7). In direct contrast to the untreated cysts no endodyogeny could be observed on the treated cysts examined to this point.


Assuntos
Encéfalo/parasitologia , Pirimetamina/uso terapêutico , Sulfaleno/uso terapêutico , Sulfanilamidas/uso terapêutico , Toxoplasma/ultraestrutura , Toxoplasmose/parasitologia , Animais , Modelos Animais de Doenças , Quimioterapia Combinada , Feminino , Masculino , Mamíferos , Pirimetamina/farmacologia , Sulfaleno/farmacologia , Toxoplasma/efeitos dos fármacos , Toxoplasmose/tratamento farmacológico
18.
J Dent Res ; 54(3): 471-4, 1975.
Artigo em Inglês | MEDLINE | ID: mdl-1056350

RESUMO

Known antimalarial compunds from several chemical classes were tested for their ability to inhibit in vitro growth of microorganisms causing dental plaque and to prevent the development of plaque in a hamster model. Approximately a third of the compounds tested inhibited in vitro growth; however, none prevented development of plaque.


Assuntos
Antimaláricos/farmacologia , Placa Dentária/prevenção & controle , Actinomyces/efeitos dos fármacos , Actinomyces/crescimento & desenvolvimento , Amodiaquina/farmacologia , Animais , Células Cultivadas , Cloroquina/farmacologia , Cricetinae , Dapsona/farmacologia , Placa Dentária/metabolismo , Placa Dentária/microbiologia , Masculino , Primaquina/farmacologia , Pirimetamina/farmacologia , Quinina/farmacologia , Streptococcus/efeitos dos fármacos , Streptococcus/crescimento & desenvolvimento , Sulfaleno/farmacologia , Tetraciclina/farmacologia , Trimetoprima/farmacologia
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