Assuntos
Anti-Helmínticos/uso terapêutico , Benzamidas/uso terapêutico , Himenolepíase/tratamento farmacológico , Hymenolepis nana , Tiadiazóis/uso terapêutico , Administração Oral , Animais , Anti-Helmínticos/toxicidade , Benzamidas/química , Benzamidas/toxicidade , Avaliação Pré-Clínica de Medicamentos , Camundongos , Estrutura Molecular , Relação Estrutura-Atividade , Tiadiazóis/química , Tiadiazóis/toxicidadeRESUMO
Trials of trichlorophen have shown its high efficacy on models of cestode infections: hymenolepiasis (at the adult and cysticercoid stages of development on three types of animals: outbred albino mice, albino rats and golden hamsters), preimaginal echinococciasis alveolaris, larval alveolar echinococciasis (at the early stage of development of the parasite in experiments on cotton rats). The high nematodical activity of trichlorophen was first found on models of trichocephaliasis in DBA/2y mice, nippostrongyloidiasis (in in vitro experiments), and aspiculuriasis in outbred mice. The agent proved to be ineffective at the tissue developmental stage of Hymenolepsis nana (H. nana), the dwarf tapeworm, in albino mice, during experimental opisthorchiasis in golden hamsters. It showed a low efficacy in treating trichinosis in outbred albino mice. Unlike carbamatebenzimidazoles, trichlorophen was inactive at the tissue stage of H. nana; it exerted no effects on the eggs of a dwarf tapeworm in trichinosis. Trichlorophen was also inactive in treating experimental opisthorchiasis in golden hamsters.
Assuntos
Anti-Helmínticos/uso terapêutico , Clorofenóis/uso terapêutico , Helmintíase/tratamento farmacológico , Administração Oral , Animais , Anti-Helmínticos/administração & dosagem , Infecções por Cestoides/tratamento farmacológico , Clorofenóis/administração & dosagem , Cricetinae , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos , Helmintíase/parasitologia , Hymenolepis/efeitos dos fármacos , Hymenolepis/fisiologia , Camundongos , Camundongos Endogâmicos DBA , Infecções por Nematoides/tratamento farmacológico , Nippostrongylus/efeitos dos fármacos , Nippostrongylus/fisiologia , Ratos , Federação RussaRESUMO
Experiments have established the high efficacy of combinations of the micronized dosage form of trichlorophen, with albendazole or medamine in treating trichocephaliasis (its causative agent being Trichocephalus muris) in DBA/2st mice and that of trichlorophen in combination with azinox or fenasal in outbred albino mice with hymenolepiasis (its causative agent being Hymenolepis nana). These combinations are promising in treating patients with cestodosis and nemadosis, respectively.
Assuntos
Anti-Helmínticos/uso terapêutico , Carbamatos , Clorofenóis/uso terapêutico , Helmintíase/tratamento farmacológico , Praziquantel/análogos & derivados , Administração Oral , Albendazol/uso terapêutico , Animais , Anti-Helmínticos/administração & dosagem , Benzimidazóis/uso terapêutico , Clorofenóis/administração & dosagem , Avaliação Pré-Clínica de Medicamentos , Quimioterapia Combinada , Himenolepíase/tratamento farmacológico , Camundongos , Camundongos Endogâmicos DBA , Niclosamida/uso terapêutico , Praziquantel/uso terapêutico , Tricuríase/tratamento farmacológicoAssuntos
Albendazol/síntese química , Albendazol/uso terapêutico , Anti-Helmínticos/síntese química , Anti-Helmínticos/uso terapêutico , Albendazol/efeitos adversos , Albendazol/farmacologia , Animais , Anti-Helmínticos/efeitos adversos , Anti-Helmínticos/farmacologia , Ensaios Clínicos como Assunto , HumanosRESUMO
The paper describes a procedure for manufacturing the new anthelminthic Tizanox. It shows it necessary to administer a larger dose of the drug than that of azinox (praziquantel) to treat experimental hymenolepiasis. However, the lower toxicity of Tizanox enhances its chemotherapeutical index.
Assuntos
Anticestoides/síntese química , Anticestoides/uso terapêutico , Himenolepíase/tratamento farmacológico , Isoquinolinas/síntese química , Isoquinolinas/uso terapêutico , Tiadiazinas/síntese química , Tiadiazinas/uso terapêutico , Animais , Anticestoides/análise , Anticestoides/toxicidade , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos , Isoquinolinas/análise , Isoquinolinas/toxicidade , Camundongos , Praziquantel/análogos & derivados , Praziquantel/uso terapêutico , Praziquantel/toxicidade , Espectrofotometria Infravermelho/estatística & dados numéricos , Tiadiazinas/análise , Tiadiazinas/toxicidadeAssuntos
Helmintíase/etiologia , Helmintíase/história , História do Século XX , Humanos , Pesquisa/história , U.R.S.S.RESUMO
New 1-[(2-acylamino)phenyl]-3, 4-dihydroisoquinolines were synthesized and tested for their acute toxicity and antitrichinosis activity. The above compounds were found to show their low toxicity and two compounds (G-1615 and G-1616) displayed a high antitrichinosis effect.
Assuntos
Antinematódeos/química , Antinematódeos/uso terapêutico , Isoquinolinas/química , Isoquinolinas/uso terapêutico , Trichinella spiralis , Triquinelose/tratamento farmacológico , Albendazol/uso terapêutico , Animais , Antinematódeos/toxicidade , Avaliação Pré-Clínica de Medicamentos , Isoquinolinas/toxicidade , CamundongosRESUMO
The paper outlines a procedure for manufacturing the anthelminthic Azinox (biltricide) using the new interfacial transfer catalyst benzyl-di-propyl (beta-hydroxyethyl)ammonium chloride. Azinox has been shown to be identical to biltricide (praziquantel) in its properties. Azinox tests on models of Opisthorchis felineus in golden hamsters and of Hymenolepis nana in albino outbred mice have indicated that the agent is not inferior to biltricide in its antitrematodal and anticestodal activities. Azinox displayed a high activity at the preimaginal stages of O. felineus and H. nana and at the larval stage of H.nana.
Assuntos
Anticestoides/síntese química , Antiplatelmínticos/síntese química , Praziquantel/análogos & derivados , Animais , Anticestoides/uso terapêutico , Anticestoides/toxicidade , Antiplatelmínticos/uso terapêutico , Antiplatelmínticos/toxicidade , Cricetinae , Avaliação Pré-Clínica de Medicamentos , Feminino , Himenolepíase/tratamento farmacológico , Himenolepíase/parasitologia , Dose Letal Mediana , Masculino , Mesocricetus , Camundongos , Opistorquíase/tratamento farmacológico , Opistorquíase/parasitologia , Praziquantel/síntese química , Praziquantel/uso terapêutico , Praziquantel/toxicidadeRESUMO
Several derivatives of 2-methylthiobenzimidazoles were synthesized and assayed for anthelmintic activity. Following these studies, 2-methylthio-5-(1-chloronaphthyloxy-2)-6-chlorobenzimidazole (G-1557) has been selected as a tichinellacide for detailed investigations.
Assuntos
Antinematódeos/síntese química , Benzimidazóis/síntese química , Animais , Antinematódeos/análise , Antinematódeos/uso terapêutico , Antinematódeos/toxicidade , Benzimidazóis/análise , Benzimidazóis/uso terapêutico , Benzimidazóis/toxicidade , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos , Feminino , Masculino , Mebendazol/uso terapêutico , Camundongos , Espectrofotometria Infravermelho , Trichinella spiralis , Triquinelose/tratamento farmacológicoAssuntos
Anticestoides/síntese química , Benzazepinas/síntese química , Himenolepíase/tratamento farmacológico , Isoquinolinas/síntese química , Animais , Anticestoides/uso terapêutico , Anticestoides/toxicidade , Benzazepinas/uso terapêutico , Benzazepinas/toxicidade , Avaliação Pré-Clínica de Medicamentos , Isoquinolinas/uso terapêutico , Isoquinolinas/toxicidade , Camundongos , Relação Estrutura-AtividadeRESUMO
In DBA/2st mice experimentally infected with Trichocephalus muris the emotional stress caused by a cat that was placed for 2 hours twice a day during 14 days or more was found to reduce the efficiency of specific drug therapy with albendasole. At the same time there was an increase in the ED84:ED16 ratio (the effective dose of the drug which allows 84 or 16% of helminths to be eliminated), which decreased elimination probability in the whole helminth populations.
Assuntos
Estresse Psicológico/fisiopatologia , Tricuríase/tratamento farmacológico , Albendazol/administração & dosagem , Animais , Gatos , Avaliação Pré-Clínica de Medicamentos , Feminino , Masculino , Camundongos , Camundongos Endogâmicos DBA , Estresse Psicológico/etiologia , Fatores de Tempo , Tricuríase/parasitologia , Tricuríase/fisiopatologia , Trichuris/isolamento & purificaçãoRESUMO
Experimental invasion of white outbred mice with Nippostrongylus brasiliensis show, that chemotherapeutic effectiveness of medamin is changing in various developmental stages of this helminth. Larva of the fourth phase is most sensitive to medamin; adult worm, especially in the beginning of oviposition, is less sensitive. Chemotherapeutic effect of medamin is increasing with prolongation of therapeutic period, increase of daily doses and degree of its dispersiveness.
Assuntos
Antinematódeos/administração & dosagem , Benzimidazóis/administração & dosagem , Carbamatos , Nippostrongylus/efeitos dos fármacos , Animais , Modelos Animais de Doenças , Avaliação Pré-Clínica de Medicamentos , Larva/efeitos dos fármacos , Larva/crescimento & desenvolvimento , Camundongos , Nippostrongylus/crescimento & desenvolvimento , Infecções por Strongylida/tratamento farmacológico , Infecções por Strongylida/parasitologia , Fatores de TempoAssuntos
Animais , Helmintíase/história , Helmintos , História do Século XX , Humanos , Parasitologia/história , U.R.S.S.RESUMO
Clinical manifestations were observed only 16 out of 61 patients aged 15-32 years who had hymenolepiasis. Despite their degree, there was impaired dexylose absorption, lower serum lysozyme activity and higher serum complement activity, depressed immunological reactivity parameters (the count of T- and B-lymphocytes, their functional activity), decreased IgA titer and increased IgE titer in the sera in all the patients observed. Six months after the effective dehelminthization, varying immunodepression still remained in all the convalescents. There types of restoration of immunological reactivity were identified: torpid, reactive and highly reactive. The torpid type was significantly more frequently observed in patients with subclinical (asymptomatic) hymenolepiasis course than in patients with its clinical manifestation.
Assuntos
Himenolepíase/imunologia , Adolescente , Adulto , Anti-Helmínticos/uso terapêutico , Formação de Anticorpos/efeitos dos fármacos , Formação de Anticorpos/imunologia , Fezes/parasitologia , Humanos , Himenolepíase/tratamento farmacológico , Himenolepíase/parasitologia , Imunidade Celular/efeitos dos fármacos , Imunidade Celular/imunologia , Imunidade Inata/efeitos dos fármacos , Imunidade Inata/imunologia , Contagem de Ovos de ParasitasRESUMO
Basic achievements in the creation of antinematodal, anticestodal and antitrematodal agents are reviewed chronologically. It is shown that the search was performed mainly among the derivatives of benzimidazole, cyclic amidines, diphenylmethane, salicyl anilides, pyrazine isoquinolines, among natural products of avermictines and milbemicines. It is noted that nowadays there is every possibility for the treatment of mass helminthiases in the USSR. However, it has been found that some drugs are associated with a certain risk and therefore the necessity for further search of safe anthelminthic agents has been emphasized.
Assuntos
Anti-Helmínticos/uso terapêutico , Anti-Helmínticos/química , Anticestoides/química , Anticestoides/uso terapêutico , Antinematódeos/química , Antinematódeos/uso terapêutico , Antiplatelmínticos/química , Antiplatelmínticos/uso terapêutico , Avaliação de Medicamentos , Helmintíase/tratamento farmacológico , Humanos , Pesquisa , U.R.S.S.RESUMO
Studies of the inbred lines of mice A/He, AKR and CBA infected with different strains of H. nana have shown that the helminth, when changing the host for another one of the same species but with different hereditary characters, happens to be insufficiently adapted to the new host. However it does not prevent the start of the infectious process. With increasing number of passages the parasite's adaptation level to the organism of the new host rises gradually. Possibilities and the adaptation level of the agent to the new host are defined as well by the adaptational mechanisms common to each specific strain of H. nana and the host's characters.