Assuntos
Antinematódeos/uso terapêutico , Benzamidas/uso terapêutico , Benzamidinas/uso terapêutico , Tiadiazóis/uso terapêutico , Trichinella spiralis/efeitos dos fármacos , Triquinelose/tratamento farmacológico , Animais , Benzamidas/química , Benzamidinas/química , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Camundongos , Estrutura Molecular , Tiadiazóis/químicaRESUMO
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
To search for new antihelminthics, the new compound N-[3-chloro-4-[(1-ethyl-2-benzimidazolyl) thio]phenyl]-2-hydroxy-3,5-dibromobenzamide (the agent G-1724) was synthesized and tested by using the models of trichocephaliasis (Trichocephalus muris) and trichinosis (Trichinella spiralis). The tests demonstrated that this agent had an nematocidal effect (71-78%).
Assuntos
Antinematódeos/uso terapêutico , Benzamidas/uso terapêutico , Benzimidazóis/uso terapêutico , Trichinella spiralis , Triquinelose/tratamento farmacológico , Tricuríase/tratamento farmacológico , Trichuris , Administração Oral , Animais , Antinematódeos/administração & dosagem , Antinematódeos/síntese química , Benzamidas/administração & dosagem , Benzamidas/síntese química , Benzimidazóis/administração & dosagem , Benzimidazóis/síntese química , Modelos Animais de Doenças , Camundongos , Triquinelose/parasitologia , Tricuríase/parasitologiaAssuntos
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
Some new bromine (chlorine) derivatives of 8-quinolyloxysalicylanilides were synthesized and tested for trichinellacidal activity. Among them there was the substance N-[3-bromophenyl-4-(5-chloroquinolinoxy)]-3,5-dibromosalicylami de which exhibited its high trichinellocidal activity (in albino mice infected with decapsulated Trichinella spiralis) that was close to that of mebendazole.
Assuntos
Antinematódeos/síntese química , Antinematódeos/farmacologia , Salicilanilidas/síntese química , Salicilanilidas/farmacologia , Trichinella spiralis/efeitos dos fármacos , Animais , Antinematódeos/uso terapêutico , Avaliação Pré-Clínica de Medicamentos , Mebendazol/uso terapêutico , Camundongos , Salicilanilidas/uso terapêutico , Relação Estrutura-Atividade , Triquinelose/tratamento farmacológicoRESUMO
The comparative study of the morphology of invasive larvae and mature males and females T. spiralis and T. pseudospiralis at the head end of the parasites has revealed 14 papillae which are located in 3 circles and 2 which are placed bilaterally, 2 amphidae, and a lanceolar stiletto with a spicular cutting edge. There are no differences in the structure of the heads of these two Trichinella species. The larval cuticle is decorated only with cross folds while longitudinal small-sized folds which are arranged in regular rows appeared in mature species. The vulva in females is located at the levels of a fifth of the body from the head, it is slit-like and oval, that in T. pseudospiralis is situated at the cuticular projection. The anus in T. pseudospiralis larvae is as a cross oval slit, that in adult females is as a hemisphere, and in adult males it is coincident with the copulation pore. As for the structure of the pseudobursa, differences are found in the size and shape of copulation processes, in the arrangement of pre- and postanal papillae against the cloaca, in the size of the formed cuticular projections in T. spiralis, in the shape of the cloacal hole. In the unscrewed copulatory bell, it opens transversely in T. spiralis and vertically in T. pseudospiralis.
Assuntos
Trichinella spiralis/ultraestrutura , Trichinella/ultraestrutura , Animais , Feminino , Larva/ultraestrutura , Masculino , Camundongos , Microscopia Eletrônica de Varredura/métodos , Propriedades de Superfície , Triquinelose/parasitologiaRESUMO
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 deals with a fatal case of trichinosis in a 61-year-old male due to acute massive gastric hemorrhage from the old silent gastric ulcer developed at week 8 after the onset of infection (or at week 3 after the appearance of the first clinical signs). At autopsy, the method of ingestion of cross-striated muscular samples revealed high Trichinella spiralis infection rates: from 135 larvae per g of muscles of the tongue to 512 larvae in the diaphragm. Infection had occurred due to long-term (1-month) ingestion of the pork obtained from a subsidiary farm of Moscow Province. A role of alcohol used by the patient for the infection period (about 30 days) and some other factors which could contribute to intensive infection and death are discussed.
Assuntos
Hemorragia Gastrointestinal/etiologia , Úlcera Gástrica/etiologia , Trichinella spiralis , Triquinelose/complicações , Doença Aguda , Animais , Evolução Fatal , Hemorragia Gastrointestinal/diagnóstico , Hemorragia Gastrointestinal/parasitologia , Hemorragia Gastrointestinal/patologia , Humanos , Masculino , Pessoa de Meia-Idade , Músculos/parasitologia , Úlcera Gástrica/complicações , Úlcera Gástrica/diagnóstico , Úlcera Gástrica/parasitologia , Úlcera Gástrica/patologia , Trichinella spiralis/isolamento & purificação , Triquinelose/diagnóstico , Triquinelose/parasitologia , Triquinelose/patologiaRESUMO
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
Anti-Helmínticos/síntese química , Benzamidas/síntese química , Sulfonamidas/síntese química , Tiadiazóis/síntese química , Animais , Anti-Helmínticos/análise , Anti-Helmínticos/uso terapêutico , Anti-Helmínticos/toxicidade , Benzamidas/análise , Benzamidas/uso terapêutico , Benzamidas/toxicidade , Avaliação Pré-Clínica de Medicamentos , Espectroscopia de Ressonância de Spin Eletrônica , Camundongos , Tamanho da Partícula , Espectrofotometria Infravermelho , Relação Estrutura-Atividade , Sulfonamidas/análise , Sulfonamidas/uso terapêutico , Sulfonamidas/toxicidade , Tiadiazóis/análise , Tiadiazóis/uso terapêutico , Tiadiazóis/toxicidade , Triquinelose/tratamento farmacológicoRESUMO
The study covers the study of three antinematodal agents: the original national drug medamine with albendazole and embovin (pyrathel pamoate), which have been reproduced at the E. I. Martsinovskii Institute of Medical Parasitology and Tropical Medicine, with murine Syphacia obvelata and Aspiculuris tetraptera infection models. The quantitative parameters of the anthelmintic action of medamine, albendazole and embivin were comparatively defined for the first time.
Assuntos
Albendazol/uso terapêutico , Antinematódeos/uso terapêutico , Benzimidazóis/uso terapêutico , Carbamatos , Modelos Animais de Doenças , Oxiuríase/tratamento farmacológico , Oxyuroidea , Pamoato de Pirantel/uso terapêutico , Animais , Avaliação Pré-Clínica de Medicamentos , Larva , Camundongos , Oxiuríase/parasitologia , Fatores de TempoRESUMO
The paper proposes the rapid technique for examining the luminescence pattern of individual systems and organs in the murine parasite Aspiculuris tetraptera. The luminescence pattern of the parasite was studied after fluorochrome-plating with rhodamine 6G, rhodamine C, coryphosphine, sodium fluorescein, acridine orange which was found to be the optimum fluorochrome. This technique is to be used in the evaluation of the effects of chemopharmaceuticals on the parasite.
Assuntos
Oxyuroidea/fisiologia , Animais , Feminino , Corantes Fluorescentes , Intestino Grosso/parasitologia , Masculino , Camundongos , Microscopia de Fluorescência/métodos , Oxiuríase/parasitologia , Oxyuroidea/anatomia & histologia , Oxyuroidea/isolamento & purificação , Coloração e Rotulagem/métodosRESUMO
The use of mebendazole as a suspension in vegetable oil enhanced the efficiency of treating experimental Echinococcus granulosus infection in outbred albino rats without increasing the dose of the drug. A sharp reduction in platelet count in the blood of the infected animals treated and untreated suggests that thrombohemorrhagic complications might be in echinococcosis. Thrombopenia in the treated animals appeared to be steady-state. A decrease in a rapid immune response in the mebendazole-treated rats, as compared to the untreated ones, is likely to be a consequence of a significant fall of antigenic immune stimulation due to suppression of the parasite's viability with the drug and to be an indicator of therapeutical efficiency.
Assuntos
Equinococose/tratamento farmacológico , Echinococcus/efeitos dos fármacos , Helianthus , Mebendazol/administração & dosagem , Óleos de Plantas/administração & dosagem , Animais , Portadores de Fármacos , Avaliação Pré-Clínica de Medicamentos , Equinococose/sangue , Equinococose/parasitologia , Interações Hospedeiro-Parasita , Larva/efeitos dos fármacos , Ratos , Óleo de Girassol , Fatores de TempoRESUMO
Salicylanilides containing quinoline moiety were synthesized and examined for acute toxicity and antinematodal activity. All the compounds were shown to possess a low toxicity. In the trials on a nematodal model (Aspiculuris tetraptera, white mice), 2 compounds--G-1570 and G-1575--were shown to be highly effective.
Assuntos
Antinematódeos/síntese química , Quinolinas/síntese química , Salicilanilidas/síntese química , Animais , Antinematódeos/uso terapêutico , Antinematódeos/toxicidade , Avaliação Pré-Clínica de Medicamentos , Dose Letal Mediana , Camundongos , Oxiuríase/tratamento farmacológico , Quinolinas/uso terapêutico , Quinolinas/toxicidade , Salicilanilidas/uso terapêutico , Salicilanilidas/toxicidade , Relação Estrutura-AtividadeRESUMO
The efficacy of metiasole, a new Russian analog of albendasole, reproduced at the E. I. Martsinovskii Institute of Medical Parasitology and Tropical Medicine, was studied in mice with Aspiculuris tetraptera invasion. Metiasole efficacy and acute toxicity were comparable to those of embovin and superior to those of medamin. Relationship between the drug efficacy and its doses and number of injections was analyzed.
Assuntos
Albendazol/uso terapêutico , Carbamatos , Oxiuríase/tratamento farmacológico , Albendazol/toxicidade , Animais , Antinematódeos/uso terapêutico , Antinematódeos/toxicidade , Benzimidazóis/uso terapêutico , Benzimidazóis/toxicidade , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos , Dose Letal Mediana , Camundongos , Pamoato de Pirantel/uso terapêutico , Pamoato de Pirantel/toxicidadeRESUMO
The study of the peripheral blood response in mice with an experimental T. spiralis infection from the 1 to the 60 days of the latter showed leucocytosis, lymphomonocytosis and neutropenia maximal at the 21--35 days of the infection along with hyperthrombocytosis and ESR elevation, with the subsequent declination up to the end of the supervision. In experimental P. pseudospiralis infection lymphomonocytosis and ESR levels were comparatively lower but eosinophilia was significantly higher.
Assuntos
Triquinelose/sangue , Animais , Sedimentação Sanguínea , Contagem de Eritrócitos , Contagem de Leucócitos , Camundongos , Contagem de Plaquetas , Fatores de TempoAssuntos
Anti-Helmínticos/síntese química , Benzimidazóis/síntese química , Ftalazinas/síntese química , Animais , Anti-Helmínticos/uso terapêutico , Anti-Helmínticos/toxicidade , Benzimidazóis/uso terapêutico , Benzimidazóis/toxicidade , Avaliação Pré-Clínica de Medicamentos , Feminino , Masculino , Camundongos , Ftalazinas/uso terapêutico , Ftalazinas/toxicidade , Relação Estrutura-Atividade , Triquinelose/tratamento farmacológicoRESUMO
Unfavourable sanitary and hygienic conditions in 2 settlements have been established; the authors revealed specific features of the invasion spreading in this focus where high invasion rates of intermediate and final hosts were associated with low invasion rates. Different factors have been established, which contribute to the invasion spreading among the population. A three-score assessment has been proposed of the manifestations of the clinical symptomatology in digestive disease in opisthorchiasis which is suitable for in the field. A retrospective analysis has been made of the reasons for ineffective chemotherapy with chloxyl in this focus. The age-related affliction with opisthorchiasis in the focus is the most adequately described by a "reversible catalytic" model with a force of infection of 0.055.