RESUMEN
The incidence of trichinosis in Russia was 0.07 per 100,000 population in 2014, which was 2.9-fold higher than that in 2013. Two WHO recommended medications mebendazole and albendazole are now used to treat humari trichinosis. The drugs are active against only mature helminths and non-encysted muscle larvae. The original oil suspension of micronized mebendazole was.found to have 100% efficacy against trichinosis in albino mice in the late muscular phase (encysted larvae) of hyperinvasion after intensive therapy under lifetime diagnostic guidance during and after a treatment cycle. The lifetime diagnostic method used to evaluate the larvicidal activity of anti-trichinosis agents in animals with experimental trichinosis revealed the signs of viaility, established a trend for deatih of Trichinella larvae, and determined their destructive changes.
Asunto(s)
Mebendazol/administración & dosificación , Trichinella spiralis/patogenicidad , Triquinelosis/tratamiento farmacológico , Albendazol/administración & dosificación , Animales , Humanos , Larva/efectos de los fármacos , Larva/patogenicidad , Ratones , Federación de Rusia , Trichinella spiralis/efectos de los fármacos , Triquinelosis/parasitologíaRESUMEN
The problem of echinococcosis has acquired special urgency in Russia in the last 10 years. The dramatically worse epidemiological situation of echinococcosis in the country is suggested by just frequent cases of cystic echinococcosis in the indigenous population of Moscow and its region, including children. Currently, albendazole that is less toxic than mebendazole remains the drug of choice, However, some authors note that E. granulosus larval cysts are moresusceptible to mebendazole than to albendazole. Both drugs mainly show parasitological activity and have no larvicidal effect particularly in larval alveococcosis. Analysis of the results of chemotherapy, with a group of benzimidazole carbamates for echinococcosis in 6 clinical centers from 5 European countries (Italy, Bulgaria, Romania, Greece, and Turkey) over the past 30 years showed that the evaluation of therapeutic effectiveness was overestimated; thus, 40% of all parasitic larval cysts that were considered dead became active again after, 2 years after the treatment. The original oil micronized mebendazole suspension tested by us in albino mice with late-stage larval cystic echinococcosis showed the properties of a highly effective and safe systemic larvicide that caused prompt death in the entire parasite population in the treated animals even in extreme hyperinvasion when the baseline parasite weight was greater than the host's one.
Asunto(s)
Equinococosis/tratamiento farmacológico , Echinococcus granulosus/efectos de los fármacos , Mebendazol/administración & dosificación , Albendazol/administración & dosificación , Animales , Equinococosis/epidemiología , Equinococosis/parasitología , Echinococcus granulosus/patogenicidad , Europa (Continente) , Humanos , Larva/efectos de los fármacos , Larva/patogenicidad , Ratones , Federación de RusiaRESUMEN
The paper describes the synthesis of the new agent G-1697 which is 4-[(benzo-2,1,3-thiadiazolyl-4)amino]-5, 6,7,8-tetrahydrobenzothieno [2,3-d] pyrimidine and the results of testing its acute toxicity and antiparasitic activity on a model of Echinococcus multilocularis invasion at the larval stage in cotton rats. The maximum nonlethal dose of G-1697 was 4.0 g/kg for outbred mice of both sexes whose weight was 14-16 g. Adult cotton rats (males) received the agent with their feed in increasing daily doses for 3 weeks continuously on days 8 to 28 after infection. The daily dose of its active ingredient varied from 0.03 to 0.35 g/kg and averaged 0.12 g/kg (the mean total dose per session was 2.47 g/kg). The baseline weight of parasitic larvocysts (PL) per animal averaged 0.28 g at the baseline. In the treated and control rats sacrificed 34 days following infection, the mean mass of PL per animal was 0.95 and 7.51 g, respectively. In the cotton rats treated with G-1697, the suppressed growth index calculated by three parameters (moderate, maximum, and minimum mass of PL in the animals of the comparable groups after treatment with regard to the similar baseline variables) was 90.8, 91.0 and 92.7, respectively, versus the controls. Among all PL found in each animal, its death was approximately 70-90% in the treated rats.
Asunto(s)
Anticestodos/síntesis química , Pirimidinas/síntesis química , Tiadiazoles/síntesis química , Animales , Anticestodos/uso terapéutico , Anticestodos/toxicidad , Relación Dosis-Respuesta a Droga , Evaluación Preclínica de Medicamentos , Equinococosis/tratamiento farmacológico , Equinococosis/parasitología , Echinococcus/efectos de los fármacos , Femenino , Larva/efectos de los fármacos , Masculino , Ratones , Pirimidinas/uso terapéutico , Pirimidinas/toxicidad , Sigmodontinae , Tiadiazoles/uso terapéutico , Tiadiazoles/toxicidad , Factores de TiempoRESUMEN
Describes specific features of development of larval multi-cystic echinococcosis in some laboratory animals infected with the Kamchatka and Kazakhstan strains of E. multilocularis. Analyses the efficacy of chemotherapy in animals infected with various strains of E. multilocularis.