Effect Of Triclabendazole Research Articles

Ultrastructural Changes in the Tegument and Tissues of Fasciola hepatica Adults and Their Eggs Due to the Effect of an Ethyl Acetate Extract of Artemisia ludoviciana Nutt. spp Mexicana.

The objective of the present work was to evaluate the effect of an ethyl acetate extract of Artemisia ludoviciana on the viability of adult Fasciola hepatica parasites and eggs. The collection of plant material was performed as described in previous reports. The dried material was macerated with ethyl acetate. Ovicidal assays were performed at concentrations of 100, 200, 300, 400 and 500mg/L A. ludoviciana extract. Bioassays of fasciolicidal efficacy in adult specimens of F. hepatica were performed at extract concentrations of 125, 250, 375 and 500mg/L. The effects of triclabendazole, a reference drug, and artemisinin were also evaluated. The ovicidal effectiveness of the extracts obtained after 16 h of incubation at concentrations of 100, 200, 300, 400 and 500mg/L was 48%, 52%, 87%, 89% and 92%, respectively (p < 0.05), and the fasciolicidal efficiencies during the first 24h post-treatment ranged from 82 to 100% (p < 0.05). In both cases, scanning electron microscopy revealed damage to the shells of the eggs treated with the extract, compromising their stability. In adult fasciolae, alterations to the integument that resulted in its erosion and detachment were observed. Histopathological studies of the affected specimens revealed damage to the tegumentary and subtegumentary cells and alterations in the ovaries, testicles and intestine. This damage was more severe after treatment with the extract than after treatment with the other compounds. Extract of A. ludoviciana causes damage to the tegument, intestine, ovaries, testes and eggs of F. hepatica.

Effect of Triclabendazole and Dexamethasone on Ovine Fascioliasis

Thirty sheep in a flock suffering from fascioliasis were selected for the trial . Clinical findings, hematological, biochemical and fecal investigations were conducted. These animals were equally divided into two groups, the 1st group was given the flukecide triclabendazole alone, at a rate of 12mg/kg body weight orally and the 2nd group was given the same dose orally together with dexamethasone at a rate 0.5 mg / kg body weight I/M. Results showed that the 2nd group gave the quickest and the best response in the treatment. This could be explained that the use of corticosteroid assisted the triclabendazole in preventing immune damage and fibroplasias inflicted by the liver flukes beside to improvement metabolic actions of the animal.

Effects of triclabendazole on secretion of danofloxacin and moxidectin into the milk of sheep: Role of triclabendazole metabolites as inhibitors of the ruminant ABCG2 transporter

ATP-binding cassette transporter G2/breast cancer resistance protein (ABCG2/BCRP) mediates drug–drug interactions that affect the secretion of drugs into milk. The aims of this study were: (1) to determine whether the major plasma metabolites of the flukicide triclabendazole (TCBZ), triclabendazole sulfoxide (TCBZSO) and triclabendazole sulfone (TCBZSO2), inhibit ovine and bovine ABCG2 and its Y581S variant in vitro, and (2) to examine whether coadministration of TCBZ with the ABCG2 substrates danofloxacin (a fluoroquinolone) and moxidectin (a milbemycin) affects the secretion of these drugs into the milk of sheep.TCBZSO and TCBZSO2 inhibited ruminant ABCG2 in vitro by reversing the reduced mitoxantrone accumulation and reducing basal to apical transport of nitrofurantoin in cells transduced with bovine variants (S581 and Y581) and the ovine variant of ABCG2. Coadministration of TCBZ with moxidectin or danofloxacin to sheep resulted in significantly reduced levels of moxidectin, but not danofloxacin, in the milk of TCBZ-treated sheep compared to sheep administered moxidectin or danofloxacin alone. The milk area under concentration time curve (AUC 0–48h) was 2.99±1.41μgh/mL in the group treated with TCBZ and moxidectin, and 7.75±3.58μgh/mL in the group treated with moxidectin alone. The AUC (0–48h) milk/plasma ratio was 37% lower in the group treated with TCBZ and moxidectin (7.34±1.51) than in the group treated with moxidectin alone (11.68±3.61). TCBZ metabolites appear to inhibit ruminant ABCG2 and affect the secretion of ABCG2 substrates into milk of sheep.

Effect of Triclabendazole and Levamisole on Experimental Hydatic Cyst in Rat

Problem statement: Hydatidosis has dispersed worldly and is one of the common dangerous diseases between human and animals and is found abundantly in areas that human, dogs and herbivorous are in close relationship. Approach: In this study, firstly, 32 rats were divided into two groups of control and case and 2000 protoscolices were injected into peritoneal hole. After two months, rats of case group were feed by drinkable 5 mL Triclabendazole + 3.41 mL Levamisole for 60 days. Then after 6 months of contamination period, rats of control group and case group killed by anesthetic drug then necropsy and guts inspection of hydatid cyst was implemented. Results: The results show that in livers of control group there are 2 cysts, in kidneys 9 cysts and in lungs 87 cases. Average of contamination in this group to hydatid cyst was 32.6 but in case group there were in liver on cyst, in kidneys 5 cysts and in lungs 63 cysts. Average of guts contamination to hydatid cyst in case group was 23. Conclusion: Analyzing results in case and control groups shows that Triclabendazole + Levamisole drugs effect was 30% that this amount is not sufficient for hydatid cyst treatment.

Effect of Triclabendazole and Levamisole on Experimental Hydatic Cyst in Rat

Problem statement: Hydatidosis has dispersed worldly and is one of the common dangerous diseases between human and animals and is found abundantly in areas that human, dogs and herbivorous are in close relationship. Approach: In this study, firstly, 32 rats were divided into two groups of control and case and 2000 protoscolices were injected into peritoneal hole. After two months, rats of case group were feed by drinkable 5 mL Triclabendazole + 3.41 mL Levamisole for 60 days. Then after 6 months of contamination period, rats of control group and case group killed by anesthetic drug then necropsy and guts inspection of hydatid cyst was implemented. Results: The results show that in livers of control group there are 2 cysts, in kidneys 9 cysts and in lungs 87 cases. Average of contamination in this group to hydatid cyst was 32.6 but in case group there were in liver on cyst, in kidneys 5 cysts and in lungs 63 cysts. Average of guts contamination to hydatid cyst in case group was 23. Conclusion: Analyzing results in case and control groups shows that Triclabendazole + Levamisole drugs effect was 30% that this amount is not sufficient for hydatid cyst treatment.

Fasciola hepatica: ultrastructural effects of a combination of triclabendazole and clorsulon against mature fluke

A study has been carried out to investigate the ultrastructural effects of triclabendazole (TCBZ) at half-normal concentration, clorsulon at half-normal concentration, and a combination of these two drugs against mature Fasciola hepatica. The Cullompton TCBZ-susceptible isolate was used for these experiments. Flukes were incubated for 24 h in vitro in TCBZ sulphoxide (7.5 microg/ml), clorsulon (5 microg/ml), or a combination of the two drugs. For the in vivo experiment, rats were dosed with TCBZ (5 mg/kg body weight), clorsulon (5 mg/kg body weight), or a combination of the two drugs, and flukes recovered after 48 h. Fine structural changes within the tegumental syncytium and tegumental cells were assessed by transmission electron microscopy. Treatment with the combination of drugs produced greater disruption to the flukes than the individual drugs at half-normal concentrations, both in vivo and in vitro; also than TCBZ.SO at normal concentration in vitro. The changes observed aid in the understanding of the gross changes to the tegumental surface described previously (Meaney M, Allister J, McKinstry B, McLaughlin K, Brennan GP, Forbes AB, Fairweather I. Parasitol Res 99:609-621, 2006). The results indicate that there are additive effects between TCBZ and clorsulon and suggest that the use of drug combinations would be of value in the treatment of TCBZ-resistant fluke.

The effect of triclabendazole (“Fasinex”) on protein synthesis by the liver fluke, Fasciola hepatica

The effect of the active sulphoxide metabolite of the anthelmintic triclabendazole (TCBZ-SX, 15–50 μg ml −1) on the incorporation of radioactively labelled [ 14C] leucine by adult Fasciola hepatica tissue slices was measured by liquid scintillation counting. In addition, the ability of the microfilament-disrupting drug, cytochalasin B, and the microtubule-disrupting drug, tubulozole-C, to inhibit protein synthesis, was assessed by similar methods and compared with TCBZ-SX. The established protein synthesis inhibitors, cycloheximide and actinomycin D were used as positive controls. All the drugs showed a significant inhibition of protein synthesis, albeit to different extents; however, TCBZ-SX was the most potent, with no significant difference between its effect and that of cycloheximide or actinomycin D. Moreover, the concentration of TCBZ-SX, above 15 μg ml −1, had little further influence on incorporation of [ 14C] leucine. This investigation demonstrates the inhibitory effect of TCBZ-SX, cytochalasin B and tubulozole-C on protein synthesis in F. hepatica and confirms the qualitative observations made in several previous ultrastructural studies