Fasciola hepatica: Mebendazole and Thiabendazole Pharmacokinetics in Sheep
Pharmacokinetics of the two anthelmintic drugs mebendazole and thiabendazole were determined in sheep before and 4, 8, 13, 19, and 25 weeks after an infestation of animals by an oral administration of 150 metacercariae of Fasciola hepatica. The parasitic pathology was ascertained by the increase in...
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| Veröffentlicht in: | Experimental parasitology 1994-09, Vol.79 (2), p.166-176 |
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| description | Pharmacokinetics of the two anthelmintic drugs mebendazole and thiabendazole were determined in sheep before and 4, 8, 13, 19, and 25 weeks after an infestation of animals by an oral administration of 150 metacercariae of
Fasciola hepatica. The parasitic pathology was ascertained by the increase in plasma enzyme activities of glutamate dehydrogenase and γ-glutamyltransferase. After oral administration of mebendazole (25 mg · kg
−1), the parent drug and especially its reduced metabolite were present in plasma of animals. A significant 1.5- to 2.7-fold increase in the mean residence time occurred by Weeks 13 to 25 postinfection. This change was related to decreases in both the elimination from the pharmacokinetic compartment representing the reduced metabolite and the area under the curve of plasma metabolite concentration versus time. A 59% decrease in MBZ reduction was demonstrated in liver microsomes prepared from 12-week-infected sheep. This reductase activity was characterized by NADPH dependency and a pH peak activity of 6.0 and was competitively inhibited by daunomycin. In sheep receiving a 50 mg · kg
−1 oral dose of thiabendazole, fascioliasis provoked only decreased plasma concentrations of the metabolite 5-hydroxythiabendazole by Weeks 4 to 25 postinfection. This change parallels an increase in urinary excretion of free metabolite but this is of minor significance in the general fate of the drug because of the prevalence of excretion as conjugates. In summary, fascioliasis appears to have more of an effect on the pharmacokinetics of mebendazole, a drug intensively metabolized by the liver into a metabolite present at high concentrations in the plasma of animals and humans. |
| doi_str_mv | 10.1006/expr.1994.1076 |
| format | Article |
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Fasciola hepatica. The parasitic pathology was ascertained by the increase in plasma enzyme activities of glutamate dehydrogenase and γ-glutamyltransferase. After oral administration of mebendazole (25 mg · kg
−1), the parent drug and especially its reduced metabolite were present in plasma of animals. A significant 1.5- to 2.7-fold increase in the mean residence time occurred by Weeks 13 to 25 postinfection. This change was related to decreases in both the elimination from the pharmacokinetic compartment representing the reduced metabolite and the area under the curve of plasma metabolite concentration versus time. A 59% decrease in MBZ reduction was demonstrated in liver microsomes prepared from 12-week-infected sheep. This reductase activity was characterized by NADPH dependency and a pH peak activity of 6.0 and was competitively inhibited by daunomycin. In sheep receiving a 50 mg · kg
−1 oral dose of thiabendazole, fascioliasis provoked only decreased plasma concentrations of the metabolite 5-hydroxythiabendazole by Weeks 4 to 25 postinfection. This change parallels an increase in urinary excretion of free metabolite but this is of minor significance in the general fate of the drug because of the prevalence of excretion as conjugates. In summary, fascioliasis appears to have more of an effect on the pharmacokinetics of mebendazole, a drug intensively metabolized by the liver into a metabolite present at high concentrations in the plasma of animals and humans.</description><identifier>ISSN: 0014-4894</identifier><identifier>EISSN: 1090-2449</identifier><identifier>DOI: 10.1006/expr.1994.1076</identifier><identifier>PMID: 7914496</identifier><identifier>CODEN: EXPAAA</identifier><language>eng</language><publisher>San Diego, CA: Elsevier Inc</publisher><subject>ACTIVIDAD ENZIMATICA ; ACTIVITE ENZYMATIQUE ; Administration, Oral ; Animals ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; Antiparasitic agents ; APPLICATION METHODS ; BENZIMIDAZOLE ; BENZIMIDAZOLES ; Biological and medical sciences ; BLOOD PLASMA ; BODY WEIGHT ; CYTOPLASMIC ORGANELLES ; DURACION ; DURATION ; DUREE ; ENZYMIC ACTIVITY ; EXCRECION ; EXCRETION ; FARMACOLOGIA ; FASCIOLA HEPATICA ; Fascioliasis - drug therapy ; Fascioliasis - metabolism ; Fascioliasis - veterinary ; FOIE ; GAMMA-GLUTAMYLTRANSFERASE ; gamma-Glutamyltransferase - blood ; GLUTAMATE DEHYDROGENASE ; Glutamate Dehydrogenase - blood ; GLUTAMATE DESHYDROGENASE ; GLUTAMATO DEHIDROGENASA ; HIGADO ; INFECTIONS ; Life Sciences ; LIVER ; Liver - enzymology ; Liver - metabolism ; Liver - parasitology ; LIVER FLUKES ; Male ; Mebendazole - administration & dosage ; Mebendazole - pharmacokinetics ; Mebendazole - therapeutic use ; Medical sciences ; METABOLITE ; METABOLITES ; METABOLITOS ; METACERCARIAE ; METHODE D'APPLICATION ; METODOS DE APLICACION ; MICROSOMES ; Microsomes, Liver - enzymology ; ORAL ADMINISTRATION ; ORGANITE CELLULAIRE ; ORGANULOS CITOPLASMICOS ; ORINA ; OVIN ; OVINOS ; Oxidation-Reduction ; PATHOGENESE ; PATHOGENESIS ; PATOGENESIS ; PESO ; PHARMACOLOGIE ; PHARMACOLOGY ; Pharmacology. Drug treatments ; PLASMA SANGUIN ; PLASMA SANGUINEO ; POIDS ; SHEEP ; Sheep Diseases - drug therapy ; Sheep Diseases - metabolism ; THIABENDAZOLE ; Thiabendazole - administration & dosage ; Thiabendazole - pharmacokinetics ; Thiabendazole - therapeutic use ; TIABENDAZOL ; TRANSFERASAS ; TRANSFERASE ; TRANSFERASES ; TREMATODA ; URINE ; WEIGHT</subject><ispartof>Experimental parasitology, 1994-09, Vol.79 (2), p.166-176</ispartof><rights>1994 Academic Press</rights><rights>1994 INIST-CNRS</rights><rights>Distributed under a Creative Commons Attribution 4.0 International License</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c421t-ac0bbbefb1dc717f5a76f6b5b92c1d78061c769d208c883c452ab9d30e87fa493</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1006/expr.1994.1076$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>230,314,780,784,885,3549,27923,27924,45994</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=4259801$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/7914496$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink><backlink>$$Uhttps://hal.inrae.fr/hal-02712426$$DView record in HAL$$Hfree_for_read</backlink></links><search><creatorcontrib>Galtier, P.</creatorcontrib><creatorcontrib>Coulet, M.</creatorcontrib><creatorcontrib>Sutra, J.F.</creatorcontrib><creatorcontrib>Birosauveur, B.</creatorcontrib><creatorcontrib>Alvinerie, M.</creatorcontrib><title>Fasciola hepatica: Mebendazole and Thiabendazole Pharmacokinetics in Sheep</title><title>Experimental parasitology</title><addtitle>Exp Parasitol</addtitle><description>Pharmacokinetics of the two anthelmintic drugs mebendazole and thiabendazole were determined in sheep before and 4, 8, 13, 19, and 25 weeks after an infestation of animals by an oral administration of 150 metacercariae of
Fasciola hepatica. The parasitic pathology was ascertained by the increase in plasma enzyme activities of glutamate dehydrogenase and γ-glutamyltransferase. After oral administration of mebendazole (25 mg · kg
−1), the parent drug and especially its reduced metabolite were present in plasma of animals. A significant 1.5- to 2.7-fold increase in the mean residence time occurred by Weeks 13 to 25 postinfection. This change was related to decreases in both the elimination from the pharmacokinetic compartment representing the reduced metabolite and the area under the curve of plasma metabolite concentration versus time. A 59% decrease in MBZ reduction was demonstrated in liver microsomes prepared from 12-week-infected sheep. This reductase activity was characterized by NADPH dependency and a pH peak activity of 6.0 and was competitively inhibited by daunomycin. In sheep receiving a 50 mg · kg
−1 oral dose of thiabendazole, fascioliasis provoked only decreased plasma concentrations of the metabolite 5-hydroxythiabendazole by Weeks 4 to 25 postinfection. This change parallels an increase in urinary excretion of free metabolite but this is of minor significance in the general fate of the drug because of the prevalence of excretion as conjugates. In summary, fascioliasis appears to have more of an effect on the pharmacokinetics of mebendazole, a drug intensively metabolized by the liver into a metabolite present at high concentrations in the plasma of animals and humans.</description><subject>ACTIVIDAD ENZIMATICA</subject><subject>ACTIVITE ENZYMATIQUE</subject><subject>Administration, Oral</subject><subject>Animals</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Antiparasitic agents</subject><subject>APPLICATION METHODS</subject><subject>BENZIMIDAZOLE</subject><subject>BENZIMIDAZOLES</subject><subject>Biological and medical sciences</subject><subject>BLOOD PLASMA</subject><subject>BODY WEIGHT</subject><subject>CYTOPLASMIC ORGANELLES</subject><subject>DURACION</subject><subject>DURATION</subject><subject>DUREE</subject><subject>ENZYMIC ACTIVITY</subject><subject>EXCRECION</subject><subject>EXCRETION</subject><subject>FARMACOLOGIA</subject><subject>FASCIOLA HEPATICA</subject><subject>Fascioliasis - drug therapy</subject><subject>Fascioliasis - metabolism</subject><subject>Fascioliasis - veterinary</subject><subject>FOIE</subject><subject>GAMMA-GLUTAMYLTRANSFERASE</subject><subject>gamma-Glutamyltransferase - blood</subject><subject>GLUTAMATE DEHYDROGENASE</subject><subject>Glutamate Dehydrogenase - blood</subject><subject>GLUTAMATE DESHYDROGENASE</subject><subject>GLUTAMATO DEHIDROGENASA</subject><subject>HIGADO</subject><subject>INFECTIONS</subject><subject>Life Sciences</subject><subject>LIVER</subject><subject>Liver - enzymology</subject><subject>Liver - metabolism</subject><subject>Liver - parasitology</subject><subject>LIVER FLUKES</subject><subject>Male</subject><subject>Mebendazole - administration & dosage</subject><subject>Mebendazole - pharmacokinetics</subject><subject>Mebendazole - therapeutic use</subject><subject>Medical sciences</subject><subject>METABOLITE</subject><subject>METABOLITES</subject><subject>METABOLITOS</subject><subject>METACERCARIAE</subject><subject>METHODE D'APPLICATION</subject><subject>METODOS DE APLICACION</subject><subject>MICROSOMES</subject><subject>Microsomes, Liver - enzymology</subject><subject>ORAL ADMINISTRATION</subject><subject>ORGANITE CELLULAIRE</subject><subject>ORGANULOS CITOPLASMICOS</subject><subject>ORINA</subject><subject>OVIN</subject><subject>OVINOS</subject><subject>Oxidation-Reduction</subject><subject>PATHOGENESE</subject><subject>PATHOGENESIS</subject><subject>PATOGENESIS</subject><subject>PESO</subject><subject>PHARMACOLOGIE</subject><subject>PHARMACOLOGY</subject><subject>Pharmacology. Drug treatments</subject><subject>PLASMA SANGUIN</subject><subject>PLASMA SANGUINEO</subject><subject>POIDS</subject><subject>SHEEP</subject><subject>Sheep Diseases - drug therapy</subject><subject>Sheep Diseases - metabolism</subject><subject>THIABENDAZOLE</subject><subject>Thiabendazole - administration & dosage</subject><subject>Thiabendazole - pharmacokinetics</subject><subject>Thiabendazole - therapeutic use</subject><subject>TIABENDAZOL</subject><subject>TRANSFERASAS</subject><subject>TRANSFERASE</subject><subject>TRANSFERASES</subject><subject>TREMATODA</subject><subject>URINE</subject><subject>WEIGHT</subject><issn>0014-4894</issn><issn>1090-2449</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1994</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp1kU2LFDEQhoMo67h69SAIfRDBQ49JJp0Pb8viusqIwu6eQyVdbUd7Om0ys6i_3jQ9jCdPIfU-KaqeEPKc0TWjVL7FX1NaM2NEuSr5gKwYNbTmQpiHZEUpE7XQRjwmT3L-TinVjIszcqYMK4RckU9XkH2IA1Q9TrAPHt5Vn9Hh2MKfOGAFY1vd9gH-Vb72kHbg448wYuFzFcbqpkecnpJHHQwZnx3Pc3J39f728rrefvnw8fJiW3vB2b4GT51z2DnWesVU14CSnXSNM9yzVmkqmVfStJxqr_XGi4aDM-2GolYdCLM5J2-Wvj0MdkphB-m3jRDs9cXWzjXKVdmSy3tW2NcLO6X484B5b3chexwGGDEeslVScqlkU8D1AvoUc07YnTozamfRdhZtZ9F2Fl0evDx2Prgdtif8aLbkr455EQxDl2D0IZ8wwRuj6TzgiwXrIFr4lgpyd2MaJhvGS6iXEIvO-4DJlr_C0WMbEvq9bWP433h_AbRyoQM</recordid><startdate>19940901</startdate><enddate>19940901</enddate><creator>Galtier, P.</creator><creator>Coulet, M.</creator><creator>Sutra, J.F.</creator><creator>Birosauveur, B.</creator><creator>Alvinerie, M.</creator><general>Elsevier Inc</general><general>Elsevier</general><scope>FBQ</scope><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><scope>1XC</scope></search><sort><creationdate>19940901</creationdate><title>Fasciola hepatica: Mebendazole and Thiabendazole Pharmacokinetics in Sheep</title><author>Galtier, P. ; Coulet, M. ; Sutra, J.F. ; Birosauveur, B. ; Alvinerie, M.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c421t-ac0bbbefb1dc717f5a76f6b5b92c1d78061c769d208c883c452ab9d30e87fa493</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1994</creationdate><topic>ACTIVIDAD ENZIMATICA</topic><topic>ACTIVITE ENZYMATIQUE</topic><topic>Administration, Oral</topic><topic>Animals</topic><topic>Antibiotics. Antiinfectious agents. Antiparasitic agents</topic><topic>Antiparasitic agents</topic><topic>APPLICATION METHODS</topic><topic>BENZIMIDAZOLE</topic><topic>BENZIMIDAZOLES</topic><topic>Biological and medical sciences</topic><topic>BLOOD PLASMA</topic><topic>BODY WEIGHT</topic><topic>CYTOPLASMIC ORGANELLES</topic><topic>DURACION</topic><topic>DURATION</topic><topic>DUREE</topic><topic>ENZYMIC ACTIVITY</topic><topic>EXCRECION</topic><topic>EXCRETION</topic><topic>FARMACOLOGIA</topic><topic>FASCIOLA HEPATICA</topic><topic>Fascioliasis - drug therapy</topic><topic>Fascioliasis - metabolism</topic><topic>Fascioliasis - veterinary</topic><topic>FOIE</topic><topic>GAMMA-GLUTAMYLTRANSFERASE</topic><topic>gamma-Glutamyltransferase - blood</topic><topic>GLUTAMATE DEHYDROGENASE</topic><topic>Glutamate Dehydrogenase - blood</topic><topic>GLUTAMATE DESHYDROGENASE</topic><topic>GLUTAMATO DEHIDROGENASA</topic><topic>HIGADO</topic><topic>INFECTIONS</topic><topic>Life Sciences</topic><topic>LIVER</topic><topic>Liver - enzymology</topic><topic>Liver - metabolism</topic><topic>Liver - parasitology</topic><topic>LIVER FLUKES</topic><topic>Male</topic><topic>Mebendazole - administration & dosage</topic><topic>Mebendazole - pharmacokinetics</topic><topic>Mebendazole - therapeutic use</topic><topic>Medical sciences</topic><topic>METABOLITE</topic><topic>METABOLITES</topic><topic>METABOLITOS</topic><topic>METACERCARIAE</topic><topic>METHODE D'APPLICATION</topic><topic>METODOS DE APLICACION</topic><topic>MICROSOMES</topic><topic>Microsomes, Liver - enzymology</topic><topic>ORAL ADMINISTRATION</topic><topic>ORGANITE CELLULAIRE</topic><topic>ORGANULOS CITOPLASMICOS</topic><topic>ORINA</topic><topic>OVIN</topic><topic>OVINOS</topic><topic>Oxidation-Reduction</topic><topic>PATHOGENESE</topic><topic>PATHOGENESIS</topic><topic>PATOGENESIS</topic><topic>PESO</topic><topic>PHARMACOLOGIE</topic><topic>PHARMACOLOGY</topic><topic>Pharmacology. Drug treatments</topic><topic>PLASMA SANGUIN</topic><topic>PLASMA SANGUINEO</topic><topic>POIDS</topic><topic>SHEEP</topic><topic>Sheep Diseases - drug therapy</topic><topic>Sheep Diseases - metabolism</topic><topic>THIABENDAZOLE</topic><topic>Thiabendazole - administration & dosage</topic><topic>Thiabendazole - pharmacokinetics</topic><topic>Thiabendazole - therapeutic use</topic><topic>TIABENDAZOL</topic><topic>TRANSFERASAS</topic><topic>TRANSFERASE</topic><topic>TRANSFERASES</topic><topic>TREMATODA</topic><topic>URINE</topic><topic>WEIGHT</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Galtier, P.</creatorcontrib><creatorcontrib>Coulet, M.</creatorcontrib><creatorcontrib>Sutra, J.F.</creatorcontrib><creatorcontrib>Birosauveur, B.</creatorcontrib><creatorcontrib>Alvinerie, M.</creatorcontrib><collection>AGRIS</collection><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>Hyper Article en Ligne (HAL)</collection><jtitle>Experimental parasitology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Galtier, P.</au><au>Coulet, M.</au><au>Sutra, J.F.</au><au>Birosauveur, B.</au><au>Alvinerie, M.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Fasciola hepatica: Mebendazole and Thiabendazole Pharmacokinetics in Sheep</atitle><jtitle>Experimental parasitology</jtitle><addtitle>Exp Parasitol</addtitle><date>1994-09-01</date><risdate>1994</risdate><volume>79</volume><issue>2</issue><spage>166</spage><epage>176</epage><pages>166-176</pages><issn>0014-4894</issn><eissn>1090-2449</eissn><coden>EXPAAA</coden><abstract>Pharmacokinetics of the two anthelmintic drugs mebendazole and thiabendazole were determined in sheep before and 4, 8, 13, 19, and 25 weeks after an infestation of animals by an oral administration of 150 metacercariae of
Fasciola hepatica. The parasitic pathology was ascertained by the increase in plasma enzyme activities of glutamate dehydrogenase and γ-glutamyltransferase. After oral administration of mebendazole (25 mg · kg
−1), the parent drug and especially its reduced metabolite were present in plasma of animals. A significant 1.5- to 2.7-fold increase in the mean residence time occurred by Weeks 13 to 25 postinfection. This change was related to decreases in both the elimination from the pharmacokinetic compartment representing the reduced metabolite and the area under the curve of plasma metabolite concentration versus time. A 59% decrease in MBZ reduction was demonstrated in liver microsomes prepared from 12-week-infected sheep. This reductase activity was characterized by NADPH dependency and a pH peak activity of 6.0 and was competitively inhibited by daunomycin. In sheep receiving a 50 mg · kg
−1 oral dose of thiabendazole, fascioliasis provoked only decreased plasma concentrations of the metabolite 5-hydroxythiabendazole by Weeks 4 to 25 postinfection. This change parallels an increase in urinary excretion of free metabolite but this is of minor significance in the general fate of the drug because of the prevalence of excretion as conjugates. In summary, fascioliasis appears to have more of an effect on the pharmacokinetics of mebendazole, a drug intensively metabolized by the liver into a metabolite present at high concentrations in the plasma of animals and humans.</abstract><cop>San Diego, CA</cop><pub>Elsevier Inc</pub><pmid>7914496</pmid><doi>10.1006/expr.1994.1076</doi><tpages>11</tpages></addata></record> |
| fulltext | fulltext |
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| ispartof | Experimental parasitology, 1994-09, Vol.79 (2), p.166-176 |
| issn | 0014-4894 1090-2449 |
| language | eng |
| recordid | cdi_hal_primary_oai_HAL_hal_02712426v1 |
| source | MEDLINE; ScienceDirect Journals (5 years ago - present) |
| subjects | ACTIVIDAD ENZIMATICA ACTIVITE ENZYMATIQUE Administration, Oral Animals Antibiotics. Antiinfectious agents. Antiparasitic agents Antiparasitic agents APPLICATION METHODS BENZIMIDAZOLE BENZIMIDAZOLES Biological and medical sciences BLOOD PLASMA BODY WEIGHT CYTOPLASMIC ORGANELLES DURACION DURATION DUREE ENZYMIC ACTIVITY EXCRECION EXCRETION FARMACOLOGIA FASCIOLA HEPATICA Fascioliasis - drug therapy Fascioliasis - metabolism Fascioliasis - veterinary FOIE GAMMA-GLUTAMYLTRANSFERASE gamma-Glutamyltransferase - blood GLUTAMATE DEHYDROGENASE Glutamate Dehydrogenase - blood GLUTAMATE DESHYDROGENASE GLUTAMATO DEHIDROGENASA HIGADO INFECTIONS Life Sciences LIVER Liver - enzymology Liver - metabolism Liver - parasitology LIVER FLUKES Male Mebendazole - administration & dosage Mebendazole - pharmacokinetics Mebendazole - therapeutic use Medical sciences METABOLITE METABOLITES METABOLITOS METACERCARIAE METHODE D'APPLICATION METODOS DE APLICACION MICROSOMES Microsomes, Liver - enzymology ORAL ADMINISTRATION ORGANITE CELLULAIRE ORGANULOS CITOPLASMICOS ORINA OVIN OVINOS Oxidation-Reduction PATHOGENESE PATHOGENESIS PATOGENESIS PESO PHARMACOLOGIE PHARMACOLOGY Pharmacology. Drug treatments PLASMA SANGUIN PLASMA SANGUINEO POIDS SHEEP Sheep Diseases - drug therapy Sheep Diseases - metabolism THIABENDAZOLE Thiabendazole - administration & dosage Thiabendazole - pharmacokinetics Thiabendazole - therapeutic use TIABENDAZOL TRANSFERASAS TRANSFERASE TRANSFERASES TREMATODA URINE WEIGHT |
| title | Fasciola hepatica: Mebendazole and Thiabendazole Pharmacokinetics in Sheep |
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