Vermox
Assessment of benzimidazole binding to individual recombinant tubulin isotypes from Haemonchus contortus.

Oxberry ME, Gear TG, Prichard RK.

Molecular Immunology Laboratory, School of Biomedical Sciences, Curtin University, Perth, Western Australia. moxberry yahoo.com

One a- and 2 beta-tubulin isotypes (isotypes 1 and 2) from the parasitic nematode Haemonchus contortus were artificially expressed in E. coli and purified to obtain tubulin that was capable of polymerizing into microtubules. Binding of [14C] mebendazole (MBZ), a benzimidazole compound, to each individual unpolymerized isotype and to microtubules polymerized from recombinant alpha- and beta-tubulin was assessed and Kd and Bmax values determined. Mebendazole bound to the individual tubulin isotypes with a stoichiometry of 1:1. Binding occurred with highest affinity to alpha-tubulin followed by beta-tubulin isotype 2 and beta-tubulin isotype 1 indicating that alpha-tubulin may play a role in benzimidazole binding to microtubules. Upon polymerization of alpha- and beta-tubulin isotype 2 into microtubules the stoichiometry of binding increased to 2:1 (mebendazole : tubulin) while binding affinity remained the same. Mebendazole binding to alpha/beta-isotype 1 microtubules remained unchanged following polymerization. The increase in the number of benzimidazole receptors on alpha/beta-isotype 2 microtubules suggests the formation of a new benzimidazole receptor upon polymerization.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11444621&dopt=Abstract mebendazole Vermox



Vermox
4-Amino-3-(3'-methoxycarbonyl-2'-thioureido)benzophenone, a prodrug of mebendazole.

Dawson M, Watson TR.

The compound 4-amino-3-(3'-methoxycarbonyl-2'-thioureido) benzophenone has shown promise as a prodrug of the anthelmintic mebendazole. The compound is stable in acid and neutral media and is rapidly hydrolysed in base. An HPLC assay procedure for mebendazole, the prodrug and their known or expected metabolites and degradation products in aqueous media and rat blood has been developed. The prodrug administrated orally to rats is rapidly converted to mebendazole. The area under the blood level versus time curve of mebendazole, in rats dosed with the prodrug, is more than twice that obtained after dosing rats with an equimolar amount of mebendazole. Only the prodrug, mebendazole and known metabolites of mebendazole are detected in rats dosed with the prodrug.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6673970&dopt=Abstract mebendazole Vermox



Vermox
The metabolic and pharmacokinetic disposition of mebendazole in the rat.

Allan RJ, Watson TR.

The metabolism and pharmacokinetics of mebendazole was studied in rats using [2'-3H]-mebendazole (biologically stable; specific activity 383.9 (mCi/mMol) and [2-14C]-mebendazole (specific activity 2.57 mCi/mMol). Analyses were performed by high pressure liquid chromatography and liquid scintillation spectrometry. About 85% of an intravenous dose was eliminated with the bile and the remainder with the urine. The majority of the dose was recovered as conjugated metabolites. The major metabolite (methyl-5(6)-(alpha-hydroxybenzyl)-2-benzimidazole carbamate) accounted for about 77% of the total recovered and 99% of it was conjugated. Anaerobic metabolism studies conducted in vitro with intestinal microorganisms obtained from rats indicated that metabolism of mebendazole did not occur in the gut, but that the intestinal microflora was able to hydrolyse conjugated metabolites which were eliminated with the bile. Mebendazole was found to have a biphasic elimination profile after intravenous administration. Its terminal plasma elimination half-life was 3.2 hours and its re-distribution half-life was 0.4 hour. After oral administration, as a solution in aqueous dimethyl sulphoxide, a bioavailability of 53% was obtained.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6673974&dopt=Abstract mebendazole Vermox



Vermox
Spinal hydatid cysts.

Pamir MN, Akalan N, Ozgen T, Erbengi A.

Eleven cases of spinal hydatid cyst are reported. The patients were admitted with symptoms of compression of the spinal cord. The cysts were localized epidurally in 10 patients and intradurally but extramedullarily in one, and were confirmed histopatholgically after surgical intervention. The results are compared with those reported in the literature. Six of the patients were female and five were male. Their ages ranged from 10 to 65 years. All of the patients were treated surgically, with an incidence of cyst recurrence of 18% and no mortality. Mebendazole (Vermox) was given to two of the patients after their operations.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6689810&dopt=Abstract mebendazole Vermox



Vermox
[Chemotherapy of human echinococcosis]

[Article in German]

Bahr R, Ammann R, Bircher J, Eckert J.

In human echinococcosis, today as in the past, surgical removal of the parasite remains the treatment of choice. Beside certain conditions, adjuvant chemotherapy with Vermox is indicated for echinococcus multilocularis as well as echinococcus granulosus. A substantial decrease of the echinococcal parasite mass under Mebendazole is not yet known. Nevertheless jaundiced patients with diffuse liver infestation with echinococcus multilocularis became jaundice-free and able to work. Mebendazole toleration is very good. A closely interrelated medical control of patients under Mebendazole therapy ought to be interdisciplinarily carried through between internists and surgeons.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6714007&dopt=Abstract mebendazole Vermox



Vermox
Liquid chromatography with electrochemical detection for monitoring mebendazole and hydroxymebendazole in echinococcosis patients.

Oosterhuis B, Wetsteyn JC, van Boxtel CJ.

A sensitive method is described for the simultaneous determination of mebendazole and hydroxymebendazole using flubendazole as an internal standard. The analytes were isolated with a single chloroform extraction from 1.0 ml of alkalinized plasma or cyst liquid samples. Separation and quantitation were performed with high-performance liquid chromatography with electrochemical detection. The limit of detection for mebendazole and hydroxymebendazole was approximately 5 and 2.5 ng/ml, respectively. The accuracy of the method was confirmed for mebendazole by a good correlation with an existing radioimmunoassay method. The method was applied for monitoring mebendazole therapy in echinococcosis patients. The results presented support the necessity of such monitoring, as most of the observed peak plasma concentrations did not reach the level regarded as minimal for therapeutic effect.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6740740&dopt=Abstract mebendazole Vermox