J Anim Sci. 2001 May;79(5):1288-94.
Effect of ruminal microflora on the biotransformation of netobimin, albendazole, albendazole sulfoxide, and albendazole sulfoxide enantiomers in an artificial rumen.

Capece BP, Calsamiglia S, Castells G, Arboix M, Cristofol C.

Department of Pharmacology and Therapeutics, Veterinary Faculty, Universitat Autonoma de Barcelona, Bellaterra, Spain.

The effect of ruminal flora on the disposition of benzimidazole anthelmintic drugs was studied in dual-flow continuous-culture fermenters (artificial rumens). Six 1,320-mL artificial rumens were inoculated with ruminal fluid and fermentation conditions were maintained constant at 39 degrees C, pH 6.4, solid dilution rate of 5%/h, and liquid dilution rate of 10%/h to simulate standard ruminal fermentation conditions. The study was repeated in two consecutive periods. Two hours after the inoculation of rumen fluid, the fermenters were fed 30 g of a 60:40 forage:concentrate ration. Within each period two fermenters per treatment were immediately dosed with 104 mg of netobimin, 52 mg of albendazole, or 39 mg of albendazole sulfoxide. Concentrations of netobimin, albendazole, albendazole sulfoxide and its enantiomers, and albendazole sulfone were analyzed by high performance liquid chromatography at 0.25, 0.5, 1, 2, 4, 6, and 8 h after dosage. Reductive metabolism by the ruminal bacteria was observed, favoring the production of albendazole, the most potent anthelmintic molecule. No differences in the production or consumption of albendazole sulfoxide enantiomers were observed, indicating that the ruminal bacteria metabolism was not enantioselective. Because benzimidazole anthelmintic drugs are generally administered orally, the ruminal flora play an important role in the bioavailability of these drugs. In our study, increased concentrations of albendazole in the three treatments, due to reductive ruminal biotransformation, suggests that ruminal biotransformation may improve the efficacy of orally administered netobim




J Ocul Pharmacol Ther. 2001 Jun;17(3):287-94.
Treatment of ocular toxocariasis with albendazole.

Barisani-Asenbauer T, Maca SM, Hauff W, Kaminski SL, Domanovits H, Theyer I, Auer H.

Department of Ophthalmology, University of Vienna Medical School, Austria. talin.barisankh-wien.ac.at

The purpose of this study was to evaluate the efficacy of combined albendazole and steroid treatment for uveitis caused by Toxocara canis in immunocompetent patients. Five patients (7 eyes) with ocular larva migrans syndrome (OLM) were used in this study. Toxocariasis was suspected based on clinical manifestations and confirmed by anti-toxocara IgG and Western blot analysis. Systemic albendazole (adults: 800 mg b.i.d.; children: 400 mg b.i.d.) was given in conjunction with steroids. Visual acuity before and after therapy, inflammatory response, side effects and toxicity were evaluated. Treatment resulted in an improved visual acuity in all patients. Mean initial Snellen visual acuity was 20/40, and mean final acuity was 20/20. There were no recurrences of uveitis throughout the observation period (average: 13.8 months; range: 3 days to 24 months). These findings suggest that albendazole, in combination with systemic steroids, is a useful regimen to treat ocular larva migrans syndrome.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11436948&dopt=Abstract albendazole Albenza




Antimicrob Agents Chemother. 2001 Aug;45(8):2256-62.
Echinococcus multilocularis alkaline phosphatase as a marker for metacestode damage induced by in vitro drug treatment with albendazole sulfoxide and albendazole sulfone.

Stettler M, Siles-Lucas M, Sarciron E, Lawton P, Gottstein B, Hemphill A.

Institute of Parasitology, University of Bern, Bern, Switzerland.

Alveolar echinococcosis (AE) is caused by the metacestode stage of the fox tapeworm Echinococcus multilocularis. The disease affects the human liver and occasionally other organs and is fatal if treatment is unsuccessful. The present chemotherapy of AE is based on the administration of benzimidazole carbamate derivatives, such as mebendazole and albendazole. Albendazole treatment has been found to be ineffective in some cases, parasitostatic rather than parasiticidal, and the recurrence rate is rather high. Therefore, chemotherapy usually involves the lifelong uptake of massive doses of albendazole and new treatment options are urgently needed. In order to avoid costly and time-consuming animal experimentation, a first step in searching for novel parasiticidal compounds could be the in vitro drug screening of novel compounds by employing metacestode cultivation. However, presently used techniques (e.g., transmission electron microscopy) for determination of parasite viability involve costly equipment and time-consuming preparation of rather large amounts of parasite material. We therefore searched for a parasite marker which can be easily traced and the presence or absence of which is indicative of parasite viability. In this study we show that the increase of E. multilocularis alkaline phosphatase activity in culture supernatants during in vitro drug treatment with albendazole derivatives correlates with the progressive degeneration and destruction of the metacestode tissue. The inexpensive and rapid assay presented here will serve as an ideal tool for performing first-round in vitro tests on the efficacy of a large number of antiparasitic compo




Parasite. 2001 Jun;8(2 Suppl):S188-90.
Improving bioavailability and anthelmintic activity of albendazole by preparing albendazole-cyclodextrin complexes.

Garcia-Rodriguez JJ, Torrado J, Bolas F.

Departmento de Parasitologia, Facultad de Farmacia, Universidad Complutense, Spain.

The bioavailability and anthelmintic activity of albendazole-cyclodextrin complexes (ABZ-CDC) compared to albendazole suspensions in carboxymethylcellulose (ABZ-CMC) was assessed in a mouse model for Trichinella infections. Swiss CD-1 mice experimentally infected with T. spiralis were treated with both formulations against enteral (adult worms) and parenteral (migrating and encysted larvae). Oral bioavailability was assessed in age matched mice treated with 50 mg/kg of both formulations. The anthelmintic effects and plasma concentration of the active metabolite albendazole-sulphoxide (ABZSO) enantiomer (-) were significantly increased following administration of ABZ-CDC in relation to ABZ-CMC.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11484352&dopt=Abstract albendazole Albenza




Parasite. 2001 Jun;8(2 Suppl):S195-8.
Efficacy of flubendazole and albendazole against Trichinella spiralis in mice.

Chung MS, Joo KH, Quan FS, Kwon HS, Cho SW.

Department of Parasitology, Korea University College of Medicine, 136-705, Seoul, Korea.

Efficacy of flubendazole and albendazole against Trichinella spiralis in mice were studied. ICR mice were experimentally infected with Trichinella spiralis and treated with either flubendazole (FBZ) or albendazole (ABZ) at four different stages of the parasite life-cycle. Oral administration of either FBZ or ABZ at 20 mg/kg and 50 mg/kg on 2 h, 8 h and 24 h (pre-adult stage) after infection eliminated 94.7-100% of adults as determined at necropsy on day 7 post infection (p.i.) and 96.9-100% of larvae on day 45 p.i. FBZ was more effective than ABZ against adult T. spiralis (at 2 to 6 days p.i.), when treated with a dosage of 20 mg/kg for 5 consecutive days (99.4% and 46.0% reduction with respect to the control group). Against migrating larval T. spiralis, FBZ was more effective than ABZ at 20 mg/kg for five consecutive days (on days 11-15 p.i.), and the reduction rate of recovered larvae were 99.6% (FBZ) and 80.8% (ABZ) respectively. FBZ was more effective against early encapsulated larval T. spiralis (at 21 to 25 days p.i.), than ABZ when both were given at 20 mg/kg for five consecutive days (99.8% and 45.4% reduction, respectively). In conclusion, flubendazole was more effective than albendazole against adult and parenteral stages of Trichinella spiralis in mice.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11484354&dopt=Abstract albendazole Albenza




Electrophoresis. 2001 Sep;22(15):3263-9.
Enantioselective analysis of albendazole sulfoxide in cerebrospinal fluid by capillary electrophoresis.

Paias FO, Lanchote VL, Takayanagui OM, Bonato PS.

Departamento de Quimica, Facultade de Filosofia, Ciencias e Letras de Ribeirao Preto, Brazil.

Albendazole (ABZ) is a benzimidazole anthelmintic drug used in the treatment of neurocysticercosis. After oral administration, ABZ is rapidly oxidized to albendazole sulfoxide (ABZSO), which has an asymmetric sulfur center, and later to albendazole sulfone (ABZSO2). ABZSO is the active metabolite responsible for the therapeutic effect of the drug. Previous studies have demonstrated pharmacokinetic differences between the two enantiomers, with the predominance of (+)-ABZSO in human biological fluids. This article describes for the first time the enantioselective analysis of ABZSO in cerebrospinal fluid (CSF) using capillary electrophoresis. The samples were prepared by liquid-liquid extraction using chloroform:isopropanol (8:2 v/v). The resolution of ABZSO enantiomers was obtained with a fused-silica capillary (60 cm x 75 microm ID) using 20 mmol/L Tris, pH 7.0, with 3.0% w/w sulfated beta-cyclodextrin as running buffer. The coefficient of variations and % relative error obtained for both within-day and between-days assays were lower than 15%. The method was linear over the concentration range of 100 to 2,500 ng/mL for each enantiomer, indicating that it is suitable for the analysis of ABZSO enantiomers in CSF from patients medicated with ABZ.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11589289&dopt=Abstract albendazole Albenza




Ann Trop Med Parasitol. 2002 Sep;96(6):595-602.
The influence of the mass administration of diethylcarbamazine, alone or with albendazole, on the prevalence of filarial antigenaemia.

Rajendran R, Sunish IP, Mani TR, Munirathinam A, Abdullah SM, Augustin DJ, Satyanarayana K.

Centre for Research in Medical Entomology (Indian Council of Medical Research), 4 Sarojini Street, Chinna Chokkikulam, Madurai-625 002, India.

The current Indian campaign for the elimination of lymphatic filariasis is largely based on mass drug administration (MDA). As part of this campaign, villagers in the Tirukoilur and Mugaiyur 'blocks' (i.e. revenue units) of Villupuram district, in Tamil Nadu, India, were treated with diethylcarbamazine (DEC), either alone (Mugaiyur) or with albendazole (Tirukoilur), in March 2001. The efficacy of treatment, in each of the two treatment arms, was evaluated by determining the percentages of the subjects who were carrying antigen from adult Wuchereria bancrofti before, 6 months and 12 months after the MDA. In a cross-sectional survey at each time-point, commercial, immunochromatographic tests were used to check 1000-1200, randomly selected, young residents (aged 2-25 years) of 18 index villages for the antigen; at least 300 villagers aged 2-9 years and at least 170 aged 10-25 years from each treatment arm were screened in each survey. Before the MDA, 12.7% of the subjects aged 2-9 years and 23.6% of those aged 10-25 years were found to be positive for the filarial antigen. Although only about 50% of villagers aged 2-9 years were successfully treated, MDA (with DEC alone or DEC plus albendazole) led to a significant (28.7%) reduction in the prevalence of antigenaemia in this age-group 6 months later (P<0.05). Although, the prevalences of antigenaemia among those aged 2-9 years were higher 12 months post-treatment than 6 months post-treatment, they were still lower (by 16%-23%) than those observed pre-treatment. The addition of albendazole to the DEC treatment appeared to offer no additiona