Int J Parasitol. 1995 Oct;25(10):1207-12.
The pharmacokinetics of albendazole metabolites following administration of albendazole, albendazole sulfoxide and netobimin to one-month- and eight-month-old sheep.

McKellar QA, Coop RL, Jackson F.

Department of Veterinary Pharmacology, University of Glasgow Veterinary School, Bearsden, U.K.

The principal metabolites detected in plasma of sheep following oral administration of albendazole (ABZ), albendazole sulfoxide (ABSO) and netobimin (NTB) each at 5.0 mg kg-1 body weight were ABSO and albendazole sulfone (ABSO2). The areas under the plasma concentration-time curve (AUC) for ABSO and ABSO2 were significantly (P < 0.05) larger following administration for ABSO than NTB in 1-month- and 8-month-old sheep. The AUC for the ABSO and ABSO2 metabolites were larger following administration of ABZ than NTB in 1-month- but not 8-month-old sheep and the AUC of the ABSO and ABSO2 metabolites were greater following ABSO than ABZ as parent compound in 8-month-old sheep only. The larger AUC values for metabolites following administration of ABSO as the parent compound were generally coincident with significantly higher maximum (Cmax) concentrations and not with persistence in the body, since mean residence times (MRT) of the metabolites were not significantly different from those determined following ABZ and NTB as parent compounds. The lower metabolite concentration following administration of NTB may have been a feature of its requirement for metabolic conversion and its larger molecular weight. Correction of AUC values for molecular weight removed any significant differences between AUC values for either metabolite in 8-month-old lambs. The corrected metabolite AUCs following NTB were, however, significantly lower than those following ABSO administration in 1-month-old lambs, suggesting that immature metabolic processes in these animals contributed to the lower relative bioavailability of NTB in this age group. Age did not affect the disposition of metaboli




J Neurol Sci. 1995 Nov;133(1-2):152-4.
Neurocysticercosis: optimal dose treatment with albendazole.

Cruz I, Cruz ME, Carrasco F, Horton J.

Ecuadorean Academy of Neurosciences, Quito, Ecuador.

Albendazole has been used successfully in the treatment of cerebral cysticercosis for several years. The published dosage schedule has varied from 15 mg/kg/day for 8 days to up to 30 days. Fifty three patients with neurocysticercosis received 8, 15 or 30 days treatment with 800 mg of albendazole daily. The present study demonstrates the effectiveness in clinical and radiological terms of albendazole 800 mg/day for 8 days for the majority of patients affected with cystic or encephalitic parenchymatous cysticercosis. There was no apparent advantage of continuation of treatment for 15 or 30 days in this series. The routine use of high dose steroids limited the effects of parasite destruction. No toxicity attributable to albendazole was encountered.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8583218&dopt=Abstract albendazole Albenza




Xenobiotica. 1996 Mar;26(3):307-19.
Nutritional condition affects the disposition kinetics of albendazole in cattle.

Sanchez SF, Alvarez LI, Lanusse CE.

Departamento de Fisiopatologia, Facultad de Ciencias Veterinarias, Universidad Nacional del Centro, Tandil, Argentina.

1. The influence of nutritional status on the plasma and abomasal fluid disposition kinetics of albendazole (ABZ) and its metabolites, albendazole sulphoxide (ABZSO) and albendazole sulphone (ABZSO2), has been investigated in the calf. 2. Free fatty acid (FFA) and beta-hydroxybutyrate (beta-OHB) serum concentrations were significantly higher in the feed-restricted (poor nutritional status) compared with control calf (optimal nutritional status). 3. ABZ parent drug was not detected in plasma at any time post-treatment and ABZSO and ABZSO2 were the metabolites detected in plasma. Both metabolites were rapidly depleted from the bloodstream. ABZ and its metabolites were recovered in abomasal fluid from 0.25 up to either 48 (ABZ) or 120h (ABZSO and ABZSO2) post-treatment. 4. The plasma disposition kinetics of both ABZ metabolites was significantly changed in the feed-restricted compared with control calf. ABZSO and ABZSO2 plasma area under the curves (AUCs) were significantly higher in the restricted animal. These enhanced AUCs correlated with significantly longer plasma half-lives (T1/2el) and mean residence times (MRTs) for these metabolites. 5. The delayed elimination of ABZ metabolites from the bloodstream correlated with the higher concentration of these molecules recovered in the abomasal fluid of the calves subjected to a dietary restriction. 6. The changes observed on disposition kinetics may reflect an impairment on the hepatic metabolism and clearance of ABZ as a consequence of FFA mobilization from adipose tissue and overproduction of ketone bodies in the liver.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8730922&dopt=Abstract albendazole Albenza




Parasitology. 1996 Aug;113 ( Pt 2):111-21.
Pharmacology and efficacy of liposome-entrapped albendazole in experimental secondary alveolar echinococcosis and effect of co-administration with cimetidine.

Wen H, New RR, Muhmut M, Wang JH, Wang YH, Zhang JH, Shao YM, Craig PS.

Department of Biological Sciences, University of Salford, UK.

Encapsulation of the benzimidazole albendazole in multilamellar liposomes results in a preparation in which this normally insoluble anti-hydatid drug is well solublilized in aqueous media. The high entrapment efficiency observed (75-87%) and the stability of the formulation make this a promising delivery vehicle for improved chemotherapy with albendazole. In particular, the high degree of association with phospholipid may give rise to increased oral bioavailability. Oral administration of albendazole in liposomes led to increased concentration and/or altered metabolism of albendazole sulphoxide (ABZSX) in liver and/or plasma in non-infected Wistar rats. Results from experiments using cotton rats (Sigmodon hispidus) infected with metacestodes of Echinococcus multilocularis show that entrapment within liposomes clearly increases the uptake of albendazole via the oral route. This was reflected by increased levels of albendazole and the two major metabolites in plasma, liver and cyst homogenate when a dose of liposomal albendazole (35 mg/kg) was given orally compared to free albendazole at 50 mg/kg. There was a 75-94% reduction in biomass of the metacestode and a significant increase in survival time for the animals treated with liposome entrapped albendazole. A clear difference in distribution of albendazole and its metabolites in the liver and the metacestode tissues in the presence of cimetidine indicated that the latter has a profound effect on the metabolism of albendazole. There appeared to be a synergistic interaction between albendazole and cimetidine, since the metabolism of albendazole was markedly altered in the combined cimetidine/ liposome-albendazole gro




Clin Infect Dis. 1996 Jun;22(6):1033-5.
Albendazole versus thiabendazole as therapy for trichinosis: a retrospective study.

Cabie A, Bouchaud O, Houze S, Khuong MA, Ruggeri C, Ancelle T, Matheron S, Coulaud JP.

Service des Maladies Infectieuses et Tropicales, Hopital Bichat Claude Bernard, Paris, France.

An outbreak of trichinosis caused by ingestion of horse meat occurred in December 1993 in France; more than 500 people were affected. We compared the immediate and midterm efficacy and tolerability of thiabendazole and albendazole as therapy for the 46 patients seen in our department. Forty-four patients (96%) were treated. The first 26 patients received thiabendazole therapy; the next 18 received albendazole therapy. All the patients were tested with prednisone. Eight relapses occurred (seven in the thiabendazole group and one in the albendazole group [not significant]). Side effects of treatment were reported by seven patients, all of whom were treated with thiabendazole (P = .01). Six months after treatment, 16 of the 31 patients who responded to a questionnaire still had symptoms, the most frequent of which were myalgias (81%) and fatigue (69%). No significant difference was observed between the two treatment groups. The immediate efficacy of thiabendazole and albendazole as therapy for trichinosis was comparable, but albendazole was better tolerated.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8783705&dopt=Abstract albendazole Albenza




Res Vet Sci. 1996 Jul;61(1):92-3.
Effect of sub-lethal doses of albendazole on the fecundity of Dictyocaulus viviparus.

Osman AM, Jacobs DE, Fisher MA, Pilkington JG, Jones PA.

Department of Pathology and Infectious Diseases, Royal Veterinary College (University of London), Hatfield, Hertfordshire.

During an evaluation of the efficacy of prolonged low-dose albendazole therapy on nematode infections in calves, it was observed that a dose-rate of 2 mg kg-1 given daily for 10 days was highly effective at expelling Dictyocaulus viviparus, but smaller doses suppressed the faecal output of larvae without killing the lungworms. A more detailed study with four experimentally infected calves given 1 mg kg-1 day-1 for 10 days showed that faecal output of larvae ceased after six to eight days but resumed four to six days after the withdrawal of the drug. The albendazole-induced sterility was therefore reversible. A subsidiary study showed that the strain of parasite used was fully susceptible to albendazole.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8819203&dopt=Abstract albendazole Albenza




Vet Res Commun. 1996;20(5):427-35.
The efficacy of an albendazole-medicated block in controlling sheep nematodes in Xinjiang province, north-west China.

Tan LX, Gong XH, Tan RF, Ni YL, Wang JC, Guo ZM, Vanselow BA.

China-Australia Sheep Research Project, Xinjiang Academy of Animal Sciences, Urumqi, Xinjiang, People's Republic of China.

Medicated feed-blocks containing 2 mg/kg albendazole were fed for 12 days to ewe-lambs naturally infected with nematode worms in north-west China. The cumulative total average intake of albendazole was 15 mg/kg body weight. This treatment was compared with a single oral drench of 15 mg/kg albendazole and with no treatment. Both albendazole treatments were 99% effective in reducing the total strongyle egg counts. The medicated block was 100% effective in reducing the total trichostrongylid worm count, although only 86.4% of the sheep consumed an adequate amount. The single drench was 97% effective. Under the management conditions available to sheep herders in the northern provinces of China, albendazole-medicated feed blocks used at strategic times could effectively control trichostrongylid nematodes.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8908723&dopt=Abstract albendazole Albenza