Arch Med Res. 1992;23(2):63-7.
Effects of albendazole on Entamoeba histolytica and Giardia lamblia trophozoites.

Chavez B, Espinosa-Cantellano M, Cedillo Rivera R, Ramirez A, Martinez-Palomo A.

Centro de Investigacion y de Estudios Avanzados del Instituto Politecnico Nacional, Mexico, DF, Mexico.

Albendazole, a benzimidazole carbamate commonly used for the treatment and control of intestinal helminthic infections, is also useful for the treatment of giardiasis. Therefore, it is of interest to determine whether the drug has activity against other intestinal protozoa, such as E. histolytica. The present results demonstrate that albendazole inhibits the growth of E. histolytica trophozoites in axenic cultures and induces fine structural changes such as polyribosome aggregation and loss of cytoplasmic vacuoles at concentrations up to 10 micrograms/ml. The viability of E. histolytica trophozoites was not affected by the drug. In contrast, lower concentrations of albendazole showed dramatic effects on G. lamblia trophozoites. These included loss of adhesiveness, striking modifications of the overall morphology of giardias, disassembly of the ventral disk, and loss of viability after prolonged treatment. The results provide further evidence on the potent antigiardial activity of albendazole and indicate that, at the concentrations used, the drug has no antiamebic activity.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1340323&dopt=Abstract albendazole Albenza




Am J Vet Res. 1992 Sep;53(9):1663-5.
Effect of repeated doses of albendazole on enantiomerism of its sulfoxide metabolite in goats.

Benoit E, Besse S, Delatour P.

INRA-DGER Laboratory of Metabolic Toxicology, School of Veterinary Medicine of Lyon, Marcy l'Etoile, France.

Five adult Saanen goats were dosed orally 3 times with albendazole (2.5 mg/kg of body weight) at 24-hour intervals, and blood samples were taken by jugular venapuncture at standardized intervals. Plasma was analyzed to determine concentrations of S-oxidation metabolites, and a chiral column was used for enantiomeric discrimination of the sulfoxide metabolite of albendazole. Marked changes were evident between the first and subsequent plasma profiles concerning, on one hand, the proportions of sulfoxide and sulfone metabolites concentrations and, on the other hand, the enantiomeric balance of sulfoxide metabolite. These correlated phenomena may be explained by the following arguments: the enzyme responsible for sulfoxidation is mainly a flavine-containing monooxygenase, whereas the enzyme responsible for sulfonation is a cytochrome-dependent monooxygenase; the latter, but not the former, is induced by albendazole; the enantioselectivities of both enzymic systems are opposite, the flavine produces the (+) sulfoxide, whereas the cytochromes can use as a substrate, specifically, the (-) sulfoxide.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1416373&dopt=Abstract albendazole Albenza




Ann Trop Med Parasitol. 1992 Apr;86(2):151-6.
Polycystic hydatid disease (Echinococcus vogeli). Treatment with albendazole.

Meneghelli UG, Martinelli AL, Bellucci AD, Villanova MG, Velludo MA, Magro JE.

Department of Internal Medicine, Faculty of Medicine of Ribeirao Preto, University of Sao Paulo, Brazil.

Six patients with polycystic hydatid disease (PHD) were treated with 10 mg kg-1 day-1 albendazole. One patient was treated continuously for eight months and another for three months. In three other patients treatment was discontinuous, consisting of a series of at least three 30-day cycles separated by 15 days without treatment. The last patient was treated continuously with 12 mg kg-1 day-1 albendazole for 51 days and then with three 30-day cycles of treatment with 10 mg kg-1 day-1 separated by 15-day drug-free intervals. Follow-up ranged from 10-30 months. Considerable clinical improvement and cyst reduction or disappearance occurred in four patients. Clinical improvement, but no changes in the hepatic alterations detected by computerized tomography, occurred in the other two patients, although a pulmonary cyst disappeared in one of them. Adverse effects were proteinuria, alopecia, leucopenia, itching and discrete elevation in aspartate transaminase, all of them reversed after the end of treatment. These results indicate that albendazole is effective for the treatment of PHD.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1417206&dopt=Abstract albendazole Albenza




Dtsch Tierarztl Wochenschr. 1992 Oct;99(10):416-8.
[The metabolism of albendazole in the isolated perfused intestine of rats]

[Article in German]

Lawrenz A, Eglit S, Kroker R.

Bundesgesundheitsamt, Robert-von-Ostertag-Institut, Berlin.

Pharmacokinetic studies on Albendazole after peroral administration demonstrate a rapid and complete biotransformation. The major metabolites Albendazole sulphoxide and -sulphone were detected in the plasma; the parent compound was only found sporadically at very low levels. These results indicate removal by the liver and/or the gut at first pass. After evidence is found that the liver has the capacity to sulphoxidize and to sulphonize Albendazole, biotransformation of the gut was examined using an isolated perfused rat gut model. A high-performance liquid chromatography method was used to simultaneously determinate Albendazole, -sulphoxide and -sulphone. Albendazole was biotransformed partly to Albendazole sulphoxide by the gut, whereby the metabolite but not the parent compound was absorbed. It is concluded, that the gut has the capacity to biotransform Albendazole. However, biotransformation is limited to the first step, the sulphoxidation.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1425320&dopt=Abstract albendazole Albenza




Hepatogastroenterology. 1992 Oct;39(5):424-6.
Prophylactic effect of albendazole in experimental peritoneal hydatidosis.

Cakmakci M, Sayek I.

Department of Surgery, Hacettepe University Medical Faculty, Ankara, Turkey.

To determine the effectiveness of prophylactic short-term administration of albendazole in experimental peritoneal hydatidosis this substance was given at a dose of 15 mg/kg for 96 hours prior to scolex implantation. In contrast to the 81.8% of the controls, only 11.1% of the experimental animals developed intraperitoneal hydatidosis over a period of 18 weeks (p < 0.001). The newly defined cyst index was also decreased from 2.09 to 0.22 by the administration of albendazole (p < 0.005). It is concluded that albendazole, when given for 96 hours prior to any suspected intraperitoneal spillage of viable hydatid cyst contents could significantly reduce secondary peritoneal hydatidosis.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1459523&dopt=Abstract albendazole Albenza




Med Parazitol (Mosk). 1992 Jan-Feb(1):47-9.
[The efficacy of Vermox and albendazole in an experimental model of nippostrongylosis in mice]

[Article in Russian]

Rashid VM.

Experiments with the model of Nippostrongylus brasiliensis and white outbred mice showed that vermox and albendazole are highly effective anthelmintics in nippostrongyliasis. The ED50 of albendazole for 7 days invasion (adult worms) is 148.9 times higher than for 4 days (fourth instar larvae) and 25.1 times higher than for 2 days (third instar larvae). The ED90/ED10 ratio for albendazole is 1.4, 4.4, and 12.4 at days 7, 4, and 2, respectively. At the adult stage, susceptibility to anthelmintics (vermox and albendazole) increases with age.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1508076&dopt=Abstract albendazole Albenza




Xenobiotica. 1992 Apr;22(4):419-26.
Metabolism of albendazole and albendazole sulphoxide by ruminal and intestinal fluids of sheep and cattle.

Lanusse CE, Nare B, Gascon LH, Prichard RK.

Institute of Parasitology, McGill University, Macdonald Campus, Quebec, Canada.

1. The metabolism of albendazole (ABZ), albendazole sulphoxide (ABZSO) and albendazole sulphone (ABZSO2) by ruminal, abomasal and ileal fluids of sheep and cattle was investigated under anaerobic conditions in vitro. 2. None of the compounds was metabolically changed by incubation with abomasal fluids of sheep and cattle. 3. ABZ and ABZSO were extensively metabolized by sheep and cattle ruminal and ileal fluids. ABZSO2 was unaffected by incubation with these gastrointestinal fluids. 4. The rate of ABZ oxidation into ABZSO was greater for cattle ruminal and ileal fluids than for sheep fluids. 5. ABZSO was reduced back to ABZ by ruminal and ileal fluids of both species. This reducing activity was significantly higher for both ruminal and ileal fluids of sheep compared with those of cattle.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1523862&dopt=Abstract albendazole Albenza