J Parasitol. 2002 Apr;88(2):395-8.
Effects of ivermectin and albendazole against Anisakis simplex in vitro and in guinea pigs.

Dziekonska-Rynko J, Rokicki J, Jablonowski Z.

Department of Parasitology, Warmia and Mazury University, Olsztyn, Poland. jdatman.uwm.edu.pl

The activity of ivermectin and albendazole against larval Anisakis simplex was tested in vitro and in experimentally infected guinea pigs. Before drug exposure the medium for half of the larvae was adjusted to pH 2.0 with 1 N HCl, whereas the other half was held at pH 7.0. To these solutions, ivermectin was added to full concentrations of 1, 2, 5, 10, 50, 100, or 200 microg/ml, and for albendazole, 300, 400, and 500 microg/ml. Animals from group I were given 0.1 ml of 1% (3.3 mg/kg) ivermectin, whereas guinea pigs from group II were each given 5-7 mg (16.6-23.3 mg/kg) of albendazole orally. The efficacy of both drugs against L, A. simplex was high in vitro and in vivo against the larvae in different organs of guinea pigs.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12054018&dopt=Abstract albendazole Albenza




J Parasitol. 1995 Oct;81(5):794-5.
Activity of benzimidazoles against cryptosporidiosis in neonatal BALB/c mice.

Fayer R, Fetterer R.

Parasite Immunobiology Laboratory, Livestock and Poultry Sciences Institute, United States Department of Agriculture, Beltsville, Maryland 20705, USA.

The need for an effective compound for the prevention and treatment of cryptosporidiosis in humans and animals has led to the testing of benzimidazoles based on reports that albendazole was clinically effective against related protozoan parasites causing microsporidiosis in humans. Albendazole and other benzimidazole derivatives were tested for prophylactic efficacy against cryptosporidiosis at dosage levels 1-3x the levels found effective for treatment of cattle or sheep for helminth infections. Daily dosage levels of thiabendazole, parbendazole, oxibendazole, mebendazole, and albendazole, as high as 200, 30, 10, 15, and 15 mg/kg of body weight, respectively, were not efficacious in neonatal mice. Although the number of parasites in histologic sections of intestine from mice mediated with 15 mg albendazole/kg of body weight was significantly lower than in unmedicated control mice, suggesting activity against the parasite, a high percentage of epithelial cells in the medicated mice were infected.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7472880&dopt=Abstract albendazole Albenza




Parasitol Res. 1995;81(5):438-40.
Anti-tubulin immunohistochemistry study of Echinococcus granulosus protoscolices incubated with albendazole and albendazole sulphoxide in vitro.

Perez-Serrano J, Denegri G, Casado N, Bodega G, Rodriguez-Caabeiro F.

Laboratory of Parasitology, Faculty of Pharmacy, University of Alcala de Henares, Madrid, Spain.

Tubulin content was immunohistochemically studied in Echinococcus granulosus protoscolices incubated with albendazole and albendazole sulphoxide alone or in combination. Tubulin immunoreactivity was very patent in the control protoscolices and was mainly located in the sucker region and the invagination channel of protoscolices. Treated protoscolices always showed less immunoreactivity than did control protoscolices. We concluded that albendazole and its metabolite albendazole sulphoxide produce tubulin alterations in E. granulosus protoscolices.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7501645&dopt=Abstract albendazole Albenza




Int J Parasitol. 1995 May;25(5):593-9.
In vitro drug susceptibility of 29 isolates of Giardia duodenalis from humans as assessed by an adhesion assay.

Farbey MD, Reynoldson JA, Thompson RC.

Institute for Molecular Genetics and Animal Disease, Murdoch University, Australia.

Twelve isolates of Giardia duodenalis from Caucasian hosts in the Perth metropolitan area, along with 16 isolates from Aborigines in the north of Western Australia and the reference isolate P1C10 were examined for their in vitro drug sensitivity. Dose-response curves were constructed for each isolate for metronidazole, the most common clinically used antigiardial agent, as well as for the benzimidazole compound albendazole. Less than a 9-fold variation was found in the susceptibility of the isolates to albendazole, while for metronidazole there was well over a 16,000-fold variation between the same group of isolates. In addition, it was found that isolates of Giardia obtained from Aboriginal hosts were significantly less sensitive to albendazole than those obtained from Caucasians. The results of this study have important implications for the continued use of metronidazole and the potential use of albendazole for the treatment of giardiasis.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7635637&dopt=Abstract albendazole Albenza




J Chromatogr B Analyt Technol Biomed Life Sci. 2003 Jan 5;783(1):237-45.
Simultaneous liquid chromatography-tandem mass spectrometric determination of albendazole sulfoxide and albendazole sulfone in plasma.

Bonato PS, Lanchote VL, Takayanagui OM.

Faculdade de Ciencias Farmaceuticas de Ribeirao Preto-USP, CEP 14040-903, Ribeirao Preto, Brazil. psbonatcfrp.usp.br

This paper describes a simple, fast, sensitive and reliable method for the simultaneous determination of albendazole sulfoxide (ASOX) and albendazole sulfone (ASON), the two most important metabolites of the drug albendazole (ABZ), in plasma samples using liquid chromatography and tandem mass spectrometry. After liquid-liquid extraction with dichloromethane, the two albendazole metabolites and the internal standard phenacetin were resolved in a CN column using the mobile phase methanol-water (4:6, v/v) acidified with 1% acetic acid. Detection by electrospray mass spectrometry was carried out in the positive ion mode. The method was linear up to 2500 and 250 ng/ml for ASOX and ASON, respectively, with mean recoveries of more than 85%. The precision and accuracy data, based on within- and between-day variations over 5 days, were lower than 15%. The quantitation limits of 0.5 and 5.0 ng/ml for ASON and ASOX are low enough for the method to be suitable for pharmacokinetic studies. Pharmacokinetic data obtained with the proposed method following oral administration of ABZ to a patient with neurocysticercosis are also reported.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12450544&dopt=Abstract albendazole Albenza




Eur J Clin Pharmacol. 2002 Nov;58(8):537-42. Epub 2002 Oct 02.
Cytochrome P450 1A1/2 induction by antiparasitic drugs: dose-dependent increase in ethoxyresorufin O-deethylase activity and mRNA caused by quinine, primaquine and albendazole in HepG2 cells.

Bapiro TE, Andersson TB, Otter C, Hasler JA, Masimirembwa CM.

Department of Biochemistry, University of Zimbabwe, Harare, Zimbabwe.

OBJECTIVE: To investigate the inductive effects of twenty-four antiparasitic drugs on cytochrome P450 (CYP) 1A1 and 1A2 enzyme activities. METHODS: Human hepatoma (HepG2) cells were exposed to antiparasitic drugs for 24 h, and the ethoxyresorufin O-deethylase (EROD) activity, indicative of CYP1A enzyme activity, was measured fluorometrically. In addition, the CYP1A1 and CYP1A2 mRNA expression levels were determined by means of quantitative reverse-transcriptase polymerase chain reaction. RESULTS: Quinine, albendazole and primaquine caused a dose-dependent increase in EROD activity of 5.5, 4.0 and 7.5-fold, at concentrations eliciting maximal induction, respectively. 2,3,7,8-tetrachlorodibenzo- p-dioxin, used as a positive control at a final concentration of 1.5 nM, caused a 30-fold increase in EROD activity. The induction of EROD activity was accompanied by an increase in CYP1A1 and CYP1A2 mRNA expression levels. Niclosamide, 4-chlorophenylbiguanide, dapsone, amodiaquine and desethylamodiaquine caused slight increases in EROD activity. No effect on CYP1A was observed for artemisinin, suramin, diethylcarbamazine, pyrimethamine, metrifonate, ivermectin, pyrantel artesunate, cycloguanil, atovaquone, melarsoprol, praziquantel, proguanil and dihydroartemisinin. CONCLUSIONS: Quinine, albendazole and primaquine induce CYP1A1 and CYP1A2 at the transcriptional level. Considering the plasma concentrations (C(max)) achieved in vivo after administration of a therapeutic dose, induction by quinine and albendazole might be of clinical significance. The induction by primaquine, however, may not be of pharmacological or toxicological significance as




J Neurol Neurosurg Psychiatry. 1995 Feb;58(2):247-9.
Single parenchymal brain cysticercus in the acute encephalitic phase: definition of a distinct form of neurocysticercosis with a benign prognosis.

Del Brutto OH.

Department of Neurology, Luis Vernaza Hospital, Guayaquil, Ecuador.

Fifty four patients with a single parenchymal brain cysticercus in the acute encephalitic phase were studied to outline the features of this form of the disease. Seizures were the presenting symptom in all cases. Twenty six patients had a single seizure and 28 had several seizures before admission. Neurological examination was normal in 45 patients and showed focal signs in nine. All patients had a single enhancing CT lesion; all but three lesions were < 20 mm. Anticonvulsants were started in every patient. Forty five patients were followed up for 18 (SD 6) months. Thirty seven of these 45 patients received albendazole. Four weeks after the trial, CT showed resolution of lesions in all cases. The remaining eight patients refused albendazole, and CT showed persistence of lesions by 16 weeks in six cases. At the end of the follow up, all patients who received albendazole were free of seizures as opposed to three of eight patients who did not receive the drug. Focal signs improved in the nine patients with these signs (all received albendazole). Recognition of this form of neurocysticercosis permits early treatment with albendazole that greatly improves the prognosis.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7876864&dopt=Abstract albendazole Albenza