Clin Neuropharmacol. 1990 Dec;13(6):559-64.
Plasma and CSF levels of albendazole and praziquantel in patients with neurocysticercosis.

Jung H, Hurtado M, Sanchez M, Medina MT, Sotelo J.

Laboratory of Neuropharmacology, National Institute of Neurology and Neurosurgery of Mexico, Mexico City.

Albendazole or praziquantel were measured in plasma and cerebrospinal fluid (CSF) in 29 patients with neurocysticercosis. Mean levels of albendazole in plasma were 0.918 microgram/ml and in CSF were 0.392 microgram/ml and levels of praziquantel were 1.640 micrograms/ml in plasma and 0.398 microgram/ml in CSF, after doses of 15 and 50 mg/kg, respectively. Drug concentrations in CSF were 43% for albendazole and 24% for praziquantel. The drug levels obtained for both drugs showed ample individual variations that were not related to age, sex, presence of inflammation in the subarachnoid space, or therapeutic effectiveness; such variations seem to be due to individual differences in pharmacokinetics. Both drugs were effective and the doses currently used of each drug seem to be optimal for therapy of neurocysticercosis.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2276121&dopt=Abstract albendazole Albenza




Clin Pharmacol Ther. 1990 Mar;47(3):347-53.
Albendazole treatment of echinococcosis in humans: effects on microsomal metabolism and drug tolerance.

Steiger U, Cotting J, Reichen J.

Department of Clinical Pharmacology, University of Berne, Switzerland.

We prospectively studied the effect of albendazole on microsomal reserve and on first-pass activation to albendazole sulfoxide in patients with hydatid disease. An aminopyrine breath test was performed in 12 patients while they were receiving albendazole treatment and while they were not. Excretion of 14CO2 in breath averaged 0.70%.kg.mmol-1 +/- 0.20%.kg.mmol-1 without treatment and 0.54%.kg.mmol-1 +/- 0.14%.kg.mmol-1 with treatment (p less than 0.005). Plasma levels of albendazole sulfoxide were measured 4 hours after the morning dose during the first and second half of the 4-week treatment cycles. In nine of the 12 patients albendazole sulfoxide levels decreased during the second half of the cycle by an average of 0.84 +/- 0.76 mumol/L (p less than 0.02). Transaminase levels increased in 10 of the 12 patients during long-term albendazole treatment, and major side effects, including hepatotoxicity, neutropenia, and alopecia, were observed in three patients. We conclude that albendazole partially inhibits microsomal enzyme function but induces its own metabolism. Hepatotoxicity and other possible severe side effects necessitate close therapeutic monitoring of patients who are given albendazole.

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Ther Drug Monit. 1990 Mar;12(2):187-90.
Therapeutic monitoring of albendazole: a high-performance liquid chromatography method for determination of its active metabolite albendazole sulfoxide.

Zeugin T, Zysset T, Cotting J.

Department of Clinical Pharmacology, University of Berne, Switzerland.

A sensitive and specific reversed-phase high-performance liquid chromatography (HPLC) method is described for the quantitative determination of albendazole sulfoxide (ASOX); since albendazole sulfone (ASON) appears only in small amounts and albendazole (ABZ) normally does not appear in human plasma, only a qualitative determination of ASON and ABZ was made in human plasma. Plasma samples were extracted three times using ethylacetate and petroleum benzine; this yielded optically clear samples which after evaporation were dissolved in the HPLC solvent and injected onto an RP-C18 column, with ultraviolet detection at 290 nm. The detection limit of the main metabolite ASOX was 50 nM and that of ASON was 100 nM. The intraday coefficient of variation for ASOX was 3.3% at a concentration of 2.2 microM, and the interday coefficients of variation were 14.5, 7.3, and 9.1% at ASOX concentrations of 0.5, 2.5, and 5.0 microM, respectively. Calibration was linear in a concentration range of 0.05-12 microM for ASOX and 0.1-8 microM for ASON, respectively. Pharmacokinetic data of a patient with echinococcosis are presented.

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Int J Parasitol. 1990 Apr;20(2):161-7.
Effect of benzimidazole drugs on tubulin in benzimidazole resistant and susceptible strains of Caenorhabditis elegans.

Enos A, Coles GC.

Department of Zoology, University of Massachusetts, Amherst 01003.

An in vitro assay was used to determine efficacy and if side resistance was present to benzimidazole anthelmintics tested against Caenorhabditis elegans after selection with albendazole. Side resistance was present to all the benzimidazoles tested, except for oxibendazole and parbendazole. At a concentration of 1 mM, all of the drugs, except thiabendazole, were effective in killing 100% of the albendazole susceptible worms. Tubulin from albendazole resistant and susceptible C. elegans was isolated and run on polyacrylamide gels. Western blots with anti-tubulin antibody showed that the albendazole resistant strain had an altered tubulin. Electron microscopy of albendazole-treated drug resistant worms showed microtubules throughout the intestinal cells. Microtubules were not observed in albendazole-treated drug susceptible worms.

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Trop Med Parasitol. 1990 Mar;41(1):46-8.
Evaluation of the treatment of intestinal helminthiases with albendazole in Djohong (North Cameroon).

Raccurt CP, Lambert MT, Bouloumie J, Ripert C.

Parasitology Unit, University of Bordeaux II, France.

246 inhabitants of Djohong, a township located in North-east Cameroon, presented with single or mixed nematode infections. They were treated by 400 mg albendazole in a single dose. The results were evaluated either with the Kato thick-smear technique and the Ritchie technique on stools and/or the Graham test: albendazole has proved to be 100% efficacious in pinworm and roundworm treatment, 63% to 84% in hookworm treatment (difference due to the type of technique used). Albendazole showed a mean efficacy in whipworm treatment (about 50% cure rate). In case of residual worm infection, the egg count is reduced from 80% to 90% which is of the utmost importance. The relative treatment failures occurring with large worm load. This systematic treatment of a whole population considerably reduces the spread of nematode eggs over the soil (18-fold for Nector americanus, 10-fold for Trichuris trichiura). This broad spectrum anthelmintic is strongly recommended in mass treatments for its efficacy and excellent tolerance, as its ovicide action reduces the probability of fecal pollution of the environment by treated patients who have residual parasites.

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Vet Parasitol. 1990 Feb;35(1-2):139-45.
Efficacy of thiophanate and albendazole against natural infections of Dicrocoelium dentriticum, Fasciola hepatica, and gastrointestinal nematodes and cestodes in sheep.

Onar E.

Pendik Hayvan Hastaliklari, Arastrima Enstitusa, Istanbul, Turkey.

The anthelmintic efficacy of thiophanate and albendazole was compared in sheep with heavy infestations of Dicrocoelium dentriticum. The effectiveness of each drug was determined by counting the numbers of D. dentriticum in animals killed 21 days after treatment. In one group, the dose of thiophanate recommended for use against gastrointestinal (GI) nematodes (50 mg kg-1 live weight) was found to be 74.4% effective against D. dentriticum. Two tablets (each containing 76 mg of active ingredient) of albendazole per 30 kg live weight were given to a second group and the dose repeated after 1 week. Under this regime, albendazole was found to be 12.7% effective against D. dentriticum. The effect of each drug on other parasites was as follows; thiophanate had no effect against Fasciola hepatica or cestodes, while albendazole was 71.5% effective against F. hepatica and 100% effective against cestodes. Both drugs were highly effective against GI nematodes.

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Eur J Clin Pharmacol. 1990;38(6):605-8.
Albendazole kinetics in patients with echinococcosis: delayed absorption and impaired elimination in cholestasis.

Cotting J, Zeugin T, Steiger U, Reichen J.

Department of Clinical Pharmacology, University of Berne, Switzerland.

The pharmacokinetics of albendazole and its main metabolite, albendazole sulphoxide, have been examined after giving a single oral dose of 200 mg albendazole to 19 patients with either Echinococcus multilocularis or E. granulosus, 5 of whom had significant extrahepatic obstruction due to the underlying disease. The AUC of albendazole sulphoxide was increased in the latter patients (mean 122 mumols.h.l-1 compared to 17 mumols.h.l-1 in the non-obstructed group). Obstructed patients had delayed absorption, ka averaging 0.39 compared to 1.41 h-1 in non-obstructed patients. The corresponding elimination rate constant, ke was also prolonged, averaging 0.041 and 0.13 h-1 in the two groups, respectively. Four patients were restudied after complete or partial resolution of the cholestasis. The pharmacokinetic parameters in them had returned towards values comparable to those in the non-obstructed patients.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2373135&dopt=Abstract albendazole Albenza