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J S Afr Vet Assoc. 1991 Dec;62(4):182-3.
Overberg research projects. XIII. A comparison of the efficacy of albendazole drench and an albendazole slow-release capsule against nematode parasites in sheep.

Louw JP, Reinecke RK.

Department of Parasitology, Faculty of Veterinary Science, University of Pretoria, Onderstepoort, Republic of South Africa.

The anthelmintic efficacy of albendazole intra-ruminal slow-release capsules (SRC) and albendazole drench against field strains of 5 genera of nematode parasites of sheep, where compared. The SRC reduced the number of L4 and adult Nematodirus by 64.1% and 58.3% and the albendazole drench by 98.1% and 99.1%, respectively. Neither formulation was more than 89.5% effective against either the L4 or adult stage of Teladorsagia. The efficacy of both formulations against the adult stages of Haemonchus, Trichostrongylus and Oesophagostomum ranged from 95.9 to 99.9%.

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Xenobiotica. 1991 Jul;21(7):917-24.
Decrease in albendazole sulphonation during experimental fascioliasis in sheep.

Galtier P, Alvinerie M, Plusquellec Y, Tufenkji AE, Houin G.

Laboratoire de Pharmacologie-Toxicologie INRA, Toulouse, France.

1. The in vivo S-oxidation of albendazole was measured from the pharmacokinetic profile of albendazole sulphoxide and sulphone determined in young male sheep receiving oral albendazole (1.9 mg/kg). Studies were carried out before, and each month after, oral infestation by 150 metacercariae of Fasciola hepatica. 2. Parasitic pathology was ascertained by clinical observation of animals, and the increase in plasma antibodies directed against liver flukes. 3. Rate of conversion of sulphoxide to sulphone and rate of sulphone elimination, were respectively decreased by 47% and 87% at week 8 post-infection, whereas significant increases in the area under plasma sulphone concentrations versus time curve and mean residence time, occurred 4-12 weeks following the infestation. 4. A 58% decrease in albendazole sulphonation was demonstrated in liver microsomal preparations obtained from 8-week-infected sheep, while there was no change in the FAD-directed sulphoxidation of albendazole. 5. The transient impairment of albendazole sulphonation could be related to the decrease in liver microsomal cytochrome P450-dependent monooxygenases observed in sheep with a similar parasitic pathology.

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Trans R Soc Trop Med Hyg. 1991 Sep-Oct;85(5):648-50.
Albendazole treatment in human taeniasis.

de Kaminsky RG.

Direccion de Investigacion Cientifica, Universidad Nacional Autonoma de Honduras.

The results are presented of albendazole trials on human taeniasis infections in Honduras, involving 56 of 68 individuals (2% of the inhabitants) found to be infected during surveys conducted in 15 rural communities. Of the 3 methods used for diagnosis of infection, the Kato cellophane thick smear showed 80% reliability, a combination of Kato and 'Scotch' tape perianal swab 88%, and clinical history of proglottid expulsion less than 50%. Individuals were treated with a dose of 400 mg of albendazole per day for 3 d, followed for 5 d to verify tapeworm expulsion, and evaluated again at 60 and 90 d to assess drug efficacy. All 56 treated individuals remained stool-negative after 60 and 90 d; a partial strobila or segments were recovered from 21 of them (37.5%). Of these, Taenia saginata was identified from 4, and T. solium from 15; 2 specimens could not be specifically identified. Based on negative stool examinations and clinical history after 60 and 90 d, albendazole seems to be a well tolerated, very effective drug for treating infections with Taenia spp. However, confirmation of these results is needed due to the difficulty of making a reliable diagnosis of such infections.

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Zhongguo Yao Li Xue Bao. 1991 Jul;12(4):367-71.
[Uptake and release of mebendazole, albendazole and albendazole sulfoxide by secondary cysts of Echinococcus granulosus in vitro]

[Article in Chinese]

You JQ, Xiao SH, Guo HF, Jiao PY.

Institute of Parasitic Diseases, Chinese Academy of Preventive Medicine, Shanghai.

Mebendazole (Meb), albendazole (Alb) or albendazole sulfoxide (AlbSO) were taken rapidly in vitro by secondary cysts of Echinococcus granulosus removed out from mice infected with protoscoleces 8-9 months previously. The amounts of the drugs taken by the cysts were apparently increased followed by exposure of the cysts to the drugs at 10 micrograms.ml-1. The Alb penetrated into the cysts was distributed mainly in cyst wall, whereas the content of Meb in cyst wall was twice as much as that in cyst fluid. The distributions of AlbSO in cyst wall and cyst fluid were similar. When the cysts in the medium were exposed to Alb, some AlbSO and albendazole sulphone were detected in both cyst wall and cyst fluid, indicating that a part of Alb was metabolized by the cysts. In another experiment cysts exposed to the drug for 2 h were transferred to the medium without the drug for another 24 h. The release rates of the 3 drugs from the cysts were alike. In 1-2 h after transfer about 65-70% of the drugs absorbed by the cysts previously were released. Twenty-four hours after exposure the release rates increased to 75-85%, and the release of the drugs from the cyst wall was somewhat faster than that from cyst fluid.

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Parasitol Res. 1991;77(4):325-8.
In vivo efficacy of albendazole against Giardia duodenalis in mice.

Reynoldson JA, Thompson RC, Meloni BP.

School of Veterinary Studies, Murdoch University, Western Australia.

The antigiardial effects of albendazole were demonstrated in vivo using experimental infections of Giardia duodenalis in mice. These results complement previous in vivo studies in which albendazole was shown to have more potent antigiardial action than the currently applied antigiardial drugs. In mice, 2-4 doses (greater than 100 mg/kg twice daily) were required for complete inhibition of cyst excretion and full elimination of trophozoites from the small intestine. The high doses necessary in mice were not unexpected and are discussed in light of the possible pharmacokinetics of albendazole in the animal model used in this study.

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J Chromatogr. 1991 May 3;566(1):244-9.
Rapid and sensitive method for the determination of albendazole and albendazole sulphoxide in biological fluids.

Hoaksey PE, Awadzi K, Ward SA, Coventry PA, Orme ML, Edwards G.

Department of Pharmacology and Therapeutics, University of Liverpool, U.K.

A sensitive and selective reversed-phase high-performance liquid chromatographic method for the determination of albendazole and its active metabolite albendazole sulphoxide in plasma has been developed. It involves single-step extraction of plasma with dichloromethane, evaporation of the solvent and chromatography on a muBondapak phenyl column with a mobile phase of water containing 1% (v/v) triethylamine-methanol-acetonitrile (70:10:20, v/v) at pH 3.1. Run time is 12 min. The assay satisfies all of the criteria required for use in clinical pharmacokinetic studies and possesses important advantages, notably speed and expense, over current methods.

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J Pharm Sci. 1991 Jan;80(1):3-10.
Simultaneous pharmacokinetic modeling of a drug and two metabolites: application to albendazole in sheep.

Galtier P, Alvinerie M, Steimer JL, Francheteau P, Plusquellec Y, Houin G.

Laboratoire de Pharmacologie-Toxicologie, INRA, Toulouse, France.

Albendazole pharmacokinetic parameters were determined in lambs after iv, oral, and intraruminal single administrations. The parent drug and two metabolites, albendazole sulfoxide and albendazole sulfone, were simultaneously determined in whole blood, plasma, and urine using an HPLC method. The parent drug was only recovered in plasma when injected intravenously. For other routes, only the two metabolites were detectable; they were present in red blood cells and plasma at equal concentrations. The pharmacokinetic parameters were determined by using compartmental models which simultaneously described the two oxidative steps and the urinary excretion of the sulfoxide derivative. Dose-dependent pharmacokinetics was studied in the dose range 0.95-3.8 mg/kg. The results showed that clearance remained constant within the tested dose range since the area under the curve normalized to the dose was similar in the cases of sulfoxide and sulfone metabolites, whatever the route of administration. The drug appeared to be extensively metabolized in the body regardless of the route of administration. Sulfoxidation probably took place in liver, but other tissues seemed to be responsible for the formation of the sulfoxide which has been described as the major anthelmintic derivative of albendazole.

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