J Parasitol. 1980 Dec;66(6):935-40.
A comparison of the effect of albendazole, cambendazole, and thiabendazole on the larval development of three hymenolepidid cestodes.

Evans WS, Hardy M, Novak M.

Flour beetles (Tribolium confusum) parasitized either by Hymenolepis diminuta, H. nana, or H. microstoma were fed continuously on flour mixed either with thiabendazole, cambendazole, or albendazole (drug concentration was always 10%) from day 1 (24 hr) to day 10 postinfection when the experiments were terminated. All drugs markedly inhibited the development of H. diminuta and H. nana. Populations of these species recovered from beetles fed anthelmintics were composed mostly of under-developed forms, many of which still retained the size and appearance of newly hatched oncospheres, whereas all the parasites recovered from the control beetles (fed only flour) reached full development. Parasites inhibited by cambendazole and albendazole recovered and reached full development within 9 days after treatment was terminated. Also, results were obtained which implied that some parasites were able to continue their development at a reduced rate in the presence of the drugs. Hymenolepis microstoma differed from the other species in its response to the drugs. Albendazole and thiabendazole had no effect on its development and it was only slightly inhibited by cambendazole. Larvae recovered from beetles fed the latter drug had all developed beyond the oncosphere stage but 3 to 5% of them repeatedly failed to reach full development. The drugs varied in their effects on the flour beetles. An average of 63% and 33% of those fed thiabendazole and cambendazole, respectively, died before the 10th day of infection. Albendazole, on the other hand, had no effect on beetle survival.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7218116&dopt=Abstract albendazole Albenza




Am J Vet Res. 1981 Jun;42(6):1062-4.
Anthelmintic efficacy of albendazole in calves with naturally acquired Fasciola hepatica infections.

Bradley RE, Randell WF, Armstrong DA.

The anthelmintic efficacy of albendazole was evaluated as an oral drench at dosages of 15.0, 10.0, and 7.5 mg/kg of body weight in 3 groups crossbred Brahman calves (n = 12 group) infected with Fasciola hepatica. Although posttreatment fluke ova counts for the 3 albendazole treatment groups were significantly (P less than 0.01) lower (av 82%) than were counts in nontreated calves, there were no significant differences in the responses to the different albendazole treatments. At necropsy, adult fluke counts in treated calves were lower (P less than 0.05) than were counts in nontreated calves, but as with ova counts, a dose-related trend was not noticed. Efficacy against adult flukes was 63.4%, 50.0%, and 56.6% for 15.0, 10.0, and 7.5 mg/kg, respectively. Activity against immature flukes was not observed in calves given the 10.0 and 7.5 mg/kg, but there was a 36% decrease of flukes in those calves given 15.0 mg/kg. Significant decreases (P less than 0.05) in fluke ova viability were observed for the 3 treatment groups in which 12.9% of ova collected at necropsy failed to embryonate (control group av 6.7%). Posttreatment weight changes were not significantly different, although gains were greater within albendazole treatment groups. Decreases in gastrointestinal parasite ova counts after treatment were 98%, 93%, and 93% for groups given 15.0, 10.0, and 7.5 mg/kg, respectively. Ova counts in nontreated calves increased 26.2% during the same period.

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J Anim Sci. 1981 Dec;53(6):1511-5.
Anthelmintic activity of albendazole against adult Metastrongylus apri in artificially infected swine.

Ferguson DL.

Three groups of five pigs experimentally infected with lungworm larvae (Metastrongylus apri) were treated with albendazole at 5, 7.5 or 10 mg/kg body weight at 35 days postinfection. The albendazole was administered in the feed. Anthelmintic efficacy, as determined by comparison of postmortem lungworm counts for the treated animals and five infected, untreated controls, was 32.6% at 5 mg/kg, 44.3% at 7.5 mg/kg and 60.7% at 10 mg/kg. The 60.7% reduction in lungworms was statistically different at the 5% level of significance. In a second experiment, three groups of five pigs experimentally infected with lungworm larvae (Metastrongylus apri) were treated continuously for 5 days with albendazole in the feed at 10, 20 or 30 ppm, starting at 35 days postinfection. The anthelmintic efficacy, again determined by comparison of postmortem lungworm counts for the treated pigs and five infected, untreated controls, was 99.2% at 10 ppm, 99.9% at 20 ppm and 100% at 30 ppm. These mean reductions from the control values were significant (P greater than .01).

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Am J Vet Res. 1980 Jul;41(7):1126-9.
Pharmacokinetics of albendazole in sheep.

Marriner SE, Bogan JA.

The concentrations of albendazole and its two major metabolites, the sulfoxide and sulfone, were measured in plasma and in ruminal and abomasal fluid of three sheep (surgically prepared with permanent ruminal and abomasal cannulae) orally given albendazole as a suspension at a dose rate of 10 mg/kg. Albendazole was not detectable in plasma at any time in one sheep (detection limit, 0.02 micrograms/ml) and in the other sheep, only transiently detectable. Albendazole sulfoxide was detectable in plasma and in abomasal fluid at mean peak concentrations of 3.2 and 26.2 micrograms/ml, respectively, 20 hours after administration. It is probable that much of the anthelmintic activity of albendazole in sheep is due to the metabolically formed sulfoxide and sulfone.

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Farmaco. 2003 Jul;58(7):527-34.
Two simple methods for the estimation of albendazole and its dosage forms using chloramine-T.

Basavaiah K, Prameela HC.

Department of Chemistry, University of Mysore, Manasagangotri, Mysore 570 006, India. basavaiahahoo.com

Two simple, rapid and reliable methods for the determination of albendazole are described. Both methods involve the use of chloramine-T as the oxidimetric reagent. In the titrimetric method, a known excess of chloramine-T is added to an acidified solution of sample, and after a specified time, the residual oxidant is determined iodometrically. Spectrophotometric procedure also involves the addition of a measured excess of chloramine-T in buffer medium of pH 2.70+/-0.1 and after the reaction is ensured to be complete, the surplus oxidant is determined by a well established colour reaction involving metol and primary arylamine that results in charge-transfer complex measurable at 520 nm. In both methods, the amount of chloramine-T corresponds to the drug content. Reaction conditions were examined and optimised. Titrimetry is based on a 1:3 stoichiometric reaction between albendazole and chloramine-T and is applicable in the range of 1-15 mg. In spectrophotometry, the absorbance was found to decrease linearly with increasing concentration of albendazole, which is corroborated by the calculated correlation coefficient value of -0.9998. The system obeys Beer's law for 2.5-25 microg x ml(-1) of albendazole. The molar absorptivity and Sandell sensitivity were calculated to be 6.24 x 10(3) l mol(-1) cm(-1) and 42.54 ng cm(-2), respectively. The limits of detection and quantification were calculated to be 1.15 and 3.83 microg x ml(-1), respectively. The proposed methods were successfully applied to the determination of albendazole in commercially available dosage forms. The reliability of the assays was established by parallel determination by the official method and recovery studies.

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J Pharm Pharmacol. 2003 Jun;55(6):757-64.
Effect of clotrimazole on microsomal metabolism and pharmacokinetics of albendazole.

Merino G, Molina AJ, Garcia JL, Pulido MM, Prieto JG, Alvarez AI.

Department of Physiology, Veterinary Faculty, University of Leon, 24071 Leon, Spain.

Albendazole is a broad spectrum anthelmintic drug widely used in human and veterinary medicine. Intestinal and hepatic albendazole metabolism leads to albendazole sulfoxide (active metabolite) and albendazole sulfone (inactive metabolite) formation. Microsomal sulfonase activity can be abolished by in-vitro interaction with clotrimazole and pharmacokinetic studies confirm this interaction. After albendazole incubation, albendazole sulfone formation was completely inhibited by 50 microM clotrimazole in intestinal incubations and a 50% inhibition was observed in hepatic incubations. The lower inhibition constant (K(i)) value observed in the intestinal incubations (9.4 +/- 1.0 microM) compared with the hepatic counterparts (23.3 +/- 15.8 microM) pointed to a greater affinity of the enzymatic systems in the intestine. Regarding the formation of albendazole sulfoxide, an inhibition close to 50% was observed in liver and intestine at 10 microM clotrimazole. The pharmacokinetic parameters obtained following the oral co-administration of albendazole sulfoxide and clotrimazole corroborated the in-vitro inhibition of albendazole sulfone formation, since the ratio of the area under the plasma concentration-time curves for the sulfoxide/sulfone (AUC(ABZSO)/AUC(ABZSO2)) was significantly higher (38.1%). In addition, the AUC and C(max) for albendazole sulfone were significantly lower. The effect of clotrimazole was also studied after prolonged treatment. Hepatic microsomal metabolism of albendazole was induced after 10 days of clotrimazole administration, with significant increases in formation of albendazole sulfoxide (40%) and sulfone (27%). These results offer further insight into the metabolism of benzimidazole drugs and highligh




J Vet Pharmacol Ther. 2003 Aug;26(4):297-302.
Stereospecific biotransformation of albendazole in mouflon and rat-isolated hepatocytes.

Velik J, Baliharova V, Skalova L, Szotakova B, Wsol V, Lamka J.

Department of Pharmacology and Toxicology and Department of Biochemical Sciences, Faculty of Pharmacy, Charles University, Hradec Kralove, Czech Republic. 95vej229af.cuni.cz

The anthelmintic albendazole (ABZ) undergoes a two-step oxidation resulting first in the formation of chiral albendazole sulfoxide (ABZSO) followed by its transformation to albendazole sulfone (ABZSO2) in many farm and laboratory animal species. Although cloven-hoofed game are also treated with ABZ, limited information concerning ABZ biotransformation in these species is available. The present study focused on in vitro ABZ sulfoxidation in hepatocytes from wild sheep-mouflon (Ovis musimon) and comparison of ABZ sulfoxidation in mouflon and rat (Rattus norvergicus) hepatocytes. ABZ was used as a substrate for primary cultures of mouflon and rat hepatocytes. Time-dependent stereospecific consumption of ABZSO and ABZSO2 formation has been investigated. The metabolites were determined by high-performance liquid chromatography with both achiral and chiral stationary phases. Although total-ABZSO formation did not significantly differ between mouflon and rat, after separation of the (+)-ABZSO and (-)-ABZSO enantiomers a significant difference between species was found. The enantiomeric ratio of (+)/(-)-ABZSO in mouflon hepatocytes was 2.8-3.8, while rat hepatocytes biotransformed ABZ to almost racemic ABZSO, with an enantiomeric ratio of 1.0-1.1. The ratio were similar for two concentrations of substrate used and stable over several time intervals. The formation of ABZSO2 was more extensive in rat (approximately five times) than in mouflon hepatocytes.

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