Disease relevance of Albendazole sulfoxide

• Albendazole and its main metabolite, albendazole-sulphoxide, were assayed in the serum from peripheral and portal blood, the liver, bile, lungs, and hydatid cyst walls and fluid [1].
• Owing to the known toxicity of the ABZSO, we stress the need for careful control to ensure adherence to the prescribed withdrawal time [2].
• The present study investigates the urinary excretion of the enantiomers of (+)- and (-)-albendazole sulfoxide (ASOX) and albendazole sulfone (ASON) in 12 patients with neurocysticercosis treated with albendazole for 8 days (7.5 mg/kg/12 h) [3].

High impact information on Albendazole sulfoxide

• In vitro comparisons demonstrated that the efficacy of albendazole, albendazole-sulfoxide, and albendazole-sulfone against pathogenic Encephalitozoon species was proportional to the degree of oxidation at a concentration of >10(-3) microgram/ml [4].
• Significant increase in non-disjunction events that involved either chromosome were observed in cells treated with ABZ or ABZSO [5].
• In the present work, we investigated the ability of ABZ and ABZSO to induce non-disjunction in cultured human lymphocytes [5].
• Both CYP3A substrates induced a reduction in the production of (-) ABZSO (sheep = 67-78%, cattle = 50-78%) by lung microsomes [6].
• These data indicate that the transport of ASOX through the blood-brain barrier is not enantioselective, but rather depends on passive diffusion [7].

Biological context of Albendazole sulfoxide

• The area under the plasma concentration vs time curve (AUC) values for ABZSO were higher in both artificially infected (64.0 micrograms h ml-1) and naturally infected (79.3 micrograms h ml-1) sheep as compared with non-infected animals (41.8 micrograms h ml-1) [8].
• Pharmacokinetics of ricobendazole after its intravenous, intraruminal and subcutaneous administration in sheep [9].
• The enantioselective disposition kinetics of the benzimidazole anthelmintic, ricobendazole (RBZ), have been characterized after its intravenous (iv) and subcutaneous (sc) administration as a racemic formulation to cattle [10].
• Ricobendazole bioavailability was poor after i.r. administration, whereas high and sustained plasma concentrations and higher bioavailability were obtained after s.c. administration [9].

Anatomical context of Albendazole sulfoxide

• 1. Two distinct microsomal pathways involved in the metabolism of albendazole (ABZ) to albendazole-sulphoxide (SO.ABZ) by pig liver microsomes have been identified and quantified [11].
• Study of the distribution of albendazole-sulphoxide (ABZ-SO) in fertilized egg compartments [12].
• 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 [13].

Associations of Albendazole sulfoxide with other chemical compounds

• MTZ did not affect the sulfoxidation of ABZ by lung microsomes, which may indicate that FMO is not involved in the production of ABZSO in this tissue [6].
• Cimetidine tended to decrease Cmax by 52% (P = 0.109) and significantly inhibited ABZSX breakdown as indicated by the prolongation of ABZSX elimination half-life from 7.4+/-3.3 hr to 19.0+/-11.7 hr (P = 0.028) [14].
• Albendazole versus ricobendazole (albendazole-sulphoxide) against enteral and parenteral stages of Trichinella spiralis in mice [15].
• A simple, rapid and reliable high performance liquid chromatographic (HPLC) method has been developed and validated for simultaneous determination of ricobendazole (RBZ) and its main metabolite albendazole sulfone (ABZSO(2)) in sheep plasma using an isocratic system with UV detection [16].
• Calves of groups 1-3 were treated, respectively, with subcutaneous injection of ivermectin (200 mcg/kg), ricobendazole (4 mg/kg) and levamisole (7.5 mg/kg), while calves of group 4 remained as untreated controls [17].

Analytical, diagnostic and therapeutic context of Albendazole sulfoxide

• AbzSOX concentrations were measured by reverse phase HPLC [18].
• However, considerable levels of ABZSO were detected in milk collected within 24 h after treatment as well as in products and by-products derived from such milk [2].
• ABZSO plasma availability was significantly greater after the ABZ-SLS (164%) co-administration compared to that obtained in the control group without surfactant [19].
• Samples were analysed by high performance liquid chromatography for ABZ, ABZSO and albendazole sulphone (ABZSO2) [20].
• Ricobendazole kinetics and availability following subcutaneous administration of a novel injectable formulation to calves [21].

References