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Published in Caroline Ashley, Aileen Dunleavy, John Cunningham, The Renal Drug Handbook, 2018
Caroline Ashley, Aileen Dunleavy, John Cunningham
Albendazole rapidly undergoes extensive first-pass metabolism. Its principal metabolite albendazole sulfoxide has anthelmintic activity and a plasma half-life of about 8.5 hours. Albendazole sulfoxide is widely distributed throughout the body including into the bile and the CSF. It is about 70% bound to plasma protein. Albendazole sulfoxide is eliminated in the bile; only a small amount appears to be excreted in the urine
Albendazole
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Results indicated that the pharmacokinetic profile of albendazole sulfoxide has been examined in a crossover fashion following administration of suspension and tablet formulations of albendazole (Penicaut et al., 1983). The pharmacokinetic parameters for albendazole sulfoxide were similar between formulations (Table 200.1). These results suggest that the poor absorption characteristics of albendazole are not formulation related.
Antiparasitic Drugs
Published in Thomas T. Yoshikawa, Shobita Rajagopalan, Antibiotic Therapy for Geriatric Patients, 2005
Albendazole has expanded the therapeutic options for patients with cystic hydatid disease due to Echinococcus granulosus (37). Surgery remains the mainstay of treatment for this disease, but it carries the risks of operative morbidity, recurrence of cysts, and spillage of fluid from the cysts, which can lead to anaphylaxis or dissemination of the infection (38). Albendazole reduces the viability of protoscolices and cysts, and its hepatic metabolite, albendazole sulfoxide, is also active against the larval cestodes. The administration of albendazole prior to surgery has been advocated in order to inactivate protoscolices and minimize the likelihood of recurring cysts (39). Drug therapy is also indicated after the spontaneous or operative rupture of cysts, and the spillage of their contents, to prevent secondary dissemination. The usual 4-week course of treatment (Table 2) often needs to be repeated two or more times. The absorption of albendazole is enhanced by taking it with fatty meals.
Albendazole solid dispersions prepared using PEG6000 and Poloxamer188: formulation, characterization and in vivo evaluation
Published in Pharmaceutical Development and Technology, 2020
Chun-Liu Dong, Si-Di Zheng, Yan-Yan Liu, Wen-Qiang Cui, Mei-Qi Hao, Bello-Onaghise God’spower, Xue-Ying Chen, Yan-Hua Li
Albendazole (ABZ, methyl [5-(propylthio)-1-H-benzimidazol-2yl]carbamate) (Figure 1) belonging to the benzimidazole carbamate, is a broad-spectrum anthelmintic agent and used as ovicide and larvicide (Balaji et al. 2007). ABZ is the first choice of WHO to treat with thorn ball larva disease in humans and animals, which has been widely used in the treatments of echinococcosis, hydatid cysts, and neurocysticercosis. Due to the low water solubility (0.01 mg/mL in the water at 25 °C) and high permeability (Tanaka et al. 2013), ABZ is classified as class II drug based on the Biopharmaceutical Classification System. Because of the low aqueous solubility, ABZ is poorly and erratically absorbed following oral administration. Moreover, ABZ could be rapidly and successively metabolized to albendazole sulfoxide (ABZ-SO) and albendazole sulfone (ABZ-SO2) when orally administered. ABZ-SO, the main anthelmintically active metabolite, has been discovered in blood and tissue after administration. However, poor/erratic gastrointestinal (GI) absorption hinders the clinical efficacy of albendazole compounds.
Current approaches to cysticidal drug therapy for neurocysticercosis
Published in Expert Review of Anti-infective Therapy, 2020
After being reviewed the recommended therapeutic approaches with cysticidal drugs for the different forms of presentation of NCC, it is important to describe the mechanisms of action of both albendazole and praziquantel and the reason why combined therapy is better than the use of a single drug. Praziquantel is a pyrazino-isoquinoline derivative. It affects calcium channels in the parasite’s surface and produces muscle contractions, paralysis, and damage of the tegument [100]. Albendazole is a benzimidazole compound that leads to selective degeneration of parasite cytoplasmic microtubules, affecting ATP formation, and also impairing glucose intake, leading to energy depletion and parasite starvation [101]. It binds to tubulin and thus interferes with cell division of the parasite. Albendazole is not active by itself, as the active molecule is albendazole sulfoxide, which results from liver metabolism of albendazole [102]. The rationale for combined therapy was noticed in a Phase II trial, where it was demonstrated a significant increase (more than 50%) in albendazole sulfoxide concentrations in patients receiving concomitant praziquantel therapy (after about 9 days of combined therapy) [103]. This, together with the attack of parasites by different pathways at the same time provide a rationale for the use of combined therapy in moderate-to-severe forms of NCC.
In vitro inhibition of the hepatic S-oxygenation of the anthelmintic albendazole by the natural monoterpene thymol in sheep
Published in Xenobiotica, 2020
Victoria Miró, Adrian Lifschitz, Paula Viviani, Carolina Rocha, Carlos Lanusse, Livio Costa, Guillermo Virkel
Reference standards (99% pure) of ABZ, albendazole sulfoxide (ABZSO), albendazole sulfone (ABZSO2) and oxibendazole (OBZ) were provided by Sigma-Aldrich Argentina. Stock solutions (5, 0.5, and 0.25 mM) of each BZD molecule were prepared in methanol (Baker Inc., Phillipsburg, USA). Benzydamine, benzydamine N-oxide, ethoxyresorufin, and resorufin were from Sigma-Aldrich Argentina. Nicotinamide adenine dinucleotide phosphate (NADP+), glucose-6-phosphate and glucose-6-phosphate dehydrogenase were from Roche and provided by Merck Argentina. Thymol (98.5% pure) was from Sigma-Aldrich Argentina. Buffer salts (KCl, NaCl, NaHCO3, Na2HPO4, NaH2PO4, K2HPO4, KH2PO4 and CH3COONH4, MgCl2, KH2PO4) and HPLC solvents (methanol and acetonitrile) were obtained from J.T Baker-Avantor (USA).