Vet Res Commun. 2003 Oct;27(7):555-66. Aspects of the pharmacokinetics of albendazole sulphoxide in sheep.
Goudah A.
Pharmacology Department, Faculty of Veterinary Medicine, Cairo University, Giza, PO Box 12211, Giza, Egypt. aymangoudotmail.com
The plasma disposition kinetics of albendazole sulphoxide (ABZSO), ((+)ABZSO and (-)ABZSO) and its sulphone metabolite (ABZSO2) were investigated in adult sheep. Six Corriedale sheep received albendazole sulphoxide by intravenous injection at 5 mg/kg live weight. Jugular blood samples were taken serially for 72 h and the plasma was analysed by high-performance liquid chromatography (HPLC) for albendazole (ABZ), ABZ sulphoxide (ABZSO) and albendazole sulphone (ABZSO2). Albendazole was not detected in the plasma at any time after the treatment, ABZSO and ABZSO2 being the main metabolites detected between 10 min and 48 h after treatment. A biexponential plasma concentration versus time curve was observed for both ABZSO and ABZSO2 following the intravenous treatment. The plasma AUC values for ABZSO and ABZSO2 were 52.0 and 10.8 (microg x h)/ml, respectively. The ABZSO2 metabolite was measurable in plasma between 10 min and 48 h after administration of ABZSO, reaching a peak concentration of 0.38 microg/ml at 7.7 h after treatment. Using a chiral phase-based HPLC method, a biexponential plasma concentration versus time curve was observed for both ABZSO enantiomers. The total body clearance was higher for the (-) than for the (+) enantiomer, the values being 270.6 and 147.75 (ml/h)/kg, respectively. The elimination half-life of the (-) enantiomer was shorter than that of the (+) enantiomer, the values being 4.31 and 8.33 h, respectively. The enantiomeric ratio (+)ABZSO/( )ABZSO at t0 was close to unity. However, the ratio in the plasma increased with time.
Filaria J. 2003 Nov 6;2(1):15. Treatment of co-infection with bancroftian filariasis and onchocerciasis: a safety and efficacy study of albendazole with ivermectin compared to treatment of single infection with bancroftian filariasis.
Makunde WH, Kamugisha LM, Massaga JJ, Makunde RW, Savael ZX, Akida J, Salum FM, Taylor MJ.
Bombo Research Field Station, P,O, Box 950, Tanga, Tanzania. hwmakundotmail.com
BACKGROUND: In order to use a combination of ivermectin and albendazole for the elimination of lymphatic filariasis, it is important to assess the potential risk of increased adverse events in individuals infected with both lymphatic filariasis and onchocerciasis. We compared the safety and efficacy of albendazole (400 mg) in combination with ivermectin (150 micrograms/kg), for the treatment of co-infections of Wuchereria bancrofti and Onchocerca volvulus with single infection of W. bancrofti. METHODS: The safety study on co-infections was a crossover, double blind design, while for the single infection of bancroftian filariasis an open design comparing two treatments was used. For co-infection, one group was allocated a single dose of ivermectin (150 micrograms/kg) plus albendazole (400 mg) (Group A). The other group received placebo (Group B). Five days later the treatment regime was reversed, with the Group A receiving placebo and Group B receiving treatment. For the single bancroftian filariasis infection, one group received a single dose of albendazole (400 mg) plus ivermectin (150 microg/kg) (Group C) while the other group received a single dose of albendazole (400 mg) alone (Group D). Blood and skin specimens were collected on admission day, day 0, and on days 2, 3, and 7 to assess drug safety and efficacy. Thereafter, blood and skin specimens were collected during the 12 months follow up for the assessment of drug efficacy. Study individuals were clinically monitored every six hours during the first 48 hours following treatment, and routine clinical examinations were perfo
J Chromatogr B Analyt Technol Biomed Life Sci. 2004 Jan 25;799(2):233-8. Albendazole sulphoxide concentrations in plasma of endemic normals from a lymphatic filariasis endemic region using liquid chromatography.
Sarin R, Dash AP, Dua VK.
Institute of Life Sciences, Nalco square, Chandrasekharpur, Near Kalinga Hospital, Bhubaneswar, Orissa 751023, India. reemasarinahoo.com
A simple and sensitive reversed-phase isocratic HPLC method for the determination of albendazole and its metabolites has been developed. The mobile phase consisting of acetonitrile-water-perchloric acid (70%) (30:110:0.06 (v/v/v)) was pumped at a flow rate of 0.80 ml/min on a 5 microm, reverse phase, Discovery RPamide C16 column with UV detection at 290 nm. The calibration graphs were linear in the range of 0.05- 1 microg/ml for albendazole, albendazole sulphoxide and albendazole sulphone. The limit of quantification was 50 ng/ml for albendazole, 25 ng/ml for albendazole sulphoxide and 30 ng/ml for albendazole sulphone. The within-day and day-to-day coefficient of variation averaged 4.98 and 6.95% for albendazole, 3.83 and 6.83% for albendazole sulphoxide and 3.44 and 5.51% for albendazole sulphone, respectively. The mean extraction recoveries of albendazole, albendazole sulphoxide and albendazole sulphone were 79.25, 93.03 and 88.78%, respectively. The method was applied to determine the plasma levels of albendazole sulphoxide in endemic normals administered with albendazole during pharmacokinetic studies.
Am J Trop Med Hyg. 2002 Mar;66(3):260-3. Effect of grapefruit juice or cimetidine coadministration on albendazole bioavailability.
Nagy J, Schipper HG, Koopmans RP, Butter JJ, Van Boxtel CJ, Kager PA.
Department of Internal Medicine, Academic Medical Center, Amsterdam, The Netherlands.
The assumed metabolic breakdown of albendazole by mucosal CYP3A4 enzymes was studied by coadministering albendazole (10 mg/kg) with grapefruit juice. Concentrations of albendazole sulfoxide (ABZSX), the active metabolite of albendazole, were compared with those after albendazole was administered with water, a fatty meal, or grapefruit juice plus cimetidine (10 mg/kg). In comparison to water, maximum ABZSX concentration (Cmax) was enhanced 6.5-fold by a fatty meal (from 0.24 +/- 0.09 mg/l to 1.55 +/- 0.30 mg/l; mean +/- SD; P < 0.001) and 3.2-fold by grapefruit juice (from 0.24 +/- 0.09 mg/l to 0.76 +/- 0.37 mg/L; P = 0.031). When grapefruit juice was combined with cimetidine, Cmax was significantly lower than with grapefruit juice alone (0.41 +/- 0.29 mg/l and 0.76 +/- 0.37 mg/l, respectively; P = 0.022). The area under the concentration-time curve from 0 to infinity (AUC(0-omega)) followed a comparable pattern. Half-life (T(1/2)) was 8.8 +/- 4.2 hr and 8.2 +/- 4.3 hr after administration with water or a fatty meal (P = 1.000). Grapefruit juice shortened T(1/2) by 46% (P = 0.026). We hypothesize that albendazole is metabolized by CYP3A4 enzymes in the intestinal mucosa. This process can be inhibited by grapefruit juice. Cimetidine decreased albendazole bioavailability.
J Vet Pharmacol Ther. 2003 Dec;26(6):421-7. Metabolism and residue depletion of albendazole and its metabolites in rainbow trout, tilapia and Atlantic salmon after oral administration.
Shaikh B, Rummel N, Gieseker C, Serfling S, Reimschuessel R.
Food and Drug Administration, Center for Veterinary Medicine, Office of Research, Laurel, MD 20708, USA. bshaikvm.fda.gov
Metabolic and residue depletion profiles of albendazole (ABZ) and its major metabolites in three fish species, rainbow trout, tilapia and Atlantic salmon are reported. Based on these profiles, similarities (or dissimilarities) between species will determine the potential to group fish species. ABZ at 10 mg/kg body weight was incorporated into fish food formulated in a gelatin base or in gel capsule and fed as a single dose to six fish from each species. Rainbow trout were held three each in a partitioned 600-L tank. Tilapia and Atlantic salmon were housed in separate 20-L tanks. Samples of muscle with adhering skin were collected at 8, 12, 18, 24, 48, 72, and 96 h postdose from trout kept at 12 degrees C, at 4, 8, 12, 24, 48, 72, 96, 120, and 144 h postdose from tilapia kept at 25 degrees C and at 8, 14, 24, 48, 72, and 96 h postdose from Atlantic salmon kept at 15 degrees C. The samples were homogenized in dry ice and subjected to extraction and cleanup procedures. The final extracts were analyzed for parent drug ABZ and its major metabolites, albendazole sulfoxide (ABZ-SO), albendazole sulfone (ABZ-SO2) and albendazole aminosulfone using high-performance liquid chromatography with fluorescence detection. ABZ was depleted by 24 h in trout and tilapia and by 48 h in salmon; ABZ-SO, a pharmacologically active metabolite, was depleted by 48 h in tilapia, by 72 h in rainbow trout and was present until 96 h in salmon; and low levels of ABZ-SO2 and albendazole aminosulfone, both inactive metabolites, were detectable at least till 96 h in all three fish species.
Xinjiang Centers of Diseases Prevention and Control National Hydatid Disease Center of China, Xinjiang, Urumqi 830002, PR China. jchaj.cninfo.net
Two regimens of albendazole emulsion (AbzE), a novel formulation, were used in the treatment of 264 cases of hepatic cystic echinococcosis. AbzE 10 mg/kg per day (calculated by albendazole base) was administered orally to 71 cases for 6 months to over 1 year. Imaging evaluation at the end of courses showed overall efficacy in 97.2%, (cure rate 60.6%, and inefficacy rate 2.8%); The follow-up study on 62 cases 3-4 years post therapeutic courses showed overall efficacy in 92.0% (cure rate 83.9%, ineffective rate 1.5% and recurrence rate 6.5%); Abz 12.5 mg/kg per day was administered orally to 193 cases for 3 months to over 1 year, resulting in an overall efficacy of 97.9%, (cure rate 75.1% and inefficacy rate 2.1%). The follow-up study in 139 cases 2-4 years post treatment demonstrated efficacy in 89.2%, (cure rate 84.2% and recurrence rate 10.8%); Mild reversible adverse reactions were observed in 14.4% of the patients. Retreatment of recurrent hydatidosis patients with AbzE provided promising results. AbzE is considered to be superior to the albendazole tablet or capsule formulations currently used in treatment of liver cystic hydatid disease.
Afr J Health Sci. 1994 Nov;1(4):169-174. Echinococcus granulosus: ultrastructural effect of albendazole therapy.
Magambo JK, Zeyhle E, Nganda NT, Raasen T, Wachira J.
Faculty of Health Sciences, Moi University, Eldoret, Kenya.
The effects of the anthelmintic Albendazole against Echinococcus granulosus hydatid cysts in Turkana patients given orally were studied by means of ultrasound as well as light microscopy, scanning and transmission electron microscopy. The treatment generally reduced the size of the cyst mass, making the patients feel well. The drug therapy caused collapse of the cyst wall and daughter cyst. The pathological changes on the germinal layer of Albendazole-treatment cysts differed widely from the untreated control hydatid tissue. The effects included morphological changes of the protoscolices, presence of lamellated bodies, necrosis with detachment of the germinal layer from the laminated layer. However, some parts of the Albendazole-treated hydatid tissue remained unaffected.
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12153343&dopt=Abstract albendazole Albenza [PubMed - as supplied by publisher]
