Albendazole

Wormicide

1. TOPIC; ALBENDAZOLE PRESENTED BY; M. BAQIR NAQVI Class no; 27 (M)- 3 RD PROFF PRESENTED TO ; MR. ZAHID RASUL NIAZI Faculty of Pharmacy , Gomal university, Dera ismail khan . 2

2. index 3

3. ANTHELMINTHICS; 4

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5. TYPES OF HELMINTHES; 6

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7. ALBENDAZOLE; INTRODUCTION; Developed in 1975. Congener of mebendazole . A broad-spectrum anthelmintic used in mixed helminthic infections. Vermicidal , larvicidal and ovicidal . Patient compliance bcz of single dose. Wide safety profile with low toxicity. Drug of choice for cestodal infections. 8

8. CHEMISTRY; Chemically albendazole consist of; “ Benzimedazole carbamate derivative ’’ Molecular wt.; 265.34 9

9. Pharmacokinetics; ADMINISTRATION; Oral administration. Given empty stomach;-- in case of Tissue parasite. Given with fatty meal;-- in case of interlumener parasite. Available in Syrup & tablet forms. ABSORPTION; In humen ----- 1-5 % In rats --------- 20-30 % In cattle ------ 50 % Absorption rate is enhanced at lower Gastric pH. 10

10. METABOLISM; Metabolized in liver by “ oxidation reactions ‘’. Oxidized into albendazole sulfoxide , by cytochrome p450 oxidases and flavin mono oxigenases . 11

11. EXCRETION; In human; mostly in Bile. ( only less than 1% through urine.) In ruminants ; about 60-70 % through urine. SOLUBILITY ; Poor water soluble. Albendazole is lipid soluble, so fatty meal enhances its absorption, allowing it to cross lipid barrier created by mucous surface of GIT. HALF LIFE ; Generally 7 – 8.5 hours. 12

12. MECHANISM OF ACTION; Degenerative changes by binding to the colchicine sensitive site of b-tubulin , thus assembly of microtubules is disturbed and polymerization is inhibited. inhibit nutritional & glucose uptake . Inhibits formation of spindle fibers for cell division, i.e it blocks the egg production & development. 13

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14. Release lysozyme that causes Degenrative changes in reticulum & mitochondria. ATP production is decreased, bcz drug inhibits metabolic enzymes i.e Malate dehydrogenase & fumerate reductase . INDICATIONS; Filariacis ; ( wucheria bancrofti ) Blockage of lymph flow, arms & legs filled with fluid, causing elephantiasis. Hydatid disease ; ( echnococcus granularis ) Cyst formation in alveoli, liver, peritoneal cavity. 15

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16. NEMATODE INFECTIONS; 17

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18. CESTODE INFECTIONS ; 19

19. ADVERSE EFFECTS; Highly efficacious, low toxicity profile. But high dose causes; GIT ; nausea, vomiting, abdominal pain. (in 10% patients.) Alopecia. (Rarely) CNS; Headache, Dizziness, seizures in case of extreme dose. HEPATIC; Jaundice, hepatitis, acute liver failure. Leukopenia, in 1% patients. HYPERSENSITIVITY; Rashes, pruritis , urticheria , fever. 20

20. CONTRA INDICATIONS; Hepatotoxicity. Known hypersensitivity. Pregnancy. Children below 2 years. Brands in Pakistan; ZENTEL . ( Glaxosmithkline ) JENZOLE . ( Jawa pharmaceuticals) BENDAZOLE . (Stanley pharmaceuticals) 21

21. Drug-Drug interactions; Antacids (cimetidine) > Half life of Albendazole from 8-19 hours. Bcz it lower the absorption rate of albendazole by reducing gastric acidity. Anti-retro viral drugs inhibit cytochrome p450 enzyme, so inhibit metabolism of albendazole . Phenytoin < half life of albendazole , by lowering its plasma concentration. 22

22. Refrences ; Lippincott’s Pharmacology (5 th edition) www.Wikipedia.com Slideshare.com Basic concept of pharmacology. (Mr. Inayatulallah Bhatti) Dr. Zahid Rasul Niazi Lectures. BUNDLE OF THANKS FOR UR ATTENTION--- Compiled by; Syed Baqir Naqvi . 23