This document summarizes information about the drug Albendazole. It begins with an introduction stating that Albendazole is a broad-spectrum anthelmintic drug developed in 1975 that is used to treat various helminth infections. It then covers Albendazole's chemistry, pharmacokinetics, mechanism of action, clinical indications, adverse effects, contraindications, and drug interactions. The key points are that Albendazole is a benzimidazole carbamate derivative that is metabolized in the liver and excreted in bile. It works by inhibiting helminth microtubule polymerization. Its clinical uses include treatment of ascariasis, cysticercosis, and other nematode

2. TOPIC; ALBENDAZOLE
 PRESENTED BY;
 M. BAQIR NAQVI
 Class no; 27 (M)- 3RD PROFF
 PRESENTED TO;
 MR. ZAHID RASUL NIAZI
Faculty of Pharmacy,
 Gomal university, Dera ismail khan.
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3. index
Theme; anthelmintics.
Introduction; Albendazole.
Chemistry
Pharmacokinetics
Mode of action
Clinical indications
Adversities
Contraindications
Drug interactions
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4. ANTHELMINTHICS;
Anti- against and Helminthes- Worms
‘’Any curative drug, used to
eradicate or reduce the number of
worms in GIT or tissue is called
anthelminthic. ’’
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6. TYPES OF HELMINTHES;
Nematodes
Trematodes
Cestodes
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8. 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.
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9. CHEMISTRY;
 Chemically albendazole consist of;
 “ Benzimedazole carbamate derivative ’’
 Molecular wt.; 265.34
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10. 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

11.  METABOLISM;
 Metabolized in liver by “ oxidation reactions ‘’.
 Oxidized into albendazole sulfoxide, by cytochrome p450 oxidases and
flavin mono oxigenases.
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12.  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.
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13. MECHANISM OF ACTION;
1) Degenerative changes by binding to the colchicine sensitive
site of b-tubulin, thus assembly of microtubules is disturbed
and polymerization is inhibited.
2) inhibit nutritional & glucose uptake.
3) Inhibits formation of spindle fibers for cell division, i.e it
blocks the egg production & development.
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15.  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.
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17. NEMATODE INFECTIONS;
• Ascariasis.(ints.obstruction, infect lungs)
Round worms (ascheris lumbricoides)
• Enterobiasis. (pruritic anus, stool with worms)
Pin worm ( enterobious vemicularis)
• Ansylostomiasis.(chronic ints. Blood loss)
Hook worm (Ancylocystoma dudenale)
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18. • Strongyloidiasis.
(it overcome immune system)
Thread worm
(Strongyloids stacomalis)
• Trichuriasis. (asymptomatic, but pain,
diarrhea etc.)
Whip worm
(Trichuris trichura)
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19. CESTODE INFECTIONS;
• Cysticercosis.(cysts in brain, nails & eyes.)
Pork tapeworm (tenia solium)
• Drug of choice,
• Dose; 400mg B.D ( 8-12 days)
Neurocysticercosis.
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20. 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.
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21. CONTRA INDICATIONS;
 Hepatotoxicity.
 Known hypersensitivity.
 Pregnancy.
 Children below 2 years.
Brands in Pakistan;
 ZENTEL. (Glaxosmithkline)
 JENZOLE. (Jawa pharmaceuticals)
 BENDAZOLE. (Stanley pharmaceuticals)
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22. 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.
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23. Refrences;
 Lippincott’s Pharmacology (5th 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.
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