Albendazole (pharmacology)

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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