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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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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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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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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