Microtubules synthesis Inhibitors
Class name Benzimidazole
Agents included are Thiabendazole, Albendazole and Mebendazole
Pharmacodynamics:- Benzimidazoles act against worms by inhibiting
micro-tubules synthesis. They inhibit beta-tubulin factors which further
activate a gene. By interacting with a gene it inhibit gene production (prevent
protein synthesis) and thus compromise cytoskeletal formation, and due to compromise
cytoskeletal formation the locomotion , attachment and other activities of worm
stops and lead to death.
Pharmacokinetics:- All the drug included in this class are in oral dosage form
(tablets and suspensions). They have comparatively different pharmacokinetic
profile. Pharmacokinetic profile of each drug is show below.
Mebendazole:- Mebendazole
is less then 10 % orally absorbed. Just like Albendazole it is highly protein
bounded. Same excretion occur through Kidney.
Both Albendazole and Mebendazole has increase in absorption when given
with food.
Thiabendazole:- It may be absorbed through the
skin but this rout is not recommended for administration. The drug is rapidly
absorbed from GIT and its metabolism is in liver by Glucronidation and
sulfonate conjugation and excreted in urine.
ADRs: - Albendazole is gentle and have fewer
side effect then others and it is well tolerated.
Common side effect of these drug are
abdominal distress (NVD) , headache , dizziness , liver enzymes elevation,
fatigue and some serological problems.
Hypersensitivity may occur (cross
Hypersensitivity may occur).
Thiabendazole can cause Stevens-Johnson syndrome and Irreversible liver
failure.
Contraindications:- All Benzimidazoles are
contraindicated in pregnancy, children less then 2 year old and liver
cirrhosis.
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