COLCHICINE
BRAND NAME:- ZYCOLCHIN, GO UNTIL 0.5mg tab.
COLCHICINE is an alkaloid used to prevent or treat gout attacks (flares), and is also used to prevent attacks of pain in the abdomen, chest, or joints caused by a certain inherited disease (familial Mediterranean fever).
PHARMACODYANIMCS :-
Colchicine reduces the pain resulting from gout and reduces flares of Familial Mediterranean fever by interfering with inflammatory pathways.This drug has a narrow therapeutic index.
PHARMACOKINETICS:-
Colchicine is rapidly absorbed orally, partly metabolized in liver and excreted in bile - undergoes enterohepatic circulation; ultimate disposal occurs in urine and faeses over many days. Binding of colchicine to intracellular tubulin contributes to its large volume of distribution and slow elimination. Inhibitors of CYP3A4 retard colchicine metabolism and enhance its toxicity.
MECHANISM OF ACTION:-
The exact mechanism of action of colchicine has not been fully established, however likely occurs via the downstream inhibition of inflammation caused by tubulin disruption.2 Studies have implied that that colchicine causes disruption of the inflammasome complex that is present in both monocytes and neutrophils, which normally leads to the activation of interleukin-1, an important mediator of inflammation.3 In addition to the above actions, colchicine acts to interfere with pathways including neutrophil adhesion and recruitment, superoxide production, the RhoA/Rho effector kinase (ROCK) pathway, as well as a type of nuclear factor κΒ (NF-κΒ) pathway, reducing inflammation.
On a molecular level, colchicine can be described as an anti-mitotic drug, blocking the mitotic activity cells in the metaphase part of the cell cycle. Specifically, colchicine binds to tubulin, forming complexes that bind to microtubules. This stops their elongation. At low concentrations, colchicine stops microtubule growth and, at elevated concentrations, colchicine causes the depolymerization of microtubules.
USE:-
Treatment of acute gout, Prophylaxis shock.
SIDE EFFECTS:-
Diarrhea, nausea, cramping, abdominal pain, and vomiting may occur.
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