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ANTIMICROTUBULES PHL 417

This article provides an overview of the mechanism of action, therapeutic uses, and side effects of two classes of antimicrotubule agents - Vinca alkaloids and Taxanes. Vinca alkaloids inhibit microtubule polymerization, while Taxanes enhance microtubule assembly.

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ANTIMICROTUBULES PHL 417

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  1. ANTIMICROTUBULES PHL 417

  2. ANTIMICROTUBULE AGENTS

  3. 1. Vinca Alkaloids • Vinblastine • Vincristine • Vinorelbine

  4. Vinca Alkaloids They are plant alkaloids extracted fromPeriwinkle plant (Vinca Rosa) 3 3

  5. VincaAlkaloidsMechanism of Action • They act by binding to  and tubulin and inhibit its polymerization into microtubules leading to preventing spindle formation in mitosing cells. • Resulting in mitotic arrest at metaphase, dissolution of the mitotic spindle, and interference with chromosome segregation. • CCS agents- M phase

  6. Vinca alkaloid Mechanism of resistance • 1- Pleiotropic drug resistances i.e. cross-resistant to a wide range of chemically dissimilar agents: vinca alkaloid, epidophyllotoxin, anthracyclines and colchicine. Due to: High level of P-glycoprotein • 2- Mutation in either  and tubulinthat prevent effective binding of vinca alkaloids

  7. Vinca alkaloidTherapeutic uses

  8. Vinca alkaloid Side effects

  9. 2. Taxanes • Paclitaxel (Taxol) • Docetaxel • Alkaloid esters derived from the bark of ash tree (Taxus brevifolia).

  10. Taxanes (cont.)Mechanism of Action • Taxanes enhance assembly of microtubules and stabilize them against depolymerization. • It binds to tubulin (at a site distinct from that used by vinca alkaloids) and promotes assembly of microtubules giving non-functional microtubule network.

  11. Taxanes (cont.)Toxicity • Paclitaxel • Neutropenia, thrombocytopenia • Peripheral neuropathy • Docetaxel • Bone marrow suppression • Neurotoxicity • Fluid retention

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