Antimicrotubules Flashcards
types of antimicrotubules
Inhibition of Polymerization
- Colchicine
- Vinca alkaloids
(vincristine, VInblastine, vinorelbine)
Inhibition of Depolymerization:
- Taxanes
MOA of antimicrotubule
MOA: Binds to tubulin, a protein that compromised of alpha and beta subunits, inhibit its polymerization. (Polymerization of tubulin is responsible for the formation of the mitotic spindle during the metaphase period of mitosis)
Vinca-Induced Toxicities
In general..
•All vincas have very low emetogenic potential! •Vesicants!
•Alopecia
Vincristine toxicities
Vincristine
•Peripheral neuropathy: maximum dose is 2 mg weekly •Ileus, constipation
•Rarely causes bone marrow suppression
Vinblastine and Vinorelbine toxicities
Vinblastine and Vinorelbine
•Dose limiting neutropenia and thrombocytopenia
•Neurologic toxicity and constipation can also occur but much lesst han vincristine
When should we adjust dose if pt take vinca alkaloid?
- ## MUST adjust doses when patient experiences hepatic dysfunction!
Vinca alkaloid interaction cyp
Many drug interactions (substrate for CYP3A4)
Antidote for vesicant effect in vinca alkaloid
- Agents are potent vesicants, apply warm pack and administer hyaluronidase 1ml as an antidote
__________ administration of vinca alkaloid is fatal.
Intrathecal administration of these agents is FATAL
Taxanes MOA
Mechanism of action: similar to vincas; except the taxanesbind preferentially to the microtubules shifting the microtubules towards polymerization –the taxanesthen stabilize against depolymerization
Taxanes require ___________________
Premedications Required for Taxanes
taxanes drugs
(Paclitaxel, Docetaxel, Ixabepilone)
Premedication for Paclitaxel
Paclitaxel (Taxol®, Anzatax®)
- PREMEDICATIONS for Hypersensitivity
- Give H1-blocker, H2-blocker, Corticosteroids
- If given Albumin stabilized anoparticle version (Abraxane®) –no premed required !
Premed for Docetaxel
Docetaxel(Taxotere®)
- PREMEDICATIONS for Edema
- Give Dexamethasone starting on the day before chemo
premed for Ixabepilone
Ixabepilone (Ixempra®)
- PREMEDICATIONS for Hypersensitivity
- Give H1 and H2 blockers: Diphenhydramine 50 mg and Ranitidine 150-300 mg PO 30 minutes before treatment