Mitotic Inhibitors Flashcards Preview

Oncology > Mitotic Inhibitors > Flashcards

Flashcards in Mitotic Inhibitors Deck (16)
Loading flashcards...
0
Q

Taxanes (3)

A

Paclitaxel
Docetaxel
Cabazitaxel

1
Q

Vinka alkaloids (3)

A

Vinicristine
Vinblastine
Vinorelbine

2
Q

Epothilones

A

Ixabepilone

3
Q

Mitotic inhibitors MOA

A

Inhibit the essential hyper-dynamic changes in micro tubule structure
Mitotic arrest–> apoptosis

4
Q

Vinka alkaloids MOA

Cell cycle M-phase specific (schedule dependent)

A

Inhibit microtubule elongation or polymerization
Drug binds where next subunit will bind on microtubule (not on subunit that is suppose to bind)
4-deacetyl is major inactive metabolite

5
Q

Taxanes and Epothilone MOA

A

Inhibit depolymerization or microtubule shortening

Drug Binds to a specific site on beta tubulin subunit

6
Q

Vinka alkaloids ADR

A

Severe vesicant/extravasation

intrathecal injection is FATAL BBW only for IV dose

7
Q

Vincristine toxicity

A
  • dose limiting NEUROTOXICITY*
8
Q

VinBlastine toxicity

A
  • dose limiting MYELOSUPPRESSION *

B=bone marrow toxicity

9
Q

VinorelBine toxicity

A
  • dose limiting MYELOSUPPRESSION *

B=bone marrow toxicity

10
Q

Paclitaxel

A

Formulated 50/50 alcohol and cremophor EL (hypersensitivity rxn) pre-treat pt.
*CYP2C8 (rare DME) to 6-hydroxypaclitaxel (major, less active metabolite)
Toxicity: *peripheral neuropathy

11
Q

Abraxane

A

Albumin bound paclitaxel: shell forms nano particles better taken up by cancer cells.
*Does NOT cause hypersensitivity rxn)
*DO NOT interchange formulation w/ paclitaxel bc mor drug is delivered to cells w/ Abraxane
Toxicity: peripheral neuropathy

12
Q

Docetaxel

A
  • Formulated w/ polysorbate 80-> hypersensitivity rxn possible pre treat pt.
    CYP3A4 metabolism to hydroxydocetaxel (major metabolite)
    Toxicity: fluid retention, myelosuppression w/neutropenia, and peripheral neuropathy
13
Q

Cabazitaxel

A

*Formulated w/ polysorbate 80-> hypersensitivity rxn, pretreat pt.
lower affinity for P-gp: drug used for docetaxel-resistant metastatic breast cancer
CYP3A4/5 metabolism to several des- and didesmethyl active metabolites
Toxicity: (end metabolite is still active so there are a lot of toxicities) neutropenia (dose limiting), peripheral neuropathy, diarrhea

14
Q

Ixabepilone (an epothilone)

A

lacks P-gp affinity

Toxicity: neutropenia, peripheral neuropathy, hypersensitivity rxn (formulated w/cremophor

15
Q

Mechanism of resistance to mitosis inhibitors

A

Vinca alkaloids: mutant p53 oncogene (cell makes protein products not responsive to vinca alkaloids)
Taxanes: P-gp mediated drug efflux