Fitzpatrick - Anti-Neoplastic Drugs, Antimitotic and G/M Phase Drugs Flashcards Preview

Hematology and Oncology > Fitzpatrick - Anti-Neoplastic Drugs, Antimitotic and G/M Phase Drugs > Flashcards

Flashcards in Fitzpatrick - Anti-Neoplastic Drugs, Antimitotic and G/M Phase Drugs Deck (14):
1

MOA of vinca drugs

INHIBIT tubulin ELONGATION/polymerization by binding to Beta tubulin subunits at forming end --> fraying continues to shorten microtubule.
- Rate of depolymerization (fraying) >>>> rate of polymerization (assembly).

2

MOA of taxane drugs

STABILIZE microtubules by binding to Beta-tubulin on forming end. Reach negative/fraying end and inhibit depolymerization by ENHANCING TUBULIN POLYMERIZATION AND (hyper)STABILIZE MICROTUBULES... unabated assembly

3

General classification of vinca alkaloids and taxane drugs.

Cell cycle specific, acting in M phase

4

Adverse effects of vincristine.

neurotoxicity
Vincristine neuropathy >>>> vinblastine neurpathy

5

Why does tx with vinca and taxane drugs often lead to MDR/tx failure?

Due to increased P-glycoprotein expression.
- Nullifies effect of drugs with MOA involving internal sites/processes.

6

Route of vinca and taxane admin.
Location of metabolization.
Route of excretion.

Admin via IV.
Metab in liver.
Excreted in bile and feces.

7

MOA of Topoisomerase inhibitors

Binds to DNA-enzyme complex and creates a "persistently cleavable complex".

8

General classification of Topoisomerase I inhibitors

Cell cycle specific, acting in S phase

9

General classification of Topoisomerase II inhibitors

Cell cycle non-specific

10

Doxorubicin (anthracycline class) MOA and toxicity - end product that damages DNA and related toxicity.

Superoxide and H2O2:
1) Damages tumor DNA
2) Toxicity - dilated cardiomyopathy, HF.

11

Adverse effect of bleomycin.

Skin and lung damage (tissues do not have hydrolase to metabolize bleo).

12

Bleomycin MOA and toxicity - end product that damages DNA and related toxicity.

Bleomycin --> DNA-Bleomycin Fe2+ --> DNA-Bleomycin Fe3+ --> superoxide and hydroxyradicals..
1) damage DNA
2) Lung damage - dyspnea, rales, dry cough, infiltrate --> fibrosis.

13

Unique toxicities:
1) Pitting edema, difficulty breathing = ?drug toxicity
2) Lung fibrosis on CSR or imagnign = ? drug toxicity

1. Doxorubicin
2. Bleomycin

14

Cancer drugs with what MOA are not prone to P-gp MDR? (**i.e. monoclonal antibodies)

Cannot/does not effect drugs with MOA involving exterior cell surface.