Pharm- Antimitotic & G/M Phase Drugs

Question 1

antimitotic drugs

Answer 1

vinca alkaloids: vincristine, vinblastine, vinorelbine

Taxanes: taxol (paclitaxel), taxotere (docetaxel)

Question 2

Vinca alkaloids distinction

Answer 2

inhibit tubulin polymerization -> block assembly of microtubules

Question 3

Taxanes distinction

Answer 3

enhance tubulin polymerization -> stabilize microtubules

Question 4

Vinblastine therapeutic uses

Answer 4

testicular cancer (w/ bleomycin & cisplatin), lymphomas, neuroblastoma

Question 5

Vincristine therapeutic uses

Answer 5

ALL (pediatric), lymphoma, neuroblastoma, Wilm’s tumor, Ewings sarcoma

Question 6

Vinorelbine

Answer 6

Advanced NSCL cancer (alone or with cisplatin)

Question 7

Paclitaxel

Answer 7

advanced breast & ovarian (w/ cisplatin)

Question 8

Docetaxel

Answer 8

Advanced breast, ovarian recurrence (taxanes are effective against solid tumors)

Question 9

Vinblastine dose limiting toxicity

Answer 9

BM suppression; vesicant- blisters

Question 10

Vincrisitine dose limiting toxicity

Answer 10

neurotoxicity; peripheral neuropathy; paralytic ileus; vesicant-blisters
-description of motor neuropathy: ex- drooping eyelids

Question 11

Vinorelbine

Answer 11

BM suppression; vesicant blisters

Question 12

Paclitaxel

Answer 12

neutropenia; thrombocytopenia; peripheral neuropathy; severe hypersensitivity during infusion- requires anti-histamine & corticosteroid pretx

Question 13

Docetaxel

Answer 13

neutropenia; peripheral neuropathy

Question 14

nephrotoxicity from cisplatin

Answer 14

hypokalemia -> damage the tubules and waste calcium -> consequence of calcium wasting

Question 15

topoisomerase inhibitors

Answer 15

cause DNA strand breaks

Question 16

epipodophyllotoxins- TI inhibitors

Answer 16

etoposide, teniposide

Question 17

Camptothecins- TI inhibitors

Answer 17

irinotecan (active metabolite SN38), topotecan

Question 18

epipodophyllotoxins distinctions

Answer 18

topoisomerase II inhibition -> DNA double strand breaks

Question 19

Camptothecins distinctions

Answer 19

Topoisomerase I inhibition -> DNA single strand breaks

Question 20

Etoposide IV, PO therapeutic uses

Answer 20

oat cell carcinoma of lung; testicular cancer (w/ cisplatin & bleomycin)

Question 21

Teniposide IV therapeutic uses

Answer 21

Efficacy vs glioma & neuroblastoma

Question 22

Irinotecan IV therapeutic uses

Answer 22

Metastatic colorectal cancer

Question 23

Topotecan IV therapeutic uses

Answer 23

2nd line various - failed prior 1st line

Question 24

Etoposide (CYP450 liver) dose limiting toxicity

Answer 24

leukopenia; secondary cancer (leukemia)
-regimen for testicular cancer with typically occurs in younger people who will live for longer periods of time so the DNA damage introduced by the etoposide has a longer time to emerge as a secondary neoplasm

Question 25

Teniposide (CYP450 liver) dose limiting toxicity

Answer 25

Leukopenia

Question 26

Irinotecan (Renal clearance) dose limiting toxicity

Answer 26

``` severe diarrhea (may be life threatening & require tx with loperamide); myelosuppression -increases survival 4-5 months ```

Question 27

Topotecan (renal clearance) dose limiting toxicity

Answer 27

neutropenia; mucositis

Question 28

DNA intercalation & oxidative scission drugs

Answer 28

cause DNA strand breaks | -Antibiotics, Anthracyclines

Question 29

Antibiotics

Answer 29

bleomycin, dactinomycin

Question 30

anthracyclines | -flat shape. they start to resemble a base pair and get physically inserted into the DNA

Answer 30

doxorubicin, daunorubicin, epirubicin, idarubicin, mitoxantrone

Question 31

Bleomycin distinctions

Answer 31

Fe2+/3+ mediated free radical generation -> DNA strand breaks -used in the regimen of testicular cancer

Question 32

dactinomycin distinctions

Answer 32

DNA intercalating agents

Question 33

doxorubicin, daunorubicin, epirubicin, idarubicin distinctions

Answer 33

- inhibit topoisomerase II - DNA intercalating agents - Free radical generation -> DNA strand breaks

Question 34

Mitoxantrone distinctions

Answer 34

inhibit topoisomerase II

Question 35

Bleomycin (SQ, IM, IV, Renal clearance) therapeutic uses

Answer 35

testicular cancer (w/ vinblastine, cisplatin or etoposide)

Question 36

Doxorubicin, Epirubicin therapeutic uses

Answer 36

wide spectrum- breast, ovarian, lung, thyroid, lymphoma, sarcoma

Question 37

Daunorubicin therapeutic uses

Answer 37

Leukemia (AML, ALL)

Question 38

Idarubicin (IV-vesicant biliary excretion) therapeutic uses

Answer 38

Leukemia (AML, ALL, CML in blast crisis)

Question 39

Mitoxantrone (IV) therapeutic uses

Answer 39

Breast, prostate, NHL

Question 40

Bleomycin dose limiting toxicity

Answer 40

pulmonary fibrosis- "bleomycin lung" - 5-10% of pts develop lung toxicity. Cumulative dose-related toxicity. Lung fxn improves with recovery, but fibrosis remains. - lung doesnt have metabolic capacity to breakdown the bleomycin -> lung is overexposed

Question 41

doxorubicin, daunorubicin, epirubicin, idarubicin dose limiting toxicity

Answer 41

Cardiotoxicity, dilated cardiomyopathy, CHF occurs over time- cumulative dose-related toxicity; myelosuppression; mucositis