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Flashcards in Pharm Chemo Drugs Deck (58)
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1

Antimetabolites

Antimetabolites

2

MOA of Antimetabolites

antimetabolites interfere with DNA and RNA formation by substituting for the normal building blocks of RNA and DNA (changing the base then once replication starts it recognizes the change in the base and blocks replication)

3

Antimetabolites are commonly used to treat what?

leukemias, breast CA, ovary, and the intestinal tract,

4

Fluoropyrimidines
-
-
MOA:

5-Fluorouracil
Capecitabine

MOA:inhibits thymidine synthesis (capecitabine is the prodrug of 5-FU)

5

what is the benefit and side effect of Capecitabine

it can be taken orally

Black Box: Monitor INR regularly with patients on oral coumadin derivatives-Increased risk of bleeding/death

6

what are the side effects of the Fluoropyrimidines

neutropenia, thrombocytopenia, and anemia; Hand–foot syndrome and diarrhea when administered as a continuous IV infusion

7

Cytidine Analogs

Cytidine Analogs

8

Cytidine Analogs

Cytarabine
Gemcitabine

9

what is the MOA of Cytidine Analogs

Cytarabine arabinose analog of cytosine
Gemcitabine- Inhibits DNA polymerase

10

what is a side effect of Cytarabine?

Cellebellar syndrome, ataxia, bone suppression with leukoplenia and thrombocytopenia and anemia.

11

Azacytidine and Decitabine
MOA:
Indicated for:
Reduces what?
Toxicity :

MOA: Nucleoside analog
indicated for: Myelogenous leukemia
It reduces the need for transaction and creates hematopoiesis
Toxic: Myelosupression

12

Purine Antimetabolites (Purine Antagonists)

Purine Antimetabolites (Purine Antagonists)

13

Purine Antimetabolites (Purine Antagonists)
-
-
-
-

Mercaptopurine (6-MP)
Thioguanine (6-TG):
Fludarabine
Cladribine and pentostatin

14

Mercaptopurine (6-MP) and Thioguanine (6-TG):
MOA:
Side effects:
Interactions:

rapidly converted to ribonucleotides that inhibit purine biosynthesis

Side effects: Hepatic toxicity

Don't use with allopurinol, Mercaptopurine metabolism is significantly decreased • REDUCE drug dose by approximately 75% when allopurinol is administered & monitor for toxicity

15

Fludarabine:
increases the risk of

infection

16

Cladribine and pentostatin
specific MOA of each

cal- resists deactivation by adenosine deaminase

pen- is a potent inhibitor of adenosine deminase

17

Do not combine pentostatin with what?

Fludarabine- risk of fatal pulmonary toxicity

18

Antifolates
-
-
MOA:
what can this cause?

Methotrexate & Pemetrexed

MOA: inhibits dihydrofolate reductates
this can cause pernicious anemia

side effects: Hepatotoxic and Renal tubularnecorisis

19

Microtubular targeting Drugs
MOA
Side effects
CA used for:
Ex
-
-
-
-

MOA: work on the M phase
Side effects: Periph N damage
Ca: Breast, lung, Myeloma, Lymphoma

Taxanes
Epothilones
Vinva alkaloids
Estramustine

20

Vinca Alkaloids
drugs: (3)
MOA:
from what plant
How is resistance developed?
s/e

Vincriostine, Vinblastine, Vinorelbine

Stop assembly of mircotubules

Natural alkaloids from periwinkle plant
resistance: Resistance develops from P-glycoprotein-decreases drug accumulation and retention in tumor cells
S/E extravasation (tx. Warm packs)-

21

Taxanes
Drugs (2)
MOA
SE:
-
-
Requires premedication with what?

Interactions
-
-

Paclitaxel and Docetaxel

MOA: Promote microtubule assembly and interfere with disassembly

S/E Doc: Water retention, Myelosupresion
Pac: Neurotoxicity and hupersensitivtiy
Pre med: corticosteroids

do not give Paclitaxel with solid tumors with baseline PMN normal or Alt/AST > 1.5 normal

22

Epothilone
Drugs (2)

May work in those resistant to pactilaxel

Epothilone and Ixabepolone

Epothilone

23

Similar to taxanes for Metastatic breast cancer

Premedicate with what?

Ixabepilone

antihistamine (may/may not need corticosteroid)

24

Estramistine

Estramustine Causes separation of microtubule-associated protein from the microtubultes- inhibits assembly

25

➢Topoisomerase inhibitors

➢Topoisomerase inhibitors

26

MOA of Topoisomerase inhibitors
MOA:
I:
II:
Examples

Manipulated (Break) DNA during replication and transcription-
I= onetime
II= two times
Examples: camptothecins, anthacyclines, epipodopyllotoxins

27

camptothecins

Topotecan and Irinotecan
Etoposide and Teniposide

28

Topotecan and Irinotecan
Inhibits:
S/E:
tx of s/e:

Inhibit topoisomerase 1

Higher risk of diarrhea (treat with loperamide)

29

Etoposide and Teniposide
inhibits:
Resistance:
Side effects:

Inhibit topoisomerase 2

Resistance - by increased cells ability to repair type 2 breaks or increased Pgp levels

SE
Severe myelosupression &Bleeding

30

Anthracene Derivatives (Anthracycline)
Drugs (4)
MOA: (2)
Side effects:
-
-
-

-what to use for s/e

Examples: Doxorubicin, Daunorubicin, Idarubicin, Epirubicin

moa: Intercalating topoisomerse inhibitors- insert or stack between base pairs of DNA AND generation of Free radicals- damage all parts of the cell

S/E:
-all Cardiotoxicity –anthracycline
-Doxorubicin= CHF at doses over 400mg/m2
-AML

use to: ➢ Use Dexrazoxane (Totect) immediately- within 6 hours- if dose puts patient at risk of delayed cardiomyopathy and cold pack if extravagation (remove ice pack 15 prior to Totect)