Antineoplastic Drugs Flashcards Preview

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Flashcards in Antineoplastic Drugs Deck (44):
1

Ifosfamide

cross links DNA and prevents synthesis.
Cell cycle nonspecific
Toxicity when it enters the cell cycle.
Oral and IV
Cyclophosphamide analog. Is an alkylating agent.

2

Cyclophosphamide

Cell cycle nonspecific. Cross links DNA and prevents synthesis. Alkylating agent. Oral, liver activation. Hemorrhagic cystitis from acroline metabolite, treat with Mesna.

3

Mesna

Is coadministered with cyclophosphamide to bind acroline to prevent hemorrhagic cystitis.

4

Busulfan

Alkylating agent. Moa cross links DNA and prevents synthesis
-needs excess hydration to counteract kidney hydration
-exit via renal excretion so monitor that they are being cleared IV treatment
Activated in Liver.

5

Cisplatin

IV Moa cross links DNA and prevents synthesis. Platinum containing compound, does not alkylate
-needs excess hydration to counteract kidney hydration
-exit via renal excretion so monitor that they are being cleared
Alkylating agent

6

Etoposide

Topoisomerase II inhibitor Cell cycle specific for S-phase and G2. Causes strand breaks in DNA IV and oral.

7

Doxyrubicin

Intercolating (between DNA like ethidium bromide stopping DNA and RNA synthesis) and Topo II inhibitor IV. Cell cycle nonspecific. Vesicant. Radiation recall. BMS. Urine Red. Antibiotic

8

Methotrexate

Analog of tetrahydrofolate inhibits DHFR. IV and oral
Alkylation of the urine makes the methotrexate excretion in the urine less toxic
Cotreat with Leucovorin and Glucarpidase

9

Leucovorin

Reduced form of folate bypasses DHFR and supplies 1C pool to help good cells with methotrexate treatment

10

Glucarpidase

enzyme used to lower methotrexate into inactive DAMPA for alternative route of elimination than kidney. IV

11

5-Fluorouracil

inhibits thyamine Synthase Cell cycle specific antimetabolite. Affects pyrimadine synthesis AE: Acute Cerebellar syndrome, lowest theraputic index. Liver elimination

12

Fludarabine

Analog of purines. IV Blocks DNA polymerase Cell cycle specific to S-Phase

13

Paclitaxiel

Antimitotic: Prevents Depolymerization of microtubules preventing Metaphase->anaphase transition. IV treatment

14

Carmustine

Antineoplastic Is an alkylating agent causes cross links in DNA and RNA leading to cell death. Crosses the BBB easily, cell cycle specific. Wafers inserted into the brain and IV. Lipophillic. Nitrosoureas

15

Temozolomide

Alkylating agent, methylation of RNA and DNA. Crosses BBB easily; lipophillic.

16

Vincristine

Depolymerization of microtubules preventing Metaphase->anaphase transition. IV treatment. Is small so crosses the BBB very well, but is effluxed out of the brain so is not as good as temozolomide and carmustine in treating brain tumors.

17

Pemetrexed

Analog of tetrahydrofolate inhibits DHFR. IV and oral
Alkylation of the urine makes the methotrexate excretion in the urine less toxic
Cotreat with Leucovorin and Glucarpidase

18

Pralatrexate

Analog of tetrahydrofolate inhibits DHFR. IV and oral
Alkylation of the urine makes the methotrexate excretion in the urine less toxic
Cotreat with Leucovorin and Glucarpidase

19

6-Mercaptopurine

S-phase specific, Inhibits purine synthesis by blocking guanylyl Kinase, resulting in pseudofeedback inhibition leading to buildup of AMP, GTP which must be made through salvage pathway. Useful for leukemia
AE: bone marrow suppression, Tumor lysis syndrome, increased uric acid

20

Capecitabine

inhibits thyamine Synthase Cell cycle specific antimetabolite. Affects pyrimadine synthesis AE: Acute Cerebellar syndrome, lowest theraputic index. Liver elimination same as 5FU

21

Azithroprine

S-phase specific, Inhibits purine synthesis by blocking guanylyl Kinase, resulting in pseudofeedback inhibition leading to buildup of AMP, GTP which must be made through salvage pathway. Useful for leukemia
AE: bone marrow suppression, Tumor lysis syndrome
Not anticancer

22

6-Thioguanine

Inhibits Guanylyl kinase
S-phase specific, Inhibits purine synthesis by blocking guanylyl Kinase, resulting in pseudofeedback inhibition Useful for leukemia
AE: bone marrow suppression, Tumor lysis syndrome increased uric acid

23

Allopurinol

Inhibits xanthine oxidase, preventing uric acid buildup and gout associated with 6 mercaptopurine due to tumor cell lysis. Use with 6- mercaptopurine results in excessive toxicity, reduce 6mcp dose

24

Cladrabine

Inhibits DNA polymerase, blocks DNA elongation, can cause repititons, mutagenic. Forces differentiation Pyrimadine.

25

Cytarabine (ARA-C)

Inhibits DNA polymerase, blocks DNA elongation, can cause repititons, mutagenic. Forces differentiation Pyrimadine. Cytodine analog. S-phase

26

Gemcitabine

Inhibits DNA polymerase, and ribonucleotide reductase leading to strand termination and Apoptosis

27

Hydroxyurea

Inhibitor of ribonucleotide reductase, preventing deoxynucleotide syntheisis from ribonucleotides. Syncronizes cells into G1, more sensitive to radiation.

28

Chlorambucil

Alkylating agent. Moa cross links DNA and prevents synthesis Nitrogen mustard. Oral, broad spectrum, lung toxicity. CCNS

29

Lomustine

Is an alkylating agent causes cross links in DNA and RNA leading to cell death. Crosses the BBB easily, cell cycle specific. Wafers inserted into the brain and IV. Lipophillic. Nitrosourea

30

Decarbazine

Alkylating agent Moa cross links DNA and prevents synthesis. CCNS. Treats hodgkins disease.

31

Mechlorethamine

Alkylating agent, cross links DNA. IV. mustard gas. Vesicant agent, rapid activation. Bone marrow suppression.

32

Melphan

Alkylating agent, cross links DNA. Given orally. Tx. multiple myeloma.

33

Procarbazine

Alkylating agent, cross links DNA. Given orally., activated by CYP450. Tx. lymphomas.
Carcinogenic-> leukemias

34

Mitomycin

Antibiotic. Cross links DNA.
Selective toxicity
Lung toxicity in 10% of pts. 50% fatal.
Kidney damage

35

Carboplatin

IV Moa cross links DNA and prevents synthesis. Platinum containing compound, does not alkylate
-needs excess hydration to counteract kidney hydration
-exit via renal excretion so monitor that they are being cleared
Alkylating agent

36

Oxaloplatin

IV Moa cross links DNA and prevents synthesis. Platinum containing compound, does not alkylate
-needs excess hydration to counteract kidney hydration
-exit via renal excretion so monitor that they are being cleared
Alkylating agent

37

Danorubicin

Intercolating (between DNA like ethidium bromide stopping DNA and RNA synthesis) and Topo II inhibitor IV. Cell cycle nonspecific. Vesicant. Radiation recall. BMS. Urine Red. Antibiotic

38

Idarubicin

Intercolating (between DNA like ethidium bromide stopping DNA and RNA synthesis) and Topo II inhibitor IV. Cell cycle nonspecific. Vesicant. Radiation recall. BMS. Urine Red. Antibiotic

39

Epirubicin

Intercolating (between DNA like ethidium bromide stopping DNA and RNA synthesis) and Topo II inhibitor IV. Cell cycle nonspecific. Vesicant. Radiation recall. BMS. Urine Red. Antibiotic

40

Mitoxatone

Intercolating (between DNA like ethidium bromide stopping DNA and RNA synthesis) and Topo II inhibitor IV. Cell cycle nonspecific. Vesicant. Radiation recall. BMS. Urine Blue. Antibiotic

41

Bleomycin

Antibiotic. Activated by hydrolase(not in lungs or skin). Topo II inhibitor-> strand breaks/ fragmentation. Lack of bone marrow suppression.
AE:hypersensitivity, GI, pulmonary fibrosis. Skin and lung damage.

42

Irinotecan

Plant alkylaloid, Top I inhibitor, DNA strand breaks. Kidney elim. Metastatic Colon cancer.
Myelosuppression, diarrhea acute-> atropine, chronic.
Severe-> dehydration

43

Topotecan

Plant alkylaloid, Top I inhibitor, DNA strand breaks. Kidney elim. Metastatic Colon cancer.
Myelosuppression, diarrhea acute-> atropine, chronic.
Severe-> dehydration

44

Trimethoprim + sulfamethoxazole

folic acid inhibitor, and blocker of dihydropteroate synthetase. They act synergistically blocking the folate pathway in bacteria