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Flashcards in Chemotherapy drugs Deck (82):
1

Which drugs kill resting and dividing cell (aka cell cycle non-specific)?

1.Cyclophosphamide
2. Chlorambucil
3. Cisplatin
4. Carboplatin
5. Actinomycin D
6. Adriamycin-doxyrubicin
7. L-asparginase

2

Which drug only kills actively diving cells (aka cell cycle specific)?

1. 5-Fluorouacil
2.. Vincristine
3. Vinblastine

3

Which drug kills actively dividing cells in the S phase?

5-Fluorouacil

4

What do vincristine and vinblastine have in common?

They all kill actively dividing cells in the M phase and are antimicrotubule agents.

5

At what level are we able to detect neoplasia in the body?

When there are 10^9 cells

6

What number of cancer cells are incompatible with life?

10^12

7

What is the ratio of cancer cells killed to regrowth when treated with chemotherapy?

2 logs of cell kill/1 log of regrowth

8

What is the equation to calculate BSA?

M2=A x (weight in grams)/10,000

9

What are the anatomical resistance methods cancer cells employ?

1. Tumor hypoxia
- Physical distance from blood vessels
-Imperfection of malignant blood vessels

2. Physiological barriers
-Blood brain barrier, skin and bone marrow
-limited penetration of drug to mass

10

What are the cellular mechanisms of resistance for cancer cells?

1. Alteration of drug targets
-upregulation of target protein
-mutation of target binding site

2. Multi Drug resistance
-Drug efflux pumps (Pgp)
-Drug conjugation with glutatione

3. Enhanced survival
-evade apoptosis
-increase DNA repair

11

Which drugs are alkylating agents?

1. Mechlorethamine
2. Cyclophosphamide
3. Chlorambucil
4. Melphalan
5. Lomustine (CCNU)
6. Streptozocin
7. Dacarbazine

12

Which drugs are nitrogen mustards?

1. Mechlorethamine
2. Melphalan
3. Cyclophosphamide
4. Chlorambucil

13

Which drugs are nitrosoureas?

1. Lomustine (CCNU)
2. Streptozocin

14

Which drugs are traizenes?

Dacarbazine

15

How do alkylating agents kill neoplastic cells?

Alkyl group binds to nucleophilic sites on DNA and RNA where adducts (bifunctional or monofunctional) generate interstrand or intrastrand and cross-links resulting in misreading of codons and single-strand breakage of DNA/RNA.

16

What is the CHOP protocol?

Treatment for lymphoma:
Week1: vincristin
Week2:cyclophosphamide
Week3: vincristin
Week4: adryamicin
Week5: no treatment

Do this 4 times with prednisone for the 1st month.

17

What is metronomic therapy?

The use of a very low dosing of cyclophosphamide or Toceranib for prolonged periods mostly to inhibit angiogenesis in solid tumors.

18

T/F: Alkylating agents have drug cross resistance.

False: there is no drug cross resistance which means you can use multiple drugs from this class and they will each be effective even if there is resistance to one.

19

Which drugs are used to treat lymphoma rescue?

1. Dacarbazine (more common)
2. L-asparginase
3. Lomustine
4. Mechlorethamine
5. Doxorubicin

20

How is mechlorethamine given and what are its major disadvantages?

It is given IV, it is a strong vesicant , and it is mutagenic and carcinogenic to bone marrow stem cells.

21

What alkylating agent is used to treat multiple myeloma?

Melphalan, in combo with

22

Which drugs involve passive diffusion into neoplastic cells?

1. Chlorambucil
2. Lomustine ( highly lipophilic)
3. Actinomycin D
4. Vincristine and Vinblastine

23

Which drugs do not require activation?

1. Mechlorethamine
2. Melphalan
3. Streptozotocin
4. Carboplatin
5. Cisplatin

24

Which drugs fall under the tyrosine kinase inhibitor class?

1. Imatinib
2. Toceranib
3. Masitinib

25

What do carboplatin and cisplatin have in common?

Commonality:
They are both platinum agents and covalently bind to DNA interstrands (90%) and intrastrands (10%) twisting the DNA around. Both used to treat osteosarcomas. .

26

What is the drug of choice for osteosarcomas?

Carboplatin

27

Which drugs should you never give to cats? Why?

1. Cisplatin: Nephrotoxicity
2. 5-fluorouracil: CNS toxicity
3. Rabacfosadine: only labeled for canines

28

What is the drug of choice for histiocytic sarcoma?

Lomustine

29

Which drug treats insulinomas?

Streptozotocin

30

What are the disadvantages of using cyclophosphamide?

It can cause neutropenia and thrombocytopenia as, well as hemorrhagic cystitis.

31

Which drugs require activation via either hepatic metabolism or the P450 pathway?

1. Cyclophosphamide (P450)
2. Chlorambucil (liver)
3. Lomustine (liver)
4. Dacarbazine (liver)

32

Which class of chemo drugs are not affected by PgP?
(multi-drug resistance/efflux pumps)?

All alkylating agents

33

Which drugs can cross the blood brain barrier?

1. Dacarbazine
2. Lomustine
3. Cytosine arabinoside

34

How are tyrosine kinase inhibitors administered?

PO

35

Which drug is used to treat chronic lymphocytic leukemia (CLL) and low-grade GI Lymphoma in cats?

Chlorambucil

36

Which drug is the least toxic of all the alkylating agents?

Chlorambucil

37

Which drugs are vesicants?

1. Mechlorethamine
2. Melphalan
3. Doxorubicin
4. Vincristine
5. Actinomycine D

38

Which drug is used as a last resort for lymphoma?

Actinomycin D

39

what is the NADIR for lomustine?

Dogs: 3 weeks
Cats: 6 weeks

40

Which drugs are considered anti-metabolites?

1. Cytosine arabinoside
2. 5-Fluorouracil
3. Gemcitabine

41

Which drug is used to treat pancreatic cancer and carcinomas, and if given in a longer infusion, will increase cellular uptake and half-life?

Gemcitabine

42

Which drugs can cause myelosuppression?

1. Cytosine arabinoside
2. 5-Fluorouracil
3. Masitinib
4. Melphalan
5. Mitoxantrone
6. Actinomycin D

43

Which drugs can cause neutropenia and thrombocytopenia?

1. Cyclophosphamide
2. Dacarbazine

44

Which drugs can cause hypersensitivity reactions?

1. Doxorubicin
2. L-asparginase

45

What drug can reverse Doxorubicin? How? What is the dose?

Dexrazoxane: acting as a intracellular iron chelator: 10x the dose of doxorubicin in the opposite leg.

46

Which drugs can cause GI toxicity?

1. Mechlroethamine
2. Dacarbazine
3. Doxorubicin
4. Mitoxantrone
5. actinomycin D
6. Cytosine arabinoside
7. 5-fluorouracil
8. Vincristine
9. Toceranib
10. Masitinib

47

Which drugs can cause nephrotoxicity?

1. Streptozotocin
2. Cisplatin
3. Doxorubicin (cats)
4. 5-Fluorouracil (dogs)
5. Vincristine

48

Which drugs can cause bone marrow suppression?

1. Mechlroethamine
2. Chlorambucil (mild)
3. Decarbazine
4. Carboplatin
5. Doxorubicin
6. Gemcitabine
7. Toceranib

49

Which drug can cause hepatoxicity and what is given in conjunction to prevent this?

Lomustine; Prophylactic liver protectant like SAM-e, milk thistle, and denamarin.

50

How do you prevent hypersensitive reactions when administering L-asparginase? What about Doxorubicin?

Use an antihistamine and dexamethasone with L-Asparginase.
Use Diphenhydramine with doxorubicin.

51

Which drugs can cause proteinuria?

1. Toceranib
2. Masitinib

52

Which drug can cause cardiotoxicity?

Doxorubicin

53

Which drugs are considered Antimicrotubule agents?

1. Vincristine
2. Vinblastine

54

Which drugs are considered anti-metabolites?

1. Cytosine arabinoside
2. 5-Fluorouracil
3. Gemcitabine

55

Which drugs are anti-tumor antibiotics?

1. Doxorubicin
2. Dexrazoxane
3. Mitoxantrone
4. Actinomycin D

56

Which drug can be used for almost any type of cancer?

Doxorubicin aka Adriamycin

57

Which drug does not induce oxygen reactive species? Which drug does?

Mitoxantrone does not induce oxygen reactive species.
Doxorubicin does induce oxygen reactive species.

58

What is the mechanism of action of anti-tumor antibiotics?

1. DNA intercalation
2. Inhibition of DNA/RNA polymerase
3. Inhibition of topoisomerase II
4. DNA alkylation
5. Inhibition of thioredoxin reductase
( Adriamycin-Doxorubicin)

59

What is mitoxantrone used for?

1. Transitional cell carcinoma
2. Lymphoma rescue
3. Carcinomas

60

How would you treat multiple myeloma?

Treat with the alkylating agent melphalan and prednisone

61

What are the uses for Lomustine?

1. Histiocytic sarcoma (DOC)
2. Lymphoma rescue
3. Epitheliotropic lymphoma
4. Malignancies of the brain
5. Mast cell tumors

62

Which drug can induce diabetes and involves cellular uptake to B cells in the pancreas by GLUT 2 ?

Streptozotocin

63

T/F: Dacarbazine is a pro-drug and an alkylizing agent.

True

64

What does methylation do?

It silences genes

65

Which drug is used to treat melanoma, brain malignancies and used in lymphoma rescue?

Dacarbazine

66

What do you need to keep in mind when you treat an animal that has transitional cell carcinoma with carboplatin?

It can cause incontinence and the urine will be toxic (filled with carboplatin) as it is excreted in the urine 70% unchanged.

67

When administering _______ to treat osteosarcomas in dogs, we never want to give loop diuretics.

Cisplatin

68

How do antimetabolites enter the cancer cells?

Active transport

69

What drug is used to treat lymphoma , leukemia and meningoencephalitis?

Cytosine Arabinoside

70

Why do we never give 5-fluorouracil to cats?

It can cause fatal CNS toxicity

71

What is 5-fluorouracil used to treat?

Mammary tumors in dogs
Transitional cell carcinomas

72

What is Rabacfosadine?

It is an antimetabolite with the name of Tanovea. Only used in dogs and to treat refractory B cell lymphoma. It is give IV once every 3 weeks for 5 times. The side effects are GI toxicity, neutropenia and pulmonary fibrosis.

73

When would we not want to use Rabacfosadine?

If a dog has pulmonary fibrosis or history of chronic pulmonary disease, and in west highland white terriers.

74

How do antimicrotubule agents work and what are they?

They are alkaloids that interfere with polymerization or depolymerization of microtubules in the M phase of cell development.

75

How would we administer Vincristine or Vinblastine and why should we take extra caution?

IV and it is an irritant and extravasation can cause serious tissue damage.

76

What do we use vincristine for?

In the CHOP protocol for lymphoma and to treat immune mediated thrombocytopenia,

77

What drug resistance can vincristine and vinblastine face from neoplastic cells?

1. PgP up regulation
2. Mutation on the microtubule target

78

How does L-asparagine work?

It is used in lymphoma rescue because when it is hydrolized to L aspartic acid, the amount of L-asparagine is reduce in circulation. Malignant lymphoblasts can't produce their own and they need it to produce proteins in order to proliferate.

79

What drugs can you use to treat mast cell tumors?

1. Toceranib
2. Masitinib
3. Lomustine (CCNU)
4. Vinblastine

80

What drug do we use to treat refractory B cell lymphoma?

Rebacfosadine aka Tanovea

81

Which drugs are used to treat conditions that are not neoplastic and what conditions are they?

1. Vincristine: Immune mediated thrombocytopenia
2. Cytosine Arabinoside: Meningoencephalitis

82

Which drugs have long NADIRs? `

1. Carboplatine (7 and 21 days)
2. Lomustine