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Pharmacology > Chemotherapy drugs > Flashcards

Chemotherapy drugs Flashcards

1
Q

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

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

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

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

Which drug kills actively dividing cells in the S phase?

A

5-Fluorouacil

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4
Q

What do vincristine and vinblastine have in common?

A

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

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5
Q

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

A

When there are 10^9 cells

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6
Q

What number of cancer cells are incompatible with life?

A

10^12

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7
Q

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

A

2 logs of cell kill/1 log of regrowth

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8
Q

What is the equation to calculate BSA?

A

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

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9
Q

What are the anatomical resistance methods cancer cells employ?

A
  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
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10
Q

What are the cellular mechanisms of resistance for cancer cells?

A
  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
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11
Q

Which drugs are alkylating agents?

A
  1. Mechlorethamine
  2. Cyclophosphamide
  3. Chlorambucil
  4. Melphalan
  5. Lomustine (CCNU)
  6. Streptozocin
  7. Dacarbazine
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12
Q

Which drugs are nitrogen mustards?

A
  1. Mechlorethamine
  2. Melphalan
  3. Cyclophosphamide
  4. Chlorambucil
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13
Q

Which drugs are nitrosoureas?

A
  1. Lomustine (CCNU)

2. Streptozocin

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14
Q

Which drugs are traizenes?

A

Dacarbazine

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15
Q

How do alkylating agents kill neoplastic cells?

A

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.

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16
Q

What is the CHOP protocol?

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

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

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17
Q

What is metronomic therapy?

A

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

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18
Q

T/F: Alkylating agents have drug cross resistance.

A

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.

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19
Q

Which drugs are used to treat lymphoma rescue?

A
  1. Dacarbazine (more common)
  2. L-asparginase
  3. Lomustine
  4. Mechlorethamine
  5. Doxorubicin
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20
Q

How is mechlorethamine given and what are its major disadvantages?

A

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

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21
Q

What alkylating agent is used to treat multiple myeloma?

A

Melphalan, in combo with

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22
Q

Which drugs involve passive diffusion into neoplastic cells?

A
  1. Chlorambucil
  2. Lomustine ( highly lipophilic)
  3. Actinomycin D
  4. Vincristine and Vinblastine
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23
Q

Which drugs do not require activation?

A
  1. Mechlorethamine
  2. Melphalan
  3. Streptozotocin
  4. Carboplatin
  5. Cisplatin
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24
Q

Which drugs fall under the tyrosine kinase inhibitor class?

A
  1. Imatinib
  2. Toceranib
  3. Masitinib
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25
Q

What do carboplatin and cisplatin have in common?

A

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. .

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26
Q

What is the drug of choice for osteosarcomas?

A

Carboplatin

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27
Q

Which drugs should you never give to cats? Why?

A
  1. Cisplatin: Nephrotoxicity
  2. 5-fluorouracil: CNS toxicity
  3. Rabacfosadine: only labeled for canines
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28
Q

What is the drug of choice for histiocytic sarcoma?

A

Lomustine

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29
Q

Which drug treats insulinomas?

A

Streptozotocin

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30
Q

What are the disadvantages of using cyclophosphamide?

A

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

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31
Q

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

A
  1. Cyclophosphamide (P450)
  2. Chlorambucil (liver)
  3. Lomustine (liver)
  4. Dacarbazine (liver)
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32
Q 
Which class of chemo drugs are not affected by PgP?
(multi-drug resistance/efflux pumps)?
A

All alkylating agents

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33
Q

Which drugs can cross the blood brain barrier?

A
  1. Dacarbazine
  2. Lomustine
  3. Cytosine arabinoside
34
Q

How are tyrosine kinase inhibitors administered?

A

PO

35
Q

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

A

Chlorambucil

36
Q

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

A

Chlorambucil

37
Q

Which drugs are vesicants?

A
  1. Mechlorethamine
  2. Melphalan
  3. Doxorubicin
  4. Vincristine
  5. Actinomycine D
38
Q

Which drug is used as a last resort for lymphoma?

A

Actinomycin D

39
Q

what is the NADIR for lomustine?

A

Dogs: 3 weeks
Cats: 6 weeks

40
Q

Which drugs are considered anti-metabolites?

A
  1. Cytosine arabinoside
  2. 5-Fluorouracil
  3. Gemcitabine
41
Q

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

A

Gemcitabine

42
Q

Which drugs can cause myelosuppression?

A
  1. Cytosine arabinoside
  2. 5-Fluorouracil
  3. Masitinib
  4. Melphalan
  5. Mitoxantrone
  6. Actinomycin D
43
Q

Which drugs can cause neutropenia and thrombocytopenia?

A
  1. Cyclophosphamide

2. Dacarbazine

44
Q

Which drugs can cause hypersensitivity reactions?

A
  1. Doxorubicin

2. L-asparginase

45
Q

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

A

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

46
Q

Which drugs can cause GI toxicity?

A
  1. Mechlroethamine
  2. Dacarbazine
  3. Doxorubicin
  4. Mitoxantrone
  5. actinomycin D
  6. Cytosine arabinoside
  7. 5-fluorouracil
  8. Vincristine
  9. Toceranib
  10. Masitinib
47
Q

Which drugs can cause nephrotoxicity?

A
  1. Streptozotocin
  2. Cisplatin
  3. Doxorubicin (cats)
  4. 5-Fluorouracil (dogs)
  5. Vincristine
48
Q

Which drugs can cause bone marrow suppression?

A
  1. Mechlroethamine
  2. Chlorambucil (mild)
  3. Decarbazine
  4. Carboplatin
  5. Doxorubicin
  6. Gemcitabine
  7. Toceranib
49
Q

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

A

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

50
Q

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

A

Use an antihistamine and dexamethasone with L-Asparginase.

Use Diphenhydramine with doxorubicin.

51
Q

Which drugs can cause proteinuria?

A
  1. Toceranib

2. Masitinib

52
Q

Which drug can cause cardiotoxicity?

A

Doxorubicin

53
Q

Which drugs are considered Antimicrotubule agents?

A
  1. Vincristine

2. Vinblastine

54
Q

Which drugs are considered anti-metabolites?

A
  1. Cytosine arabinoside
  2. 5-Fluorouracil
  3. Gemcitabine
55
Q

Which drugs are anti-tumor antibiotics?

A
  1. Doxorubicin
  2. Dexrazoxane
  3. Mitoxantrone
  4. Actinomycin D
56
Q

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

A

Doxorubicin aka Adriamycin

57
Q

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

A

Mitoxantrone does not induce oxygen reactive species.

Doxorubicin does induce oxygen reactive species.

58
Q

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

A
  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
Q

What is mitoxantrone used for?

A
  1. Transitional cell carcinoma
  2. Lymphoma rescue
  3. Carcinomas
60
Q

How would you treat multiple myeloma?

A

Treat with the alkylating agent melphalan and prednisone

61
Q

What are the uses for Lomustine?

A
  1. Histiocytic sarcoma (DOC)
  2. Lymphoma rescue
  3. Epitheliotropic lymphoma
  4. Malignancies of the brain
  5. Mast cell tumors
62
Q

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

A

Streptozotocin

63
Q

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

A

True

64
Q

What does methylation do?

A

It silences genes

65
Q

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

A

Dacarbazine

66
Q

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

A

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

67
Q

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

A

Cisplatin

68
Q

How do antimetabolites enter the cancer cells?

A

Active transport

69
Q

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

A

Cytosine Arabinoside

70
Q

Why do we never give 5-fluorouracil to cats?

A

It can cause fatal CNS toxicity

71
Q

What is 5-fluorouracil used to treat?

A

Mammary tumors in dogs

Transitional cell carcinomas

72
Q

What is Rabacfosadine?

A

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
Q

When would we not want to use Rabacfosadine?

A

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

74
Q

How do antimicrotubule agents work and what are they?

A

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

75
Q

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

A

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

76
Q

What do we use vincristine for?

A

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

77
Q

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

A
  1. PgP up regulation

2. Mutation on the microtubule target

78
Q

How does L-asparagine work?

A

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
Q

What drugs can you use to treat mast cell tumors?

A
  1. Toceranib
  2. Masitinib
  3. Lomustine (CCNU)
  4. Vinblastine
80
Q

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

A

Rebacfosadine aka Tanovea

81
Q

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

A
  1. Vincristine: Immune mediated thrombocytopenia

2. Cytosine Arabinoside: Meningoencephalitis

82
Q

Which drugs have long NADIRs? `

A
  1. Carboplatine (7 and 21 days)

2. Lomustine

Pharmacology (11 decks)

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