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FPP MSS > Anti-Neoplasm Drugs > Flashcards

Anti-Neoplasm Drugs Flashcards

1
Q

Name three alkylating agents used to treat cancer.

A

Mechlorethamine, Cyclophosphamide, Carmustine

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2
Q

What is Mechlorethamine?

A

A cell-cycle nonspecific bifunctional alkylating agent that produces DNA cross-links and is so highly reactive that it disappears from blood in seconds to minutes.

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3
Q

What cancer does Mechlorethamine treat?

A

It is used in combo therapy for Hodgkin’s and non-Hodgkin’s lymphoma.

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4
Q

What are side effects of alkylating agents?

A

Hematopoiesis suppression, GI effects and alopecia (hair loss); they affect rapidly dividing tissues the most

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5
Q

What is Cyclophosphamide?

A

An alkylating agent that is a pro-drug activated by liver cytochrome P450s to Phosphoramide mustard and Acrolein. The Phosphoramide mustard is the alkylating agent and the Acrolein causes bladder toxicity (sterile hemorrhagic cystitis)

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6
Q

How is the sterile hemorrhagic cystitis/bladder toxicity caused by Acrolein prevented?

A

It can be partially prevented with Mesna.

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7
Q

What cancers does Cyclophosphamide treat?

A

It has broad spectrum of activity and can treat a wide variety of cancers.

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8
Q

What is Carmustine?

A

An alkylating agent that crosses the blood brain barrier very well.

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9
Q

What does Carmustine treat?

A

Brain tumors, multiple myeloma and melanoma (It crosses BBB very well).

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10
Q

Name 5 Antimetabolite drugs.

A

Mercaptopurine Thioguanine, Methotrexate, Cytarabine, Hydroxyurea, Fluorouracil

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11
Q

What are common properties of Antimetabolites?

A

They are structural analogs of compounds required for intermediary metabolism and have the greatest effectiveness in tumors where cell proliferation is rapid. They are S-phase specific.

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12
Q

What is the mechanism of Methotrexate (MTX)?

A

It is an Antimetabolite. It binds to dihydrofolate reductase and prevents formation of tetrahydrofolate. (Which is necessary for synthesis of purines and pyrimidines).

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13
Q

What is Leucovorin?

A

Folinic acid; It can be given following high doses of methotrexate to rescue the normal cells which have an increased ability to bring in Leucovorin relative to tumor cells

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14
Q

What are the side effects of Methotrexate?

A

Intestinal epithelium damage, Bone marrow suppression, Renal tubular necrosis, and it displaces other drugs from serum albumin

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15
Q

What is Methotrexate indicated for?

A

Acute Lymphocytic Leukemia

Choriocarcinoma (#1)

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16
Q

What is the mechanism of Fluorouracil (5-FU)?

A

It is a pyrimidine analog that is activated to FUTP in cells, which inhibits RNA synthesis and to FdUMP, which interferes with thymidylate synthase and ultimately DNA synthesis.

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17
Q

What are the indications for Fluorouracil (5-FU)?

A

Broad spectrum of use; stomach, COLON, pancreas, ovary, head and neck, BREAST, bladder and basal cell carcinoma

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18
Q

What are the side effects of Fluorouracil?

A

Nausea
Anorexia
Diarrhea
Myelosuppression

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19
Q

What is the mechanism of Cytarabine (Ara-C)?

A

It is a pyrimidine analog that competes for phosphorylation of cytidine. It competes for incorporation into DNA and causes chain termination.

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20
Q

What are the side effects of Cytarabine?

A

Myelosuppression (dose-limiting)

Neurotoxicity

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21
Q

What are the indications for Cytarabine?

A

Acute leukemia like Acute Myelocytic Leukemia

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22
Q

What is the mechanism of Mercaptopurine?

A

Purine analog that is converted to ribonucleotide that inhibits RNA and DNA synthesis

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23
Q

What are the side effects of Mercaptopurine?

A

Bone marrow depression
N/V
Anorexia
Jaundice

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24
Q

What are the uses of Mercaptopurine?

A

Acute leukemias

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25
Q

How do nonfunctional copies of TPMT affect Mercaptopurine toxicity?

A

TPMT converts 6-MP into inactive 6-methyl-MP and if a patient does not have functional TPMT they cannot tolerate Mercaptopurine because of BM toxicity.

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26
Q

What is the mechanism of hydroxyurea?

A

It inhibits ribonucleotide reductase which blocks the conversion of ribonucleotides to dNTPs and thereby prevents DNA synthesis. It arrests cells at the G1S interface.

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27
Q

What are the uses of Hydroxyurea?

A

It is useful in conjunction with radiation and is used for Granulocytic Leukemia.

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28
Q

What are the side effects of Hydroxyurea?

A

Hematopoietic depression

GI disturbances

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29
Q

What are Vinca alkaloids and what is their mechanism?

A

Vincristine and Vinblastine are Natural Products that bind to tubulin and inhibit proper formation of microtubules and mitotic spindle.

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30
Q

What are the uses of Vincristine?

A

Acute Lymphocytic Leukemia
Lymphomas
Wilm’s tumor
Neuroblastoma

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31
Q

What are the side effects of Vincristine?

A

Less BM toxicity than Vinblastine
Alopecia
Neuromuscular abnormalities like peripheral neuropathy

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32
Q

What are the uses of Vinblastine?

A

Lymphomas

Breast cancer

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33
Q

What are the side effects of Vinblastine?

A 
Strongly myelosuppressive (dose-limiting)
Epithelial ulcerations`
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34
Q

What is an example of a Taxane and what is their mechanism of action?

A

Paclitaxel; enhances assembly and stability of microtubules by binding to Beta subunit of tubulin (different binding site than vinca alkaloids), it blocks late in G2 phase

35
Q

What are the uses of Paclitaxel?

A

Refractory ovarian cancer, breast cancer (It can interfere with DNA repair, intensifying the effects of DNA damage by cisplatin or cyclophosphamide)

36
Q

What are the side effects of Paclitaxel?

A

Dose-limiting leukopenia
Peripheral Neuropathy
Myalgia/arthralgia

37
Q

What is the mechanism of Doxorubicin?

A

It is a cycle-specific phase non-specific anti tumor antibiotic.

1) Intercalates in DNA, distorting DNA helix
2) Causes lipid peroxidation and free radical generation
3) Binds to DNA + topoisomerase II (prevents resealing)

38
Q

What are the uses for Doxorubicin?

A

Wide spectrum of activity - most widely prescribed agent of this class (One of the few with anti-angiogenic properties)

Lymphomas
Breast
Ovary
Small cell lung

39
Q

What are the side effects of Doxorubicin?

A

Cardiomyopathy (dose related, role of ROS)
Bone marrow depression
Alopecia
GI problems

40
Q

What is the mechanism of Bleomycin?

A

It is a mixture of iron-containing glycopeptides that bind to DNA and cause oxidative-like damage to DNA which leads to DNA strand breaks. (Iron is critical to mechanism) Phase specific for G2

41
Q

What are the uses of Bleomycin?

A

Germ cell tumors of testes and ovaries
Head and Neck
Lung
Lymphomas

42
Q

What are the side effects of Bleomycin?

A

Minimal myelosuppression
Pulmonary toxicity (pneumonitis, fibrosis, dose related, cumulative, potentially fatal)
Skin vesiculation, hyperpigmentation

(Lung and skin have lowest levels of bleomycin hydrolase which inactivates bleomycin)

43
Q

What is the mechanism of Etoposide (VP16)?

A

Irreversibly stabilizes DNA-topoisomerase II complex which results in dsDNA breaks that cannot be repaired. Blocks in late G2 phase.

44
Q

What are the uses of Etoposide (VP16)?

A

Lymphoma
Acute Leukemia
Small cell lung
Testis

45
Q

What are the side effects of Etoposide?

A

Leukopenia (dose limiting)
N/V
Diarrhea
Alopecia

46
Q

What is the mechanism of Filagrastim (G-CSF)?

A

It is a granulocyte colony stimulating factor that promotes progenitors of neutrophils and expands the absolute population of neutrophils providing quicker recovery from bone marrow suppression. (The goal is to limit chemotherapy-induced neutropenia)

47
Q

What are the side effects of Filgrastim?

A

Bone pain

48
Q

What is the mechanism of Trastuzumab?

A

It is a monoclonal antibody that binds to the HER2 neu receptor to block proliferation of cells.

49
Q

What are the uses of Trastuzumab?

A

Breast cancers that over express HER2 (Tend to be less responsive to anti-estrogen strategies and to many drugs except for anthracyclines (doxorubicin) and paclitaxel)

50
Q

What are the side effects of Trastuzumab?

A

Cardiomyopathy (often reversible)
Hypersensitivity (anaphylaxis)
Infusion reactions (fever, chills)

51
Q

What is the mechanism of Cisplatin?

A

It is a platinum coordination complex and when it is hydrolyzed it yields activated species which cause DNA cross links. Cycle-specific phase-nonspecific.

52
Q

What are the uses for Cisplatin?

A

Wide anti tumor spectrum
Testicular cancer
Ovarian cancer
Head, neck, bladder, small cell lung, colon, esophagus

53
Q

What are the side effects of Cisplatin?

A 
Nephrotoxicity
Ototoxicity
Peripheral neuropathy
Electrolyte disturbances
N/V (100%)
Myelosuppression
54
Q

What is the mechanism of Procarbazine?

A

Activated in vivo by liver to a methylating agent which causes chromosomal damage (Atypical alkylating agent, no cross-resistance with other alkylating agents)

55
Q

What are the uses for Procarbazine?

A

Hodgkin’s lymphoma

56
Q

What are the side effects of Procarbazine?

A

Myelosuppression

N/V

57
Q

When are hormones and hormone antagonists useful for cancer therapy?

A

Useful against tumors that are steroid hormone dependent (33% of breast cancers respond to hormonal therapy and 66% of breast cancers with good estrogen receptor content respond to hormonal therapy)

58
Q

What are the possible strategies of hormone therapy?

A

1) Opposite steroidal compounds (estrogens for prostate cancer)
2) Anti-hormonal compounds

59
Q

What is the mechanism of Prednisone?

A

It binds to steroid receptors to

1) arrest cells at G1
2) depress expression of many growth-related genes
3) induce nucleases which may modulate cell lysis

60
Q

What are the uses of Prednisone?

A

Lympholytic for Lymphoma
Lymphocytic Leukemia
Breast Cancer
Lymphoid tumors with high steroid receptor content
Palliative effects: anti-emetic, stimulates appetite, anti-inflammatory

61
Q

What are complications and side effects of Prednisone?

A

Potential complication is immunosuppression
At normal doses, limited myelosuppression
Weight gain, fluid retention, psychologic effects

62
Q

What is the mechanism of Tamoxifen?

A

It is a non-steroidal anti-estrogen that competitively blocks estrogen receptors in breast tissue. Cytostatic; tumor regrows when tamoxifen removed.

63
Q

What are the uses for Tamoxifen?

A

1) Advanced post-menopausal breast cancer
2) Pre-menopausal metastatic breast cancer
3) Breast cancer prophylaxis for women at high risk
- Estrogen agonist in bone tissue - may prevent post-menopausal osteoporosis

64
Q

What are the side effects of Tamoxifen?

A

N/V
Hot flashes
Fatigue
Bone and other musculoskeletal pain

65
Q

What is the mechanism of Raloxifene?

A

Estrogen receptor antagonist

66
Q

What is the mechanism of Letrozole?

A

Non-steroidal aromatase inhibitor that blocks conversion of androgens to estrogens

67
Q

What are the uses of Letrozole?

A

1st line treatment of post-menopausal advanced or metastatic breast cancer

68
Q

What are the side effects of Letrozole?

A

Hot flashes
Nausea
Fatigue
Bone and other musculoskeletal pain

69
Q

What is the mechanism of Leuprolide?

A

GnRH analog that desensitizes GnRH signaling after 2-4 weeks and decreases LH/FSH and testosterone to castration levels

70
Q

What is the use of Leuprolide?

A

Advanced hormonally responsive prostate cancer

71
Q

What are the side effects of Leuprolide?

A

Hot flashes

Impotence

72
Q

What is the mechanism of Flutamide?

A

Nonsteroidal anti-androgen that blocks androgen receptors

73
Q

What is the use of Flutamide?

A

Metastatic prostate cancer

74
Q

What are the side effects of Flutamide?

A

Gynecomastia
Diarrhea
Hepatotoxicity

75
Q

What is multi-drug resistance mediated by?

A

ATP-dependent drug efflux pumps

76
Q

What drugs is MDR prominent for?

A

Vincristine, vinblastine, doxorubicin, bleomycin, etoposide, paclitaxel

77
Q

What are the principles of combination chemotherapy?

A

1) different cell cycle specificities
2) active as single agents
3) non-overlapping toxicities
4) different mechanisms of action

78
Q

What is sequential blockade?

A

Simultaneous action of two inhibitors acting on different steps of a linear metabolic pathway
Examples: Hydroxyurea + Cytarabine or Methotrexate + 5-FU

79
Q

What is concurrent inhibition?

A

Inhibitors block two separate pathways that lead to the same end product

80
Q

What is complementary inhibition?

A

One drug affects the function of an end product while the other drug affects the synthesis of that end product
Example: Cytarabine inhibits DNA synthesis and Doxorubicin causes DNA damage

81
Q

What is rescue?

A

The patient’s normal cells are rescued from the treatment

Example: Leucovorin to rescue cells after high dose methotrexate exposure

82
Q

What is synchronization?

A

Synchronize cells so they are in one phase and then use a drug that is specific for that phase
Example: Low doses of fluorouracil to block S phase and then high dose cytarabine to kill in S phase

83
Q

What is recruitment?

A

Mobilizing slowly/non-proliferating cells; bring cells out of G0 and back into cell cycle

FPP MSS (6 decks)

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