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Pharmacology > Exam 9: Anti Cancer Agents > Flashcards

Exam 9: Anti Cancer Agents Flashcards

(60 cards)

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1
Q

What do we need to know for each agent?

A

Category
Mechanism
Toxicity
Only need to know specific uses when noted explicitly (seriously, don’t try to memorize a bunch of other shit)

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2
Q

Name 2 nitrogen mustards

A

Mechlorethamine

Cyclophosphamide

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3
Q

Name 1 nitrosourea

A

Carmustine

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4
Q

Name one platinum complex

A

Cisplatin

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5
Q

Name 1 folic acid analog

A

Methotrexate

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6
Q

Name 1 purine analog

A

Mercaptopurine

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7
Q

Name 2 pyrimidine analogs

A

Fluorouracil

Cytarabine

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8
Q

Name 2 anthacycline antibiotics

A

Daunorubicin

Doxorubicin

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9
Q

Name 4 vinca alkaloids, epipodophylotoxins, and taxanes

A

Vinblastine
Vincristine
Etoposide
Paclitaxel

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10
Q

Name 2 corticosteroids used in cancer treatment

A

Prednisone

Dexamethasone

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11
Q

Name one estrogen/antiestrogen

A

Tamoxifen

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12
Q

Name one Tyrosine Kinase inhibitor

A

Imatinib

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13
Q

Name one monoclonal antibody used for cancer treatment

A

Trastuzumab

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14
Q

What is a difference in general usefulness in cell cycle specific vs cell cycle non-specific agents?

A

CCS are better at treating tumors with lots of cells that are proliferating
CCNS are better in low-growth solid tumors

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15
Q

What are the cell cycle non specific agents?

A

All the alkylators and the 2 antibiotics:
Mechlorethamine, Cyclophosphamide, Carmustine, Cisplatin
and
Daunorubicin
Doxorubicin

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16
Q

What are three alkylating agents?

A

Mechlorethamine
Cyclophosphamide
Carmustine
Cisplatin (kind of, causes cross linking without actual alkylation)

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17
Q

What is the mechanism of alkylating agents?

A

Alkylation of Nitrogen 7 on Guanine

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18
Q

What are 3 consequences of alkylation of Guanine?

A
  1. Miscoding of DNA strands (won’t interact with complementary base)
  2. Incomplete repair of alkylated segment (breaks/depurination)
  3. Excessive cross linking of DNA and inability for strand separation
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19
Q

Are alkylating agents CCS or CCNS?

A

CCNS

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20
Q

What are toxicities of Alkylating agents?

A

Acute- Nausea, vomiting
Long Term- Bone marrow depression
These are the main toxicities seen in most cancer drugs, except when explicitly noted

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21
Q

Mechlorethamine mechanism

A

Alkylation of Nitrogen 7 on Guanine

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22
Q

Cyclophosphamide mechanism

A

Alkylation of Nitrogen 7 on Guanine

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23
Q

Cyclophosphamide pharmacokinetic consideration

A

Prodrug

Must be activated by p450 enzyme

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24
Q

Carmustine mechanism

A

Alkylation of Nitrogen 7 on Guanine

Nirtosurea

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25
What is a pharmacodynamic feature of carmustine?
Highly lipid soluble
26
Cisplatin mechanism
Bifunctional alkylating agent | Causes cross linking
27
Cisplatin toxicity
Nephrotoxic and Ototoxic
28
Cisplatin class
Platinum complex
29
Are antimetabolites CCS or CCNS?
CCS
30
Methotrexate Mechanism
Folic acid analog | Inhibits dihydrofolate reductase, preventing creation of Tetrohydrofolate needed for DNA synthesis
31
What protects normal cells with methotrexate use?
Leucovorin (Folinic acid) | Bypasses metabolic block by methotrexate
32
What phase is affected by Methotrexate?
S phase (DNA synthesis)
33
Methotrexate toxicity
Acute- Nausea, vomiting | Long Term- Bone marrow depression
34
Methotrexate uses
Psoriasis, Rheumatoid arthritis
35
Mercaptopurine mechanism
Purine analog | Inhibits enzymes of purine interconversion, decreasing nucleotide synthesis
36
What cell cycle phase is affected by Mercaptopurine?
S phase
37
5-Fluorouracil mechanism
Pyrimidine analog | Inhibits thymidylate synthetase covalently, inhibiting DNA synthesis (S phase)
38
5-Fluorouracil toxicity
Less GI effects than other cancer drugs
39
Cytarabine mechanism
Pyrimidine analog Converted to cytarabine triphosphate Inhibits DNA polymerase by competing with deoxycitidine triphosphate S phase specific
40
Daunorubicin and Doxorubicin mechanism
Intercalate and bind to DNA between base pairs, uncoiling DNA, destroying template (Not CCS)
41
When is the most effect seen with Daunorubicin and Doxorubicin
S phase, but still considered non specific
42
Daunorubicin and Doxorubicin toxicity
Cardiomyopathy (Dilated) | *** Pretty sure this will be a test question.
43
Vinblastine and Vincristine Mechanism
Vinca Alkaloids Bind to tubulin and disrupt the mitotic spindle apparatus Prevents segregation of chromosomes in metaphase
44
What phase are Vinca alkaloids specific for?
Mitosis phase (Metaphase)
45
What toxicity is associate with Vincristine and Vinblastine?
Neurological side effects (eg. peripheral neuropathy) | Also general toxicities seen in most cancer drugs
46
Etoposide mechanism
Forms a complex with Topoisomerase II and DNA resulting in DNA breaks and cell death. Specific for G2 phase
47
What cell cycle phase is Etoposide specific for?
G2
48
Paclitaxel mechanism
Antimicrotubule agent. Enhances microtubule assembly Stabilizes microtubules (they can't depolymerize) Specific for G2 and M phase
49
What cell cycle phase is Paclitaxel specific for?
G2 and M phases
50
Prednisone and Dexamethasone mechanism
Lipid soluble, diffuse into cells, affect transcription of genes in the nucleus. Suppress mitosis in lymphocytes G1 phase specific
51
What cell cycle phase are corticosteroids specific for?
G1
52
Tamoxifen mechanism
Non steroidal anti estrogen Blocks estrogen receptors (nuclear transcription factors) that stimulate growth G1 phase specific
53
What cell cycle phase is Tamoxifen specific for?
G1
54
Tamoxifen toxicities
Short term: Menopausal symptoms (Hot flashes, headaches, fatigue, etc.) Long term: visual changes, vaginal bleeding, ocular toxicity, thromboembolism, thrombocytopenia Most Serious: Can promote tumor growth and increase incidence of endometrial cancer
55
Tamoxifen use
Estrogen receptor positive invasive breast cancer | Often used for breast cancer in men
56
Imantinib mechanism
Inhibits Bcr-Abl tyrosine kinase | Inhibits proliferation and triggers apoptosis in Bcr-Abl-positive leukemia cell lines
57
Imantinib uses (2)
Acute Lymphocytic Leukemia (ALL) | Ph+ (Philadelphia chromosome + 9:22) Chronic Myeloid Leukemia (CML)
58
Trastuzumab mechanism
(Herceptin) IgG1 monoclonal antibody that binds to the the EGF receptor HER-2 Down regulates the receptor's tyrosine kinase activity which are involved in metastasis Phase G1 specific
59
Trastuzumab uses
Breast cancers that overexpress EGF2 | In combo with paclitaxel is the first line treatment for HER2-overexpressing metastatic breast cancer
60
What is the first line treatment for HER2-overexpressing metastatic breast cancer?
Trastuzumab and Paclitaxel

Pharmacology (34 decks)

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