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MI Immuno/Heme > Cancer Pharmacology > Flashcards

Cancer Pharmacology Flashcards

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1
Q

What Tx counteracts the myelosuppressive side-effects of cancer drugs?

A

Prophylactic administration of growth factors protect against myelosupression

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2
Q

Primary toxicity of cisplatin

A

nephrotoxicity

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3
Q

How to prevent methotrexate-induced nephrotoxicity

A

Alkalinization of urine and leucovorin rescue

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4
Q

How to prevent cycloposphamide-induced hemorrhagic cystitis

A

Concomitant use of MESNA

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5
Q

What cancer drugs have a low or negligible myelosupressive mechanism?

A

Vincristine

Bleomycin

Cisplatin

Asparaginase

Trastuzumab

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6
Q

What cancer drugs can cause acoustic nerve damage?

A

Cisplatin/Carboplatin

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7
Q

How do chemotherapeutic drugs cause nasuea and vomiting?

A

Major receptors involved:

5-HT3 receptor

NK1 receptor

Dopamine receptor

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8
Q

Serotonin receptor antagonist used to Tx nausea

A

5-HT3 antagonist:

Ondanestron and granisetron

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9
Q

Neurokinin-1 receptor antagonist to Tx nausea

A

NK-1 antagonist:

Aprepitant and fosaprepitant

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10
Q

Dopamine antagonist to Tx nausea

A

promethazine, prochlroperazine

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11
Q

Which pathway is activates the emetic response within 24 hours after initiation of chemotherapy

A

The peripheral pathway- acute chemotherapy-induced emesis

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12
Q

Mechlorethamine

A

Component of MOPP regimen for Hodgkin’s disease

Alkylating agent that is activated into its intermediate in body fluids

Given IV and can have pronounced vesicant activity and cuase extravasation, tissue necrosis, and sloughing

Nitrogen mustard

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13
Q

Chlorambucil

A

Indications:

Chronic lymphocytic leukemia
Hodgkin lymphoma
Non-Hodgkin lymphoma

Given PO - alkylating compound with 70-100% bioavailability

US Boxed Warning: Bone marrow suppression

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14
Q

Cyclophosphamide

A

Clinical uses:

Leukemias/lymphomas and cancers of soft tissues and neuroblastoma

Also an immunosuppressant drug

Converted to active metabolite phosphoramide mustard by liver P450 - metabolites alkylate DNA

Given IV - no vesicant effects

Dose-limiting myelosuppression, hemorrhagic cystitis due to production of acrolein (risk can be decreased w/ use of 2-mercaptoethane-sulfonate [MESNA])

Cardiac dysfunction, pulmonary fibrosis, and excessive ADH secretion may occur

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15
Q

Cisplatin

A

Kills cells in all stages of the cell cycle inhibits DNA biosynthesis, and binds DNA through the formation of interstrand cross-links

Inside cell - drug is converted to positively charged intermediate that binds DNA and forms both interstrand and intrastrand cross-links

Used in solid tumors (cancer of testis, ovary, bladder, lun, H&E, neuroblastoma, osteogenic sarcoma)

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16
Q

Cisplatin ADME

A

Given IV and cleared in unchanged form by kidneys

Toxicity:

Nephrotoxic (reduced by forceful hydration)

Neurotoxic (peripheral neuritis, acoustic nerve damage)

Myelosuppresssion, nausea and vomiting

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17
Q

Procarbazine

A

Prodrug converted to active intermediate that can cause DNA strand breaks due to formation of free radicals (inhibits DNA/RNA and protein synthesis - prolongs interphase, and produces chromosome breaks)

Used as component of the MOPP regimen

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18
Q

MOPP regimen

A

Mechlorethamine, vincristine, procarbazine, and prednisone used to Tx Hodgkins disease

Used in combination w/ BEACOPP regimen

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19
Q

Nitrosoureas

A

Carmustine and lomustine

Undergo spontaneous degradation in body fluid w/ formation of metabolites that alkylate DNA (do not cause cross-resistance w/ other alkylating agents)

Carmustine is highly lipohilic and can easily enter brain

Neurotoxicity and hepatoxic

Used in brain tumors

Can also cause pulmonary toxicity

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20
Q

Mechanism of drug resistance to cytotoxic Abx’s

A

Increased production of glycoprotein P-170 which leads to an increased efflux of the drug from tumor cells

Enhanced rates of DNA repair

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21
Q

Anthracyclines

A

Doxorubicin and Daunorubicin

Fx:
1. intercalate between DNA bps
2. Inhibit topoisomerase II
3. Generate free radicals which can oxidize DNA bases

Tox:

Severe cardiomyopathy - acute form w/i 2-3 days after beginning regimen (dexrazoxane - chelates iron - can reduce cardiac damage)

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22
Q

Doxorubicin

Clinical use

A

aka Adriamycin

Component of the ABVD regimen for Hodgkin’s disease; also used in many solid tumors

Anthracycline

ABVD = doxorubicin, bleomycin, vinblastine, and dacarbazine (originally developed for Pt’s w/ disease resistant to MOPP)

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23
Q

ABVD Regimen

A

ABVD = doxorubicin, bleomycin, vinblastine, and dacarbazine (originally developed for Pt’s w/ disease resistant to MOPP)

Regimen for Hodgkin’s disease and also used in many solid tumors

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24
Q

Dactinomycin

A

Antitumor Abx isolated from Streptomyces - binds tightly to dsDNA through intercalation between adjacent guanine-cytosine bps and inhibits all forms of DNA-dependent RNA synthesis

Clinical use:

Mainly to Tx pediatric tumors such as Wilm’s tumor (affects kidneys)

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25
Daunorubicin
Used in acute myelogenous leukemia | Anthracycline
26
Bleomycin
CCS drug that acts in the **G2 phase** of the cell cycle Associated w/ pulmonary fibrosis in 2-3% of Pt's Clinical use: ABVD regimen for Hodgkin's disease - used in lymphomas, lung and testicular cancers
27
Acquired resistance to antimetabolite therapy
Methotrexate - decreased target receptor affinity Mercaptopurine/thioguanine/cytarabine/fluorouracil - reduced activation of prodrugs Mercaptopurine/fluorouracil/mehotrexate - decreased sensitivity of a target enzyme
28
Methotrexate
**Competively inhibits dihdrofolate reductase** resulting in decreased synthesis of tetrahydrofolate Clinical use: Acute leukemias, lymphomas, choriocarcinoma, breast and lung cancer Also used in graft rejection control, RA, and psoriasis ## Footnote THFA is used in purine/pyrimidine synthesis
29
What enzyme do mercaptopurine and thioguanine inhibit when they are transformed into false purine nucleotides?
Phophsoribosylpyrophosphate synthetase and phosphoribosylpyrophosphate aminotransferase ## Footnote Critical for synthesis of phosphoribosylamine - essential in purine synthesis
30
Fludarabine
Nucleotide analog which is **phosphorylated intracelluarly** and incorporated into DNA and RNA - metabolite interferes w/ DNA synthesis through **inhibition of DNA polymerase ribonucleotide reductase** Clinical use: Mainly for remission maintenance in **acute lymphoblastic leukemia (ALL)** and is the DOC for **chronic lymphocytic leukemia (CLL)** | Induces apoptosis ## Footnote May cause peripheral neuropathy (neurotoxic) Long term use may cause hepatotoxicity
30
Pentostatin
**Inhibits adenosine deaminase** - leads to intracellular accumulation of adenosine - blocks DNA synthesis
31
Allopurinol increases the toxicity of what drug used to treat hematologic cancers?
Mercaptopurine (6-MP) - converted to an inactive metabolite (6-thiouric acid) by oxidation catalyzed by xantine oxidase
32
Fluorouracil
Activated to a false nucleotide which inhibits thymidylate synthease - reduces availability of thymidylic acid - impairing DNA synthesis Clinical use: Slow growing, solid tumors (H&E, bladder, stomach, and colon cancers) ## Footnote Capecitabine is a prodrug converted to 5-fluorouracil
33
Cytarabine (cytosine arabinoside)
Activated to false nucleotide that is incorporated at the terminal position of a growing DNA chain **Used in acute myelogenous leukemia** | Can cause neurotoxicity after intrathecal administration
34
What antimitotic drugs bind to tubulin and inhibit tubulin polymerization (prevents microtubule assembly)
Vincristine and vinblastine
35
Vincristine clinical uses
Component of MOPP regiment Also leukemias, lymphomas, and Wilms' tumor
36
Vinblastine clinical uses
Componenet of ABVD regimen Also used to Tx neuroblastoma and testicular cancer
37
What antimitotic drugs bind to tubulin and inhibit tubulin depolymerization?
Paclitaxel and docetaxel (**taxanes**) prevent microtubule disassembly They are used to Tx breast and ovarian cancers
38
Etoposide
Podophyllin analogue - **inhibits topoisomerase II** Mainly used to Tx testicular and small cell lung cancers, but is also used to **Tx Hodgkin's and non-Hodgkin's lymphomas** ## Footnote Mainly act in the S and G2 phases of cell cycle
39
Topotecan
Camptothecin analogue - inhibits topoisomerase I Used to Tx ovarian and lung cancer ## Footnote Mainly act in the S and G2 phases of cell cycle
40
Asparaginase
Ezyme isolated from bacteria that **acts in the G1 phase** of the cell cycle by **depleting serum asparagine** - results in inhibition of protein synthesis in some neoplastic cells (lymphoblastic leukemic cells) that are not able to synthesize R Mainly used in luekemias and lymphomas
41
Hydroxyurea
Analog of urea - inhibits DNA synthesis in **S phase** by **inhibiting ribonucleotide reductase** - depletes deoxynucleosides Used to Tx melanoma and chronic myelogenous leukemia
42
IFN-α in cancer Tx
Approved for Tx of hairy cell leukemia, chronic myelogenous leukemia, malignant melanoma, and Kaposi sarcoma ## Footnote increased host expression of major histocompatibility complex antigens, enhanced phagocytic activity of macrophages, and augmentation of the **proliferation and survival of cytotoxic T cells.**
43
Erlotinib
Reversible inhibitor of **epidermal growth factor receptor (EGFR) tyrosine kinase** Competitively inhibits ATP binding at the site of the kinase - **regulates G1 restriction**
44
Rituximab
mAb to the **CD20** surface protein on normal and malignant B lymphocytes Used in non-Hodgkin's lymphomas ## Footnote May cause reactivation of Hep B or rarely JC virus (w/ progressive multifocal leukencrephalopathy)
45
Trastuzumab
mAb to **human epidermal growth factor receptor 2** (HER-2) - may be overexpressed in some primary breast carcinoma Used in HER-2 + metastatic breast and gastric cancers | Toxic: cardiac dysfunction
46
Bevacizumab
**Anti-angiogenic drug that inhibits VEGF from binding to it receptor** - especially on endothelial cells Humanized IgG1 mAB Approved for Pt's w/ metastatic colorectal cancer Used off label by intravitreal injection to slow progression of neovascular macular degeneration
47
Gemtuzumab ozogamicin
Humanized mAb against **CD33** covalently linked to a derivative of caliheamicin (potent antitumor Abx) **CD33 present on most hematopoietic cells** - on more than 80% of acute mylogenous leukemias Following binding to CD33 - undergoes endocytosis; cleavage of calicheamicin from Ab takes place w/i the lysosome - enters nucleus and binds in the minor groove of DNA and causes dsDNA break and cell death
48
Aletuzumab
Humanized **IgG-kappa mAb that binds to CD52 Ag** CD52 is found on subset of normal neutrophils and on all B/T lymphocytes Approved for Tx of B-cell chronic lymphocytic leukemia Also used in Tx of Pt's w/ relapsing forms of multiple sclerosis
49
Anastrazole
Aromatase inhibitor Aromatase catalyzes conversion of andostenedione to estrone
50
Fulvestrant
Competitive estrogen receptor antagonist (effective in some Pt's that have become resistant to tamoxifen)
51
Drugs used in prostatic carcinoma
**Leuprolide** and **goserelin** (GnRH agonist) - inhibit release of LH and FSH when administered in constant doses **Flutamide** - competitive androgen receptor antagonist
52
Why are glucocorticoids used in conjunction w/ chemotherapy regimens?
1. Their lymphocytotoxic action (Tx of lymphocytic leukemia/lymphoma and multiple myeloma) 2. Anti-inflammatory and immunosuppressant actions - pallative therapy 3. Decreases chemotherapy induced NV
53
Anthracycline antibiotics - cell cycle nonspecific
54
A patient recently diagnosed with chronic lymphocytic leukemia began a treatment with chlorambucil. The mechanism of action of the drug is likely due to?
the formation of covalent bonds with nucleophile groups on DNA bases.
55
Vincristine
56
Cell cycle nonspecific cancer drugs
57
C. Dactinomycin E. Vincristine F. Etoposide
58
What cytotoxic Abx is cell cycle specific?
Bleomycin | G2 phase
59
Side-effects associated w/ most cancer therapeutics
N&V Alopecia Myelosuppression
60
C. Increased synthesis of glycoprotein P-170
61
A. The formation of covalent bonds w/ nucleophile groups on DNA bases ## Footnote Answer choic B = Cytarabine (cytosine arabinoside)
62
When is leucovorin rescue used during chemotherapy?
In conjugation w/ methotrexate
63
D. Inhibits both purine and pyrimidine synthesis
64
A. Inhibition of thymidylate synthetase
65
B. Bleomycin
66
A. Depletion of endothelial growth factors for angiogensis ## Footnote Bevacizumab blocks VEGF activity
67
## Footnote Bonus: what Abx is associated with ototoxicity
A. Cisplatin ## Footnote Bonus: aminoglycosides
68
D. Dactinomycin binds to dsDNA inhibiting DNA transcription
69
C. Inhibiting uric acid formation after cell lysis
69
A. To improve chemotherapy-induced NV | i.e. aprepitant and fosaprepitant
70
E. Xanthine oxidase | Can lead to toxic accumulation
71
B. Rituximab
72
D. Cisplatin and paclitaxel
73
B. It is highly lipid soluble and therefore can easily enter the brain | Carumstine = nitrosourea ## Footnote Can be associated w/ pulmonary toxicity
74
D. Cyclophosphamide
75
C. MESNA (2-mercaptoethane sulfonate)

MI Immuno/Heme (35 decks)

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