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Pharmacology > Oncology > Flashcards

Oncology Flashcards

0
Q

Busulfan

A

MOA: Alkylating age–cross links DNA

Uses: CML. Also used to ablate patients bone marrow before bone marrow transplantation.

Toxicity: severe myelosuppression, pulmonary fibrosis, hyperpigmentation

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1
Q

Cyclophosphamide

A

MOA: Alkylating agent. covalently crosslinks (interstrand) DNA at guanine N-7; requires bioactivation by liver

Uses: solid tumors, leukemia, lymphomas, some brain cancers

Toxicity: myelosuppression, bladder toxicity (hemorrhagic cystitis), partially prevented with mesna (thiol group of mesna binds toxic metabolites)

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2
Q

Cisplatin

A

MOA: cross-links DNA

Uses: testicular, bladder, ovarian, and lung carcinomas

Toxicity: nephrotoxicity and acoustic nerve damage. Protect nephrotoxicity with amifostine (free radical scavenger) and chloride diuresis

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3
Q

Carmustine

A

MOA: nitrosoureas Alkylating agent. Cross links DNA. Requires bioactivation. Crosses the BBB into CNS.

Uses: brain tumors

Toxicity: CNS toxicity (convulsions, dizziness, ataxia)

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4
Q

Topotecan

A

MOA: Topoisomerase I inhibitor–prevents DNA unwinding and replication

Uses: ovarian and small cell lung cancers

Toxicity: severe myelosuppression, diarrhea

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5
Q

Etoposide

A

MOA: Topoisomerase II inhibitor–prevents re-ligation of DNA after Double stranded breaks and increases DNA degradation

Uses: solid tumors (particularly testicular and small cell lung cancers), leukemias, lymphomas

Toxicity: myelosuppression, GI irritation, alopecia

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6
Q

Doxorubicin

A

MOA: generate free radicals. Intercalates in DNA leading to breaks in DNA and decreased replication.

Uses: solid tumors, leukemia, lymphomas

Toxicity: dilated cardiomyopathy, myelosuppression, alopecia. Dexrazoxane (iron chelating agent) used to prevent cardiotoxicity.

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7
Q

Bleomycin

A

MOA: induces free radical formation which causes breaks in DNA strands

Uses: testicular cancer, Hodgkin’s lymphoma

Toxicity: pulmonary fibrosis, skin reactions, alopecia, hypersensitivity reactions, mucositis

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8
Q

Dactinomycin

A

MOA: Intercalates in DNA

Uses: Wilms tumor, Ewing sarcoma, rhabdomyosarcoma, germ cell tumors (childhood tumors)

Toxicity: myelosuppression

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9
Q

Methotrexate

A

MOA: frolic acid analog that Inhibits dihydrofolate reductase, which converts dihydrofolate to tetrahydrofolate in order to participate in pyrimidine biosynthesis. Decreases dTMP and thus decreases DNA and protein synthesis

Uses: 1. Cancers: leukemias, lymphomas, choriocarcinomas, sarcomas 2. Non-Neoplastic: abortion, ectopic pregnancy, rheumatoid arthritis, psoriasis, IBD

Toxicity: myelosuppression (reversible with leucovorin-folinic acid-“rescue”, mucositis (painful mouth ulcers), teratogenic, macrovesicular fatty change in liver

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10
Q

5-fluorouracil

A

MOA: Pyrimidine analog bio activated to 5F-dUMP, which covalently complexes folic acid–this complex inhibits thymidylate synthase leading to decreased dTMP and decreased DNA and protein synthesis

Uses: colon cancer, pancreatic cancer, basal cell carcinoma (topical)

Toxicity: myelosuppression (which is not reversible with leucovorin), overdose: “rescue” with uridine. Photosensitivity

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11
Q

6-Mercaptopurine

A

MOA: Purine analog that leads to decreased de novo purine synthesis. Activated by HGPRT.

Uses: preventing organ rejection, RA. Leukemia, IBD

Toxicity: bone marrow, GI, liver. Metabolized by xanthine oxidase, thus have increases toxicity with allopurinol, which inhibits their metabolism

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12
Q

Paclitaxel

A

MOA: Taxane, anti-microtubule agent. Hyperstabilizes polymerized microtubules in M phase so that mitosis spindle cannot break down (anaphase cannot occur)

Uses: ovarian ca, breast ca

Toxicity: myelosuppression, hypersensitivity reaction, alopecia

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13
Q

Vinblastine

A

MOA: microtubule inhibitor. Vinca alkaloid, anti-microtubule agent. Binds B-tubulin and inhibits it’s polymerization into microtubules, thereby preventing mitotic spindle formation and M phase arrest

Uses: solid tumors, leukemias, and lymphomas

Toxicity: myelosuppression

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14
Q

Tamoxifen

A

MOA: Selective estrogen receptor modulator–non-steroidal ligand for the ER that competes with endogenous estradiol–evokes tissue specific effects. Antagonist in breast and agonist in gone.

Uses: breast ca treatment and prevention

Toxicity: menopausal symptoms, partial agonist in endometrium increases risk for endometrial cancer

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15
Q

Imatinib

A

MOA: tyrosine kinase inhibitor that binds to the ATP binding site of BCR-ABL and c-kit–> growth arrest and apoptosis

Uses: CML, GI stromal tumors

Toxicity: fluid retention

16
Q

Trastuzimab

A

MOA: Anti-HER2 specificity–a tyrosine kinase inhibitor. Help skill breast cancer cells that over express HER2 through inhibition of HER2-initiated cellular signaling and antibody-dependent cytotoxicity

Uses: HER2 positive breast cancer and gastric cancer

Toxicity: cardio toxicity,

17
Q

Bevacizumab

A

MOA: Anti-VEGF specificity–inhibits angiogenesis

Uses: solid tumors (colorectal cancer, renal cell carcinoma)

Toxicity: hemorrhage and impaired wound healing

18
Q

Cytarabine

A

MOA: pyrimidine analog leading to inhibition of DNA polymerase

USES: leukemias, lymphomas

TOXICITY: leukopenia, thrombocytopenia, megaloblastic anemia.

19
Q

Azathioprine

A

MOA: Purine analog that leads to decreased de novo purine synthesis. Activated by HGPRT.

Uses: preventing organ rejection, RA, SLE. Leukemia, IBD

Toxicity: bone marrow, GI, liver. Metabolized by xanthine oxidase, thus have increases toxicity with allopurinol, which inhibits their metabolism

20
Q

6-thioguanine

A

MOA: Purine analog that leads to decreased de novo purine synthesis. Activated by HGPRT.

Uses: preventing organ rejection, RA. Leukemia, IBD

Toxicity: bone marrow, GI, liver. Metabolized by xanthine oxidase, thus have increases toxicity with allopurinol, which inhibits their metabolism

21
Q

Daunorubicin

A

MOA: generate free radicals. Intercalates in DNA leading to breaks in DNA and decreased replication.

Uses: solid tumors, leukemia, lymphomas

Toxicity: dilated cardiomyopathy, myelosuppression, alopecia. Dexrazoxane (iron chelating agent) used to prevent cardiotoxicity.

22
Q

Ifosfamide

A

MOA: Alkylating agent. Same as cyclophosphamide. covalently crosslinks (interstrand) DNA at guanine N-7; requires bioactivation by liver

Uses: solid tumors, leukemia, lymphomas, some brain cancers

Toxicity: myelosuppression, bladder toxicity (hemorrhagic cystitis), partially prevented with mesna (thiol group of mesna binds toxic metabolites)

22
Q

Lomustine

A

MOA: nitrosoureas Alkylating agent. Cross links DNA. Requires bioactivation. Crosses the BBB into CNS.

Uses: brain tumors

Toxicity: CNS toxicity (convulsions, dizziness, ataxia)

23
Q

Semustine

A

MOA: nitrosoureas Alkylating agent. Cross links DNA. Requires bioactivation. Crosses the BBB into CNS.

Uses: brain tumors

Toxicity: CNS toxicity (convulsions, dizziness, ataxia)

23
Q

Streptozocin

A

MOA: nitrosoureas Alkylating agent. Cross links DNA. Requires bioactivation. Crosses the BBB into CNS.

Uses: brain tumors

Toxicity: CNS toxicity (convulsions, dizziness, ataxia)

23
Q

Vincristine

A

MOA: microtubule inhibitor. Vinca alkaloid, anti-microtubule agent. Binds B-tubulin and inhibits it’s polymerization into microtubules, thereby preventing mitotic spindle formation and M phase arrest

Uses: solid tumors, leukemias, and lymphomas

Toxicity: neurotoxicity (areflexia, peripheral neuritis), paralytic ileus

23
Q

Carboplatin

A

MOA: cross-links DNA

Uses: testicular, bladder, ovarian, and lung carcinomas

Toxicity: nephrotoxicity and acoustic nerve damage. Protect nephrotoxicity with amifostine (free radical scavenger) and chloride diuresis

23
Q

Teniposide

A

MOA: Topoisomerase II inhibitor–prevents re-ligation of DNA after Double stranded breaks and increases DNA degradation

Uses: solid tumors (particularly testicular and small cell lung cancers), leukemias, lymphomas

Toxicity: myelosuppression, GI irritation, alopecia

23
Q

Irinotecan

A

MOA: Topoisomerase I inhibitor–prevents DNA unwinding and replication

Uses: colon cancer

Toxicity: severe myelosuppression, diarrhea

23
Q

Hydroxyurea

A

MOA: inhibits ribonucleotide reductase–>decreases DNA synthesis

USES: melanoma, CML, sickle cell disease (increases HbF)

TOXICITY: bone marrow suppression, GI upset

24
Q

Prednisone

A

MOA: May trigger apoptosis. May even work on non dividing cells.

USES: most commonly used glucocorticoid in cancer chemo. Used in CLL, non-Hodgkin lymphoma, also as immunosuppressant

TOXICITY: Cushing like symptoms, weight gain, central obesity, muscle breakdown, cataracts, acne, osteoporosis, HTN, peptic ulcers, hyperglycemia, psychosis

25
Q

Prednisolone

A

MOA: May trigger apoptosis. May even work on non dividing cells.

USES: most commonly used glucocorticoid in cancer chemo. Used in CLL, non-Hodgkin lymphoma, also as immunosuppressant

TOXICITY: Cushing like symptoms, weight gain, central obesity, muscle breakdown, cataracts, acne, osteoporosis, HTN, peptic ulcers, hyperglycemia, psychosis

26
Q

Raloxifene

A

MOA: Selective estrogen receptor modulator–non-steroidal ligand for the ER that competes with endogenous estradiol–evokes tissue specific effects. Antagonist in breast and agonist in gone.

Uses: prevent osteoporosis

Toxicity: no increased risk of endometrial cancer because it is an estrogen receptor antagonist

27
Q

Rituximab

A

MOA: monoclonal antibody against CD20, which is found on most B-cell neoplasms

USES: non-Hodgkin lymphoma, rheumatoid arthritis (with MTX), ITP

TOXICITY: increases risk of progressive multi focal leukoencephalopathy

28
Q

Vemurafenib

A

MOA: small molecule inhibitor forms of the B-Raf kinase with the V600E mutation

USES: metastatic melanoma

29
Q

Cladribine

A

MOA: antimetabolite. Purine analog–>multiple mechanisms (e.g. Inhibition of DNA polymerase, DNA strand breaks)

USES: hairy cell leukemia

TOXICITY: leukopenia, thrombocytopenia, megaloblastic anemia

30
Q

Erlotinib

A

MOA: EGFR tyrosine kinase inhibitor

USES: non-small cell lung carcinoma

Toxicity: rash

31
Q

Amifostine

A

Prophylactic measure used with cisplatin and carboplatin chemo. Free radical scavenger used to prevent nephrotoxicity.

Pharmacology (13 decks)

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