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Pharm > Anti-Cancer > Flashcards

Anti-Cancer Flashcards

1
Q

Methotrexate

*ant-metabolite

A
  • Folic acid analog, inhibits DHF reductase = dec. dTMP = dec. DNA & protein synthesis.
  • Uses:
  • -Cancers: leukemias, lymphomas, choriocarcinoma, sarcomas.
  • -Non-neoplastic: abortion, ectopic pregnancy, rheumatoid arthritis, psoriasis, IBD.
  • Tox: BMS (reversible w/leucovorin), Macrovesicular fatty change in liver, Mucositis, Teratogenic.
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2
Q

5-fluorouracil (5-FU)

*ant-metabolite

A
  • Complexes folic acid & inhibits thymidylate synthase = dec.Ž dTMP Ž= dec DNA and protein synthesis.
  • flucytosine (anti-fungal) metabolized to 5-FU
  • Use: Colon cancer, pancreatic cancer, basal cell carcinoma (topical).
  • Tox: BMS (reversible w/uridine), photosensitivity.

**causes thymine-less death.

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3
Q

Cytarabine (arabinofuranosyl cytidine)

*ant-metabolite

A
  • Pyrimidine analog =>Ž inhibition of DNA polymerase.
  • Use: leukemias, lymphomas.
  • Tox: BMS, megaloblastic anemia.
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4
Q

Azathioprine, 6-mercaptopurine (6-MP), 6-thioguanine (6-TG)

A

-Purine (thiol) analogs = dec.  de novo purine synthesis. Activated by HGPRT. Inhibits PRPP amidotransferase (PRPP -> IMP)
-Use: Preventing organ rejection, RA, SLE (azathioprine).
Leukemia, IBD (6-MP, 6-TG).
-Tox: Bone marrow, GI, liver. Azathioprine & 6-MP are
metabolized by xanthine oxidase; thus both have inc.
 toxicity with allopurinol, which inhibits their metabolism.

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5
Q

Dactinomycin (actinomycin D)

A
  • Intercalates in DNA.
  • Use: Wilms tumor, Ewing sarcoma, rhabdomyosarcoma. Used for childhood tumors (“children act out”).
  • Tox: BMS
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6
Q

Doxorubicin (Adriamycin), daunorubicin

A

-Generate free radicals & intercalate in DNA = dec. DNA rep.
-Use: Solid tumors, leukemias, lymphomas.
-Tox: Cardiotoxicity (dilated cardiomyopathy), BMS, alopecia. Toxic to tissues following extravasation.
Dexrazoxane (iron chelating agent), used to prevent
cardiotoxicity.

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7
Q

Bleomycin

A
  • Free radical formation
  • Use: Testicular cancer, HL.
  • Tox: Pulm. fibrosis, skin changes, mucositis.
  • *NO BMS.
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8
Q

Cyclophosphamide, ifosfamide

*Alkylating agents

A

-Covalently X-link DNA at guanine N-7. Require
bioactivation by liver.
-Use: Solid tumors, leukemia, lymphomas, and some brain cancers.
-Tox: BMS; hemorrhagic cystiti (prevent w/mesna).

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9
Q

Nitrosoureas (carmustine, lomustine, semustine,
streptozocin)
*Alkylating agents

A
  • Require bioactivation. Cross BBB. Cross-links DNA.
  • Use: Brain tumors (including glioblastoma multiforme).
  • Tox: CNS tox. (convulsions, dizziness, ataxia).
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10
Q

Busulfan

*Alkylating agent

A
  • Cross-links DNA.
  • Use: CML. Also used to ablate patient’s bone marrow before bone marrow transplantation.
  • Tox: Severe BMS, pulm. fibrosis, hyperpigmentation.
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11
Q

Vincristine, vinblastine

A

-Inhibit MT polymerization.
-Use: Solid tumors, leukemias, and lymphomas.
-Tox:
–Vincristine = neurotoxicity (areflexia, peripheral neuritis),
paralytic ileus. **NO BMS
–Vinblastine = blasts bone marrow (suppression).

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12
Q

Paclitaxel, other taxols

A
  • inhibit MT depol.
  • Use: Ovarian and breast carcinomas.
  • Tox: BMS, alopecia, hypersensitivity.
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13
Q

Colchicine

A
  • Inhibit MT polymerization (impairing leukocyte chemotaxis and degranulation).
  • Use: Gout, cancer.
  • Tox: GI
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14
Q

Cisplatin, carboplatin

A
  • Cross-link DNA
  • Use: Testicular, bladder, ovary, and lung carcinomas.
  • Tox: Nephrotoxicity and acoustic nerve damage. Prevent nephrotox w/amifostine and chloride diuresis.
  • *NO BMS
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15
Q

Etoposide, teniposide

A
  • inhibit topoisomerase 2 => inc. DNA degradation.
  • Use: Solid tumors (particularly testicular and small cell lung cancer), leukemias, lymphomas.
  • Tox: BMS, GI irritation, alopecia.
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16
Q

Irinotecan, topotecan

A
  • inhibit topoisomerase 1 => prevent DNA unwinding & replication.
  • Use: Colon cancer (irinotecan); ovarian and small cell lung cancers (topotecan).
  • Tox: Severe BMS, diarrhea.
17
Q

Hydroxyurea

A
  • Inhibits ribonucleotide reductase => dec. DNA Synthesis (S-phase specific). Also inc. Hb-F.
  • Use: Melanoma, CML, sickle cell disease.
  • Tox: Bone marrow suppression, GI upset.
18
Q

Prednisone, prednisolone

A

-Trigger apoptosis. May even work on nondividing cells.
-Use: CLL, NHL.
-Tox: Cushing-like symptoms; weight gain, central obesity, muscle breakdown, cataracts, acne,
osteoporosis, hypertension, peptic ulcers, hyperglycemia, psychosis.

19
Q

Tamoxifen

A

-SERM
Breast = antagonist
Bone = agonist
Endometrum = agonist

20
Q

raloxifene

A

-SERM
Breast = antagonist
Bone = agonist
Endometrum = antagonist

21
Q

Trastuzumab (Herceptin)

A
  • Kills Her2 (c-erbB2), a tyrosine kinase receptor) positive breast cancer cells.
  • Tox: cardiotoxicity
  • “Heart”ceptin.
22
Q

Imatinib (Gleevec)

A
  • Tyrosine kinase inhibitor of bcr-abl (Ph. chrom. fusion gene in CML) and c-Kit (common in GI stromal tumors).
  • Tox: fluid retention
23
Q

Rituximab

A
  • Mab against CD20, found on most B-cell neoplasms.
  • Use: NHL, rheumatoid arthritis (with MTX), ITP.
  • Tox: inc. risk of progressive multifocal leukoencephalopathy.
24
Q

Vemurafenib

A
  • Inhibitor of forms of the B-Raf kinase with the V600E mutation.
  • Use: metastatic melanoma
25
Q

Bevacizumab

A
  • Mab against VEGF. Inhibits angiogenesis.
  • Use: Solid tumors (colorectal cancer, renal cell carcinoma).
  • Tox: Hemorrhage and impaired wound healing.

Pharm (12 decks)

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