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70 Cards in this Set

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Cardiac toxicity

*Doxorubicin, *daunorubicin
What drug acts on G2 phase?
Bleomycin
What drug acts on M phase?
Vinblastine, vincristine, paclitaxel
Neurologic toxicity
*Vincristine (peripheral neuropathy), *cisplatin (ototoxicity), paclitaxel
What drug acts on G0 phase?
Alkylating agents, antitumor antibiotics, cisplantin, and nitrosourea (lomustine, carmustine)
What drug acts on S phase?
Antimetabolites: cytarabine, 6-mercaptopurine, 6-thioguanine, methotrexate, hydroxyurea

Inhibits topoisomerase II: etoposide
Major SE of bleomycin
Pulmonary fibrosis
Toxicity of anticancer drugs commonly affect?
Rapidly dividing cells: bone marrow, GI tract, hair follicles, and gonads (gametes).

Often, bone marrow suppression is dose limiting.
Renal toxicity
Cisplatin*, methotrexate
Hepatic toxicity
*6-MP, *busulfan, cyclophosphamide
Pulmonary toxicity
*Bleomycin, busfulfan, procarbazine
Immunosuppressive toxicity
*Cyclophosphamide, *methotrexate
Hemorrhagic cystitis

Leukemia

Pancreatitis
Cyclophosphamide

Procarbazine

Asparaginase
Question: ******A 32 year old woman underwent segmental mastectomy for a breast tumor of 3 cm diameter. Lymph node sampling revealed 2 involved nodes. Because chemotherapy is of established value in her situation, she underwent postoperative treatment with antineoplastic drugs. The regimen consisted of doxorubicin followed by cyclophosphamide/methotrexate/fluorouracil. Adjunctive drugs included tamoxifen because the tumor cells were hormone receptor-positive.
****
Question: ****Which of the following best describes the mechanism of anticancer action of cellular metabolites of fluorouracil?
Irreversible inhibition of thymidylate synthase.

5-FU forms 5-dUMP, which blocks the synthesis of thymine nucleotides. DNA synthesis is inhibited by decrease dTMP.
Question: ***The chemotherapy undertaken by this PT caused acute hemorrhagic cystitis. Which drug was most likely to be responsible for this toxicity?
Cyclophosphamide.

Acrolein, is a toxic metabolite of cyclophosphamide that is concentrated in the urine and associated with hemorrhagic cystitis.

Mensa, can prevent this complication.
Question: ***After several cycles of chemotherapy, the PT was found to have a high resting pulse rate. A noninvasive radionuclide scan revealed evidence of cardiomyopathy. The drug that is most likely responsible for the cardiac toxicity is?
Doxorubicin.

A high resting pulse rate is one of the first signs of cardiotoxicity resulting from anthracyclines, which include arrhythmias, cardiomyopathies, and CHF.
Question: Which of the following is a cell cycle-specific anticancer drug that acts mainly in the M phase of the cell cycle?
Taxanes: paclitaxel, and docetaxel

They have effects on the microtubules.
Question: An adult PT is being treated for acute leukemia which a combination of anticancer drugs that includes cyclophosphamide, mercaptopurine, methotrexate, vincristine, and prednisone. He is also using ondansetron for emesis, a chlorhexidine mouthwash to reduce mucositis, and laxatives. The Pt complains of "pins and needle" sensations in the extremities and muscle weakness. He is not able to execute a deep knee bend or get up out of a chair without using his arm muscles. He is also very constipated. If these problems are related to the chemotherapy, what drug is the most likely causative agent.
Vincristine.

Note: Constipation is the most common symptom of autonomic neuropathy.
Question: What drug is used in combination therapy for testicular carcinoma and is also associated with nephrotoxicity?
Cisplatin, which has nephrotoxicity characteristics.
Question: A cancer cell that is resistant to the effects of both vincristine and methotrexate probably has developed the resistance as a result of which of the following mechanisms?
Increased expression of a P-glycoprotein transporter.

P-glycoprotein family of transporters moves foreign molecules out of cells.
Question: @@@A 23 year old man with Hodgkin's lymphoma was treated unsuccessfully with the MOPP regimen (mechlorethamine, vincristine, prednisone, procarbazine). He subsequently underwent a successful course of therapy with the ABVD regimen (doxorubicin, bleomycin, vinblastine, dacarbazine).
@@@@
@@@Question: What class of anticancer drugs used in the treatment of this PT is cell cycle specific (CCS) and used in both the MOPP and ABVD regimens?
Plant alkaloids
@@@Question: During the second course of drug treatment (ABVD regimen), this PT developed dyspnea, a nonproductive cough, and intermittent fever. Chest x-ray film revealed pulmonary infiltration. If these problems are due to the anticancer drugs to which he has been exposed, which of the following is the most likely causative agent?
Bleomycin.
Question: Cyclophosphamide, doxorubicin, fluoxymesterone, methotrexate, trastuzumab, have all been used for treatment of breast carcinoma. Which one has specific activity in a subset of female breast cancers.
Trastuzumab, a monoclonal AB to breast cancer cells that over-express HER-2 protein.
Question: If allopurinol is used adjunctively in cancer chemotherapy to offset hyperuricemia, the dosage of this anticancer drug should be reduced to 25% of normal.
Mercaptopurine.

The antimetabolite mercaptopurine is metabolized by xanthine oxidase. In the presence of an inhibitor of this enzyme toxic levels will be reached.
Question: This drug is used in combination therapy for testicular carcinoma. It is a CCS drug that acts in the S via interactions with topoisomerase II.
Etoposide
Question: This antimetabolite inhibits DNA polymerase and is one of the most active drugs in leukemias. Although myelosuppression is dose limiting, the drug may also cause cerebellar dysfunction, including ataxia and dysarthria.
Cytarabine.

A pyrimidine antimetabolite that inhibits DNA polymerase.

Used for acute leukemias.
What is an oncogene?
A mutant form of a normal gene that is found in naturally occurring tumors and which, when expressed in non-cancerous cells, causes them to behave like cancer cells.
What is a cell-cycle-nonspecific (CCNS) drug?
Acts during the resting phase. Also, occurs acts when the cell is transversing the cell cycle.

Note: since they act on DNA; they have the worse toxicity. They can be used with low- and high-growth fraction
Cell cycle-specific (CCS) drug?
Only acts when the cell is traversing the cell cycle.

Note: Leukemia and lymphomas respond better to CCS
What are three examples of rescure therapy?
Leucovorin: is a folinic rescue for methotrexate.

Mercaptoethanesulfonate (MESNA): "traps" acrolein released from cyclophosphamide to reduce hemorrhagic cystitis.

Dexrazoxane: protects against cardiac toxicity against free radical produced by doxorubicin
What is the MOA of alkylating agents? What kind of drug are they?
They are CCNS drugs.

They form reactive species that alkylate nucleophilic groups on DNA bases. This leads to cross-linking of bases, abnormal base-pairing, and DNA breakage.

Note: Tumor cell reistance occurs via DNA repair, decreased drug permeability, and producing of trapping agents such as thiols.
What are some alkylating agents?
Cyclophosphamide

Nitrosoureas (carmustine, lomustine)

Alkyl sulfonates (busulfan)

Platinum analogs: cisplatin, carboplatin

Others: procarbazine
What are the MOA and SE from cyclophosphamide?

What is a breakdown product from this drug, and what is the treatment for this?
Attacks guanine N7

Hemorrhagic cystitis, myelosuppression, hepatotoxicity.

Acrolein, which can be decreased by hydration and use of mercaptoethanesulfonate (mensa).
What is cyclophosphamide used for?
Solid and hematologic malignancies (eg., breast, ovarian, non-Hodgkin lymphoma, leukemia, neuroblastoma)

Note: this alkylating agent works in G0 phase; therefore, non-rapidly dividing cell--but also, rapidly dividing.
What is mechlorethamine best known for?
Part of the MOPP protocol for treatment of Hodgkin lymphoma.
What is cisplatin used for? MOA
Cross-link DNA

Genitourinary tumors (testicular, ovarian, bladder) and other solid tumors (lung, stomach)

Nephrotoxicity, ototoxicity, BUT does not cause bone marrow suppression.
What is procarbazine MOA?

What is it used for?

Its SE?
Forms hydrogen peroxide, generating free radicals that cause DNA strand scission.

Part of MOPP regimen for Hodgkin's lymphoma.

Inhibits monoamine oxidase (do not ingest tyramine foods: cheese, wine, smoked meat), disulfiram-like reaction, and is leukemogenic.
What drugs belong to nitrosoureas, what are they used for?
Carmustine, lomustine. Suffix: --mustine

They are highly lipid soluble. They are used for brain tumors (e.g., glioblastoma multiforme)
What antimetabolites act on: folic acid, purines, and pyrimidines?

What kind of drug are they, and what phase of the cell cycle do they work on?
Folic acid: methotrexate, on DHF reductase

Purines: mercaptopurine, thioguanine

Pyrimidines: fluorouracil, cytarabine, gemcitabine.

CCS drugs that act in the S phase.

Note: in addition to cytotoxic effects on neoplastic cells, they also have immunosuppressant actions.
What is the MOA of methotrexate?

SE, and what can be used to prevent this?
Inhibits dihydrofolate reductase, leading to decrease synthesis of thymidylate, purine nucleotides, and a.a.

Bone marrow suppression. Leucovorin, a folinic acid, rescue. And long term use with pulmonary and hepatotoxicity
What is methotrexate used for?
Variety of malignancies (lymphomas, acute leukemias, primary CNS lymphomas, solid tumors, choriocarcinoma)

Used as an immunosuppressant (RA, psoriasis, scleroderma, Crohn disease)

Abortificacient when administration with a prostaglandin (treat missed abortions or ectopic pregnancy).
What is the MOA of mercaptopurine and thioguanine?

SE?
Purine antimetabolites. Activated by HGPRTase

HGPRTases converts them into purine analog to inhibit purine synthesis.

Bone marrow suppression and hepatic dysfunction.

Note: 6-TG can be given with allopurinol, while 6-MP has complications.
What are mercaptopurine and thioguanine used for?
Leukemias (especially acute lymphoblastic leukemia and chronic myelocytic leukemia).
What is the MOA of fluorouracil (5-FU)?

What is it used for?
5-FU is converted into 5-FdUMP, which inhibits thymidylate synthase, leading to "thymineless death."

Solid tumors (colon, bladder, breast, head and neck, etc.)

Can also be used topically for keratoses and basal cell carcinoma.

Myelosuppresion, neurotoxicity, photosensitivity.

Note: uracil replaces thymine during DNA transcription--thymineless death! Rescue with thymidine.
What is the MOA of cytarabine?

What is unique about cytarabine?
Pyrimidine antimetabolite. Is activated to AraCTP by kinases, an inhibitor of DNA polymerase.

Of all antimetabolites, it is the most specific for the S phase of the cell cycle.
What is the MOA of gemcitabine?
Converted into di- and tri-phosphate nucleotide reductase, which diminishes the pool of deoxyribonucleoside triphosphates required for DNA synthesis.

Pancreatic cancer (and also non-small cell lung cancer, bladder cancer, and non-Hodgkin's lymphoma).
What is the MOA of vincristine and vinblastine, and what cell cycle is it effective in? What's different about their SE?
They block the formation of mitotic spindle; therefore, they mainly act in the M phase of cell cycle

Vincristine: neurotoxicity (peripheral neuritis), paralytic ileus

VinBLASTine: BLAST bone marrow suppression.
What are the vinca alkaloids used for?
Vincristine: ALL, part of MOPP protocol, Wilms' tumor, neuroblastoma.

Vinblastine: testicular carcinoma, various lymphomas.
What are the SE of vincristine and vinblastine?
Vincristine: peripheral neuropathy

Vinblastine: severe bone marrow suppression. vinBLASTine BLAST bone marrow.
What is the MOA of etoposide and teniposide? What cell cycle does it act in?
Induces DNA breakage by inhibition of topoisomerase II.

Late S, early G2.
What is etoposide used for?

SE?
Solid tumors (even small cell carcinoma, also testicular, prostate, glioblastome multiforme) and hematologic malignancies (lymphoma, leukemia)

Myelosuppression, alopecia.
What are the 2 camptothecins, MOA, and SE?
Topotecan and irinotecan DNA damage by inhibiting topoisomerase I.

Topotecan, 2nd line drug for advanced ovarian cancer and small cell lung cancer. Irinotecan for metastatic colorectal cancer.

Myelosuppression.
What are the two taxanes? What are their MOA and how are they different than vinca alkaloids?
Paclitaxel and docetaxel. Suffix: -taxel

They interfere with mitotic spindle. They act differently than vinca alkaloids since they prevent microtubule disassembly into tubulin monomers (promote stabilization, which halt mitosis from entering anaphase).

Solid tumors

Myelosuppression, peripheral neuropathy.
nect/o
to bind,
tie, connect
What is MOA of anthracyclines, and what drugs belong to this class? What type of drug?
Doxorubicin Suffix: -rubicin

3 MOA: intercalate between base pairs and block DNA and RNA synthesis; generation of free radicals; inhibit topoisomerase II

CCNS

Other: daunorubicin, idarubicin
What are doxorubicin, daunorubicin, and idarubicin used for?

SE, and what may protect against one of the major SE?
Doxorubicin: solid tumors (breast, ovary, etc), hematologic malignancies (leukemia, lymphoma, myeloma).

Daunorubicin: acute leukemias

Idarubicin: AML

Cardiac toxicity (dexrazoxane can help reduce free radical formation in the myocardial cells by acting as a iron-chelator ), myelosuppresion
What is the MOA of bleomycin? What type of drug? Its use, and SE?
Generates free radicals that bind to DNA to cause breaks and inhibit DNA synthesis.

CCS: G2

Testicular cancer, squamous cell carcinomas, and Hodgkin lymphoma.

Pulmonary fibrosis, allergic reactions. Myelosuppression is RARE. Bleomycin has long toxicity.
What is mitomycin mainly used for?
Hypoxic tumor cells.
What is a tyrosine kinase inhibitor, what does it work on, and what is it used for?

SE?
Imatinib, which have activity against the protein product bcr-abl on the Philadelphia chromosome for CML

Also, GI stromal tumors that express c-kit tyrosine kinase.

Fluid retention causing edema, CHF
What drug acts as a monoclonal AB and its purpose?

SE?
Trastuzumab, recognizes breast cancer cells that overexpress the HER-2/neu receptor for epidermal growth factor.

Cardiotoxicity.
What are some epidermal growth factor receptors (EGFR) inhibitors?
EGFR is involved in cellular proliferation, invasion, metastasis, and angiogenesis

Cetuximab: metastatic colon cancer and combination with radiation for head and neck cancer.

Panitumumab: refractory metastatic colorectal cancer.

Gefitinib and erlotinib: 2nd line for non-small cell lung cancner, and erlotinib for advanced pancreatic cancer.
What monoclonal AB binds to vascular endothelial growth factor (VEGF)?
VEGF plays a role in angiogenesis required for tumor metastasis.

Bevacizumab: colorectal, breast, non-small cell lung, and renal cancer.

Arterial thromboembolic events, GI perforations, wound healing complications, proteinuria.
What interferon is especially effective against neoplasms, such as hairy cell leukemia, chronic myelogenous leukemia, and T-cell lymphomas?

What is rituximab and asparaginase used for?

SE of asparaginase?
Interferon alpha.

Rituximab: non-Hodgkin's lymphoma

Asparaginase: depletes serum asparagine; used for treatment of T-cell auxotrophic cancers (leukemia and lymphomas)

Pancreatitis
What is MOA for tamoxifen and raloxifene, its purpose, and SE?
Tamoxifen: estrogen receptor antagonist for breast cancer and prevents osteoporosis by being an agonist in bone.

Raloxifene: mix estrogen agonist/antagonist. Treats osteoporosis and reduce risk of breast cancer. Does NOT increase PT's risk for endometrial cancer.

SE: endometrial cancer (with tamoxifen--partial agonist here), thromboembolism, hot flashes, vaginal bleeding.
What drugs be used in prostatic carcinoma?
Flutamide, an androgen receptor antagonist.

GnRH agonist: leuprolide, goserelin, and nafarelin.
What are anastrozole and letrozole used for?
Inhibit aromatase, enzyme used to convert androstenedione to estrone.

Used for advanced breast cancer.
MOA of hydroxyurea
Inhibitor of the enzyme ribonucleotide reductase, which converts ribonucleotides to deoxyribonucleotides for DNA synthesis
What is a treat for sick cell anemia that is a DNA inhibitor? And why?
Hydroxyurea

Increases HbF (reason, unknown), anti-inflammatory effect by decrease WBC production