Hem & Onc - Pharm (Individual Cancer Drugs & Common Chemotoxicities) Flashcards

Pg. 405-407 in First Aid 2014 or Pg. 373-375 in First Aid 2013 Sections include: -Cisplastin, carboplatin -Etoposide, teniposide -Irinotecan, topotecan -Hydroxyurea -Prednisone, prednisolone -Tamoxifen, raloxifene -Trastuzumab (Herceptin) -Imatinib (Gleevec) -Rituximab -Vemurafenib -Bevacizumab -Common chemotoxicities

1
Q

What drug has the same mechanism of Cisplatin? What is their mechanism?

A

Carboplatin; Cross-link DNA

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2
Q

For what cancers are cisplatin and/or carboplatin used clinically?

A

(1) Testicular (2) Bladder (3) Ovary (4) Lung (carcinomas)

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3
Q

What are the toxicities associated with Cisplatin/carboplatin?

A

(1) Nephrotoxicity (2) Acoustic nerve damage

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4
Q

What prevents the nephrotoxicity effect of cisplatin/carboplatin?

A

Amifostine (free radical scavenger) & chloride diuresis

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5
Q

What drug has the same mechanism as Etoposide? What is their mechanism?

A

Teniposide; Inhibit topoisomerase II –> decreased DNA degradation; Think: “ eTOPOside inhibits TOPOisomerase II”

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6
Q

For what 3 major cancers are etoposide and/or teniposide used clinically?

A

(1) Solid tumors (particularly testicular and small cell lung cancer) (2) Leukemias (3) Lymphomas

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7
Q

What are the toxicities associated with etoposide/teniposide?

A

(1) Myelosuppression (2) GI irritation (3) Alopecia

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8
Q

What is the mechanism of hydroxyurea?

A

Inhibits nucleotide reductase –> decreased DNA synthesis (S-phase specific)

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9
Q

For what is hydroxyurea used clinically?

A

(1) Melanoma (2) CML (3) Sickle cell disease (increase HbF)

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10
Q

What are the toxicities associated with hydroxyurea?

A

(1) Bone marrow suppression (2) GI upset

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11
Q

What is the name of another drug that functions similarly to Prednisone? What is their proposed mechanism?

A

Prednisolone; May trigger apoptosis, may even work on nondividing cells

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12
Q

For what are prednisone and/or prednisolone used clinically?

A

(1) Most commonly used glucocorticoid in cancer chemotherapy - Used in CLL, non-Hodgkin’s lymphomas (part of combination chemotherapy regimen) (2) Immunosuppressant (e.g., autoimmune diseases)

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13
Q

What are the toxicities associated with prednisolone and/or prednisone?

A

Cushing-like symtoms: weight gain, central obesity, muscle breakdown, cataracts, acne, osteoporosis, hypertension, peptic ulcers, hyperglycemia, psychosis

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14
Q

What is a drug that shares the same mechanism as Tamoxifen? What is their mechanism?

A

Raloxifene; SERMs - receptor antagonists in breast and agonists in bone. Block binding of estrogen to estrogen receptor-positive cells

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15
Q

For what are Tamoxifen and/or Raloxifene used clinically?

A

(1) Breast cancer treatment (tamoxifen only) and prevention (2) Raloxifene also useful to prevent osteoporosis

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16
Q

What are the toxicities associated with Tamoxifen versus Raloxifene?

A

TAMOXIFEN - partial agonist in endometrium, which increases risk of endometrial cancer; “hot flashes”; RALOXIFENE - no increase in endometrial carcinoma because it is an endometrial antagonist

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17
Q

What is the brand name of Trastuzumab? What is its mechanism?

A

Herceptin; Monoclonal antibody against HER-2 (c-erbB2), a tyrosine kinase. Helps kill breast cancer cells that overexpress HER-2, through inhibition of HER2-initiated cellular signaling and antibody-dependent cytotoxicity

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18
Q

For what is Trastuzumab (Herceptin) used clinically?

A

HER 2-positive breast cancer and gastric cancer; Think: “her-2 tras2zumab”

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19
Q

What is the toxicity associated with Trastuzumab (Herceptin)?

A

Cardiotoxicity; Think: “HEARTceptin damages the HEART”

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20
Q

What is the brand name for Imatinib? What is its mechanism?

A

Gleevec; Tyrosine kinase inhibitor of bcr-abl (Philadelphia chromosome fusion gene in CML) and c-Kit (common in GI stromal tumors)

21
Q

For what is Imatinib (Gleevec) used clinically?

A

(1) CML (2) GI stromal tumors

22
Q

What is the toxicity/side effect associated with Imatinib (Gleevec)?

A

Fluid retention

23
Q

What is the mechanism of Rituximab?

A

Monoclonal antibody against CD20, which is found on most B-cell neoplasms

24
Q

What are 3 conditions for which Rituximab is clinically used?

A

(1) Non-Hodgkin’s lymphoma (2) Rheumatoid arthritis (with methotrexate) (3) ITP

25
Q

What drugs are used in combination for rheumatoid arthritis?

A

Methotrexate & Rituximab

26
Q

What is the mechanism of Vemurafenib?

A

Small molecule inhibitor of forms of B-Raf kinase with V600E mutation

27
Q

For what is Vemurfenib used clinically?

A

Metastatic melanoma

28
Q

What is the mechanism of Bevacizumab?

A

Monoclonal antibody against VEGF = inhibits angiogenesis

29
Q

For what is Bevacizumab used clinically?

A

Solid tumors (colorectal cancer, renal cell carcinoma)

30
Q

Draw the “chemo-tox man,” labeling common chemotoxicities and the drugs associated with each of them.

A

See pg. 375 in First Aid for drawing

31
Q

What drug(s) commonly cause(s) acoustic nerve damage? What other toxicity does/do it/they cause?

A

Cisplatin/Carboplatin; Nephrotoxicity

32
Q

What drug(s) commonly cause(s) peripheral neuropathy?

A

Vincristine

33
Q

What drug(s) commonly cause(s) pulmonary fibrosis?

A

Bleomycin & Busulfan

34
Q

What drug(s) commonly cause(s) cardiotoxicity?

A

Doxorubicin & Trastuzumab

35
Q

What drug(s) commonly cause(s) nephrotoxicity? What other toxicity does/do it/they cause?

A

Cisplatin/Carboplatin; Acoustic nerve damage

36
Q

What drug(s) commonly cause(s) hemorrhagic cystitis?

A

Cyclophosphamide

37
Q

What drug(s) commonly cause(s) myelosuppression?

A

5-FU, 5-MP, & Methotrexate

38
Q

What toxicity(-ies) do cisplatin/carboplatin commonly cause?

A

(1) Acoustic nerve damage (2) Nephrotoxicity

39
Q

What toxicity(-ies) does vincristine commonly cause?

A

Peripheral neuropathy

40
Q

What toxicity(-ies) do bleomycin & busulfan commonly cause?

A

Pulmonary fibrosis

41
Q

What toxicity(-ies) do doxorubicin & trastuzumab commonly cause?

A

Cardiotoxicity

42
Q

What toxicity(-ies) does cyclophosphamide commonly cause?

A

Hemorrhagic cystitis

43
Q

What toxicity(-ies) do 5-FU and 6-MP commonly cause? What other drug commonly causes this as well?

A

Myelosuppression; Methotrexate

44
Q

What is the mechanism of Irinotecan? What is another drug that shares this mechanism?

A

Inhibit topoisomerase I and prevent DNA unwinding and replication

45
Q

What is the clinical use for Irinotecan?

A

Colon cancer (irinotecan)

46
Q

What are 2 clinical uses for Topotecan?

A

Ovarian and small cell lung cancers (topotecam)

47
Q

What 2 toxicities are associated with Irinotecan and Topotecan?

A

(1) Severe myelosuppression (2) Diarrhea

48
Q

What is the toxicity associated with Rituximab?

A

Increased risk of progressive multifocal leukoencephalopathy

49
Q

What toxicity(-ies) is (are) associated with Bevacizumab?

A

Hemorrhage and impaired wound healing