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Pharm > Cancer III > Flashcards

Cancer III Flashcards

1
Q

What do DNA intercalating agents do?

A

Bind DNA through intercalation between specific bases, blocking DNA, RNA or both synthesis; cause DNA strands to break and interfere with cell replication; CCNS

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2
Q

Dactinomycin (Actinomycin D, Cosmegen): Mech, Thera, Important SE’s, SE’s, Misc

A

Class:
Mech: Intercalates G-C base pairs of DNA, interfering with DNA-dependant RNA polymerase; also causes ssDNA breaks
Thera: Pediatric tumors (Wilms’ tumor, rhabdomyosarcoma Ewing’s sarcoma); choriocarcinoma in women
Important side effects: Hematopoietic suppression with pancytopenia
Other side effects: Anorexia, nausea, vomiting

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3
Q

Daunorubicin (Cerubidine)

A

Class: Anthracyclines
Mech: Intercalate between DNA base pairs and donate electrons to O2 to form superoxide; superoxide reacts with itself to form H2O2 –> cleaved in the presence of Fe to form OH radical, which cleaves DNA
Thera: AML
Important SE’s: Irreversible dose-dependent cardiotoxicity; alopecia
Other SE’s: Myelosuppression (neutropenia), stomatitis, GI disturbances
Misc: Dexrazoxane is cardio-protective

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4
Q

Idarubicin (Idamycin)

A

Class: Anthracyclines
Mech: Intercalate between DNA base pairs and donate electrons to O2 to form superoxide; superoxide reacts with itself to form H2O2 –> cleaved in the presence of Fe to form OH radical, which cleaves DNA
Thera: AML
Important SE’s: Irreversible dose-dependent cardiotoxicity; alopecia
Important SE’s: Myelosuppression (neutropenia), stomatitis, GI disturbances
Misc: Dexrazoxane is cardio-protective

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5
Q

Doxorubicin (Adriamicin, Doxil)

A

Class: Anthracyclines
Mech: Intercalate between DNA base pairs and donate electrons to O2 to form superoxide; superoxide reacts with itself to form H2O2 –> cleaved in the presence of Fe to form OH radical, which cleaves DNA
Thera: Sarcomas, breast and lung carcinomas, malignant lymphomas
Important SE’s: Irreversible dose-dependent cardiotoxicity; alopecia
Other SE’s: Myelosuppression (neutropenia), stomatitis, GI disturbances
Misc: Dexrazoxane can be used to prevent cardiotoxic effects

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6
Q

Epirubicin (Ellence)

A

Class: Anthracyclines
Mech: Intercalate between DNA base pairs and donate electrons to O2 to form superoxide; superoxide reacts with itself to form H2O2 –> cleaved in the presence of Fe to form OH radical, which cleaves DNA
Thera: Metastatic breast cancer, gastric cancer
Important SE’s: Irreversible dose-dependent cardiotoxicity; alopecia
Other SE’s: Myelosuppression (neutropenia), stomatitis, GI disturbances
Misc: Dexrazoxane can be used to prevent cardiotoxic effects

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7
Q

Bleomycin (Blenoxane)

A

Mech: Acts in G2 phase of cell cycle. Binds to DNA, producing ss- and dsDNA breaks
Thera: Combination therapy for testicular tumors or Hodgkin’s disease; squamous cell carcinomas and lymphomas
Important SE’s: Pulmonary toxicity (pulmonary fibrosis); cutaneous toxicity (hyperpigmentation, hyperkeratosis, erythema); hyperthermia
Other SE’s: Minimally myelo- and immunosuppressive (often used in combo therapy); headache, nausea, vomiting
Misc: Dexrazoxane can be used to prevent cardiotoxic effects

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8
Q

What are microtubule inhibitors in general?

A

Inhibit mitosis and cause metaphase arrest by interfering with microtubule function (tubulin (de)polymerization); CCS

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9
Q

Vinblastine (Velban)

A

Class: Vinca alkaloids
Mech: Block tubulin polymerization into microtubules
Thera: Metastatic testicular tumors (with bleomycin, cisplatin); component of ABVD used for Hodgkin’s disease
Other SE’s: Myelosuppression, nausea, vomiting

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10
Q

Vincristine (Oncovin)

A

Class: Vinca alkaloids
Mech: Block tubulin polymerization into microtubules
Thera: Childhood ALL (with glucocorticoids); Hodgkin’s and non-Hodgkin’s lymphomas
Important SE’s: Dose-limiting neurotoxicity (peripheral neuropathy)
Other SE’s: Relatively low bone marrow toxicity

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11
Q

Paclitaxel (Taxol, Abraxane)

A

Class: Taxanes
Mech: Block microtubule depolymerization into tubulin
Thera: Metastatic breast, ovarian, lung, and head and neck cancers
Important SE’s: Peripheral neuropathy
Other SE’s: Neutropenia; hypersensitivity reactions

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12
Q

How does Docetazel (Taxotere) compare with Paclitaxel?

A

Thera: Metastatic breast, ovarian, lung, and head and neck cancers; ALSO!! hormone refractory prostate cancer

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13
Q

What do topoisomerase inhibitors do?

A

Prevent the resealing of topo I (ssDNA) and topo II (dsDNA); CCS

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14
Q

Etoposide (Etopophos)

A

Class: Epipodophyllotoxins
Mech: Inhibits topoisomerase II
Thera: Testicular carcinoma, lung cancer, and non-Hodgkin’s lymphoma
Other SE’s: Dose-limiting myelosuppression (neutropenia), oral mucositis

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15
Q

Teniposide (Vumon): how is it different from etoposide?

A

Thera: ALL

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16
Q

Irinotecan (Camptosar)

A

Class: Camptothecin analogs
Mech: Inhibits topoisomerase I
Thera: Advanced colorectal cancer; lung, ovarian, cervical and brain tumors
Other SE’s: Severe neutropenia, severe diarrhea

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17
Q

How does topotecan (hycamtin) differ from irinotecan?

A

Thera: Ovarian and small cell lung cancer

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18
Q

What does hormone therapy attempt to target?

A

Treatment of hormone-dependent neoplasms

19
Q

Prednisone (Meticorten)

A

Class: Glucocorticoids
Mech: Inhibit mitosis in lymphocytes
Thera: ALL; combination for Hodgkin’s, non-Hodkin’s, multiple myeloma, and CLL

20
Q

How is dexamethasone different from prednisone?

A

Thera: Reduces edema in brain and spinal cord tumors with radiation therapy

21
Q

Tamoxifen (Soltamox)

A

Class: Selective estrogen-receptor modulators (SERMs)
Mech: Competes with estradiol for binding to estrogen receptor
Thera: ER-positive breast cancer, or as adjuvant therapy following primary breast tumor excision; prevention of breast cancer in high-risk patients
Important SE’s: Hot flushes, hair loss; increased risk of endometrial cancer; increased risk of thromboembolic events
Other SE’s: Nausea and vomiting

22
Q

Fulvestrant (Faslodex)

A

Class: Selective estrogen-receptor downregulators (SERDs)
Mech: Binds with much higher affinity (>100-fold) to estrogen receptor than tamoxifen, inhibiting dimerization, increasing degradation, and reducing overall ER levels
Thera: Posmenopausal women with ER-positive metastatic breast cancer

23
Q

Aminoglutethamide (Cytadren)

A

Class: Aromatase inhibitors
Mech: Inhibits function of aromatase
Thera: Relatively weak, used against breast cancer
Important SE’s: Significant

24
Q

Anastrozole (Arimidex)

A

Class: Aromatase inhibitors
Mech: Inhibits function of aromatase
Thera: First-line for ER-positive breast cancer in postmenopausal women

25
Q

Letrozole (Femara)

A

Class: Aromatase inhibitors
Mech: Inhibits function of aromatase
Thera: ER-positive breast cancer in postmenopausal women

26
Q

Exemestane (Aromasin)

A

Class: Aromatase inhibitors
Mech: Steroidal inhibitor of aromatase
Thera: ER-positive breast cancer in postmenopausal women

27
Q

Leuprolide (Lupron)

A

Class: GnRH analogs
Mech: Binds GnRH receptor; inhibits release of FSH & LH
Thera: Androgen ablation therapy, along with AR blockers

28
Q

How is goserelin (Zoladex) different relative to leuprolide?

A

IT’S NOT!!!

29
Q

Flutamide (Eulexin)

A

Class: Nonsteroidal androgen-receptor blockers
Mech: Competes with androgen for AR binding
Thera: Androgen ablation therapy, along with GnRH analogs

30
Q

Bicalutamide (Casodex)

A

See flutamide (eulexin)

31
Q

Imatinib (Gleevac): misc

A

Class: Tyrosine Kinase inhibitor
Mech: Inhibits Abl kinase by binding where ATP should go; also inhibits PDGFR and c-kit; metabolized by cytochrome P450
Thera: First line therapy for CML; also, gastrointestinal tumor (GIST)
Important SE’s: Nausea and vomiting, fluid retention, muscle cramps, arthralgia
Other SE’s: Myelosuppression
Misc: Oral (1/day)

32
Q

Gefitinib (Iressa)/ Erlotinib (Tarceva)

A

Class: Tyrosine Kinase inhibitor
Mech: Inhibit epidermal growth factor receptor (EGFR) tyrosine kinase
Thera: Non-small lung cancer

33
Q

Nilotinib (Tasigna)

A 
Class: Tyrosine Kinase inhibitor
Mech: Inhibits Abl kinase
Thera: Imatinib-resistant CML
Important SE's: Myelosuppression
Other SE's: QT prolongation, hepatotoxicity, electrolyte abnormalities
Misc: Oral (2/day)
34
Q

Dasatinib (Sprycel)

A

Class: Tyrosine Kinase inhibitor
Mech: Inhibits Abl & Src kinases
Thera: Imatinib-resistant CML
Important SE’s: Myelosuppression, bleeding, fluid retention, pulmonary arterial hypertension
Other SE’s: Diarrhea, nausea and vomiting, weakness, infections
Misc: Oral (1/day)

35
Q

Rituximab (Rituxan)

A

Class: Monoclonal antibody
Mech: CD20 B-cell antibody that can directly activate apoptosis, activate complement, or activate cell-mediated cytotoxicity (e.g., T cells, NK cells)
Thera: Non-Hodgkin’s lymphomas
Important SE’s: Infusion reactions, tumor lysis syndrome (TLS), severe mucocutaneous reactions, progressive multifocal leukoencephalopathy (PML)
Other SE’s: Skin reactions, irregular heartbeat, muscle or joint pain
Misc: Patients need careful monitoring

36
Q

Trastuzumab (Herceptin)

A

Monoclonal antibody
Mech: Unknown HER2/neu (ErbB2) receptor antibody mechanism (enhanced receptor endocytosis or blocking homo- or heterodimerization)
Thera: HER2/neu-overexpressing metastatic breast cancer
Important SE’s: Hypersentivity reaction; ventricular dysfunction
Misc: Usually combined with taxanes; enhances doxorubicin cardiotoxicity

37
Q

Cetuximab (Erbitux)

A

Class: Monoclonal antibody
Mech: EGFR1 (ErbB1)
Thera: EGFR-positive metastatic colorectal cancer
Important SE’s: Allergic reactions, sudden cardiac death, dermatologic problems, infections, renal failure, electrolyte abnormalities
Other SE’s: Asthenia/malaise, fever, nausea, constipation, interstitial pneumonitis
Misc: Clinical trials, probably combine with cisplatin

38
Q

Ipilimumab (Yervoy)

A

Class: Human monoclonal antibody
Mech: Cytotoxic T-Lymphocyte Antigen 4 inhibitor; stimulates immune system
Thera: Melanoma

39
Q

Hydroxyurea (Hydrea)

A

Mech: Inhibits ribonucleoside diphosphate reductase
Thera: CML (replaced by Imatinib), polycythemia vera, essential thrombocythemia; treatment for sickle cell disease (increases Hb-F)

40
Q

Retinoids

A

Mech: ATRA induces terminal differentiation in malignant immature promyelocytes, which subsequently apoptose
Thera: APL
Important SE’s: “Leukocyte Activation Syndrome” (LAS), an increase in WBCs (fever, weight gain, respiratory distress, serosal effusion, renal failure)
Misc: Combined w/anthracyclines; corticosteroids used to block “LAS”

41
Q

Arsenic Trioxide (Trisenox)

A

Thera: Relapsed APL

42
Q

Thalidomide (Thalomid)

A

Thera: Multiple myeloma and myelodysplastic syndromes

43
Q

Interferons

A

Thera: Hairy-cell leukemia, CML, and AIDS-related Kaposi’s sarcoma

Pharm (23 decks)

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