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COM Heme and Lymph Exam 1 > Chemo Pharm > Flashcards

Chemo Pharm Flashcards

1
Q

Cyclophosphamide

A
  1. Alkylating agent (bis-chloroethyl amine)
  2. Aldophosphamide generates cytotoxic metabolites
  3. Adverse effects-hemorrhagic cystitis, need IV hydration during therapy
  4. Uses: NHL, lymphoid malignancies, breast and ovarian cancers, solid pediatric tumors, Burkitts
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2
Q

Mechlorethamine

A
  1. Alkylating agent (bis-chloroethyl amine)
  2. Topical tx for cutaneous T-cell lymphoma
  3. Rarely used today b/c it is so reactive
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3
Q

Melphalan

A
  1. Alkylating agent (bis-chloroethyl amine)
  2. Only given IV
  3. Adverse effects-mostly hematological
  4. Use: multiple myeloma (+ dexamethasone)
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4
Q

Chlorambucil

A
  1. Alkylating agent (bis-chloroethyl amine)
  2. Given orally
  3. Adverse effects-N/V, but well tolerated
  4. Use CLL
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5
Q

Name the 4 bis-chloroethyl amine alkylating agents

A

Cyclophosphamide, mechlorethamine, melphalan, chlorambucil

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6
Q

Carmustine

A
  1. Alkylating agent (nitrosourea)
  2. Alkylates DNA, lipophilic so crosses BBB
  3. Adverse effects-profound myelosuppression
  4. Use: malignant gliomas
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7
Q

Streptozocin

A
  1. Alkylating agent (nitrosourea)
  2. High affinity for cells in islets of Langerhans
  3. Adverse effects-nausea, renal/hepatic toxicity
  4. Uses: Pancreatic islet cell carcinoma, carcinoid tumors
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8
Q

Name the 2 Nitrosourea alkylating agents

A

Carmustine, Streptozocin

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9
Q

Thiotepa

A
  1. Alkylating agent (aziridine)
  2. Crosslinks DNA via hepatic CYPs
  3. Adverse effects-mucosal and CNS toxicity, coma, seizure
  4. Use: transplants for hematological malignancies
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10
Q

Busulfan

A
  1. Alkylating agent (alkylsulfonate)
  2. Alkylates DNA?
  3. Adverse effects-Myelosuppression; Pulmonary fibrosis, GI mucosal damage, hepatic VOD at high dose
  4. Use: CML
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11
Q

Name the aziridine and alkylsulfonate alkylating agents

A

Thiotepa, Busulfan

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12
Q

Procarbazine

A
  1. Alkylating agent (non-classic)
  2. Methylates DNA, produces chromosome breaks
  3. Adverse effects-carcinogenic potential, increased risk secondary cancer, augments sedative effects
  4. Uses: Hodgkin disease, gliomas
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13
Q

Dacarbazine

A
  1. Alkylating agent (non-classic)
  2. Methylating agent
  3. Adverse effects-myelosuppression, severe N/V
  4. Uses: HODGKINS, melanoma, adult sarcoma
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14
Q

Bendamustine

A
  1. Alkylating agent (non-classic)
  2. Crosslinks DNA, inhibits mitotic checkpoints
  3. Adverse effects-myelosuppression, mucositis
  4. Uses: CLL, NHL
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15
Q

Name the 3 non-classic alkylating agents

A

Procarbazine, dacarbazine, bendamustine

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16
Q

Cisplatin

A
  1. Alkylating agent (platinum analog)
  2. Crosslinks DNA, inhibits DNA synthesis/function
  3. Adverse effects-Nephrotoxicity (prevent with hydration and Cl diuresis), Ototoxcity, N/V, neuropathy, anaphylaxis
  4. Uses: Testicular, ovarian, head and neck, cervix, endometrium, lung, rectal and anal carcinomas; childhood neoplasms
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17
Q

Carboplatin

A
  1. Alkylating agent (platinum analog)
  2. Crosslinks DNA, inhibits DNA synthesis/function
  3. Adverse effects-BETTER tolerated than cisplatin, thrombocytopenia, hypersensitivity
  4. Uses: Ovarian cancer, SCLC, alternative to cisplatin
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18
Q

Oxaliplatin

A
  1. Alkylating agent (platinum analog)
  2. Crosslinks DNA, inhibits DNA synthesis/function
  3. Adverse effects-neurotoxicity, possible leukemia and pulmonary fibrosis
  4. Colorectal and gastric cancer
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19
Q

Name the 3 platinum analog alkylating agents

A

Cisplatin, Carboplatin, Oxaliplatin

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20
Q

Methotrexate

A
  1. Antimetabolite (antifolate)
  2. Inhibits THF, interferes with DNA/RNA/proteins
  3. Adverse effects-multiple drug-drug interactions
  4. Uses: breast cancer, head and neck cancer, osteogenic sarcoma, CNS lymphoma, NHL, bladder cancer, choriocarcinoma
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21
Q

Pemetrexed

A
  1. Antimetabolite (antifolate)
  2. Activity in S-phate, inhibits TS
  3. Adverse effects-myelosuppression, rash, mucositis, diarrhea, fatigue, hand-foot syndrome
  4. Uses: mesothelioma, NSCLC
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22
Q

Pralatrexate

A
  1. Antimetabolite (antifolate)
  2. Inhibits DHFR, TS, other enzymes
  3. Adverse effects-myelosuppression, rash, mucositis, diarrhea, fatigue
  4. Use: relapsed or refractory peripheral T-cell lymphoma
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23
Q

Name the 3 antifolate antimetabolites

A

Methotrexate, Pemetrexed, Pralatrexate

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24
Q

5-fluorouracil (5-FU)

A
  1. Antimetabolite (fluoropyrimidine)
  2. Inhibits DNA synthesis, interferes with RNA processing
  3. Adverse effects-myelosuppression, GI toxicity, skin toxicity, neurotoxicity
  4. Uses: most widely used for COLORECTAL cancer, breast cancer, stomach cancer, pancreatic cancer, esophageal cancer, hepatocellular cancer, head and neck cancers, anal cancer
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25
Capecitabine
1. Antimetabolite (fluoropyrimidine) 2. Prodrug that is metabolized to 5-FU 3. Adverse effects-diarrhea, hand foot syndrome, myelosuppresion, N/V, mucositis, alopecia 4. Uses: metastatic breast cancer, metastatic colorectal cancer, part of the XELOX regimen
26
TAS-102
1. Antimetabolite (fluoropyrimidine) 2. Inhibits TS, DNA synthesis, DNA function 3. Adverse effects-Myelosuppression (neutropenia), GI toxicity 4. Use: progressive, refractory colorectal cancer
27
Name the 3 fluoropyrimidine antimetabolites
5-FU, capecitabine, TAS-102
28
Cytarabine
1. Antimetabolite (deoxycytidine) 2. S-phase secific, blocks DNA polymerase A and B 3. Adverse effects-myelosuppression, mucositis, N/V, neurotoxicity 4. Use: hematologic malignancies-AML, NHL
29
Gemcitabine
1. Antimetabolite (deoxycytidine) 2. inhibits ribonucleotide reductase, DNA polymerase A and B 3. Adverse effects-myelosuppression (neutropenia), N/V 4. Uses: Advanced pancreatic cancer, NSCLC, bladder cancer, ovarian cancer, soft tissue sarcoma, NHL
30
Name the 2 deoxycytidine antimetabolites
Cytarabine, Gemcitabine
31
6-mercaptopurine (6-MP)
1. Antimetabolite (purine antagonist) 2. Inhibits purine synthesis 3. Adverse effects-Toxicity with allopurinol 4. Use: Acute leukemia in childhood BALL/TALL
32
6-thioguanine (6-TG)
1. Antimetabolite (purine antagonist) 2. Inhibits purine synthesis 3. Adverse effects-? 4. Use: synergizes with cytarabine in adult acute leukemia
33
Fludarabine
1. Antimetabolite (purine antagonist) 2. Inhibits DNA polymerase A and B 3. Adverse effects-myelosuppression, immunosuppresent (opporutinistic PCP infection) 4. Uses: low grade NHL, CLL
34
Cladribine
1. Antimetabolite (purine antagonist) 2. Directly incorporated into DNA, interferes with DNA polymerase A and B 3. Adverse effects-myelosuppression, immunosuppression 4. Uses: Hairy cell leukemia, CLL, low grade NHL
35
Name the 4 purine antagonist antimetabolites
6-MP, 6-TG, fludarabine, cladribine
36
Vinblastine
1. Natural product (vinca alkaloid) 2. Inhibits microtubule assembly (M phase) 3. Adverse effects-N/V, bone marrow suppression, alopecia, blistering 4. Uses: Hodgkins, NHL, breast cancer, germ cell cancer
37
Vincristine
1. Natural product (vinca alkaloid) 2. Inhibits microtubule assembly in M phase 3. Adverse effects-neurotoxicity, peripheral sensory neuropathy, many others 4. Uses: ALL in children, Hodgkins, NHL, multiple myeloma, pediatric tumors
38
Vinorelbine
1. Natural product (vinca alkaloid) 2. Inhibits microtubule assembly in M phase 3. Adverse effects-N/V, transiently elevated LFTs, neurotoxicity, SIADH 4. Uses: NSCLC, breast cancer, ovarian cancer
39
Name the 3 vinca alkaloid natural products
Vinblastine, Vincristine, Vinorelbine
40
Paclitaxel
1. Natural product (taxane) 2. Binds/stabilizes microtubules, mitotic spindle poison in M phase 3. Adverse effects-N/V, hypotension, arrhythmias, hypersensitivity, myelosuppression, peripheral sensory neuropathy 4. Uses: Ovarian, advanced breast, NSCLC, SCLC, head and neck, esophageal, prostate, bladder cancers, Kaposi's sarcoma
41
Docetaxel
1. Natural product (taxane) 2. Binds/stabilizes microtubules, mitotic spindle poison in M phase 3. Adverse effects-hypersensitivity, neurotoxicity, fluid retention, myelosuppression (neutropenia) 4. Uses: 2nd line tx for advanced breast cancer, NSCLC, main activity in head and neck, SCLC, gastric, ovarian and bladder cancers
42
Carbazitaxel
1. Natural product (taxane) 2. Binds/stabilizes microtubules, mitotic spindle poison in M phase 3. Adverse effects-Myelosuppression, neurotoxicity, allergic reactions 4. Use: multi-drug resistant tumor (poor substrate for P-glycoprotein)
43
Ixabepilone
1. Natural product - NOT a taxane 2. Microtubule inhibitor, dynamic inhibition 3. Adverse effects: myelosuppression, hypersensitivity, neurotoxicity (peripheral sensory neuropathy) 4. Use: Metastatic breast cancer
44
Name the 3 taxanes and 1 microtubule inhibitor natural products
Taxanes: Paclitaxel, Docetaxel, Carbazitaxel | MT inhibitor: Ixabepilone
45
Etoposide
1. Natural product (epipodophyllotoxin) 2. Complexed with topoisomerase II, inhibits DNA synthesis 3. Adverse effects-N/V, hypotension, alopecia, myelosuppression 4. Uses: germ cell cancer, SCLC, NSCLC, Hodgkins, NHL, gastric cancer
46
Topotecan
1. Natural product (camptothecin) 2. Inhibits topoisomerase I, DNA damage 3. Adverse effects myelosuppression (neutropenia), diarrhea 4. Uses: 2nd line tx for advanced ovarian cancer and SCLC
47
Irinotecan
1. Natural product (camptothecin) 2. Inhibits topoisomerase I, DNA damage 3. Adverse effects-myelosuppression, GI toxicity 4. Uses: Metastatic adenocarcinoma of pancreas
48
Name the 1 epipodophyllotoxin and 2 camptothecin natural products
Epipodophyllotoxin - etoposide | Camptothecins - topotecan, irinotecan
49
Doxorubicin
1. Antibiotic (anthracycline) 2. Inhibits topoisomerase II, free radicals 3. Adverse effects-myelosuppression (neutropenia), cardiotoxicity) 4. Uses: Breast, endometrial, ovarian, testicular, thyroid, stomach, bladder, liver lung cancers; hematologic malignancies-ALL, multiple myeloma, Hodgkins, NHL
50
Daunorubicin
1. Antibiotic (anthracycline) 2. Inhibits topoisomerase II, free radicals 3. Adverse effects-myelosuppression (neutropenia), cardiotoxicity 4. Uses: AML
51
Idarubicin
1. Antibiotic (anthracycline) 2. Inhibits topoisomerase II, free radicals 3. Adverse effects-myelosuppression (neutropenia), cardiotoxicity 4. Uses: AML
52
Epirubicin
1. Antibiotic (anthracycline) 2. Inhibits topoisomerase II, free radicals 3. Adverse effects-myelosuppression (neutropenia), cardiotoxicity 4. Uses: early stage breast cancer, metastatic breast cancer, gastroesophageal cancer
53
Mitoxantrone
1. Antibiotic (anthracycline) 2. Binds to DNA to produce strand breakage 3. Adverse effects-myelosuppression (leukopenia), cardiotoxicity, blue discoloration of fingernails sclera urine 4. Uses: advanced prostate cancer, low grade NHL, breast cancer, AML (ped and adult)
54
Dexrazoxane
1. NOT an anthracycline 2. Iron-chelating agent 3. Prevents/reduces anthracycline-induced cardiotoxcitiy
55
Name the 5 anthracycline anti-tumor antibiotics; Also, name the agent used to reduce anthracycline induced cardiotoxicity
Anthracyclines-Doxorubicin, daunorubicin, idarubicin, epirubicin, mitoxantrone Other agent-dexrazoxane
56
Mitomycin
1. Anti-tumor antibiotic 2. Generates an alkylating agent that crosslinks DNA 3. Adverse effects-N/V, myelosuppression, mucositis, anorexia, fatigue 4. Use: SCC of anus
57
Bleomycin
1. Anti-tumor antibiotic 2. DNA and iron binding regions, induces single and double strand breaks following free radical formation 3. Adverse effects-Pulmonary toxicity (pneumonitis w/ cough, dyspnea, crackles), allergic rxn, hypotension, skin toxicity, pulm fibrosis, mucositis, alopecia 4. Use: Hodgkins, NHL, germ cell tumors, head and neck cancer, SCC of skin/cervix/vulva
58
Imantinib
1. Tyrosine kinase inhibitor 2. Inhibits Bcr-Abl, PDGFR, c-kit 3. Adverse effects-N/V, fluid retention w/ edema, dirrhea, myalgias, CHF 4. Uses: CML Ph+, gastrointestinal stromal tumors
59
Dasatinib
1. Tyrosine kinase inhibitor 2. Inhibits Bcr-Abl, c-kit, PDGFR-B 3. Adverse effects-? 4. Uses: CML, Ph+ ALL resistant to imantinib
60
Nilotinib
1. Tyrosine kinase inhibitor 2. Inhibits Bcr-Abl (high affinity), c-kit, PDGFR-B 3. Adverse effects-? 4. Uses: CML (esp w/ resistance and chronic phase)
61
Bosutinib
1. Tyrosine kinase inhibitor 2. Inhibits Bcr-Abl 3. Adverse effects-N/V, diarrhea, fluid retention, myelosuppression, skin rash, hepatotoxicity 4. Use: CML (esp resistant/intolerant to other tx)
62
Ponatinib
1. Tyrosine kinase inhibitor 2. Inhibits Bcr-Abl, mutant Bcr-Abl, many other kinases 3. Adverse effects-? 4. Use: CML (adults-chronic, accelerated, blast phase w/ resistance/intolerance)
63
Name the 5 tyrosine kinase inhibitors
Imatinib, Dosantinib, Milotinib, Bosutinib, Ponantinib
64
Cetuximab
1. EGFR inhibitor 2. monoclonal Ab directed against EGFR 3. Adverse effects-skin rash, hypersentivity, hypomagnesemia (overall well tolerated) 4. Use: metastatic coon cancer (combo w/ irinotecan, oxaliplatin), head and neck cancer (w/ radiation)
65
Panitumumab
1. EGFR inhibitor 2. monoclonal Ab directed against EGFR 3. Adverse effects-rash, hypomagnesemia, less often hypersensitivity rxn 4. Uses: refractory metastatic CRC, used in FOLFOX regimen, 2nd line combo w/ irinotecan
66
Necitumumab
1. EGFR inhibitor 2. monoclonal Ab directed against EGFR 3. Adverse effects-rash, hypomagnesemia, hypersensitivity 4. Uses: Squamous NSCLC (w/ gemcitabine, cisplatin)
67
Erlotinib
1. EGFR inhibitor 2. Small molecule inhibitor of TK domain on EGFR 3. Adverse effects-rash, diarrhea, anorexia, fatigue 4. Uses: 1st line tx metastatic NSCLC, maintenance NSCLC, advanced pancreatic cancer (w/ gemcitabine)
68
Afatinib
1. EGFR inhibitor 2. Small molecule inhibitor of TK domains on EGFR 3. Adverse effects-rash, diarrhea, anorexia, fatigue 4. Use: 1st line tx metastatic NSCLC
69
Osimertinib
1. EGFR inhibitor 2. Small molecule inhibitor 3. Adverse effects-cardiac toxicity (QT prolongation, cardiomyopathy), rash, diarrhea, anorexia, fatigue 4. Use: metastatic EGFR mutatnt NSCLC
70
Bevacizumab
1. VEGF inhibitor 2. Monoclonal Ab targetting all forms VEGF-A 3. Adverse effects-HTN, increased thromboembolic events, delayed wound healing, GI perf, proteinuria 4. Uses: Metastatic CRC (w/ 5-FU, irinotecan, oxaliplatin), 1st line for metastatic CRC with fluoropyrimidines, metastatic NSCLC and breast cancer
71
Ziv-aflibercept
1. VEGF inhibitor 2. Fusion protein w/ EC domains of VEGF receptors 3. Adverse effects-HTN, increased thromboembolic events, delayed wound healing, GI perf, proetinuria 4. Uses: Used in FOLFIRI reginmen for metastatic CRC
72
Ramucirumab
1. VEGF inhibitor 2. IgG1 Ab targeting VEGF-R2 receptor 3. Adverse effects-HTN, increased thromboembolic events, delayed wound healing, GI perf, proteinuria 4. Uses: Advanced gastric or GEJ adenocarcinoma, metastatic NSCLC, metastatic CRC
73
Sorafenib
1. VEGF inhibitor 2. Small molecule inhibitor of RTKs 3. Adverse effects-HTN, bleeding, fatigue, skin rash 4. Use: advance renal cell, hepatocellular cancers
74
Sunitinib
1. VEGF inhibitor 2. Inhibits multiple RTKs 3. Adverse effects-HTN, bleeding, fatigue, CHF risk 4. Use: advanced renal cell cancer, gastrointestinal stromal tumors
75
Pazopanib
1. VEGF inhibitor 2. Small molecule inhibitor of multiple RTKs 3. Adverse effects-HTN, bleeding, fatigue 4. Use: advanced renal cell cancer
76
Name all 1. EGFR inhibitors, 2. VEGF inhibitors
1. Cetuximab, panitumumab, necitumumab, erlotinib, afantanib, osinermitib 2. Bevacizumab, ziv-aflibercept, ramucivumab, sorafemib, sunitifib, pazopanib

COM Heme and Lymph Exam 1 (2 decks)

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