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CMBM Exam 5 > Antineoplastic Drugs > Flashcards

Antineoplastic Drugs Flashcards

1
Q

Drug Resistance

A
  • Decreased permeation/increased drug efflux via P-glycoprotein transporter (e.g., methotrexate and vincristine)
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2
Q

The Alkylating Agents

A
  • AKA Nitrogen Mustards (CCNS agents)
  • Mechlorethamine
  • Cyclophosphamide
  • Chlorambucil
  • Busulfan
  • Carmustine
  • Cisplatin
  • Oxaliplatin
  • Carboplatin
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3
Q

Nitrogen Mustards (CCNS agents)

A
  • Alkylating Drugs
  • Mechlorethamine
  • Cyclophosphamide
  • Chlorambucil
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4
Q

Nitrogen Mustards MOA

A
  • Alkylate DNA; inhibit cell division
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5
Q

Nitrogen Mustards Cancer Cell Resistance

A
  • Increased DNA repair
  • Decreased drug permeability
  • Increased glutathione S-transferase activity (i.e., augments conjugation of alkylating agent)
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6
Q

Nitrogen Mustards Clinical Uses

A
  • Hodgkin’s and non-Hodgkin’s lymphoma (NHL)
  • Ovarian cancers and solid tumors in children
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7
Q

Cyclophosphamide Toxicity

A
  • Nitrogen Mustard
  • Acrolein (cytotoxic metabolite)- hemorrhagic cystitis; blood in the urine- can ultimately lead to kidney failure
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8
Q

Alkyl Sulfonates

A
  • Alkylating Drugs
  • Busulfan
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9
Q

Alkyl Sulfonates Clinical Uses

A
  • Busulfan
  • Chronic myeloid leukemia (CML)

*can treat but bone marrow transplant the only cure

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10
Q

Alkyl Sulfonates MOA

A
  • Alkylate DNA; inhibit cell division
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11
Q

Busulfan Adverse Effects

A
  • Sulfonate alkylator
  • Decreases mainly granulocytes; pulmonary fibrosis, skin pigmentation
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12
Q

Nitrosoureas (CCNS agents)

A
  • Alkylating Agents
  • Carmustine
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13
Q

Nitrosoureas (CCNS agents) Clinical Uses

A
  • Carmustine
  • Hodgkin’s and NHL, brain cancer
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14
Q

Nitrosoureas MOA

A
  • Carmustine
  • Alkylate DNA (guanine)- inhibit cell division
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15
Q

Metal Salt (CCNS agents)

A
  • Alkylating Drugs
  • Cisplatin
  • Oxaliplatin
  • Carboplatin
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16
Q

Metal Salts Clinical Uses

A
  • Wide use solid tumors; lung/testicular/ovarian/breast
  • Oxaliplatin- colorectal and pancreatic cancer
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17
Q

Metal Salts MOA

A
  • Intra strand cross-linking of double-stranded DNA
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18
Q

Cisplatin Adverse Effects

A
  • Metal salt; platinum analog
  • Dose-limiting nephrotoxicity (renal tubular damage); use hydration/diuretics (mannitol); amifostine
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19
Q

Cytotoxic Antibiotics

A
  • Anthracyclines (CCNS agents)

*Doxorubicin hydrochloride

*Daunorubicin

*Mitoxantrone

*Idarubicin

  • Bleomycins (CCS agents)

*Bleomycin sulfate

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20
Q

Doxorubicin Clinical Uses

A
  • Cytotoxic antibiotics
  • Widely used lymphomas, leukemias, and many solid tumors (e.g., osteosarcomas, lung/testicular/ovarian/breast cancers), use w/ other anti-cancer agents (e.g., cyclophosphamide, cisplatin and 5-FU).
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21
Q

Doxorubicin MOA

A
  • Cytotoxic antibiotic
  • DNA intercalation, inhibits topoisomerase II, binds Fe DNA to form free radicals to cause DNA strand scissions
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22
Q

Coxorubicin Toxicity

A
  • Cytotoxic antibiotic
  • Causes congestive heart failure (CHF) w/ long-term use (>3wks.), use Fe chelator (Dexrazone) to reduce cardiotoxicity
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23
Q

Bleomycin Sulfate Clinical Uses

A
  • Cytotoxic antibiotic
  • Head/neck, testicular, cervix, esophagus, lung, Hodgkin’s/NHL
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24
Q

Bleomycin Sulfate MOA

A
  • Cytotoxic antibiotic
  • Glycopeptide antibiotic intercalator
  • Binds Fe DNA to form free radicals that cause DNA strand breaks, aka scissions
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25
Q

Common Toxicities of Alkylating and Antibiotic Drugs

A
  • Myelosuppression

*anemia

*infection

*bleeding

  • Nausea, vomiting, GI ulceration and inflammation
  • Skin and mucocutaneous ulceration
  • Alopecia
  • Secondary neoplasia
  • Teratogenic and carcinogenic effects
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26
Q

Antimetabolites

A
  • Folate antagonist (CCS agents)

*methotrexate

  • Purine analogues (CCS agents)

*mercaptopurine

  • Pyrimidine analogues (CCS agents)

*fluorouracil (5-FU)

*cytarabine

*gemcitabine

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27
Q

Methotrexate MOA

A
  • Antimetabolite
  • Dihydrofolate reductase (DHFR) inhibition (i.e., folic acid antagonist)
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28
Q

Methotrexate Drug Resistance

A
  • Antimetabolite
  • Increased P-glycoprotein transporter in cancer cells leads to resistance
  • Decreased drug transport, polyglutamate formation, DHFR affinity and increased DHFR protein, P170 glycoprotein transporter
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29
Q

Methotrexate Clinical Uses

A
  • Antimetabolite
  • Wide use: ALL, NHL, choriocarcinoma, solid tumors; also rheumatoid arthritis, psoriasis, organ transplantation
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30
Q

Mercaptopurine MOA

A
  • Antimetabolite
  • Inhibits DNA synthesis via inhibition of purines (i.e. adenosine and guanine)
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31
Q

Mercaptopurine Clinical Uses

A
  • Childhood acute leukemia
32
Q

Fluorouracil (5-FU) MOA

A
  • Antimetabolite
  • Irreversible inhibition of thymidylate synthase, referred to as “thymineless death” resulting in inhibition of DNA synthesis
33
Q

Fluorouracil Clinical Uses

A
  • Antimetabolite
  • Use for Carcinomas: used mostly in solid tumors of GI (esp. colon), bladder, breast, head and neck, skin (topical application)
34
Q

Cytarabine MOA

A
  • Antimetabolite
  • Competitive inhibitor of DNA polymerase
35
Q

Cytarabine Clinical Uses

A
  • Very active for adult acute myelogenous leukemia (AML)
36
Q

Gemcitabine MOA

A
  • Antimetabolite
  • Inhibits DNA polymerase and DNA repair enzymes
37
Q

Gemcitabine Clinical Uses

A
  • Antimetabolite
  • New analog of cytarabine, less toxicity; an influenze-like syndrome, mild BMS; used pancreatic, ovarian, bladder and lung cancers
38
Q

Plant-Derived Products

A
  • Vinca alkaloids (CCS agents)

*vincristine

*vinblastine

*vinorelbine

  • Topoisomerase I Inhibitors (Camptothecins)

*irinotecan

*topotecan

  • Topoisomerase II Inhibitors (Podophyllotoxins)(CCS agents)

*etoposide

*teniposide

  • Taxanes (CCS agents)

*paclitaxel

39
Q

Vincal alkaloids MOA

A
  • Plant-Derived Products
  • Vincristine, Vinblastine, Vinorelbine
  • Mitotic inhibitors: metaphase arrest
40
Q

Vinca alkaloids toxicity

A
  • Plant-Derived Products
  • Vincristine, Vinblastine, Vinorelbine
  • Meylosuppression (vinblastine)
  • Neurotoxicity (vincristine)
41
Q

Vinca alkaloids Clinical Uses

A
  • ALL, Hodgkin’s/NHL lymphomas, Wilms tumor
42
Q

Etoposide Clinical Uses

A
  • Plant-Derived Product; Topoisomerase II inhibitor
  • Broad spectrum use; and Teniposide primarily used in combination drug regimens for lung (small cell), prostate and testicular carcinoma
43
Q

Paclitaxel Clinical Uses

A
  • Plant-Derived Product; Taxane
  • Advanced breast, ovarian and lung cancer
44
Q

Paclitaxel MOA

A
  • Planter-Derived Product; Taxane
  • Acts in M phase, inc polymerization of mitotic spindle, blocks disassembly
  • Mitotic inhibitor; metaphase arrest
45
Q

Paclitaxel Adverse Effects

A
  • Plant-Derived Product; Taxane
  • Peripheral neuropathy
  • Neutropenia (BMS)
46
Q

Enzymes

A
  • 1-Asparaginase
47
Q

1-Asparaginase MOA

A
  • Enzyme
  • Inhibition of protein synthesis (i.e., cancer cells lack asparagine synthetase)
48
Q

1-Asparaginase Clinical Uses

A
  • Enzyme
  • ALL
49
Q

Hormonal Agents

A
  • Glucocorticoids

*prednisone

*dexamethasone

  • Estrogens/Antiestrogens

*tomoxifen citrate

*aromatase inhibitors: Letrazole, Anastazole

  • Androgens/Antiandrogens

*flutamide: androgen receptor antagonist

  • Luteinizing Hormone- releasing hormone (LH-RH) antagonists

*Leuprolide

50
Q

Prednisone, Dexamethasone Clinical Uses

A
  • Hormonal agents
  • Hodgkin’s, NHL, chronic lymphocytic leukemia (CLL)
51
Q

Prednisone, Dexamethasone MOA

A
  • Hormonal agents
  • Suppress lymphocyte mitosis
52
Q

Tamoxifen citrate MOA

A
  • Hormonal agent; Antiestrogen
  • Estrogen receptor antagonist
53
Q

Estrogen/Antiestrogens Clinical Uses

A
  • Hormonal agents
  • Tamoxifen and aromatase inhibitors (letrazole, anastrozole)
  • Breast Cancer
54
Q

Flutamide MOA

A
  • Hormonal agent; Antiandrogen
  • Androgen receptor antagonist
55
Q

Flutamide Clinical Uses

A
  • Hormonal agent; Antiandrogen
  • Prostate cancer
56
Q

Leuprolide Clinical Uses

A
  • Hormonal agent; Leuteinizing hormone
  • Prostate cancer
57
Q

Dacarbazine, Procarbazine MOA

A
  • Methylation of DNA thereby inhibiting DNA synthesis

*used in a lot of regiments

58
Q

Dacarbazine, Procarbazine Clinical Uses

A
  • Used lymphomas, brain tumors
59
Q

Imatinib MOA

A
  • Inhibits ABL portion of abnormal BCR-ABL tyrosine kinase in CML
  • Mild side effects, allows pats to live relative comfortably for years
60
Q

Nilotinib MOA

A
  • Similar to imatinib but w/ higher potency, also effective in resistance to imatinib; now considered first-line therapy in the chronic phase of CML
61
Q

Monoclonal Antibodies

A
  • Trastuzumab (HERCEPTIN)
  • Bevacizumab (AVASTATIN)
  • Rituximab
  • Tositumomab
  • Alemtuzumab
62
Q

Trastuzumab MOA

A
  • Monoclonal antibody
  • Blocks HER-2 receptor
63
Q

Trastuzumab Clinical Uses

A
  • Used in breast cancer
  • Approved in breast tumors that over express HER 2 (~30% of cases)
64
Q

Bevacizumab MOA

A
  • Monoclonal antibody
  • Binds VEGF
65
Q

Bevacizumab Clinical Uses

A
  • Used in colorectal/lung cancer
66
Q

Oxaliplatin Clinical Uses

A
  • Metal Salt
  • Colorectal, pancreatic cancers/combined w/5-FU and leucovorin (FOLFOX regimen)
67
Q

Oxaliplatin Adverse Effects

A
  • Metal salt
  • BMS, peripheral neuropathy, diarrhea
68
Q

Carboplatin Clinical Uses

A
  • Metal salt
  • Similar used as cisplatin

*less hydration needed

69
Q

Carboplatin Adverse Effects

A
  • Metal salt
  • Similar to cisplatin

*more BMS, less nephrotoxicity

70
Q

Doxorubicin Adverse Effects

A
  • Cytotoxic antibiotic
  • Chronic cumulative dose-dependent cardiomyopathy/irreversible CHF due to Fe mediated free radical generation
71
Q

Dexrazoxane

A
  • Chelates Fe prevents iron-mediated free radical generation, used to reduce cardiotoxicity of doxorubicin
72
Q

Bleomycin Adverse Effects

A
  • Dose-related pulmonary pneumonitits w/ progression to fibrosis (most serious toxic effect)
73
Q

Leucovorin

A
  • “Rescue” (activated folate) administer w/ high dose MTX (weak acid), adm within 24-36 hr; inc. dose if plasma MTX remains elevated; nephrotoxicity/alkalinize urine and hydrate persone to minimize toxicity
74
Q

Methotrexate Adverse Effects

A
  • BMS, GI tract/ulcers, skin, heaptic/pulmonary fibrosis, teratogen
  • Drug interactions; highly plasma protein bound drugs can displace MTX to inc. toxicity
75
Q

5-Fluorouracil (5-FU) Adverse Effects

A
  • Catabolized by dihydropyrimidine dehydrogenase (DPD); 5% of CA patients are deficient leading to increased BMS
76
Q

Docetaxel

A
  • Paclitaxel analog, used in advanced breast/ovarian cancer
  • ADRs: neutropenia, neurotoxicity

CMBM Exam 5 (11 decks)

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