Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

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)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

The Alkylating Agents

A
  • AKA Nitrogen Mustards (CCNS agents)
  • Mechlorethamine
  • Cyclophosphamide
  • Chlorambucil
  • Busulfan
  • Carmustine
  • Cisplatin
  • Oxaliplatin
  • Carboplatin
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Nitrogen Mustards (CCNS agents)

A
  • Alkylating Drugs
  • Mechlorethamine
  • Cyclophosphamide
  • Chlorambucil
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Nitrogen Mustards MOA

A
  • Alkylate DNA; inhibit cell division
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Nitrogen Mustards Clinical Uses

A
  • Hodgkin’s and non-Hodgkin’s lymphoma (NHL)
  • Ovarian cancers and solid tumors in children
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Cyclophosphamide Toxicity

A
  • Nitrogen Mustard
  • Acrolein (cytotoxic metabolite)- hemorrhagic cystitis; blood in the urine- can ultimately lead to kidney failure
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Alkyl Sulfonates

A
  • Alkylating Drugs
  • Busulfan
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Alkyl Sulfonates Clinical Uses

A
  • Busulfan
  • Chronic myeloid leukemia (CML)

*can treat but bone marrow transplant the only cure

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Alkyl Sulfonates MOA

A
  • Alkylate DNA; inhibit cell division
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Busulfan Adverse Effects

A
  • Sulfonate alkylator
  • Decreases mainly granulocytes; pulmonary fibrosis, skin pigmentation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Nitrosoureas (CCNS agents)

A
  • Alkylating Agents
  • Carmustine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Nitrosoureas (CCNS agents) Clinical Uses

A
  • Carmustine
  • Hodgkin’s and NHL, brain cancer
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Nitrosoureas MOA

A
  • Carmustine
  • Alkylate DNA (guanine)- inhibit cell division
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Metal Salt (CCNS agents)

A
  • Alkylating Drugs
  • Cisplatin
  • Oxaliplatin
  • Carboplatin
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Metal Salts Clinical Uses

A
  • Wide use solid tumors; lung/testicular/ovarian/breast
  • Oxaliplatin- colorectal and pancreatic cancer
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Metal Salts MOA

A
  • Intra strand cross-linking of double-stranded DNA
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Cisplatin Adverse Effects

A
  • Metal salt; platinum analog
  • Dose-limiting nephrotoxicity (renal tubular damage); use hydration/diuretics (mannitol); amifostine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Cytotoxic Antibiotics

A
  • Anthracyclines (CCNS agents)

*Doxorubicin hydrochloride

*Daunorubicin

*Mitoxantrone

*Idarubicin

  • Bleomycins (CCS agents)

*Bleomycin sulfate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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).
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Doxorubicin MOA

A
  • Cytotoxic antibiotic
  • DNA intercalation, inhibits topoisomerase II, binds Fe DNA to form free radicals to cause DNA strand scissions
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Coxorubicin Toxicity

A
  • Cytotoxic antibiotic
  • Causes congestive heart failure (CHF) w/ long-term use (>3wks.), use Fe chelator (Dexrazone) to reduce cardiotoxicity
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Bleomycin Sulfate Clinical Uses

A
  • Cytotoxic antibiotic
  • Head/neck, testicular, cervix, esophagus, lung, Hodgkin’s/NHL
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Common Toxicities of Alkylating and Antibiotic Drugs
- Myelosuppression \*anemia \*infection \*bleeding - Nausea, vomiting, GI ulceration and inflammation - Skin and mucocutaneous ulceration - Alopecia - Secondary neoplasia - Teratogenic and carcinogenic effects
26
Antimetabolites
- Folate antagonist (CCS agents) \*methotrexate - Purine analogues (CCS agents) \*mercaptopurine - Pyrimidine analogues (CCS agents) \*fluorouracil (5-FU) \*cytarabine \*gemcitabine
27
Methotrexate MOA
- Antimetabolite - Dihydrofolate reductase (DHFR) inhibition (i.e., folic acid antagonist)
28
Methotrexate Drug Resistance
- 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
29
Methotrexate Clinical Uses
- Antimetabolite - Wide use: ALL, NHL, choriocarcinoma, solid tumors; also rheumatoid arthritis, psoriasis, organ transplantation
30
Mercaptopurine MOA
- Antimetabolite - Inhibits DNA synthesis via inhibition of purines (i.e. adenosine and guanine)
31
Mercaptopurine Clinical Uses
- Childhood acute leukemia
32
Fluorouracil (5-FU) MOA
- Antimetabolite - Irreversible inhibition of thymidylate synthase, referred to as "thymineless death" resulting in inhibition of DNA synthesis
33
Fluorouracil Clinical Uses
- Antimetabolite - Use for Carcinomas: used mostly in solid tumors of GI (esp. colon), bladder, breast, head and neck, skin (topical application)
34
Cytarabine MOA
- Antimetabolite - Competitive inhibitor of DNA polymerase
35
Cytarabine Clinical Uses
- Very active for adult acute myelogenous leukemia (AML)
36
Gemcitabine MOA
- Antimetabolite - Inhibits DNA polymerase and DNA repair enzymes
37
Gemcitabine Clinical Uses
- Antimetabolite - New analog of cytarabine, less toxicity; an influenze-like syndrome, mild BMS; used **pancreatic**, ovarian, bladder and lung cancers
38
Plant-Derived Products
- 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
Vincal alkaloids MOA
- Plant-Derived Products - Vincristine, Vinblastine, Vinorelbine - Mitotic inhibitors: metaphase arrest
40
Vinca alkaloids toxicity
- Plant-Derived Products - Vincristine, Vinblastine, Vinorelbine - Meylosuppression (vinblastine) - Neurotoxicity (vincristine)
41
Vinca alkaloids Clinical Uses
- ALL, Hodgkin's/NHL lymphomas, Wilms tumor
42
Etoposide Clinical Uses
- 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
Paclitaxel Clinical Uses
- Plant-Derived Product; Taxane - Advanced breast, ovarian and lung cancer
44
Paclitaxel MOA
- Planter-Derived Product; Taxane - Acts in M phase, inc polymerization of mitotic spindle, blocks disassembly - Mitotic inhibitor; metaphase arrest
45
Paclitaxel Adverse Effects
- Plant-Derived Product; Taxane - Peripheral neuropathy - Neutropenia (BMS)
46
Enzymes
- 1-Asparaginase
47
1-Asparaginase MOA
- Enzyme - Inhibition of protein synthesis (i.e., cancer cells lack asparagine synthetase)
48
1-Asparaginase Clinical Uses
- Enzyme - ALL
49
Hormonal Agents
- 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
Prednisone, Dexamethasone Clinical Uses
- Hormonal agents - Hodgkin's, NHL, chronic lymphocytic leukemia (CLL)
51
Prednisone, Dexamethasone MOA
- Hormonal agents - Suppress lymphocyte mitosis
52
Tamoxifen citrate MOA
- Hormonal agent; Antiestrogen - Estrogen receptor antagonist
53
Estrogen/Antiestrogens Clinical Uses
- Hormonal agents - Tamoxifen and aromatase inhibitors (letrazole, anastrozole) - Breast Cancer
54
Flutamide MOA
- Hormonal agent; Antiandrogen - Androgen receptor antagonist
55
Flutamide Clinical Uses
- Hormonal agent; Antiandrogen - Prostate cancer
56
Leuprolide Clinical Uses
- Hormonal agent; Leuteinizing hormone - Prostate cancer
57
Dacarbazine, Procarbazine MOA
- Methylation of DNA thereby inhibiting DNA synthesis \*used in a lot of regiments
58
Dacarbazine, Procarbazine Clinical Uses
- Used lymphomas, brain tumors
59
Imatinib MOA
- Inhibits ABL portion of abnormal BCR-ABL tyrosine kinase in CML - Mild side effects, allows pats to live relative comfortably for years
60
Nilotinib MOA
- 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
Monoclonal Antibodies
- Trastuzumab (HERCEPTIN) - Bevacizumab (AVASTATIN) - Rituximab - Tositumomab - Alemtuzumab
62
Trastuzumab MOA
- Monoclonal antibody - Blocks HER-2 receptor
63
Trastuzumab Clinical Uses
- Used in breast cancer - Approved in breast tumors that over express HER 2 (~30% of cases)
64
Bevacizumab MOA
- Monoclonal antibody - Binds VEGF
65
Bevacizumab Clinical Uses
- Used in colorectal/lung cancer
66
Oxaliplatin Clinical Uses
- Metal Salt - Colorectal, pancreatic cancers/combined w/5-FU and leucovorin (FOLFOX regimen)
67
Oxaliplatin Adverse Effects
- Metal salt - BMS, peripheral neuropathy, diarrhea
68
Carboplatin Clinical Uses
- Metal salt - Similar used as cisplatin \*less hydration needed
69
Carboplatin Adverse Effects
- Metal salt - Similar to cisplatin \*more BMS, less nephrotoxicity
70
Doxorubicin Adverse Effects
- Cytotoxic antibiotic - Chronic cumulative dose-dependent cardiomyopathy/irreversible CHF due to Fe mediated free radical generation
71
Dexrazoxane
- Chelates Fe prevents iron-mediated free radical generation, used to reduce cardiotoxicity of doxorubicin
72
Bleomycin Adverse Effects
- Dose-related pulmonary pneumonitits w/ progression to fibrosis (most serious toxic effect)
73
Leucovorin
- "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
Methotrexate Adverse Effects
- BMS, GI tract/ulcers, skin, heaptic/pulmonary fibrosis, teratogen - Drug interactions; highly plasma protein bound drugs can displace MTX to inc. toxicity
75
5-Fluorouracil (5-FU) Adverse Effects
- Catabolized by dihydropyrimidine dehydrogenase (DPD); 5% of CA patients are deficient leading to increased BMS
76
Docetaxel
- Paclitaxel analog, used in advanced breast/ovarian cancer - ADRs: neutropenia, neurotoxicity

CMBM Exam 5 (11 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions