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Antineoplastics Flashcards

1
Q

Mechlorethamine: (explain/give the following) a. Class b. Mechanism c. Pharmacokinetics d. Therapeutic use e. adverse effects

A

a. Alkylating agent (nitrogen mustard) b. Type I. Bifunctional alkylating agent: produces cross-links in DNA. c. IV. No CNS penetration. Highly reactive. Disappears from blood in seconds to minutes d. Hodgkin’s and non-hodgkin’s lymphoma e. nausea/vomiting, myelosuppression, mild alopecia

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2
Q

Name three alkylating agent antineoplastic drugs

A
  1. mechlorethamine (nitrogen mustard) 2. cyclophosphamide (nitrogen mustard) 3. carmustine (BCNU) (nitrosourea)
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3
Q

Name two vinca alkaloid antineoplastic drugs

A
  1. Vinblastine 2. Vincristine
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4
Q

Name five antimetabolite antineoplastic drugs

A
  1. methotrexate (MTX) 2. 5-fluorouracil (5-FU) 3. cytarabine (Ara-C) 4. mercaptopurine (MCP) 5. hydroxyurea
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5
Q

Name one taxane antineoplastic drug

A
  1. Paclitaxel
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6
Q

Name four antiestrogenic antineoplastic drugs and the sub-class of each

A
  1. temoxifen (TAM) - nonsteroidal antiestrogen 2. letrozole - aromatase (CYP19) inhibitor 3. leuprolide - GnRH analog 4. flutamide - nonsteroidal antiandrogen
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7
Q

Name one corticosteroid antineoplastic drug

A
  1. prednisone
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8
Q

Name one atypical alkylating agent antineoplastic drug

A
  1. procarbazine
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9
Q

Name one metal complex used as an antineoplastic drug

A
  1. cisplatin (platinum coordination complex)
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10
Q

Name one monoclonal antibody used as an antineoplastic drug

A
  1. trastuzumab (Herceptin)
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11
Q

Name two antibiotic agents used as antineoplastic drugs

A
  1. doxorubicin 2. bleomycin (BLM)
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12
Q

Name one epipodphyllotoxin used as an antineoplastic drug

A
  1. etoposide (VP16)
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13
Q

Name one BRM used as an antineoplastic drug

A
  1. filgrastim
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14
Q
A
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15
Q

Mechlorethamine: mechanism of action

A

Type I (nitrogen mustard). Bifunctional alkylating agent: produces cross-links.

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16
Q

Cyclophosphamide: mechanism of action

A

Type III (nitrogen mustard). Prodrug activated in liver by CYP450 → active compound phosphoramide mustard acts as akylating agent. Acrolein (byproduct) causes bladder toxicity

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17
Q

Mechanism of action: carmustine (BCNU)

A

alkylating agent. produces cross-links in DNA

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18
Q

Mechanism of action: Methotrexate

A

antimetabolite:

Binds to DHFR → blocks formation to FH4 → blocks purine and pyrimidine synthesis

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19
Q

Mechanism of action: 5-fluorouracil (5-FU)

A

antimetabolite

Pyrimidine analog → activated to FUTP → inhibits RNA synthesis
Pyrimidine analog → activated to FdUMP → interferes with thymidylate synthase → inhibit DNA synthesis

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20
Q

Mechanism of action: cytarabine (Ara-C)

A

antimetabolite

Pyrimidine (cytadine) analog → competes for phosphorylation of cytidine → also competes with cytidine for incorporation into DNA → causes chain termination

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21
Q

Mechanism of action: mercaptopurine

A

antimetabolite
Purine analog → converted in cells (by HGPRT) to ribonucleotide that inhibits purine synthesis. Further converted and misincorporated into DNA and RNA

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22
Q

Mechanism of action: hydroxyurea

A

antimetabolite

Substituted urea → inhibits ribonucleotide reductase → blocks conversion to dNTPs → prevents DNA synthesis → arrests cell at G1-S interface

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23
Q

Mechanism of action: vinblastine

A

vinca alkaloid

Binds tubulin → prevents formation of microtubules and mitotic spindle

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24
Q

Mechanism of action: vincristine

A

vinca alkaloid

Binds tubulin → prevents formation of microtubules and mitotic spindle

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25
Mechanism of action: paclitaxel
taxane ## Footnote Binds tubulin beta-subunity → enhances assembly and stability of microtubules → arrests cells in late G2 phase (G2/M interface) Can also interfere with DNA repair – intensifying effect of cisplatin or cyclophosphamide
26
Mechanism of action: **doxorubicin**
Antibiotic Antitumor antibiotic (similar to tetracyclines) → intercalates in DNA (distorts helix). Also causes lipid peroxidation and ROS generation. Also binds DNA topoisomerase II → prevents resealing of DNA strand breaks
27
Mechanism of action: **bleomycin (BLM)**
Antibiotic Iron-containing glycopeptide that binds to DNA → causes oxidative-like damage to DNA → DNA strand breaks (single and double)
28
Mechanism of action: **etoposide (VP16)**
Epipodphyllotoxin Irreversible stabilizes DNA-topoisomerase II complexes → results in dsDNA breaks that cannot be repeaired → arrests cell in late G2 phase (G2/M interface)
29
Mechanism of action: **fligrastim (G-CSF)**
BLM Granulocyte colony stimulating factor → promotes neutrophil progenitors → expands absolute population of neutrophils → counteracts the effects of chemotherapy-induced neutropenia
30
Mechanism of action: **trastuzumab (Herceptin)**
Monoclonal antibody Monoclonal antibody → binds HER2 receptor (human epidermal growth factor receptor 2) → blocks proliferation of cells (25-30% of metastatic breast cancers express HER2R
31
32
Mechanism of action: **cisplatin**
Metal complex Platinum coordination complex → hydrolysis yields activated species which cross-links DNA → inhibits transcription, repair, protein recognition → produces apoptosis Also covalently binds thioredoxin reductase (TrxR – overexpressed by many cancers) → directly promotes apoptosis
33
Mechanism of action: **procarbazine**
atypical alkylating agent activated in vivo by liver to methylating agent → chromosomal damage
34
Mechanism of action: **prednisone**
Corticosteroid ## Footnote Bind steroid receptors → modulate cell growth, including: arrest cells at G1, depress growth gene expression, induce nucleases (promote cell lysis)
35
Mechanism of action: **tamoxifen (TAM)**
Antiestrogenic - non-steroidal Nonsteroidal antiestrogen → competitively blocks estrogen receptors in breast tissue. → cells halt at G0/G1 interface. Also elevates sex hormone-binding globulin → decreases free estradiol levels Off-label use: estrogen agonist in bone tissue → may prevent post-menopausal osteoporosis
36
Mechanism of action: **letrozole**
Antiestrogenic Aromatase (CYP19) inhibitor → binds heme domain → blocks conversion of androgens to estrogens → prevents stimulation of ER+ cells
37
Mechanism of action: **leuprolide**
Antiandrogenic GnRH analog → initially stimulates LH and FSH → testosterone surge (and disease flare) → LH/FSH burnout after 2-4 wks → decrease testosterone to castration levels
38
Mechanism of action: **flutamide**
Antiandrogenic Nonsteroidal antiandrogen → blocks androgen receptors
39
Therapeutic use: mechlorethamine
Hodgkin's and non-Hodgkin's lymphoma
40
Therapeutic use: cyclophosphamide
Broad spectrum anti-cancer (most widely used alkylating agent)
41
Therapeutic use: carmustine (BCNU)
Brain tumors multiple myeloma melanoma
42
Therapeutic use: methotrexate
Acute lymphblastic leukemia (ALL) Choriocarcinoma
43
Therapeutic use: 5-fluorouracil (5-FU)
Broad spectrum: stomach, colon, pancreas, overy, head, neck, breast, bladder. Basal cell carcinoma. \*\*GI and breast are most common applications\*\*
44
Therapeutic use: cytarabine (Ara-C)
**Acute leukemias Acute myelocytic leukemia (AML)** Lymphomas Head and neck cancer
45
Therapeutic use: mercaptopurine
Acute leukemias Chronic granulocytic anemia
46
Therapeutic use: hydroxyurea
Granulocytic leukemia
47
Therapeutic use: vinblastine
**Lymphomas Breast cancer** Testicular cancer Bladder cancer
48
Therapeutic use: vincristine
Acute lymphocytic leukemia Lymphomas Wilm's tumor Neuroblastoma
49
Therapeutic use: paclitaxel
Ovarian cancer (with cisplatin) → high TGF-beta tumors
50
Therapeutic use: doxorubicin
``` Wide spectrum (most prescribed in its class) Lymphomas, breast, ovary, small cell lung ```
51
Therapeutic use: bleomycin
**Germ cell tumors of testes and ovaries Head, neck, lung, lymphomas** Skin, esophagus, genitourinary
52
Therapeutic use: etoposide (VP16)
Lymphomas, acute leukemia, small cell lung, testis, Kaposi's sarcoma
53
Therapeutic use: filgrastim (G-CSF)
Lessens risk of infection and restores neutrophil count enough for patients to resume therapies that otherwise suppress bone marrow
54
Therapeutic use: trastuzumab (Herceptin)
Metastatic breast cancer (1st line with paclitaxel) Other HER2-positive cancers
55
Therapeutic use: cisplatin
Wide anti-tumor spectrum Testicular cancer (with etoposide and belomycin) Ovarian cancer (cisplatin + paclitaxel) Head, neck, bladder, small cell lung, colon, esophagus
56
Therapeutic use: procarbazine
Hodgkin's lymphoma
57
Therapeutic use: prednisone
Lymphoma, lymphocytic leukemia Breast cancer Palliative effects: anti-emetic, stimulates appetite, anti-inflammatory
58
Therapeutic use: tamoxifen (TAM)
Advanced post-menopausal breast cancer (adjuvant, in combo with surg/rad/chemo) Pre-menopausal metastatic breast cancer Breast cancer prophylaxis for high-risk populations
59
Therapeutic use: letrozole
Post-menopausal locally-advanced or metastatic breast cancer (1st line treatment)
60
Therapeutic use: leuprolide
Prostate cancer (advanced, hormonally-responsive – 1st line)
61
Therapeutic use: flutamide
Metastatic prostate cancer (used in combination with GnRH agonist or a 2nd line therapy)
62
Which of the alkylating agents has the greatest CNS penetration?
carmustine (BCNU)
63
Adverse effects: alkylating agents
1. Nausea/vomiting 2. myelosuppression 3. alopecia mechlorethamine: 1, 2, mild 3 cyclophosphamide: 1, limited 2, 3. Also bladder toxicity carmustine: 1, delayed 2
64
Which of the alkylating agents has bladder toxicity as a major adverse effect? What is used to counter it?
Cyclophosphamide counteract with: mesna
65
What is leucovorin?
Example of **rescue** leucovorin = folinic acid, does not require DHFR Used following high-dose methotrexate therapy Normal cells have greater capacity to take up leucovorin than tumor cells
66
Side effects: methotrexate
Intestinal epithelial damage (diarrhea, bleeding), bone marrow supporession, renal tubular necrosis (counter: alkalinize urine), displacement of other drugs
67
All antimetabolites are specific for what phase of the cell cycle?
S phase
68
Adverse effects: 5-fluorouracil
(usually delayed): Nausea, anorexia, diarrhea, myelosuppression
69
Adverse effects: cytarabine (Ara-C)
myelosuppression (dose-limiting) Neurotoxicity
70
Adverse effects: mercaptopurine
Bone marrow suppression, vomiting, nausea, anorexia, jaundice TPMT polymorphism related toxicity
71
Adverse effects: hydroxyurea
Hematopoietic depression, GI disturbances
72
Adverse effects: vinblastine
Strong myelosuppression Epithelial ulcerations
73
Adverse effects: vincristine
**Less myelosuppression than vinblastine** Alopecia Neuromuscular abnormalities and peripheral neuropathy Bronchospasm, cramps, nausea/vomiting/diarrhea
74
Adverse effects: paclitaxel
**Leukopenia (dose-limiting) Peripheral neuropathy Myalgia, arthralgia** Hypersensitivity, alopecia, nausea/vomiting, mild cardiotoxicity
75
Adverse effects: doxorubicin
Dilated cardiomyopathy (cumulative) → due to ROS and low GSH peroxidase in heart tissue → reduce effect with detrazoxane (Fe chelating agent) Bone marrow depression Alopecia GI problems
76
Adverse effects: bleomycin (BLM)
Minimal myelosuppression \*\*\*Pulmonary toxicity (cumulative, fatal) → due to low levels of bleomycin hydrolase Skin vesiculation, hyperpigmentation Fever, alopecia
77
Which antineoplastic has the unique adverse effect of **pulmonary toxicity**
bleomycin (BLM)
78
Adverse effects: etoposide (VP16)
leukopenia (dose-limiting), nausea/vomiting/diarrhea, alopecia
79
Adverse effects: filgrastim (G-CSF)
``` Bone pain (33%) Hyperuricemia, leukocytosis ```
80
Adverse effects: trastuzumab (Herceptin)
Cardiomyopathy (reversible) Hypersensitivity (severe) Infusion reactions (fever, chills)
81
Adverse effects: cisplatin
**\*\*Nephrotoxicity (dose-related, lethal)** **Ototoxicity (tinnitus, HF loss)** Peripheral neuropathy Electrolyte disturbances Nause/vomiting (100%) Myelosuppression (mild/moderate)
82
Which antineoplastic drug has the dose-related nephrotoxicity as a major adverse effect?
cisplatin
83
Adverse effects: procarbazine
Myelosuppression, nausea/vomiting Secondary malignancies (prolonged use) Central & peripheral neurotoxicity
84
Adverse effects: prednisone
Immunosuppression Myelosuppression (limited) Weight gain, fluid retention, psychological effects
85
Adverse effects: tamoxifen (TAM)
nausea/vomiting, menopause-like symptoms (hot flashes), fatigue, bone/musculoskeletal pain May increase risk of uterine/endometrial cancer (prolonged use → increases cell growth in these tissues)
86
Adverse effects: letrozole
Hot flashes Nausea Fatigue Bone/musculoskeletal pain Decreased bone mineral density
87
Adverse effects: leuprolide
Disease flare (1st 1-2 wks) Hot flashes Impotence
88
Adverse effects: flutamide
Gynecomastia, impotence Diarrhea Hepatotoxicity (rare)
89
What is the active form of tamoxifen (TAM)?
endoxifen, converted from tamoxifen by CYP2D6 2D6 ultrafast metabolizers experience greater adverse effects
90
Which antineoplastic drugs destabilize microtubles?
Vinca alkaloids: ## Footnote **vinblastine** **vincristine**
91
Which antineoplastic drugs stabilize microtubules?
Taxanes: **paclitaxel** locks cells in the G2/M interface -\> may have some use as a radiosensitizer since cells may be more vulnerable to radiation therapy here
92
Which anti-neoplastic drug has anti-angiogenic properties?
doxorubicin
93
Which drug has major dilated cardiomyopathy as a side effect and state the reason for this specific side effect
Doxorubicin - generates H2O2, which is normally quenched by glutathione peroxidase. Cardiac muscle expresses little of this enzyme and is therefore especially vulnerable. **dexrazoxane** can be used to lessen cardiomyopathy (chelates Fe -\> preventing free radical damage)
94
Which antineoplast requires chelated Fe?
Bleomycin (BLM)
95
What is a BRM?
Biological response modifier - naturally occurring proteins or therapeutic molecules designed to mimic or impact natural proteins example: **filgrastim (G-CSF)**
96
Which enzyme is responsible for the conversion of androgens to estrogens?
aromatase (CYP19)
97
Multi-drug resistance (MDR) to antineoplastic drugs is accomplished primarily by what mechanism? For which classes of drugs is this a prominent problem?
ATP-dependent drug efflux pumps example: p-glycoprotein Especially prominent for: vinca alkaloids, antibiotics, etoposide, taxanes
98
What is **sequential blockade**?
Simultaneous action of two inhibitors acting on different steps of a linear metabolic pathway examples: hydroxyurea + cytarabine methotrexate + 5-FU
99
What is **concurrent inhibition**?
Inhibitors block two separate pathways that lead to the same end product examples: none
100
What is **complementary inhibition**?
One drug affects the function of an end-product, and the other drug affects the synthesis of that end product example: **cytarabine + doxorubicin** cytarabine inhibits DNA synthesis, doxorubicin cause DNA damage
101
What is **rescue**?
Counteract a major toxicity or particular effect on normal cells so that dose or length of treatment may be increased (or continue) examples: methotrexate + leucovorin bone marrow transplant
102
What is **synchronization**?
Synchronize cells so that most are in the same phase. Then use a drug specific to that phase to kill as many tumor cells as possible. example: low-dose 5-FU to block in S-phase, followed by high-dose cytarabine to kill cells in S-phase
103
What is **recruitment**?
Mobilize slowly-proliferating or G0 cells back into the cell cycle so that they are more vulnerable to therapy example: cycle-nonspecific (alkylating agent), following by cycle-specific drug
104
Which antineoplastic drugs are known to have a high risk of secondary malignancy in humans (3)
mechlorethamine carmustine etoposide
105
Killing of tumors follows what order of kinetics?
First-order kinetics (constant dose of drug kills a constant fraction of tumor cells)
106
Define Class I antineoplastic drug
Cell cycle-nonspecific
107
Define Class II antineoplastic drug
Cell cycle-specific, phase-specific
108
Define class III antineoplastic drug
Cycle-specific, phase-nonspecific
109
Which Class II drugs act in: 1. G1 phase 2. S phase 3. G2 phase 4. M phase
1. prednisone 2. cytarabine, fluorouracil, methotrexate, mercaptopurine, hydroxyurea 3. bleomycin, etoposide, paclitaxel 4. vinblastine, vincristine
110
Class II drugs are usually administered how often?
Continuous infusion or frequent small dose
111
Class III drugs are usually administered how often?
single large dose - to take advantage of their sparing effect of normal cells that may be in G0 during treatment
112
113
Define IC90
The dose of an antineoplastic drug that results in 90% reduction in a cell population (1 log kill)
114
2-log kill results in the death of what percentage of a cell population?
99%

FPP_MSS (30 decks)

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