Cancer Drugs - Exam 3 Flashcards

1
Q

Cyclophosphamide
(Cytoxan, Neosar)

Alkylating Agents
Nitrogen mustards
Most widely used
alkylating agent!

A

Mech: Binding to guanine molecules to
prevent separation
of DNA strands
pro drug
Use: not vesicant, admin IV or PO
SE: ACUTE
HEMORRHAGIC
CYSTITIS!!!
Admin w/ Mesna
(Mesnex) and adequate hydration!
-Bone marrow
suppression!
Dose limiting
Notes:

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2
Q

Carmustine
(BiCNU, Gliadel)

Nitrosureas
(Alkylating agent)

A

Mech: Bifunctional alkylating compound
Highly lipophilic
(good crossing BBB)
Use:
SE: Bone marrow
suppression!
Dose limiting
Notes:

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3
Q

Cisplatin
(Platinol-AQ)

Platinum compounds
(-platin)

A

Mech: Forms cross-links
btwn DNA strands
Use: 1st line therapy for
ovarian cancer and
non-small cell lung
cancer

SE: -Kidney damage
(reduced w/
hydration,
diuretic)
-Severe nausea,
Vomiting
-Peripheral
neuropathy
Notes:

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4
Q

Methotrexate
(Rheumatrex, Trexall)

Folic Acid Analogs
Antimetabolites

A

Mech: Inhibits an enzyme
in folic acid activation , cannot synth folic acid!
S Phase specific!
Use: High dose admin to
be effective against
cancer cells!
Leucovorin given to
help protect normal
cells
SE: -Bone marrow
suppression
-Kidney damage
-Fetal
malformation

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5
Q

Cytarabine
(cytosine arabinoside
or Ara-C)

Pyrimidine analogs
(cytosine, uracil, Thymine)

A

Mech: Incorporated into DNA, suppresses further DNA synth
S phase specific!
Use:
SE: Bone marrow suppression!
Pulmonary edema
Liver damage
Kidney damage

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6
Q

Mercaptopurine
(Purinethol)
Prodrug , activated in cells

Purine analogs
(Adenine, Guanine)

A

Mech: Incorporated into DNA, suppresses further DNA synth
S phase specific
Use:
SE: Bone marrow suppression
Mild hepatotoxicity

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7
Q

Etoposide
(Toposar)

Topoisomerase inhibitors

A

Mech: Permits cleaving of the DNA but does not permit
repair! Cell death occurs due to accumulation of DNA with multiple breaks
Use: Protein binding HIGH (will increase serum level of warfarin, SSRI, etc. )
SE: Bone marrow suppression

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8
Q

Doxorubicin
(adriamycin) – conventional

Doxorubicin
(Doxil, Caelyx) – liposomal

Rubicin = red in color! RED DEVIL

Anti-tumor antibiotics Anthrocyclines

A

Mech: Intercalation with DNA, slips btwn base pairs and
distorts structure of DNA
Use: Liposomal assoc w/ infusion reactions but more likely to
just target cancer cells
SE: Infusion reaction with liposomal form!

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9
Q

Dactinomycin
(Actinomycin D)

Non-anthracyclines

A

Mech: Intercalates w/ DNA & distorts structure, inhibits RNA & protein synthesis
SE: Bone marrow suppression

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10
Q

Vincristine

Vinca alkaloids
Mitotic Inhibitors
(Vin-)

A

Mech: Block mitosis during metaphase
Disrupts assembly of microtubules by binding to tubulin
Cell stops in metaphase = apoptosis
Use: ** BONE MARROW SPARRING!!**
SE: Peripheral neuropathy!
Dose-limiting tox!
Disrupts neuro-tubules in neurons!

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11
Q

Vinblastine
(Veblan)

A

Mech: Block mitosis during metaphase
Disrupts assembly of microtubules by binding to tubulin
Cell stops in metaphase = apoptosis
SE: neurotoxicity less common, less severe than vincristine
Bone marrow suppression dose limiting

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12
Q

Paclitaxel
(Abraxane, Taxol)

Taxanes

A

Mech: Promotes formation of microtubule bundles
Inhibits cell division
Promotes apoptosis
SE: Severe hypersensitivity reaction with Taxol!
Pre treat w/ H2 blocker, antihistamine, glucocorticoid
-Bone marrow
suppression may
be dose limiting!

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13
Q

Asparaginase
(Elspar)

A

Mech: Asparaginasae is an enzyme that converts
asparagine into aspartic acid.
Asparagine is an essential amino acid Needed for protein synth!
Use: Limited to Acute Lymphoblastic Leukemia (ALL)
SE: Coagulation deficiencies,
Liver, kidney, pancreas damage

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14
Q

Tamoxifen
(Nolvadex)
Gold standard
for endocrine tx
of breast cancer

Anti-estrogens

A

Mech: Prodrug that is converted into active form by CYP450
Blocks estrogen receptors , deprive tumor cells of growth promoting influence of estrogen
Activates estrogen receptors in bone, liver, uterus
SE: Increased risk of endometrial cancer and thrombosis!
-Menopause like symptoms

Use of CYP450 inhibitors can negate effect of tamoxifen

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15
Q

Anastrozole
(Arimidex)

Aromatase inhibitors

A

Mech: Adrenal androgens converted into estrogen by
Aromatase in peripheral tissues
Use: ER pos breast cancer in POSTMENOPAUSAL WOMEN !!
SE: Musculoskeletal pain
Osteoporosis and fractures

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16
Q

Trastuzumab
(Herceptin)

Anti-Human
Epidermal Growth
Factor Receptor 2
(HER2) Antibodies

(-tuzumab)

A

Mech: Mab that blocks HER2 receptors
- inhibits proliferation
- promotes abx dependent cell death
Use: HER2 pos BC in pre/post menopausal women
SE: Cardio toxicity = arrhythmias & HF
-Flu like
symptoms
(Fatigue, chills,
fever, nausea)
-Potentially fatal
hypersensitivity
reaction

17
Q

Lapatinib
(Tykerb)

Kinase inhibitor

A

Mech: inhibits 2 enzymes involved in cell signal transduction = blocks signal that promotes growth of the tumor
Use: HER2 pos BC ONLY!
SE: Diarrhea, nausea, vomiting, Fatigue

18
Q

Leuprolide
(Eligard, Lupro)

Synthetic analog of GnRH
GnRH agonists

A

Mech: INITIALLY cause release of hormones that stim INCREASED prod of testosterone, flares symptoms and growth. W/ continued exposure, GnRH receptors become desensitized and less testosterone is produced.
Co admin with androgen receptor blocker Flutamide to reduce the flare!
SE: Erectile dysfunction
Reduced libido
Gynecomastia

19
Q

Degarelix
(Firmagon)

GnRH antagonist

A

Mech: Block the GnRH receptors in pituitary
– Reduces production of hormones that stimulate
the testes to produce testosterone
– NO INITIAL FLARE OF PROSTATE CANCER
Use: Used for adv prostate cancer, admin SQ
SE: not enough testosterone = ED, Reduced libido, Gynecomastia

20
Q

Flutamide

Androgen receptor antagonist

A

Mech: blocks androgen receptors
Use: only indicated for prostate cancer, often admin w/ GnRH agonist
SE: Not enough testosterone = ED, reduced libido, Gynecomastia

21
Q

Abiraterone
(Zytiga)

CYP17 inhibitor

A

Mech: inhib of CYP17, an enzyme necessary for androgen synthesis
Use: in combination with prednisone to treat METASTATIC castration-resistant prostate cancer
SE: Not enough testosterone = ED, reduced libido, Gynecomastia, hypokalemia, edema

22
Q

Bevacizumab
(Avastin)

Angiogenesis inhibitors

A

Mech: Monoclonal ab!
Binds to VEGF (compound that stims vessel prolif)
-cannot bind to receptors on vascular endothelium that promote vessel growth
– New vessel growth does not occur
Use: deprive solid tumors of blood supply. CANNOT KILL TUMORS THAT ALREADY EXIST!
SE: GI perforation and/or thromboembolism
**If occurs STOP drug and never use again! **
Hemorrhage in brain, lung, GI, vagina