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Block 3 - Fundamentals and Heme > Anticancer Drugs > Flashcards

Anticancer Drugs Flashcards

(49 cards)

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0
Q

What are three confounding factors making chemotherapy more difficult?

A

Tumor doesn’t idle between doses - it seeks to repopulate, But patient needs time to recover
Tumor not homogenous - cells on surface grow faster, must penetrate
Tumors develop resistance over time - multiple drug resistant pump exports variety of drugs

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1
Q

What does it mean that cell kill with chemotherapy is first order?

A

Fixed percentage of cells can be killed with cancer drug per dose
Also called logarithmic kill

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2
Q

What are anti metabolites? What is their major use?

A

Analogs of purines or pyrimidines or corresponding nucleosides
Many are pro drugs
Inhibit DNA polymerase or cause chain termination
Some inhibit synthesis of bases or nucleosides directly
Major use is leukemia and lymphomas

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3
Q

Fluorouracil (5FU) - mechanism of action

A

Activated to 5-FdUMP which mimics dUMP, the substrate for thymidylate synthase, which synthesizes thymidine nucleotides
Thymidine levels drop and cells in s phase killed
Nucleotides derived can also incorporate into DNA or RNA

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4
Q

Fluorouracil - adverse effects

A

Bone marrow depression

Oral and GI ulcers

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5
Q

Fluorouracil - therapeutic uses

A

Pancreatic cancer and other adenomas

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6
Q

Cytarabine - mechanism of action

A

Cytosine analog
Converted to triphosphate, incorporates into DNA, and inhibits chain elongation
Cells exposed in s phase die - block between g1 and s

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7
Q

Cytarabine - therapeutic uses

A

Single most important agent for AML

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8
Q

Methotrexate - mechanism of action

A

Analog of folic acid
Binds to mammalian DHFR and inhibits it - depletes building blocks for DNA and RNA synthesis and buildup of toxic product
Cells in s phase most sensitive

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9
Q

Methotrexate with leucovorin

A

Normal cells exposed to high dose methotrexate can be rescued by leucovorin if given within 36 hrs - a folate coenzyme

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10
Q

Methotrexate - adverse effects

A

Myelosuppression and GI ulceration

*Pneumonitis

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11
Q

Methotrexate - therapeutic uses

A

Leukemias
Choriocarcinoma and other neoplasms
Anti inflammatory

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12
Q

Methotrexate - resistance

A

Caused by amplification of DHFR gene

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13
Q

DNA alkylating agents - mechanism of action

A

Contain chemical groups that can cyclize to generate positively charged reactive intermediates that can be attacked by lone pair of electrons on nitrogen or oxygen
Result is alkylation of DNA and cross linking of strands
Toxic - don’t discriminate between cancer and normal cells
Phase nonspecific but cells don’t die until they enter s phase

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14
Q

Cyclophosphamide

A

Alkylating agent - nitrogen mustard
Oral and inactive until pass through liver and activated by p450 oxidase - easier to administer and less toxic
*Can irritate bladder causing hemorrhagic cystitis - avoid dehydration

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15
Q

Alkylating agents - adverse effects

A

Bone marrow suppression

GI ulcers

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16
Q

Alkylating agents - therapeutic uses

A

Leukemias and solid tumors

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17
Q

Cisplatin - mechanism of action

A

Platinum complex alkylating agents
Bifunctional - react with guanines on same or different DNA strands
Water replaces chlorides creating carbonium ions that are attacked by N7 of guanine bases

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18
Q

Cisplatin - adverse effects

A

Ototoxicity and peripheral neuropathy
*Renal toxicity if dehydrated
Nausea and vomiting
Myelosuppressive

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19
Q

Cisplatin - therapeutic uses

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A

Solid tumors - particularly testicular and ovarian

20
Q

Mechlorethamine

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A

Nitrogen mustard alkylating agent

21
Q

Anthracyclines - mechanism of action

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A

Antibiotics produces by a fungus
Tetracycline ring that can intercalate into DNA
Can be reduced within cells generating semiquinones that autoxidize and generate reactive oxygen radicals
Cause DNA strand breaks by radical damage or interfering with topoisomerase type II

22
Q

Anthracyclines (doxorubicin) - adverse effects

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A

*Unique cardiomyopathy - usually irreversible, happens with cumulative overdose
Dose dependent

23
Q

Doxorubicin

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A

Anthracycline

Major use in carcinomas of breast, ovary, uterus, testicle, and lung, and for many sarcomas

24
Bleomycin - mechanism of action
Chelates iron and copper and binds to DNA Leads to toxic radicals that cause strand breaks and chromosomal aberrations Concentrates in late s and g2 - g2 specific agent
25
Bleomycin - adverse effects
Not toxic to bone marrow *Pulmonary fibrosis Various skin conditions inc hyper pigmentation and ulcers
26
Bleomycin - therapeutic uses
Effective against germ cell tumors of testes and ovary and for squamous cell carcinomas
27
Irinotecan - mechanism of action
A camptothecin Bind and inhibit topoisomerase I Results in first single stranded DNA breaks then double strand during s phase when DNA polymerase collides with drug enzyme complex S phase specific Metabolized to SN-38 - elim by glucoronidation by UGT1A1
28
Irinotecan - side effects
Nausea Leukopenia Patients with less active UGT1A1 more susceptible
29
Irinotecan - uses
Several solid tumors, particularly ovarian, lung, breast, and colorectal cancer
30
Etoposide
Epipodophyllotoxin Bind and inhibits topoisomerase II leading to DNA breaks Useful against leukemias and lymphomas
31
Vinca alkaloids (vincristine, vinblastine)
Bind tubulin alpha beta dimers and prevent formation of MTs M phase specific Myelosuppressive and neurotoxic *peripheral neuropathy
32
Where is vincristine used vs. vinblastine?
Vincristine - childhood leukemias and lymphomas | Vinblastine - testicular cancer and other solid tumors
33
Paclitaxel
A taxane Bind to existing MTs and inhibits disassembly which inhibits mitosis Effective for breast and ovarian cancers
34
Prednisone
Glucocorticoid Great for leukemias Better response in children Resistance quickly unless other drugs used together
35
Tamoxifen
Selective estrogen receptor modulator - binds competitively Treatment of breast cancer - only tumors with this receptor respond Prophylactic treatment in women at high risk Better response in post menopausal women w/ lower estrogen Hot flashes often accompany first use
36
Anastrozole
Nonsteroidal reversible inhibitor of aromatase Aromatase catalyzes conversion to estrogen in peripheral tissues in post menopausal women Useful for estrogen sensitive breast tumors
37
Flutamide
Anti androgen Treatment for prostate cancer Combo with GnRH agonist to cause chemical castration
38
Leuprolide
GnRH agonist Cause transient release of FSH and LH followed by feedback inhibition to cease testosterone production Treatment of prostate cancer Combo with flutamide to block effect of initial FSH/LH surge
39
Bevacizumab
Monoclonal antibody that binds to and inhibits VEGF Colorectal, breast, and lung cancer (but not breast anymore) Side effects are increased bleeding and slow wound healing
40
What type of cancer has interleukin-2 been approved for?
Malignant metastatic melanoma | Appears active for other tumors and leukemias
41
Bortezomib
Inhibits proteosome | I-kappaB degradation allows NF-kappaB to migrate to nucleus and activate genes but this degradation doesn't happen now
42
Tretinoin (ATRA)
Binds to RAR and displaces transcription inhibitor to promote differentiation Treats APL ATRA syndrome - pulmonary infiltration causing inflammation and *respiratory distress, can be prevented by adding glucocorticoids
43
Thalidomide
Role in inhibiting angiogenesis and stimulating immune system Imp in treatment of multiple myeloma Blocking of TNF and VEGF pathways and prevents production of il-6 which normally promotes adhesion of tumor cells to bone marrow stroma
44
How are colony stimulating factors used in the treatment of cancer?
Increase number of normal blood cells | Epo, granulocytes colony stimulating factor and granulocytes-macrophage colony stimulating factor all available
45
What is one combination of drugs given commonly but limited in dose due to overlapping toxicities?
Cyclophosphamide and doxorubicin
46
What is the primary treatment for brain metastases and why?
Radiation | Most chemotherapy doesn't cross BBB
47
What is dose dense treatment?
Admin of same doses and number of cycles of chemotherapy but over shorter time Combine with growth factor support to maintain blood counts at acceptable range
48
What is one drug that is synergistic with irinotecan?
5-fluorouracil

Block 3 - Fundamentals and Heme (8 decks)

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