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Cancer Chemotherapy Drugs
Drugs
42
Medical
Graduate
11/15/2012

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Cards

Term
How do cancer cell acquire invasiveness?
Definition
Expression of metalloproteases and tolerance to normal survival factors secreted by neighboring cells
Term
In general, when do you prefer to use a Cell Cycle Specific Chemo drug?
Definition
For hematologic malignancies and solid tumors w/ high growth fraction
Term
In general, when do you prefer to use a Cell Cycle Non-Specific Chemo drug?
Definition
For solid tumors w/ high or low growth fraction
Term
What are 5 general chronic toxicities associated w/ cancer drugs?
Definition
Leukemia, cardiotoxicity (esp w/ anthracyclines), sterility, neuropathy, and nephropathy
Term
MOA for alkylating agents?
Definition
transfer of alkyl group to cellular constituents. Typically at N7 of guanine --> cross linking of DNA --> cytotoxic. Classified as CCNS
Term
How do cells become resistant to alkylating agents and what are some adverse effects?
Definition
increased DNA repair, decrease permeability, and increase glutathione
Standard + mucositis + busulfan causes pulmonary fibrosis and hepatic toxicity.
Term
Cyclophosphamide MOA? Toxic effects? Treatment for effects? Uses?
Definition

Prodrug converted to Acrolein in liver. May cause hemorrhagic cystitis. Treat w/ mesna. SEs - hepatotoxicity. Treats NHL, ovarian, breast, and neuroblastoma

Alkylating agent -> CCNS

Term
Nitrosoureas (carmustine and lomustine)
What class? Special property?
Definition
Alkylating agent.
Lipid soluble and crosses BBB
Term
Procarbazine
Class? adverse effects?
Definition
Alkylating agent.
adverse effects - myelosuppression, pulmonary toxicity, neurotoxicity, leukomogenic, and teratogenic
Term
Platinum Analog MOA? Adverse Effects? Uses? main example?
Definition
CCNS - complexes w/ DNA --> strand links --> cytotoxicity.
Nephrotoxicity, ototoxicity from neurotoxicity.
Uses - solid tumors: testicular, ovarian, bladder, lung.
Cisplatin
Term
Carboplatin
Dose-limiting SE?
other adverse effects?
Uses?
Definition
myelosuppression is Dose limiting
Used for solid tumors: testicular, ovarian, lung, bladder.
Term
General MOA for antimetabolites?
Definition
targets aspects of cellular metabolism that makes them more susceptable to cancer drugs. Thus they generally do not cause acute toxicities.
Term
Methotrexate
MOA?
Resistance mechanism?
Adverse Effects? Rescue from effects with?
Uses?
Definition
CCS antimetabolite
Folic acid analong that prevents DHFR causing block in thymidilate production -> DNA and RNA synthesis block. Does not cross BBB.
Resistant via decreased permiability, increase DHFR, low DHFR affinity for MTX, decreased retention
Adverse Effects - mucositis, myelosuppression, nephrotoxicity. Rescue w/ leucovorin
Uses - Leukemia, lymphoma, breast cancer
Term
6-thiopurines (6-mercaptopurine and 6-thioguanine)
Class? MOA? Adverse Effects?
Definition
purine antagonist antimetabolite
convereted by HGPRT to incorporate into DNA and RNA -> cytotoxicity
SEs - myelosuppression, immunosuppression, hepatotoxicity
Term
Fludarabine and Cladribine
Class? MOA?
Definition
Purine antagonist antimetabolite
both must be phosphoryloated to triphosphate to be active.
Term
5-Fu
Class? MOA?
give with what to potentiate effects?
Adverse Effects?
Uses?
Definition
Pyrimidine antagonist antimetabolite CCS
Prodrug that undergoes series of rxns -> FdUMP preventing synthesis of thymidine
Give w/ leucovorin to potentiate effects by stabilizing the THF, FdUMP, TS complex.
SEs - nausea, diarrhea, mucositis, bone marrow suppression, alopecia
Hand Foot syndrome is dose limiting
Used for breast, ovarian, head and neck cancers
Term
Capecitabine
class? MOA? SEs?
Definition
pyrimidine antagonist antimetabolie CCS
prodrug that eventually is converted to 5-Fu in the tumor cell by thymidilate phosphorylase giving more specificity. then same MOA as 5-Fu. Same SEs as 5-Fu.
Term
Cytarabine
Class?
MOA?
Uses?
Definition
pyrimidine antagonise antimetabolite CCS
S-phase specific effects limiting its use to hematologic malignancies (particularly ALL)
Term
Gemcitabine
class? MOA? Toxicity?
Definition
pyrimidine antagonist antimetabolite CCS
MOA: analog of deoxycytidine that must be phosphorylated to be active
Myelosuppression is dose limiting
Term
Vinblastine, Vincristine, vinorelbine
MOA? adverse affects shared by all three?
Definition
inhibits microtubule formation via binding of B subunit.
SEs - rapid action causes hyperuricemia which may precipitate gout. give allopurinol.
If extravastated --> cellulitis.
Term
Vinblastine side effects? Uses?
Definition
Bone marrow suppression
low neurotoxicity
GI problems.
Hodgkins, NHL, Breast, Testicular
Term
Vincristine
Side Effects?
Uses?
Definition
limited myelosuppression but higher neurotoxic effects.
Less GI effects.
ALL, Hodgkins, Leukemias, Wilms
Term
Vinorelbine
Side effects?
Definition
intermediate myelosuppression
low neurotoxicity
most likely cause granulocytopenia
Term
Paclitaxel and Docetaxel
Class?
Adverse Effects?
Definition
plant alkaloids Taxanes CCS
causes myelosuppression
Cumulative effects causing neurotoxicity.
Hypersensitivity rxn - treat w/ CS and antihistamines beforehand.
Term
Etoposide, and Teniposide
Class?
MOA?
Adverse effects?
Definition
plant alkaloid Epipodophyllotoxin
MOA: inhibits DNA topoisomerase II causing strand breakage. blocking late S-G2 phase
SEs - dose reduction in renal pts.
Term
Topotecan
Class?
MOA?
Adverse Effects?
Definition
plant alkaloid camptothecin
MOA: inhibits topoisomerase I
Reduce dose for renal pts
Term
Irinotecan
Class? MOA? Adverse Effects?
Definition
plant alkaloid camptothecins
Inhibits topoisomerase I
Reduce dose in liver dysfunction pts.
Term

what class does the -rubicin and mitoxantrone drugs fall into? MOA?

Dose limiting Adverse effects?

Adverse effects that are a result of its MOA?

Definition

all drugs ending in rubicin are antitumor antibiotics of the anthracycline class

They inhibit topoisomerase II and generate free radicals.

Myelosuppression is dose limiting. and cardiotoxicity from the free radicals.

Term
MOA and adverse effects for anthracyclines
Definition
inhibition of topoisomerase II leading to DNA strand breakage
SEs - myelosuppression is dose limiting.
Term
Bleomycin
class? MOA? adverse effects?
Definition
antitumor antibiotic that is CCS
MOA: bifunctional molecules that bind DNA w/ one end and chelates Fe2+ with the other end
SEs - pulmonary fibrosis is dose limiting. Mucocutaneous reactoins
Term
Prednisone effect on cancer?
Definition
decreases lymphoid mass and induces remission of ALL
Term
Tamoxifen
class? MOA? Uses?
Definition
Hormonal agen
MOA: competitive partial agonist inhibitor of estrogen
Used in breast cancer
Term
Flutamide and Bicalutamide
Class? MOA?
Definition
Hormonal agent
Antagonist at the androgen receptor (testosterone promotes growth of the prostate)
Term
Leuprolide and goserelin
Class? MOA? Uses?
Definition
GnRH agonist
MOA: initial surge in LH and FSH followed by inhibition of LH and FSH release and inhibition of testosterone release.
Treats prostate cancer.
Term
Anastrozole, letrozole, and exemestane
Class?
Definition
Hormonal agenst that inhibit aromatase and prevents conversion of steroids into androgens
Term
Ways that monoclonal antibodies are used in cancer? 5 ways
Definition
Ab dependent lysis
Complement dependent lysis
Localized delivery of radiation
Localized delivery of chemo
Inhibit angiogenesis.
Term
Bevacizumab (Avastin)
Definition
binds to circulating VEGF and prevents angiogenesis. Used in colon and lung cancer
Term
Rituximab
Definition
Binds to CD20 on B-Cells causing AB dependent or complement dependent lysis. Treats NHL.
Term
Trastuzumab (Herceptin)
Definition
Used to treat breast cancer because it binds to HER-2/Neu and causes Ab dependent lysis.
Term
Imatinib
Class? MOA? Use?
Definition
Tyrosine kinase inhibitor
MOA: inhibits PDGF
Treats CML
Term
name 3 bone marrow sparing agents
Definition
cisplatin, bleomycin and vincristine
Term
What are the general toxicities associated w/ chemo drugs? acute and chronic
Definition
Acute: nausea, vomitting, bone marrow suppression, alopecia, neutropenai and thrombocytopenia
Chronic: Leukemia, Cardiotoxicity (Anthracyclines), sterility, neuropathy, nephropathy
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