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40 Cards in this Set

  • Front
  • Back
Induction therapy
- when the tumor is known to be sensitive
- when the feasibility of surgical removal or radiation destruction of the main tumor mass is poor
G1 drugs
- steriod hormones
M drugs
- vinca alkyloids
- paclitaxel
G2 drugs
- bleomycin
- podophyllotoxins
S drugs
- antimetabolites
- podophyllotoxins
CCNS drugs
- alkylating agents
- most antibiotics
Myelosuppression in chemo
- WBC decrease and thrombocytopenia the limiting factors
- G-CSF and GM-CSF being used to accelerate BM
- agents that affect receptors for NT dopamine (D2) and serotinin (5-HT), which trigger N and V
– 5-HT3 receptor antagonists (Ondansetron)
- dopamine D2-receptor antagonists (prochlorperazine, metoclopramide)
most common 2nd malignancy from chemo
Alkylating agents - mechanism
alkylate DNA and cause DNA cross-linking, impairing DNA replication
alkylating agents - toxicity
- myelosuppression, except cisplatin with renal toxicity
- N and V
alkylating agents - resistance
- inc repair, dec perm, inc production of glutathione, an inactivator
- if a tumor is resistant to one alkylating agent, it will also be relatively resistant to others
- alkylating agent
- nigrogen mustard
- a prodrug, requiring activation by hepatic cytochrome P450 oxidase
- alkylating agent
- High lipid solubility facilitates CNS entry
- used for brain tumors
- alkylating agent
- inorganic metal complex
- low myelosuppression with cisplatin, instead, renal toxicity
Antimetabolites - chemistry
- synthetic structural analogs of normal cellular components required for DNA synthesis
- CCS - S phase
Antimetabolites - toxicity
Antimetabolites - resistance
altered target, decrease in activating enzyme, decreased intracellular concentration
- Antimetabolite
- antagonist of folic acid
- blocks DHFR
- Leucovorin “rescue” (folinic acid admin) can overcome enzyme block and overcome some toxicity
- resistance due to dec drug uptake, mutant DHFR, inc DHFR expression
Purine analougs
- Antimetabolite
- 6-MP and 6-TG
- require intracellular conversion by HGPRT to 6-TIMP and dTGTP
- resistance usually decreased HGPRT activity
- antimetabolite
- pyrimidine analoug
- inhibits thymidylate synthase and leads to thymineless death by blocking DNA synthesis
- activated to 5-FdUMP
- antimetabolite
- pyrimidine analoug
- inhibits DNA polymerase and DNA synthesis
- activated to Ara-CTP
Plant Derivatives for chemo
- CCS, inhibition of mitotic spindle function
- cause myelosuppression, except vincristine (peripheral neuropathy)
Vinca alkaloids
- plant alkyloid
- Vinblastine and Vincristine
- CCS (M-phase) bind tubulin
- vincristine causes peripheral neuropathy
- plant alkyoid
- Etoposide
- CCS (S/G2), binds and inhibits topoisomerase II religation, resulting in DNA strand breaks
- plant alkyoid
- Paclitaxel
- bind to tubulin, but promotes polymerization of microtubules
Antibiotics for chemo
- natural compounds isolated from soil fungus streptomyces
- Antibiotic
- effects topoisomerase II
- causes myelosuppression - also irreversible cumulative cardiac toxicity
- Antibiotic
- unlike other antibiotics, CCS (S) , binding to DNA, causing DNA strand breaks by oxygen radical formation
- pulmonary toxicity
- not MDR
hormones and chemo
- sex hormones stimulate the proliferation of certain tissues
- Lack of severe toxicity to normal tissue
- hormone
- binds estrogen receptor in G1
- confined to palliative treatment of estrogen-dependent, estrogen receptor positive breast cancers
Gonadotropin-Releasing Hormone Agonists
- hormones
- Leuprolide and Goserelin are analogs of GnRH
- treatment leads to downreg of receptor and loss of stimulation
- redueces testosterone a lot
- CCS (S-phase) inhibits ribonucleotide reductase
- converts blood asparagine to aspartic acid for Inhibition of protein synthesis
- can casue allergic reaction
Trastuzumab (Herceptin®)
- humanized monoclonal Ab that recognizes HER2
- HER2 overexpression is correlated with poor patient prognosis in breast and ovarian cancers
- mild toxicity
- use for breast cancer
Gefitinib (Iressa®)
- protein tyrosine kinase inhibitor
- Inhibits EGFR/HER1 R TK
- used for lung cancer
- causes rash and diarrhea
- 10% response rate for NSCLC
Erlotnib (Tarveca)
- Inhibits EGFR/HER1 R TK
- used for Lung And Colon Cancers
- causes rash and diarrhea
Cetuximab (Erbitux®)
- humanized monoclonal Ab
- Inhibits EGFR/HER1 R TK
- used Colon Cancers
- causes rash and diarrhea
- a 10.8% response - growth delayed by 1.5 months
– if used w/ irinotecan, 22.9% response and growth delayed by 4.1 months
Imatinib (Gleevec®)
- Inhibition Of The BCR-ABL Tyrosine Kinase on Ph chrom
- used CML and GIST
- Resistance due to mutation of BCR-Abl
Bevacizumab (Avastin®)
- Inhibition of VEGF Receptor Tyrosine Kinase Activation
- used for Tumor Angiogenesis