Drugs Flashcards
1
Q
Cyclophosphamide
A
- Classical drug
- Alkylating agent
- React covalently with DNA
- Most cross-link strands
- Classical toxicities; hemorrhagic cystitis
- Mustard gas
- Metabolized by CypP450
- Used for solid and hematogenous tumors
2
Q
Folic acid antagonists (methotrexate)
A
- Classical drug
- Antimetabolite
- Purine and pyrimidine inhibitor
- Inhibits DHFR and carbon transfers needed for purine ring synthesis and dTMP synthesis from dUMP
- Classical toxicities
- Renal and liver toxicity
- Myelosuppression
- Lymphomas and leukemias
3
Q
Pyrimidine analogs (fluorouracil)
A
- Classical drug
- Antimetabolites
- Pyrimidine synthesis inhibitor
- Blocks dTMP formation from dUMP
- Classical toxicities
- CNS symptoms (ataxia, confusion)
- Jaundice
- Myelosuppression
- Solid tumors
4
Q
Purine analogs (6-mercaptopurine)
A
- Classical drug
- Antimetabolites
- Purine synthesis inhibitor
- Incorporated into DNA when phosphorylated disrupting structure and function
- Classical toxicities
- Myelosuppression
- Childhood ALL and other leukemias and lymphomas
- toxic when used with allopurinol
5
Q
Vinca alkaloids (vincristine/vinblastine)
A
- Classical drug
- Mitotic inhibitor
- Bind to tubulin to disrupt microtubule formation resulting in metaphase arrest
- Neurotoxicity, bone marrow hypoplasia
- Myelosuppression
- Peripheral neuropathy
- Lymphoma, sarcoma, solid tumors
6
Q
Taxanes (paclitaxel)
A
- Classic drug
- Mitotic inhibitor
- From the bark of yew tree
- Bind to tubulin to disrupt microtubule disassembly resulting in metaphase arrest.
- Myelosuppression
- Peripheral neuropathy
- Cardiac arrhythmia and conduction block
- Breast and ovarian cancers
7
Q
Topoisomerase inhibitors
A
- Classical drug
- Binds to topoisomerase
- Endonuclease activity works but ligase activity does not
- End up with a lot of ds DNA breaks
- Could result in secondary leukemias
8
Q
Cytotoxic antibiotics
A
- Classical drug
- Intercalate between base pairs and inhibit synthesis
- Generate free radicals that break ds DNA
- Cardiotoxicity
9
Q
cisplatin/carboplatin
A
- Classical drug
- Heavy metals
- Cross linking agents
- Used in lung, breast, bladder, GI, ovarian cancers
- Nephrotoxic
- Myelosuppression
- Neuropathy
- ototoxicity
10
Q
Retinoic acid
A
- Classical drug
- Used for APL associated with t(15;17)
- Causes DIC but high levels stimulate broken RAR by releasing corepressors
11
Q
Estrogens, antiestrogens, antiandrogens
A
- New drug
- Hormone therapy
- Treatment of hormone dependent tumors
- Alter transcription to trigger genetic programs allowing differentiation of tumor cells
- Toxicities: immunosuppression, growth alterations, changes in feminization and masculinization, CV disease
12
Q
imatinib/Gleevec
A
- New drug
- Small molecule
- Bcr-Abl TK inhibitor in CML
- Blocks ATP binding site
- Toxicities in GI, Skin, myelosuppression, hepatic, HTN
13
Q
trastuzumab/Herceptin, bevacizumab/Avastin
A
- New drug
- Monoclonal antibodies
- Trastuzumab: RhMAb to EGFR subunit HER-2 in breast cancer and induces apoptosis
- Has cardiotoxicity
-Bevacizumab: RhMAb against VEGFR which reduces vascularization of tumor in colorectal cancer, AMD
14
Q
CAR T cells
A
- New drug
- Immunotherapy
- Antibodies against CTLA4, PD-1, CD47
- Cancer and autoimmune diseases
15
Q
New antineoplastics induce apoptosis by acting as
A
- Signal transduction inhibitors of driver mutations, commonly inhibiting tyrosine or serine/threonine kinases
- Angiogenesis inhibitors
- Antibodies directed against tumor antigens
- CAR T-cells engineered to express tumor antigen receptors
- Antibodies serving as checkpoint inhibitors that sensitize the immune system to tumor neoantigens
