Pharmacology - Antineoplastic Drugs (Exam 5) Flashcards
MOA of alkylating agents
- Nucleophilic substitution to form a cyclic sulfonium ion
- This very reactive intermediate tends to cause permanent alkylation of the guanine nucleotide in DNA strands
- This can prevent cellular division and lead to programmed cell death (Apoptosis) because of the DNA Damage response (DDR).
MOA of anti-metabolites
inhibits DNA, RNA, protein synthesis
May also interfere with cellular metabolism and inhibit mitosis
MOA of antibiotics
Intercalates with DNA causing topisomerase stalling
MOA of vinca alkaloids
Bind tubulin and prevent microtubule polymerization
How does the mechanism of platinum drugs induce DNA damage?
Covalent binding to DNA -> inhibits DNA replication -> cell cycle gets arrested -> cessation of cancer cell proliferation
How does the mechanism of campothecin drugs induce DNA damage?
Target TOPO I -> interferes with DNA replication -> DNA damage
How does the mechanism of podophyllotoxins induce DNA damage?
Targets TOPO II
The goal of _______________ is to eradicate every viable tumor cell without significantly damaging normal host tissue.
chemotherapy
Cell division requires 2 things. What are they?
1) coordinated microtubules
2) DNA synthesis
Name 2 microtubule modulating agents
taxanes and epothilones
Name one etoposide that works by targeting TOPO II
podophyllotoxin
Mechanism of action of anti-folates
block thymidylate synthesis aka purine synthesis
How does taxane induce cell cycle arrest?
binds tubulin and prevents microtubule depolymerization -> this prevents formation of the mitotic spindle so cells are arrested in the M phase
How does epothilones induce cell cycle arrest?
inhibit microtubule function
A platinum based drug that binds to DNA and inhibits replication
cisplatin
Dental implications of anthracyclins
-soreness of the mouth
-mouth ulcers
-mucositis
Examples of differentiating agents
retinoic acid (there are others but he said focus on this)
Bisphosphonates modulate?
Bone metabolism
Dental implication of bisphosphonates
Osteonecrosis of the jaw (mandible more than maxilla)
T/F: Chemotherapy only acts directly on the DNA of the cell
False! it’s direct OR indirect
Difference b/w chemotherapy and targeted therapy
Chemo: non-specific toxicity (less effective, more side effects)
Targeted: hit tumor specific characteristics (more effective, less toxic)
Name a hormone agonist and antagonist
agonist: prednisone
antagonist: tamoxifen
MOA of hormone agonist (prednisone)
Binds glucocorticoid receptors to suppress inflammation
MOA of hormone antagonist (tamoxifen)
Binds estrogen receptor and blocks its interaction with estrogen