Chemo 3 and 4 Flashcards
What are the 3 classes of antimitotic (spindle poisons) drugs
- Vinca Alkaloids
- Taxanes
What are the 3 Vinca alkaloids
- Vinblastine
- Vincristine
- Vinorelbine
What do vinca alkaloids inhibit
tubulin polymerization which blocks assembly of microtubules
What are the 2 Taxanes
- Taxol (Paclitaxel)
- Taxotere (Docetaxel)
What do Taxanes do
enhance tubulin polymerization to stabilize microtubules
Therapeutic use of Vinblastin
- testicular cancers (with bleomycin and cisplatin)
- lymphomas
- neuroblastoma
therapeutic use of vincristine
- ALL
- lymphoma
- neuroblastoma
- Wilms tumor
- Ewings sarcoma
therapeutic use of vinorelbine
-Advanced NSCLC
in general what are Taxanes effective against
solid tumors
therapeutic use of Paclitaxel?
Docetaxel?
- advanced breast and ovarian cancer
- advanced breast and ovarian recurrence
What vinca alkaloid causes peripheral neuropathy
Vincristine
What cell cycle phase do Vinca Alkaloids and Taxanes affect
M-phase
If you give Vincristine and neuropathy is severe, what should you replace it with
Vinblastine
Treatment with Vinca and Taxane drugs commonly leads to multi drug resistance due to increased expression of what?
P-glycoprotein
Cancer drugs with mechanisms that involve what are NOT prone to P-glycoprotein multi-drug resistance?
What are the important drugs in this category?
- the exterior cell surface
- monoclonal antibodies
What are the 2 classes of topoisomerase inhibitors?
tell which topoisomerase they inhibit ans what kind of breaks they cause
- Epipodophyllotoxins (topoisomerase II . . double strand)
- Camptothecins (top. I . . single strand)
What are the 2 Epipodophyllotoxins?
- Etoposide
- Teniposide
What are the 2 Camptothecins?
- Irinotecan (active metabolite SN38)
- Topotecan
Therapeutic use of Etoposide
- Oat cell carcinoma of Lung
- Testicular cancer (with cisplatin and bleomycin)
Therapeutic use of Teniposide
-Glioma and neuroblastoma
Therapeutic use of irinotecan
-metastatic colorectal cancer
therapeutic use of Topotecan
-2nd line after failed drugs
How are Etoposide and Teniposide metabolized
CYP450 . .Liver
How are Irinotecan and Topotecan metabolized
Renal clearance
what is the dose limiting toxicity of Irinotecan
-Severe Diarrhea (may be life threatening and require treatment with loperamide)
What phase of the cell cycle to topoisomerase II inhibitors affect?
topoisomerase I?
- Mixed
- S phase
What are the 2 classes of drugs that cause DNA intercalation and Oxidative Scission
- Antibiotics
- Anthracyclines
What are the 2 antibiotics used?
- Bleomycin
- Dactinomycin
What are the Anthracyclines?
- Doxorubicin
- Daunorubicin
- Epirubicin
- Idarubicin
- MItoxantrone
What does Bleomycin do
Fe mediated free radical generation which breaks DNA
What does Dactinomycin do
DNA intercalating
What do Doxorubicin, Daunorubicin, Epirubicin, and Idarubicin do
intercalating agents
What does Mitoxantrone do
inhibits topoisomerase II
Therapeutic use of Bleomycin
Testicular cancer
Therapeutic use of Doxorubicin and Epirubicin
-Wide spectrum . . Breast and ovarian
Therapeutic use of Mitoxantrone
Breast
dose limiting toxicity of Bleomycin
pulmonary fibrosis
dose limiting toxicity of Anthracyclines
Cardiotoxicity, dilated cardiomyopathy, congestive heart failure
Co treatment with what other cardiotoxic agent is a risk factor for Anthracyclin Cardiotoxicity
Trastuzumab
Why does Bleomycin cause skin and lung damage?
those tissues do not have the enzyme hydrolase required to metabolize it
Does Bleomycin cause significant myelosuppression?
No
What phase of the cell cycle does Bleomycin affect
G2 phase
What phase of the cell cycle do Anthracyclines affect?
S and G2
name the drugs and the toxicities in the ABVD regimen for Hodgkin’s lymphoma
- Adriamycin (Doxorubicin): Cardiotoxic
- Bleomycin: pulmonary fibrosis
- Vinblastine: peripheral neuropathy
- Dacarbazine: Nausea/vomiting, myelosuppression
Name the drugs and toxicities in the CHOP regimen for NHL
- Cyclophosphamide: hemorrhagic cystitis
- Hydroxy-daunorubicin (doxorubicin): cardiotoxicity
- Oncovin (Vincristine): peripheral neuropathy
- Prednisone: hyperglycemia, osteopenia
What are the Xanthine drugs that can have over exposure when given with gout medications Allopurinol and Febuxostat?
- 6-Mercaptopurine
- Azothioprine
- Theophylline
What drug is given with drugs that cause tumor lysis syndrome
Allopurinol
What are the results from Tumor lysis syndrome
- Hyperkalemia
- Hyperphosphatemia
- HYPERURICEMIA: crystals and Acute renal failure
