Chemo 5 Flashcards
Cell cycle non specific drugs are _____ dependent
Dose . . .
cell cycle specific drugs are more schedule dependent
What are the triazenes and what do they do
- Dacarbazine
- Procarbazine
- Temozolomide
-DNA alkylation. Methylation of Guanasine O6, N7
What are the Nitrosoureas and what do they do?
Carmustine
Lomustine
-Alkylation THEN crosslinking guanosine O6, N7. also Protein carbamoylation
What is streptozocin used for
insulinomas
What are Nitrosoureas used for
Brain tumors
What is Dacarbazine used for
metastatic melanoma
what is Procarbazine used for
Malignant glioma
What is temozolomide used for
Treatment resistant glioma and astrocytoma
What are the nitrogen mustards?
- cyclophosphamide
- Ifosfamide
- Mechlorethamine
how are Cyclophosphamide and Ifosfamide activated
CYP450
What does Melphalan target?
Treat?
Phenylalanine transporters
-Multiple myeloma
What route of administration is Chlorambucil?
What does it treat?
oral
-CLL
What does busulfan treat
CML
What does Estramustine treat
Advanced prostate cancer
what is the M in MOPP treatment for Hodgkin disease
Mechlorethamine
What happens if you miss the vein or infuse Mechlorethamine too fast?
blisters or necrosis
What is the active metabolite of cyclophosphmide?
Toxic one?
- phosphoramide
- Acrolein: urotoxix to bladder
What CYP450s metabolize cyclophosphamide and Ifosfamide?
2B6 and 34A
Ifosfamide has similar metabolites as Cyclophosphamide except it also has one extra. . what is it
-Chloroacetaldehyde (Neurotoxicity)
What is given prophylactically before administration of cyclophasphamide to diminish the toxic effect of Acrolein on the bladder
MESNA
What is used for castration resistant prostate cancer?
What is the complication?
- Estramustine
- Thromboembolic events
route of administration of Carmustine?
Lomustine?
IV
oral
Dacarbazine (IV) and Temozolomide (PO) both have what same activated metabolite
Methyltriazene imidazole carboximide
Does Dacarbazine or Temozolomide penetrate into the CNS well
Temozolomide
What enzyme in tumors influences the efficacy of Temozolomide
O6-MGMT
What is a biomarker for temozolomide efficacy
Epigenetic silencing of MGMT . . we want it to be silenced
What are the organo-platinum drugs
- Cisplatin
- Carboplatin
- Oxaloplatin
What is cisplatin used for
Testicular cancer
What is Carboplatin used for
Ovarian cancer
What is Oxaloplatin used for
colorectal cancer
What is the dose limiting toxicity of cisplatin
- Acute renal failure
- Ototoxicity later in life and is permanent
What is the dose limiting toxicity of Oxaloplatin
cold induced neuropathy . . don’t give ice cubes
how does cisplatin enter cells
diffusion and Cu2+ transporter
What kind of crosslinking does cisplatin do that is difficult for the tumor to repair
INTRA strand. . . . same strand
