Anti-Neoplastic Agents Flashcards
MECHLORETHAMINE
Alkylating Agent
No longer used
PROPERTIES:
*VESICANT (blistering)
*BIFUNCTIONAL
Side Effects: Nausea vomiting, etc.
CYCLOPHOSPHAMIDE (CYTOXAN®)
Alkylating Agent
Activated in the Liver by P450.
Hemhorrhagic Cytitis (urinary bladder inflammation)
IFOSFAMIDE
Alkylating Agent, like Cyclophosphamide
*LESS MYELOSUPPRESSIVE
NITROSOUREA ALKYLATING AGENTS
Lipid soluble! Can be used in brain, etc.
CCNU would be an example of an abreviation. NU = Nitrosourea.
Lomustine and Carmustine are examples
Mechanisms of Action
- ALKYLATES DNA: CROSS LINKS
- Might be effective in CARBAMOYLATES PROTEIN (ADDS UREA MOIETY)
Side Effects: CNS
Platinums
CISPLATIN
OXALIPLATIN
Uses:
TESTICULAR
CISPLATIN
Nephrotoxicity
Severe Nausea
Ototoxic
OXALIPLATIN
LESS RESISTANCE
MITOMYCIN
TEMPORARY BENEFICIAL EFFECTS (not curative agent)
Anti-Metabolites
Methotrexate
6-Mercaptopurine
Pro-Drug
Picks up a Ribose and a Phosphate
Interferes with RNA and DNA.
TOXICITIES:
***HEMATOLOGICAL
***THERAPEUTIC PLACE:
ANTI – LEUKEMIC CHEMOTHERAPY
GOUT:
Allopurinol very similar to Hypoxanthine. Lots of purines are kicked out due to neoplasm death.
6-MP is metabolized via Xanthine oxidase. So, it becomes toxic. So, allopurinol needs to be given in a lower dose, or you will have toxicity issues.
6-Thioguanine
Uses:
ADULT ACUTE LEUKEMIA
5-FLUOROURACIL
Pro-drug
Pyrimadine antagonist
THYMIDYLATE SYNTHASE INHIBITED BY 5-FdUMP
Thymine less death. If you don’t have Thymine, you don’t have DNA.
Interferes with dUMP
TOXICITIES:***HEMATOLOGICAL
THERAPEUTIC PLACE: SOLID TUMORS ]:
CYTOSINE ARABINOSIDE
[CYTARABINE]
Pro-drug
Pyrimidine analog
Inactive unless gets all the phosphates (3) and the Ribose
**AFFECTS RNA / DNA METABOLISM
TOXICITIES:***HEMATOLOGICAL
THERAPEUTIC PLACE: - NOT for SOLID TUMORS!
- ACUTE GRANULOCYTIC / ACUTE MYELOID LEUKEMIAS)
Methotrexate
Anti-Metabolite (Anti-Folic Acid)
Inhibits Folate Reductase:
Methotrexate stops FH2 to FH4.
Carbon transfer from Methylene to FH4 and then transfers to dUMP to make TMP. That pathway is stopped also.
effectively stops the one carbon transfer necessary to make Thimadine.
Needs to pick up Glutamate to be active, so tumor has more of the enzyme adding glutamate. So, its more functional in Tumor cells.
Toxicity:
*MYELOSUPPRESSION (LEUKOPENIA, THROMBOCYTOPENIA) (LIFE – THREATENING INFECTION)
*GI ULCERS (STOMATITIS)
* NEPHROTOXICITY
Antidote: CITROVORUM FACTOR (LEUCOVORIN ) - Can give patient a lethal dose, and then an antedote.
- What it is: N5 - FORMYL THF, FOLINIC ACID
Uses:
CHORIOCARCINOMA
ACUTE LYMPHOCYTIC LEUKEMIA