Chemo Pharm Flashcards
Cyclophosphamide
- Alkylating agent (bis-chloroethyl amine)
- Aldophosphamide generates cytotoxic metabolites
- Adverse effects-hemorrhagic cystitis, need IV hydration during therapy
- Uses: NHL, lymphoid malignancies, breast and ovarian cancers, solid pediatric tumors, Burkitts
Mechlorethamine
- Alkylating agent (bis-chloroethyl amine)
- Topical tx for cutaneous T-cell lymphoma
- Rarely used today b/c it is so reactive
Melphalan
- Alkylating agent (bis-chloroethyl amine)
- Only given IV
- Adverse effects-mostly hematological
- Use: multiple myeloma (+ dexamethasone)
Chlorambucil
- Alkylating agent (bis-chloroethyl amine)
- Given orally
- Adverse effects-N/V, but well tolerated
- Use CLL
Name the 4 bis-chloroethyl amine alkylating agents
Cyclophosphamide, mechlorethamine, melphalan, chlorambucil
Carmustine
- Alkylating agent (nitrosourea)
- Alkylates DNA, lipophilic so crosses BBB
- Adverse effects-profound myelosuppression
- Use: malignant gliomas
Streptozocin
- Alkylating agent (nitrosourea)
- High affinity for cells in islets of Langerhans
- Adverse effects-nausea, renal/hepatic toxicity
- Uses: Pancreatic islet cell carcinoma, carcinoid tumors
Name the 2 Nitrosourea alkylating agents
Carmustine, Streptozocin
Thiotepa
- Alkylating agent (aziridine)
- Crosslinks DNA via hepatic CYPs
- Adverse effects-mucosal and CNS toxicity, coma, seizure
- Use: transplants for hematological malignancies
Busulfan
- Alkylating agent (alkylsulfonate)
- Alkylates DNA?
- Adverse effects-Myelosuppression; Pulmonary fibrosis, GI mucosal damage, hepatic VOD at high dose
- Use: CML
Name the aziridine and alkylsulfonate alkylating agents
Thiotepa, Busulfan
Procarbazine
- Alkylating agent (non-classic)
- Methylates DNA, produces chromosome breaks
- Adverse effects-carcinogenic potential, increased risk secondary cancer, augments sedative effects
- Uses: Hodgkin disease, gliomas
Dacarbazine
- Alkylating agent (non-classic)
- Methylating agent
- Adverse effects-myelosuppression, severe N/V
- Uses: HODGKINS, melanoma, adult sarcoma
Bendamustine
- Alkylating agent (non-classic)
- Crosslinks DNA, inhibits mitotic checkpoints
- Adverse effects-myelosuppression, mucositis
- Uses: CLL, NHL
Name the 3 non-classic alkylating agents
Procarbazine, dacarbazine, bendamustine
Cisplatin
- Alkylating agent (platinum analog)
- Crosslinks DNA, inhibits DNA synthesis/function
- Adverse effects-Nephrotoxicity (prevent with hydration and Cl diuresis), Ototoxcity, N/V, neuropathy, anaphylaxis
- Uses: Testicular, ovarian, head and neck, cervix, endometrium, lung, rectal and anal carcinomas; childhood neoplasms
Carboplatin
- Alkylating agent (platinum analog)
- Crosslinks DNA, inhibits DNA synthesis/function
- Adverse effects-BETTER tolerated than cisplatin, thrombocytopenia, hypersensitivity
- Uses: Ovarian cancer, SCLC, alternative to cisplatin
Oxaliplatin
- Alkylating agent (platinum analog)
- Crosslinks DNA, inhibits DNA synthesis/function
- Adverse effects-neurotoxicity, possible leukemia and pulmonary fibrosis
- Colorectal and gastric cancer
Name the 3 platinum analog alkylating agents
Cisplatin, Carboplatin, Oxaliplatin
Methotrexate
- Antimetabolite (antifolate)
- Inhibits THF, interferes with DNA/RNA/proteins
- Adverse effects-multiple drug-drug interactions
- Uses: breast cancer, head and neck cancer, osteogenic sarcoma, CNS lymphoma, NHL, bladder cancer, choriocarcinoma
Pemetrexed
- Antimetabolite (antifolate)
- Activity in S-phate, inhibits TS
- Adverse effects-myelosuppression, rash, mucositis, diarrhea, fatigue, hand-foot syndrome
- Uses: mesothelioma, NSCLC
Pralatrexate
- Antimetabolite (antifolate)
- Inhibits DHFR, TS, other enzymes
- Adverse effects-myelosuppression, rash, mucositis, diarrhea, fatigue
- Use: relapsed or refractory peripheral T-cell lymphoma
Name the 3 antifolate antimetabolites
Methotrexate, Pemetrexed, Pralatrexate
5-fluorouracil (5-FU)
- Antimetabolite (fluoropyrimidine)
- Inhibits DNA synthesis, interferes with RNA processing
- Adverse effects-myelosuppression, GI toxicity, skin toxicity, neurotoxicity
- Uses: most widely used for COLORECTAL cancer, breast cancer, stomach cancer, pancreatic cancer, esophageal cancer, hepatocellular cancer, head and neck cancers, anal cancer
Capecitabine
- Antimetabolite (fluoropyrimidine)
- Prodrug that is metabolized to 5-FU
- Adverse effects-diarrhea, hand foot syndrome, myelosuppresion, N/V, mucositis, alopecia
- Uses: metastatic breast cancer, metastatic colorectal cancer, part of the XELOX regimen
TAS-102
- Antimetabolite (fluoropyrimidine)
- Inhibits TS, DNA synthesis, DNA function
- Adverse effects-Myelosuppression (neutropenia), GI toxicity
- Use: progressive, refractory colorectal cancer
Name the 3 fluoropyrimidine antimetabolites
5-FU, capecitabine, TAS-102
Cytarabine
- Antimetabolite (deoxycytidine)
- S-phase secific, blocks DNA polymerase A and B
- Adverse effects-myelosuppression, mucositis, N/V, neurotoxicity
- Use: hematologic malignancies-AML, NHL
Gemcitabine
- Antimetabolite (deoxycytidine)
- inhibits ribonucleotide reductase, DNA polymerase A and B
- Adverse effects-myelosuppression (neutropenia), N/V
- Uses: Advanced pancreatic cancer, NSCLC, bladder cancer, ovarian cancer, soft tissue sarcoma, NHL
Name the 2 deoxycytidine antimetabolites
Cytarabine, Gemcitabine