Term
| mechlorethamine [Mustargen] |
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Definition
alkylating agent - CCNS but more susceptible in late G1 & M phase;
Toxicity:
1) N/V
2) bone marrow depression; |
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Term
| cyclophosphamide [Cytoxan] |
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Definition
alkylating agent - CCNS, ACTIVATION in LIVER (CYP P450);
Toxicities:
1) N/V
2) bone marrow depression |
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Term
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Definition
alkylating agent - CCNS, HIGHLY LIPID SOLUBLE --> Crosses BBB;
Toxicities:
1) N/V
2) leukopenia, thrombocytopenia;
Uses:
also used for BRAIN TUMORS (crosses BBB easily) |
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Term
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Definition
alkylating agent - CCNS but more susceptible in G1;
Platinum coordination compound;
Toxicities:
1) N/V
2) bone marrow depression
3) NEPHROTOXICITY and OTOTOXICITY |
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Term
| methotrexate [Methotrexate] |
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Definition
antimetabolite - folic acid analog - CCS (S phase), inhibits dihydrofolate reductase blocking conversion of folic acid to tetrahydrofolate;
poor CNS penetration;
use along with leucovorin --> bypasses metabolic block to protect normal cells;
Toxicities:
1) MILD N/V
2) bone marrow depression
Other Tx:
PSORIASIS, RHEUMATOID ARTHRITIS |
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Term
| mercaptopurine [Purinethol] |
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Definition
antimetabolite - purine analog - CCS (S phase) - inhibits enzymes of purine interconversion
Toxicities:
1) N/V
2) bone marrow depression |
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Term
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Definition
antimetabolite - pyrimidine analog - CCS (S phase) on PROLIFERATING CELLS - blocks conversion of deoxyuridylate to thymidylate;
Toxicities:
1) N/V
2) bone marrow depression |
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Term
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Definition
antimetabolite - pyrimidine analog - CCS (S phase) - inhibits DNA polymerase by competing with substrate;
Toxicities:
1) N/V
2) bone marrow depression |
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Term
| daunorubicin HCl [Cerubidine], doxorubicin HCl [Adriamycin] |
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Definition
natural products - antibiotics - CCNS - intercalates & binds DNA --> uncoils DNA;
Toxicities:
1) N/V
2) bone marrow depression
3) CARDIOTOXIC |
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Term
| vinblastine sulfate [Velban], vincristine sulfate [Oncovin] |
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Definition
natural products - vinca alkaloids - CCS (M phase) - disrupts mitotic spindle during mitosis;
Toxicities:
1) MILD N/V
2) bone marrow depression
3) NEUROLOGICAL TOXICITY
4) local irritant |
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Term
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Definition
natural products - podophyllotoxin - CCS (G2 phase) - topoisomerase inhibitor --> DNA breaks;
Toxicities:
1) N/V
2) LEUKOPENIA
3) ALOPECIA |
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Term
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Definition
natural product - taxane isolated from Western Yew - CCS (G2 & M phases) - antimicrotubule agent that promotes microtubule assembly, enhancing tubulin polymerization;
1st line tx of metastatic breast cancer, used with trastuzumab (Herceptin);
Toxicity:
1) N/V
2) ALOPECIA
3) bone marrow depression |
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Term
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Definition
hormonal - adrenocorticosteroid - CCS (G1 phase) - binds to cytosolic receptors & affects DNA & RNA & protein synthesis; suppresses lymphocytes & macrophages;
Toxicities:
1) Short: none
2) Long period: IATROGENIC CUSHING'S SYNDROME, OSTEOPOROSIS, INFECTIONS, ULCERS
Indications for Use:
1) breast carcinoma
2) leukemia & lymphoma (adult), acute leukemia (childhood)
3) immunosuppressant |
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Term
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Definition
hormonal - adrenocorticosteroid - CCS (G1 phase) - binds to cytosolic receptors & affects DNA & RNA & protein synthesis; suppresses lymphocytes & macrophages;
Toxicities:
1) Short: none
2) Long period: IATROGENIC CUSHING'S SYNDROME, OSTEOPOROSIS, INFECTIONS, ULCERS
Indications for Use:
1) breast carcinoma
2) leukemia & lymphoma (adult), acute leukemia (childhood)
3) immunosuppressant |
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Term
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Definition
hormonal - antiestrogen - CCS (G1 phase) - competes with estradiol for binding to cytoplasmic estrogen receptors --> DNA, RNA, and protein synthesis reduced;
Toxicities:
1) Short period: HOT FLASHES, N/V
2) Long period: visual disturbances, hypercalcemia, vaginal bleeding
3) POTENTIAL TUMOR-PROMOTING ACTIVITY --> increased risk of ENDOMETRIAL CANCER
Indication for Use:
BREAST CARCINOMA (women & men) |
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Term
| imatinib mesylate [Gleevec] |
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Definition
tyrosine kinase inhibitor - CCS (G1 phase) - Bcr-Abl protein tyrosine kinase inhibitor; cell proliferation inhibitor & induction of apoptosis;
Metabolized by CYP3A4;
Toxicities:
1) Short period: ABDOMINAL PAIN, N/V;
2) Long period: fatigue, joint pain, fluid retention, cramps, edema, rash
Indications for Use:
ACUTE LYMPHOCYTIC LEUKEMIA;
Ph+ (Philadelphia chromosome +) MYELOID LEUKEMIA |
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Term
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Definition
monoclonal antibody - CCS (G1 phase);
MoA:
1) binds to extracellular domain of human epidermal growth factor receptor HER-2;
2) Downregulation of EGF receptor tyrosine kinase signaling activity;
3) G1 cell cycle arrest;
Toxicities:
1) Short period: N/V, diarrhea;
2) Long period: anemia, neutropenia, infections, fatigue, infusion rxns, rash;
Indications for Use:
1) adjuvant breast cancer
2) metastatic breast cancer - used with paclitaxel [Taxol] as 1st line agent |
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Term
| Cell cycle-specific (CCS) Agents |
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Definition
| effective drugs in tx of hematologic malignancies & other tumors in which large proportion of cells are PROLIFERATING or are in the GROWTH FRACTION - antimetabolites, podophyllin alkaloid, vinca alkaloids |
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Term
| Cell cycle-nonspecific (CCNS) Agents |
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Definition
| drugs effective in low-growth solid tumors - alkylating agents, antibiotics, cisplatin |
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Term
| leucovorin (folinic acid) |
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Definition
| drug that bypasses metabolic block caused by methotrexate, protecting normal cells |
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