Chemo Drugs Flashcards
Alkylating agents
- nitrogen mustards –> Mechlorethamine, Cyclophosphamide
- nitrosureas –> Carmustine
Mechlorethamine
MECH: induce alkyl groups in dna; causes dna crosslinks and strand breaks
Cell cycle non specific
USE: Hodgkin’s lymphoma
TOX: hematopoiesis suppression; damage to intestinal mucosa; nausea, vom
Cyclophosphamide
MECH: induce alkyl groups in dna; cause dna crosslinks and strand breaks; ACTIVATED IN LIVER by cytoP450
Cycle specific/phase nonspecific
USE: v broad spectrum–> hodgin’s lymphoma, non hodgkins lymphoma, multiple myeloma, neuroblastoma, leukemia, carcinoma of endometrium/breast/lung
TOX: hematopoiesis suppression; damage to intestinal mucosa; nausea, vom; STERILE HEMORRAGIC CYSTITIS
Carmustine
MECH: induce alkyl groups into dna; cause dna crosslinks, strand breaks; HIGHLY LIPOPHILIC - CROSSES BBB
Cell cycle non specific
USE: BRAIN tumors; multiple myeloma; melanoma
TOX: hematopoiesis suppression; damage to intestinal mucosa; nausea, vom
Antimetabolites
- folate analogs: Methotrexate
- pyrimidine analogs: Fluorouracil, Cytarabine
- purine analogs: Mercaptopurine, Hydroxyurea
Methotrexate
MECH: binds dihydrofolate reductase; prevents formation of THF
S phase specific
USE: acute lymphocytic leukemia; choriocarcinoma
TOX: intestinal epithelium; bone marrow suppression; renal tubular necrosis
**REQ rescue of host cells w/ LEUCOVORIN
Fluorouracil
MECH: activated in cells to FUTP to inhib rna syn and FdUMP to interfere w/ thymidylate synthetase and dna syn
S phase specific
USE: carcinoma of stomach, colon, pancreas, ovary, head and neck, breast, bladder; topical cream for basal cell carcinomas
TOX: nausea; anorexia; diarrhea; myelosuppression
Cytarabine
MECH: cytidine analog; competes w/cytidine for all 3 phosphorylation steps to dCTP; cytarabine tri phosphate competes w/ dCTP for incorporation into dna –> dna chain termination
S phase specific
USE: acute leukemias
TOX: myelosuppression; neurotox
Mercaptopurine
MECH: purine analog; converted in cells to ribonucleotide –> inhib rna and dna syn
S phase specific
USE: acute leukemias
TOX: bone marrow depression; vomiting, nausea; anorexia; jaundice
Hydroxyurea
MECH: inhib ribonucleotide reductase –> blocks dna syn
S phase specific (arrest at G1-S interface)
USE: chronic granulocytic leukemia; head and neck cancer
TOX: hematopoietic depression; GI disturbances
Natural Products
- vinca alkaloids –> vinblastine, vincristine
- taxanes –> paclitaxel
Vinblastine
MECH: binds to tubulin –> inhib proper formation of microtubules and mitotic spindle
M phase specificity
USE: Hodgkins, non hodgkins; breast cancer
TOX: STRONGLY myelosuppressive; epithelial ulcerations
Vincristine
MECH: binds to tubulin –> inhib proper formation of microtubules and mitotic spindles
M phase specificity
USE: acute lymphocytic leukemia; Hodgkins and non hodgkins lymphoma; Wilm’s tumor; neuroblastoma; rhabdomyosarcoma
TOX: alopecia; neuromusc abnorm (incl peripheral neuropathy); significantly LESS bone marrow suppression
Paclitaxel
MECH: enhances assembly and stability of microtubules by binding to beta subunit of tubulin
Late in G2 phase
USE: refractory ovarian cancer; breast cancer
TOX: dose limiting leukopenia; peripheral neuropathy; myalgia/arthralgia
Antitumor antibiotics
Doxorubicin
Belomycin
Doxorubicin
MECH: intercalates btwn dna base pairs –> distorting dna helix; causes lipid peroxidation and free radical gen; binds to dna and Topo II
Cycle specific/phase nonspecific
USE: Hodgkins and non hodgkins lymphoma; breast, ovary, small cell lung cancers
TOX: dialated CARDIOMYOPATHY; bone marrow depression; alopecia; GI disturbances
Bleomycin
MECH: glycopeptides that bind dna –> oxidative like damage to dna = dna strands break
Phase specific for G2
USE: germ cell tumors of testes and ovaries; head, neck, lung lymphomas
TOX: DOSE REL PULMONARY TOX; vesiculation of skin; hyperpigmentation; MINIMAL myelosuppression/immunosuppression
Etoposide
MECH: stabilizes dna topo II complexes –> double strand dna breaks
Late G2 phase
USE: lymphomas; acute nonlymphocytic leukemia; small cell carcinoma of the lung; testicular cancer
TOX: leukopenia; nausea vom; diarrhea; alopecia
Filgrastim (G-CSF)
MECH: stim granulocyte (neutrophil) prod by the marrow
USE: given post myelosuppressive agents to speed neutrophil recovery
TOX: bone pain
Trastuzumab
MECH: monoclonal Ab that binds to HER2 receptor
USE: breast cancers that OVEREXPRESS HER2
TOX: CARDIOMYOPATHY; hypersensitivity; infusion rxn: fever, chills
Cisplatin
MECH: platinum coordination complex; hyrolation –> activated species = dna crosslinks
Cycle specific/ phase non specific
USE: WIDE ANTITUMOR SPECTRUM: testes, ovary, head, neck, bladder, colon, esophagus, small cell lung
TOX: NEPHRO, OTO, peripheral neuropathy, electrolyte disturbance; nausea, vom; mild to mod myelosuppression
Procarbazine
MECH: activated in vivo to a methylating agent –> chromosomal damage
G1 and S phase
USE: Hodgkin’s lymphoma
TOX: myelosuppression; nausea, vom
Prednisone
MECH: bind to steroid receptors; depresses rna syn of many growth related genes; induces nucleases which may mod cell lysis
Arrest cells at G1
USE: anti emetic effect; pallative therapy; acute and chronic lymphocytic leukemia; Hodgkin’s dz, non Hodgkin’s lymphoma; breast cancer
TOX: limited myelosuppression
Tamoxifen
MECH: antiestrogen that blocks estrogen receptors; activated by CYP2D6 (**less effective if CYP2D6 is inhibited)
USE: POST MENOPAUSAL breast cancer; breast cancer PROPHYLAXIS in women at high risk
TOX: hot flashes; fatigue; nausea; bone and other musculoskeletal pain
