Antineoplastic Drugs Flashcards
Ifosfamide
cross links DNA and prevents synthesis. Cell cycle nonspecific Toxicity when it enters the cell cycle. Oral and IV Cyclophosphamide analog. Is an alkylating agent.
Cyclophosphamide
Cell cycle nonspecific. Cross links DNA and prevents synthesis. Alkylating agent. Oral, liver activation. Hemorrhagic cystitis from acroline metabolite, treat with Mesna.
Mesna
Is coadministered with cyclophosphamide to bind acroline to prevent hemorrhagic cystitis.
Busulfan
Alkylating agent. Moa cross links DNA and prevents synthesis
-needs excess hydration to counteract kidney hydration
-exit via renal excretion so monitor that they are being cleared IV treatment
Activated in Liver.
Cisplatin
IV Moa cross links DNA and prevents synthesis. Platinum containing compound, does not alkylate
-needs excess hydration to counteract kidney hydration
-exit via renal excretion so monitor that they are being cleared
Alkylating agent
Etoposide
Topoisomerase II inhibitor Cell cycle specific for S-phase and G2. Causes strand breaks in DNA IV and oral.
Doxyrubicin
Intercolating (between DNA like ethidium bromide stopping DNA and RNA synthesis) and Topo II inhibitor IV. Cell cycle nonspecific. Vesicant. Radiation recall. BMS. Urine Red. Antibiotic
Methotrexate
Analog of tetrahydrofolate inhibits DHFR. IV and oral
Alkylation of the urine makes the methotrexate excretion in the urine less toxic
Cotreat with Leucovorin and Glucarpidase
Leucovorin
Reduced form of folate bypasses DHFR and supplies 1C pool to help good cells with methotrexate treatment
Glucarpidase
enzyme used to lower methotrexate into inactive DAMPA for alternative route of elimination than kidney. IV
5-Fluorouracil
inhibits thyamine Synthase Cell cycle specific antimetabolite. Affects pyrimadine synthesis AE: Acute Cerebellar syndrome, lowest theraputic index. Liver elimination
Fludarabine
Analog of purines. IV Blocks DNA polymerase Cell cycle specific to S-Phase
Paclitaxiel
Antimitotic: Prevents Depolymerization of microtubules preventing Metaphase->anaphase transition. IV treatment
Carmustine
Antineoplastic Is an alkylating agent causes cross links in DNA and RNA leading to cell death. Crosses the BBB easily, cell cycle specific. Wafers inserted into the brain and IV. Lipophillic. Nitrosoureas
Temozolomide
Alkylating agent, methylation of RNA and DNA. Crosses BBB easily; lipophillic.
Vincristine
Depolymerization of microtubules preventing Metaphase->anaphase transition. IV treatment. Is small so crosses the BBB very well, but is effluxed out of the brain so is not as good as temozolomide and carmustine in treating brain tumors.
Pemetrexed
Analog of tetrahydrofolate inhibits DHFR. IV and oral
Alkylation of the urine makes the methotrexate excretion in the urine less toxic
Cotreat with Leucovorin and Glucarpidase
Pralatrexate
Analog of tetrahydrofolate inhibits DHFR. IV and oral
Alkylation of the urine makes the methotrexate excretion in the urine less toxic
Cotreat with Leucovorin and Glucarpidase
6-Mercaptopurine
S-phase specific, Inhibits purine synthesis by blocking guanylyl Kinase, resulting in pseudofeedback inhibition leading to buildup of AMP, GTP which must be made through salvage pathway. Useful for leukemia
AE: bone marrow suppression, Tumor lysis syndrome, increased uric acid
Capecitabine
inhibits thyamine Synthase Cell cycle specific antimetabolite. Affects pyrimadine synthesis AE: Acute Cerebellar syndrome, lowest theraputic index. Liver elimination same as 5FU
Azithroprine
S-phase specific, Inhibits purine synthesis by blocking guanylyl Kinase, resulting in pseudofeedback inhibition leading to buildup of AMP, GTP which must be made through salvage pathway. Useful for leukemia
AE: bone marrow suppression, Tumor lysis syndrome
Not anticancer
6-Thioguanine
Inhibits Guanylyl kinase
S-phase specific, Inhibits purine synthesis by blocking guanylyl Kinase, resulting in pseudofeedback inhibition Useful for leukemia
AE: bone marrow suppression, Tumor lysis syndrome increased uric acid
Allopurinol
Inhibits xanthine oxidase, preventing uric acid buildup and gout associated with 6 mercaptopurine due to tumor cell lysis. Use with 6- mercaptopurine results in excessive toxicity, reduce 6mcp dose
Cladrabine
Inhibits DNA polymerase, blocks DNA elongation, can cause repititons, mutagenic. Forces differentiation Pyrimadine.
Cytarabine (ARA-C)
Inhibits DNA polymerase, blocks DNA elongation, can cause repititons, mutagenic. Forces differentiation Pyrimadine. Cytodine analog. S-phase
Gemcitabine
Inhibits DNA polymerase, and ribonucleotide reductase leading to strand termination and Apoptosis
Hydroxyurea
Inhibitor of ribonucleotide reductase, preventing deoxynucleotide syntheisis from ribonucleotides. Syncronizes cells into G1, more sensitive to radiation.
Chlorambucil
Alkylating agent. Moa cross links DNA and prevents synthesis Nitrogen mustard. Oral, broad spectrum, lung toxicity. CCNS
Lomustine
Is an alkylating agent causes cross links in DNA and RNA leading to cell death. Crosses the BBB easily, cell cycle specific. Wafers inserted into the brain and IV. Lipophillic. Nitrosourea
Decarbazine
Alkylating agent Moa cross links DNA and prevents synthesis. CCNS. Treats hodgkins disease.
Mechlorethamine
Alkylating agent, cross links DNA. IV. mustard gas. Vesicant agent, rapid activation. Bone marrow suppression.
Melphan
Alkylating agent, cross links DNA. Given orally. Tx. multiple myeloma.
Procarbazine
Alkylating agent, cross links DNA. Given orally., activated by CYP450. Tx. lymphomas.
Carcinogenic-> leukemias
Mitomycin
Antibiotic. Cross links DNA.
Selective toxicity
Lung toxicity in 10% of pts. 50% fatal.
Kidney damage
Carboplatin
IV Moa cross links DNA and prevents synthesis. Platinum containing compound, does not alkylate
-needs excess hydration to counteract kidney hydration
-exit via renal excretion so monitor that they are being cleared
Alkylating agent
Oxaloplatin
IV Moa cross links DNA and prevents synthesis. Platinum containing compound, does not alkylate
-needs excess hydration to counteract kidney hydration
-exit via renal excretion so monitor that they are being cleared
Alkylating agent
Danorubicin
Intercolating (between DNA like ethidium bromide stopping DNA and RNA synthesis) and Topo II inhibitor IV. Cell cycle nonspecific. Vesicant. Radiation recall. BMS. Urine Red. Antibiotic
Idarubicin
Intercolating (between DNA like ethidium bromide stopping DNA and RNA synthesis) and Topo II inhibitor IV. Cell cycle nonspecific. Vesicant. Radiation recall. BMS. Urine Red. Antibiotic
Epirubicin
Intercolating (between DNA like ethidium bromide stopping DNA and RNA synthesis) and Topo II inhibitor IV. Cell cycle nonspecific. Vesicant. Radiation recall. BMS. Urine Red. Antibiotic
Mitoxatone
Intercolating (between DNA like ethidium bromide stopping DNA and RNA synthesis) and Topo II inhibitor IV. Cell cycle nonspecific. Vesicant. Radiation recall. BMS. Urine Blue. Antibiotic
Bleomycin
Antibiotic. Activated by hydrolase(not in lungs or skin). Topo II inhibitor-> strand breaks/ fragmentation. Lack of bone marrow suppression.
AE:hypersensitivity, GI, pulmonary fibrosis. Skin and lung damage.
Irinotecan
Plant alkylaloid, Top I inhibitor, DNA strand breaks. Kidney elim. Metastatic Colon cancer.
Myelosuppression, diarrhea acute-> atropine, chronic.
Severe-> dehydration
Topotecan
Plant alkylaloid, Top I inhibitor, DNA strand breaks. Kidney elim. Metastatic Colon cancer.
Myelosuppression, diarrhea acute-> atropine, chronic.
Severe-> dehydration
Trimethoprim + sulfamethoxazole
folic acid inhibitor, and blocker of dihydropteroate synthetase. They act synergistically blocking the folate pathway in bacteria
