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Mechloroethamine (Mustargen)
Rapidly acting Hygroscopic & unstable Active drug is present for only a few min IV- causes severe local rxns Vesicant Myelosuppression Leukopenia Thrombocytopenia Nausea Vomiting MOPP regimen to treat Hodgkin & other lymphomas Mycosis fungoides Alykalating Agent
Cyclophosphamide (Cytoxan)
Most widely used Metabolically activated P450 to 4-hcpa—which is nonenzymatically cleaved to aldophosphamide In tumor cells it is cleaved to phosphoramide mustard= toxic to tumor cells & it is cleaved to acrolein (suspected to cause hemorrhagic cystitis- toxic to bladder) Orally IV IM Immunosuppresion Bladder toxicity Less incidence of thrombocytopenia Reversible alopecia Nausea Vomiting   MESNA- neutralizes acrolein at acidic pH in urine, decreases bladder toxicity   Lymphoma Leukemia Mycosis fungoides Multiple myeloma Retinoblastoma Breast Ovarian Sm cell lung   Also used in some autoimmune conditions Alkylating Agent
Isofamide  (Ifex)
Cyclophosphamide analog with less potential to cause hemorrhagic cystitis   CNS & UT (bladder) toxicity limit its use to special application   MESNA Osteosarcoma & Pediatric malignancies (better than Cytoxan) Testicular cancer Stem cell rescue Alykating Agent
Melphalan  (Alkeran)
Derivative of N-mustard- Contains phenylalanine Lower reactivity Oral Myelosuppression NO alopecia Naus/Vom- infrequent Multiple myeloma Ovary carcinoma Alkylating Agent
Bulsulfan (myleran)
Introduces a 4C crosslink into DNA Selectively myelosuppressive—inhibits granulocytopoiesis Oral Relatively non-toxic Adverse effects related to myelosuppression Naus/vom on occasion High doses- rare- fatal pulmonary fibrosis “busulfan lung” Chronic myelogenous/granulocytic leukemia   Alkyl Sulfonate  Agent
Chlorambucil   (Leukeran)
Derivative of N-mustard-contains an aromatic ring Slowest acting N-mustard Oral Least toxic Less severe bone marrow suppression Chronic lymphocytic leukemia Some lymphoma Hodgkin Alkyalating Agent
Carmustine (BiGNU) (Gliadel)
Highly lipophilic Cross BBB Can carbamylate intracell mol IV Myelosuppressive (delayed effect- up to 6 wks) Renal failure possible Hodgkin Lymphoma Brain tumors Nitrosoureas
Lomustine (CeeNU)
Highly lipophilic Cross BBB Can carbamylate intracell mol Oral Myelosuppressive (delayed effect- up to 6 wks) Renal failure possible Hodgkin Lymphoma Brain tumors Nitrosoureas
Semustine (methyl-CCNU)
Highly lipophilic Cross BBB*** Can carbamylate intracell mol Oral Myelosuppressive (delayed effect- up to 6 wks) Renal failure possible Hodgkin Lymphoma Brain tumors Nitrosoureas
Streptozocin (Zanosar)
Natural Ab that is composed of methylnitrosourea linked to the 2-C of glucose   Requires in vivo activation Oral NOT myelosuppressive Nausea Vomiting Renal toxicity= dose-limiting effect Can cause diabetes*** Pancreatic islet cell carcinoma Carcinoid Nitrosoureas
Dacarbazine (DTIC-Dome)
Activated in the liver to a cell killing methylating metabolite IV ABVD regimen Moderately myelosuppressive Nausea Vomiting Flu-like symptoms Hodgkin Malignant melanoma Soft tissue carcinoma Triazene Alkyalating Agent
Thiotepa
Converted rapidly by liver mixed-fxn oxidases to its active metabolite TEPA Used for high dose chemo regimens IV Absorption is unpredictable IV to bladder Myelosuppression Ovarian cancer Recurrent bladder cancer- IV to bladder Ethylenimine Alkyalating Agent
Temozolomide (Temodar)
Similar to DTIC Oral Hematologic & GI toxicities Brain tumors: Anaplastic astrocytoma Glioblastoma multiforme Malignant melanoma Uterine leiomyosarcoma Tertrazine Alkyalting Agent
Methotrexate (MTX)
Folic acid analogue that competitively inhibits dihydrofolate reductase (DHFR) This reduces the pool of tetrahydrofolate req for the conversion of dUMPàdTMP   Net result= indirect inhibition of DNA synthesis Also inhibits RNA and protein synthesis Also inhibits enzymes involved in folate metabolism (dihydrofolate reductase)   It is transported into cells by folate carriers and activated to various forms of polyglutamate Poorly transported across the BBB Oral IV IM Intrathecally- for CNS therapy   Excreted in the urine 50% plasma protein bound- can be replaced by ASPIRIN Myelosuppressive (produces severe leukemia, BM aplasia, thrombocytopenia)   Dose monitoring & leucovorin (folinic acid- converted to an essential factor for thymidylate synthetase) “rescue” are important   GI disturbances Alopecia Headache Mucositis Renal Toxicity possible bc crystalluria of the 7-OH metabolite of MTX   R results from transport defects & amplifications or alterterations in the gene for dihydrofolate reductase Childhood acute lymphoblastic leukemia Choriocarcinoma Trophoblastic in women   In combo for Burkitt’s, non-Hodgkin lymphomas Osteogenic sarcoma Lung carcinoma Head/neck carcinoma   Severe psoriasis Immunosuppression following a transplant RA Crohn Takayasu arteritis Wegener granulomatosis   Therapeutic abortion Antimetabolite
Pemetrexed (Alimta)
Inhibition of thymidylate synthetase Transported into cell by folate carriers & activated to various forms of polyglutamate   Myelosuppression Mesothelioma (w. cisplatin) Antimetabolite
Cytarabine (ara-C) (Cytosar-U)
Pyrimidine antagonist that is an analogue of 2’-deoxycytidine Accumulation of metabolite inhibits the activity of DNA polymerase If incorporated into DNAàaltered fxn in S phase IV continuous infusion Intrathecally Myelosuppressive (can produce sever leukopenia, thrombocytopenia, anemia)   GI disturbances   R via changes in enzymes required for conversion of the nucleoside to various phosphory forms Induction of remission in acute leukemia *AML Non-Hodgkin lymphoma Antimetabolite
Fluorouracil (5-FU) (Adrucil)
Pyrimidine antagonist that needs to be converted to F-dUMP- which inhibits thymidylate synthetase and thus the production of dTMP & DNA, by forming ternary complex btwn itself & the enzyme Parenterally Topically for skin cancers Myelosuppression   GI disturbances Alopecia Neuro effects

R due to decreased conversion to F-dUMP or altered or amplified thymidylate synthetase Solid carcinomas Breast & GI carcinomas Metastatic colon carcinomas (sometimes by infusion into hepatic a)   Premalignant keratosis Superficial basal cell Antimetabolite
6-Mercaptopurine (Purinethol)
Purine antagonist (analog of hypoxanthine) Causes Base mispairing Must be converted to ribonucleotide by the salvage pathway enzyme HGPRT to produce 6-thioGMP Can be further phosphor & is incorporated into DNA Oral Bone marrow depression is the dose-limiting toxicity   GI disturbances Anorexia Nausea Vomiting   R- due to deficiency in tumor cells of HGPRT ALL AML   Crohn Antimetabolite
6-thioguanine
Purine antagonist (analog of guanine) Must be converted to ribonucleotide by the salvage pathway enzyme HGPRT to produce T-IMP T-IMP accum & inhibits nucleotide metabolism at several steps Can be converted into thioguanine derivatives & be incorporated into DNA Oral (absorption in incomplete) Bone marrow depression is the dose-limiting toxicity   Less severe GI Remission reduction & maintenance of AML Antimetabolite
Gemcitabine (Gemzar)
More lipophilic & longer t1/2 Pyrimidine antagonist- inhibits DNA synthesis via chain termination IV Myelosuppresion Pancreatic caner Non-sm-cell lung cancer Bladder cancer Antimetabolite
Azathioprine (Imuran)
Substituted imidazole attached to the sulfur in 6MP Slow release form of 6 MP  
transplants
Vinblastine (Velban) (Velsar)
Disrupt MT assembly & the formation of the mitotic spindle Metaphase arrest   IV   Excreted in bile Bone marrow suppression with leukopenia is the dose-limiting toxicity Neurological tox Nausea Vomiting Alopecia Ulceration from SC extravasation PVB regimen   Lymphoma- Hodgkin Testicular Cancer Neuroblastoma   Several solid tumors Natural Products
Vincristine (Oncovin) (Vincasar)
Disrupt MT assembly & the formation of the mitotic spindle Metaphase arrest   IV   Excreted in bile Less toxic to bone marrow Peripheral neuropathies are the dose-limiting toxicity   Severe constipation alopecia Use w. prednisone to induce remissions in childhood leukemia MOPP- Hodgkin CHOP- non-Hodgkin Rhabdomyosarcoma Nephroblastoma natural products
Paclitaxel (Taxol)
Bark of yew tree Stabilizes MT formation to disassembly with arrest in mitosis- prevents depolymerization M-phase specific IV *Myelosuppresion & Peripheral neuropathies- dose-limiting toxicities   HS specific to the vehicle (castor oil/ethanol) for admin   R- expression of PGP Ovarian Breast Non-sm cell lung Kaposi Taxane Natural Product
Etoposide (VePesid)
Block cells at the boundary of S phase & prevent entry into G2 Forming a ternary complex with Topo II & DNAà 2x stranded DNA break Do NOT disrupt MT- causes mitotic arrest IV Leukopenia is the dose-limiting toxicity Recalcitrant testicular tumors w. cisplatin for sm. Cell lung & AML Epipodophyllotoxins - natural
Dactinomycin (Actinomycin D) (Cosmegen)
Chromophore containing peptides isolated from Streptomyces   Potent cytotoxic agent Intercalates btwn adj guanosine-cytosine base prs of the DNA 2x helix to form a very stable complex Causes frame shift mutations Also inhibits DNA dep RNA Pol   Phase NONSPECIFIC Strongly impairs RNA synthesis & to a less extent DNA synthesis IV Bone marrow suppression is the dose-limiting toxicity   Gi disturbances Oral ulcers Alopecia   R- PGP, increased glutathione peroxidase activity, Decreased Topo II Rhabdomyosarcoma Wilms in children   Choriocarcinoma   Gestational trophoblastic tumor Metastatic testicular carcinoma Ewing sarcoma natural antibiotic
Doxorubicin (Adriamycin) (Doxil)
Anthracyclin Ab DNA-intercalating agent- block synthesis of DNA & RNA Also fragment DNA bc of the inhibition of Topo II or the generation of superoxide anion radicals   Disrupts the cell mem DNA scission Toxic during S-phase IV   Excreted in bile Reversible acute & irreversible chronic cardiomyopathies Myelosuppressive   Red urine- not blood GI   One of the most widely used ABVD- Hodgkin CHOP- non-Hogkin CAF- breast M-VAC- bladder carcinoma VAD- multiple myeloma   Leukemias Lymphomas Thyroid GIST Ovarian Sm-cell lung
Bleomycin (Blenoxane)
Mixture of copper-chelating glycopeptides produced by Streptomyces verticillus Causes DNA chain scission & fragmentation Oxidative release of bases Cells with chromo aberrations accum in the G2 phase   It is inactivated by bleomycin hydrolase- found in many tissues (except skin & lung) Parenterally Dose-related pulmonary toxicity that may be fatal Cutaneous toxicity – hyperpigmentation, ulceration   R- increased levels of hydrolase or increased DNA repair Testicular carcinoma Squamous cell carcinoma ABVD- Hodgkin & non-Hodgkin
Cisplatin (Platinol)
Small platinum coordination complex that enters cells by diffusion and active transport Intracellular replacement of its chloride atoms by H2O Complexing w DNA to form crosslinks Adj guanines are most freq crosslinkedàinhibition of DNA rep & trans Effects most prominent during S phase IV   Slow renal excretion Dose-limiting toxicity is cumulative damage to the renal tubules- may be irrev @ high doses Prevented by hydration and diuresis   Nausea Vomiting   Ototoxic Peripheral neuropathy   Moderately myelosuppressive Testicular tumors (w. bleomycin & vinblastine PVB) Head & Neck Ovarian (w. doxorubicin) Bladder carcinomas    
Mitomycin C
Metabolically active to a bifxnal alkylating agent Very reactive     Palliative regiment for gastric cancer FAM
Carboplatin (CBDCA) (JM-8) (Paraplatin)
IV Less severe toxicities Myelosuppression- dose-limiting toxicity *Ovarian cancer Non-Hodgkin Non-sm cell lung Testicular Transitional in UT
Procarbazine (Matulane)
Substituted hydrazine that needs to be activated metabolically Produces chromo breaks & inhibits DNA & RNA & protein synthesis - denaturation   Lipophilic- enters cells by diffusion Found in CSF Oral Leukopenia Thrombocytopenia GI   Myelosuppression is dose dependent   Augments the effects of sedatives Infertility Weak MAOI – may cause HTN (esp w. high tyramine content food)   10% risk in causing acute leukemia MOPP-Hodgkin Non-hodgkin Brain tumor
Hydroxyurea (Hydrea) (Droxia)
Inhibits ribonucleoside diphosphate reductase which catalyzes the conversion of ribonucleotides to deoxyribonucleotides and is crucial for the synthesis of DNA -during S phase   Oral   Excreted in the urine Hematopoietic depression Chronic Granulocytic leukemia Synergizes with radiotherapy
L-asparaginase (Elspar)
Some neuplastic cells have low/no asparagine synthestase so require exogenous asparagine for growth   Enzyme that reduces levels of L-asparaginase, an aa not synthesized by some tumors, to inhibit protein synthesis and cell division   Synergistic with MTX when the folic acid analogue is admin prior to L-asp IV IM Minimally marrow suppressive Toxic to the liver and pancreas   HS   Hemorrhaging due to the inhibit of clotting factor synthesis Lymphoblastic leukemia Induction of remission of ALL (vincristine/prednisone)
IL-2 (Aldesleukin) (Proleukin)
Metastatic kidney cancer Melanoma
IFN a-2b (Intron-A)
Hairy cell leukemia Kaposi
Lenalidomide (Revlimid)
Tumor necrosis factor modifiers Analog of thalidomide- increased potency   Decreased toxicity
Thalidomide (Thalomid)
Tumor necrosis factor modifiers Assist in the degradation of THF-a mRNA encoding protein   Sedation Constipation Peripheral neuropathy (30%)   Highly teratogenic Brain tumor Kaposi Multiple myeloma
Imatinib (Gleevec) Dasatinib (Sprycel)
Specific for Bcr-Abl oncoprotein Inhibits other kinases Oral Edema Nausea Vomiting Chronic myelogenous leukemia GI stromal tumors GIST (c-kit) Specific for Bcr-Abl oncoprotein   Oral Edema Nausea Vomiting Chronic myelogenous leukemia ALL
Gefitinib (Iressa) Erlotinib (Tarceva)
Inhibitor of EGFR TK Oral Severe diarrhea Acne Derm Non-sm cell lung (gemcitabine/cisplatin) Inhibitor of EGFR TK Oral Rash Diarrhea Cough Non-sm cell lung Advanced pancreatic cancer
Rituximab (Rituxan)
Chimeric Ab to IgG that binds to CD20 Ag on B cells Cell lysis (secondary to ADCC)   Derm GI   Neutropenia Used for relapsed Non-Hodgkin lymphoma (R-CHOP) Mantle cell lyphoma
Trastuzumab (Herceptin)
Humanized IgG Ab against the EGFR HER2/neu which is overexpressed in 25-30% of breast cancers Expression of this proteinàdecreased survival due to more aggressive disease Net effect =arrest of the cell cycle via Ab-mediated cytotoxicity   Diarrhea Hematological effects HER2/neu + breast cancers w. paclitaxel
Cetuximab (Erbitux)
Chimerica IgG Ab to EGFR Actually blocks the receptor unlike imatinib Inhibition of cancer cell growth & induction of apoptosis Overexpression of EGFR in crc is assoc w/ decreased survival   Severe rash EGFR crc (w. irinotecan)
Bevacizumab (Avastin)
1st humanized IgG directed against human VEGF interaction w. receptor (angiogenesis)   Derm GI   Proteinuria HTN Congestive HF   Bowel perforation- rare Metastatic colon cancer w/ 5-FU
prednisone - (hydroxycortisone) (dexamethasone)
Lymphocytic & antimitotic Oral Significant systemic effects- no long term use Psych Acute leukemia in children Malignant lymphoma Hodgkin Non-hodgkin (CHOP & MOPP)  
Mitotane (o,p-DDD) (Lysodren)
Inhibits GC synthesis Causes atrophy of the tumors w/in zona reticularis & fasciculate by unknown mxn Oral CNS depression dose-limiting toxicity Nausea Vomiting Lethargy Derm Inoperable adrenocortical carcinoma
Megestrol (Megace) Hydroxyprogesterone Medroxyprogesterone
Progestin Treatment -Endometrial hyperplasia & carcinoma 2nd line therapy for metastatic hormone-dependent breast cancer   Used to stimulate appetite & in AIDS related cachexia
Somatostatin
Growth hormone release inhibiting hormones Natural growth inhibitor

Txt for pancreatic islet tumors
Diethylstilbestrol
Inhibit the effects of endogenous androgens   Cardiac & cerebrovascular complications Carcinoma breast/endometrium/ovary Androgen-dep metastatic carcinoma   Combine w/ orchiectomy
Leuprolide (Lupron)
Admin w. anti-androgen flutamide or bicalutamide which block the translocation of androgen receptors to the nucleus- prevent testosterone action   Initial admin may cause increased levels of LH/FSH- & testosterone- exacerbation of disease Prostatic carcinoma Estrogen+ breast cancer
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