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Pharm Exam II
Antineoplastics
| What is MOA? | Class/ Subclass1/Subclass 2 | Structure | Indication | Adverse Effects | Metabolism/ T1/2 | Drug |
|---|---|---|---|---|---|---|
| Inhibits Dihydrofolate Reductase; without it, cannot convert dietary folate to tetrahydrofolate req'd for thymidine & purine synth. | Anti-neoplastic - DNA synth inhib; Folate Antagonist | Folic Acid Analog | Immunosuppression, Varied - ALL, Meningeal Mets, trophoblastic tumors, breast CA, non-Hodgkin's lymphoma | Myelosuppression (bone marrow, GI), oral ulceration | Mostly eliminated as parent compound & metabolites in urine | Methotrexate |
| Blocks DNA synthesis by: inhibition of DNA Polymerase and & incorporates into the tumor cell's DNA - thereby inhibiting production of cytosine | Anti-neoplastic - DNA Synthesis Inhibitor & Pyrimidine Antagonist | Cytosine Analogue | AML (Acute Myeloid Leukemia) | N/V (mild)/Myelosupression/Oral & GI ulceration; High doses will damage liver, heart, other organs | this is a prodrug req's tumor cell enzymes to convert to active metabolite; Can be admin. IV or Sub cu; If given parenterally: extensively metabolized before renal excretion; crosses blood-brain barrier | Cytarabine |
| Two, b/c two active metabolites: 5FdUMP: inhibits thymidylate synthetase thus preventing synthesis of thymidine; then 5FdUTP incorporates into the tumor cell's RNA & interferes with RNA function | Anti-neoplastic - DNA Synthesis Inhibititor & Pyrimidine Antagonist | Thymine Analogue | Solid tumors ONLY; breast, colorectal, gastric tumors, Squamous cell tumors in head & neck | N/V (mild)/Myelosupression (esp. after bolus injection)/Oral & GI ulceration; High doses will damage liver, heart, other organs | this is a prodrug req's tumor cell enzymes to convert to active metabolite;Can be admin. IV or topically; If given parenterally: extensively metabolized before renal excretion | Fluorouracil |
| This is a prodrug; Forms cross links (covalent bonds) between itself and guanine b/c attack the N7 nitrogen of guanine; this keeps DNA from uncoiling when needed for replication | Anti-neoplastic - DNA Alkylating Drug; Immunosuppressant | (blank) | IV, Orally (completely absorbed); ALL, CLL, non-Hodkin's, breast, lung and ovarian cancer (also rheumatoid dz, autoimmune nephrititis) | Alopecia/N/V (mild if P.O., but severe if IV)/ Myelosuppression (this is the side effect that is the DOSE LIMITING TOXICITY), Hemorrhagic cystitis (b/c partly converted to acrolein) | Cytochrome P450 - active metabolite: phosphoramide | Cyclophosphamide |
| This Rx is converted to active intermediate after reacting w/ H2O; this causes a rxn bet. it & guanine; this leads to intrastrand cross linking in neighboring guanine residues; x-links cause DNA to bend, lose norm conformation & therefore fxn. | Anti-neoplastic - DNA Alkylating Drug, Platinum Compound | Inorganic Platinum Derivative | 1st Line Rx for: testicular, ovarian, cervical & bladder cancers; also used in Melanoma & other solid tumors | N/V/ Nephrotoxicity (b/c lose K & Mg leading to dec. glomerular filtration) | Kidneys | Cisplatin |
| inserts self into DNA by binding between paired bases; this distorts the structure & causes uncoiling; also inhib. enzyme topo II | Anti-neoplastics - DNA Intercalating | (blank) | IV; Broad spectrum: most active Rx against breast CA; used in Hodkin's dz, bladder CA, Ovarian CA, Gastric Cacinoma, other hematologic CA's & | MAIN ONE: Cardiotoxicity,N/V/ Alopecia, Mucosal Ulcers/ Myelosuppression | Met. in liver; Lg volumes of dist. & t1/2; DO NOT admin. w/ cyclosporine, cyclophosphamide & mercaptopurine (Inc. toxicity); Verapamil (can cause inc. of cytotoxicity b/c inhib Pgp which transports anthracylines out of cells | Doxorubicin |
| Greatest effect during G2 phase; intercalates DNA & also causes cytotoxicity by an iron-catalyzed free-radical formation & DNA strand breakage | Anti-neoplastics - DNA Intercalating | Mix of two peptides | Most widely used anti-tumor Abx; useful in Hodgkin's & non-Hodkin's lymphoma; testicular Ca & other solid tumors | Most serious: Pneumonitis that can lead to interstitiala fibrosis & Skin findings; Extravasation during IV/ Myelosupression (v. lil)/ Cardiotoxicty (BOTH of these being THE dose-limiting effects)/ N/V (dose-related) | Widely distributed; Excreted Renally; DO NOT admin. w/ cyclosporine, cyclophosphamide & mercaptopurine (Inc. toxicity); Verapamil (can cause inc. of cytotoxicity b/c inhib Pgp which transports anthracylines) | Bleomycin |
| M-phase specific: Mitosis Inhibitor via interference of microtubule fxn: by binding to tubulin & blocking tubulin polymerization, there is no spindle formation & thus no cell division | Anti-neoplatic - Mitosis Inhibitor - Microtubule DEstabilizer | Vinca Alkaloid from periwinkle | Hematologic CA's; some solid tumors like sm. cell carinoma, neuroblastoma, sarcoma | Dose-limiting Neurotoxicity (Peripheral Neuropathy | Extensive Metab.; Excretion via biliary excretion | Vincristine |
| Binds to tubulin & blocks depolymerization of tubulin | Anti-neoplastic - Mitosis Inhibitor - Microtubule Stabilizer | Plant Alkaloid from Yew trees | 1st line Tx in: mets ovarian CA (combo'd w/ Cisplatin); non-small cell carcinoma; Tx of mets breast CA unresp. to 1st line Tx | Dose-limiting Myelosuppression (part. Neutropenia); also can cause Neurotoxicity./ Alopecia | Admin. via IV; Elimination via metabolism & biliary excretion | Paclitaxel |
| Inhibit the re-sealing of breaks in double-stranded DNA | Anti-neoplastic - Topoisomerase Inhibitor (Topo II) | Natural substance extracted fr. Madrake or mayapple plant; Semisynthetic: Etoposide | Broad-spectrum: hematologic cancers & solid tumors, esp. testicular CA, lung Ca, non-Hodgkin's lymphoma | Well-tolerated; Dose limiting: Myelosuppression; mild N/V; Alopecia (& low-incidence of 2dary nonlymphocytic lymphoma) | Bioavailability varies greatly if admin. P.O.; Eliminated Unchanged in Urine | Etoposide |
| Prevents re-sealing of nicks in single strands of DNA | Anti-neoplastic - Topoisomerase Inhib. (Topo I) | Camptothecin Analogues | Admin. IV; Recurring colon Cancer or progressive colon CA after fluorouracil Tx | Dose-limiting toxicity: Myelosuppression; diarrhea/mild N/V/ Alopecia | Rapid metab. into active Metabolite (SN-38); Eliminated primarily via bile | Irinotecan |
| Inhibits estrogen in tumor cells that are estrogen-receptor positive; inhibits proliferation of the cancerous cells | Anti-neoplastic - Estrogen Antagonist | Estrogen R. Antagonist | Admin. orally for Breast CA; adjuvant Tx | N/V/ Hot flashes/ Vaginal bleeding/ Inc. risk of endometrial CA | Well absorbed in gut; then converted to sev. metabolites in liver; enterohepatic cycling & biliary excretion; t1/2: 7 days | Tamoxifen |
| given continously (rather than in pulsatile fashion) causing a negative feedback mech. whereby LH secretion by pituitary is suppressed | Anti-neoplastic - GnRH Agonist (but Anti-androgen) | GnRH Analogue | Tx of inoperable prostate cancer | (blank) | (blank) | Leuprolide |
| Competitive Antagonism w/ testosterone for Androgen R. thereby blocking testosterone stimulation of prostate carcinoma cells | Anti-neoplastic -Anti-adrogen | (blank) | Tx of inoperable prostate CA | N/ Gynecomastia/ Impotence/ Hot flashes/ hepatitis | (blank) | Flutamide |
| cause lymphocytotoxic effect | Anti-inflammatory - Glucocorticosteroid | (blank) | Lymphocytic leukemias, lymphomas, multiple myeloma | No myelosuppression or other serious organ damage in most; often used in combo w/ Rx's that affect DNA fxn or mitosis | Intermediate-acting | Prednisone |
| binds to CD20 antigen (believed to reg. early step in cell cycle initiation) found on surface of over 90% of non-Hodgkin's lymphoma cells (& norm. B lymphocytes) | Monoclonal Antibody (tu - tumor, xi - chimeric) | Human-murine antibody | Relapsed or refractory non-Hodgkin's lymphoma | (blank) | Given IV | Rituximab |
| Binds to the Epidermal Growth Factor R. (EGFR) that's over-expressed in cert. human cancers (part. Colon CA) | Monoclonal Antibody - Cetuximab (tu - tumor, xi - chimeric | EGFR Human-murine antibody | Colon Cancer in combo with Irinotecan | Acne-like skin rash; 3% of patients: hypersensitivity | (blank) | Cetuximab |
| antibody against VEGF; prevents biding of VEGF to receptors on endothelial cells & thus inhib. new blood vessel formation - something tumor cells need to survive | Monoclonal Antibody - Bevacizumab (ci- circulation; u - human) | VEGF Human antibody | Colon Cancer given in combo with Irinotecan | GI bleed/ perforation; Pulm. hemorrhage; other thromboembolic events | (blank) | Bevacizumab |
| inhibits the bcr-Abl tyrosine kinase expressed by Philadelphia chromosome in CML; therefore inhibits leukemic cell proliferation & induces apoptosis; also inhibits c-kit activity | Monoclonal Antibody - Imatinib | bcr-Abl tyrosine kinase inhibitor | 1st line Tx of Chronic Myeloid Leukemia; GI stromal tumors | (blank) | (blank) | Imatinib |
| Aromatase inhibitor: this inhibition prevents the transformation of sex hormones into estrogen needed by breast cancer tumors in post-menopausal women for tumor growth | Anti-neoplastic/ Anti-estrogen | (blank) | Breast Cancer | (blank) | (blank) | Anastrozole |
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