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Chemotherapy
Abx and Cancer Drugs
136
Medical
Graduate
06/14/2009

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Term
Quinupristin/Dalfopristin
Definition
For Gram positive (staph, strep. enterococcus) that are Vancomycin resistant. Give IV. Pain, arthralgia, and thrombophlebitis are common.
Term
Linezolid
Definition
For gram positives that are vancomycin resistant. Broader spectrum than Quinupristin/Dalfopristin. Give orally. Reversible thrombocytopenia.
Term
Sulfonamides
Definition
Analogs of PABA, block synthesis of Folic Acid. Crystalize in acidic urine, broad spectrum
Term
Trimethoprim
Definition
Trimethoprim inhibits dihydrofolate reductase. Give with a Sulfa, which blocks PABA, for sequential inhibition.
Term
Flucytosine (5-fluorocytosine)
Definition
Metabolized to 5-FU by fungi. Blocks nucleic acid synthesis. Oral, excreted unmetabolized. Depresses bone marrow, GI upset.
Term
Nitrofurantoin
Definition
Urinary tract antiseptic. Resistance is rare. Damages DNA.
Term
Methenamine
Definition
Decomposes in water to formaldehyde, especially in acidic conditions, i.e. urine. Broad spectrum. DO NOT MIX WITH SULFONAMIDES
Term
Acyclovir
Definition
Guanosine nucleoside analog. Good vs. Herpes, CMV, Epstein-Barr virus. Chain terminator, give oral or topical, goes to CSF. (Metabolized by viral kinases, which activate it's chain terminating properties)
Term
Gancyclovir
Definition
Guanosine nucleoside analog. Good vs Herpes and CMV. Given orally. TERATOGENIC, affects bone marrow
Term
Iododeoxyuridine
Definition
Thymidine analog, good vs Herpes (DNA viruses). Incorporated into DNA. Very toxic, use only topically, ex. for conjuctivitis
Term
Vidarabine
Definition
Adenosine analog. Good for DNA viruses. Given with Acyclovir sometimes. Chain terminator.
Term
Adefovir didivoxil
Definition
Adenosine analog. Given orally as a pro-drug. Inhibits viral polymerase.
Term
Amantadine
Definition
Specific for Influenza A. Inhibits proton channel M2, prevents acidification of vesicle and uncoating of virus. Some CNS problems in 1/3 or patients. High resistance rates
Term
Oseltamivir
Definition
Treatment and prevention of Influenza A. Inhibits viral neuraminidase
Term
Zanamivir
Definition
Treatment and prevention of Influenza A and B. Targets viral neuraminidase. Taken as an inhaled powder.
Term
Interferons
Definition
Used for Hepatitis B & C. Block penetration, uncoating, RNA and protein synthesis. Usually use alpha (cells make beta)
Term
Lamivudine
Definition
Cytosine analog. Targets Hepatitis B, inhibits DNA polymerase and reverse transcriptase. Taken as a powder.
Term
Lamivudine
Definition
Cytosine analog. Targets Hepatitis B, inhibits DNA polymerase and reverse transcriptase. Taken as a powder.
Term
Zidovudine (AZT)
Definition
Thymidine analog. Blocks reverse transcriptase (good vs HIV), taken orally. Causes fatigue, anemia. Metabolized by liver, renal excretion.
Term
Didanosine
Definition
Purine nucleoside analog (adenosine), blocks reverse transcriptase (good vs HIV) Given orally with an antacid. Can cause peripheral neuropathy.
Term
Nevirapine
Definition
Non-nucleoside reverse transcriptase inhibitor (good for HIV). Given orally, but can cause liver toxicity.
Term
Efavirenz
Definition
Non-nucleoside reverse transcriptase inhibitor. Given orally, some CNS toxicity in half of patients (abnormal dreams, impaired concentration)
Term
Indinavir
Definition
Viral protease inhibitor. Causes liver toxicity, hyperglycemia, hyperlipidemia, fat redistribution
Term
Enfuvirtide
Definition
Inhibits fusion of HIV with CD4+ cells. Expensive.
Term
Maraviroc
Definition
Binds to CCR5 co-receptor on CD4+ T cells, blocking HIV. No effect on CXCR4 receptor. Oral.
Term
Trastuzumab
Definition
Monoclonal antibody that targets HER2 gene. For breast cancer. Loss of gene PTEN predicts resistance to treatment with Trastuzumab.
Term
Rituximab
Definition
Monoclonal antibody for B-Cell lymphoma. Targets a surface Ag.
Term
Imatinib
Definition
Tyrosine Kinase inhibitor, for chronic myeloid leukemia. Can cause neutropenia, thrombocytopenia.
Term
Gefitinib
Definition
Blocks growth signals mediated by tyrosine kinase, good against TK associated with Epidermal Growth Factor (EGF). Good for advanced non-small cell lung cancer.
Term
Cetuximab
Definition
Monoclonal antibody against epidermal growth factor receptor (EGFR)
Term
Avastin
Definition
Antibody, targets Vascular Endothelial Growth Factor (VEGF). Anti-cancer.
Term
Sorafenib and Sutent
Definition
Newer tyrosine kinase inhibitors, act on Vascular Endothelial Growth Factors (VEGF), anti-cancer.
Term
miRNA and siRNA
Definition
siRNA- breakdown of target mRNA. miRNA - interferes with translation
Term
Temozolomide
Definition
An alkylating agent, most effective in patients with methylated MGMT (an enzyme that repairs alkylation damage to DNA)
Term
Sarcosine
Definition
Important metabolite for monitoring prostate cancer cell activity: measure of aggresiveness
Term
Dolasetron
Definition
Serotonin receptor antagonist, prevents nausea and vomiting due to cancer chemotherapy
Term
Palonosetron
Definition
Serotonin receptor antagonist, prevents nausea and vomiting due to cancer chemotherapy
Term
Dexamethasone
Definition
A corticosteroid that prevents nausea and vomiting due to cancer chemotherapy
Term
Chlorambucil
Definition
Alkylating agent, good vs. chronic leukemias, least toxic alkylating drug (ergo, good for chronic conditions)
Term
Cyclophosphamide
Definition
Alkylating cancer chemotherapy, requires metabolic activation in liver. Causes some liver toxicity and requires a normal liver.
Term
BCNU
Definition
Alkylating cancer chemotherapy. Lipid soluble, goes to CNS.
Term
Busulfan
Definition
Alkylating cancer chemotherapy
Term
Methotrexate
Definition
Folic acid analog (antimetabolite). Cycle active- affects DNA synthesis, kills replicating cells. Can not be administered if renal function is impaired. (Similar to trimethoprim, but works on mammals).
Term
Folinic Acid
Definition
Can 'rescue' methotrexate-induced host toxicity
Term
6-Mercaptopurine
Definition
Purine analog- inhibits purine nucleotide synthesis. Cancer chemotherapy.
Term
Thioguanine
Definition
Purine analog. Metabolism required. Cancer chemotherapy.
Term
5-Fluorouracil (5-FU)
Definition
Pyrimidine analog. Cancer chemotherapy. Causes hair loss.
Term
Cytarabine
Definition
Pyrimidine analog, cancer chemotherapy.
Term
Gemcitabine
Definition
Non-cycle active, pyrimidine analog. Metabolism required. Inhibits DNA synthesis and DNA template activity. Good vs. a variety of solid tumors.
Term
Tegafur
Definition
Pro-drug, metabolized to fluorouracil
Term
Uracil
Definition
Competitive inhibitor of dihydropyrimidine dehydrogenase- results in higher plasma levels of fluorouracil than protracted IV fluorouracil
Term
Taxol
Definition
Blocks microtubule formation and mitosis (cycle active). Cancer chemotherapy
Term
Vincristine
Definition
Inhibits mitosis, cycle active, for acute leukemia. CNS toxic. (A VincaAlkyloid)
Term
Vinblastine
Definition
Inhibits mitosis (metaphase arrest) cycle active. For Hodgkins disease, testicular tumors, solid tumors.
Term
Actinomycin D
Definition
Inhibits RNA synthesis, NON-cycle active. Very toxic. (Cancer chemotherapy)
Term
Bleomycin
Definition
Causes DNA strand breaks. Non-cycle active. For testicular cancer, lymphomas, solid tumors
Term
Doxorubicin
Definition
Blocks RNA synthesis, non-cycle active, CNS tumors. Cardiac toxicity and hair loss.
Term
Mitomycin
Definition
Alkylating agent, for solid tumors.
Term
Tamoxifen
Definition
Antiestrogen, blocks estrogen mediated cell division. Metabolized in liver to active form by CYP2D6, which also metabolizes Paxil and Prozac- don't give w/ those drugs.
Term
Flutamide
Definition
Anti-androgen, for metastatic prostate cancer. Life prolonging, oral drug. May cause gyenecomastia.
Term

Cisplatin

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Definition
Similar to alkylating agents. Prevents cell division, renal toxicity. Given IV.
Term
Vancomycin
Definition
Inhibits peptidoglycan formation, narrow spectrum (G+), nephrotoxic and causes hearing loss.
Term
Bacitracin
Definition
Topical, use for G+, inhibits peptidoglycan formation. Can be used for GI infections.
Term
Penicillin G
Definition
Low acid stability, sensitive to penicillinase, narrow spectrum. Given by shot.
Term
Phenoxymethyl Penicillin (Pen V)
Definition
High acid stability, sensitive to penicillinase, narrow spectrum
Term
Methicillin
Definition
Low acid stability, not sensitive to penicillinase, narrow spectrum
Term
Dicloxacillin
Definition
High acid stability, no penicillinase sensitivity, narrow spectrum
Term
Nafcillin
Definition
Low acid stability, no penicillinase sensitivity, narrow spectrum
Term
Augmentin
Definition
Amoxicillin + clavulanic acid. High acid stability, sensitive to penicillinase (but protected by clavulanic acid). Broad spectrum
Term
Ticarcillin
Definition
Low acid stability, sensitive to penicillinase, broad spectrum
Term
Piperacillin + Tazobactam
Definition
Low acid stability, sensitive to penicillinase (protected by Tazobactam), broad spectrum
Term
Which Penicillins are penicillinase resistant?
Definition
Oxacillin, Dicloxacillin, Cloxacillin are narrow spectrum, and penicillinase resistant
Term
Carbenicillin
Definition
Not orally administered penicillin
Term
Azlocillin
Definition
New, broad spectrum penicillin. Given IV. Some bone marrow suppression.
Term
Which antibiotics are effective against anaerobes?
Definition
Piperacillin, Clindamycin, Imipenem (a carbapenem) and 3rd generation cephalosporins
Term
Cephalexin, Cephazolin
Definition
1st gen Cephalosporins. Similar to broad spectrum penicillins
Term
Cefaclor
Definition
2nd gen cephalosporin
Term
Cefotaxime, Cefixime
Definition
3rd gen. cephalosporins. Good vs. anaerobes. More effective against G- than G+, also distribute to CNS
Term
Cefipime
Definition
4th gen cephalosporin. Renal toxicity, never give a cephalosporin with an aminoglycoside
Term
Imipenem
Definition
Carbapenem. VERY broad spectrum. Must be given IV with cillistatin to prevent renal degredation.
Term
Meropenem
Definition
Carbapenem. VERY broad spectrum. Must be given IV with cillistatin to prevent renal degredation.
Term
Ertapenem
Definition
Carbapenem. VERY broad spectrum. Must be given with Cillistatin to prevent renal degradation.
Term
Monobactams
Definition
Broad for G-, but also good for G+ staph. infections. Given IV.
Term
Polymyxin
Definition
Disrupts cell membrane (bacteriocidal). Nephrotoxic, topical use only. Narrow spectrum, G-, resistance is rare. Good for Pseuodmonas
Term
Amphotericin B
Definition
Binds to ergosterol receptors on cell membrane. Very nephrotoxic. Given IV.
Term
Nystatin
Definition
Binds to ergosterol on cell membrane. Antifungal. Very nephrotoxic, topical use only.
Term
Ketoconazole
Definition
Inhibits 14-alpha-sterol demethylase. Anti-fungal specific. Does not got to CNS, given orally. Decreases steroid biosynthesis.
Term
Itraconazole
Definition
Inhibits 14-alpha-sterol demethylase. Low gastric pH enhances absorption. No CNS.
Term
Fluconazole
Definition
Inhibits 14-alpha-sterol demethylase. Does go to CNS. Anti-fungal. Azole antifungals can inhibit cyp450 metabolism of other drugs, may cause anorexia, vomiting.
Term
Terbinifine
Definition
Inhibits squalene epoxidase. Can't combine w/ Amphotericin B because it reduces ergosterol.
Term
5-Fluorocytosine
Definition
Metabolized to 5-FU by fungi. Suppresses bone marrow.
Term
Ciprofloxacin and Levofloxacin
Definition
Fluoroquinolones. Inhibit bacterial gyrases and topoisomerases. Good vs G- bacilli (not anaerobes). Active in urine, good for UTIs. Cartilage damage- not for kids.
Term
Rifampin
Definition
Inhibits RNA polymerase, blocks initiation. More effective vs G+. Turns fluids orange. Renal excretion, cannot give if person has renal insufficiency. Increases metabolism of other drugs, especially anticoagulants. TERATOGENIC
Term
Nitrofurantoin
Definition
Damages bacterial DNA. Metabolized to active form. Resistance is rare. Turns urine brown.
Term
Aminoglycosides
Definition
Inhibit protein synthesis. Good for G- bacilli, and Staph. Renal toxicity, especially if given w/ a Cephalosporin. Ototoxicity (CN VIII). Blocks NMJ. Good hydration to avoid toxicity. Use for pseudomonas or klebdiella. May induce biofilms.
Term
What are the four aminoglycosides?
Definition
Gentamicin, Amikacin, Tobramycin, Netilmicin
Term
Tetracyclines
Definition
Decrease protein synthesis and inhibit tRNAs. Can cause discoloration of teeth and phototoxicity. Also kill normal flora, can lead to superinfection. Bind to 30s subunit.
Term
Name the four Tetracycline drugs.
Definition
Tetracycline, Oxytetracycline, Doxycyline (IV or Oral) and Minocycline (Oral only.) Very broad spectrum, even vs Entamoeba, mycoplasma, chlamydia
Term
Chloramphenicol
Definition
Broad spectrum (including rickettsiae). Goes to total body water. Conjugated to glucuronic acid by liver. May cause aplastic anemia or bone marrow suppression. Can cause cardiovascular toxicity in children.
Term
Erythromycin
Definition
Mostly G+, binds 50s subunit. Injection is painful, oral better. No CNS, not good for UTIs, mild liver toxicity.
Term
Clarithromycin
Definition
Macrolide (binds 50s subunit) slightly broader than erythromycin
Term
Azithromycin
Definition
Better than erythromycin, longer half life, broader spectrum
Term
Telithromycin
Definition
Macrolide. Alters taste perception, liver toxicity. Limited to serious respiratory tract infections.
Term
Probenicid
Definition
Uricosuric agent, reduces reabsorption of uric acid to prevent gout. Can NOT be given with salicylates, or to people with uric acid kidney stones.
Term
Sulfinpyrazone
Definition
Uricosuric agent, reduces reabsorption of uric acid to prevent gout. Can NOT be given with salicylates, or to people with uric acid kidney stones.
Term
Febuxostat
Definition
Selective inhibitor of xanthine oxidase. Prevents formation of uric acid, to combat gout.
Term
Allopurinol
Definition
Inhibits xanthine oxidase and uric acid formation. Does not alter acute goute attacks.
Term
Colchicine
Definition
For gout. Inhibits activation of leukocytes. Not for use during pregnancy, use with caution in cases of hepatic or renal failure or cardiovascular disease. Anti-inflammatory.
Term
CTLA4Ig
Definition
Binds to substrates of CD28 (CD80 and CD86)which prevents T cell activation. Inhibits disease progression. Anti-inflammatory.
Term
Omalizumab (anti-IgE)
Definition
inhibits immune system response to allergens (anti-inflammatory)
Term
Glatiramer acetate
Definition
Binds to MHC class II molecules and competes with myelin antigens. For Multiple Sclerosis (MS). Anti-inflammatory.
Term
Cortistatin
Definition
Binds to immune cells (anti-inflammatory)
Term
Efalizumab
Definition
Monoclonal antibody against CD11a, which is important for PMN migration. Anti-inflammatory.
Term
Leflunomide
Definition
Inhibits synthesis of pyrimidines, decreases lymphocyte proliferation. Liver toxicity, initial hypertension. Anti-inflammatory
Term
Hydroxychloroquine
Definition
anti-inflammatory
Term
Azathioprine
Definition
Inhibits synthesis of purines. Anti-inflammatory.
Term
Anakinra
Definition
IL-1 receptor antagonist (anti-inflammatory)
Term
Tocilizumab
Definition
Monoclonal AB that acts as an antagonist to IL-6. Anti-inflammatory
Term
Adalimumab and Infliximab
Definition
Monoclonal antibodies that bind TNF. Anti-inflammatory
Term
Etanercept
Definition
Mimics TNF receptor. Anti-inflammatory.
Term
Zafirlukast
Definition
Leukotriene receptor antagonist. For asthma.
Term
Montelukast
Definition
Leukotriene receptor inhibitor. For asthma.
Term
Zileuton
Definition
Blocks synthesis of leukotrienes. Used to treat asthma.
Term
Acetaminophen
Definition
Tylenol, COX inhibitor. Analgesic, antipyretic, NOT anti-inflammatory. May cause allergy or HEPATIC NECROSIS. Increases risk of renal failure. No GI irritation or changes to bleeding time.
Term
Glucocorticoids
Definition
Induce lipocortin (inhibits phospholipase A2), inhibits APP, inhibits cytokines.
Term
COX2 inhibitors
Definition
May cause MI's, or toxic epidermal necrosis and Stevens-Johnson syndrome
Term
Propionic Acid derivatives (ex. Ibuprofen, naproxen, -EN)
Definition
Reversible inhibition of COX, better tolerated than aspirin. Not for pregnant women. May cause tinnitus, peripheral edema, rash.
Term
Aspirin
Definition
Prototypical salycilate. Inhibits COX irreversibly. Good for arthritis, pain, fever, bad for children (Reye's syndrome), tinnitus and hearing loss
Term
Acetaminaphen
Definition
Tylenol.  Good for fever and pain, but not inflammation.  Can cause liver necrosis.  No GI effects, no increase in bleeding time.
Term
Name 3 antiinflammatory steroids
Definition
Prednisone, Prednisolone, Hydrocortisone
Term
Misoprostol
Definition
PGE1 analog, given with NSAIDs to minimize adverse GI effects
Term
Name 6 uses of  NSAIDS
Definition
Antipyretic, pain, inflammation, close ductus arteriousus in infants, treat thromboembolic disorders, prophylaxis for high risk colon cancer
Term
Name two proprionic acid derivatives
Definition
Ibuprofen and Naproxen
Term
Indomethacin
Definition
An acetic acid derived  NSAID, with high incidence of CNS side effects
Term
Name 5 antimetabolites (that block purine synthesis [2]and pyrimidine synthesis [3])
Definition
Purine synthesis: 6-mercaptopurine and thioguanine.  Pyrimidine synthesis: 5-FU, cytarabine, gemcitabine.  They  must be metabolized.
Term
Retampulin
Definition
Topical antibiotic for Staph. and Strep. Binds to 50s subunit, inhibits both peptide bond formation and binding of tRNA to ribosome
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