Chemotherapeutics Review 14 July :22 AM

Abacavir Antiretroviral Nucleoside reverse transcriptase inhibitor (NRTI)

Acyclovir Antiherpes Purine analog Phosphorylated to inhibitor of viral DNA polymerase

Albendazole Antihelminthic Treatment of intestinal roundworms

Alemtuzumab Antineoplastic Anti-CD52 antibody

Amantadine Antiviral Antiparkinson Treatment of Influenza A Inhibits replication at the stage of uncoating

Amikacin Aminoglycoside antibiotic Bactericidal protein synthesis inhibitor 30S ribosome Freezes initiation

Aminoglutethimide Antineoplastic Immunosuppressive Glucocorticoid antagonist Aromatase inhibitor (decreases steroid synthesis)

Aminoglycosides Antibiotics Bactericidal protein synthesis inhibitors 30S ribosome Freeze initiation

Ampicillin Penicillin antibiotic Cell wall synthesis inhibitor Amino penicillin Inhibits peptidoglycan cross-linking

Amphotericin B Antifungal Polyene antibiotic Binds to ergosterol and alters permeability Systemic

Amsacrine Antineoplastic Miscellaneous

Anastrozole Antineoplastic Antiestrogen Aromatase inhibitor

Anti-thymocyte globulin Immunosuppressive Anti-T cell antibody

Arsenicals Tropical antiparasitic Treatment of African Trypanosomiasis in CNS Melarsoprol

L-asparaginase Antineoplastic Protein synthesis inhibitor

Atovaquone Antimalarial Depolarizes parasitic mitochondria and inhibits electron transport

Azathioprine Immunosuppressive Antineoplastic Antimetabolite (“pseudofeedback inhibition” of HGPRT and PRP)

Azithromycin Macrolide antibiotic Bacteriostatic protein synthesis inhibitor 50S ribosome Inhibits translocation

Aztreonam New  lactam antibiotic Monobactam

Bacitracin Antibiotic Cell wall synthesis inhibitor Topical, not a  lactam, Inhibits dephosphorylation of bactoprenol

Basiliximab Immunosuppressive Anti-CD25 (interleukin 2 receptor) Organ transplant (antirejection)

Benzathine penicillin G Penicillin antibiotic Cell wall synthesis inhibitor Inhibits peptidoglycan cross-linking Repository preparation

Bleomycin Antineoplastic Natural product Antibiotic

Busulfan Antineoplastic Alkylating Agent

Carbenicillin Penicillin antibiotic Cell wall synthesis inhibitor Anti-pseudomonal penicillin Inhibits peptidoglycan cross-linking

Carmustine (BCNU) Antineoplastic Alkylating Agent

Cefaclor Cephalosporin antibiotic Cell wall synthesis inhibitor 2 nd generation Oral

Cefadroxil Cephalosporin antibiotic Cell wall synthesis inhibitor 1 st generation Oral

Cefepime Cephalosporin antibiotic Cell wall synthesis inhibitor 4 th generation CSF penetration

Cefotaxime Cephalosporin antibiotic Cell wall synthesis inhibitor 3 rd generation CSF penetration

Cefoxitin Cephalosporin antibiotic Cell wall synthesis inhibitor 2 nd generation

Ceftazidime Cephalosporin antibiotic Cell wall synthesis inhibitor 3 rd generation

Ceftriaxone Cephalosporin antibiotic Cell wall synthesis inhibitor 3 rd generation CSF penetration

Cefuroxime Cephalosporin antibiotic Cell wall synthesis inhibitor 2 nd generation CSF penetration

Cephalexin Cephalosporin antibiotic Cell wall synthesis inhibitor 1 st generation Oral

Cephalosporins Antibiotics  lactam Cell wall synthesis inhibitors Inhibit cross-linking of peptidoglycan

Cephalothin Cephalosporin antibiotic Cell wall synthesis inhibitor 1 st generation Oral

Chloramphenicol Antibiotic Bacteriostatic protein synthesis inhibitor 50S ribosome Inhibits peptide bond formation

Chloroquine Antimalarial Intercalates in DNA Binds to ferriprotoporphyrin

Cidofovir Antiherpes Pyrimidine analog Phosphorylated to inhibitor of viral DNA polymerase

Ciprofloxacin Fluoroquinolone antibiotic DNA replication inhibitor Inhibits bacterial DNA gyrase

Cisplatin Antineoplastic Miscellaneous Cross-linking agent

Clarithromycin Macrolide antibiotic Bacteriostatic protein synthesis inhibitor Antiulcer 50S ribosome Inhibits translocation

Clavulanic acid  -lactamase inhibitor Combined with antibacterials

Clindamycin Antibiotic Bacteriostatic protein synthesis inhibitor 50S ribosome Anaerobic infections

Clotrimazole Imidazole antifungal Inhibits synthesis of ergosterol Lanosterol 14  demethylase inhibitor

Cloxacillin Penicillin antibiotic Cell wall synthesis inhibitor Penicillinase resistant penicillin Inhibits peptidoglycan cross-linking

Cyclophosphamide Antineoplastic Alkylating Agent

Cycloserine Antibiotic Cell wall synthesis inhibitor Secondary TB drug Inhibits formation of Park nucleotide

Cyclosporine Immunosuppressive Antineoplastic Binds cyclophilin Inhibits calcineurin

Cyproterone acetate Antiandrogen Antineoplastic androgen receptor antagonist

Cytarabine (AraC) Antineoplastic Antimetabolite

Dacarbazine Antineoplastic Alkylating Agent

Daclizumab Immunosuppressive Anti-CD25 (interleukin 2 receptor) antibody Organ transplant (anti-rejection)

Dactinomycin Antineoplastic Natural product Antibiotic

Dapsone Sulfone antibiotic Nucleic acid and protein synthesis inhibitor Inhibits dihydropteroate synthetase Leprosy

Daunorubicin Antineoplastic Anthracycline antibiotic Natural product

Delavirdine Antiretroviral Non-nucleoside reverse transcriptase inhibitor (NNRTI)

Dexamethasone Adrenocorticosteroid Glucocorticoid Antineoplastic Anti-inflammatory steroid Not by inhalation

Didanosine Antiretroviral Nucleoside reverse transcriptase inhibitor (NRTI) Dideoxyinosine (ddI)

Diethylcarbamazine Antihelminthic Treatment of intestinal and tissue roundworms

Doxorubicin Antineoplastic Anthracycline antibiotic Natural product

Doxycycline Tetracycline antibiotic Bacteriostatic protein synthesis inhibitor 30S ribosome Prevents aminoacyl tRNA attachment

Efavirenz Antiretroviral Non-nucleoside reverse transcriptase inhibitor (NNRTI)

Enfuvirtide (T-20) Antiretroviral Fusion inhibitor

Erythromycin Macrolide antibiotic Bacteriostatic protein synthesis inhibitor 50S ribosome Inhibits translocation

Ethambutol Antibiotic Major drug for tuberculosis

Ethionamide Antibiotic Secondary drug for tuberculosis

Etoposide Antineoplastic Natural product Plant alkaloid

Exemestane Antineoplastic Antiestrogen Aromatase Inhibitor

Famciclovir Antiherpes Purine analog Phosphorylated to an inhibitor of viral DNA polymerase

Fluconazole Triazole antifungal Inhibits synthesis of ergosterol by inhibiting lanosterol 14  demethylase

Flucytosine Antifungal Converted by fungi to 5-fluorouracil  faulty RNA and DNA synthesis

Fluorinated Quinolones ciprofloxacin, norfloxacin Antibiotics DNA replication inhibitors Inhibit bacterial DNA gyrase

5-Fluorouracil Antineoplastic Antimetabolite Thymidylate synthase inhibitor

Foscarnet Antiherpes Pyrophosphate analog Directly inhibits viral DNA polymerase

Fulvestrant Antineoplastic Antiestrogen Estrogen receptor antagonist

Ganciclovir Antiherpes Purine analog Phosphorylated to an inhibitor of viral DNA polymerase

Gemtuzumab Antineoplastic Anti-CD33 antibody

Gentamicin Aminoglycoside antibiotic bactericidal protein synthesis inhibitor 30S ribosome Freezes initiation

Goserelin Antineoplastic Gonadotropin releasing hormone (GnRH) agonist

Griseofulvin Antifungal Binds to microtubules

Hydroxyurea Antineoplastic Miscellaneous Ribonucleotide reductase inhibitor

Ibritumomab Antineoplastic Anti-CD20 antibody

Imatinib Antineoplastic Miscellaneous Tyrosine kinase inhibitor

Imipenem/Cilastatin New  lactam antibiotic Cilastatin inhibits a kidney dipeptidase that inactivates imipenem

Indinavir Antiretroviral Protease inhibitor (PI)

Interferon alpha Antiviral for hepatitis Antineoplastic Cytokine Anti-angiogenesis

Interleukin 2 Cytokine Antineoplastic

Interleukin 11 Cytokine Antineoplastic (supporting agent)

Iodoquinol Antiparasitic Treatment of protozoal infections

Iressa Antineoplastic Miscellaneous Tyrosine kinase inhibitor

Isoniazid Antibiotic Inhibits biosynthesis of mycolic acids Major drug for tuberculosis

Itraconazole Triazole antifungal Inhibits synthesis of ergosterol by inhibiting lanosterol 14  demethylase

Ivermectin Antihelminthic Treatment of intestinal and tissue roundworms

Ketoconazole Imidazole antifungal Inhibits synthesis of ergosterol by inhibiting lanosterol 14  demethylase

Lamivudine Antiretroviral Nucleoside reverse transcriptase inhibitor (NRTI)

Letrozole Antineoplastic Antiestrogen Aromatase Inhibitor

Leucovorin Antineoplastic (supporting agent) Folic acid analogue (used in methotrexate rescue)

Leuprolide Antineoplastic Gonadotropin releasing hormone (GnRH) agonist

Linezolid Oxazolidinone antibiotic Protein synthesis inhibitor 50S ribosomal subunit

Lomustine (CCNU) Antineoplastic Alkylating Agent

Macrolides erythromycin, azithromycin, clarithromycin Antibiotics Bacteriostatic protein synthesis inhibitors 50S ribosome

Mebendazole Antihelminthic Treatment of intestinal roundworms

Mechlorethamine Antineoplastic Alkylating Agent

Mefloquine Antimalarial Treatment and prophylaxis for chloroquine resistant Plasmodium

Meglumine antimonate Tropical antiparasitic Organic antimonial Treatment of Leishmaniasis

Melarsoprol Tropical antiparasitic Treatment of African Trypanosomiasis in CNS

Melphalan Antineoplastic Alkylating Agent

6-Mercaptopurine Antineoplastic Antimetabolite (“pseudofeedback inhibition” of HGPRT and PRP – purine synthesis)

Mesna Antineoplastic (supporting agent) Prevent hemorrhagic cystitis due to cyclophosphamide

Methenamine Urinary tract antiseptic Decomposes to formaldehyde in acidic environment

Methicillin Penicillin antibiotic Cell wall synthesis inhibitor Pencillinase resistant penicillin Inhibits peptidoglycan cross-linking

Methotrexate Immunosuppressive Antineoplastic Folic acid antagonist Dihydrofolate reductase inhibitor

Metronidazole Antibiotic Antiparasitic Antiulcer Anaerobes Reduction leads to intermediates that damage DNA

Miconazole Imidazole antifungal Inhibits synthesis of ergosterol by inhibiting lanosterol 14  demethylase

Minocycline Tetracycline antibiotic Bacteriostatic protein synthesis inhibitor 30S ribosome Prevents aminoacyl tRNA attachment

Mitomycin C Antineoplastic Natural product Antibiotic

Muromonab-CD3 Immunosuppressive Mouse monoclonal anti-CD3 antibody Organ transplant (anti-rejection)

Mycophenolate Immunosuppressive Inhibits inosine monophosphate dehydrogenase activity

Nafcillin Penicillin antibiotic Cell wall synthesis inhibitor Penicillinase resistant penicillin Inhibits peptidoglycan cross-linking

Nalidixic acid Urinary tract antiseptic Quinolone Inhibits bacterial DNA gyrase

Neomycin Aminoglycoside antibiotic Bactericidal protein synthesis inhibitor 30S ribosome Freezes initiation Topical

Netilmicin Aminoglycoside antibiotic Bactericidal protein synthesis inhibitor 30S ribosome Freezes initiation

Nevirapine Antiretroviral Non-nucleoside reverse transcriptase inhibitor (NNRTI)

Nifurtimox Tropical antiparasitic Treatment of South American Trypanosomiasis; Chagas disease

Nitrofurantoin Urinary tract antiseptic Reduction leads to intermediates that damage DNA

Norfloxacin Fluoroquinolone antibiotic DNA replication inhibitor Inhibits bacterial DNA gyrase

Nystatin Antifungal Polyene antibiotic Binds to ergosterol & alters permeability Topical

Organic antimonials Tropical antiparasitic Treatment of Leishmaniasis sodium stibogluconate meglumine antimonate

Oseltamivir Antiviral Inhibits neuraminidase and decreases viral release Treatment of Influenza A & B

Oxacillin Penicillin antibiotic Cell wall synthesis inhibitor Pencillinase resistant penicillin Inhibits peptidoglycan cross-linking

Oxytetracycline Tetracycline antibiotic Bacteriostatic protein synthesis inhibitor 30S ribosome Prevents aminoacyl tRNA attachment

Paclitaxel Antineoplastic Natural product Plant alkaloid (taxane)

Palivizumab Antiviral Monoclonal antibody against the surface of respiratory syncytial virus

Para-aminosalicylic acid Antibiotic Nucleic acid and protein synthesis inhibitor Inhibits dihydropteroate synthetase Secondary TB drug

Paromomycin Antiparasitic Aminoglycoside antibiotic Treatment of protozoal infections

Penciclovir Antiherpes Purine analog Phosphorylated to inhibitor of viral DNA polymerase

Penicillins  lactam antibiotics Cell wall synthesis inhibitors Inhibit cross-linking of peptidoglycan

Penicillin G Penicillin antibiotic Cell wall synthesis inhibitor Acid labile Inhibits peptidoglycan cross-linking

Penicillin V Penicillin antibiotic Cell wall synthesis inhibitor More acid resistant than Penicillin G Inhibits peptidoglycan cross-linking

Pentostatin Antineoplastic Miscellaneous Enzyme inhibitor (blocks purine synthesis)

Piperacillin Penicillin antibiotic Cell wall synthesis inhibitor Anti-pseudomonal penicillin Inhibits peptidoglycan cross-linking

Polymyxin B Antibiotic Disrupts gram negative cell membrane Binds phosphatidylethanolamine Bactericidal

Praziquantel Antihelminthic Treatment of trematode (fluke) and cestode (tapeworm) infections

Primaquine Antimalarial Eliminates hepatic forms of plasmodium

Procaine Penicillin G Penicillin antibiotic Cell wall synthesis inhibitor Repository preparation Inhibits peptidoglycan cross-linking

Pyrantel Pamoate Antihelminthic Treatment of intestinal roundworms

Pyrazinamide Antibiotic Major drug for tuberculosis

Pyrimethamine Antimalarial Protein and nucleic acid synthesis inhibitor Plasmodial dihydrofolate reductase inhibitor

Ribavirin Antiviral Primarily used as aerosol for respiratory syncytial virus

Rifampin Antibiotic Nucleic acid synthesis inhibitor Inhibits DNA dependent RNA polymerase Major drug for TB

Rimantadine Antiviral Inhibits replication at the stage of uncoating Treatment of Influenza A

Ritonavir Antiretroviral Protease inhibitor (PI)

Rituxumab Antineoplastic Anti-CD20 antibody

Saquinavir Antiretroviral Protease inhibitor (PI)

Silver sulfadiazine Sulfonamide antibiotic Microbial nucleic acid and protein synthesis inhibitor Inhibits dihydropteroate synthetase Topical

Sirolimus Immunosuppressive Binds FKBP, inhibits mTOR (mammalian kinase target of rapamycin) & cell cycle progression Rapamycin

Sodium stibogluconate Tropical antiparasitic Organic antimonial Treatment of Leishmaniasis

Spectinomycin Antibiotic Bacteriostatic protein synthesis inhibitor 30S ribosome

Streptomycin Aminoglycoside antibiotic Bactericidal protein synthesis inhibitor 30S ribosome Freezes initiation

Sulfacetamide Sulfonamide antibiotic Microbial nucleic acid and protein synthesis inhibitor Inhibits dihydropteroate synthetase Topical

Sulfadoxine Sulfonamide antibiotic Microbial nucleic acid and protein synthesis inhibitor Dihydropteroate synthetase inhibitor

Sulfamethoxazole Sulfonamide antibiotic Microbial nucleic acid and protein synthesis inhibitor Inhibits dihydropteroate synthetase

Sulfisoxazole Sulfonamide antibiotic Nucleic acid and protein synthesis inhibitor Inhibits dihydropteroate synthetase

Sulfonamides Antibiotics Nucleic acid and protein synthesis inhibitors Inhibit dihydropteroate synthetase

Suramin Tropical antiparasitic Treatment of African Trypanosomiasis

Tacrolimus Immunosuppressive Antineoplastic Binds FKBP (FK506 binding protein) Inhibits calcineurin

Tamoxifen Antineoplastic Antiestrogen Estrogen receptor anatagonist

Terbinafine Allylamine antifungal Inhibits ergosterol synthesis by inhibiting squalene epoxidase

Tetracycline Antibiotic Bacteriostatic protein synthesis inhibitor Antiulcer 30S ribosome Prevents aminoacyl tRNA attachment

Thalidomide Antineoplastic Anti-angiogenic Anti-TNF  Leprosy (not antibiotic)

Thiabendazole Antihelminthic Treatment of intestinal roundworms

6-Thioguanine Antineoplastic Antimetabolite (“pseudofeedback inhibition” of HGPRT and PRP – purine synthesis)

Thiotepa Antineoplastic Alkylating agent

Ticarcillin Penicillin antibiotic Cell wall synthesis inhibitor Anti-pseudomonal penicillin Inhibits peptidoglycan cross-linking

Tobramycin Aminoglycoside antibiotic Bactericidal protein synthesis inhibitor 30S ribosome Freezes initiation

Trastuzumab Antineoplastic Anti-HER2 antibody

Trifluridine Antiherpes Pyrimidine analog Phosphorylated to inhibitor of viral DNA polymerase

Trimethoprim Antibiotic Protein and nucleic acid synthesis inhibitor Inhibits bacterial dihydrofolate reductase

Trimetrexate Antibiotic Folic acid antagonist Treatment for Pneumocystis carinii

Tumor necrosis factor  Cytokine Antineoplastic

Valacyclovir Antiherpes Purine analog Phosphorylated to inhibitor of viral DNA polymerase

Valganciclovir Antiherpes Purine analog Phosphorylated to inhibitor of viral DNA polymerase

Vancomycin Antibiotic Inhibits cell wall synthesis Not a  lactam

Vinblastine Antineoplastic Vinca alkaloid Natural product

Vincristine Antineoplastic Vinca alkaloid Natural product

Voriconazole Triazole antifungal Inhibits synthesis of ergosterol by inhibiting lanosterol 14  demethylase

Zalcitabine Antiretroviral Nucleoside reverse transcriptase inhibitor (NRTI) Dideoxycytidine (ddC)

Zanamivir Antiviral Inhibits neuraminidase and decreases viral release Treatment of Influenza A & B

Zidovudine Antiretroviral Nucleoside reverse transcriptase inhibitor (NRTI) Azidothymidine (AZT)