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2004-2005Chemotherapeutics
Review
April 19, 202312:53 AM
Abacavir
Antiretroviral
Nucleoside reverse transcriptase inhibitor (NRTI)
Acyclovir
Antiherpes
Purine analogPhosphorylated to inhibitor of
viral DNA polymerase
Albendazole
Antihelminthic
Treatment of intestinal roundworms
Alemtuzumab
Antineoplastic
Anti-CD52 antibody
Amantadine
AntiviralAntiparkinson
Treatment of Influenza A Inhibits replication
at the stage of uncoating
Amikacin
Aminoglycoside antibioticBactericidal protein synthesis
inhibitor
30S ribosomeFreezes initiation
Aminoglutethimide
AntineoplasticImmunosuppressive
Glucocorticoid antagonistAromatase inhibitor
(decreases steroid synthesis)
Aminoglycosides
AntibioticsBactericidal protein synthesis
inhibitors
30S ribosomeFreeze initiation
Ampicillin
Penicillin antibioticCell wall synthesis inhibitor
Amino penicillinInhibits peptidoglycan cross-
linking
Amphotericin B
AntifungalPolyene antibiotic
Binds to ergosterol and alters permeability
Systemic
Amsacrine
Antineoplastic
Miscellaneous
Anastrozole
AntineoplasticAntiestrogen
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
ImmunosuppressiveAntineoplastic
Antimetabolite(“pseudofeedback inhibition” of
HGPRT and PRP)
Azithromycin
Macrolide antibioticBacteriostatic protein synthesis
inhibitor
50S ribosome Inhibits translocation
Aztreonam
New lactam antibiotic
Monobactam
Bacitracin
AntibioticCell 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 antibioticCell wall synthesis inhibitor
Inhibits peptidoglycan cross-linking Repository preparation
Bleomycin
Antineoplastic
Natural productAntibiotic
Busulfan
Antineoplastic
Alkylating Agent
Carbenicillin
Penicillin antibioticCell wall synthesis inhibitor
Anti-pseudomonal penicillinInhibits peptidoglycan cross-
linking
Carmustine (BCNU)
Antineoplastic
Alkylating Agent
Cefaclor
Cephalosporin antibioticCell wall synthesis inhibitor
2nd generationOral
Cefadroxil
Cephalosporin antibioticCell wall synthesis inhibitor
1st generationOral
Cefepime
Cephalosporin antibioticCell wall synthesis inhibitor
4th generationCSF penetration
Cefotaxime
Cephalosporin antibioticCell wall synthesis inhibitor
3rd generationCSF penetration
Cefoxitin
Cephalosporin antibioticCell wall synthesis inhibitor
2nd generation
Ceftazidime
Cephalosporin antibioticCell wall synthesis inhibitor
3rd generation
Ceftriaxone
Cephalosporin antibioticCell wall synthesis inhibitor
3rd generationCSF penetration
Cefuroxime
Cephalosporin antibioticCell wall synthesis inhibitor
2nd generationCSF penetration
Cephalexin
Cephalosporin antibioticCell wall synthesis inhibitor
1st generationOral
Cephalosporins
Antibiotics lactam
Cell wall synthesis inhibitorsInhibit cross-linking of
peptidoglycan
Cephalothin
Cephalosporin antibioticCell wall synthesis inhibitor
1st generationOral
Chloramphenicol
AntibioticBacteriostatic protein synthesis
inhibitor
50S ribosomeInhibits peptide bond formation
Chloroquine
Antimalarial
Intercalates in DNABinds to ferriprotoporphyrin
Cidofovir
Antiherpes
Pyrimidine analogPhosphorylated to inhibitor of
viral DNA polymerase
Ciprofloxacin
Fluoroquinolone antibioticDNA replication inhibitor
Inhibits bacterial DNA gyrase
Cisplatin
Antineoplastic
MiscellaneousCross-linking agent
Clarithromycin
Macrolide antibioticBacteriostatic protein synthesis
inhibitor Antiulcer
50S ribosomeInhibits translocation
Clavulanic acid
-lactamase inhibitor
Combined with antibacterials
Clindamycin
AntibioticBacteriostatic protein synthesis
inhibitor
50S ribosomeAnaerobic infections
Clotrimazole
Imidazole antifungal
Inhibits synthesis of ergosterolLanosterol 14 demethylase
inhibitor
Cloxacillin
Penicillin antibioticCell wall synthesis inhibitor
Penicillinase resistant penicillinInhibits peptidoglycan cross-
linking
Cyclophosphamide
Antineoplastic
Alkylating Agent
Cycloserine
AntibioticCell wall synthesis inhibitor
Secondary TB drugInhibits formation of Park
nucleotide
Cyclosporine
ImmunosuppressiveAntineoplastic
Binds cyclophilinInhibits calcineurin
Cyproterone acetate
AntiandrogenAntineoplastic
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 productAntibiotic
Dapsone
Sulfone antibioticNucleic acid and
protein synthesis inhibitor
Inhibits dihydropteroate synthetase
Leprosy
Daunorubicin
Antineoplastic
Anthracycline antibiotic Natural product
Delavirdine
Antiretroviral
Non-nucleoside reverse transcriptase inhibitor (NNRTI)
Dexamethasone
AdrenocorticosteroidGlucocorticoidAntineoplastic
Anti-inflammatory steroidNot by inhalation
Didanosine
Antiretroviral
Nucleoside reverse transcriptase inhibitor (NRTI)
Dideoxyinosine (ddI)
Diethylcarbamazine
Antihelminthic
Treatment of intestinaland tissue roundworms
Doxorubicin
Antineoplastic
Anthracycline antibioticNatural product
Doxycycline
Tetracycline antibioticBacteriostatic protein synthesis
inhibitor
30S ribosomePrevents aminoacyl tRNA attachment
Efavirenz
Antiretroviral
Non-nucleoside reversetranscriptase inhibitor (NNRTI)
Enfuvirtide (T-20)
Antiretroviral
Fusion inhibitor
Erythromycin
Macrolide antibioticBacteriostatic protein synthesis
inhibitor
50S ribosomeInhibits translocation
Ethambutol
Antibiotic
Major drug for tuberculosis
Ethionamide
Antibiotic
Secondary drug for tuberculosis
Etoposide
Antineoplastic
Natural productPlant alkaloid
Exemestane
AntineoplasticAntiestrogen
Aromatase Inhibitor
Famciclovir
Antiherpes
Purine analogPhosphorylated to an inhibitor
ofviral 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 Quinolonesciprofloxacin, norfloxacin
AntibioticsDNA replication inhibitors
Inhibit bacterial DNA gyrase
5-Fluorouracil
Antineoplastic
AntimetaboliteThymidylate synthase inhibitor
Foscarnet
Antiherpes
Pyrophosphate analogDirectly inhibits viral DNA
polymerase
Fulvestrant
AntineoplasticAntiestrogen
Estrogen receptor antagonist
Ganciclovir
Antiherpes
Purine analogPhosphorylated to an inhibitor
of viral DNA polymerase
Gemtuzumab
Antineoplastic
Anti-CD33 antibody
Gentamicin
Aminoglycoside antibioticbactericidal protein synthesis inhibitor
30S ribosomeFreezes initiation
Goserelin
AntineoplasticGonadotropin releasing
hormone(GnRH) agonist
Griseofulvin
Antifungal
Binds to microtubules
Hydroxyurea
Antineoplastic
MiscellaneousRibonucleotide reductase
inhibitor
Ibritumomab
Antineoplastic
Anti-CD20 antibody
Imatinib
Antineoplastic
MiscellaneousTyrosine kinase inhibitor
Imipenem/Cilastatin
New lactam antibiotic
Cilastatin inhibits akidney dipeptidase that inactivates imipenem
Indinavir
Antiretroviral
Protease inhibitor (PI)
Interferon alpha
Antiviral for hepatitisAntineoplastic
Cytokine
Anti-angiogenesis
Interleukin 2
Cytokine Antineoplastic
Interleukin 11
Cytokine Antineoplastic (supporting
agent)
Iodoquinol
Antiparasitic
Treatment of protozoal infections
Iressa
Antineoplastic
MiscellaneousTyrosine 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 intestinaland tissue roundworms
Ketoconazole
Imidazole antifungal
Inhibits synthesis of ergosterol by inhibiting lanosterol 14
demethylase
Lamivudine
Antiretroviral
Nucleoside reverse transcriptase inhibitor (NRTI)
Letrozole
AntineoplasticAntiestrogen
Aromatase Inhibitor
Leucovorin
Antineoplastic (supporting agent)
Folic acid analogue(used in methotrexate rescue)
Leuprolide
AntineoplasticGonadotropin releasing hormone (GnRH) agonist
Linezolid
Oxazolidinone antibioticProtein synthesis inhibitor
50S ribosomal subunit
Lomustine (CCNU)
Antineoplastic
Alkylating Agent
Macrolideserythromycin, azithromycin, clarithromycin
AntibioticsBacteriostatic 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 antimonialTreatment 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 cystitisdue to cyclophosphamide
Methenamine
Urinary tract antiseptic
Decomposes to formaldehydein acidic environment
Methicillin
Penicillin antibioticCell wall synthesis inhibitor
Pencillinase resistant penicillin Inhibits peptidoglycan cross-
linking
Methotrexate
ImmunosuppressiveAntineoplastic
Folic acid antagonistDihydrofolate reductase
inhibitor
Metronidazole
AntibioticAntiparasitic
Antiulcer
AnaerobesReduction leads to intermediates
that damage DNA
Miconazole
Imidazole antifungal
Inhibits synthesis of ergosterol by inhibiting lanosterol 14
demethylase
Minocycline
Tetracycline antibioticBacteriostatic protein synthesis
inhibitor
30S ribosomePrevents aminoacyl tRNA attachment
Mitomycin C
Antineoplastic
Natural productAntibiotic
Muromonab-CD3
Immunosuppressive
Mouse monoclonal anti-CD3 antibody
Organ transplant (anti-rejection)
Mycophenolate
Immunosuppressive
Inhibits inosine monophosphate dehydrogenase activity
Nafcillin
Penicillin antibioticCell wall synthesis inhibitor
Penicillinase resistant penicillinInhibits peptidoglycan cross-
linking
Nalidixic acid
Urinary tract antiseptic
QuinoloneInhibits bacterial DNA gyrase
Neomycin
Aminoglycoside antibioticBactericidal protein synthesis
inhibitor
30S ribosomeFreezes initiation
Topical
Netilmicin
Aminoglycoside antibioticBactericidal protein synthesis
inhibitor
30S ribosomeFreezes 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 antibioticDNA replication inhibitor
Inhibits bacterial DNA gyrase
Nystatin
AntifungalPolyene antibiotic
Binds to ergosterol & alters permeability
Topical
Organic antimonials
Tropical antiparasitic
Treatment of Leishmaniasis
sodium stibogluconatemeglumine antimonate
Oseltamivir
Antiviral
Inhibits neuraminidase anddecreases viral release
Treatment of Influenza A & B
Oxacillin
Penicillin antibioticCell wall synthesis inhibitor
Pencillinase resistant penicillinInhibits peptidoglycan cross-
linking
Oxytetracycline
Tetracycline antibioticBacteriostatic protein synthesis
inhibitor
30S ribosomePrevents aminoacyl tRNA attachment
Paclitaxel
Antineoplastic
Natural productPlant alkaloid (taxane)
Palivizumab
Antiviral
Monoclonal antibody againstthe surface of
respiratory syncytial virus
Para-aminosalicylic acid
AntibioticNucleic acid and
protein synthesis inhibitor
Inhibits dihydropteroate synthetase
Secondary TB drug
Paromomycin
AntiparasiticAminoglycoside antibiotic
Treatment of protozoal infections
Penciclovir
Antiherpes
Purine analogPhosphorylated to inhibitor of
viral DNA polymerase
Penicillins
lactam antibioticsCell wall synthesis inhibitors
Inhibit cross-linking of peptidoglycan
Penicillin G
Penicillin antibioticCell wall synthesis inhibitor
Acid labileInhibits peptidoglycan cross-
linking
Penicillin V
Penicillin antibioticCell wall synthesis inhibitor
More acid resistant than Penicillin G
Inhibits peptidoglycan cross-linking
Pentostatin
Antineoplastic
MiscellaneousEnzyme inhibitor
(blocks purine synthesis)
Piperacillin
Penicillin antibioticCell wall synthesis inhibitor
Anti-pseudomonal penicillinInhibits peptidoglycan cross-
linking
Polymyxin B
AntibioticDisrupts gram negative cell
membrane
Binds phosphatidylethanolamineBactericidal
Praziquantel
Antihelminthic
Treatment of trematode (fluke) and cestode (tapeworm)
infections
Primaquine
Antimalarial
Eliminates hepatic forms of plasmodium
Procaine Penicillin G
Penicillin antibioticCell wall synthesis inhibitor
Repository preparationInhibits peptidoglycan cross-
linking
Pyrantel Pamoate
Antihelminthic
Treatment of intestinal roundworms
Pyrazinamide
Antibiotic
Major drug for tuberculosis
Pyrimethamine
AntimalarialProtein and nucleic acid
synthesis inhibitor
Plasmodial dihydrofolate reductase inhibitor
Ribavirin
Antiviral
Primarily used as aerosol for respiratory syncytial virus
Rifampin
AntibioticNucleic acid synthesis inhibitor
Inhibits DNA dependent RNA polymerase
Major drug for TB
Rimantadine
Antiviral
Inhibits replicationat 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 antibioticMicrobial 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
AntibioticBacteriostatic protein synthesis
inhibitor
30S ribosome
Streptomycin
Aminoglycoside antibioticBactericidal protein synthesis
inhibitor
30S ribosomeFreezes initiation
Sulfacetamide
Sulfonamide antibioticMicrobial nucleic acid
and protein synthesis inhibitor
Inhibits dihydropteroate synthetase
Topical
Sulfadoxine
Sulfonamide antibioticMicrobial nucleic acid
and protein synthesis inhibitor
Dihydropteroate synthetase inhibitor
Sulfamethoxazole
Sulfonamide antibioticMicrobial nucleic acid
and protein synthesis inhibitor
Inhibits dihydropteroate synthetase
Sulfisoxazole
Sulfonamide antibioticNucleic acid and
protein synthesis inhibitor
Inhibits dihydropteroate synthetase
Sulfonamides
AntibioticsNucleic acid and
protein synthesis inhibitors
Inhibit dihydropteroate synthetase
Suramin
Tropical antiparasitic
Treatment of African Trypanosomiasis
Tacrolimus
ImmunosuppressiveAntineoplastic
Binds FKBP (FK506 binding protein)
Inhibits calcineurin
Tamoxifen
Antineoplastic Antiestrogen
Estrogen receptor anatagonist
Terbinafine
Allylamine antifungal
Inhibits ergosterol synthesis by inhibiting squalene epoxidase
Tetracycline
AntibioticBacteriostatic protein synthesis
inhibitor Antiulcer
30S ribosomePrevents aminoacyl tRNA attachment
Thalidomide
Antineoplastic
Anti-angiogenicAnti-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 antibioticCell wall synthesis inhibitor
Anti-pseudomonal penicillinInhibits peptidoglycan cross-
linking
Tobramycin
Aminoglycoside antibioticBactericidal protein synthesis
inhibitor
30S ribosomeFreezes initiation
Trastuzumab
Antineoplastic
Anti-HER2 antibody
Trifluridine
Antiherpes
Pyrimidine analogPhosphorylated to inhibitor of
viral DNA polymerase
Trimethoprim
AntibioticProtein and nucleic acid
synthesis inhibitor
Inhibits bacterial dihydrofolate reductase
Trimetrexate
Antibiotic
Folic acid antagonist Treatment for Pneumocystis
carinii
Tumor necrosis factor
CytokineAntineoplastic
Valacyclovir
Antiherpes
Purine analogPhosphorylated to inhibitor of
viral DNA polymerase
Valganciclovir
Antiherpes
Purine analogPhosphorylated to inhibitor of
viral DNA polymerase
Vancomycin
AntibioticInhibits cell wall synthesis
Not a lactam
Vinblastine
Antineoplastic
Vinca alkaloidNatural product
Vincristine
Antineoplastic
Vinca alkaloidNatural 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 neuraminidaseand decreases viral release
Treatment of Influenza A & B
Zidovudine
Antiretroviral
Nucleoside reverse transcriptase inhibitor (NRTI)
Azidothymidine (AZT)