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)