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209 Cards in this Set
- Front
- Back
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Cell Wall Biosynthesis
Glycopeptides Structured around a heptapeptide with covalently linked side chains with sugar additions Bacteriostatic against Gram+ cocci Bactericidal for Gram+ rods Including penicillinase producers and methicillin-resistant strains Not effective against Gram- Last resort for some strains of C. difficile Binds D-Ala-D-Ala terminus of the murine monomer (substrate) Red Man syndrome |
Vancomycin
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Cell Wall Biosynthesis
Glycopeptides Structured around a heptapeptide with covalently linked side chains with sugar additions Extended half-life elimination Once daily dosing, fewer side effects No pain or tissue necrosis after intramuscular injection No ototoxicity |
Teicoplanin
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β-Lactams
Bactericidal, require actively growing infection Inhibition by binding the enzyme Penicillins Natural Penicillins Common feature is the 6-aminopenicillanic acid nucleus composed of a thiazolide ring fused to a β-lactam ring Most active penicillins against Gram+ Only 1/3 of oral dose absorbed Add procaine or benzathine to delay absorption from IM injection site Add probenecid to delay elimination |
Penicillin G
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β-Lactams
Bactericidal, require actively growing infection Inhibition by binding the enzyme Penicillins Natural Penicillins Common feature is the 6-aminopenicillanic acid nucleus composed of a thiazolide ring fused to a β-lactam ring Acid stable form with better absorption after oral administration |
Penicillin V
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β-Lactams
Bactericidal, require actively growing infection Inhibition by binding the enzyme Penicillinase-Resistant Penicillins Resist β-lactamase produced by S. aureus and S. epidermidis Gram+ only Resistance related to failure to bind to penicillin binding proteins Not given orally |
Methicillin
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β-Lactams
Bactericidal, require actively growing infection Inhibition by binding the enzyme Penicillinase-Resistant Penicillins Resist β-lactamase produced by S. aureus and S. epidermidis Gram+ only |
Cloxacillin
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β-Lactams
Bactericidal, require actively growing infection Inhibition by binding the enzyme Extended Range Penicillins First penicillins effective against Gram- For E.coli, P. mirabilis, H. influenzae, Salmonella, Shigella, Neisseria More completely absorbed after oral admin than ampicillin |
Amoxicillin
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β-Lactams
Bactericidal, require actively growing infection Inhibition by binding the enzyme Extended Range Penicillins First penicillins effective against Gram- For E.coli, P. mirabilis, H. influenzae, Salmonella, Shigella, Neisseria |
Ampicillin
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β-Lactams
Bactericidal, require actively growing infection Inhibition by binding the enzyme Anti-Pseudomonal Penicillins (2) Carboxylated derivatives extend range of ampicillin to P. aeruginosa, indole positive Proteus, and Enterobacter |
Carbenicillin
Ticarcillin |
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β-Lactams
Bactericidal, require actively growing infection Inhibition by binding the enzyme Anti-Pseudomonal Penicillins N-acyl derivatives |
Pipericillin
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β-Lactams
Bactericidal, require actively growing infection Inhibition by binding the enzyme Cephalosporins Similar basic structure and mode of action to the penicillins Can cause bleeding due to bleeding disorders or Vitamin K deficiency First Generation Narrow spectrum, against Staph and Strep Surgical prophylaxis Not effective for MRSA |
Cefazolin
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β-Lactams
Bactericidal, require actively growing infection Inhibition by binding the enzyme Cephalosporins Similar basic structure and mode of action to the penicillins Can cause bleeding due to bleeding disorders or Vitamin K deficiency Second Generation Increased action against Gram- like E. coli and Proteus Decreased action against Gram+ Effective for H. influenzae and K. pneumoniae For community acquired pneumonia |
Cefuroxime
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β-Lactams
Bactericidal, require actively growing infection Inhibition by binding the enzyme Cephalosporins Similar basic structure and mode of action to the penicillins Can cause bleeding due to bleeding disorders or Vitamin K deficiency Second Generation Increased action against Gram- like E. coli and Proteus Decreased action against Gram+ B. fragilis and other anaerobes Prophylaxis during intra-abdominal surgery (2) |
Cefotetan
Cefoxitin |
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β-Lactams
Bactericidal, require actively growing infection Inhibition by binding the enzyme Cephalosporins Similar basic structure and mode of action to the penicillins Can cause bleeding due to bleeding disorders or Vitamin K deficiency Second Generation Increased action against Gram- like E. coli and Proteus Decreased action against Gram+ • Sometimes classes as a carbacephem |
Loracarbef
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β-Lactams
Bactericidal, require actively growing infection Inhibition by binding the enzyme Cephalosporins Similar basic structure and mode of action to the penicillins Can cause bleeding due to bleeding disorders or Vitamin K deficiency Third Generation Good penetration of CNS, bone, lungs, urinary tract High activity against Gram- • Choice for N. gonorrhea and B. burgdorferi |
Ceftriazone
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β-Lactams
Bactericidal, require actively growing infection Inhibition by binding the enzyme Cephalosporins Similar basic structure and mode of action to the penicillins Can cause bleeding due to bleeding disorders or Vitamin K deficiency Third Generation Good penetration of CNS, bone, lungs, urinary tract High activity against Gram- • For multidrug-resistant Gram- infections, such as P. aeruginosa (2) |
Ceftazidime
Cefoperazone |
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β-Lactams
Bactericidal, require actively growing infection Inhibition by binding the enzyme Cephalosporins Similar basic structure and mode of action to the penicillins Can cause bleeding due to bleeding disorders or Vitamin K deficiency Fourth Generation • Better against Gram+ because of resistance to β-lactamases |
Cefepime
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β-Lactams
Bactericidal, require actively growing infection Inhibition by binding the enzyme Carbapenems Extremely broad spectrum Resistant to β-lactamases, not resistant to metallo-β-lactamases Given in combination with cilastatin, a dipeptidase inhibitor |
Imipenem
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β-Lactams
Bactericidal, require actively growing infection Inhibition by binding the enzyme Carbapenems Extremely broad spectrum Less susceptible to hydrolysis by renal tubule dipeptidase Less nephrogenic |
Meropenem
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β-Lactams
Bactericidal, require actively growing infection Inhibition by binding the enzyme Monobactams Excellent against Gram-, poor against Gram+ Can be used instead of aminoglycoside The only one that does not show cross-allergenicity with other β-lactam antibiotics |
Aztreonam
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Antibiotics; Nucleic Acid biosynthesis
Sulfonamides Broad spectrum Structural analogs and competitive antagonists of PABA at dihydropteroate synthase |
Sulfisoxazole
Sulfamethoxazole |
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Antibiotics; Nucleic Acid biosynthesis
Benzylpyrimidines Broad Spectrum Selective inhibitor of bacterial dihydrofolate reductase |
Trimethoprim
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Antibiotics; Cell Membrane potential; Lipopeptides
Spectrum For complicated skin and skin structure infections Retains activity against resistant Gram+ Binds to membranes and forms membrane channels in a Ca2+ dependent manner Pharmacokinetics IV only Excreted by kidney Does not cross blood-brain barrier |
Daptomycin (Cubicin)
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Antibiotics
Protein Synthesis 30S Glycylcyline Binds 30S. Prevents binding of aminoacyl tRNA Bacteriostatic against Gram+ and Gram-, especially for tetracycline resistance Binds 30s and inhibits binding of the aminoacyl-tRNA into the A site |
Tigecycline
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Antibiotics
Protein Synthesis 30S Aminoglycosides Bind 30S. Interfere with initiation complex and cause misreading of mRNA Contains amino sugars linked to an aminocyclitol ring by glycosidic bonds Broad spectrum bacteridical against Gram- Inner membrane transport is oxygen-dependent--not effective for anaerobes Binds the 16S rRNA in the 30S subunit, interferes with formation of the initiation complex Enhanced activity with β-lactams |
Streptomycin
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Antibiotics
Protein Synthesis 30S Tetracyclines Bind 30S, prevent binding of aminoacyl tRNA Bacteriostatic against Gram+ and Gram- aerobes and anaerobes Binds 30S, prevents binding of aminoacyl-tRNA during protein synthesis Crosses plasma membrane by active transport (2) |
Tetracycline
Doxycycline |
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Antibiotics
Protein Synthesis 50S Oxazoladinones Bind 50S, prevents formation of initiation complex Bacteriostatic against Gram positive strains Prevents formation of the initiation complex and 70S ribosomal complex Binds 50S subunit and prevents protein synthesis Mutations of the 23 S rRNA prevent binding of the drug Inhibits MAO |
Linezolid
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Antibiotics
Protein Synthesis 50S Chloramphenicols Binds 50S to inhibit peptidyl transferase Not used in the US Broad spectrum Binds reversibly to the 50S subunit to prevent binding of the aminoacyl tRNA in the A site Gray baby syndrome |
Chloramphenicol
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Antibiotics
Protein Synthesis 50S Macrolides Binds 50S, inhibits translocation Inactivated by gastric acid, but absorbed in upper small intestine MLSB determinants create resistance (3) |
Erythromycin
Clarithromycin Azithromycin |
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Antibiotics
Protein Synthesis 50S Lincosamides Binds 50S, inhibits translocation Bacteriostatic against Gram+ and anaerobes Binds the P and A sites of the 50S rRNA Does not reach the CNS Resistance due to ribosomal methylation (MLSB) |
Clindamycin
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Antibiotics
Protein Synthesis 50S Type B streptogramins Binds 50S, inhibits translocation Bactericidal against Gram+ Binds 50S and inhibits 50S translocation step; same site as macrolides |
Streptogramin B (guinupristin)
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Antibiotics
Protein Synthesis 50S Type B streptogramins Binds 50S, inhibits translocation Bactericidal against Gram+ Induces a conformation change in the 50S rRNA |
Streptogramin A (dalfopristin)
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Antibiotics
Protein Synthesis 50S Type B streptogramins Binds 50S, inhibits translocation Combo of Streptogramin A and B |
Synercid
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Antibiotics
Protein Synthesis 50S Ketolides Binds 50S, inhibits translocation Gram + and Gram- Binds 50S, similar to macrolides Liver toxicity and failure (critical adverse effect) |
Telithromycin
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Antibiotics; DNA replication or Transcription
Fluoroquinolones Bactericidal, Primarily for Gram- Inhibits DNA gyrase (topoisomerase II), preventing relaxation of supercoiled DNA Primary for Gram+ Inhibits topoisomerase IV (2) |
Ciprofloxacin
Levofloxacin |
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Antibiotics; Nitroimidazole
For anaerobes Nitro group of nitrosohydroxyl amino moiety is reduced causing DNA strand breaks |
Metronidazole
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Antibiotics; RNA replication or Transcription
Rifamycin Inhibits RNA synthesis Non-covalently binds to the β subunit of the DNA-dependent RNA polymerase Oral preparation Good CNS penetration Deacetylated in the liver Induces CYP3A4 |
Rifampin
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Antibiotics; RNA replication or Transcription
Rifamycin Inhibits RNA synthesis Non-covalently binds to the β subunit of the DNA-dependent RNA polymerase For traveler's diarrhea Not absorbed from GI |
Rifaximin
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Antivirals, Penetration and Uncoating;
Interfere with viral uncoating by blocking viral M2 proton channel For prophylaxis of influenza A (2) |
Amantadine
Rimantidine |
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Antivirals, Penetration and Uncoating;
Saturated fatty alcohol that inhibits fusion of viral envelope to cell membrane For HSV-1 |
Docosanol
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Antivirals, Penetration and Uncoating;
• 36 residue synthetic peptide gp41 that blocks fusion of HIV to lymphocytes |
Enfuvirtide
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Antivirals, Assembly and Release;
Prophylaxis and treatment of influenza A and B Inhibits viral neuraminidase, inhibiting cleavage of sialic acid Blocks budding of new virus (2) |
Zanamivir (Relenza)
Oseltamivir |
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Antivirals; Humanized Monoclonal Antibodies;
Directed against the F protein of RSV Approved for prophylactic treatment of RSV |
Palivizumab
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Antivirals; Viral Nucleic Acid Synthesis;
Inhibits thymidylate synthetase and feedback inhibits other steps in pyrimidine biosynthesis Drug of choice for the treatment of herptetic conjunctival keratitis |
Trifluidine
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Antivirals; Viral Nucleic Acid Synthesis;
Synthetic nucleoside whose phosphorylated form inhibits inosine monophosphate dehydrogenase For RSV and hepatitis C (with interferon alphas) |
Ribavirin
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Antivirals; Viral Nucleic Acid Synthesis;
Guanosine analogue that is phosphorylated by thymidine kinase and inhibits viral DNA polymerase. Causes chain termination Drug of choice for herpes encephalitis and chickenpox |
Acyclovir
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Antivirals; Viral Nucleic Acid Synthesis;
Prodrug form of acyclovir that is converted to acyclovir during first-pass metabolism Reduces transmission of HSV-2 by 50% |
Valacyclovir (Valtrex)
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Antivirals; Viral Nucleic Acid Synthesis;
Acyclovir analogue that is effective for treatment of herpes labialis |
Penciclovir
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Antivirals; Viral Nucleic Acid Synthesis;
• Prodrug form of penciclovir, used to treat herpes labialis and genital herpes |
Famciclovir
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Antivirals; Viral Nucleic Acid Synthesis;
Acyclic guanine nucleoside analogue phosphorylated by CMV ULP& phosphotransferase For severe CMV infections in immunocompromised hosts and CMV retinitis |
Ganciclovir (Cytovene)
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Antivirals;
Nucleoside reverse transcriptase inhibitors (NRTIs) Can cause lactic acidosis as a result of mitochondrial toxicity Synthetic thymidine analogue that competes with dTTP for binding to reverse transcriptase Prolongs the lives of patients with AIDS Decreases transmission of virus from mother to fetus |
Zidovudine (AZT)
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Antivirals;
Nucleoside reverse transcriptase inhibitors (NRTIs) Can cause lactic acidosis as a result of mitochondrial toxicity Deoxyadenosine analog that can cause peripheral neuropathy and fatal pancreatitis |
Didanosine (ddI)
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Antivirals;
Nucleoside reverse transcriptase inhibitors (NRTIs) Can cause lactic acidosis as a result of mitochondrial toxicity Can be used for hepatitis B (2) |
Lamivudine (3TC)
Emtricitabine (FTC) |
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Antivirals;
Nucleoside reverse transcriptase inhibitors (NRTIs) Can cause lactic acidosis as a result of mitochondrial toxicity Can cause peripheral neuropathy (2) |
Stavudine (d4T)
Zalcitabine (ddC) |
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Antivirals;
Nucleoside reverse transcriptase inhibitors (NRTIs) Can cause lactic acidosis as a result of mitochondrial toxicity Guanosine analog with less hematopoietic toxicity than AZT Can cause rash and anaphylaxis--don't rechallenge |
Abacavir
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Antivirals;
Nucleoside reverse transcriptase inhibitors (NRTIs) Can cause lactic acidosis as a result of mitochondrial toxicity Guanine nucleoside analogue Inhibits HBV reverse transcriptase and HBV DNA polymerase |
Entevacir
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Antivirals;
Nucleoside reverse transcriptase inhibitors (NRTIs) Can cause lactic acidosis as a result of mitochondrial toxicity Thymidine analogue Inhibits HBV reverse transcriptase and HBV DNA polymerase |
Telbivudine
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Antivirals; Nucleotide reverse transcriptase inhibitors;
Acyclic nucleoside phosphonate that as a diphosphate inhibits HIV reverse transcriptase Does not require nucleoside kinase activity |
Tenofovir disoproxil
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Antivirals; Nucleotide reverse transcriptase inhibitors;
Acyclic nucleoside phosphonate For resistant CMV retinitis or smallpox vaccine reactions |
Cidofovir
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Antivirals; Nucleotide reverse transcriptase inhibitors;
For continuous use treatment of HBV |
Adefovir
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Antivirals; Non-Nucleoside reverse transcriptase inhibitors;
Can cause serious heptatotoxicity |
Nevirapine
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Antivirals; Non-Nucleoside reverse transcriptase inhibitors;
Crosses blood brain barrier |
Efavirenz
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Antivirals; Drug of choice for acyclovir-resistant herpes in AID patients
Inhibits HSV and CMV-encoded DNA polymerase, HIV reverse transcriptase |
Foscarnet
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Antivirals; Protein Synthesis;
HIV protease inhibitors Bind to catalytic site of HIV protease, blocking cleavage of gag-pol precursor Should only be used in combination therapy Associated with lipodystrophies Inhibit CYP3A4 Use in low doses to alter pharmakokinetics of a second protease inhibitor |
Ritonavir
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Antivirals; Protein Synthesis;
HIV protease inhibitors Bind to catalytic site of HIV protease, blocking cleavage of gag-pol precursor Should only be used in combination therapy Associated with lipodystrophies Inhibit CYP3A4 • OK to rechallenge with drug after rash resolves (2) |
Amprenavir Fosamprenavir
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Antivirals; Protein Synthesis;
HIV protease inhibitors Bind to catalytic site of HIV protease, blocking cleavage of gag-pol precursor Should only be used in combination therapy Associated with lipodystrophies Inhibit CYP3A4 • Lowest incidence of lipodystrophies |
Atazanavir
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Antivirals; Protein Synthesis;
HIV protease inhibitors Bind to catalytic site of HIV protease, blocking cleavage of gag-pol precursor Should only be used in combination therapy Associated with lipodystrophies Inhibit CYP3A4 • Ritonavir and Lopinavir combo |
Kaletra
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Antivirals; Interferons;
For Hep B anc C and a variety of malignancies Major effect at the level of viral protein synthesis |
Interferon alphas
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Antivirals; Antisense Oligonucleotides;
Antisense oligonucleotide complimentary to IE2 of CMV Binds IE2 mRNA, thus reducing expression For CMV retinits in AIDS patients |
Fomivirsen
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Antifungals;
Cell Membranes Polyenes Conjugated double bond system with a macrolide ring Bind to sterols and perturb membrane structure Soluble enough for IV admin Can cause impaired renal function |
Amphotericin B
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Antifungals;
Cell Membranes Polyenes Conjugated double bond system with a macrolide ring Bind to sterols and perturb membrane structure • Insoluble, used for superficial infections and GI infections |
Nystatin
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Antifungals;
Cell Membranes Azoles For superficial and systemic fungal infections Inhibit 14-α-demethylase which is involved in ergosterol biosynthesis Suitable for oral use Drug of choice for Candida esophagitis |
Fluconazole
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Antifungals;
Cell Membranes Azoles For superficial and systemic fungal infections Inhibit 14-α-demethylase which is involved in ergosterol biosynthesis Suitable for oral use |
Ketoconazole
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Antifungals;
Cell Membranes Azoles For superficial and systemic fungal infections Inhibit 14-α-demethylase which is involved in ergosterol biosynthesis Suitable for oral use Choice of treatment for dermatophytoses and onychomycosis |
Itraconazole
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Antifungals;
Cell Membranes Azoles For superficial and systemic fungal infections Inhibit 14-α-demethylase which is involved in ergosterol biosynthesis Drug of choice for resistant candidiasis |
Posoconazole
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Antifungals;
Cell Membranes Azoles For superficial and systemic fungal infections Inhibit 14-α-demethylase which is involved in ergosterol biosynthesis Drug of choice for treatment of invasive aspergillosis |
Voriconazole
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Antifungals;
Allylamines Inhibits fungal squalene epoxidase For tinea infections |
Terbinafine
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Antifungals; Pyridones
Pyridone antifungal agent that inhibits uptake of essential extracellular nutrients Only approved drug for topical treatment of dermatophyte infections |
Ciclopirox olamine
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Antifungals; Echinocandins
Noncompetitive inhibitors of β-(1,3)-β-D-glucan synthase, responsible for a cell-wall component For candidiasis and invasive aspergillosis |
Caspofungin
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Antifungals; Echinocandins
Noncompetitive inhibitors of β-(1,3)-β-D-glucan synthase, responsible for a cell-wall component For candidiasis |
Micafungin
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Antifungals; Nucleic Acid synthesis
Cytosine analogue Frequent resistance, so must use with amphotericin B |
Flucytosine
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Antifungals
Mitotic inhibitors Insoluble compound that disrupts microtubule function resulting in aberrant mitoses For fungal infections of the skin, hair, and nails |
Griseofulvin
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Chemotherapy; Alkylating Agents; Nitrogen mustards
Alkylate DNA, primarily at the N-7 position of guanine • Stable enough for oral administration |
Melphalan
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Chemotherapy; Alkylating Agents; Nitrogen mustards
Alkylate DNA, primarily at the N-7 position of guanine • Similar to melphalan |
Chlorambucil
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Chemotherapy; Alkylating Agents; Nitrogen mustards
Alkylate DNA, primarily at the N-7 position of guanine Must be activated by CYP2C9 to aldophosphamide Reduced hepatotoxicity |
Cyclophosphamide
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Chemotherapy; Alkylating Agents; Nitrogen mustards
Alkylate DNA, primarily at the N-7 position of guanine • Cyclophosphamide derivative used for testicular cancer |
Ifosfamide
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Chemotherapy; Alkylating Agents; Ethylenimines
Reactive ethylenimonium ring is already formed For breast and ovarian cancer |
Thiotepa
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Chemotherapy; Alkylating Agents; Alkylsulfonates
• Bifunctional methanesulfonate |
Busulfan
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Chemotherapy; Alkylating Agents; Nitrosoureas
Chloroethylnitrosureas Heterobifunctional compounds that are capable of alkylation, DNA crosslinking, and carbamoylation of proteins Lipid soluble agents that disappear rapidly from plasma (2) |
Carmustine (BCNU)
Lomustine (CCNU) |
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Chemotherapy; Alkylating Agents; Triazenes
Inhibits RNA and protein synthesis more than DNA synthesis No alkylating specificity |
Dacarbazine (DTIC)
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Chemotherapy; Alkylating Agents; Triazenes
Does not require hepatic activation For anaplastic astrocytoma |
Temozolomide
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Chemotherapy; Alkylating Agents; Others
Platinum coordination complex, chloride ions dissociate For testicular cancer, ovarian carcinoma, and head and neck cancers |
Cisplatin (Platinol)
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Chemotherapy; Alkylating Agents; Others
• Cisplatin analogue that is not cross-resistant |
Oxaliplatin
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Chemotherapy; Alkylating Agents; Others
• Cisplatin analogue that has substantially less renal toxicity |
Carboplatin
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Chemotherapy; Alkylating Agents; Others
Nonspecific alkylator after metabolic activation For Hodgkin's disease |
Procarbazine
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Chemotherapy; Natural Products; Vinca Alkaloids
Two of the most potent plant-derived antitumor agents Binds tubulin, favoring depolymerization Resistance due to MDR |
Vincristine
Vinblastine |
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Chemotherapy; Natural Products;
Vinca Alkaloids • Semisynthetic derivative of vinblastine with increased specificity for microtubules |
Vinorelbine
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Chemotherapy; Natural Products;
Taxanes Treatment of breast and ovarian cancer when chemotherapy has failed Inhibits disassembly of microtubules, blocking reorganization Resistance due to MDR |
Paclitaxel (Taxol)
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Chemotherapy; Natural Products;
Taxanes • Semisynthetic analogue of paclitaxel |
Docetaxel
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Chemotherapy; Natural Products;
Epipodophyllotoxins Semisynthetic glycosidic derivatives from a mandrake plant Inhibit topoisomerase II For Hodgkin's disease, diffuse histiocytic lymphoma, and small cell carcinoma of the lung (2) |
Etoposide (VP-16)
Teniposide (VM-26) |
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Chemotherapy; Natural Products;
Camptothecin derivatives Inhibit topoisomerase I • Prodrug effective in the treatment of metastatic colorectal cancer |
Irinotecan
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Chemotherapy; Natural Products;
Camptothecin derivatives Inhibit topoisomerase I • For treatment of ovarian and small cell lung carcinoma |
Topotecan
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Chemotherapy; Natural Products;
Antibiotics Composed of a planar phenoxazone to which identical polypeptides are attached Intercalates between adjacent G:C base pairs Inhibits RNA at low, RNA and DNA at high concentrations Causes radiation sensitization |
Dactinomycin (acinomycin D)
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Chemotherapy; Natural Products;
Antibiotics DNA and iron binding region S peptide binds to DNA, leading to depurination and depyrimidation Resistance due to bleomycin hydrolase |
Bleomycin
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Chemotherapy; Natural Products;
Antibiotics • Cause DNA intercalation and introduce single strand breaks (3) |
Daunorubicin
Doxorubicin Mitoxantrone |
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Chemotherapy; Natural Products;
Antibiotics Anthracyclines • Iron chelator that inhibits free radical formation and can be used to reduce cardiac damage |
Dexrazoxane
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Chemotherapy; Antimetabolites; General
Folic acid analogue, inhibits dihydrofolate reducatase (DHFR) Inhibits dUMP-->dTMP Affects pyrimidine biosynthesis and purine ring structure Resistance is due to increased DHFR activity and reduced transport |
Methotrexate
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Chemotherapy; Antimetabolites; General
• Effectively aborts MTX toxicity by supplying reduced folate to cells |
Leucovorin
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Chemotherapy; Antimetabolites; General
Inhibits ribonucleotide reductase, inhibits DNA synthesis, and blocks cells at the G1/S boundary For a variety of malignancies Bone marrow suppression |
Hydroxyurea
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Chemotherapy; Antimetabolites;
Pyrimidine analogues Prototype pyrimidine analogue 5-FdUMPis a potent suicide inhibitor of thymidylate synthase (TS) Resistance due to overexpression of TS |
5-FU
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Chemotherapy; Antimetabolites;
Pyrimidine analogues 5-FU prodrug catalyzed by thymidine phosphorylase For metastatic breast and colon cancer |
Capecitabine
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Chemotherapy; Antimetabolites;
Pyrimidine analogues Good activity against advanced breast cancer, non-small-cell lung cancer, pancreatic adenoma, and ovarian carcinoma |
Gemcitabine
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Chemotherapy; Antimetabolites;
Pyrimidine analogues Inhibits DNA methyltransferases resulting in hypomethylation Effective for treatment of myelodysplastic syndrome |
Azacitidine
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Chemotherapy; Antimetabolites;
Pyrimidine analogues Cytidine analogue effective in the treatment of hematologic malignancies Inhibits DNA polymerase Resistance due to decreased cytosine kinase activity |
Cytosine arabinose
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Chemotherapy; Antimetabolites;
Purine Analogues Prototypic purine analogues Converted to mononucleotides which feedback inhibit de novo purine synthesis Converted to triphosphates which are incorporated into DNA and RNA Resistance due to HPRT mutations or overexpression of TPMT(2) |
6-mercaptopurine
6-thioguanine |
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Chemotherapy; Antimetabolites;
Purine Analogues Inhibits adenosine deaminase, resulting in the accumulation of dATP For hairy cell leukemia |
Pentostatin
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Chemotherapy; Others;
Enzymes Converts asparagine to aspartate Deprives cells of the essential amino acid |
Asparaginase
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Chemotherapy; Others;
Tyrosine Kinase Inhibitors Competitively blocks the ARP-binding site of the c-able kinase in CML Can cause congestive heart failure |
Imatinib mesyltate (Gleevec)
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Chemotherapy; Others;
Tyrosine Kinase Inhibitors Inhibit EGF receptor-associated tyrosine kinase For treatment of non-small cell carinoma of the lung and pancreatic cancer (2) |
Erlotinib
Gefitinib |
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Chemotherapy; Others; Antibodies
Directed against the EGF receptor For head and neck and metastatic colorectal cancer |
Cetuximab
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Chemotherapy; Others; Antibodies
Induces antibody-dependent cell-mediated cytotoxicity For treatment of p185-her2 positive breast cancer |
Trastuzumab (Herceptin)
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Chemotherapy; Others; Antibodies
Directed against the VEGF receptor Inhibits angiogenesis |
Bevacizumab
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Chemotherapy; Others; Antibodies
Anti-CD20 antibody that promotes complement mediated lysis of malignant B-cells in CD-20 positive non-Hodgkin's B cell lymphoma Can result in HBV reactivation |
Rituximab
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Chemotherapy; Others; Antibodies
• Directed against myeloid cell surface antigen CD33 |
Gemtuzumab ozogamicin (Mylotarg)
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Chemotherapy; Others;
Biologic Response modifiers • Histone deacetylase inhibitor used to treat primary cutaneous T cell lymphoma |
Vorinostat
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Chemotherapy; Others;
Biologic Response modifiers • Proteasome inhibitor used for treatment of multiple myeloma and mantel cell lymphoma |
Bortezomib
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Chemotherapy; Others;
Biologic Response modifiers • First line therapy for promyelocytic leukemia |
All-trans-retinoic acid (vitamin A)
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Chemotherapy; Others;
Biologic Response modifiers Bisphosphonates useful for the treatment of hypercalcemia and osteolytic bone lesions in multiple myeloma Inhibit osteoclast activity and induce osteoclast apoptosis (2) |
Pamidronate
Zoledronate |
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Cancer Chemotherapy; Hormonal Agents; Breast Cancer
Antiestrogens Prevents binding to the Estrogen Receptor in a competitive fashion Can reduce total cholesterol and preserve bone density |
Tamoxifen
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Cancer Chemotherapy; Hormonal Agents; Breast Cancer
Antiestrogens Selective estrogen receptor modulator (SERM) Just as effective as tamoxifen with fewer side effects |
Raloxifen
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Cancer Chemotherapy; Hormonal Agents; Breast Cancer
True Estrogen Receptor Antagonists; Pure estrogen receptor antagonist For postmenopausal women whose cancer is unresponsive to tamoxifen |
Fulvestrant (Faslodex)
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Cancer Chemotherapy; Hormonal Agents; Breast Cancer
Aromatase inhibitors Inhibits the conversion of cholesterol to pregnenolone, reducing all classes of steroids Inhibits conversion of androstenedione into estrone and estradiol |
Aminoglutethimide
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Cancer Chemotherapy; Hormonal Agents; Breast Cancer
Aromatase inhibitors Selective and irreversible inhibitor of aromatase As effective as tamoxifen for advanced breast cancer, first line therapy |
Anastrozole
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Cancer Chemotherapy; Hormonal Agents; Breast Cancer
Aromatase inhibitors Selective and irreversible inhibitors of aromatase First line therapy after tamoxifen (2) |
Letrozole
Exemestane |
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Cancer Chemotherapy; Hormonal Agents; Breast Cancer
Progesterone Agonists • Benefit likely due to suppression of adrenal steroid synthesis and estrogen receptor levels (2) |
Megestrol
Medroxyprogesterone |
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Cancer Chemotherapy; Hormonal Agents; Breast Cancer
Gonadotropin-releasing hormone agonists Prolonged use leads to desensitization of FSH and LH-producing cells Can be used for metastatic breast cancer or prostate cancer |
Leuprolide
Goserelin |
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Cancer Chemotherapy; Hormonal Agents; Breast Cancer
Others • Antibody against HER2/erb-2, a member of the epidermal growth factor receptor family |
Trastuzumab (Herceptin)
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Cancer Chemotherapy; Hormonal Agents; Breast Cancer
Others For advanced breast cancer expressing high levels of HER-2 that no longer respond to trastuzumab Tyrosine kinase inhibitor |
Lapatinib (Tykerb)
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Cancer Chemotherapy; Hormonal Agents; Prostate Cancer
Non-steroidal anti-androgens Prevents the binding of endogenous androgens to the androgen receptor Pure androgen antagonist |
Flutamide
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Cancer Chemotherapy; Hormonal Agents; Prostate Cancer
Non-steroidal anti-androgens More effective in prostate cancer than flutamide Less likely to cause diarrhea or other side effects |
Bicalutamide
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Cancer Chemotherapy; Hormonal Agents; Prostate Cancer
Steroidal anti-androgens • Occasionally used for prostate cancer (2) |
Megestrol
Medroxyprogesterone |
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Cancer Chemotherapy; Hormonal Agents; Prostate Cancer
Gonadotropin-releasing hormone agonists Equivalent antitumor effects in prostate cancer as surgical castration or diethylstilbestrol treatment (2) |
Leuprolide
Goserelin |
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Cancer Chemotherapy; Hormonal Agents; Prostate Cancer
Gonadotropin-releasing hormone agonists Suppressive effects on LH and FSH production Numerous side effects |
Diethylstilbestrol
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Cancer Chemotherapy; Hormonal Agents; Prostate Cancer
Adrenal enzyme synthesis inhibitor • Inhibits P450 enzymes involved in steroid biosynthesis |
Ketoconazole
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Mycobacterial Treatments;
First-line Agents Combine the greatest level of efficacy with an acceptable level of toxicity Primary drug for chemotherapy of tuberculosis Inhibits the synthesis of mycolic acids Intracellular and Extracellular levels are similar Administer with pyridoxine B6 Activated by catalase peroxidase on the KatG gene |
Isoniazid
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Mycobacterial Treatments;
First-line Agents Combine the greatest level of efficacy with an acceptable level of toxicity Given in combination with INH Inhibits bacterial DNA dependent RNA polymerase Causes an orange-red coloration of urine Reduces the half-life of many drugs |
Rifampin
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Mycobacterial Treatments;
First-line Agents Combine the greatest level of efficacy with an acceptable level of toxicity Acts as a long-acting rifampin Avoid in pregnancy or HIV |
Rifapentine
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Mycobacterial Treatments;
First-line Agents Combine the greatest level of efficacy with an acceptable level of toxicity Inhibits the synthesis of arabinogalactan Few side effects except for optic neuritis Do not give to children |
Ethambutol
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Mycobacterial Treatments;
First-line Agents Combine the greatest level of efficacy with an acceptable level of toxicity Inhibits mycobacterial fatty acid synthase I gene involved in mycolic acid synthesis Contraindicated with liver disease or gout |
Pyrazinamide
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Mycobacterial Treatments;
Second-line Agents Fluoroquinolones |
Levofloxacin
Moxifloxacin Ofloxacin |
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Mycobacterial Treatments;
Second-line agents Does not kill intracellular microbes Causes ototoxicity and nephrotoxicity |
Streptomycin
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Mycobacterial Treatments;
Second-line agents Inhibits the synthesis of mycolic acids (similar to INH) Causes intense gastric irritation |
Ethionamide
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Mycobacterial Treatments;
Second-line agents Similar to sulfonamides High concentrations are reached in the urine |
Aminosalicylic Acid (PAS)
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Mycobacterial Treatments;
Second line agents • Irreversible inhibitor of alanine racemase and D-Ala-D-ALA synthetase agents |
Cycloserine
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Mycobacterial Treatments;
Other drugs All are given parenterally There is some cross-resistance between these antibiotics (4) |
Capreomycin
Viomycin Kanamycin Amikacin |
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Mycobacterial Treatments;
Mycobacterium avium complex • Standard to prevent drug resistance (3) |
Clarithromycin, Azithromycin, Ethambutol
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Mycobacterial Treatments;
Mycobacterium avium complex • May be necessary to add to the drug regime (3) |
Rifabutin, Clofazimine, Quinolone
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Mycobacterial Treatments;
Hansen's disease Paucibacillary with 5 or few lesions Inhibits folate synthesis, same as the sulfonamides Can cause hemolysis |
Dapsone
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Mycobacterial Treatments;
Hansen's disease Paucibacillary with a single skin lesion (3) |
Rifampin
Minocycline Ofloxacin |
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Mycobacterial Treatments;
Hansen's disease Multibacillary with 6 or more lesions • Acts very slowly, mechanism of action unknown |
Clofazimine
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Mycobacterial Treatments;
Hansen's disease Others • Mandatory use of two contraceptives and monthly pregnancy test |
Thalidomide
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Antimalarials; Arylaminoalcohols
Rapidly kill blood stage of P. falciparum DOC for acute severe disease Cardiotoxicity |
Quinidine
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Antimalarials; Arylaminoalcohols
Rapidly kill blood stage of P. falciparum DOC for most P. falciparum regions Prophylaxis of MDR malaria in the US Neuropsychiatric concerns, contraindicated in seizure patients |
Mefloquine
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Antimalarials;
4-aminoquinolones Kills blood stage parasites by accumulating in the acid vacuole of the parasite and interfering with heme polymerase P. falciparum resistance DOC for Rx and Px for non-P.falciparum malaria |
Chloroquine
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Antimalarials;
8-aminoquinolones For hypnozoites in the liver Terminal prophylaxis Contraindicated for G-6-PD deficiency and pregnancy |
Primaquine
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Antimalarials;
Antibiotics For blood stage treatment Slow acting but effective DOC for prophylaxis in mefloquine resistant P.falciparum areas |
Doxycycline
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Antimalarials;
Combination chemicals Combo proguanil and atovaquone For uncomplicated multi-drug resistant P.falciparum There are concern of development to proguanil resistance |
Malarone
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Antimalarials;
Individual Drugs Quinine Quinidine |
Cinchona Alkaloids
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Antimalarials; Individual Drugs
• Rapid acting blood schizonticide indicated for the treatment of mild-to-moderate P.falciparum and P. vivax |
Halofantrine HCl (phenanthrenemethanol)
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Antimalarials; Individual Drugs
Extracts from Chinese medicinal plants Most rapidly acting of all antimalarials |
Artemisinin Derivatives
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Antimalarials; Individual Drugs
Combo that inhibits dihydrofolate reductase and conversion of PABA For chloroquine-resistant P.falciparum |
Fansidar (Pyrimethamine-Sulfadoxine)
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Antiparasitics
Amebiasis Lumenal Drug Liberates iodine which is the active amebicide |
Iodoquinol
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Antiparasitics
Amebiasis Lumen drug Aminoglycoside antibiotic, acts on protein synthesis |
Paromomycin
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Antiparasitics
Amebiasis Mixed amebicide Acts as an electron sink to prevent the terminal electron transport system from reoxidizing NADH to NADPH Avoid during pregnancy |
Metronidazole
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Antiparasitics
Cryptosporidiosis Inhibits pyruvate-ferredoxin oxidoreductase |
Nitazoxanide
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Antiparasitics
Cyclosporiasis |
TMP/SMZ
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Antiparasitics
Giardiasis 85-95% effective Mixed amebicide Acts as an electron sink to prevent the terminal electron transport system from reoxidizing NADH to NADPH Avoid during pregnancy |
Metronidazole
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Antiparasitics
Giardiasis Available in pediatric suspension Inhibits pyruvate-ferredoxin oxidoreductase |
Nitazoxanide
|
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Antiparasitics
Giardiasis Used to treat pregnant women |
Paromomycin
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Antiparasitics
Isosporiasis |
TMP/SMZ
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Antiparasitics
Trichomoniasis Drug of choice Mixed amebicide Acts as an electron sink to prevent the terminal electron transport system from reoxidizing NADH to NADPH Avoid during pregnancy |
Metronidazole
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Antiparasitics
Trichomoniasis Restores the acidic environment |
Vinegar douches
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Antiparasitics
AIDS patients Toxoplasmosis • Folate antagonist |
Pyrimethamine with sulfadiazine
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Antiparasitics
AIDS patients Toxoplasmosis • Folic acid supplement to prevent bone marrow suppression |
Leucovorin
|
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Antiparasitics
AIDS patients Toxoplasmosis • Antibiotics prophylactic treatment |
TMP/SMZ
|
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Antiparasitics
AIDS patients Toxoplasmosis • Prophylactic treatment (3) |
Pyrimethamine Dapsone Leucovorin
|
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Antiparasitics
AIDS patients Pneumocystosis (PCP) • Drug of choice but high incidence of adverse reactions |
TMP/SMZ
|
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Antiparasitics
AIDS patients Pneumocystosis (PCP) • Second line drugs of choice (2) |
Pentamidine
Atovaquone |
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Antiparasitics
AIDS patients Pneumocystosis (PCP) • Prophylactic treatment, necessary in AIDS patients (2) |
TMP/SMZ
Aerosolized pentamidine |
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Antiparasitics
AIDS patients Protozoan infections Inhibitory analog of ubiquinone which interferes with mitochondrial electron transport |
Atovaquone
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Antiparasitics
AIDS patients Protozoan infections Causes selective breaks in the kinetoplast mini-circle DNA of trypanosomes Can cause diabetes |
Pentamidine isethionate
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Antiparasitics
Babesiosis (2) |
Clindamycin
Quinine |
|
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Antiparasitics
African Trypanosomiasis T. brucei gambiense • Initial stage |
Pentamidine
|
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Antiparasitics
African Trypanosomiasis T. brucei gambiense Late stage Arsenical, which reacts with sulfhydryl groups in protein Very toxic |
Melarsoprol
|
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Antiparasitics
African Trypanosomiasis T. brucei gambiense Late stage and relapses Suicide inhibitor of ornithine decarboxylase |
Eflornithine
|
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Antiparasitics
African Trypanosomiasis T. brucei rhodesiense Initial stage Inhibits large numbers of enzymes |
Suramin
|
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Antiparasitics
African Trypanosomiasis T. brucei rhodesiense Late stage and relapses |
Melarsoprol
|
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Antiparasitics
Chagas Disease Amastigotes and extracellular mastigote Converted to a superoxide radical and a peroxide |
Nifurtimox
|
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Antiparasitics
Leishmaniasis Drug of choice in the US Trivalent form inhibits the parasite's phosphofructokinase |
Sodium stibogluconate
|
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Antiparasitics
Leishmaniasis Second line for mucocutaneous or visceral leishmaniasis |
Amphotericin B
|
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Antiparasitics
Leishmaniasis Second line for cases which are resistant |
Pentamidine
|
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Antihelminthics
Nematode infections Benzimadozoles Useful with highly infected populations Contra-indicated in pregnancy |
Mebendazole
|
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Antihelminthics
Nematode infections Benzimadozoles Has replaced other drugs as the drug of choice for a number of intestinal helminths Contra-indicated in cirrhosis or pregnancy |
Albendazole
|
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Antihelminthics
Nematode infections Benzimadozoles Treatment for Strongyloides stercoralis (threadworm) |
Thiabendazole
|
|
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Antihelminthics
Nematode infections Others For pinworm and hookworm Depolarizing neuromuscular blocker leading to release of acetylcholine and persistent nicotinic stimulation |
Pyrantel pamoate
|
|
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Antihelminthics
Antifilarial Agents • May have an effect on the surface coat of the parasite |
Diethylcarbamazine
|
|
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Antihelminthics
Antifilarial Agents Highly potent and broad spectrum antihelminthic activity Causes an influx of chloride ions through specific channels |
Ivermectin
|
|
|
Antihelminthics
Schistosomiasis and Tapeworm infections Broad spectrum against schistosomes, and drug of choice for tapeworms Increases permeability to calcium ions |
Praziquantel
|
|
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Antihelminthics
Schistosomiasis and Tapeworm infections Second drug of choice for tapeworms Potent inhibitor of fumarate reductase, blocking ATP production |
Niclosamide
|
