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35 Cards in this Set
- Front
- Back
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chemotherapeutic agents
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drugs that act against diseases
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antimicrobial agents
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drugs that treat infections
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Paul Erlich
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Magic Bullets: arsenic compounds that killed microbes
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Alexander Fleming
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Penicillin
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Gerhard Domagk
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sulfanilamide
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Antibiotics
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Antimicrobial agents produced naturally by organisms
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Greatest numbers of antibiotics derived from:
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Streptomyces (bacterium); Bacillus (bacterium); Penicillium (fungi); Cephalosporium (fungi)
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Beta-lactams
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bind to enzymes that cross-link NAM subunits
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Vancomycin and Cycloserine
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Interfere with particular alanine-alanine bridges that link NAM subunits in many Gram-positives
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Bacitracin
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Blocks secretion of NAG and NAM from cytoplasm
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Isoniazid and Ethambutol
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Disrupt mycolic acid formation in mycobacterial species
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Phosphonomycin
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Blocks coversion of UDP-NAG to UDP-NAM by blocking pyruvyl transferase
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Aminoglycosides (Streptomycin, Gentamycin)
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Change shape of 30s so that mRNA is misread
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Streptogramins, Lincosamides, macrolides
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bind to 50s subunit, blocking proper mRNA movement through the ribosome
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Tetracycline
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Block docking site (A) of 30s subunit
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Fomiversen
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blocks ribosomal subunits from attaching to mRNA by creating a complementary strand of nucleic acids to the mRNA strand
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Polyenes, Gramicidin
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Form channel through cytoplasmic membrane and damage its integrity. Polyenes: Nystatin and Amphotericin B attach to ergosterol in fungal membranes
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Azoles and Allyamines
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inhibit ergosterol synthesis
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Polymixin
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disrupts cytoplasmic membranes of Gram-negatives: toxic to human kidneys
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Pyrazinamide
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disrupts transport across cytoplasmic membrane of M. tuberculosis
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Praziquantel and Ivermectin
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Work against cytoplasmic membranes of parasites by changing permeability
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Sulfonamides, Trimethoprim
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Inhibit metabolism of PABA
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Amantadine, Rimantadine, weak organic bases
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Prevent uncoating of viruses
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Protease inhibitors
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interferes with protease enzyme that HIV uses
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Nucleotide analogs (Acyclovir, Ribavarin, Azidothymidine)
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Interfere with function of nucleic acids
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Quiolones and Fluoroquinolones (Ciprofloxacin, Nalidixic acid)
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Act against prokaryotic DNA gyrase
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Rifampin
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inhibits RNA polymerase during transcription (good against M. tuberculosis
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Clofazimine
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binds to DNA of Mycobacterium leprae
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Pentamidine and Propamidine
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bind to protozoan DNA
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Reverse transcriptase inhibitors
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works against HIV uses in replication cycle
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Metronidazole
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Nitro group enters cells and is reduced in cytoplasm and forms cytotoxic compounds that disrupt the bacterial or protozoan DNA
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Attachment Antagonists
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block viral attachment or receptor proteins so that viruses cannot attach
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Mechanisms of microbial resistance
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Production of enzyme that destroys drug (beta-lactamase), slow or prevent entry of drug into cell, alter target of drug (sulfonamides), alter metabolic chemistry, pump antimicrobial drug out of cell, biofilm producing bacteria
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MfpA protein of M. tuberculosis
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Binds DNA gyrase preventing binding of fluoroquinolone drugs
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Superdrugs
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Multiple drug resistant pathogens
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