14.1, 14.3 Flashcards
What are the prominent drugs in B-lactams
Penicillin, cephalosporin, monobactam, carbapenem
Presence of lactam ring and is similar to peptidoglycan subunit makes it a _____
B-lactams
Which B-lactams derives from fungi; mostly against G+, some G- ?
Penicillins
Which B-lactams are similar to penicillins; resistance to B-lactamases
Cephalosporins
Which B-lactams is broad spectrum against G+/G- ?
Carbapenems
Which B-lactams is narrow spectrum, G- only
Monobactams
What is the MOA of B-lactams?
inhibitors of cell wall synthesis; blocks cross-linking of peptide chains in new peptidoglycan
What cell wall drugs binds to end of peptide chain to block subunits from adding to peptidoglycan backbone; G+ only
Vancomycin
What cell wall drugs is derived from B. Subtilis; blocks transport of peptidoglycan precursors ?
Bacitracin
What inhibitors of protein synthesis bind to 30S subunit of ribosome and impair “proofreading” ability
Aminioglycosides
What is streptoycin, gentamicin, and neomycin examples of?
Aminoglycosides
What inhibitor of protein synthesis bind to 30S; blocks association of tRNA with ribosome
Tetracyclines
What 3 inhibitors of protein synthesis binds to 50S subunit and inhibit peptide bond formation in specific combos of amino acids?
Macrolides, Lincosamides, Chloramphenicol
Macrolides’ spectrum? Cidal or static?
Broad spectrum, -static
What inhibitor of protein synthesis has a narrow spectrum; -static; particularly active against streptococcal and staphylococcal infections?
Lincosamides
Which inhibitor of protein synthesis is broad spectrum; static; rarely used now because of serious side effects
Chloramphenicol
What inhibitor of Protein synthesis binds to the 50S ribosomal subunit and interferes with association of 30S and other factors? What spectrum and is it static or cidal?
Oxazolidinones; broad spectrum, -static
What inhibitor of membrane function is lipophilic and interacts with LPS to disrupt outer and inner membrane of Gram (-) and targets host membranes?
Polymyxins
Which inhibitor of membrane function is a cyclic lipopeptide that inserts and disrupts Gram + membrane?
Daptomycin
Which inhibitor of nucleic acid synthesis interferes w/ DNA replication; not very selective in toxicity? What spectrum and is it cidal or static?
metronidazole; broad spectrum, -cidal
What inhibitor of nucleic acid synthesis blocks RNA polymerase activity; can treat semi-dormant M. Tuberculosis; BUT can be antagonistic and hepatotoxic? What spectrum (effect on G+/G-); cidal or static
Rifampin; narrow spectrum, cidal
Which inhibitor of nucleic acid synthesis inhibits DNA gyrase enzyme; selective toxicity but many side effects? What type of spectrum; cidal or static?
Fluoroquinolones; broad spectrum; cidal
What inhibitor of metabolic pathways halts folic acid synthesis and production of pyrimidines and purines; often used trimethoprim? What spectrum; static or cidal?
Sulfonamides (sulfa drugs); Broad spectrum; static alone
Which inhibitor of metabolic pathways inhibits later stage of folic acid synthesis? What is combined with this to make it cidal?
Trimethoprim; sulfamethoxalzale
Which inhibitor of metabolic pathways involves specific toxicity for mycobacteria to block synthesis of mycolic acid
Isoniazid
Which inhibitor of ATP Synthase inhibits mycobacterial growth; exact mechanisms is unknown but evidence shows interference with ATP synthase and reducing available ATP
Diarylquinolines
When did ancestors use antimicrobials
350 AD
When were the first drugs developed by science?
Early 1900s
What is it called when theres drugs that target living cells and tissues? Are antimicrobial drugs are categorized in this term?
Chemotherapy; yes, they target microbes
Who scanned through 600 arsenic compounds to find cure for syphilis w/o killing host and found a compound that targeted treponema pallidum and established modern drug discovery methods?
Paul Ehrlich
Who used synthetic dye, prontosil, to treat strep infections and what did this 1st synthetic antimicrobial open the door for?
Josef, Klarer, Fritz Mietzch, and Gerhard Domagk; sulfa drugs and other synthetic antimicrobials
Who accidentally discovered antibiotic from Penicillium notatum growing on bacterial agar plate w/ Staphylococci (1928)?
Alexander Flemming
What was the first natural antibiotic?
Penicillin
Who used X-rays to analyze the structure of penicillin and what was it used for?
Dorthy Hodgkins; used to create modified penicillins (semisynthetic antimicrobial)
Who studied soil microbes and discovered several antimicrobials and what are the source of >50% of natural antibiotics?
Selman Waksman; actinomycetes
