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Unit 2: Antimicrobial Chemotherapeutics (Ch. 33-35)

Terms in this set (39)

What Type of Topoisomerase is used for decatenation?
Type II DNA gyrase
What is the most common type of topoisomerase that is targeted by antibiotics?
Type II DNA gyrase
Quinlones- What type of inhibitors, action on growth of bacteria, and on gram + or - cells
bactericidal, type II, gram -
Drug example of Quinolones
Ciprofloxacin- bactericidal; inhibit DNA gyrase (gram-negative), and TOPIV (gram positive
What drug class targets RNA polymerase that controls transcription in bacteria
Rifampin
Rifampin- What type of inhibitors, action on growth of bacteria, and on gram + or - cells
bactericidal, inhibits RNA synthesis, allows initiation but blocks elongation, treatment of TB (mycobacterium)
Aminoglycosides- what subunit is targeted, what effect on growth of bacteria, drug examples, and effect on translation
30S subunit, bactericidal, · streptomycin, neomycin, tobramycin, etc., induce misreading and halt protein synthesis
Spectinomycin- what subunit is targeted, what effect on growth of bacteria, and effect on translation
30S subunit, bacteriostatic, prevent translocation of 70S
Tetracycline- what subunit is targeted, what effect on growth of bacteria, drug examples, effect on translation, what is it used to treat
30S subunit, bacteriostatic, doxycline, inhibit tRNA binding to A site, used to treat anthrax
Macrolides- what subunit is targeted, what effect on growth of bacteria, drug examples, effect on translation, what is it used to treat
50S subunit, bacteriostatic, erythromycin (Azithromycin and clarithromycin), inhibit translocation, used to treat pulmonary infections and Legionnaires' disease
Chloroamphenicol- what subunit is targeted, what effect on growth of bacteria, effect on translation, what is it used to treat
50S subunit, bacteriostatic, inhibit peptidyl transferase, used to treat typhoid fever, meningitis, and rickettsia
Lincosamides- what subunit is targeted, what effect on growth of bacteria, drug examples, effect on translation, what is it used to treat
50S subunit, bacteriostatic, Clindamycin, inhibit peptidyl transferase, treatment of anaerobic bacterial infections
Streptogramins- what subunit is targeted, what effect on growth of bacteria, drug examples, effect on translation, what is it used to treat
50S subunit, bactericidal, Dalfopristin, guinupristinin; inhibits peptidyl transferase and translocation, used to treat enterococcus and streptococcus
Oxazolidinones-what subunit is targeted, what effect on growth of bacteria, drug examples, what is it used to treat
50S subunit, bacteriostatic, Linezolid, used to treat MRSA and other penicillin and vancomycin-resistant bacteria
What are the inhibitors of murein monomer synthesis
Fosfomycin, cycloserine, bacitracin
What are the inhibitors of murein polymer synthesis
vancomycin
what are the inhibitors of polymer crosslinking
penicillin, methicillin, amoxicillin, and ampicillin
Gram-positive cell wall charactertistics
several layers of peptidoglycan made of murein, thin periplasmic space, no porins
Gram-negative cell wall charactertistics
LPS, porins, thick periplasmic space, single layer of murein
Mycobacteria cell wall characteristics
single layer of murein, porins, extractable phospholipids, mycolic acids, arabinogalactan
What are the three steps in cell wall synthesis and where do they occur?
Murein monomer synthesis- amino acids and sugar building blocks (intracellular) Murein monomer polymerization (membrane) polymer cross-linking (extracellular, periplasmic space)
Fosfomycin- what step of cell wall synthesis does it inhibit, what target does it inhibit, what does it treat
inhibits murein monomer synthesis, PEP analogue inhibits MurA in gram-negative urinary tract infections
Cycloserine- what step of cell wall synthesis does it inhibit, what target does it inhibit
inhibits murein monomer synthesis, D-Ala analogue inhibits alanine racemase/synthase
Bacitracin- what step of cell wall synthesis does it inhibit, what target does it inhibit, what does it treat
inhibits murein monomer synthesis, peptide antibiotic inhibits dephosphorylation of BP
Vancomycin- what step of cell wall synthesis does it inhibit, how does it affect bacterial growth, what target does it inhibit, what does it treat
inhibitor of murein polymer synthesis, bactericidal, inhibits transglycosidase, treats MRSA
What are the major classes of drugs used as inhibitors of polymer crosslinking
Cephalosporins, Monobactams, carbapenems
What is the difference between penicllin G and penicillin V
penicillin G (intravenous)
penicillin V (oral)
Why are beta-lactamase inhibitors useful when using Amoxicillin and Ampicillin and what are the two inhibitors used?
increased effectiveness in combination with beta-lactamase inhibitor
What are the 4-generation of cephalosporins and what are they used to treat and when are they a useful treatment over penicillins
1st generation- cefazolin (broad spectrum)
2nd generation- cefotetan (intra-abdominal)
3rd generation- ceftriaxone (gram-negative, Lyme disease) 4th generation- cefepime (broad spectrum)
useful treatment over penicillin when patient is allergic
What beta-lactam antibiotic is used if you are very allergic to penicillins
Monobactams
What beta-lactam antibiotic can cause seizures
Carbapenems
Explain how a person can become allergic to penicillin
a person's immune system becomes hypersensitive to the drug and mistakenly reacts to the drug as a harmful substance
What are the two major classes of antimycobacterial agents and are they static or cidal and give an example of each
Arabinogalactan synthesis inhibitors: bacteriostatic, ethambutol
Mycolic acid synthesis inhibitors: Pyrazinamide (inhibit FAS1; bactericidal), Isoniazid (inhibit FAS2; bactericidal)
What is the 4-regimen TB treatment and what determines what is used
4-drug regimen for TB treatment (isoniazid resistance greater that 4%)
Rifampin, Streptomycin, Isoniazid, and Ethambutol
What is the 3-regimen TB treatment and what determines which is used
3-drug regimen if isoniazid resistance is low. Leave out Ethambutol (visual impairment side effects)
What are the 5 antifungal drug targets and give an example of each
Ergosterol synthesis inhibitors (terbinafine, ketoconazole, fluconazole)

Cell wall synthesis inhibitors (echinocandins)

fungal nucleic acid synthesis inhibitors (flucytosine)

fungal mitosis inhibitors (Grisefulvin)

Fungal mitosis stability inhibitors (Amphotericin B)
What are the 3 ergosterol synthesis inhibitors and what class do they represent and what are they used to treat and how?
Terbinafine- treatment of ringworm, inhibits squalene epoxidase, oral and topical formulations

Ketoconazole- topical antifungal treatment, 14-alpha-Sterol-Demethylase inhibitor

Fluconazole- treats fungal meningitis, 14-alpha-Sterol-Demethylase inhibitor, oral and topical
What drug is selective for fungi because they have a cytosine permease
Flucytosine
What drug forms channels in the fungi by binding to ergosterol and is a polyene macrolide agent
Amphotericin B
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