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P3 - Therapy 3 - Antibiotic MOAs
P3 - Therapy 3 - Antibiotic MOAs
14
Pharmacology
Professional
01/22/2013

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Term
Beta-lactams
Definition
Competitive inhibitors of penicillin binding protein (PBP) preventing PBP from cross-linking the peptidoglycan strands of the bacterial cell wall resulting in bacterial lysis. (bactericial)(Penicillins, Cephalosporins, Carbapenems, Monobactams)
Term
Beta-Lactamase Inhibitors
Definition
Suicide substrates for beta-lactamase preventing its hydrolytic action on penicillin; it also directly binds to the PBP increasing the antibacterial activity of beta-lactams (Clavulanic Acid, Sulbactam, Tazobactam, Clavulanate)
Term
Cyclic Glycopeptides
Definition
Uses Ca+ to insert tail into bacterial plasma membrane then aggregates forming a pore allowing K+ to move out of the bacterial cell resulting in depolarization of the membrane and loss of action potential. This halts all metabolic activity in the cell including DNA, RNA, and protein synthesis. Cell lysis does not occur. (Daptomycin)
Term
Cell Membrane Agents
Definition
Binds to lipopolysaccharide in the gram negative cell wall disrupting its structure allowing the leakage of cellular contents. (Bactericidal)(Polymyxin B, E)
Term
Fluoroquinolones
Definition
Prevent bacterial DNA synthesis by blocking topoisomerase II (DNA gyrase), which unwinds DNA for initiation of replication, and topoisomerase IV, which separates replicated chromosomal DNA into daughter cells. (Ciprofloxacin, Levofloxacin, Moxifloxacin, Gemifloxacin, Ofloxacin)
Term
Nitroimidazoles
Definition
Causes loss of DNA's helical structure and also strand breakage. (Metronidazole)
Term
Rifamycins
Definition
Inhibit the beta subunit of DNA-dependent RNA polymerase preventing RNA formation and ultimately DNA synthesis (Rifampin)
Term
Folic Acid Inhibitors
Definition
Structural analog of para-aminobenzoic acid (PABA), the normal substrate for dihydropteroate synthase. Acts as a competitive inhibitor for dihydropteroate synthase preventing dihydrofolic acid production, a substance necessary for purine and, ultimately, DNA synthesis. Timethoprim works to additionally block dihydrofolate reductase, an enzyme that is responsible for tetrahydrofolic acid formation, another component in the formation of purines and ultimately DNA. The addition of trimethoprim makes the combination bactericical. Without trimethoprim, sulfmethoxazole is only bateriostatic. (Sulfamethoxazole+Trimethoprim)
Term
Tetracyclines
Definition
Blocks incoming, charged tRNA from binding to the 30S subunit of the bacterial ribosome preventing protein synthesis. (Bacteriostatic)(Doxycycline, Minocycline)
Term
Glycylcyclines
Definition
Same MOA as tetracycline. (Bacteriostatic)(Tigecycline)
Term
Macrolides
Definition
Bind to the 50S subunit of the bacterial ribosome preventing the aminoacyl translocation of the forming protein stopping its synthesis. (Erythromycin, Azithromycin, Clarithromycin)
Term
Nitrofurans
Definition
Reduced by flavoproteins to active intermediates that may inactivate or damage ribosomal proteins, DNA, and RNA (Nitrofurantoin)
Term
Lincosamides
Definition
They bind to the 23s portion of the 50S subunit of bacterial ribosomes and cause premature dissociation of the peptidyl-tRNA from the ribosome. (Clindamycin)
Term
Fidaxomicin
Definition
Inhibits RNA synthesis by inhibiting RNA polymerase.
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