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56 Cards in this Set
- Front
- Back
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importance of beta-lactam ring
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chief structural requirement for biologic activity; antibacterial activity of penicillin resides in the ring
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coverage of PCN G
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highest activity against gram (+) bacteria, anaerobes
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is PCN effective against Staph aureus?
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NO!
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does PCN G have antipseudomonal activity?
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no
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How is PCN G eliminated?
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kidneys
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What is the effect of Probenacid on PCN G?
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block tubular secretion of PCN G and is used to ↑ systemic level in severe infections
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PCN G is the DOC for what?
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N. meningitides
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What is the administration route for PCN V?
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oral; acid resistant
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What are the penicillinase resistant penicillins?
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Nafcillin
Oxacillin Cloxacillin Dicloxacillin Methicillin |
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How are Oxacillin, Nafcillin and Cloxacillin metabolized?
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liver metabolism, renal excretion
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What are the extended spectrum penicillins?
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Ampicillin
Amoxicillin |
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What is the importance of combining Ampicillin and Amoxicillin with penicillinase inhibitors?
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covers anaerobes
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What are the anti-pseudomonal penicillins?
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Carbenicillin
Ticarcillin Mezlocillin Piperacillin |
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What are the beta-lactamase inhibitors?
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Clavulanic acid
Sulbactam Tazobactam |
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What is Aztreonam?
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monobactam
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Is Aztreonam resistant to penicillinase?
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yes
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What is the coverage of Aztreonam?
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ONLY works against gram negatives
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is Aztreonam safe to use in pts with PCN allergy?
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yes
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Are carbapenems resistant to penicillinase?
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yes
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What are the carbapenem drugs?
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Imipenem
Cilastatin Meropenem Ertapenem |
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What must Imipenem be administered with?
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inhibited by dihydro-peptidase so used in combination with Cilistatin
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What is the coverage of Carbapenems?
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broad spectrum activity (anaerobes, gram (+), and gram(-) rods)
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MOA for vancomycin?
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inhibits elongation of peptidoglycan chain
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Coverage of vancomycin?
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effective against gram (+) bacteria & anaerobes only
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What are the therapeutic uses for vancomycin?
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DOC for MRSA
given orally for C. difficile pseudomembranous colitis |
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How is vancomycin excreted?
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kidney - filtered, NOT reabsorbed
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Adverse effects of vancomycin
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ototoxic & nephrotoxic
“Red Man Syndrome” from histamine release |
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MOA of fosfomycin?
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inhibits first step in cell wall synthesis
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can fosfomycin be combined with beta-lactams?
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yes b/c their mechanisms are different
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therapeutic use for fosfomycin?
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alternative for uncomplicated UTI in women
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coverage of bacitracin?
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gram (+) bacteria
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adverse effect of bacitracin?
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nephrotoxicity
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MOA for cycloserine?
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competes with D-alanine for two enzymes, L-alanine racemase and D-alanine synthetase, both of which are involved in the incorporation of D-alanine into bacterial cell walls. Cycloserine inhibits both enzymes and peptidoglycan synthesis, resulting in a weak cell wall and eventually cell lysis.
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therapeutic use for cycloserine?
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used as second line for multi-resistant TB
also used for UTIs |
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adverse effects of cycloserine?
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CNS effects
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MOA for macrolides
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binds reversibly to 50 S ribosomal subunits and interferes with the translocation step wherein the nascent peptide chain is moved from the A to the P site (ultimately inhibiting protein synthesis of the bacteria).
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coverage for macrolides?
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gram (+)
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adverse effects for erythromycin?
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diarrhea due to stimulation of motilin receptors and inhibition of cyt P450 system
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adverse effects of clarithromycin?
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least amount of diarrhea but still inhibits the P450 system
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adverse effects of azithromycin?
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no effect on the P450 system because it is excreted into the bile but it is NOT metabolized by the liver. In terms of diarrhea, it is in between erythromycin and clarithromycin
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what main adverse effect do all macrolides have?
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can cause prolonged QT and torsades de pointes. Erythromycin has a double effect on QT due to it’s direct effect and through the inhibition of hepatic metabolism of other drugs, thus increasing their serum concentration
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what is telithromycin?
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ketolide which is a derivative of macrolides
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coverage of telithromycin?
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broad spectrum with greater bacterial killing effect than macrolides
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adverse effect of telithromycin
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hepatotoxicity
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coverage of clindamycin?
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excellent coverage against Staph aureus and good coverage against anaerobes. Both gram positive and negative agents are susceptible
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therapeutic use for clindamycin?
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accumulates in the bones and is a good treatment of osteomyelitis due to effect against Staph aureus
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adverse effect of clindamycin?
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pseudomembranous colitis
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MOA for Dalfopristin and Quinupristin
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irreversibly binds to the 50S subunit
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therapeutic uses for Dalfopristin and Quinupristin
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vancomyocin resistant Enterococcus faecium & complicated Staph. Aureus skin infections
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how is Dalfopristin and Quinupristin administered?
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IV
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problem with Dalfopristin and Quinupristin
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inhibits cytochrome P450 3A4 and will decrease the elimination of drugs metabolized by this enzyme (don’t have to worry about Digoxin b/c it’s excreted by the kidneys)
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What is linezolid?
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Oxazolidinone which binds to the 50S subunit
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coverage of linezolid?
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gram (+)
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does linezolid have CNS penetration?
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yes
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how is linezolid metabolized?
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spontaneous metabolization and is NOT metabolized by the liver
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major problem with linezolid
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reversible non-selective MAO inhibitor which causes a lot of drug interactions (can’t eat fava beans from those pesky Mediterranean restaurants anymore b/c BP will increase)
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