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62 Cards in this Set
- Front
- Back
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Aminoglycosides
-MOA |
Bactericidal
Bainds 30S subunit, blocks initiation complex, misreads RNA, inhibits translocation, cell death Disrupts polysomal structure, nonfunxnal monosomes |
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Aminoglycosides
-Uses |
Gram- nosocomial infxn
Mycobacteria (2nd line strepto/amikacin) Pseudomonas Gram+ (esp in synergy w/cell-wall active agent) Gram- rods-enterobacteriaiciae, acinetobacter, pseudomonas Only for SERIOUS IFXNS |
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Aminoglycosides
-PK |
Concentration dependent (One large, infrequent dose)
IM, SQ, IV, low BA Topical--neomycin, kanamycin Renal elimination short t1/2 Bad penetration lungs, bone, CNS, abscess Less active in acidic env't or Ca/Mg Gram-neg=high dose systemic, low UTI Gram-pos=low dose, synergy PHARM MONITORING |
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Aminoglycosides
-AEs |
Nephrotoxicity (rev)
Ototoxicity (irrev) neuromm blockade high dose Allergy |
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Aminoglycosides
-Resistance |
Due to enzymatic inactivation (enterbacteraciae)
Altered membrane permeability (pseudomonas) Targe site mutation Gent>Tobra>Amik against pseudomonas |
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Gentamicin
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Aminoglycoside
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Tobramycin
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Aminoglycoside
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Amikacin
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Aminoglycoside
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Neomycin
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Aminoglycoside
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Streptomycin
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Aminoglycoside
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Lincosamides
-MOA |
Bacteriostatic
Inhibits peptidyl transferase by binding 50S subunit |
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Lincosamides
-Spectrum |
Aspiration pneumonia, SSTIs
Anaerobic infxn, acne Not C. dif Staph (comm acquired MRSA) strep Anaerobes NOT atypicals/enterococci |
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Lincosamides
-PK |
Concentration independent
high BA PO or IV Liver metabolism biliary and renal excretion Minimal CNS penetration |
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Lincosamides
-AE |
Pseudomembranous colitis
Disarrhea Ab pain, Nausea Rash |
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Lincosamides
-Resistance |
Alterations in target site
MSLB gene Gram positives often cross resistant w/macrolides and streptogramins D test positive=clindamycin resistant |
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Clindamycin
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Lincosamide
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Macrolides
-MOA |
Bacteriostatic
Inhibits translation by binding 23SrRNA of 50S: blocks exit tunnel for new peptides |
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Macrolides
-Spectrum |
Community acquired pneumonia
URTIs STDs MAI/MAC PUD S. pneumo Atypicals GNR (H flu M catarrhalis) H pylori |
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Macrolides
-PK |
High intracellular concentrations
Concentration-independent High BA, PO, IV Excellent lung penetration, poor CNS Azithromycin-2 phase elimination (long clinically) Hepatic/biliary elimination Clarithromycin/azithromycin have less resistance |
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Macrolides
-AEs |
GI N/V/D w/hi doses esp w/erythromycin
Rash Drug interaxns-low with azithro, erythro/clarithro inhibit CYP450, increases QT, potential torsades |
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Macrolides
-Resistance |
Efflux pump
Altered target site MSLB gene |
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Erythromycin
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Macrolide
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Clarithromycin
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Macrolide
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Azithromycin
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Macrolide
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Ketolides
-MOA |
Macrolide analogue w/ increased activity against s.pneumo
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Ketolides
-Spectrum |
CAP outpatient
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Ketolides
-PK |
PO only 1x/day
eliminated biliary renal |
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Ketolides
-AEs |
similar to macrolides w/addt toxicity (hepatotoxicity)
Visual disturbances Fainting episodes |
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Ketolides
-Resistance |
Poor substrate to efflux pumps
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Telithromycin
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Ketolide
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Tetracyclines
-MOA |
Bacteriostatic
Reversibly binds 16SrRNA of 30S to block tRNA from binding ribosome-mRNA complex |
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Tetracyclines
-Spectrum |
BROAD spectrum
CAP, tick disease, PUD, STDs, SIADH Acne Atypicals GNR, GPC B. anthracis, B. burgdorferi, Y. pestis, T. pallidum, H. pylori Minocycline against MRSA |
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Tetracyclines
-PK |
Concentration independent
High BA, PO, no IV, crosses placenta Poor CNS penetration Mino/doxy hepatically elim, tetra renally |
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Tetracyclines
-AEs |
Tooth discoloration
Contra Teens Contra pregnancy N/V/borborygmous Drug interaxns-multivalent cations, lower absorption w/ milk no absorp Cell-wall synthesis inhibitors decrease cidal activity |
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Tetracyclines
-Resistance |
Widespread
efflux pump formation of ribosomal protection protins that interfere w/binding |
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Telithromycin
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Ketolide
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Minocycline
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Tetracycline
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Tetracycline
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Tetracycline
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Doxycycline
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Tetracycline
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Glycylcyclines
-MOA |
Modified tetracycline w/expanded spectrum
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Glycylcyclines
-Spectrum |
SSTIs
intra-abdominal infxn not c.dif GNR GPC including MRSA/VRE not pseudomonas or proteus-not things that start with a p |
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Glycylcyclines
-PK |
IV only
biliary excretion t1/2=30-36 hr Large Vd |
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Glycylcyclines
-AEs |
N/V dose dependent
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Glycylcyclines
-Resistance |
Extra side chain prevents efflux pump
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Tigecycline
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Glycylcyclines
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Chloramphenicol
-MOA |
Bacteriostatic
Binds 23s rRNA of 50S to inhibit protein synthesis by blocking tRNA (prevent aa linking), blocking peptidyl transferase |
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Chloramphenicol
-Uses |
BROAD spectrum
VRE strep, staph, enterococci, VRE anaerobes GNR, NOT pseudomonas |
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Chloramphenicol
-PK |
High BA, PO, IV
topical good CNS but dont use because bacteriostatic Hepatic metabolism via conjugation |
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Chloramphenicol
-AEs |
Gray baby syndrome-inability to conjugate chlor deficient in glucuronosyltransferase, vomiting, flaccidity, gray color, resp distress, metabolic acidosis CONTRA neonates
Bone marrow suppression, dose-related, idiopathic Drug interactions, increases levels of phenytoin, phenobarbital, warfarin |
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Chloramphenicol
-Resistance |
Enzymatic inactivation
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Streptogramins
-MOA |
Bactericidal when used in combo!
Bacteriostatic v.enterococcus faecium Binds to different parts of 23s rRNA of 50S to prevent elongation |
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Streptogramins
-Spectrum |
Narrow spectrum
VRenterococcus faecium MRSA infxns Staph, strep atypicals |
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Streptogramins
-PK |
IV only
hepatically metabolized Some CNS penetration |
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Streptogramins
-AEs |
Phlebitis, myalgias
hepatotoxicity line crystallization when mixed with saline Drug interaxns |
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Streptogramins
-Resistance |
Altered target site
-MSLB Efflux pump |
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Quinupristin/dalfopristin
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Synercid
Streptogramin |
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Oxazolidinones
-MOA |
Bacteriocidal in strep
Bacteriostatic in enterococci/staph |
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Oxazolidinones
-Spectrum |
Narrow spectrum
MRSA or VRE Gram + aerobes |
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Oxazolidinones
-PK |
High BA, PO, IV
t1/2=4-6 hr Dual hepatic metabolism and renal elimination |
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Oxazolidinones
-AEs |
Weak inhibitor of MAO so CONTRA SSRI's
Potential for increased BP w/tyramine containing food and sympathomimetics $$$ Myelosuppression, thrombocytopenia |
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Oxazolidinones
-Restance |
Altered target site
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Linezolid
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Oxazolidinones
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