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85 Cards in this Set
- Front
- Back
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What is drug class of vancomycin
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glycopeptide antibiotic
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Vancomycin is NARROW spectrum BACTERICIDAL antibiotic, with activity ONLY against
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Gram + organism
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Vancomycin has good activty against
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S. Aurues, and S. edpidermidis, both MRSA and MRSE, and other staph and strep, and enterococcu
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Does vancomycin have good activyt against Gram+ ANAEROBES
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yes, including glostridum
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Does Vanco have any activity against Gram- bacteria, and why
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NO, b/c the large molecular weight prevent it from penetrating the outer membrane
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What is the Drug of choice for MRSA and MRSE
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Vancomycin
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MOA of Vancomycin
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inhibits CELL WALL synsthsis by high affinity binding to the cell wall precursos D-alanyl-Dalaine
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Does the MOA of vancomycin involve PBP
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NO--why its effective against MRSA and MRSE
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Vancomycin is bactericidal BUT not as rapid as B-lactam, AKA
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slowly cidal
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What is MAJOR mechanism of resistance of Vacomycin
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change of D-alayl-D-alanine to
D-alanyl D-LACTE |
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Change of D-alanyl-D-alanine to D-alaynl-D-LACTATE, results in
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prevening the binding of vanco, and cell wall systhesis can continue
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Change id D-alaynl-Dlactate is MOST common in
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ENTEROCOCCI
VRE--Vancomycin-RESISTANT enterocci, paricullar VREF--entecococcu faecium |
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What is less common mechanism of resistance of vanco
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plasmid mediated mechanisms
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What is oral absorption of vanco
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POOR--must be aministered IV
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When can oral routes be used for Vancomycin
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to treat Clostrium Difficule, b/c infectio is localized in the colonic mucosa
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Can Vancomycin be adminstered IM, like aminoglycosides
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NO---can cause muscle necorsis
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What is volume of distrubtion of Vancomycin
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Well distruction
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What is elimination of Vacomycin
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70% renally, the remainer unknown
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What is 1/2 of Vancomycin
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4-6 hrs
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What are the 3 MAJOR adverse effect of Vancomycin
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Red man syndrome
Nephrotoxicity Phelbitits |
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What is Red man syndrome or Red neck syndrome (SIGNS)
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prutis, flushing of face, neck and upper extremeties, rash, hypotension and tachcardia
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Red man syndrome occurs 10-20 minutes after start of infusion,and mediated by what
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histamine release
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Is Red man syndrome a TRUE hypersenstiivty
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NO--histmaine relaste
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How can Red Man syndrome be managed
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slowing infusion rate, and pre-adminstering antihistamines
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Nephrotoxicity is NOT as common b/c Vancomycin today has less impurites, however increased risk when
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given with aminoglycoside
>4gram/day |
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Ototoxicity is rare with vacomycin,, is phelbits and pain comon with vanco
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YES
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What drug class Telavancin
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Lipoglycopetide
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Telvancin is also bactericidal activity, which is conc. dept or time dept
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CONC. dependent
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Is Vaco, time dependen or Conc depent
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TIME depdendent
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What is spectrum of activity of Telavancin
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Great against Gram+, including MRSA and VSE (ESPECIALLY VRE)
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How is Televancin administered
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IV
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What is half-life of Telvacin
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7-11 hrs once daily dosing
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What is MOA of Televacin
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Inhibtis Cell wall sysnthesis by interfeing with transglycosides, and transpetidades
2. Distrupts bacteriam membrane fxn |
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How does Televacin distrupt bacterial membrane fxn
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inserting into the membrane and causing depolarization
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What are teh MAIN Adverse effects of Televacin
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Altered taste (nickel)
Foamy urine |
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Has Telvacin been FDA approved
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NOT YET
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Streptogramins antibtiocs consists of what
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TWO types
Type A and Type B Type A Dalfopristin Type B Quinupristin |
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Streptograms are membrane of the MLS which is
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Macrolide-lincosamide and streogramin group--b/c of similar MOA
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Whatis MOA of MLS
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act at robsome to inhibt protein syntheis
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What was the 1st streogramin antiotics in the US
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Synercid (Dalopristin and Quinpristin
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The combinatio of quinpritin and daloprsint is fixed ratio, and SEPARATELY they are
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bacteriostatic, halting protein syntheis
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Togerther combination of quinupristin and dalfopristin, are
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BACTERICIDAL, and act synergistically to inhibit protein synstheiss
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Synericd is NARROW spectum bactericidal antibiotic only activity against
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Gram + organism
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Specturm of activity of Synercid
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S. Aureus(MRSA) and S. epidermidis, and other stapy and streop, and entercoccos including VREF
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MOA of Synercid is Type A or Dalfopristin binds to 50S ribosomal subunits and causes
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conformation change ALLOWS Type B to bind to 50S ribosomal subunit
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What happens after Type B (Quinupristin binds to 50S ribosomal subinit
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inhibits protein synthsis
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What is Major mechanism of resistance of Synercid
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palsmid mediated
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What are the MAJOR adverse effective synercid, and WHY it is NOT used clinically
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PHELBITIS (75%), can be SERVERE--thromophebitis
Arthragia/myagia Elevated heatpic enzyme |
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How is Phelbitis managed
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using a central venous catheter
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Arthalgia/myagia can be SEVERE (3-12%), and often requires
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analgesics (APAP, NSAIDS and opitates)
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Synercid also have many drug interactions becuase it inhibts
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CYP3A4 enzymes
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What is the only reason Synercid may be used
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allergies to B-lactams or resistance
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What drug class is Linezolid
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oxazolidinone
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What is made Linezolid extremely population
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ORALLY absrobed
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Linezolid is NARROW spectrum agenet, is it bactericidal or basteriostatic
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STATIC
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Spectrum of activity of Linzezolid
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Gram + organisms ONLY
Stapy aureas (MRSA), S. epidermidis, and other stapy, and strepoccis, and enterococcos |
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What makes Linezolid better Specturm of activity then Synercid
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activity against BOTH enterococcus E. ffaecalis and E. faecium
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Linezolid inhibits a early step in bacterial protein synthesis by binds to
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BOTH 50S and 30S, and prevents formation of 70S ribosome complex
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Does Linezolid block elogation or termination
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NO
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The unique MOA of Linezolid, seems to prevent cross-resistance with other antibiotics
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YES
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Resistance with Linzelid si unusual, but occurs where
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mutation in Domain V of the 50S ribosomal subunit
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Resistance with Linezolid usually only occus in cases with
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VRE, prolonged courses >21 days, or indivudals with prostetic devies, or abscesses
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What is ORAL bioavailabilty
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100%--similar to IV
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What is effect of food on Linezolid
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slight decrease RATE but NOT exent
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Linzeolid has AWESOME volunte to VD 40-50L, and how is it metabolized
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by livers, and elminted in the urine
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Linezolid is SAFE and well tolerated, with common SE nausea, vomiting, diarrhea, and what less SEs
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Elevated transaminses
Reversible Bone marrow suppresion Taste alteraterions |
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What is a unquire taste alteration or tongue discolroatino with Linezolid
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gun mental color
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Does Linezolid have any effect on CYP450
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NO
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What is the MAJOR drug interaction with Linezolid
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REVERSIBLE monoamine oxidase inhibitor, interaction with SSIR
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What is resulting interaction of SSRIs and Linezolid
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Sterotengic syndrome--weight benfits vs risk
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Can you just stop SSRI before giviing Linezolid
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NO--long half-lifes not an option
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What drug class is Daptomycin
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cyclic lipopeptide
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Daptomycin is NARROW spectum drug only active against
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Gram+ organisms
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Daptomycin is BACTERICIDAL, and time dependent or concentration dept
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Concentration dept
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Spectrum of activity of Daptomycin
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S. aureus, S. epidermidis, MRSA, MRSE, other staph, strepa nd esteroccous, including VRE
Gram + ANEROBES |
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MOA of Daptomycin,
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Binds to Gram+ cell membrane and insert tail with Ca+ help
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Daptomycin is dependent on
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Calcium
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Daptomycin binds to gram+ membrane and insertes tail, it results
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Depolarizes membrane, and efflux of K+ and destory concentration gradient, and cell dealth
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Mechansims of resistance to Daptomycin
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RARE
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How is Daptomycin adminstered
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IV
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What is the volume of distribution of Daptomycin
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ONLY ONE---POOR
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Why is volume of distrubition of Daptomycin poor
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rapidly inactivated by surfacatnat does not get into respiratory ttissue
NO EFFECT on pneumonia |
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What is elimination of Daptomycin
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Renally
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Daptomycin is safe and well toleraction, GI, and CNS, and rash, what is unique
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elevation in CPK
creatine phosphokinases elevation in transaminases |
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Should CPK be moinitor with Daptomycin
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YES==1-2x week, and concerns with statins
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