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Vancomycin, Tetracyclines, Macrolides, Clindamycin, Fluoroqu
Everything else... except fungals
119
Pharmacology
Graduate
08/22/2010

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Term
Vancomycin coverage
Definition
gram(+) bugs including anaerobes
no gram (-) activity
Term
DOC for MRSA infections
Definition
vancomycin
Term
Used for Ampicillin R enterococci
Definition
vancomycin, however now 50% are R to vanc
Term
Used for Penicillin R strep pneumo
Definition
Can use vanc, but a fluoroquinolone such as moxi or levo will work as long as it's not meningitis
Term
P.O dosing of vancomycin
Definition
used for resistance strains of C. dificile in pseudomembranous colitis, however, Vanc is generally NOT absorbed through the GI tract. I.V. only for systemic infections
Term
T/F Vanc penetrates CSF
Definition
False, it is a very large molecule
Term
Elimination of Vanc
Definition
Renal, so monitor renal fxn.
Term
Vanc side effects, give 4
Definition
Ototoxicity
Renal toxicity
Red- man syndrome
allergic rxns and rash
Term
Is Red man syndrome an allergic rxn?
Definition
NO, too quick a vanc injection gives a histamine reaction, so infuse it slowly
Term
Treatement of MDR strep pneumo infections
Definition
Van or moxi or levo
Term
treatment of Hospital infections caused by MRSA
Definition
vanc for 14 days i.v.
Term
Treatment of ampicillin R enterococcal infections e.g. E. faecium
Definition
Vanc
Term
Empiric therapy for bacterial meningitis
Definition
treat with ceftriaxone + vanc: vanc added to cover PCN Resistance
add i.v. ampicillin to cover Listeria if < 2 years old
Term
Empiric therapy for febrile neutropenia
Definition
a. pip/tazo or cefepime
add van when there is evidence of gram + infection or awaiting culture results
Term
Empiric therapy for Gram + bacteremia
Definition
Use Vanc until you know what bug is causing the infection
Term
#1 bug cultured from blood samples
Definition
coag negative staph and 90% it is S. epid due to contamination
Term
DOC for C. difficile intections
Definition
metronidazole,
give 2 courses of po metro, if patient still has infection or inf is life threatening, treat with po. vanc
Term
Most freq used tetracyclines
Definition
tetracycline HCL, doxycycline, and minocycline
Term
Tetracycline MOA
Definition
inhibit protein synth by binding 30s A site blocking tRNA
Term
T/F, tetracyclines are bacterocidal
Definition
False, static only
Term
Spectrum of tetracyclines
Definition
65% of staph aureus are susceptible
covers strep, but no GBS, so doxycycline will not cover SSTIs caused by GBS
Term
Used in combination with amoxicillin or cephalexin to treat serious SSTIs.
Definition
Tetracyclines; amox or cephalexin are added to cover GBS and beta-hemolytic strep
Term
T/F tetracyclines have poor gram(-) activity
Definition
TRUE
Term
Excellent activity against intracellular pathogens such as Mycoplasma, Chlamydia, and Rickettsia
Definition
Tetracyclines
Term
Good for atypical CAP
Definition
Tetracyclines
Term
Used for the treatment of Lyme disease, Borrelia burgdorferi and B. recurrentis
Definition
Tetracyclines
Term
Active against Yersinia pestic, Enamoeba histolytica and Plasmodium falciparum (malaria)
Definition
Tetracyclins, doxy, mino
Term
Bacterial R mech for Tetracyclines
Definition
mutation which protects the drug binding site and/or and efflux pump. Doxy may still work. Tige overcomes both mech of Resistance
Term
Preparations of Tetracyclines available
Definition
all i.v. and p.o. except tigecylcine which is i.v. only
Term
Contraindications for P.O. tetracycline
Definition
p.o. with milk, multivitamins, Ca, Mg, Al, or Fe will chelate preventing drug abs.
Term
oral bioavailability of doxycycline and minocycline
Definition
100%
Term
dosage of doxycycline and minocycline
Definition
long half-lives and slow elimination so 2x daily
Term
Liver and tetracyclines
Definition
highly conc in the bile so check LFT's,
minocycline is partially metabolized by the liver
Term
DOC for patients with renal dysfunction
Definition
Doxycycline b/c it is elim by fecal excretion
Term
Toxicity of Tetracyclines
Definition
GI, esp with tige
tooth discoloration
photosensitization
hepatotoxic in large doses
superinfections
Term
Contraindications for tetracycline use
Definition
pregnant femails and children under 15 due to bone deformity due to Ca binding
Term
Superinfection side effects of Tetracyclines
Definition
over growth of Clostridium difficile, staph, Candida leading to:
disturbed GI fxn
oral, anal, vaginal candidiasis
C. dif pseudm colitis - treat with metro
Term
Treatment of CAP
Definition
Doxycycline
Term
Impoprtant organisms in CAP Typical:
Definition
extracellular
trep pneumo
H. influ
Morax catarrhalis
Term
Important organisms in CAP atypical:
Definition
M. pneumo
Chlamydia spp.
Legionella spp.
Term
DOC for rickettsial infections
Definition
tetracyclines
Term
DOC for CAP
Definition
doxycycline
tetracyclines cover all of the typical and atypical bugs causing CAP
Term
tetracycline MRSA coverage
Definition
doxycycline and minocycline cover 95% for community acquired MRSA strains
Term
Treatement of acne
Definition
Tetracyclines esp. minocycline
Term
Therapeutic use of Tigecycline
Definition
given i.v. for infections caused by MDR Acinetobacter spp, MRSA, and Stenotrophomonas maltophilia. Very low serum levels due to tolerability issues at higher doses. Avoid in bacteremic patients
Term
Macrolides, what are the drugs
Definition
erythromycin i.v. hurts, p.o. severe n/v
clarithromycin p.o only
azithromycin i.v. and p.o.
Term
Macrolide MOA
Definition
inhibition of protein synthesis
binds to 50s subunit at the peptidyltransferase site inh transloc.
elongation stops and prot synth is terminated
Term
T/F Macrolides are bacteriocidal
Definition
FALSE
Term
Macrolide spectrum of activity
Definition
Moderate gram (+) activity includ S. pneumo
only 7% of Staph aur isolates are susceptible to macrolides at UHS
Term
Are Macrolides active against MRSA, VRE of enterococcus
Definition
NO
Term
Macrolides with improved Gram (-) activity
Definition
clarithromycin and azithromycin
Term
Mechanism of Macrolide resistance
Definition
"ribosomal protection" drug binding site has been modified by a bacterial methylase
also have drug efflux pumps
Term
What is the p.o. bioavail of erythromycin?
Definition
acid labile which limits po bioavailability
Erthromycin esters are less acid labile and have better bioavailability
Term
Absorption of clarithromycin an azithromycin
Definition
GOOD and well absorbed bioavail = 0.5
Term
Erythromycin and azithromycin excretion
Definition
bile only
Term
Clarithromycin excretion
Definition
metabolized by the liver and the metabolites are excreted in the urine
Term
DOC's for atypical pathogens in CAP? Give order of preference, and rational
Definition
azi > clari = erythro
high intracellular concentrations and penetration of most tissues except brain and CSF
Term
Best Macrolide to the treatment of CAP
Definition
Clarithromycin b/c it yields good intracellular and extracellular drug concentrations
Term
Macrolide side effects
Definition
motility GI upset and cramping, clarithromycin metallic tast, and azithromy 2g will make you throw up
Term
Macrolide drug interactions? Give order of interference
Definition
All inhibit CYP450 and prevent hepatic metabolism of many other drugs. Eryth is worst, clarith is better, and azith has the least CYP450 interactions
Term
DOC for treatment of outpatient CAP
Definition
clarithromycin b/c clari produces high intracellular to cover atypical bugs and sufficient extracellular concentrations to cover the typical bugs
Term
Typical CAPS
Definition
S. pneumo
H flu
M. cat
Term
Atypical CAPs
Definition
intracellular
M. pneumo
Chlamydia
Legionella
Term
Gold standard for treat ment of legionella infections
Definition
any macrolide, but alos levo and moxifloxacin
Term
Treatment of Myco avium, Chlamydia, Mycoplasma, though not Myco tb.
Definition
Macrolides, erythromycin, clarithromycin, or azithromycine
Term
Treatment of acne
Definition
erythromycin pads
Term
Macrolides for treatment of pediatric otitis media
Definition
NO
Term
Telithromycin
Definition
a 1st gen ketolide/ 3rd gen macrolide with a black box warning
Term
Clindamysing MOA
Definition
Binds to the 50S subunit at the peptidytransferase site, which, inhibits translocation - stops protein synth
Term
T/F clindamycin is Bactericidal
Definition
FALSE
Term
Clindamycin Spectrum of activity
Definition
good for Gram + inhibits toxin production
SSTIs caused by S. aureus and B-hemolytic strep
Term
Can you use clindamycin for someone with a PCN allergy
Definition
YES
Term
T/F Clindamycin has good gram - activity and covers VRE
Definition
FALSE
Term
Used to treat aspiration pneumonia
Definition
Clindamycin b/c it has good Gram + anaerobe coverage
Term
You can use Clindamycin for GI surgery?
Definition
NO, decreasing susceptibility of gram (-) anaerobes
Term
Can clindamycin be given P.O.?
Definition
YES good p.o. bioavailability
Term
Clindamycin penetrates most body fluids and tissues except ?
Definition
CSF and brain
Term
Metabolism of Clindamycin
Definition
Hepatic/bile
Term
Toxicity of clindamycin
Definition
Rash, diarrhea due to bowel flora change
AND C. dif is historically linked to clindamycin
Term
Treat pseudomembranous colitis with?
Definition
Metro then Vanc
Term
DOC for aspiration pneumonia
Definition
Clindamycin b/c good for Gram (+) anaerobic
Term
Other Therapeutic uses of Clindamycin which are similar to the rest of the macrolides
Definition
SSTIs, PCN allergic patients, acne, community acquired MRSA.
Term
Treatment of Osteomyelitis
Definition
Clindamycin
Term
Treatment of infection in patients with diabetes mellitus
Definition
Clindamycin
Term
What is a fluoroquinalone? and name the major ones
Definition
it is a fluorinated derivative of nalidixic acide (toxic, lab only)
levofloxacin
moxifloxacin
ciprofloxacin
Term
Fluoroquinolone MOA
Definition
Inhibit DNA synthesis by inhibitin Topo II and IV
Topo II allows normal gene transcr and DNA repl
Topo IV req for the sep of replicated DNA
Term
Are FQ cidal or static?
Definition
rapidly bactericidal = concentration dependent killing
Term
General FQ spectrum of activity
Definition
Good against Gram (-) but limited effectiventss against gram (+)
Term
Gram (+) relative FQ activity
Definition
moxi = gemi > levo > cipro
Term
Relative Antipseudomonal activity of FQs
Definition
levo = cipro >> moxi = gemi
Term
Relative gram (-) activity of FQs
Definition
relatively equal
Term
Anaerobic activity of FQ's
Definition
moxi > levo = cipro
do NOT use FQ's for anaerobi infections:
use pip-tazo or combine FQ with metronidazole
Term
Are FQ's good for intracellular paths
Definition
YES, e.g. atyp paths causing CAP which are?

Mycoplasm
Legionells
Chlamydia
Term
Can you use FQ's for MRSA
Definition
NO, 50% R in S.A.
Usuall y not active against MRSA
Term
What do you use to treat MRSA?
Definition
P.o. clindamycin, trim-sulfa, or doxycycline;
i.v. vanc for serious MRSA.
inpatient SSTIs use Doxy + i.i. cefazolin. dox covers MRSA and cefazolin covers GBS
Term
DOC for MDR Strep pneumo.
Definition
FQ, use levo, moxi, and gemi
Term
Can you use cipro for S. pneum inf. ?
Definition
NO remember:
g+ activity moxi = gemi > levo> cipro
Term
Where do FQ resistant Strep pneumo infections originate:
Definition
Nursing Homes, so do not use FQ's
Treat them with???

pip-tazo or cefepime, or even add a aminoglycoside like gentamicin ... or an antipseudomonal FQ
Term
What are the anti-pseudomonal FQ's?
Definition
levo mostly as 50% are cipro R
Term
DOC for outpatient treatment of CAP
Definition
Macrolides
Term
DOC for inpatient treatment of CAP
Definition
FQ's
Term
why do you use these different drugs for in and out patient CAP, FQ and macrolides respectively?
Definition
CDC guidelines discourage the use of FQ' to treat outpatient CAP b/c it will lead to increased resistance of Strep pneumo to the FQ's
Term
Are FQ's effective against Enterococcus or VRE?
Definition
NO,
Term
What are the anti-pseudomonal FQ drugs? Are they best for pseudomonal infection treatment?
Definition
Cipro and levo can be used but they are no longer reliable.
Use an antipseudomonal B lactam like Pip-tazo
Term
What UTI's are FQ's effective treatment for?
Definition
Mostly outpatient E.coli UTIs. Res is becoming a problem in hospitals. Use Nitrofurantoin.
Term
Drug effective against 75% of E. coli strains at UH
Definition
Ciprofloxin
Term
General administration and absorption of FQs?
Definition
F = 0.9 so p.o. == i.v.
Oral FE, Ca, Al and Mg supp and antacids chelate FQ decreasing GI absorption
Term
Dairy and antacids affect which FQ?
Definition
Cipro bioavailability is decreased
Term
Dairy does not affect which FQ's?
Definition
levofloxacin and gemifloxacin
Term
Can you treat UTI's with moxi? Why? Why not? What else is there?
Definition
can't use moxi as only a small amount of it ends up in the urine, mostly hepatic metabolism
Use levo or cipro as they are eliminated renally
Term
Major toxicity of FQ's
Definition
Damage growing cartilage - no kids
Tendon rupture
Phototoxicity - cirpo
Q-T prolongation - amplifideed with sotalol or amiodarone, CONTRAindicated
Term
1st line drugs for inpatient treatment of CAP
Definition
ceftriaxone + a macrolide like clarithromycin
Term
Can you use FQ for nursing home patients with CAP
Definition
NO
Term
Explain the difference between complicated and uncomplicated UTIs and what drug you'd use to treat?
Definition
FQ's are 1st line for complicated UTIs
Uncompl is infection in a structurally and neurologically normal urinary tract
Complicated - cath, neph abnormal, hospit patients, upper UTI,
again no FQ's for nursing home patients
Term
What systemic infection can you use FQ's to treat?
Definition
Salmonella spp.
Term
DOC for MDR S. pneumo (not meningitis)?
Definition
levo or moxi as they have enhanced Gram (+) activity
Term
Can you use cipro for MDR S. pneumo?
Definition
NO
Term
Other FQ therapies
Definition
Diarrhea from salmonella, shigella, campy, and E. coli
Term
Can you use FQ's for SSTI's
Definition
NO, 50% of all MRSA are FQ Resist
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