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143 Cards in this Set
- Front
- Back
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PG wall is part of what and not part of what?
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part of gram + and gram -
NOT party of atypicals |
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what class of drugs will not work against atypicals?
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B-lactam drugs and vancomycin
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summarize first stage of cell wall synthesis
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NAG->NAM-> adds L-ala, D-glut, and L-lys = UDP-NAM tripeptide
D-ala racemase converts L-ala to D-ala then D-ala D-ala is added to give UDP-NAM pentapeptide |
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D-ala racemase is found only in what kind of cells?
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prokaryotes +eukaryotes(man)
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Whati s the "intermed block" that is the final product of stage 1?
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UDP-N-acetylmuramylpentapeptide
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cyclic analog of D-ala?
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D-cycloserine
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D-cycloserine inhibits?
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final product of first stage synth. -UDP NAM pentapeptide
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how does D-cycloserine work?
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suicide substrate-irreversibly binds D-ala racemase-preventing D-ala formation
COMP(REVERS.) inhibits-D-ala, D-ala synthetase ALSO INHIB. racemase of HOST-potentially TOXIC!! |
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Fosfomycin inhibits ?
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cytoplasmic enzyme enolpyruvate transferase
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fosfomycin use?
specialy good for? |
for uncomplicated UTI's
safe in preggers |
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Resistance to fosfomycin
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resist. is due to inadequate transp into cell
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summary of 2nd stage of synth
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NAM pentapeptide(1ST) + NAG
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once the NAG-NAM is formed in 2nd stage what happens?
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5 glycines are added to the L-lys
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chemical name for a "brick"
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NAG-NAM-pentapeptide-5gly
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how does Vanco work?
What stage? |
recognizes the D-ala D-ala and binds to this, prevents the elongation of the cell wall
stage 2 |
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how do bugs become resistant to Vanco?
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mutate the D-ala D-ala to D-ala D-lactic acid
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bacitracin info
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Gram posiive only
topically only-nephrotoxic oraly bind the phospholipid transp. to prevent recycling cell still makes UDP-NAMpentapetide INSIDE cytoplasm |
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Vanco DOC for?
cidal or static? |
MRSA
MRSE cidal |
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Vanco S.E.
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R.O.N.
redman synd. Ototoxicity(may be irrevers.) Nephrotoxic(reversible) |
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polymyxins gen info
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"detergents"-disrupt cell memb. gram neg. ONLY
No effect on cell wall synth. |
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Polymyxin used for?
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systemic uses
KAP Klebsiella (ESBL) Ancinetobacter Pseudomonas aeruginosa |
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Natural Penicillins excellent against?
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gram positive, including anaerobes
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DOC for gram positive cocci?
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Natural penicillins
except C. Diff |
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DOC for gram positive rods?
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Natural penicillin (Pen G +V)
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DOC for nisseria meningitis?
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Natural Penicillin
used to be Nissiera gonorrhea but its resistant now....Other DOC is Ceftriaxone |
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DOC of syphillis
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Natural Penicillins
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Pen G info
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acid labile
erratic absorption so IV, IM shortest T1/2 of any penicillin Not effect. against gram neg. bacilli |
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Third stage of cell wall synthesis
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crosslinking, accomplished by TRANSPEPTIDASE enzyme
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B-lactam drugs look like?
gen mech? |
look like D-ala D-ala
bind to the transpeptidase enzyme and ultimately form covalent bondand cell autolyses |
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Pen V info
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acid stable
ORAL, and IM |
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procain penicillin AKA
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IM Pen G
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Benzathine penicillin AKA
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IM Pen G with ammonium base to last UP TO 30 DAYS!
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Benzathine Pen G DOC for?
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not so much Gonorrhea but syphillis
propyxlaxis of Strp. pyrogenes(rheumatic fever) |
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DOC for stap aureus?
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Penicillinase Resistant Penicillins
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B-lactamase resistanct penicillins are gen used to tx ONLY...
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staphylococcal species that produce penicillinase
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what are the B-lactamase resistant drugs?
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CONDOM
Cloxacillin Oxacillin Naficillin Dicloxacillin Methicillin |
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CONDOM drugs
DOC for oral? DOC for IV? DOC for renal failure |
Oral-Dicloxacillin
IV-Oxacillin RF-naficillin(mainly bile) but no red. in dose is needed for renal pts with other CONDOM drugs |
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why can most CONDOM drugs be give to renal insuff. pts
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cause they are mostly protein bound...so eliminated in bile
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gen info about methicillin
S.E. of methicillin..why its no longer used... |
first penicillinase resitant penicillin, IV(not stomach acid stable)
S.E.-internal nephritis |
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which CONDOM drug is oral DOC?
IV DOC? |
O-Dicloxacillin
IV-Oxacillin |
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naficillin S.E.
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neutropenia and reversible bone marrow suppression
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Does nafcillin show significant increase in half life for pts with reduced renal function?
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NO....you would think yes, but the CONDOM drugs are excreted also by billary
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what do aminopenicillins cover?
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still gram positive like nat. penicillins....but also gram negative bacilli (rods)
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all pencillins contain what?
aminopenicillins contain these plus? |
B-lactam
at LEASE 1 ioniazble carboxyl group NH2->zwitterionic |
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aminopenicillin cover which gram negs?
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SS HEMP+B
-shigella -salmonella -H. flu -Ecoli -M. cat -Proteus mirabilis B. frag(must be comboed with b-lactamse inhib) |
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DOC for ampicillin resist. enterococcus
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vanco +/- aminoglycides
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ampicillin
preferable route of admin? S.E. |
IV choice
can cause *PSUEDOMEMBRANOUS COLITIS* wipes out gut flora(diarrhea)-cause superinfection |
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ampicillin is DOC for ?(3)
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Proteus Mirabilis
Enterococcus *Listeria* |
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Anti-Pseudomonal Penicillins tx?
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serious, nosicromial gram neg. infections (aeruginosa)
Proteus species + B.frag |
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carbenicillin indanyl sodium
route? class? |
Oral
Anti-psuedomonal penicillin |
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name drugs in anti-psuedomonal penicillins?
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M.P.CAT
mezlocillin Piperacillin(most potent) Carbenicillin Azlocillin Ticarcillin |
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which of the M.P.CAT drugs are more hydrophillic?
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M.A.P-contain a urea group
mezo azo pipe |
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DOC for non-meningital pseudomonas
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pipercillin/tazobactam(zosyn)
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which 2 anti-psuedomonal can cause hypoK
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TC(two carboxy)
Ticarcillin Carbenicillin watch in renal + CHF |
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T or F
B-lactamase inhibitors exhibit no anti-bacterial activity of their own |
True
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are B-lacatmase inhib revers or irrevers?
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irreversible (suicide inhibitors)
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combo B-lactamase inhib for IV?
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clavulanic acid/ticarcillin-IV
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What are the B-lactamse inhibitors not good against?
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B-lactamases in enterobacteriacae, AMP-C beta lactamases, and metalo-B lactamases
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sulbactam is comboed with?
tazobactam is comboed with? |
ampicillin-IV use
piperacillin |
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what does probenacid do when taken with a penicillin
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-prevents the secretion of drug-increasing serum levels
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Pencillin allergic rxn's
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formation of hapten->antibody formation
macropapular rash->steven johnson syndrome anaphalytic shock if allergic to 1-allergic to ALL |
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Gen S.E. of penicillins
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prolonged bleeding(Ticarcillin + carbenicillin)
Seizures(Pen G)-block GABA |
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ampicillin is better than amoxicillin in txing?
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shigella and salmonella but is not DOC
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where are B-lactamases in gram +?
gram -? |
+-secreted outside cell into surrounding media
- conc. in periplasmic spaces btwn envelope and cytoplasmic memb. |
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mech of resistance to Pencillins
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-make B-lactamases
-mutate the PBP to not recognize penicillins -alter the transport porin(mainly gram neg) |
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Pencillins distribute well exceptions are?
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eye, brain(CSF), prostate, bones/joints
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if the bug is methacillin resistant, will a pencillin or a CONDOM drug work?
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NEITHER
ALL B-LACTAMase resistant drugs/B lactam drugs are ineffective against MR bugs |
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ampicillin may cause rashes espically in pts with COEXISTING...
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CMV or Epstein-Barr Virus
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name drugs of 1st gen Cephs?
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cephalexin
cefadroxil cefazolin |
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T or F
Cephs have a B-lactam ring and are not B-lactamase resistant |
False
-do have B-lactam ring AND are stable to gram + B-lactamase |
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DOC for surgical prophylaxis
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cefazolin
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1st gen ceph coverage
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Gram +'s and PEc
Proteus mirabilis(not indole) Ecoli |
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oral 1st gen cephs?
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DR, ALEX DRAIN'S
cephalexin cefadroxil cephradine |
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RANK of stability to B-lactamases for the cephs?
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4th>cephamycins(2nd gen)>3rd gen>2nd gen> 1st gen
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2nd gen ceph drugs?
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cefaclor
cefpodoxime cefuroxime cefprozil cefoxitin(cephmycin) cefotetan(cephamycin) |
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coverage of 2nd gen cephs?
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UPPER respiratory
PEc + HEN H. flu EnteroBACTER(NOT enterococcus) Neisseria 2nd +3rd gen not reliable against enterobacter cuz AMPC |
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cephamycin drugs
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METAL TAN FOX
cefmetazole, cefotetan, cefoxitin cover anerobes(B.frag) but not DOC b-lactamse resist. |
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3rd gen cephalosporins
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cefotaxime, ceftazidime, ceftriaxone, cefoperazone
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DOC for psuedomonas aeruginosa
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ceftazidine
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gold standard for gram - enterbact.
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3rd generation cephalosporins
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ceftriaxone and ceftaxime are most active cephs against?
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Strept pneumoniae
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cephalosporin that has 80% biliary excretion
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cefoperazone
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DOC for psuedomonal meninginitis
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ceftazidime
cefepime can also be used |
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4 oral 3rd gen cephalosporins
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ce-fixi'me
cef-dinir cef-dito-ren cefti-but-en |
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S.E. of cef-tri-axone
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causes biliary sludging
pronikerous |
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DOC for non-meningital pseduomonas areuginosa
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piperacillin/tazobactam or ticarcillin/clavulanic acid and aminoglycide
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cephs that cross the BBB
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cef-tri-axone
cef-taz-idime cefo-taxi-me ce-fur-ox-ime cefepime |
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3rd gen that have some anerobe coverage
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cefotaxime
ceftizoxime cefrtiaxone |
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cephs resistent to common B-lactamases
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cephamycins
3rd gen 4th gen |
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cephs resistant to staph b-lactamases
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ALL cephs
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ESBL resistant cephs
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carbapenems
cephamycins b-lactamase inhibitors |
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AMP-C resistant cephs
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4th gen more resistant, but carabapenems are better
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2 cephs that dont require renal dosage adjustment
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cefoperazone
ceftriaxone |
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longest half life of cephs
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ceftriaxone
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drugs with MTT side chain?
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MET TAN MAN in endZONE
cefMETazole cefoteTAN cefmandole cefoperazone |
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cefepime coverage
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4th gen
covers gram positives and negatives -most B-lactamase resist ceph |
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DOC for tx of neonatal meningitis by H. flu
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ceftriaxone or cefotaxime
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longest elimination half life of cephs
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ceftriaxone
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cefepime is stable against?
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Amp-C groups- Citrobacter, Enterobacter, Serratia
but DOC is still carbapenems for above |
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ESBLs can easily hydrolize what?
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mostly 3rd gen...the oxyimino containing drugs
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imipenem coverage?
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basically all gram pos and gram neg
-plus anerobes |
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imipenem is a DOC for?
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CAKES
Citrobacter acintobacter Klebsilla Enterobacter Serratia -do cover Enterococcus faecalis but not faceium |
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cilistatin MOA
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specific inhibitor of the brush border DEHYDROPEPTIDASE enzymes
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enzyme that inactivates imipenem
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renal dehydropeptidases
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T or F
imipenem is B-lactamase unstable |
F
it is STABLE |
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which carbapenem has the higher rsk of seizures?
lower? |
higher-imipenem
lower- meropenem |
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are carbapenems IV or oral?
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ALL are IV
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Meropenem coverage
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like imipenem but great against gram negative aerobes and less gram positive
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meropenem combo?
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none-it is stable to the dehydropeptidases-so not comboed with cilastatin
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Ertapenem doesnt cover?
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took APE out
acinetobacter pseudomonas enterococcus |
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monobactam drug?
coverage? |
aztreonam
only gram - aerobes, NO anerobes serious gram neg. in lung, bone, UTI or blood |
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aztreonam stability?
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very stable to B-lactamases
exception is ESBL-hydrolize drug because drug has oxyimino group |
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least cross allergic to B-lactam
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aztreonam
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DOC for enterococcus
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ampicillin or Pen G(V)
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monobactam that crosses the BBB
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aztreonam
alt for 3rd or 4th gen ceph for menigitis of gram neg bacilli |
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which carbapenem should be used in children?
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meropenem cause less seizures than imipenem
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DOC for nocardia?
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bactrim
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are sulfonamides bateriostatic or bacterocidal?
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S-for static
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sulfasalazine
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converted to asaparin in colon-tx's collitis
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tx for chlamydia trachomatis
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sulfacetamide
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prontosil
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prodrug
activated only in vivo |
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DOC for leprosy
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dapsone
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2-3rd line tx of TB
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PAS para-aminosalicyclic acid-like PABA-inhibits dihydropteroate synth
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S.E. of sulfonamides
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HARK
hemolytic anemia-in g6p dehydrogenase deficent pts allergy rash-->Steven johnson synd kernicterus |
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how to avoid crystalluria with sulfs
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give 3 sulfs at 1/2normal dose-prevents supersaturating the urine
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S.E. of the TMZ portion of bactrim
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leukopenia
granuloctopenia megaloblastic anemia thrombocytopenia |
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TMP reduces DHFR....why doesnt it dec humans?
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50,000 x more selective for bacterial DHFR
high doses it loses this selectivity |
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antidote to high TMP
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follinic acid-bacteria can't absorb but humans can...(exception**Enterococcus*)
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spectrum of sulfonamides?
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gram positive
negative aerobes atypical bacteria, some protozoa poor anerobe coverage |
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where are sulfonamides main area of penetration?
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EVERY WHERE!!!
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main use of SMZ/TMP
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UTI
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Sulfonamides DOC
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NO B.U.T C.L.a.P.S
NOcardia burns UTI(complicated and non) toxoplasma gondii clamydia trachoma leprosy pneumocytosis jerovecii stenotrop. maltophilla |
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is sulfonamide an acid or a base?
pKa? |
acid
10.4 |
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first sign in hematouria in sulfs
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crystalizing out in urine
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modern sulfonamides pka is?
how? |
5 to 6
removed 1 H and added an R group |
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how to prevent crystalizing out
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1/2 dose of 3 of drugs
force fluids or basify the urine |
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what does pyromethoprim inhibit
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the protoza form of DHFA
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do sulfonamides have a B-lactam ring?
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NOPE
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TMP like MTX does what?
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prevents DHFA to THFA by inhibiting the enzyme DHFR
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resistance mech for sulfonamides
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bacteria overproduces PABA to outcompete the drug
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dont use what with sulfonamides?
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methianmine
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DOC for proteus
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amoxicillin
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DOC for listeria and enterococcus
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ampicillin
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