8/19/2019 Tabel Antibiotik.docx

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Drug Mechanism  of   Action Mechanism  of Resistance

Spectrum  of   Activity Pharmacology Indications  for   Use Toxicity

Trimethoprim-

Sulfamethoxazole

(TMP-SM!

synergistic  drug

com"o

#se$uential

interference  %ith  folicacid  synthesis#Sulfa  is  a  structuralanalog  of   PA&A'

competes  for   enymedihydropteroate

synthetase

#TMP  is  a  competitiveinhi"itor   of dihydropteroic  acid

Sulfa

#decreased permea"ility  (plasmid!#increased  PA&A

 production

TMP#synthesis  of dihydrofolate

reductase  %ithdecreased  affinity  for TMP

#overproduction  of dihydrofolate

reductase

&road  spectrum "actericidal#)ram*

staphylococci+

streptococci+  listeria+

 ,T  enterococci#)ram-

e.  coli+  /le"siella+ proteus+  salmonella+shigella+  vi"rio+neisseria+  h  influenae#misc.

 pneumocystis+

ocardia+  chlamydia

#com"o  anti"iotic  012ratio  of   TMP1Sulfa'serum  ratio  0134#oral  and  parenteral#%ell  distri"uted'  good

levels  in  lungs+/idneys+  "iliary  tree+and  5,S#partially  meta"oliedin  liver+  excreted  inurine

#UTIs

#prostatitis#pneumocystis  cariniiinfection  (AIDS!#diarrheal  illness  due

to  salmonella+  shigella+enterotoxigenic  e.  coli#upper   and  lo%er respiratory  infections#infections  caused  "y

 p.  cepacia+  nocardia

#hypersensitivity  rxns(rash+  fever!+  rareStevens  6ohnsonsyndrome  (mucosaland  cutaneous  illness

seen  in  AIDS  pts!#)I  7   nausea+vomiting+  diarrhea#(rare!  hepatitis+mego"lastic  anemia+increased  serumcreatinine

Mechanism  of   Action Mechanism  of Resistance

Spectrum  of   Activity Pharmacology Indications  for   Use Toxicity

Chloramphenicol   #"inds  peptidyltransferase+  acomponent  of   the  24s

ri"osome

#presence  of   enymechloramphenicoltransacetylase

(acetylates  the  drug!

Mostly  "acteriostaticmay  "e  "acteriocidalagainst  pneumococcus

and  neisseria#"road  spectrumaero"ic  )ram*most  )ram-most  anaero"esric/settsia

#higher   levels  %ithRA8  vs  I9#%ell  distri"uted

throughout  "ody'  5S:levels  ;4-24!  ototoxicity

Mechanism  of   Action Mechanism  of Resistance

Spectrum  of   Activity Pharmacology Indications  for   Use Toxicity

st1  GenerationCephalosporins

5efaolin+

5ephalothin+5ephalexin  (oral!+5efaclor   (oral!

#li/e  penicillins+  inhi"itenymatic  rxns  neededfor   sta"le  "acterial  %a

ll

synthesis  "y  "inding  to

P&Ps

#permea"ility  7   failureof   cephalosporins  toreach  receptor   sites#destroyed  "y  "eta-lactamase

#alteration  of   P&Ps

 "actericidal#)ram*  coccis.  pneumoniae+  s.  aureus+

 ,T  enterococci

#)ram-  rodse.  coli+  /le"siella+  proteusmira"ilis

#hydrophilic  moleculesthat  achieve  excellentdrug  levels  in  lung+/idney+  muscle+  "one+

 placenta+  interstitial+synovial+  and

 peritoneal  fluids+  and  inurine

#eliminated  via  /idney(pro"enecid  "loc/ssecretion  of   somecompounds!

#common  infections#surgical  prophylaxis#s/in  and  soft  tissueinfections

#hypersensitivity  (rash+urticaria+  eosinophilia+fever+  anaphylaxis  7 rare!

#leu/openia  and  rarelyhemolytic  anemia#superinfection  %ithfungi  or   resistant)ram-  organisms#phle"itis+  false*  tests(5oom"s+  glucose!

nd2 

GenerationCephalosporins

5efuroxime

5efoxitin5efotetan

#li/e  penicillins+  inhi"itenymatic  rxns  neededfor   sta"le  "acterial  %allsynthesis  "y  "inding  toP&Ps

#permea"ility  7   failureof   cephalosporins  toreach  receptor   sites#destroyed  "y  "eta-lactamase  (cefuroxime

is  STA&8  to  plasmidmediated  penicillinases!#alteration  of   P&Ps

 "actericidal

#)ram*  coccis.  pneumoniae+  less  s.aureus+  ,T  enterococci#)ram-  rods

e.  coli+  /le"siella+  proteusmira"ilis

#cefuroxime  covers  h.influenae

•cefoxitin  and  cefotetanincreased  anaero"e  coverage+

 "acteroides

#parenteral  drugs#hydrophilic  moleculesthat  achieve  excellentdrug  levels  in  lung+/idney+  muscle+  "one+

 placenta+  interstitial+synovial+  and

 peritoneal  fluids+  and  inurine

#eliminated  via  /idney(pro"enecid  "loc/ssecretion  of   somecompounds!

#upper   respiratorytract infections (h.inuenzae)#)I  tract orainfections

#hypersensitivity  (rash+urticaria+  eosinophilia+fever+  anaphylaxis  7 rare!

#leu/openia  and  rarely

hemolytic  anemia#superinfection  %ithfungi  or   resistant)ram-  organisms#phle"itis+  false*  tests(5oom"s+  glucose!

rd3 

GenerationCephalosporins

cefotaxime

ceftriaxoneceftaidime

#li/e  penicillins+  inhi"itenymatic  rxns  neededfor   sta"le  "acterial  %allsynthesis  "y  "inding  toP&Ps

#permea"ility  7   failureof   cephalosporins  toreach  receptor   sites#STA&8  to  plasmamediated  "eta-

lactamases#alteration  of   P&Ps

 "actericidal

•cefotaxime: highly 

active  against  s.

pneumoniae;  n.

meningitides,  h.

influenzae,  e.  coli,klebsiella,  NOT  p.

aeruginosa

•ceftriaxone1  s.  pneumoniae+

n.  gonorrhea+  ".  "urgdorferi

•ceftaidime1  less  )ram*activity  "ut  can  /ill  p.aeruginosa

#cefotaxime  and

ceftriaxone achievegood CSF levelsceftazidime ade!uateCSF levels

#ceftriaxone  longerhalf"life and moreactive thancefotaxime a single#$ does can %ill for&'"' hrs

#cefotaximeE  drug  of choice  for   meningitis#ceftriaxoneE

outpatient  coverage  of septic  pneumococcal

 pts+  n.  gonorrhea+  and5,S  lyme  disease

#hypersensitivity  (rash+urticaria+  eosinophilia+fever+  anaphylaxis  7 rare!

#leu/openia  and  rarely

hemolytic  anemia#superinfection  %ithfungi  or   resistant)ram-  organisms#phle"itis+  false*  tests(5oom"s+  glucose!

Mechanism  of   Action Mechanism  of Resistance

Spectrum  of   Activity Pharmacology Indications  for   Use Toxicity

Beta-lactamase

inhiitors

Sul"actam

5lavulanic  acidTao"actam

#high  affinity  for  plasmid-mediated  "eta-lactamases

5om"ination1

(penicillin  *  "eta-lactamase  inhi"itor 

!iperacilin  "

Tazoactam

#"inds  P&Ps'  enymesinvolved  in  cell  %all

 "iosynthesis

#"eta-lactamase

inhiitors(tazoactam) higha*nity for plasmidmediated enzymes

#)ram-  can  change porin  channel permea"ility

 preventing  drug  fromreaching  receptor   site#efflux  pumps#alteration  of   P&Ps(esp.  in  )ram*!

 "actericidal  '  "roadspectrum

#)ram*

streptococci+

enterococci+

meningococci+treponema  pallidum(syphilis!+  mostanaero"es

#)ram-

 pseudomonas

aeruginosa+acteroides+  proteus

Carapenems

Imipenem

Meropenem

#"inds  P&P-3#permea"ility  through

 porin  channels

#STA&8  to  "eta-lactamase'  "ut  alternateenymes  that  canhydrolye

•alteration  of   porinchannels

 "actericidal

'  FU)spectrum

%ills most +ram,-+ram"- andanaeroic acteriaincludingpseudomonasaeruginosadoes /0 %ill:$1S2- enterococcus-c. di*cile

#allergic  rxns  similar   to penicillin

#(>!  #mipenem maylo3er seizurethreshold

#onoactams

Atreonam

#only  inds +ram"454s#STA&8  to eta"lactamase

 "actericidal' ,ARRG  spectrum,8H  aero"ic )ram-rods'  including  p.aeruginosa

#can  use  in  place  of   anaminoglycoside#can  use  in  penicillinallergic  pts  (little  cross-reactivity!

Drug Mechanism  of   Action Mechanism  of Resistance

Spectrum  of   Activity Pharmacology Indications  for   Use Toxicity

!enicillin   #"inds  penicillin  "inding proteins  (transpeptidases+car"oxypeptidases!'

enymes  involved  in  cell%all  (peptidoglycan!

 "iosynthesis

#"eta-lactamase

cleaves  "eta-lactamring  and  inactivatesdrug(chromosomal  or 

 plasmid  mediated!#)ram-  can  change

 porin  channel permea"ility

 preventing  drugfrom  reachingreceptor   site#efflux  pumps#alteration  of   P&Ps(esp.  in  )ram*!

 "actericidal

#)ram*

streptococci+

enterococci+meningococci+

treponema  pallidum(syphilis!+  mostanaero"es

#poor   activity  against)ram-  rods

#some  oral  use#minor   meta"olism#excreted  "y/idneys  via  tu"ular secretion

(pro"enecid  %ill "loc/!

#%ell  distri"uted  tolungs+  liver+  /idney+muscle+  "one  and

 placenta

#high  urinary  and "ile  concentrations

#hypersensitivity

(rash'  anaphylaxis!act  as  haptens  tocom"ine  %ith  human

 proteins

maCor   determinantE penicilloyl

(uticaria  and  laterxns!

minor   determinantE "enylpenicilloate

(anaphylaxis  andaccelerated  rxns!

$mpicillin

(aminopenicillins!#"inds  pencillin indingproteins(transpeptidases-

caroxypeptidases)enzymes involved in cell3all iosynthesis#"etter   penetrationthrough outer m of +ram" than penicillin +and etter inding to454s

#"eta-lactamase

cleaves  "eta-lactamring  and  inactivates

drug(chromosomal  or 

 plasmid  mediated!#)ram-  can  change

 porin  channel permea"ility

 preventing  drugfrom  reachingreceptor   site#efflux  pumps#alteration  of   P&Ps(esp.  in  )ram*!

 "actericidal

#)ram*streptococci+  enterococci

(unless  they  express "eta-lactamases!

#)ram-

hemophilus+  e.coli+salmonella+  shigella("ut  many  )ram-  have

 plasmid  mediatedresistance!

#oral  and  I9 #rash  is  common

Semisynthetic

penicillinase-resistant 

penicillins

(,afcillin+  xacillin+Methicillin!

#"inds  penicillin  "inding

 proteins  (transpeptidases+car"oxypeptidases!'enymes  involved  in  cell%all  (peptidoglycan!

 "iosynthesis

#"ul/y side chains inhi"it

action of staph "eta-lactamases

#"ul/   prevents  them

from  gettingthrough  )ram- porins

 "actericidal

#used primarily forstaphylococci

#)ram*

pneumococci-streptococci-/0 enterococci

#Methicillin  7   least

 protein  "ound  of   thegroup#,afcillin  7   high

 "iliary  excretion#Isoxaolyl

 penicillins

(parenteral  and  I9orms!

#serious

staphylococcusaureus infections(cellulites-endocarditis- sepsis)