ANTIBACTERIAL DRUGS HY Flashcards
MECH OF ACTION OF ANTIBACTERIAL DRUGS
1)Inhibition of bacterial cell-wall
synthesis
2)Inhibition of bacterial protein
synthesis
3) Inhibition of nucleic synthesis
4) Inhibition of folic acid synthesis
bacterial cell wall synthesis inhibitor include
mnemonic = AIM
Penicillin cephalosporin Imipenem, Meropenem Aztreonam Vancomycin
Beta lactam drugs inc
Penicillins, cephalosporins,
imipenem/meropenem, aztreonam
except vancomycin
MOA of B Lactam drugs
Bacterial cell wall is cross-linked polymer of polysaccharides and pentapeptides
Penicillins interact with cytoplasmic membrane-binding proteins
(PBPs)
to ……inhibit transpeptidation reactions involved in cross-linking,
the final steps in cell-wall synthesis
Mechanisms of resistance
1)Penicillinases (beta-lactamases) break lactam ring structure (e.g.,staphylococci)
2)Structural change in PBPs (e.g., methicillin-resistantStaphylococcus
aureus [MRSA], penicillin-resistant pneumococci)
3)Change in porin structure (e.g., Pseudomonas)
Generations of Penecillin
1)Narrow spectrum s
Penicillin G
Penicillin V
2)very Narrow spectrum R
Nafcillin
Oxacillin
3)Broad spectrums
Ampicillin
Amoxicillin
4)Extended spectrums
Piperacillin
Ticarcillin
SPECTRUM OF 1ST GEN
Streptococcal and
meningococcal infections
• syphilis
SPECTRUM OF 2nd gen
Staph infections not MRSA
Broad spectrums Ampicillin Amoxicillin Extended spectrums Piperacillin Ticarcillin spectrum
greater activity vs gram negative bacteria
pharmacokinetics of Penicllin
Renal elemination , hence dose modification required in renal dys
biliary elimination of nafcillin and oxacillin
Adverse effects of
have S hence Hypersensitivity (1-4) 7perc ,
utricial rash or anaphylaxis
Complete cross allergenecity between indivisual penecillin
Gi distress ,
Jarisch-Herxheimer reaction in treatment of syphilis
Q)Give cephalosporin classfication with examples of each group
Cephalosporins
First generation
Cephalexin
Cefazolin
2nd generation
Cefuroxime
Third generation
Ceftriaxone
Cefixime
Forth generation
Cefepime
which second generation cephalosporin enter CNS
cefurixime
pharmacokinetics
Renal elimination
hence dose modification is required in patients with renal dys
CEFTRIAXONE eliminated via liver
1st generation cephalosporin uses and spectrum
strong gram possitve coverage and some gram negative(kleibsela , proteus)
third generation cepohalosporin uses
Emperic management of sepsis and meningitis
pneumonia and gonorrhea
ADVERSE EFFECT OF CEPHALOSPORINS
Side effects:
Hypersensitivity:Incidence: 2%
Wide range, but rashes and drug fever most common
Positive Coombs test, but rarely hemolysis
Assume complete cross-allergenicity between cephalosporins
partial cross-allergenicity with penicillins (about 5%
COOMBES TEST IS POSSTIVE in….
Cephalosporin
carbapenem names …
Imipenem with cilastatin ,meropene m
why is imipenem given with cilastatin
cilastatin is a renal DEHYDROPEPTIDASE INHIBITOR
hence it inhibits renal metabolism of imipenem to a nephrotoxic metabolite
give spectrum ofcarbapenems and pharmakokinetic
Broad spectrum includes Gram-positive cocci
PRSP strains (not MRSA),
gram-negative rods
are B lactamase resistant
Both drugs undergo renal elimination— ↓ dose in renal dysfunction
Adverse Effect of carbapenem
l Side effects:
− GI distress
− Drug fever (partial cross-allergenicity with penicillins)
− CNS effects, including seizures with imipenem in overdose or renal
dysfunction
Partial Cross allergenicity with …
penecillin
Aztreonam are b lactamse resistant or sensitive
resistant