Antibiotics Flashcards
Mechanism of beta lactams
- Penicillins
- Cephalosporins
- penicillins bind penicillin binding proteins (PBPs)
- PBPs involved in synthesis of peptidoglycan binding –> cell wall synthesis inhibits –> lysis - inhibit cross linking of peptidoglycan chains –> weak cell wall
- facilitate damageby autolysins d/t weakened/absent cell wall - may up regulate
bacteriocidal
Penicillin coverage and toxicity
b-lactam
PCN G - IV form
PCN V - oral form
Gram + cocci: S. pneumo S. pyogenes Actinomyces Grp B strep - neonatally Spriochetes - syphilis
Gram + rods:
Clostridium
listeria
Bacillus
Gram - cocci:
Neisseris - if not penicillinase resistant
MC toxicity:
HSR
Hemolytic anemia
Thrombocytopenia
Resistance mechanisms to penicillin
Penicilinase - type b-lactamase
-produced in periplasm gram - organims
coded by plamids
alteration of b-lactam target - PBP
Penicilinase resistant penicillins
Bulky R group blocks penicillinase (b-lactamase) binding
Methicillin (lab use only)
Nafcillin
Oxacillin
Dicloxacillin
use: Staph aureus
MRSA - altered binding target site
Toxicity:
Methicillin - interstitial nephritis
Rest: HSR
Aminopenicillins
Ampicillin (IV)
Amoxicillin (PO)
Penicillinase (b-lactamase) sensitive Broader spectrum: "HEELPSS" H.flu Ecoli Enterococci Listeria Proteus mirabilis Salmonella Shigella
UTIs - kids
Neonatal infection s- ampicillin IV
Prophylaxis against Viridans strep endocarditis
SE:
HSR
Rash w/ mononucleosis caused pharyngitis
-full body rash
B-lactamase inhibitor
enhance spectrum of drug
used in combination:
Clavulanic acid + amoxicilin - resistant OM
Clavulanic acid + piperacillin
Sulbactam + ampicillin - IV, surgery
Tazobactam + piperacillin
Antipseudomonal abx
Ticarcillin
Carbenicillin
Piperacillin
Extended spectrum
Pseudomonas
gram - rods
susceptible to penicillinase
-add B-lactamase inhibitor
Cephalosporins general
B-lactam mechanism
Bactericidal
Less susceptible to penicillinases
LAME against: Listeria Atypicals - mycoplasma, chlamydia MRSA - except 5th gen Enterococci
Toxicity:
HSR - 5-10% cross reactivity to PCNs
Increased nephrotoxicity if used w/ aminoglycosides
Disulfam like rxn - rare
1st gen cephalosporins
Cefazolin
Cephalexin
Gram + cocci Gram - "PEcK" Proteus mirabilis Ecoli Klebsiella
UTIs - cephalexin for prophylaxis
URIs
Prophylaxis against viridan strep endocarditis
Cefazolin - post op surgical infection - MSSA
2nd gen cephalosporins
Cefoxitin
Cefaclor
Cefuroxime
Cefprozil
Gram + cocci w/ 1st gen Gram - "HENS PEcK" Hflu Enterobacter Neisseria sp. (not urethritis gonorrhea tx) Serratia marcescens
Proteus mirabilis
Ecoli
Klebsiella
3rd gen cephalosporins
Ceftriaxone (IV, IM)
Cefotaxime
Ceftazidine
Cefdinir
Serious Gram - infecitons, resistant to other b-lactams
“HENS PEcK” + Citrobacter
gram - meningitis
gram + S. pneumo only!
Ceftriaxone - longest t 1/2
- Neisseria gonorrhoeae - IM
- excreted in bile, good for renal failure pts
Ceftazidime - pseudomonas
Cefdinir - recurrent OM
4th gen cephalosporins
Cefepime
broad spectrum
-most gram + of 1st and 2nd gen
Gram -
Pseudomonas
5th gen cephalosporins
Ceftaroline
Broad spectrum MRSA No Pseudomonas coverage Community acq pneumonia complicated skin infections (MRSA)
Aztreonam
monocyclic B-lactam
inhibits cell wall synthesis - binds PBP3 “azTHREE-onam”
Synergicstic w/ aminoglycosides - gentamicin
no cross allergenisity w/ PCN
“Aminoglycoside pretender”
Gram - “PEcKS”
no gram + or anaerobe coverage
Can use in PCN allergy, renal insufficiency (no renal involvement)
non toxic
Carbapenems
Imipenem - cilastatin (inhibitor of renal dehydropeptidase 1 –> decreased inactivation)
Meropenem
Ertapenem
Doripenem
Broad spectrum: Gram + cocci gram - rods anaerobes Pseudomonas
B-lactamase resistant
binding PBPs
Empiric tx of life threatening infections - sick!
does NOT cover MRSA
meropenem - decrease risk of seizures, not inactivated in renal tubules
Toxicity:
GI distress
skin rash
some CNS toxicity - imipenem
Vancomycin
inhibit cell wall synthesis
inhibit cell wall mucopeptide formation by binding D-ala-D-ala moieties of cell wall precursors
inhibit cell wall glycopeptide polymerization
Bactericidal
Gram +
poor oral availability - IV for systemic
Use: MRSA Enterococci VRE C. diff - oral - stays in GI Coag - staph epidermidis endocarditis (R-side)
Toxicity: “NOT”
Nephrotoxicity
Ototoxicity
Thrombophlebitis
Vancomycin resistance mechanism
D-ala-D-ala to D-ala-D-lac
Red man syndrome
Vancomycin associated
diffuse flusing of whole body non specific mast cell degranulation avoid w/: -antihistamine pretreatment -slow down infusion -can restart
30 S and 50 S inhibitors
“buy AT 30, CCELL at 50”
30S:
Aminoglycosides
Tetracyclines
50S: Chloramphenicol Clindamycin Erythromycin (macrolides) Lincomycin Linezolid