Antimicrobials Flashcards
How to administer Penicillin G?
IV and IM
How to administer Penicillin V?
oral
MoA of Penicillin G, V
Bind penicillin-binding proteins (transpeptidase)
Block transpeptidase cross-linking of peptidoglycan
Activate autolytic enzymes
Toxiticty of Penicillin G & V
Hypersensitivity rxn, hemolytic anemia
Ampicillin and Amoxicillin used to treat:
H. influenzae, E. coli, Listeria monocytogenes, Proteus mirabilis, Salmonella, Shigella, entercocci
Ampicillin and Amoxicillin Toxicity
Hypersensitivity rxn, Rash, Pseudomembranous colitis
Penicillinase-resistant penicillins
Oxacillin, Nafcillin, Dicloxacillin - because bulky R group blocks access of beta-lactamase to beta-lactam ring
How to treat S. aureus but not MRSA
Oxacillin, Nafcillin, Dicloxacillin
Toxicity of Oxacillin, Nafcillin, Dicloxacillin
Hypersensitivity rxn and interstitial nephritis
Antipseudomonals
Ticarcillin, Piperacillin
Beta-lactamase inhibitors
Clavulanic Acid, Sulbactam, Tazobactam (CAST)
MoA of Cephalosporins
Inhibit cell wall synthesis, bactericidal
First Generation Cephalosporin
Cefazolin and Cephalexin
against gram positive cocci, Proteus mirabilis, E. coli, Klebsiella pneumoniae
Drug used prior to Sx to prevent S. aureus wound infections.
Cefazolin
2nd Generation Cephalosporin
Cefoxitin, Cefaclor, Cefuroxime
Gram positive cocci, H. infleunza, Enterobacter aerogenes, Neisseria spp., Proteus mirabilis, E. coli, Klebsiella pneumonia, Serratia marcescens
3rd Generation Cephalosporin
Ceftriaxone, Cefotaxime, Ceftazidine
Tx for meningitis and gonorrhea
Ceftriaxone
Tx for Pseudomonas
Ceftazidime
4th Generation Cephalosporin
Cefepime, increase activity against Pseudomonas and gram positive organism
5th Generation Cephalosporin
Ceftaroline
Toxicities for Cephalosporins
Hypersensitivity reactions, Vitamin K deficiency, increased nephrotoxicities of aminoglycosides
Clinical Use for Aztreonam
Gram negative rods only
for penicillin-Ax pts and those with renal insufficiency
MoA of Carbapenems
Broad-spectrum, beta-lacatmase resistant
Administer with cilastatin to decreased inactivation of drug in renal tubules
Toxicities of Carbapenems
GI distress, skin rash, and CNS toxicity (seizures) at hgih plasma levels
MoA of vancomycin
inhibits cell wall peptidoglycan formation by binding D-ala D-ala portion of cell wall precursors
Used to Tx MRSA and C. diff
Vancomycin
Red Man Syndrome
Caused by Vancomycin, prevent with pretreatment with antihistamines) - nephrotoxicity, ototoxicity, thrombophlebitis and diffuse flushing
30S inhibitors
Aminoglycosides (bactericidal)
Tetracycline (bacteriostatic)
50S inhibitors
Chloramphenicol, Clindamycin, Erythromycin (macrolides), Linezolid
Aminoglycosides
Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin
Mechanism of Aminoglycosides
bactericidal, inhibit formation of initiation complex and cause misreading of mRNA.
Block translocation
Require O2 for uptake
Toxicity of Aminoglycosides
Nephrotoxicity, Neuromuscular blockade, Ototoxicity, Teratogen
MoA of Tetracyclines
Binds 30S and prevent attachment of aminoacyl-tRNA, limited CNS penetration
How Doxycycline is eliminated
Fecally, thus can be used in patients with renal failure
What can’t you eat with Tetracyclines
calcium, antacids or iron-containing preparations because of divalent cations
This drug is able to accumulate intracellularly therefore kills Chlamydia and Rickettsia
Tetracyclines
Toxicity of Tetracyclines
discolors teeth and inhibits bone growth in children, photosensitivity
Macrolides
Azithromycin, Clarithromycin, Erythromycin
MoA of Macrolides
Iinhibit protein synthesis by blocking translocation
Binds 23S of rRNA of the 50S ribosomal subunit
Bacteriostatic
Toxicity of Macrolides
GI motility, Arrhythmia from porlonged QT, acute Cholestatic Hepatitis, Rash, Eosinophilia
Blocks peptidyltransferase at 50S ribosomal subunit. Bacteriostatic
Chloramphenicol
Mechanism of resistance is plasmid-encoded acetyltransferase inactivates this drug.
Chloramphenicol
Toxicity is Chloramphenicol
Anemia (dose dependent), Aplastic Anemia, Gray Baby Syndrome (in premature infants because they lack liver UDP-glucuronyl transferase)
Causes Pseudomembranous colitis
Clindamycin
Treats anaerobes above the diaphragm
Clindamycin
Treats anaerobes below the diaphragm
Metronidazole
If a bacteria methylate 23S rRNA binding site, it prevents this set of drugs from working
Macrolides (end in -mycin)
If bacteria have a plasmid-encoded pumps to decrease uptake or increase efflux, it preventsthis set of drugs from working
Tetracyclines (including doxycycline and minocycline)
MoA of Sulfonamides
Inhibit folate synthesis. PABA antimetabolites inhibit dihydropteroate synthase.
Hemolysis if G6PD deficient from this drug
Sulfonamides
This drug could cause nephrotoxicity (tubulointerstitial nephritis)
Sulfonamides
MoA of Trimethoprim (TMP)
Inhibits bacterial dihydrofolate reductase
TMP-SMX Used for
UTIs, Shigella, Salmonella, Pneumocystis jirovecii, toxoplasmosis prophylaxis
Toxicity from Trimethoprim
Megaloblastic Anemia, Leukopenia, Granulocytopenia
Inhibit DNA gyrase (topoisomerase II) and topoisomerase IV.
Fluoroquinolones (end in -floxacin)
Drug that can cause tendonitis, tendon rupture, leg cramps, and myalgias.
Fluoroquinolones (end in -floxacin)
Reason not to use Fluorquinolones in Pregnant, Nursing mothers and children <18years old
Damages cartilage
This drug with my resistant if the bacteria gets a chromosome-encoded mutation in DNA gyrase, plasmid-mediated resistance, efflux pumps.
Fluoroquinolones
MoA of Metronidazole
Forms free radical metabolites in bacteria cell that damage DNA
Triple Therapy for H. pylori
PPI, Clarithromycin, Metronidazole