DRUG CLASS AND MECHANISM OF ANTIBACTERIALNAME ACTION COMMENT HALF-LIFE TOXICITY SPECTRUMPenicillinsPenicillin G β-Lactam mechanism: Prototype. Hydrolyzed Short Low, but rarely an Streptococcal species inhibits bacterial cell by all β-lactamases allergic reaction may except enterococci wall by binding to be life threatening and penicillin-resistant penicillin-binding pneumococci, proteins (PBPs). It Neisseria species inhibits the final except lactamase- transpeptidation step producing gonococci of peptidoglycan synthesis in the bacterial cell wallAntistaphylococcalMethicillin β-Lactam mechanism. First Short Interstitial nephritis Staphylococcal Also penicillinase antistaphylococcal species (methicillin resistant and acid drug sensitive) and stable streptococcal species except enterococcus
Oxacillin Short Interstitial nephritis Narrow spectrum; generally used for staphylococcal infections onlyNafcillin Short Interstitial nephritis“Easy” gram-negativeAmpicillin β-Lactam mechanism Hydrolyzed by all β- Short Low; diarrhea and StreptococcalAmoxicillin lactamases Medium rash species, including many enterococci, Neisseria species (non– lactamase producing), Haemophilus influenzae (non– lactamase producing), some Escherichia coli and Proteus mirabilisExpanded spectrumCarbenicillin β-Lactam mechanism Hydrolyzed by all β- Short High sodium load. Greatly expanded lactamases Inhibition of platelet gram-negative aggregation spectrum while still active against streptococcal species, including enterococci. Moderate antianaerobe activity. May not be reliable as the sole agent for established gram- negative rod infections
Ticarcillin β-Lactam mechanism Same Short Same, but less activity against enterococciVery advanced spectrumMezlocillin β-Lactam mechanism Hydrolyzed by all β- Short Low Same as expanded-Piperacillin lactamases Same Short Low spectrum penicillins but with more activity against Pseudomonas, Acinetobacter, and Serratia speciesβ-Lactamase β-Lactam Low; same asinhibitor mechanism, plus constituent β-lactamcombinationClavulanic acid plus Clavulanic acid mechanism: β- lactamase inhibitor that increases the antibacterial activity of β-lactam antibioticsTicarcillin Short Same as ticarcillin or amoxicillin plus staphylococci (methicillin sensitive), lactamase-positive H. influenzae and some lactamase-producing gram-negative rods, and anaerobes
Cephalosporins―First‖ generation β-Lactam mechanism Streptococcal species except enterococci,Short half-life staphylococcal species Cephalothin Prototype of class Short Low (methicillin sensitive), Cephapirin Short Low and ―easy‖ gram-Longer half-life negative rods Cefazolin Medium Low―Second‖ generation β-Lactam mechanism Same as first-generation cephalosporins withPoor anaerobic activity expanded gram- negative activity not Shorter half-life including Pseudomonas, Acinetobacter, or Serratia Cefamandole Short Low Cefuroxime Medium Low Longer half-life Ceforanide Reduced Long Cefonicid antistaphylococcal Long activity Good anaerobic Same as above, plusactivity many anaerobes Short half-life Cefoxitin Short Low Longer half-life Cefmetazole Medium Low Cefotetan Long Prolonged prothrombin
―Third‖ generation β-Lactam Very active against most gram- mechanism negative rods except Poor Pseudomonas Pseudomonas, Acinetobacter,activity and Serratia. Poor against anaerobes. Less activity against Short half-life streptococcal and Cefotaxime Short Low staphylococcal species than Ceftizoxime Medium Low first-and second-generation cephalosporins. Long half-life Ceftriaxone Long LowGood Pseudomonasactivity Cefoperazone Medium Low Same as above plus activity against many Pseudomonas, Ceftazidime Medium Low Acinetobacter, and Serratia species Cefepime Medium Low Same as above with increased activity against gram-positive cocci
MonobactamsAztreonam β-Lactam Safe for most Short Low Excellent activity against most mechanism: patients with gram-negatives, including preference to penicillin allergy Pseudomonas and Serratia. PBP-3 of gram- Inactive against gram-positive negative cocci, anaerobes, and most bacteria. Very Acinetobacter strains stable against β- lactamasesCarbapenems β-Lactam mechanism, plusImipenem/cilastatin Cilastatin Provided in Short Low. Seizures in Extremely broad gram-positive mechanism: combination with certain high-risk and gram-negative aerobic and inactivates cilastatin to patients anaerobic. Modest activity dehydropeptidas prevent renal against enterococci. Inactive es, which would breakdown and against Stenotrophomonas normally break renal toxicity (formerly Xanthomonas) the β-lactam ring maltophilia of imipenem in the proximal tubuleMeropenem Provided alone Short Reduced potential Same activity as imipenem without cilastatin for seizures
QuinolonesPoor anaerobic Inhibit bacterialactivity enzyme DNA- gyrase, thus inhibiting DNA replicationNorfloxacin Oral only; urine Long Low Very broad Gram- levels only Interaction leads to negative activity. accumulation of Gram-positive and theophylline very broad gram- negative activity,Ciprofloxacin Oral and Long including intravenous Pseudomonas, (applies to all Acinetobacter, and below) Serratia. Poor activity against anaerobesOfloxacin Racemic mixture Long of levofloxacin (active) and dextrofloxacin (inactive)Levofloxacin Long
Aminoglycosides Bind to a specific All have a low ratio Medium Nephrotoxicity and Extremely broad protein in the 30S of therapeutic-to-toxic nerve VIII toxicity, coverage of gram- subunit of the levels. All are both auditory and negative rods. Poor bacterial ribosome, frequently vestibular activity against which leads to faulty underdosed. All streptococci. Some alignment or exhibit a significant synergism with recognition by RNA postantibiotic effect[*] penicillin or during initiation of vancomycin against microbial peptide enterococci. No chain formation activity against anaerobesGentamicin See above Medium See above Most active against enterococci and Serratia spp.Tobramycin See above Medium Statistically but More active against questionably Pseudomonas spp. clinically significant decrease in nephrotoxicityAmikacin See above Medium See above Active against a (aminoglycosides) significant number of gentamicin- and tobramycin-resistant organismsNetilmicin See above Medium See above See above (aminoglycosides) (aminoglycosides)
Vancomycin Inhibits cell Only IV. No Very long Hypotension Streptococcal wall synthesis oral absorption and histamine species, by binding to release including many carboxyl phenomena enterococci, subunits on (redman staphylococci peptide syndrome) (including subunits during methicillin- containing free infusion. resistant D-alanyl-D- strains), alanine Clostridium (different site species. No from β- activity against lactams—no gram-negative cross rods resistance), plus may affect permeability of membrane, plus may inhibit RNA synthesis
StreptograminsQuinupristin/dalfo Binds to different Significant Medium Reversible Most gram-pristin sites on the 50S postantibiotic transaminase positive subunit of effect[*] elevations pathogens, bacterial including ribosomes A 5- to vancomycin- 10-fold decrease resistant in the dissociation Enterococcus constant of faecium, quinupristin is methicillin- seen in the resistant presence of Staphylococcus dalfopristin aureus and Staphylococcus epidermidis, and penicillin- resistant Streptococcus pneumoniae but not Enterococcus faecalis
OxazolidinonesLinezolid Attaches to the Oral or IV Long Reversible Most gram- 50S subunit of monoamine positive the bacterial oxidase bacteria, ribosome and inhibition with including inhibits protein the potential to methicillin- synthesis interact with resistant S. adrenergic or aureus and serotoninergic vancomycin- drugs and resistant cause enterococci hypertension
MacrolidesErythromycin Attaches to the Oral or IV Medium Cholestasis with Most gram- 50S subunit of estolate (IV) form positive, the bacterial Neisseria, ribosome and Campylobacter, may interfere Mycoplasma, with translocation Chlamydia, reactions of the Rickettsia, peptide chains LegionellaTetracyclinesTetracycline Inhibit protein Oral or IV Long Stain teeth of Many gram- synthesis by children positive, easyDoxycycline attaching to the Oral or IV Very long Same gram-negative 30S subunit of rods, some the bacterial anaerobes, ribosome Rickettsia, Chlamydia, Mycoplasma
Antifungal TriazolesFluconazole Inhibition of Oral or IV Very long Elevation of Most fungi cytochrome P- liver function except 450–dependent test result Candida ergosterol krusei, synthesis Candida glabrataVoriconazole Long Visual Most fungi disturbances, fever
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