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By Valentin Sosa MD
DRUG CLASS AND       MECHANISM OF                                                                   ANTIBACTERIAL
NAME                 ACTION               COMMENT              HALF-LIFE   TOXICITY                 SPECTRUM
Penicillins
Penicillin 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 wall




Antistaphylococcal
Methicillin          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 only
Nafcillin                                                        Short    Interstitial nephritis
“Easy” gram-negative
Ampicillin             β-Lactam mechanism Hydrolyzed by all β-   Short    Low; diarrhea and        Streptococcal
Amoxicillin                               lactamases             Medium   rash                     species, including
                                                                                                   many enterococci,
                                                                                                   Neisseria species
                                                                                                   (non– lactamase
                                                                                                   producing),
                                                                                                   Haemophilus
                                                                                                   influenzae (non–
                                                                                                   lactamase producing),
                                                                                                   some Escherichia coli
                                                                                                   and Proteus mirabilis
Expanded spectrum
Carbenicillin          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
                                                                                                 enterococci
Very advanced spectrum
Mezlocillin            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 species

β-Lactamase            β-Lactam                                          Low; same as
inhibitor              mechanism, plus                                   constituent β-lactam
combination
Clavulanic acid plus   Clavulanic acid
                       mechanism: β-
                       lactamase inhibitor
                       that increases the
                       antibacterial activity of
                       β-lactam antibiotics

Ticarcillin                                                      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 with
Poor 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, plus
activity                                                                                             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     Low



Good Pseudomonas
activity
 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
Monobactams


Aztreonam           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-
                    lactamases

Carbapenems         β-Lactam
                    mechanism, plus

Imipenem/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
                    tubule


Meropenem                             Provided alone       Short   Reduced potential Same activity as imipenem
                                      without cilastatin           for seizures
Quinolones
Poor anaerobic   Inhibit bacterial
activity         enzyme DNA-
                 gyrase, thus
                 inhibiting DNA
                 replication
Norfloxacin                          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
                                                                                    anaerobes
Ofloxacin                            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
                                                                                                 anaerobes

Gentamicin                                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
                                                                        nephrotoxicity

Amikacin                                  See above          Medium     See above                Active against a
                                                                        (aminoglycosides)        significant number of
                                                                                                 gentamicin- and
                                                                                                 tobramycin-resistant
                                                                                                 organisms

Netilmicin                                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
Streptogramins

Quinupristin/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
Oxazolidinones

Linezolid    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
Macrolides
Erythromycin    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                                                 Legionella




Tetracyclines
Tetracycline    Inhibit protein    Oral or IV   Long        Stain teeth of   Many gram-
                synthesis by                                children         positive, easy
Doxycycline     attaching to the   Oral or IV   Very long   Same             gram-negative
                30S subunit of                                               rods, some
                the bacterial                                                anaerobes,
                ribosome                                                     Rickettsia,
                                                                             Chlamydia,
                                                                             Mycoplasma
Antifungal Triazoles
Fluconazole    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
                                                                       glabrata
Voriconazole                              Long        Visual           Most fungi
                                                      disturbances,
                                                      fever

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Clasficacion de antimicrobianos sabinston cirugia

  • 2. DRUG CLASS AND MECHANISM OF ANTIBACTERIAL NAME ACTION COMMENT HALF-LIFE TOXICITY SPECTRUM Penicillins Penicillin 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 wall Antistaphylococcal Methicillin β-Lactam mechanism. First Short Interstitial nephritis Staphylococcal Also penicillinase antistaphylococcal species (methicillin resistant and acid drug sensitive) and stable streptococcal species except enterococcus
  • 3. Oxacillin Short Interstitial nephritis Narrow spectrum; generally used for staphylococcal infections only Nafcillin Short Interstitial nephritis “Easy” gram-negative Ampicillin β-Lactam mechanism Hydrolyzed by all β- Short Low; diarrhea and Streptococcal Amoxicillin lactamases Medium rash species, including many enterococci, Neisseria species (non– lactamase producing), Haemophilus influenzae (non– lactamase producing), some Escherichia coli and Proteus mirabilis Expanded spectrum Carbenicillin 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
  • 4. Ticarcillin β-Lactam mechanism Same Short Same, but less activity against enterococci Very advanced spectrum Mezlocillin 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 species β-Lactamase β-Lactam Low; same as inhibitor mechanism, plus constituent β-lactam combination Clavulanic acid plus Clavulanic acid mechanism: β- lactamase inhibitor that increases the antibacterial activity of β-lactam antibiotics Ticarcillin Short Same as ticarcillin or amoxicillin plus staphylococci (methicillin sensitive), lactamase-positive H. influenzae and some lactamase-producing gram-negative rods, and anaerobes
  • 5. 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 with Poor 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, plus activity many anaerobes Short half-life Cefoxitin Short Low Longer half-life Cefmetazole Medium Low Cefotetan Long Prolonged prothrombin
  • 6. ―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 Low Good Pseudomonas activity 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
  • 7. Monobactams Aztreonam 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- lactamases Carbapenems β-Lactam mechanism, plus Imipenem/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 tubule Meropenem Provided alone Short Reduced potential Same activity as imipenem without cilastatin for seizures
  • 8. Quinolones Poor anaerobic Inhibit bacterial activity enzyme DNA- gyrase, thus inhibiting DNA replication Norfloxacin 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 anaerobes Ofloxacin Racemic mixture Long of levofloxacin (active) and dextrofloxacin (inactive) Levofloxacin Long
  • 9. 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 anaerobes Gentamicin 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 nephrotoxicity Amikacin See above Medium See above Active against a (aminoglycosides) significant number of gentamicin- and tobramycin-resistant organisms Netilmicin See above Medium See above See above (aminoglycosides) (aminoglycosides)
  • 10. 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
  • 11. Streptogramins Quinupristin/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
  • 12. Oxazolidinones Linezolid 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
  • 13. Macrolides Erythromycin 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 Legionella Tetracyclines Tetracycline Inhibit protein Oral or IV Long Stain teeth of Many gram- synthesis by children positive, easy Doxycycline attaching to the Oral or IV Very long Same gram-negative 30S subunit of rods, some the bacterial anaerobes, ribosome Rickettsia, Chlamydia, Mycoplasma
  • 14. Antifungal Triazoles Fluconazole 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 glabrata Voriconazole Long Visual Most fungi disturbances, fever