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