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Antibiotics
USES
Treatment of wide range of gram-positive or gram-
negative bacterial infections, suppression of intestinal
flora before surgery, control of acne, prophylactically to
prevent rheumatic fever, prophylactically in high-risk
situations (e.g., some surgical procedures or medical
conditions) to prevent bacterial infection.
ACTION
Antibiotics are natural or synthetic compounds that
have the ability to kill or suppress the growth of micro-
organisms.
One means of classifying antibiotics is by their anti-microbial
spectrum. Narrow-spectrum agents are effective against
few microorganisms (e.g., aminoglycosides are effective
against gram-negative aerobes), whereas broad-spectrum
agents are effective against a wide variety of microorgan-
isms (e.g., fluoroquinolones are effective against gram-
positive cocci and gram-negative bacilli).
Antimicrobial agents may also be classified based on their
mechanism of action.
• Agents that inhibit cell wall synthesis or activate en-
zymes that disrupt the cell wall, causing a weakening
in the cell, cell lysis, and death. Include penicillins,
cephalosporins, vancomycin, imidazole antifungal
agents.
• Agents that act directly on the cell wall, affecting
permeability of cell membranes, causing leakage of
intracellular substances. Include antifungal agents
amphotericin and nystatin, polymyxin, colistin.
Antibiotics
• Agents that bind to ribosomal subunits, altering
protein synthesis and eventually causing cell death.
Include aminoglycosides.
• Agents that affect bacterial ribosome function, alter-
ing protein synthesis and causing slow microbial
growth. Do not cause cell death. Include chloram-
phenicol, clindamycin, erythromycin, tetracyclines.
• Agents that inhibit nucleic acid metabolism by bind-
ing to nucleic acid or interacting with enzymes nec-
essary for nucleic acid synthesis. Inhibit DNA or RNA
synthesis. Include rifampin, metronidazole, fluoro-
quinolones (e.g., ciprofloxacin).
• Agents that inhibit specific metabolic steps necessary
for microbial growth, causing a decrease in essential
cell components or synthesis of nonfunctional ana-
logues of normal metabolites. Include trimethoprim,
sulfonamides.
• Agents that inhibit viral DNA synthesis by binding to
viral enzymes necessary for DNA synthesis, prevent-
ing viral replication. Include acyclovir, vidarabine.
SELECTION OF ANTIMICROBIAL AGENTS
The goal of therapy is to achieve antimicrobial action at
the site of infection sufficient to inhibit the growth of the
microorganism. The agent selected should be the most
active against the most likely infecting organism, least
likely to cause toxicity or allergic reaction. Factors to
consider in selection of an antimicrobial agent include the
following:
• Sensitivity pattern of the infecting microorganism
• Location and severity of infection (may determine
route of administration)
• Pt’s ability to eliminate the drug (status of renal and
hepatic function)
• Pt’s defense mechanisms (includes both cellular and
humoral immunity)
• Pt’s age, pregnancy status, genetic factors, allergies,
CNS disorder, preexisting medical problems

CATEGORIZATION OF ORGANISMS BY GRAM STAINING

Gram-Positive Cocci Gram-Negative Cocci Gram-Positive Bacilli Gram-Negative Bacilli
Aerobic Aerobic Aerobic Aerobic
Staphylococcus aureus Neisseria gonorrhoeae Listeria monocytogenes Escherichia coli
Staphylococcus epidermidis Neisseria meningitidis Bacillus anthracis Klebsiella pneumoniae
Streptococcus pneumoniae Moraxella catarrhalis Corynebacterium diphtheriae Proteus mirabilis
Streptococcus pyogenes Anaerobic Serratia marcescens
Viridans streptococci Clostridium difficile Acinetobacter spp.
Enterococcus faecalis Clostridium perfringens Pseudomonas aeruginosa
Enterococcus faecium Clostridium tetani Enterobacter spp.

Antibiotics
Anaerobic Actinomyces spp. Haemophilus influenzae
Peptostreptococcus spp. Legionella pneumophila
Peptococcus spp. Anaerobic
Bacteroides fragilis
Fusobacterium spp.

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CLASSIFICATIONS
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Antibiotic: Aminoglycosides
USES ACTION

Treatment of serious infections when other less-toxic
agents are not effective, are contraindicated, or require
adjunctive therapy (e.g., with penicillins or cephalospo-
rins). Used primarily in the treatment of infections caused
by gram-negative microorganisms, such as those caused
by Proteus, Klebsiella, Pseudomonas, Escherichia coli,
Serratia, and Enterobacter. Inactive against most gram-
positive microorganisms. Not well absorbed systemically
from GI tract (must be administered parenterally for sys-
temic infections). Oral agents are given to suppress intes-
tinal bacteria.
Antibiotic: Aminoglycosides
Bactericidal. Transported across bacterial cell membrane;
irreversibly bind to specific receptor proteins of bacterial
ribosomes. Interfere with protein synthesis, preventing
cell reproduction and eventually causing cell death.

ANTIBIOTIC: AMINOGLYCOSIDES
Name Availability Dosage Range Side Effects
Amikacin (Amikin) I: 50 mg/ml, 250 mg/ml A: 7.5 mg/kg q12h or Nephrotoxicity, neurotoxicity, ototoxicity (both auditory and
15–20 mg/kg once daily vestibular), hypersensitivity (skin itching, redness, rash,
C: 7.5 mg/kg q12h swelling)
Gentamicin I: 10 mg/ml, 40 mg/ml A: 5–7 mg/kg once daily or Same as amikacin
(Garamycin) 1–2.5 mg/kg q8h
C: 1–2.5 mg/kg q8h
Neomycin T: 500 mg A: 1 g for 3 doses as preop Nausea, vomiting, diarrhea
Tobramycin (Nebcin) I: 10 mg/ml, 40 mg/ml A: 5–7 mg/kg once daily or Same as amikacin
1–2.5 mg/kg q8h
C: 1–2.5 mg/kg q8h
A, Adults; C (dosage), children; I, injection; T, tablets.

Antibiotic: Cephalosporins
USES
Broad-spectrum antibiotics, which, like penicillins, may
be used in a number of diseases, including respiratory
diseases, skin and soft tissue infection, bone/joint infec-
tions, genitourinary infections, prophylactically in some
surgical procedures.
First-generation cephalosporins have activity against
gram-positive organisms (e.g., streptococci and most
staphylococci) and activity against most gram-negative
organisms, including Escherichia coli, Klebsiella pneu-
moniae, Proteus mirabilis, Salmonella, and Shigella.
ANTIBIOTIC: CEPHALOSPORINS
Name Availability
First-Generation
Cefadroxil (Duricef) C: 500 mg
T: 1 g
S: 125 mg/5 ml, 250 mg/5 ml,
500 mg/5 ml
ACTION
Second-generation cephalosporins have same effective-
ness as first-generation and increased activity against gram-
negative organisms, including Haemophilus influenzae,
Neisseria, Enterobacter, and several anaerobic organisms.
Third-generation cephalosporins are less active against
gram-positive organisms but more active against the En-
terobacteriaceae with some activity against Pseudomonas
aeruginosa, Serratia spp., and Acinetobacter spp.
Fourth-generation cephalosporins have good activity
against gram-positive organisms (e.g., Staphylococcus
Dosage Range
A: 500 mg–1 g q12h
C: 15 mg/kg q12h
aureus) and gram-negative organisms (e.g., Pseudomo-
nas aeruginosa, E. coli, Klebsiella, and Proteus).
Fifth-generation cephalosporins have good activity
against gram-positive organisms (e.g., Staphylococcus
aureus, Streptococcus spp.) and gram-negative organ-
isms (e.g., E. coli, Klebsiella spp.).
Cephalosporins inhibit cell wall synthesis or activate en-
zymes that disrupt the cell wall, causing cell lysis and cell
death. May be bacteriostatic or bactericidal. Most effective
Antibiotic: Cephalosporins
against rapidly dividing cells.
Side Effects
Abdominal cramps/pain, fever, nausea,
vomiting, diarrhea, headaches,
oral/vaginal candidiasis
Continued
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CLASSIFICATIONS

ANTIBIOTIC: CEPHALOSPORINS—cont’d
Name Availability
Cefazolin (Ancef) I: 500 mg, 1 g, 2 g
Cephalexin (Keflex, Keftab) C: 250 mg, 500 mg
T: 250 mg, 500 mg, 1 g
Second-Generation
Cefaclor (Ceclor) C: 250 mg, 500 mg
T (ER): 500 mg
S: 125 mg/5 ml, 187 mg/5 ml,
250 mg/5 ml, 375 mg/5 ml
Cefotetan I: 1 g, 2 g
Cefoxitin (Mefoxin) I: 1 g, 2 g
Cefprozil (Cefzil) T: 250 mg, 500 mg
S: 125 mg/5 ml, 250 mg/5 ml
Cefuroxime (Ceftin, Kefurox, Zinacef) T: 125 mg, 250 mg, 500 mg
S: 125 mg/5 ml, 250 mg/5 ml
I: 750 mg, 1.5 g
Dosage Range
A: 500 mg–2 g q6–8h
C: 25–100 mg/kg/day
divided q6–8h
A: 250 mg–1 g q6–12h
C: 25–100 mg/kg/day
divided q6–8h
A: 250–500 mg q8h
C: 20–40 mg/kg/day q8–12h
A: 500 mg–3 g q12h
C: 20–50 mg/kg q12h
A: 1–2 g q6–8h
C: 80–160 mg/kg/day
divided q6h
A: 500 mg q12–24h
C: 7.5–15 mg/kg q12h
A (PO): 125–500 mg q12h
(IM/IV): 750 mg–1.5 g q8–12h
C (PO): 10–15 mg/kg q12h
(IM/IV): 50–150 mg/kg/day
divided q8h
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Antibiotic: Cephalosporins
Side Effects
Fever, rash, diarrhea, nausea, pain at
injection site
Headache, abdominal pain, diarrhea,
nausea, dyspepsia
Rash, diarrhea, increased transaminases
May have serum sickness–like reaction
Diarrhea, increased AST, ALT,
hypersensitivity reactions
Diarrhea
Dizziness, abdominal pain, diarrhea,
nausea, increased AST, ALT
Diarrhea, nausea, vomiting, thrombophlebitis,
increased AST, ALT
 Third-Generation

Cefdinir (Omnicef) C: 300 mg A: 300 mg q12h or 600 mg Headache, hyperglycemia, abdominal
S: 125 mg/5 ml once daily pain, diarrhea, nausea
C: 7 mg/kg q12h or 14 mg/kg
once daily
Cefditoren (Spectracef) T: 200 mg A: 200–400 mg q12h Diarrhea, nausea
C: (.11 yrs): 200–400 mg q12h
Cefotaxime (Claforan) I: 500 mg, 1 g, 2 g A: 1–2 g q4–12h Rash, diarrhea, nausea, pain at injection
C: 50–200 mg/kg/day site
divided q4–6h
Cefpodoxime (Vantin) T: 100 mg, 200 mg A: 100–400 mg q12h Rash, diarrhea, nausea
S: 50 mg/5 ml, 100 mg/5 ml C: 5 mg/kg q12h
Ceftazidime I: 500 mg, 1 g, 2 g A: 500 mg–2 g q8–12h Diarrhea, pain at injection site
(Fortaz, Tazicef, Tazidime) C: 30–100 mg/kg q8h

Antibiotic: Cephalosporins
Ceftibuten (Cedax) C: 400 mg A: 400 mg once daily Headache, nausea, diarrhea
S: 90 mg/5 ml, 180 mg/5 ml C: 4.5 mg/kg bid or 9 mg/kg
once daily
Ceftriaxone I: 250 mg, 500 mg, 1 g, 2 g A: 1–2 g q12–24h Rash, diarrhea, eosinophilia, increased
(Rocephin) C: 50–100 mg/kg/day AST, ALT
divided q12–24h
Fourth-Generation
Cefepime (Maxipime) I: 500 mg, 1 g, 2 g A: 1–2 g q8–12h Rash, diarrhea, nausea; increased AST,
C: 50 mg/kg q8–12h ALT
Fifth-Generation
Ceftaroline (Teflaro) I: 400 mg, 600 mg A: 600 mg q12h Headache, insomnia, rash, pruritus,
diarrhea, nausea

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A, Adults; C, capsules; C (dosage), children; ER, extended-release; I, injection; S, suspension; T, tablets.
CLASSIFICATIONS
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Antibiotic: Fluoroquinolones
USES ACTION

Antibiotic: Fluoroquinolones
Fluoroquinolones act against a wide range of gram-negative structure infections, urinary tract infections, and sexually Bactericidal. Inhibit DNA gyrase in susceptible microor-
and gram-positive organisms. They are used primarily in transmitted diseases. ganisms, interfering with bacterial DNA replication and
the treatment of lower respiratory infections, skin/skin repair.

ANTIBIOTIC: FLUOROQUINOLONES
Name
Ciprofloxacin
(Cipro)
Gemifloxacin (Factive)
Levofloxacin (Levaquin)
Moxifloxacin (Avelox)
Norfloxacin (Noroxin)
Ofloxacin
A, Adults; I, injection; OS, oral solution; PO, oral; S, suspension; T, tablets.
Availability Dosage Range Side Effects
T: 100 mg, 250 mg, 500 mg, 750 mg A (PO): 250–750 mg q12h; Dizziness, headaches, anxiety, drowsiness,
S: 250 mg/5 ml, 500 mg/5 ml (IV): 200–400 mg q12h insomnia, abdominal pain, nausea, diarrhea,
I: 200 mg, 400 mg vomiting, phlebitis (parenteral)
T: 320 mg A: 320 mg once daily Headache, dizziness, rash, diarrhea, nausea
T: 250 mg, 500 mg, 750 mg A (PO/IV): 250–750 mg/day Headache, insomnia, dizziness, rash, nausea,
I: 250 mg, 500 mg, 750 mg as single dose diarrhea, constipation
OS: 250 mg/10 ml
T: 400 mg A: 400 mg/day Headache, dizziness, insomnia, nausea, diarrhea
I: 400 mg
T: 400 mg A: 400 mg q12h Same as ciprofloxacin
T: 200 mg, 300 mg, 400 mg A: 200–400 mg q12h Dizziness, headache, insomnia, abdominal
cramps, diarrhea, nausea

Antibiotic: Macrolides
USES ACTION
Macrolides act primarily against most gram-positive mi- Bacteriostatic or bactericidal. Reversibly binds to the P
croorganisms and some gram-negative cocci. Azithromy- site of the 50S ribosomal subunit of susceptible organ-
cin and clarithromycin appear to be more potent than isms, inhibiting RNA-dependent protein synthesis.
erythromycin. Macrolides are used in the treatment of
pharyngitis/tonsillitis, sinusitis, chronic bronchitis, pneu-
monia, uncomplicated skin/skin structure infections.

ANTIBIOTIC: MACROLIDES
Name Availability Dosage Range Side Effects
Azithromycin (Zithromax) T: 250 mg, 600 mg A (PO): 500 mg once, then 250 mg PO: Nausea, diarrhea, vomiting,

Antibiotic: Macrolides
S: 100 mg/5 ml, 200 mg/5 ml, 1-g packet once daily abdominal pain
I: 500 mg (IV): 500 mg/day IV: Pain, redness, swelling at
C (PO/IV): 5–10 mg/kg once daily injection site
Clarithromycin (Biaxin) T: 250 mg, 500 mg A: 250–500 mg q12h Headaches, loss of taste, nausea,
T (XL): 500 mg C: 7.5 mg/kg q12h vomiting, diarrhea, abdominal pain/
S: 125 mg/5 ml discomfort
Erythromycin T: 200 mg, 250 mg, 333 mg, 400 mg, A (PO): 250–500 mg q6h PO: Nausea, vomiting, diarrhea,
(EES, Eryc, EryPed, 500 mg (IV): 500 mg–1 g q6h abdominal pain
Ery-Tab, Erythrocin, PCE) C: 250 mg C (PO): 7.5 mg/kg q6h IV: Inflammation, phlebitis at injection
S: 100 mg/2.5 ml, 125 mg/5 ml, (IV): 15–50 mg/kg/day in divided site
200 mg/5 ml, 250 mg/5 ml, 400 mg/5 ml doses q6h

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A, Adults; C, capsules; C (dosage), children; I, injection; S, suspension; T, tablets; XL, long-acting.
CLASSIFICATIONS

Antibiotic: Penicillins
USES
Penicillins (also referred to as beta-lactam antibiotics)
may be used to treat a large number of infections, includ-
ing pneumonia and other respiratory diseases, urinary
tract infections, septicemia, meningitis, intra-abdominal
infections, gonorrhea and syphilis, bone/joint infection.
Penicillins are classified based on an antimicrobial
spectrum:
Natural penicillins are very active against gram-positive
cocci but ineffective against most strains of Staphylococ-
cus aureus (inactivated by enzyme penicillinase).
ANTIBIOTIC: PENICILLINS
Name Availability
Natural
Penicillin G benzathine I: 600,000 units, 1.2 million units,
(Bicillin, Bicillin LA) 2.4 million units
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ACTION
Antibiotic: Penicillins
Penicillinase-resistant penicillins are effective Penicillins inhibit cell wall synthesis or activate enzymes,
against penicillinase-producing Staphylococcus au- which disrupt the bacterial cell wall, causing cell lysis and
reus but are less effective against gram-positive cocci cell death. May be bacteriostatic or bactericidal. Most
than the natural penicillins. effective against bacteria undergoing active growth and
Broad-spectrum penicillins are effective against division.
gram-positive cocci and some gram-negative bacteria
(e.g., Haemophilus influenzae, Escherichia coli, Pro-
teus mirabilis, Salmonella, and Shigella).
Extended-spectrum penicillins are effective against
gram-negative organisms, including Pseudomonas ae-
ruginosa, Enterobacter, Proteus spp., Klebsiella, Ser-
ratia spp., and Acinetobacter spp.
Dosage Range Side Effects
A: 1.2–2.4 million units as Mild diarrhea, nausea, vomiting,
single dose �
headaches, sore mouth/tongue,
C: 25,000–50,000 units/kg as Â�vaginal itching/discharge, allergic
single dose �reaction (including anaphylaxis, skin
rash, urticaria, pruritus)
Penicillin G potassium
(Pfizerpen)
Penicillin V potassium
(Apo-Pen-VK)
Penicillinase-Resistant
Dicloxacillin
(Dynapen, Pathocil)
Nafcillin (Unipen)
Oxacillin (Bactocill)
Broad-Spectrum
Amoxicillin (Amoxil, Trimox)
Amoxicillin/clavulanate
(Augmentin)
I: 1, 2, 3, 5 million-unit vials
T: 250 mg, 500 mg
S: 125 mg/5 ml, 250 mg/5 ml
C: 125 mg, 250 mg, 500 mg
S: 62.5 mg/5 ml
I: 500 mg, 1 g, 2 g
C: 250 mg, 500 mg
S: 250 mg/5 ml
I: 250 mg, 500 mg, 1 g, 2 g
T: 125 mg, 250 mg, 500 mg, 875 mg
C: 250 mg, 500 mg
S: 50 mg/ml, 125 mg/5 ml, 250 mg/5 ml
T: 250 mg, 500 mg, 875 mg
T (chewable): 125 mg, 200 mg,
250 mg, 400 mg
S: 125 mg/5 ml, 200 mg/5 ml,
250 mg/5 ml, 400 mg/5 ml
A: 2–4 million units q4h Rash, injection site reaction, phlebitis
C: 100,000–250,000 units/kg/
day divided q4–6h
A: 250–500 mg q6–8h Diarrhea, nausea, vomiting
C: 25–50 mg/kg/day in
divided doses q6–8h
A: 125–500 mg q6h Abdominal pain, diarrhea, nausea
C: 25–50 mg/kg/day divided
q6h
A (IV): 500 mg–2 g q4–6h Inflammation, pain, phlebitis
C (IV): 50–150 mg/kg/day in Increased risk of interstitial nephritis
divided doses q4–6h
A (IV): 1–2 g q4–6h Diarrhea, nausea, vomiting
C (IV): 25–50 mg/kg q6h Increased risk of hepatotoxicity,
interstitial nephritis
Antibiotic: Penicillins
A: 250–500 mg q8h or Diarrhea, colitis, nausea
500–875 g q12h
C: 20–90 mg/kg/day divided
q8–12h
A: 875 mg q12h or Diarrhea, rash, nausea, vomiting
250–500 mg q8h
C: 25–90 mg/kg/day divided
q12h
Continued
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CLASSIFICATIONS
ANTIBIOTIC: PENICILLINS—cont’d

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Name Availability Dosage Range Side Effects
Ampicillin C: 250 mg, 500 mg A (PO): 250–500 mg q6h Nausea, vomiting, diarrhea

Antibiotic: Penicillins
(Principen) S: 125 mg/5 ml, 250 mg/5 ml (IV): 500 mg–2 g q6h
I: 125 mg, 250 mg, 500 mg, 1 g, 2 g C (PO): 12.5–50 mg/kg q6h
(IV): 25–50 mg/kg q6h
Ampicillin/sulbactam I: 1.5 g, 3 g A: 1.5–3 g q6h Local pain at injection site, rash,
(Unasyn) C: 25–50 mg/kg q6h diarrhea
Extended-Spectrum
Piperacillin/tazobactam I: 2.25 g, 3.375 g, 4.5 g A: 3.375 g q6h or 4.5 g q6–8h Diarrhea, insomnia, headache, fever,
(Zosyn) C: 240–300 mg/kg/day rash
divided q8h
Ticarcillin/clavulanate I: 3.1 g A: 3.1 g q4–6h Colitis, nausea, vomiting, diarrhea
(Timentin) C: 200–300 mg/kg/day
divided q4–6h
A, Adults; C, capsules; C (dosage), children; I, injection; PO, oral; S, suspension; T, tablets.