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Antibiotics
USES ACTION

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

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

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 ACTION
Broad-spectrum antibiotics, which, like penicillins, may Second-generation cephalosporins have same effective- aureus) and gram-negative organisms (e.g., Pseudomo-
be used in a number of diseases, including respiratory ness as first-generation and increased activity against gram- nas aeruginosa, E. coli, Klebsiella, and Proteus).
diseases, skin and soft tissue infection, bone/joint infec- negative organisms, including Haemophilus influenzae,
Fifth-generation cephalosporins have good activity
tions, genitourinary infections, prophylactically in some Neisseria, Enterobacter, and several anaerobic organisms.
against gram-positive organisms (e.g., Staphylococcus
surgical procedures.
Third-generation cephalosporins are less active against aureus, Streptococcus spp.) and gram-negative organ-
First-generation cephalosporins have activity against gram-positive organisms but more active against the En- isms (e.g., E. coli, Klebsiella spp.).
gram-positive organisms (e.g., streptococci and most terobacteriaceae with some activity against Pseudomonas
Cephalosporins inhibit cell wall synthesis or activate en-
staphylococci) and activity against most gram-negative aeruginosa, Serratia spp., and Acinetobacter spp.
zymes that disrupt the cell wall, causing cell lysis and cell
organisms, including Escherichia coli, Klebsiella pneu-
Fourth-generation cephalosporins have good activity death. May be bacteriostatic or bactericidal. Most effective
moniae, Proteus mirabilis, Salmonella, and Shigella.

Antibiotic: Cephalosporins
against gram-positive organisms (e.g., Staphylococcus against rapidly dividing cells.

ANTIBIOTIC: CEPHALOSPORINS
Name Availability Dosage Range Side Effects
First-Generation
Cefadroxil (Duricef) C: 500 mg A: 500 mg–1 g q12h Abdominal cramps/pain, fever, nausea,
T: 1 g C: 15 mg/kg q12h vomiting, diarrhea, headaches,
S: 125 mg/5 ml, 250 mg/5 ml, oral/vaginal candidiasis
500 mg/5 ml

Continued

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CLASSIFICATIONS
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ANTIBIOTIC: CEPHALOSPORINS—cont’d

Antibiotic: Cephalosporins
Name Availability Dosage Range Side Effects
Cefazolin (Ancef) I: 500 mg, 1 g, 2 g A: 500 mg–2 g q6–8h Fever, rash, diarrhea, nausea, pain at
C: 25–100 mg/kg/day injection site
divided q6–8h
Cephalexin (Keflex, Keftab) C: 250 mg, 500 mg A: 250 mg–1 g q6–12h Headache, abdominal pain, diarrhea,
T: 250 mg, 500 mg, 1 g C: 25–100 mg/kg/day nausea, dyspepsia
divided q6–8h
Second-Generation
Cefaclor (Ceclor) C: 250 mg, 500 mg A: 250–500 mg q8h Rash, diarrhea, increased transaminases
T (ER): 500 mg C: 20–40 mg/kg/day q8–12h May have serum sickness–like reaction
S: 125 mg/5 ml, 187 mg/5 ml,
250 mg/5 ml, 375 mg/5 ml
Cefotetan I: 1 g, 2 g A: 500 mg–3 g q12h Diarrhea, increased AST, ALT,
C: 20–50 mg/kg q12h hypersensitivity reactions
Cefoxitin (Mefoxin) I: 1 g, 2 g A: 1–2 g q6–8h Diarrhea
C: 80–160 mg/kg/day
divided q6h
Cefprozil (Cefzil) T: 250 mg, 500 mg A: 500 mg q12–24h Dizziness, abdominal pain, diarrhea,
S: 125 mg/5 ml, 250 mg/5 ml C: 7.5–15 mg/kg q12h nausea, increased AST, ALT
Cefuroxime (Ceftin, Kefurox, Zinacef) T: 125 mg, 250 mg, 500 mg A (PO): 125–500 mg q12h Diarrhea, nausea, vomiting, thrombophlebitis,
S: 125 mg/5 ml, 250 mg/5 ml (IM/IV): 750 mg–1.5 g q8–12h increased AST, ALT
I: 750 mg, 1.5 g C (PO): 10–15 mg/kg q12h
(IM/IV): 50–150 mg/kg/day
divided q8h
 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 Availability Dosage Range Side Effects
Ciprofloxacin T: 100 mg, 250 mg, 500 mg, 750 mg A (PO): 250–750 mg q12h; Dizziness, headaches, anxiety, drowsiness,
(Cipro) 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)
Gemifloxacin (Factive) T: 320 mg A: 320 mg once daily Headache, dizziness, rash, diarrhea, nausea
Levofloxacin (Levaquin) 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
Moxifloxacin (Avelox) T: 400 mg A: 400 mg/day Headache, dizziness, insomnia, nausea, diarrhea
I: 400 mg
Norfloxacin (Noroxin) T: 400 mg A: 400 mg q12h Same as ciprofloxacin
Ofloxacin T: 200 mg, 300 mg, 400 mg A: 200–400 mg q12h Dizziness, headache, insomnia, abdominal
cramps, diarrhea, nausea
A, Adults; I, injection; OS, oral solution; PO, oral; S, suspension; T, tablets.

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
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Antibiotic: Penicillins
USES ACTION

Antibiotic: Penicillins
Penicillins (also referred to as beta-lactam antibiotics) Penicillinase-resistant penicillins are effective Penicillins inhibit cell wall synthesis or activate enzymes,
may be used to treat a large number of infections, includ- against penicillinase-producing Staphylococcus au- which disrupt the bacterial cell wall, causing cell lysis and
ing pneumonia and other respiratory diseases, urinary reus but are less effective against gram-positive cocci cell death. May be bacteriostatic or bactericidal. Most
tract infections, septicemia, meningitis, intra-abdominal than the natural penicillins. effective against bacteria undergoing active growth and
infections, gonorrhea and syphilis, bone/joint infection. Broad-spectrum penicillins are effective against division.
gram-positive cocci and some gram-negative bacteria
Penicillins are classified based on an antimicrobial
(e.g., Haemophilus influenzae, Escherichia coli, Pro-
spectrum:
teus mirabilis, Salmonella, and Shigella).
Natural penicillins are very active against gram-positive
Extended-spectrum penicillins are effective against
cocci but ineffective against most strains of Staphylococ-
gram-negative organisms, including Pseudomonas ae-
cus aureus (inactivated by enzyme penicillinase).
ruginosa, Enterobacter, Proteus spp., Klebsiella, Ser-
ratia spp., and Acinetobacter spp.

ANTIBIOTIC: PENICILLINS
Name Availability Dosage Range Side Effects
Natural
Penicillin G benzathine I: 600,000 units, 1.2 million units, A: 1.2–2.4 million units as Mild diarrhea, nausea, vomiting,
(Bicillin, Bicillin LA) 2.4 million units 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 I: 1, 2, 3, 5 million-unit vials A: 2–4 million units q4h Rash, injection site reaction, phlebitis

(Pfizerpen) C: 100,000–250,000 units/kg/
day divided q4–6h
Penicillin V potassium T: 250 mg, 500 mg A: 250–500 mg q6–8h Diarrhea, nausea, vomiting
(Apo-Pen-VK) S: 125 mg/5 ml, 250 mg/5 ml C: 25–50 mg/kg/day in
divided doses q6–8h
Penicillinase-Resistant
Dicloxacillin C: 125 mg, 250 mg, 500 mg A: 125–500 mg q6h Abdominal pain, diarrhea, nausea
(Dynapen, Pathocil) S: 62.5 mg/5 ml C: 25–50 mg/kg/day divided
q6h
Nafcillin (Unipen) I: 500 mg, 1 g, 2 g 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
Oxacillin (Bactocill) C: 250 mg, 500 mg A (IV): 1–2 g q4–6h Diarrhea, nausea, vomiting
S: 250 mg/5 ml C (IV): 25–50 mg/kg q6h Increased risk of hepatotoxicity,
I: 250 mg, 500 mg, 1 g, 2 g interstitial nephritis

Antibiotic: Penicillins
Broad-Spectrum
Amoxicillin (Amoxil, Trimox) T: 125 mg, 250 mg, 500 mg, 875 mg A: 250–500 mg q8h or Diarrhea, colitis, nausea
C: 250 mg, 500 mg 500–875 g q12h
S: 50 mg/ml, 125 mg/5 ml, 250 mg/5 ml C: 20–90 mg/kg/day divided
q8–12h
Amoxicillin/clavulanate T: 250 mg, 500 mg, 875 mg A: 875 mg q12h or Diarrhea, rash, nausea, vomiting
(Augmentin) T (chewable): 125 mg, 200 mg, 250–500 mg q8h
250 mg, 400 mg C: 25–90 mg/kg/day divided
S: 125 mg/5 ml, 200 mg/5 ml, q12h
250 mg/5 ml, 400 mg/5 ml

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.