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Agent

Mechanism of Action

Dosage

Benefits

Side Effects

Notes

Nafcillin sodium or oxacillin sodium

Inhibition of cell-wall synthesis by attaching to penicillin-binding-protein targets

1.5-2.0 g iv, every 4-6 h for 4-6 wk

Active against methicillin-sensitiveS. aureus or coagulase-negative staphylococci

Neutropenia, interstitial nephritis, hepatitis, rash

Home use is difficult without a portable infusion pump due to frequent administration.

Used more commonly in patients with bacteremia and infective endocarditis

Cefazolin

Inhibition of cell-wall synthesis by attaching to penicillin-binding-protein targets

1-2 g iv, every 8 h for 4-6 wk

Active against methicillin-sensitiveS. aureus or coagulase-negative staphylococci, and β-hemolytic streptococci

Fever, rash, thrombophlebitis, diarrhea

Vancomycin

The bactericidal action of vancomycin results primarily from inhibition of cell-wall biosynthesis. In addition, vancomycin alters bacterial-cell-membrane permeability and RNA synthesis

15 mg/kg iv, every 12 h for 4-6 wk

Active against MRSA or coagulase-negative staphylococci

Ototoxicity, red man/neck syndrome, nausea, vomiting, neutropenia

Monitor drug concentration regularly.

Could be used as an alternative to cefazolin and nafcillin in patients with serious allergy to β-lactam

Linezolid

Linezolid binds to a site on the bacterial 23S ribosomal RNA of the 50S subunit and prevents the formation of a functional 70S initiation complex, which is an essential component of the bacterial translation process

600 mg po or iv, every 12 h for 6 wk

Active against vancomycin-resistant enterococci, vancomycin intermediate S. aureus

Diarrhea, headache, nausea, myelosuppression

High oral bioavailability.

Could be used as an alternative to vancomycin or β-lactam in drug intolerance, resistance, or treatment failure.

Patients receiving linezolid need to avoid consuming large amounts of foods or beverages with high tyramine content

Levofloxacin

Inhibition of bacterial topoisomerase IV and DNA gyrase, enzymes required for DNA replication, transcription, repair, and recombination

500 mg/d po or iv

Active against S. aureus and coagulase-negative staphylococci, and aerobic gram-negative bacilli

Nausea, vomiting, diarrhea, headache, QT prolongation

High oral bioavailability.

Could be used in hardware-associatedosteomyelitis as an alternative to β-lactam or vancomycin in association with rifampin

Rifampin

Rifampin inhibits DNA-dependent RNA polymerase activity in susceptible microorganisms

600-900 mg, bid or tid

Active against susceptible S. aureusand coagulase-negative staphylococci

Nausea, vomiting, heartburn, thrombocytopenia, abnormal liver function tests, drug-drug interaction

Rapid emergence of resistance when used as monotherapy.

Should always be used in association with quinolones in hardware-associatedosteomyelitis as an alternative to β-lactam or vancomycin

Aqueous crystalline penicillin G

Inhibition of cell-wall synthesis by attaching to penicillin-binding-protein targets

20 × 10⁶U/24h iv, either continuously or in six equally divided doses for 4-6 wk

Active against penicillin-susceptible streptococci, enterococci

Rash or urticaria, hypersensitivity reactions, pseudomembranous colitis

Could be used as a continuous infusion using a portable infusion pump in an ambulatory setting

Ceftriaxone

Inhibition of cell-wall synthesis by attaching to penicillin-binding-protein targets

1-2 g iv or im, every 24 h for 4-6 wk

Active against manyEnterobacteriaceae, β hemolytic streptococci

Rash, injection site pain, diarrhea, reversible gallbladder disease

Used once daily, convenient for outpatient therapy

Cefepime

Inhibition of cell-wall synthesis by attaching to penicillin-binding-protein targets

1-2 g iv, every 12 h for 4-6 wk

Active againstEnterobacteriaceae,P. aeruginosa orEnterobacter spp

Diarrhea, dyspepsia, headache, pseudomembranous colitis, phlebitis, transient elevation in liver function tests

Meropenem

Inhibition of cell-wall synthesis by attaching to penicillin-binding-protein targets

1g iv, every 8 h for 4-6 wk

Active againstEnterobacteriaceae,P. aeruginosa orEnterobacter spp

Diarrhea, nausea, vomiting

Expensive, broad-spectrum

* Recommendations are for adult, non-pregnant patients with normal renal function.

bid = twice daily; DNA = deoxyribonucleic acid; im = intramuscular; iv = intravenous; MRSA = methicillin-resistantStaphylococcus aureus; po = oral; RNA = ribonucleic acid; tid = three times daily.