Indications
Treatment of the following infections caused by susceptible
organisms: Uncomplicated skin and skin structure
infections, Bone and joint infections, Uncomplicated
and complicated urinary tract infections, Respiratory
tract infections, Complicated intra-abdominal infections
(with metronidazole), Septicemia. Empiric treatment of
febrile neutropenic patients.
Action
Binds to the bacterial cell wall membrane, causing cell
death. Therapeutic Effects: Bactericidal action
against susceptible bacteria. Spectrum: Similar to
that of second- and third-generation cephalosporins,
but activity against staphylococci is less, whereas activity
against gram-negative pathogens is greater, even for
organisms resistant to first-, second-, and third-generation
agents. Notable is increased action against: Enterobacter,
Haemophilus influenzae (including-lactamase-
producing strains), Escherichia coli, Klebsiella
pneumoniae, Neisseria, Proteus, Providencia, Pseudomonas
aeruginosa, Serratia, Moraxella catarrhalis(
including-lactamase-producing strains). Not
active against methicillin-resistant staphylococci or enterococci.
Pharmacokinetics
Absorption: Well absorbed after IM administration;
IV administration results in complete bioavailability.
Distribution: Widely distributed. Crosses the placenta;
enters breast milk in low concentrations. Some
CSF penetration.
Protein Binding: 20%.
Metabolism and Excretion: 85% excreted unchanged
in urine.
Half-life: Adults—2 hr (qin renal impairment);
Children 2 mo–6 yr—1.7–1.9 hr.
TIME/ACTION PROFILE
ROUTE ONSET PEAK DURATION
IM rapid 1–2 hr 12 hr
IV rapid end of infusion
12 hr
Contraindications/Precautions
Contraindicated in: Hypersensitivity to cephalosporins;
Serious hypersensitivity to penicillins.
Use Cautiously in: Renal impairment (pdosing/q
dosing interval recommended if CCr 60 mL/min); History
of GI disease, especially colitis; Patients with hepatic
dysfunction or poor nutritional status (may be at
qrisk of bleeding); Geriatric patients (dose adjustment
due to age-relatedpin renal function may be necessary);
OB, Lactation: Pregnancy and lactation (safety
not established).
Adverse Reactions/Side Effects
CNS: ENCEPHALOPATHY, SEIZURES (qrisk in renal impairment),
aphasia, headache. GI: CLOSTRIDIUM DIFFICILE-
ASSOCIATED DIARRHEA (CDAD), diarrhea, nausea,
vomiting. Derm: rashes, pruritis, urticaria. Hemat:
bleeding, eosinophilia, hemolytic anemia, neutropenia,
thrombocytopenia. Local: pain at IM site, phlebitis at
IV site. Misc: allergic reactions including ANAPHYLAXIS,
superinfection, fever.
Interactions
Drug-Drug: Probenecidpexcretion andqblood
levels. Concurrent use of loop diuretics or aminoglycosides
mayqrisk of nephrotoxicity.
Route/Dosage
IM (Adults): Mild-to-moderate uncomplicated or
complicated urinary tract infections due to Escherichia
coli—0.5–1 g every 12 hr.
IV (Adults): Moderate-to-severe pneumonia—1–2
g every 12 hr. Mild-to-moderate uncomplicated or
complicated urinary tract infections—0.5–1 g
every 12 hr. Severe uncomplicated or complicated
urinary tract infections, moderate-to-severe uncomplicated
skin and skin structure infections,
complicated intra-abdominal infections—2 g every
12 hr. Empiric treatment of febrile neutropenia—2
g every 8 hr.
IV (Children 1 mo–16 yr): Uncomplicated and
complicated urinary tract infections, uncomplicated
skin and skin structure infections, pneumonia—50
mg/kg every 12 hr (not to exceed 2 g/dose). Febrile
neutropenia—50 mg/kg every 8 hr (not to exceed 2
g/dose).
IV (Neonates postnatal age 14 days): 50 mg/kg
every 12 hr.
IV (Neonates postnatal age 14 days): 30 mg/kg
every 12 hr; consider 50 mg/kg every 12 hr for Pseudomonas
infections.
Renal Impairment
IM, IV (Adults): (See Manufacturer’s specific recommendations)
CCr 30–60 mL/min—0.5–1 g every 24
hr or 2 g every 12–24 hr; CCr 11–29 mL/min—0.5–
2 g every 24 hr; CCr 11 mL/min—250 mg–1 g
every 24 hr.
Availability (generic available)
Powder for injection: 500 mg, 1 g, 2 g. Premixed
containers: 1 g/50 mL D5W, 2 g/100 mL D5W.
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