Indications
Treatment of the following infections caused by susceptible
organisms: Respiratory tract infections, Skin and
skin structure infections, Bone and joint infections (not
cefaclor or cefprozil), Urinary tract infections (not cefprozil).
Cefotetan and cefoxitin: Intra-abdominal
and gynecologic infections. Cefuroxime: Meningitis,
gynecologic infections, and Lyme disease. Cefaclor,
cefprozil, cefuroxime: Otitis media. Cefoxitin and
cefuroxime: Septicemia. Cefotetan, cefoxitin, cefuroxime:
Perioperative prophylaxis.
Action
Bind to bacterial cell wall membrane, causing cell
death. Therapeutic Effects: Bactericidal action
against susceptible bacteria. Spectrum: Similar to
that of first-generation cephalosporins but haveqactivity
against several other gram-negative pathogens including:
Haemophilus influenzae, Escherichia coli,
Klebsiella pneumoniae, Morganella morganii, Neisseria
gonorrhoeae (including penicillinase-producing
strains), Proteus, Providencia, Serratia marcescens,
Moraxella catarrhalis. Not active against methicillinresistant
staphylococci or enterococci. Cefuroxime:
Active against Borrelia burgdorferi. Cefotetan and
cefoxitin: Active against Bacteroides fragilis.
Pharmacokinetics
Absorption: Cefotetan, cefoxitin, and cefuroxime—
well absorbed following IM administration. Cefaclor,
cefprozil, and cefuroxime—well absorbed following
oral administration.
Distribution: Widely distributed. Penetration into
CSF is poor, but adequate for cefuroxime (IV) to be
used in treating meningitis. All cross the placenta and
enter breast milk in low concentrations.
Metabolism and Excretion: Excreted primarily
unchanged by the kidneys.
Half-life: Cefaclor—30–60 min; cefotetan—3–
4.6 hr; cefoxitin—40–60 min; cefprozil—90 min;
cefuroxime—60–120 min (all areqin renal impairment).
TIME/ACTION PROFILE
ROUTE ONSET PEAK DURATION
Cefaclor PO rapid 30–60 min 6–12 hr
Cefaclor POCD
unknown unknown 12 hr
Cefotetan IM rapid 1–3 hr 12 hr
Cefotetan IV rapid end of infusion
12 hr
Cefoxitin IM rapid 30 min 4–8 hr
Cefoxitin IV rapid end of infusion
4–8 hr
Cefprozil PO unknown 1–2 hr 12–24 hr
Cefuroxime
PO
unknown 2–3 hr 8–12 hr
Cefuroxime
IM
rapid 15–60 min 6–12 hr
Cefuroxime IV rapid end of infusion
6–12 hr
Contraindications/Precautions
Contraindicated in: Hypersensitivity to cephalosporins;
Serious hypersensitivity to penicillins.
Use Cautiously in: Renal impairment (pdose/q
dosing interval recommended for: cefotetan if CCr 30
mL/min, cefoxitin if CCr 50 mL/min, cefprozil if CCr
30 mL/min, cefuroxime if CCr 30 mL/min); Patients
with hepatic dysfunction, poor nutritional state, or cancer
may be atqrisk for bleeding; History of GI disease,
especially colitis; Cefprozil (oral suspension) contains
aspartame and should be avoided in patients with phenylketonuria;
Geri: Dose adjustment due to age-related
pin renal function may be necessary; may also be atq
risk for bleeding with cefotetan or cefoxitin; OB, Lactation:
Have been used safely.
Adverse Reactions/Side Effects
CNS: SEIZURES (high doses). GI: CLOSTRIDIUM DIFFICILE-
ASSOCIATED DIARRHEA (CDAD), diarrhea, cramps,
nausea, vomiting. Derm: rashes, urticaria. Hemat:
agranulocytosis, bleeding (qwith cefotetan and cefoxitin),
eosinophilia, hemolytic anemia, neutropenia,
thrombocytopenia. Local: pain at IM site, phlebitis at
IV site. Misc: allergic reactions including ANAPHYLAXIS
and SERUM SICKNESS, superinfection.
Interactions
Drug-Drug: Probenecidpexcretion andqblood
levels. If alcohol is ingested within 48–72 hr of cefotetan,
a disulfiram-like reaction may occur. Cefotetan
mayqrisk of bleeding with anticoagulants, antiplatelet
agents, thrombolytics, and NSAIDs. Antacidspabsorption
of cefaclor. Concurrent use of aminoglycosides
or loop diuretics mayqrisk of
nephrotoxicity.
Route/Dosage
Cefaclor
PO (Adults): 250–500 mg every 8 hr or 375–500 mg
every 12 hr as extended-release tablets.
PO (Children 1 mo): 6.7–13.4 mg/kg every 8 hr or
10–20 mg/kg every 12 hr (up to 1 g/day).
Cefotetan
IM, IV (Adults): Most infections—1–2 g every 12
hr. Severe/life-threatening infections—2–3 g every
12 hr. Urinary tract infections—500 mg–2 g every
12 hr or 1–2 g every 24 hr. Perioperative prophylaxis—
1–2 g 30–60 min before initial incision (onetime
dose).
Renal Impairment
IM, IV (Adults): CCr 10–30 mL/min—Usual adult
dose every 24 hr or 1⁄2 usual adult dose every 12 hr;
CCr 10 mL/min—Usual adult dose every 48 hr or 1⁄4
usual adult dose every 12 hr.
Cefoxitin
IM, IV (Adults): Most infections—1 g every 6–8 hr.
Severe infections—1 g every 4 hr or 2 g every 6–8
hr. Life-threatening infections—2 g every 4 hr or 3 g
every 6 hr. Perioperative prophylaxis—2 g 30–60
min before initial incision, then 2 g every 6 hr for up to
24 hr.
IM, IV (Children and Infants 3 mo): Most infections—
13.3–26.7 mg/kg every 4 hr or 20–40 mg/kg
every 6 hr. Perioperative prophylaxis—30–40 mg/
kg within 60 min of initial incision, then 30–40 mg/kg
every 6 hr for up to 24 hr.
Renal Impairment
IM, IV (Adults): CCr 30–50 mL/min—1–2 g every
8–12 hr; CCr 10–29 mL/min—1–2 g every 12–24
hr; CCr 5–9 mL/min—0.5–1 g every 12–24 hr; CCr
5 mL/min—0.5–1 g every 24–48 hr.
Cefprozil
PO (Adults): Most infections—250–500 mg every
12 hr or 500 mg every 24 hr.
PO (Children 6 mo–12 yr): Otitis media—15 mg/
kg every 12 hr. Acute sinusitis—7.5–15 mg/kg every
12 hr (higher dose should be used for moderate-to-severe
infections).
PO (Children 2–12 yr): Pharyngitis/tonsillitis—
7.5 mg/kg every 12 hr. Skin/skin structure infections—
20 mg/kg every 24 hr.
Renal Impairment
PO (Adults and Children 6 mo): CCr 30 mL/
min—1⁄2 of usual dose at normal dosing interval.
Cefuroxime
PO (Adults and Children 12 yr): Pharyngitis/tonsillitis,
maxillary sinusitis, uncomplicated UTIs—
250 mg every 12 hr. Bronchitis, uncomplicated skin/
skin structure infections—250–500 mg every 12 hr.
Gonorrhea—1 g (single dose). Lyme disease—500
mg every 12 hr for 20 days.
PO (Children 3 mo–12 yr): Otitis media, acute
bacterial maxillary sinusitis, impetigo—250 mg
every 12 hr.
IM, IV (Adults): Uncomplicated urinary tract infections,
skin/skin structure infections, disseminated
gonococcal infections, uncomplicated pneumonia—
750 mg every 8 hr. Bone/joint infections, severe
or complicated infections—1.5 g every 8 hr.
Life-threatening infections—1.5 g every 6 hr. Meningitis—
3 g every 8 hr. Perioperative prophylaxis—
1.5 g IV 30–60 min before initial incision; 750 mg IM/
IV every 8 hr can be given when procedure prolonged.
Prophylaxis during open-heart surgery—1.5 g IV at
induction of anesthesia and then every 12 hr for 3 additional
doses. Gonorrhea—1.5 g IM (750 mg in two
sites) with 1 g probenecid PO.
IM, IV (Children and Infants 3 mo): Most infections—
12.5–25 mg/kg every 6 hr or 16.7–33.3 mg/
kg every 8 hr (max dose6 g/day). Bone and joint
infections—50 mg/kg every 8 hr (max dose6 g/
day). Bacterial meningitis—50–60 mg/kg every 6 hr
or 66.7–80 mg/kg every 8 hr.
Renal Impairment
IM, IV (Adults): CCr 10–29 mL/min—Give standard
dose every 24 hr; CCr 10 mL/min (no hemodialysis)—
Give standard dose every 48 hr; Hemodialysis—
Give an additional dose at end of each dialysis
session.
Availability
Cefaclor (generic available)
Capsules: 250 mg, 500 mg. Extended-release tablets:
375 mg, 500 mg. Oral suspension (strawberry):
125 mg/5 mL, 187 mg/5 mL, 250 mg/5 mL,
375 mg/5 mL.
Cefotetan (generic available)
Powder for injection: 1 g/vial, 2 g/vial, 10 g/vial.
Premixed containers: 1 g/50 mL, 2 g/50 mL.
Cefoxitin (generic available)
Powder for injection: 1 g/vial, 2 g/vial, 10 g/vial.
Premixed containers: 1 g/50 mL D5W, 2 g/50 mL
D5W.
Cefprozil (generic available)
Tablets: 250 mg, 500 mg. Oral suspension (bubblegum
flavor): 125 mg/5 mL, 250 mg/5 mL.
Cefuroxime (generic available)
Tablets: 250 mg, 500 mg. Powder for injection: 750
mg/vial, 1.5 g/vial, 7.5 g/vial. Premixed containers:
750 mg/50 mL, 1.5 g/50 mL.
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