cefotaxime

REMS

Treatment of the following infections caused by susceptible organisms:
- Skin and skin structure infections,
- Bone and joint infections,
- Urinary tract infections,
- Gynecological infections including gonorrhea,
- Lower respiratory tract infections,
- Intra-abdominal infections,
- Septicemia,
- Meningitis,
- Lyme disease.
Perioperative prophylaxis.

Action ⬆ ⬇

Binds to the bacterial cell wall membrane, causing cell death.

Therapeutic effects:

Bactericidal action against susceptible bacteria.

Spectrum:

Similar to that of second-generation cephalosporins, but activity against staphylococci is less, whereas activity against gram-negative pathogens is greater, even for organisms resistant to first- and second-generation agents.
Notable is increased action against:
- Acinetobacter,
- Citrobacter,
- Enterobacter,
- Haemophilus influenzae(including β-lactamase-producing strains),
- Haemophilus parainfluenzae,
- Escherichia coli,
- Klebsiella pneumoniae,
- Morganella morganii,
- Neisseria gonorrhoeae and meningitidis,
- Proteus,
- Providencia,
- Serratia,
- Moraxella catarrhalis,
- Borrelia burgdorferi.
Has some activity against anaerobes, includingBacteroides fragilis.
Not active against methicillin-resistant staphylococci.

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed following IM administration; IV administration results in complete bioavailability.

Distribution: Widely distributed. Crosses the placenta; enters breast milk in low concentrations. CSF penetration better than with first- and second-generation agents.

Metabolism/Excretion: Partly metabolized to active metabolite; 20–36% excreted unchanged in the urine.

Half-Life: Premature neonates: 5–6 hr; Full–term neonates: 2–3.4 hr; Children: 1.5 hr; Adults: 1–1.5 hr (↑ in renal impairment).

Time/Action Profile ⬆ ⬇

(blood levels)

ROUTE	ONSET	PEAK	DURATION
IM	rapid	0.5 hr	4–12 hr
IV	rapid	end of infusion	4–12 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity to cephalosporins;
Serious hypersensitivity to penicillins.

Use Cautiously in:

Renal impairment (↓ dose recommended if CCr <20 mL/min);
History of GI disease, especially colitis;
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Geri: Dosage adjustment may be necessary due to age-related in renal function.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: pruritus, rash, urticaria

GI: CLOSTRIDIOIDES DIFFICILE-ASSOCIATED DIARRHEA (CDAD), diarrhea, nausea, vomiting

Hemat: agranulocytosis, bleeding, eosinophilia, hemolytic anemia, neutropenia, thrombocytopenia

Local: pain at IM site, phlebitis at IV site

Neuro: SEIZURES (HIGH DOSES)

Misc: ANAPHYLAXISALLERGIC REACTIONS INCLUDING , superinfection

Interactions ⬆ ⬇

Drug-drug:

Probenecid↓ excretion and increases serum levels.
Concurrent use of aminoglycosides, NSAIDs, or loop diuretics may ↑ risk of nephrotoxicity.

Route/Dosage ⬆ ⬇

IM IV (Adults and Children >12 yr): Most uncomplicated infections: 1 g every 12 hr; Moderate or severe infections: 1–2 g every 6–8 hr; Life-threatening infections: 2 g every 4 hr (maximum dose: 12 g/day); Gonococcal urethritis/cervicitis or rectal gonorrhea in females: 500 mg IM (single dose); Rectal gonorrhea in males: 1 g IM (single dose); Perioperative prophylaxis: 1 g 30–90 min before initial incision (one-time dose).
IM IV (Children 1 mo-12 yr): <50 kg : 100–200 mg/kg/day divided every 6–8 hr; Meningitis: 200 mg/kg/day divided every 6 hr;Invasive pneumococcal meningitis–225–300 mg/kg/day divided every 6–8 hr;≥ 50 kg: see adult dosing.
IV (Neonates 1–4 wk): 50 mg/kg every 6–8 hr.
IV (Neonates ≤1 wk): 50 mg/kg every 8–12 hr.

Renal Impairment

IM IV (Adults ): CCr <20 mL/min: ↓dose by 50%.

Availability ⬆ ⬇

(Generic available)

Lyophilized powder for injection: 500 mg; 1 g; 2 g; 10 g

Assessment ⬆ ⬇

Assess patient for infection (vital signs; appearance of wound, sputum, urine, and stool; WBC) at beginning of and throughout therapy.
Before initiating therapy, obtain a history to determine previous use of and reactions to penicillins or cephalosporins. Persons with a negative history of penicillin sensitivity may still have an allergic response.
Obtain specimens for culture and sensitivity before initiating therapy. First dose may be given before receiving results.
Observe patient for signs and symptoms of anaphylaxis (rash, pruritus, laryngeal edema, wheezing). Discontinue the drug and notify health care professional immediately if these symptoms occur. Keep epinephrine, an antihistamine, and resuscitation equipment close by in the event of an anaphylactic reaction.
Monitor bowel function. Diarrhea, abdominal cramping, fever, and bloody stools should be reported to health care professional promptly as a sign of
Clostridioides difficile
-associated diarrhea (CDAD). May begin up to several wk following cessation of therapy.

Lab Test Considerations:

May cause positive results for Coombs' test.
- May cause ↑ serum AST, ALT, alkaline phosphatase, bilirubin, LDH, BUN, and serum creatinine.
- May rarely cause leukopenia, neutropenia, agranulocytosis, thrombocytopenia, and eosinophilia.

Implementation ⬆ ⬇

IM: Reconstitute IM doses with sterile or bacteriostatic water for injection.
- Inject deep into a well-developed muscle mass; massage well.
IV: Monitor injection site frequently for phlebitis (pain, redness, swelling). Change sites every 48–72 hr to prevent phlebitis.
- If aminoglycosides are administered concurrently, administer in separate sites, if possible, at least 1 hr apart. If second site is unavailable, flush lines between medications.

IV Administration:

Reconstitute with at least 10 mL of sterile water for injection. Do not use preparations containing benzyl alcohol for neonates.
Rate: Administer slowly over 3–5 min at a concentration of 100 mg/mL (maximum 150 mg/mL in fluid-restricted patients).
Intermittent Infusion: Diluent: Reconstituted solution may be further diluted in D5W, D10W, lactated Ringer's solution, D5/0.25% NaCl, D5/0.45% NaCl, D5/0.9% NaCl, or 0.9% NaCl.Concentration: 20–60 mg/mL. Solution may appear light yellow to amber. Solution is stable for 24 hr at room temperature and 5 days if refrigerated.
Rate: Administer over 20–30 min.

Patient/Family Teaching ⬆ ⬇

Advise patient to report signs of superinfection (furry overgrowth on the tongue, vaginal itching or discharge, loose or foul-smelling stools) and allergy.
Instruct patient to notify health care professional if fever and diarrhea develop, especially if stool contains blood, pus, or mucus. Advise patient not to treat diarrhea without consulting health care professional.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇