Yes

Antibiotic, Cephalosporin (First Generation)

Treatment of infections when caused by susceptible strains in respiratory, genitourinary, gastrointestinal, skin and soft tissue, bone and joint infections; septicemia; treatment of susceptible gram-positive bacilli and cocci (never enterococcus); some gram-negative bacilli including E. coli, Proteus, and Klebsiella may be susceptible

B

Hypersensitivity to cephalothin or cephalosporins

Modify dosage in patients with severe renal impairment, prolonged use may result in superinfection; use with caution in patients with a history of penicillin allergy, especially IgE-mediated reactions (eg, anaphylaxis, urticaria); may cause antibiotic-associated colitis or colitis secondary to C. difficile

1% to 10%: Gastrointestinal: Diarrhea, nausea, vomiting

<1%: Maculopapular and erythematous rash, dyspepsia, pseudomembranous colitis, bleeding, pain and induration at injection site

Other reactions with cephalosporins include anaphylaxis, erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome, dizziness, fever, headache, CNS irritability, seizures, decreased hemoglobin, neutropenia, leukopenia, agranulocytosis, pancytopenia, aplastic anemia, hemolytic anemia, interstitial nephritis, toxic nephropathy, vaginitis, angioedema, cholestasis, hemorrhage, prolonged PT, serum-sickness reactions, superinfection

Symptoms of overdose include neuromuscular hypersensitivity, convulsions especially with renal insufficiency; many beta-lactam antibiotics have the potential to cause neuromuscular hyperirritability or seizures

Hemodialysis may be helpful to aid in the removal of the drug from the blood, otherwise most treatment is supportive or symptom directed

Probenecid decreases renal clearance of cephalothin; aminoglycosides may increase risk of nephrotoxicity

Reconstituted solution is stable for 12-24 hours at room temperature and 96 hours when refrigerated; for I.V. infusion in NS or D₅W solution is stable for 24 hours at room temperature, 96 hours when refrigerated or 12 weeks when frozen; after freezing, thawed solution is stable for 24 hours at room temperature or 96 hours when refrigerated

Inhibits bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins (PBPs) which in turn inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls, thus inhibiting cell wall biosynthesis. Bacteria eventually lyse due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) while cell wall assembly is arrested.

Distribution: Does not penetrate the CSF unless the meninges are inflamed; crosses the placenta; small amounts appear in breast milk

Protein binding: 65% to 80%

Metabolism: Partially deacetylated in the liver and kidney

Half-life: 30-60 minutes

Time to peak serum concentration: I.M.: Within 30 minutes

Elimination: 50% to 75% of a dose appearing as unchanged drug in urine

I.M., I.V.:

Postnatal age <7 days:

<2000 g: 20 mg every 12 hours

>2000 g: 20 mg every 8 hours

Postnatal age >7 days:

<2000 g: 20 mg every 8 hours

>2000 g: 20 mg every 6 hours

Children: 75-125 mg/kg/day divided every 4-6 hours; maximum dose: 10 g in a 24-hour period

Adults: 500 mg to 2 g every 4-6 hours

Dosing interval in renal impairment:

Cl_cr 10-50 mL/minute: Administer every 6-8 hours

Cl_cr <10 mL/minute: Administer every 12 hours

Continuous arteriovenous or venovenous hemodiafiltration (CAVH) effects: Administer 1 g every 8 hours

Cephalothin can be administered IVP over 3-5 minutes at a maximum concentration of 100 mg/mL or I.V. intermittent infusion over 30-60 minutes at a final concentration for I.V. administration of less than or equal to 100 mg/mL

Observe for signs and symptoms of anaphylaxis during first dose

Positive direct Coombs', false-positive urinary glucose test using cupric sulfate (Benedict's solution, Clinitest®, Fehling's solution), false-positive serum or urine creatinine with Jaffé reaction, false-positive urinary proteins and steroids

May cause nervousness; case reports of euphoria, delusion, illusions, and depersonalization with cephalosporins

May rarely cause neutropenia; use caution with clozapine and carbamazepine

No information available to require special precautions

No effects or complications reported

Do not admix with aminoglycosides in same bottle/bag

Powder for injection, as sodium: 1 g, 2 g (50 mL)

Donowitz GR and Mandell GL, "Beta-Lactam Antibiotics," N Engl J Med, 1988, 318(7):419-26 and 318(8):490-500.

Pickering LK, O'Connor DM, Anderson D, et al, "Comparative Evaluation of Cefazolin and Cephalothin in Children," J Pediatr, 1974, 85(6):842-7.

Yasuhara H, Kobayashi S, Sakamoto K, et al, "Pharmacokinetics of Amikacin and Cephalothin in Bedridden Elderly Patients," J Clin Pharmacol, 1982, 22(8-9):403-9.