Ceftriaxone

Ceftriaxone is an antibiotic useful for the treatment of a number of bacterial infections. This includes middle ear infections, endocarditis, meningitis, pneumonia, bone and joint infections, intra-abdominal infections, skin infections, urinary tract infections, gonorrhea, and pelvic inflammatory disease. It is also sometimes used before surgery and following a bite wound to try to prevent infection.

Molecular Structure

Ceftriaxone

Class of Drug

Cephalosporin, third generation

Mechanism of Action

Binds to penicillin-binding proteins and disrupts or inhibits bacterial cell wall synthesis.

Susceptible organisms in vivo: Gram positive: excellent against streptococci and Streptococcus pneumoniae. Does not cover staphylococci and Enterococcus.
Gram negative: excellent against Neisseria meningitidis, Neisseria gonorrhoeae, Escherichia coli, Proteus mirabilis, Klebsiella pneumoniae, Morganella

Indications / Dosage / Route

Routes of Administration: IV or IM

Condition: General infections

Dose: Adults: IV, IM 1-2 g/d q24h. Maximum: 4 g/d.

Children: other than meningitis: IV, IM 50-75 mg/d in divided doses. Maximum: 2 g/d.

Condition: Meningitis

Dose: Adults: IV, IM 2 g/d q12h (or 1 g/d q12h).

Children: : IV, IM 100 mg/kg/d, once daily or 2 doses/d. Maximum: 4 g/d. Usual duration of therapy: 7-14 days.

Condition: Serious miscellaneous infections other than meningitis including skin and skin structure infections

DoseChildren IV, IM 50-75 mg/kg/d, divided doses q12h. Maximum: 2 g/d.

Condition: Acute otitis media (bacterial)

Dose: Adults IM 250 mg as single dose

Children : IM 50 mg/kg as single dose. Maximum: 1 g. Uncomplicated gonorrhea.

Adjustment of Dosage

None.

Food and Drug Interactions

Food: Not applicable.

Pregnancy: Category B.

Lactation: Appears in breast milk. American Academy of Pediatrics considers cephalosporins to be compatible with breastfeeding.

Contraindications: Hypersensitivity to other cephalosporins or related antibiotics, eg, penicillin.

Warnings / Precautions

> Use with caution in patients with the following conditions: kidney disease, penicillin allergy, elderly.

> Avoid in orthotopic liver transplant because of the risk of biliary sludge formation.

> It is recommended to continue therapy for at least 2-3 days after symptoms are no longer present. For group A beta-hemolytic streptococcal infections, therapy should be continued for 10 days.

> Before use, determine if patient had previous hypersensitivity reaction to cephalosporins or penicillins. Incidence of cross-sensitivity to penicillins is 1-16%. A negative response to penicillin does not preclude allergic reaction to a cephalosporin.

> Watch bilirubin levels if the use is prolonged.

Clinically Important Drug Interactions

> Drug that increases effects/toxicity of ceftriaxone: probenecid.

> Ceftriaxone increases effects/toxicity of following drugs: aminoglycosides, loop diuretics.

Adverse Reactions

> Common: None.

> Serious: hepatitis, hypersensitivity reactions, pseudomembra-nous colitis, nephrotoxicity, bone marrow suppression, hemolytic anemia.

Parameters to Monitor

> CBC with differential and platelets, serum BUN and creatinine, liver enzymes.

> Temperature for sign of drug-induced persistent fever.

> Signs and symptoms of antibiotic-induced bacterial or fungal superinfection.

> Signs and symptoms of renal toxicity.

> Signs and symptoms of fluid retention, particularly in patients receiving sodium salts of cephalosporins.

Advice to Patient

None.

Further Useful Info

> Uses for ceftriaxone are as follows: Acute bacterial meningitis: effective against Neisseria meningitidis, Hemophilus influenzae, and, most importantly, Streptococcus pneumoniae even when not susceptible to penicillin. It does not cover Listeria. Community-acquired pneumonia: effective against all important pathogens other than atypical organisms for which a macrolide or a quinolone is added (Legionella, Mycloplasma, Chlamydia). Nosocomial infection, eg, pneumonia; not recommended as monotherapy because of resistance from Pseudomonas aeruginosa and ESBL-producing Enterobacteriaceae.

> A great advantage of ceftriaxone is once-a-day use (other than in meningitis). It is therefore often used for home IV infusion.

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