‍Ceftriaxone 500mg 

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Vial 500mg

Ceftriaxone

Description

Ceftriaxone is a broad spectrum β – lactam antibiotic of third generation cephalosporin.

Clinical pharmacology

Ceftriaxone kills bacteria by interfering in the synthesis of the bacterial cell wall. Ceftriaxone binds with high affinity to penicillin binding proteins (PBP) in bacterial cytoplasmic membrane and by acylation of membrane-bound transpeptidase enzymes, prevent cross-linkage of peptidoglycan chains, which is necessary for bacterial cell wall strength and rigidity.

Also cell division and growth are inhibited and elongation of susceptible bacteria and lysis frequently occur. Rapidly dividing bacteria are those most susceptible to the action of Ceftriaxone .

Antibacterial activity

Ceftriaxone has a high degree of stability in the presence of beta-lactamases, both penicillinases and cephalosporinases, of gram-negative and gram-positive bacteria. , Aerobic gram-negative bacteria:acinetobacter calcoaceticus, enterobacter aerogenes, entrobacter cloacae,E.coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella oxytoca, klebsiella pneumoniae, moraxella catarrhalis, morganella morganii , neissera gonorrhoea, neisseria meningitidis, proteus mirabilis, proteus vulgaris, serratia marcscens

Aerobic gram-positive microorincluding penicillinase-producing strains of N.gonorrhoeae and most enterobacteriaceae (Citrobacter, E.coli Enterobacter, Klebsiella, Morganella, Proteus, Providencia, and Serratia species). Ceftriaxone is not as active against gram-positive cocci as are the first and second generation cephalosporins.

Pharmacokinetics

Oral absorption -----

Presystemic metabolism -----

Plasma half – life Range 6-9 h

Volume of distribution 0.15 l.kg ^-1

Plasma protein binding 95%

Indication

-1Lower respiratory tract infections.

-2Acute bacterial otitis media.

-3Skin and skin structure infections.

-4Urinary tract infections.

-5Uncomplicated gonorrhea(cervical/urethral and rectal)

-6Pelvic inflammatory disease (PID).

-7Bacteremia, septicemia.

-8Bacterial meningitis.

-9Bone and joint infections

-10Intra-abdominal infections

-11Prevention of postoperative infections.

Contraindication

Ceftriaxone is contraindicated in patients with known allergy to the cephalosporin class of antibiotics.

Precaution

· Before Ceftriaxone administration, previous hypersensitivity reactions to cephalosporins or penicillins must be determined because of cross hypersensitivity among β-lactams.

· Ceftriaxone should be used with caution when administered to hyperbilirubinemic neonates, specially premature neonates.

· Patients with impaired hepatic function do not generally require a reduction in dose. However, in patients with both impaired hepatic & renal function, the daily dose should not exceed 2 grams.

· Long-term therapy with Ceftriaxone may allow for the overgrowth of Candida albicans, resulting in oral candidiasis.

· Risk – benefit should be considered when history of bleeding disorders, gastrointestinal diseases, specially ulcerative colitis, regional enteritis, or antibiotic associated colitis exist. (Ceftriaxone may cause pseudomembranous colitis).

· Preoperative (preoperative, intraoperative, and post operative) prophylactic administration of Ceftriaxone usually should be discontinued within 24 hours following surgery.

Pregnancy

Pregnancy category B.

There are no adequate and well controlled studies in pregnant women. Therefore Ceftriaxone should be used during pregnancy only if clearly needed.

Breast feeding

Ceftriaxone is excreted in human milk in low concentrations. Caution should be exercised when it is administered to a nursing woman.

Dosage

The dosing and strengths of the dosage form available are expressed in terms of Ceftriaxone base. (Not the sodium salt).

Usual adult dose

· Uncomplicated gonorrhea, Intramuscular, 250 mg (base) as a single dose.

· Preoperative prophylaxis: Intravenous, 1 gram (base) one – half to two hours prior to the start of surgery.

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