Mechanism of Action
Ceftriaxone is a bactericidal agent that acts by inhibition of bacterial cell wall synthesis. Ceftriaxone has activity in the presence of some beta-lactamases, both penicillinases and cephalosporinases, of Gram-negative and Gram-positive bacteria.
Sulbactam is an irreversible inhibitor of β-lactamase; it binds to the enzyme and does not allow it to degrade the antibiotic.
Brands of Ceftriaxone / Sulbactam in Kenya
Bactisul®, Zawadi Healthcare Ltd
Cebactum®, Leben Laboratories Pvt Ltd
Ceftafair-SB® , Mankind Pharma Ltd
Lasoxone-S®, Laso Healthcare Pvt. Ltd.
Marcef-S®, Marksans Pharma Limited
Onecef-SB®, Zawadi Healthcare Ltd
Sefixi®, Sakar Healthcare Ltd.
Sulbactomax®, Venus Remedies Limited
Trixon-S®, Lincoln Pharmaceuticals Ltd
Lower Respiratory Tract Infections: caused by Streptococcus pneumoniae, Staphylococcus aureus, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Escherichia coli, Enterobacter aerogenes, Proteus mirabilis or Serratia marcescens.
Acute bacterial otitis media: caused by Streptococcus pneumoniae, Haemophilus influenzae (including beta-lactamase producing strains) or Moraxella catarrhalis (including beta-lactamase producing strains).
Skin and skin structure infections: caused by Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pyogenes, Viridans group streptococci, Escherichia coli, Enterobacter cloacae, Klebsiella oxytoca, Klebsiella pneumoniae, Proteus mirabilis, Morganella morganii,* Pseudomonas aeruginosa, Serratia marcescens, Acinetobacter calcoaceticus, Bacteroides fragilis* or Peptostreptococcus species.
Urinary tract infections (complicated and uncomplicated) caused by Escherichia coli, Proteus mirabilis, Proteus vulgaris, Morganella morganii or Klebsiella pneumoniae.
Uncomplicated gonorrhea (cervical/urethral and rectal) caused by Neisseria gonorrhoeae, including both penicillinase- and nonpenicillinase-producing strains, and pharyngeal gonorrhea caused by nonpenicillinase-producing strains of Neisseria gonorrhoeae.
Pelvic inflammatory disease: caused by Neisseria gonorrhoeae. Ceftriaxone for Injection, USP, like other cephalosporins, has no activity against Chlamydia trachomatis. Therefore, when cephalosporins are used in the treatment of patients with pelvic inflammatory disease and Chlamydia trachomatis is one of the suspected pathogens, appropriate antichlamydial coverage should be added.
Bacterial septicemia :caused by Staphylococcus aureus, Streptococcus pneumoniae, Escherichia coli, Haemophilus influenzae or Klebsiella pneumoniae.
Bone and joint infections caused by Staphylococcus aureus, Streptococcus pneumoniae, Escherichia coli, Proteus mirabilis, Klebsiella pneumoniae or Enterobacter species.
Intra-abdominal infections: caused by Escherichia coli, Klebsiella pneumoniae, Bacteroides fragilis, Clostridium species (Note: most strains of Clostridium difficile are resistant) or Peptostreptococcus species.
Meningitis caused by Haemophilus influenzae, Neisseria meningitidis or Streptococcus pneumoniae. Ceftriaxone has also been used successfully in a limited number of cases of meningitis and shunt infection caused by Staphylococcus epidermidis and Escherichia coli.
Surgical prophylaxis: The preoperative administration of a single 1 g dose of Ceftriaxone may reduce the incidence of postoperative infections in patients undergoing surgical procedures classified as contaminated or potentially contaminated (e.g., vaginal or abdominal hysterectomy or cholecystectomy for chronic calculous cholecystitis in high-risk patients, such as those over 70 years of age, with acute cholecystitis not requiring therapeutic antimicrobials, obstructive jaundice or common duct bile stones) and in surgical patients for whom infection at the operative site would present serious risk (e.g., during coronary artery bypass surgery). Although Ceftriaxone has been shown to have been as effective as cefazolin in the prevention of infection following coronary artery bypass surgery, no placebo-controlled trials have been conducted to evaluate any cephalosporin antibiotic in the prevention of infection following coronary artery bypass surgery.
Ceftriaxone is contraindicated in patients with known hypersensitivity to ceftriaxone, any of its excipients or to any other cephalosporin. Patients with previous hypersensitivity reactions to penicillin and other beta lactam antibacterial agents may be at greater risk of hypersensitivity to ceftriaxone
Premature neonates: Ceftriaxone is contraindicated in premature neonates up to a postmenstrual age of 41 weeks (gestational age + chronological age).
Hyperbilirubinemic neonates: Hyperbilirubinemic neonates should not be treated with ceftriaxone. Ceftriaxone can displace bilirubin from its binding to serum albumin, leading to a risk of bilirubin encephalopathy in these patients.
Neonates Requiring Calcium Containing IV Solutions
Ceftriaxone is contraindicated in neonates (≤ 28 days) if they require (or are expected to require) treatment with calcium-containing IV solutions, including continuous calcium-containing infusions such as parenteral nutrition because of the risk of precipitation of ceftriaxone-calcium
Intravenous administration of ceftriaxone solutions containing lidocaine is contraindicated. When lidocaine solution is used as a solvent with ceftriaxone for intramuscular injection, exclude all contraindications to lidocaine. Refer to the prescribing information of lidocaine.
ADVERSE DRUG REACTIONS
Gastrointestinal – pancreatitis, stomatitis and glossitis.
Genitourinary – oliguria, ureteric obstruction, post-renal acute renal failure.
Dermatologic – exanthema, allergic dermatitis, urticaria, edema; acute generalized exanthematous pustulosis (agep) and isolated cases of severe cutaneous adverse reactions (erythema multiforme, stevens-johnson syndrome or lyell’s syndrome/toxic epidermal necrolysis) have been reported.
Hematological changes: isolated cases of agranulocytosis (< 500/mm3) have been reported, most of them after 10 days of treatment and following total doses of 20 g or more.
Nervous system disorders: convulsion
Other, adverse reactions: symptomatic precipitation of ceftriaxone calcium salt in the gallbladder, kernicterus, oliguria, and anaphylactic or anaphylactoid reactions.
- Ceftriaxone will increase the level or effect of argatroban by anticoagulation.
ceftriaxone decreases effects of BCG vaccine live by pharmacodynamic antagonism. Contraindicated. Wait until Abx Tx complete to administer the live bacterial vaccine.
- Do not use ANY calcium-containing solutions (including Ringer or Harmann solutions) in combination with IV ceftriaxone; risk of potentially fatal particulate precipitation in lungs, kidneys. Separate by at least 48 hrs.
- Ceftriaxone will increase the level or effect of bivalirudin by anticoagulation. Avoid or Use Alternate Drug. cephalosporins may decrease prothrombin activity
- Ceftriaxone decreases effects of BCG vaccine live by pharmacodynamic antagonism.
- Ceftriaxone increases effects of dalteparin by anticoagulation. Avoid or Use Alternate Drug. Cephalosporins may decrease prothrombin activity.
- Ceftriaxone increases effects of enoxaparin by anticoagulation. Avoid or Use Alternate Drug. cephalosporins may decrease prothrombin activity.
- Ceftriaxone will decrease the level or effect of bazedoxifene/conjugated estrogens by altering intestinal flora.
- Chloramphenicol decreases effects of ceftriaxone by pharmacodynamic antagonism.
- Tetracyclines (Doxycycline, Minocycline, Tigecycline, Demeclocycline, Tetracycline) decreases effects of ceftriaxone by pharmacodynamic antagonism.
- Ceftriaxone increases toxicity of furosemide by pharmacodynamic synergism.
Clinical | Pharmacokinetic data
Routes of Administration:
Onset of Action:
Elimination Half life:
Legal Status | Dosage forms & Strengths
Narcotic Drugs and Psychotropic Substances (Control ) Act Schedule:
Dosage Forms | Strengths:
- Ceftriaxone / Sulbactum