Ceftriaxone

Uses

Ceftriaxone is used for the treatment of the following infections when caused by susceptible organisms:

Lower Respiratory Tract Infections caused by Streptococcus pneumoniae, Staphylococcus aureus, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, E. coli, Enterobacter aerogenes, Proteus mirabilis, Serratia marcescens.

Acute Bacterial Otitis Media caused by Streptococcus pneumoniae, Haemophilus influenzae (including beta-lactamase producing strains), Moraxella catarrhalis (including beta-lactamase producing strains).

Skin and Skin Structure Infections caused by Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pyogenes, Viridans group streptococci, E. coli, Enterobacter cloacae, Klebsiella oxytoca, Klebsiella pneumoniae, Proteus mirabilis, Morganella morganii, Pseudomonas aeruginosa, Serratia marcescens, Acinetobacter calcoaceticus, Bacteroides fragilis, Peptostreptococcus species.

Urinary Tract Infections (complicated and uncomplicated) caused by E. coli, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Klebsiella pneumoniae.

Uncomplicated Gonorrhea (cervical, urethral, pharyngial 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.

Bacterial Septicemia caused by Staphylococcus aureus, Streptococcus pneumoniae, E. coli, Haemophilus influenzae, Klebsiella pneumoniae.

Bone and Joint Infections caused by Staphylococcus aureus, Streptococcus pneumoniae, E. coli, Proteus mirabilis, Klebsiella pneumoniae, Enterobacter species.

Intra-abdominal Infections caused by E. coli, Klebsiella pneumoniae, Bacteroides fragilis, Clostridium species, Peptostreptococcus species.

Meningitis caused by Haemophilus influenzae, Neisseria meningitidis, Streptococcus pneumoniae. Ceftriaxone has also been used successfully in a limited number of cases of meningitis and shunt infection caused by Staphylococcus epidermidis and E. coli.

Surgical Prophylaxis: The preoperative administration of a single 1 gm dose of Ceftriaxone may reduce the incidence of postoperative infections in patients undergoing surgical procedures classified as contaminated or potentially contaminated.

Ceftriaxone is also used to associated treatment for these conditions: Arthritis gonococcal, Bacterial Endocarditis, Bacterial Infections, Bacterial Sepsis, Bacterial Sinusitis, Bone and Joint Infections, Brain abscess, Chancroid, Community Acquired Pneumonia (CAP), Conjunctivitis gonococcal neonatal, Epididymitis, Epiglottitis, Gonococcal infection of pharynx, Gonococcal pelvic inflammatory disease, Intra-Abdominal Infections, Lower respiratory tract infection bacterial, Lyme Neuroborreliosis, Meningitis, Bacterial, Ophthalmia neonatorum due to gonococcus, Postoperative Infections, Prosthetic Joint Infection, Salmonella Typhi Infection, Septic Arthritis, Shigellosis, Skin and Subcutaneous Tissue Bacterial Infections, Syphilis, Vulvovaginitis gonococcal, Whipple Disease, Bacterial otitis media, Complicated Bacterial Urinary Tract Infections, Susceptible Bacterial Infections, Uncomplicated Gonorrhea, Uncomplicated Urinary tract infection bacterial

How Ceftriaxone works

Ceftriaxone works by inhibiting the mucopeptide synthesis in the bacterial cell wall. The beta-lactam moiety of ceftriaxone binds to carboxypeptidases, endopeptidases, and transpeptidases in the bacterial cytoplasmic membrane. These enzymes are involved in cell-wall synthesis and cell division. Binding of ceftriaxone to these enzymes causes the enzyme to lose activity; therefore, the bacteria produce defective cell walls, causing cell death.

Dosage

Ceftriaxone dosage

Generally, Ceftriaxone should be taken once or equally devided twice a day for 4-14 days. Ceftriaxone therapy should be continued for at least 2 days after the sign and symptoms of infection have disappeared.

The usual duration of therapy is 4 to 14 days; in complicated infections longer therapy may be required. No dosage adjustment is required for patients with renal or hepatic impairment.

Use the solution immediately after reconstitution of powder.

Side Effects

Generally Ceftriaxone is well tolerated. However, few side effects including nausea, vomiting, diarrhea, dizziness and fever may occur.

Toxicity

Ceftriaxone overdose may increase the risk of urolithiasis and subsequent post-renal acute renal failure (PARF). Other symptoms of overdose unavailable in the literature. However, they are likely similar to the adverse effects of the medication. If overdose of ceftriaxone occurs, treat with symptomatic and supportive treatment, as ceftriaxone levels will not be reduced by dialysis.

Precaution

Ceftriaxone should be administered with caution to individuals with a history of gastrointestinal disease, particularly colitis.

Interaction

May increase nephrotoxicity of aminoglycosides. May diminish therapeutic effect of BCG, typhoid vaccine, Na picosulfate. May increase anticoagulant effect of vit K antagonists (e.g. warfarin). May increase serum level with probenecid.

Food Interaction

Ceftriaxone Drug Interaction

Moderate: furosemide, furosemideUnknown: aspirin, aspirin, amoxicillin / clavulanate, amoxicillin / clavulanate, albuterol / ipratropium, albuterol / ipratropium, lvp solution, lvp solution, insulin isophane, insulin isophane, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol

Ceftriaxone Disease Interaction

Major: colitis, hyperbilirubinemiaModerate: gallbladder disease, pancreatitis, prothrombin time alterations, renal/liver disease, liver disease, seizure disorders

Volume of Distribution

The apparent volume of distribution of an intravenous or intramuscular dose in healthy patients is 5.78 to 13.5 L. The volume of distribution of an intravenous or intramuscular dose in septic patients is 6.48 to 35.2 L. Ceftriaxone has good enough CSF penetration to be used as an effective treatment of bacterial meningitis.

Elimination Route

Ceftriaxone is only given as an injection, either intramuscularly or intravenously. Ceftriaxone is less than 1% bioavailable if given orally.

Half Life

The elimination half-life of ceftriaxone is 5.8-8.7 hours. The half-life of ceftriaxone in the middle ear fluid has been estimated to be 25 hours.

Clearance

The plasma clearance of ceftriaxone in healthy adults receiving a 0.15-3g dose is 0.58 to 1.45 L/hour. The renal clearance of ceftriaxone is 0.32 to 0.73 L/hour. In intensive care unit patients, ceftriaxone's total drug clearance was 0.96L/h (0.55-1.28 L/h), and unbound drug clearance was 1.91 L/h (1.46-6.20 L/h).

Elimination Route

Ceftriaxone is primarily eliminated in the urine (33-67%). The remainder is eliminated through secretion in the bile and removed from the body via the feces.

Pregnancy & Breastfeeding use

Pregnancy: The safety of Ceftriaxone in the treatment of infections during pregnancy has not been established. Ceftriaxone should only be used during pregnancy if the likely benefit outweighs the potential risk to the fetus and/or the mother.

Lactation: Ceftriaxone is excreted in breast milk at low concentrations. Therefore, caution should be exercised when Ceftriaxone is administered to a nursing mother.

Contraindication

Ceftriaxone should not be given to patients with a history of hypersensitivity to cephalosporin antibiotics. It is contraindicated in premature infants during the first 6 weeks of life. Its safety in human pregnancy has not been established. Ceftriaxone is contraindicated in neonates 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.

Acute Overdose

There is no specific antidote. Treatment of over dosage should be symptomatic.

Storage Condition

Store below 25°C, protected from light & moisture. Use reconstituted solutions immediately.

Reconstituted solutions are stable for 6 hours at room temperature and for 24 hours at 2°-8°C. It should not be mixed in the same syringe with any drug other than 1% Lidocaine Hydrochloride injection BP (for IM injection only).

Innovators Monograph

You find simplified version here Ceftriaxone