Ceftriaxone
Brand name:- Oframax, Monocef, Monotax 0.25,0.5.1.0g per vial inj.
Ceftriaxone is an antibiotic belonging to the cephalosporin group, which is used to treat bacterial infections in your body. It is effective in infections of the brain (e.g., meningitis), lungs (e.g., pneumonia), ear, urinary tract, skin & soft tissues, bones & joints, blood, and heart.
Pharmacodynamic:-
Ceftriaxone is a cephalosporin/cephamycin beta-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms. Ceftriaxone has in vitro activity against gram-positive aerobic, gram-negative aerobic, and anaerobic bacteria.The bactericidal activity of ceftriaxone results from the inhibition of cell wall synthesis and is mediated through ceftriaxone binding to penicillin-binding proteins (PBPs). Ceftriaxone is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, and cephalosporinases and extended-spectrum beta-lactamases.However, resistance to ceftriaxone usually occurs through beta-lactamase hydrolysis, altered PBPs, or reduced bacterial cell permeability.Ceftriaxone should not be mixed with or giving in the same IV line as diluents/products containing calcium as they may cause ceftriaxone to precipitate.Ceftriaxone use may also cause biliary sludge or gallbladder pseudolithiasis.
Mechanism of action:-
Ceftriaxone is a third-generation antibiotic from the cephalosporin family of antibiotics.[6] It is within the β-lactam family of antibiotics. Ceftriaxone selectively and irreversibly inhibits bacterial cell wall synthesis by binding to transpeptidases, also called transamidases, which are penicillin-binding proteins (PBPs) that catalyze the cross-linking of the peptidoglycan polymers forming the bacterial cell wall. The peptidoglycan cell wall is made up of pentapeptide units attached to a polysaccharide backbone with alternating units of N-acetylglucosamine and N-acetylmuramic acid.PBPs act on a terminal D-alanyl-D-alanine moiety on a pentapeptide unit and catalyze the formation of a peptide bond between the penultimate D-alanine and a glycine unit on an adjacent peptidoglycan strand, releasing the terminal D-alanine unit in the process. The structure of ceftriaxone mimics the D-alanyl-D-alanine moiety, and the PBP attacks the beta-lactam ring in ceftriaxone as if it were its normal D-alanyl-D-alanine substrate.The peptidoglycan cross-linking activity of PBPs is a construction and repair mechanism that normally helps to maintain bacterial cell wall integrity, so the inhibition of PBPs leads to damage and destruction of the cell wall and eventually to cell lysis.
Used:-
used in the treatment a wide variety of bacterial infections.
Side effects:-
Most side effects do not require any medical attention and disappear as your body adjusts to the medicine. Consult your doctor if they persist or if you’re worried about them
#Common side effects of ceftriaxone
•Diarrhea
•Abnormal liver function tests
•Rash
•Increased white blood cell count (eosinophils), Decreased white blood cell count, Low blood platelets, Increased liver enzymes
Dose:-
•For skin/soft tissue/ urinary infection: 1-2 g i.v. or i.m./ day.
•Meningitis:4g followed by 2 g i.v. (children 75-100mg / kg ) once daily for 7-10days.
• Typhoid: 4g i.v daily × 2days followed by 2g/day (children 75mg/kg) till 2 days after fever subsides.
( As directed by your doctor).
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