Target intelligence / Profile preview

Ceftriaxone

Molecular classification
Small molecule, Beta-lactam antibiotic, Third-generation cephalosporin
01

Overview

Ceftriaxone is a third-generation cephalosporin antibiotic and is not a biological target; rather, it is a therapeutic agent that acts upon bacterial penicillin-binding proteins (PBPs) (PubChem CID 5479530). It belongs to the beta-lactam class of antibiotics and is characterized by its broad-spectrum activity against both Gram-positive and Gram-negative bacteria (Wikipedia). The molecule functions by inhibiting the transpeptidation step of peptidoglycan synthesis, which is critical for maintaining the integrity of the bacterial cell wall (Guide to Pharmacology). This inhibition leads to cell wall weakening and subsequent bacterial cell death through osmotic lysis (StatPearls). Ceftriaxone is notable for its high penetration into the cerebrospinal fluid and its long half-life, making it a primary choice for treating meningitis and other severe systemic infections (Drugs.com). While primarily an antimicrobial, research has also explored its role in upregulating the glutamate transporter GLT-1 for potential neuroprotective effects (PubMed). Clinically, it is administered parenterally and is frequently used for the treatment of gonorrhea, pneumonia, and skin infections (NIH). However, its use is associated with safety concerns such as biliary sludge formation and potential interactions with calcium-containing products, particularly in neonates (LiverTox).

Other names
RocephinCeftriaxone sodiumCeftriaxonum
02

Mechanism of action

Ceftriaxone inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), which are enzymes responsible for the final transpeptidation step of peptidoglycan synthesis (Guide to Pharmacology).

03

Biological functions

Bacterial cell wall synthesis inhibitionBactericidal activityGlutamate transporter upregulation
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Disease associations

Bacterial infectionMeningitisPneumoniaGonorrheaSepsisLyme disease
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Safety considerations

AnaphylaxisBiliary sludge (pseudolithiasis)Calcium-ceftriaxone precipitation in neonatesClostridioides difficile-associated diarrheaKernicterus in neonates
06

Interacting drugs

Calcium

4 more in the full profile.

07

Biomarkers

Minimum Inhibitory Concentration (MIC)fT > MICProcalcitoninC-reactive protein (CRP)

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