Drug intelligence / Profile preview

ceftriaxone + lidocaine

Development stage
Unknown
Lead developer
Roche
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intramuscular
01

Overview

Ceftriaxone + lidocaine is a combination used for intramuscular (IM) injection, where the antibiotic ceftriaxone is reconstituted with a solution of 1% lidocaine hydrochloride. Ceftriaxone is a third-generation cephalosporin antibacterial that acts by inhibiting bacterial cell wall synthesis through binding to penicillin-binding proteins, leading to cell lysis and death. Lidocaine is a local anesthetic that blocks voltage-gated sodium channels in neuronal membranes, preventing nerve impulse conduction and thereby reducing pain at the injection site. The addition of lidocaine significantly decreases the pain associated with IM administration of ceftriaxone without affecting its antibacterial efficacy[1][2][3][5][6][7]. This combination is indicated for severe bacterial infections such as meningitis, pneumonia, typhoid fever, shigellosis, leptospirosis, relapsing fevers, pyelonephritis, neurosyphilis; and for sexually transmitted infections like gonorrhea[7][8]. The mixture must only be administered intramuscularly—never intravenously—due to safety concerns related to systemic absorption of lidocaine[3][5][6].

Other names
ceftriaxone with lidocaineceftriaxone/lidocaineceftriaxone sodium powder + lidocaine IM
02

Targets

PBP (Penicillin-binding protein family)NaV alpha (Voltage-gated sodium channel alpha subunit family)

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