Norvancomycin (monohydrochloride)

Norvancomycin hydrochloride is a cell wall synthesis inhibitor targeting peptidoglycan precursors of Gram-positive bacteria and cannot pass the blood-brain barrier. Norvancomycin hydrochloride can competitively bind to peptidoglycan precursors, irreversibly inhibit bacterial cell wall synthesis, and exert antibacterial activity. Norvancomycin hydrochloride is mainly used in the study of Gram-positive bacterial infections, especially infections caused by methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-resistant Staphylococcus epidermidis (MRSE). Norvancomycin hydrochloride can also be incorporated into the bionic calcium phosphate coating of titanium implants to enhance antibacterial activity and inhibit postoperative orthopedic infections^[1][2]. In Vitro: Norvancomycin hydrochloride (100-1000 mg/L; 48 h) can be coated with biomimetic calcium phosphate coating. The effective content increases first and then stabilizes with the increase of solution concentration. Norvancomycin hydrochloride reaches 2.16 μg/mg coating at 600 mg/L, and the release is fast first and then slow^[1].
In the in vitro antibacterial experiment, the inhibition zone of Norvancomycin hydrochloride (100-800 mg/L; 24 h) against Staphylococcus aureus increases with the increase of concentration, significantly inhibiting bacterial adhesion^[1]. In Vivo: Norvancomycin (100 mg/kg; intravenous injection; single dose; single) hydrochloride is widely distributed in various tissues in male SD rats 2 hours after administration, with the concentration order being kidney > lung > stomach > intestine > spleen > heart > liver > brain, and Norvancomycin hydrochloride can not be detected in the brain^[2].
The pharmacokinetics of Norvancomycin (100 mg/kg; intravenous injection; single dose; single) in male Kunming mice shows that its elimination half-life is 42.43 minutes and the clearance rate is 0.0233 mL·kg^-1·min^-1[2].