VANCOMYCIN HYDROCHLORIDE- vancomycin hydrochloride injection, powder, lyophilized, for solution
Meitheal Pharmaceuticals Inc.
To reduce the development of drug-resistant bacteria and maintain the effectiveness of Vancomycin Hydrochloride for Injection, USP and other antibacterial drugs, Vancomycin Hydrochloride for Injection, USP should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.
Vancomycin Hydrochloride for Injection, USP, is a white or off-white to light tan-colored lyophilized powder or cake, for preparing intravenous (IV) infusions, in single-dose vials each containing the equivalent of 500 mg or 1 gram vancomycin base. 500 mg of the base is equivalent to 0.34 mmol. When reconstituted with Sterile Water for Injection to a concentration of 50 mg per mL, the pH of the solution is between 2.5 and 4.5. This product is oxygen sensitive. Vancomycin Hydrochloride for Injection, USP should be administered intravenously in diluted solution (see DOSAGE AND ADMINISTRATION), AFTER RECONSTITUTION FURTHER DILUTION IS REQUIRED BEFORE USE .
Vancomycin is a tricyclic glycopeptide antibiotic derived from Amycolatopasis orientalis (formerly Nocardia orientalis). The chemical name for vancomycin hydrochloride is [3S -[3R *,6S *( S *),7S *,22S *,23R *,26R *,36S *,38aS *]]-3-(2-Amino-2-oxoethyl)-44-[[2-O -(3-amino-2,3,6-trideoxy-3-C-methyl-α -L-lyxo -hexopyranosyl)-β-D-glucopyranosyl]oxy]-10,19-dichloro-2,3,4,5,6,7,23,24,25,26,36,37,38,38a-tetradecahydro-7,22,28,30,32-pentahydroxy-6-[[4-methyl-2-(methylamino)-1-oxopentyl]amino]-2,5,24,38,39-pentaoxo-22H -8,11:18,21-dietheno-23,36- (iminomethano)-13,16:31,35-dimetheno-1H ,16H -[1,6,9]oxadiazacyclohexadecino[4,5-m ][10,2,16]-benzoxadiazacyclotetracosine-26-carboxylic acid, monohydrochloride. Vancomycin hydrochloride has the following structural formula:
C66 H75 Cl2 N9 O24 •HCl M.W. 1485.71
Vancomycin hydrochloride is poorly absorbed after oral administration.
In subjects with normal kidney function, multiple intravenous dosing of 1 gram of vancomycin hydrochloride (15 mg/kg) infused over 60 minutes produces mean plasma concentrations of approximately 63 mcg/mL immediately after the completion of infusion, mean plasma concentrations of approximately 23 mcg/mL 2 hours after infusion, and mean plasma concentrations of approximately 8 mcg/mL 11 hours after the end of the infusion. Multiple dosing of 500 mg infused over 30 minutes produces mean plasma concentrations of about 49 mcg/mL at the completion of infusion, mean plasma concentrations of about 19 mcg/mL 2 hours after infusion, and mean plasma concentrations of about 10 mcg/mL 6 hours after infusion. The plasma concentrations during multiple dosing are similar to those after a single dose.
The mean elimination half-life of vancomycin from plasma is 4 to 6 hours in subjects with normal renal function. In the first 24 hours, about 75% of an administered dose of vancomycin hydrochloride is excreted in urine by glomerular filtration. Mean plasma clearance is about 0.058 L/kg/h, and mean renal clearance is about 0.048 L/kg/h. Renal dysfunction slows excretion of vancomycin. In anephric patients, the average half-life of elimination is 7.5 days. The distribution coefficient is from 0.3 to 0.43 L/kg. There is no apparent metabolism of the drug. About 60% of an intraperitoneal dose of vancomycin hydrochloride administered during peritoneal dialysis is absorbed systemically in 6 hours. Serum concentrations of about 10 mcg/mL are achieved by intraperitoneal injection of 30 mg/kg of vancomycin hydrochloride. However, the safety and efficacy of the intraperitoneal use of vancomycin hydrochloride has not been established in adequate and well-controlled trials (see PRECAUTIONS).
Total systemic and renal clearance of vancomycin may be reduced in the elderly. Vancomycin is approximately 55% serum protein bound as measured by ultrafiltration at vancomycin serum concentrations of 10 to 100 mcg/mL. After intravenous administration of vancomycin hydrochloride, inhibitory concentrations are present in pleural, pericardial, ascitic, and synovial fluids; in urine; in peritoneal dialysis fluid; and in atrial appendage tissue. Vancomycin does not readily diffuse across normal meninges into the spinal fluid; but, when the meninges are inflamed, penetration into the spinal fluid occurs.
The bactericidal action of vancomycin hydrochloride results primarily from inhibition of cell-wall biosynthesis. In addition, vancomycin hydrochloride alters bacterial-cell-membrane permeability and RNA synthesis. There is no cross-resistance between vancomycin hydrochloride and other antibiotics. Vancomycin hydrochloride is not active in vitro against gram-negative bacilli, mycobacteria, or fungi.
The combination of vancomycin hydrochloride and an aminoglycoside acts synergistically in vitro against many strains of Staphylococcus aureus , Streptococcus bovis , enterococci, and the viridans group streptococci.
Vancomycin hydrochloride has been shown to be active against most strains of the following microorganisms, both in vitro and in clinical infections as described in the INDICATIONS AND USAGE section.
Aerobic gram-positive microorganisms
Enterococci (e.g., Enterococcus faecalis)
Staphylococci, including Staphylococcus aureus and Staphylococcus epidermidis (including heterogeneous methicillin-resistant strains)
Viridans group streptococci
The following in vitro data are available, but their clinical significance is unknown .
Vancomycin hydrochloride exhibits in vitro MIC’s of 1 mcg/mL or less against most (≥ 90%) strains of streptococci listed below and MIC’s of 4 mcg/mL or less against most (≥ 90%) strains of other listed microorganisms; however, the safety and effectiveness of vancomycin hydrochloride in treating clinical infections due to these microorganisms have not been established in adequate and well-controlled clinical trials.
Aerobic gram-positive microorganisms
Streptococcus pneumoniae (including penicillin-resistant strains)
Anaerobic gram-positive microorganisms
For specific information regarding susceptibility test interpretive criteria and associated test methods and quality control standards recognized by FDA for this drug, please see: https://www.fda.gov/STIC.
Vancomycin Hydrochloride for Injection is indicated for the treatment of serious or severe infections caused by susceptible strains of methicillin-resistant (β-lactam-resistant) staphylococci. It is indicated for penicillin-allergic patients, for patients who cannot receive or who have failed to respond to other drugs, including the penicillins or cephalosporins, and for infections caused by vancomycin hydrochloride-susceptible organisms that are resistant to other antimicrobial drugs. Vancomycin Hydrochloride for Injection is indicated for initial therapy when methicillin-resistant staphylococci are suspected, but after susceptibility data are available, therapy should be adjusted accordingly.
Vancomycin Hydrochloride for Injection is effective in the treatment of staphylococcal endocarditis. Its effectiveness has been documented in other infections due to staphylococci, including septicemia, bone infections, lower respiratory tract infections, skin and skin structure infections. When staphylococcal infections are localized and purulent, antibiotics are used as adjuncts to appropriate surgical measures.
Vancomycin Hydrochloride for Injection has been reported to be effective alone or in combination with an aminoglycoside for endocarditis caused by S. viridans or S. bovis. For endocarditis caused by enterococci (e.g., E. faecalis), Vancomycin Hydrochloride for Injection has been reported to be effective only in combination with an aminoglycoside.
Vancomycin Hydrochloride for Injection has been reported to be effective for the treatment of diphtheroid endocarditis. Vancomycin Hydrochloride for Injection has been used successfully in combination with either rifampin, an aminoglycoside, or both in early-onset prosthetic valve endocarditis caused by S. epidermidis or diphtheroids.
Specimens for bacteriologic cultures should be obtained in order to isolate and identify causative organisms and to determine their susceptibilities to vancomycin hydrochloride.
To reduce the development of drug-resistant bacteria and maintain the effectiveness of Vancomycin Hydrochloride for Injection and other antibacterial drugs, Vancomycin Hydrochloride for Injection should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy.
The parenteral form of vancomycin hydrochloride may be administered orally for treatment of antibiotic-associated pseudomembranous colitis produced by C. difficile and for staphylococcal enterocolitis. Parenteral administration of vancomycin hydrochloride alone is of unproven benefit for these indications. Vancomycin hydrochloride is not effective by the oral route for other types of infections.
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