AMPICILLIN AND SULBACTAM- ampicillin sodium and sulbactam sodium injection, powder, for suspension
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To reduce the development of drug-resistant bacteria and maintain the effectiveness of Ampicillin and Sulbactam for Injection, USP and other antibacterial drugs. Ampicillin and Sulbactam for Injection, USP should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.
Ampicillin and Sulbactam for Injection, USP is a sterile, injectable antibacterial combination, consisting of the semisynthetic antibiotic ampicillin sodium and the beta-lactamase inhibitor sulbactam sodium for intravenous and intramuscular administration.
Ampicillin sodium is derived from the penicillin nucleus, 6-aminopenicillanic acid. Chemically, it is monosodium (2S, 5R, 6R)-6-[(R)-2-amino-2-phenylacetamido]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate. The structural formula is:
Chemical formula: C16 H18 N3 NaO4 S
Sulbactam sodium is a derivative of the basic penicillin nucleus. Chemically, sulbactam sodium is sodium penicillinate sulfone; sodium (2S, 5R)-3, 3-dimethyl-7-oxo-4-thia-1-azabicyclo [3.2.0] heptane-2-carboxylate 4, 4-dioxide. The structural formula is:
Chemical formula: C8 H10 NNaO5 S
Ampicillin and Sulbactam for Injection, USP parenteral combination, is available as a white to off-white dry powder for reconstitution. Ampicillin and Sulbactam for Injection, USP dry powder is freely soluble in aqueous diluents to yield pale yellow to yellow solutions containing ampicillin sodium and sulbactam sodium equivalent to 250 mg ampicillin per mL and 125 mg sulbactam per mL. The pH of the solutions is between 8.0 and 10.0.
Dilute solutions (up to 30 mg ampicillin and 15 mg sulbactam per mL) are essentially colorless to pale yellow. The pH of dilute solutions remains the same.
Each 1.5 gram vial contains: 1.5 g Ampicillin and Sulbactam for Injection (equivalent to 1 g ampicillin as the sodium salt plus 0.5 g sulbactam as the sodium salt). The sodium content per vial is 4.7 mEq (107 mg).
Each 3 gram vial contains: 3 g Ampicillin and Sulbactam for Injection (equivalent to 2 g ampicillin as the sodium salt plus 1 g sulbactam as the sodium salt). The sodium content per vial is 9.3 mEq (214 mg).
Immediately after completion of a 15 minute intravenous infusion of ampicillin and sulbactam for injection, peak serum concentrations of ampicillin and sulbactam are attained. Ampicillin serum levels are similar to those produced by the administration of equivalent amounts of ampicillin alone. Peak ampicillin serum levels ranging from 109 to 150 mcg/mL are attained after administration of 2000 mg of ampicillin plus 1000 mg sulbactam and 40 to 71 mcg/mL after administration of 1000 mg ampicillin plus 500 mg sulbactam. The corresponding mean peak serum levels for sulbactam range from 48 to 88 mcg/mL and 21 to 40 mcg/mL, respectively. After an intramuscular injection of 1000 mg ampicillin plus 500 mg sulbactam, peak ampicillin serum levels ranging from 8 to 37 mcg/mL and peak sulbactam serum levels ranging from 6 to 24 mcg/mL are attained.
The mean serum half-life of both drugs is approximately 1 hour in healthy volunteers. Approximately 75 to 85% of both ampicillin and sulbactam are excreted unchanged in the urine during the first 8 hours after administration of ampicillin and sulbactam for injection to individuals with normal renal function. Somewhat higher and more prolonged serum levels of ampicillin and sulbactam can be achieved with the concurrent administration of probenecid.
In patients with impaired renal function the elimination kinetics of ampicillin and sulbactam are similarly affected, hence the ratio of one to the other will remain constant whatever the renal function. The dose of ampicillin and sulbactam for injection in such patients should be administered less frequently in accordance with the usual practice for ampicillin (see DOSAGE AND ADMINISTRATION).
Ampicillin has been found to be approximately 28% reversibly bound to human serum protein and sulbactam approximately 38% reversibly bound.
The following average levels of ampicillin and sulbactam were measured in the tissues and fluids listed:
|TABLE A Concentration of Ampicillin and Sulbactam for Injection in Various Body Tissues and Fluids|
|Fluid or Tissue||Dose (grams) Ampicillin/Sulbactam||Concentration (mcg/mL or mcg/g) Ampicillin/Sulbactam|
|Peritoneal Fluid||0.5/0.5 IV||7/14|
|Blister Fluid (Cantharides)||0.5/0.5 IV||8/20|
|Tissue Fluid||1/0.5 IV||8/4|
|Intestinal Mucosa||0.5/0.5 IV||11/18|
Penetration of both ampicillin and sulbactam into cerebrospinal fluid in the presence of inflamed meninges has been demonstrated after IV administration of ampicillin and sulbactam.
The pharmacokinetics of ampicillin and sulbactam in pediatric patients receiving ampicillin and sulbactam are similar to those observed in adults. Immediately after a 15 minute infusion of 50 to 75 mg ampicillin and sulbactam per kg body weight, peak serum and plasma concentrations of 82 to 446 mcg ampicillin/mL and 44 to 203 mcg sulbactam/mL were obtained. Mean half-life values were approximately 1 hour.
Ampicillin is similar to benzyl penicillin in its bactericidal action against susceptible organisms during the stage of active multiplication. It acts through the inhibition of cell wall mucopeptide biosynthesis. Ampicillin has a broad spectrum of bactericidal activity against many gram-positive and gram-negative aerobic and anaerobic bacteria. (Ampicillin is, however, degraded by beta-lactamases and therefore the spectrum of activity does not normally include organisms which produce these enzymes).
A wide range of beta-lactamases found in microorganisms resistant to penicillins and cephalosporins have been shown in biochemical studies with cell free bacterial systems to be irreversibly inhibited by sulbactam. Although sulbactam alone possesses little useful antibacterial activity except against the Neisseriaceae , whole organism studies have shown that sulbactam restores ampicillin activity against beta-lactamase producing strains. In particular, sulbactam has good inhibitory activity against the clinically important plasmid mediated beta-lactamases most frequently responsible for transferred drug resistance. Sulbactam has no effect on the activity of ampicillin against ampicillin susceptible strains.
The presence of sulbactam in the ampicillin and sulbactam for injection formulation effectively extends the antibiotic spectrum of ampicillin to include many bacteria normally resistant to it and to other beta-lactam antibiotics. Thus, ampicillin and sulbactam for injection possesses the properties of a broad-spectrum antibiotic and a beta-lactamase inhibitor.
While in vitro studies have demonstrated the susceptibility of most strains of the following organisms, clinical efficacy for infections other than those included in the indications section has not been documented.
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