Amsulvex

Amsulvex

ampicillin + sulbactam

Manufacturer:

North China Pharma

Distributor:

Sannovex
Full Prescribing Info
Contents
Sultamicillin: Ampicillin sodium, sulbactam sodium.
Description
Ampicillin sodium/Sulbactam sodium parenteral combination, is available as a white to off-white dry powder for reconstitution. Ampicillin sodium is derived from the penicillin nucleus, 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 and has a molecular weight of 371.39. Its chemical formula is C16H18N3NaO4S. 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. Its chemical formula is C8H10NNaO5S with a molecular weight of 255.22.
Action
Pharmacology: General: Immediately after completion of a 15-minute intravenous infusion of Amsulvex, 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 40 to 71 mcg/mL are attained 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.
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 AMSULVEX in such patients should be administered less frequently in accordance with the usual practice for ampicillin.
Microbiology: 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 Neisseriaciae, 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 AMSULVEX formulation effectively extends the antibiotic spectrum of ampicillin to include many bacteria normally resistant to it and to other beta-lactam antibiotics. Thus, AMSULVEX 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.
Gram-Positive Bacteria: Staphylococcus aureus (beta-lactamase and non-beta-lactamase producing), Staphylococcus epidermidis (beta-lactamase and non-beta-lactamase producing), Staphylococcus saprophyticus (beta-lactamase and non-beta-lactamase producing), Streptococcus faecalis*** (Enterococcus), Streptococcus pneumoniae*** (formerly D. pneumoniae), Streptococcus pyogenes***, Streptococcus viridans***.
Gram-Negative Bacteria: Hemophilus influenzae (beta-lactamase and non-beta-lactamase producing). Moraxella (Branhamella) catarrhalis (beta-lactamase and non-beta-lactamase producing). Escherichia coli (beta-lactamase and non-beta-lactamase producing). Klebsiella species (all known strains are beta-lactamase producing). Proteus mirabilis (beta-lactamase and non-beta-lactamase producing), Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Morganella morganii, and Neisseria gonorrhoeae (beta-lactamase and non-beta-lactamase producing).
Anaerobes: Clostridium species***, Peptococcus species***, Peptostreptococcus species, Bacteroides species, including B. fragilis.
***These are not beta-lactamase producing strains and, therefore, are susceptible to ampicillin alone.
Indications/Uses
Infections due to beta-lactamase producing H. influenza including those of the respiratory tract, bones, joints and soft tissues; polymicrobial infections with mixed aerobic and anaerobic such as diabetic foot, gynecologic infections, intra-abdominal infections; urinary tract infections due to susceptible organisms.
Dosage/Direction for Use
1.5-12 g/day in divided doses: Mild infection 1.5-3 g, moderate infection: Up to 6 g, severe infection Up to 12 g. Neonate 150 mg/kg/day. Prophylaxis of surgical infections 1.5-3 g at the induction of anesthesia and may be repeated 6-8 hourly.
Directions for Use: General Dissolution Procedures: Ampicillin and Sulbactam for Injection sterile powder for intravenous and intramuscular use may be reconstituted with any of the compatible diluents described in this insert. Solutions should be allowed to stand after dissolution to allow any foaming to dissipate in order to permit visual inspection for complete solubilization.
Preparation for Intravenous Use: 1.5 Gram and 3 Gram Vials of Sterile Powder: Initially, vials for intravenous use may be reconstituted with Sterile Water for Injection to yield solutions containing 375 mg ampicillin and sulbactam per mL (250 mg ampicillin/125 mg sulbactam per mL). An appropriate volume should then be immediately diluted with any of the following suitable parenteral diluents to yield solutions containing 3 to 45 mg ampicillin and sulbactam per mL (2 to 30 mg ampicillin/1 to 15 mg sulbactam per mL). Reconstitution of AMSULVEX, at the specified concentrations, with these diluents provide stable solutions for the time periods indicated in the following table: (After the indicated time periods, any unused portions of solutions should be discarded.) (See Table 1.)

Click on icon to see table/diagram/image

Preparation for Intramuscular Injection: 1.5 G and 3 G Vials: Vials for intramuscular use may be reconstituted with Sterile Water for Injection USP, 0.5% Lidocaine Hydrochloride Injection USP or 2% Lidocaine Hydrochloride Injection USP. Consult the following table for recommended volumes to be added to obtain solutions containing 375 mg Ampicillin and Sulbactam per mL (250 mg ampicillin/125 mg sulbactam per mL). Note: Use only freshly prepared solutions and administer within one hour after preparation.
*There is sufficient excess present to allow withdrawal and administration of the stated volumes. (See Table 2.)

Click on icon to see table/diagram/image

While reversible glycogenosis was observed in laboratory animals, this phenomenon was dose- and time-dependent and is not expected to develop at the therapeutic doses and corresponding plasma levels attained during the relatively short periods of combined ampicillin/sulbactam therapy in man.
Contraindications
The use of this combination is contraindicated in individuals with a history of an allergic reaction to any of the penicillins.
Storage
Store at temperatures not exceeding 25°C. Protect from light.
MIMS Class
ATC Classification
J01CR01 - ampicillin and beta-lactamase inhibitor ; Belongs to the class of penicillin combinations, including beta-lactamase inhibitors. Used in the systemic treatment of infections.
Presentation/Packing
750 mg powd for inj (vial) 10's. 1.5 g powd for inj (vial) 10's.
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