AUGMENTIN ES-600

AUGMENTIN ES-600- amoxicillin and clavulanate potassium powder, for suspension
Dr Reddys Laboratories Inc

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1111 PRESCRIBING INFORMATION

To reduce the development of drug-resistant bacteria and maintain the effectiveness of AUGMENTIN ES-600 Powder for Oral Suspension and other antibacterial drugs, AUGMENTIN ES-600 Powder for Oral Suspension should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.

DESCRIPTION

AUGMENTIN ES-600 Powder for Oral Suspension is an oral antibacterial combination consisting of the semisynthetic antibiotic amoxicillin and the β-lactamase inhibitor, clavulanate potassium (the potassium salt of clavulanic acid). Amoxicillin is an analog of ampicillin, derived from the basic penicillin nucleus, 6-aminopenicillanic acid. The amoxicillin molecular formula is C16 H19 N3 O5 S•3H2 O, and the molecular weight is 419.46. Chemically, amoxicillin is (2S ,5R ,6R)-6-[(R)-(-)-2-Amino-2-(p -hydroxyphenyl)acetamido]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid trihydrate and may be represented structurally as:

Amoxicillin Chemical Structure
(click image for full-size original)

Clavulanic acid is produced by the fermentation of Streptomyces clavuligerus. It is a β-lactam structurally related to the penicillins and possesses the ability to inactivate a wide variety of β-lactamases by blocking the active sites of these enzymes. Clavulanic acid is particularly active against the clinically important plasmid-mediated β-lactamases frequently responsible for transferred drug resistance to penicillins and cephalosporins. The clavulanate potassium molecular formula is C8 H8 KNO5 , and the molecular weight is 237.25. Chemically, clavulanate potassium is potassium (Z)-(2R ,5R)-3-(2-hydroxyethylidene)-7-oxo-4-oxa-1-azabicyclo[3.2.0]-heptane-2-carboxylate and may be represented structurally as:

Clavulanate Potassium Chemical Structure

Inactive Ingredients:

Powder for Oral Suspension- Colloidal silicon dioxide, strawberry cream flavor, xanthan gum, aspartamea , sodium carboxymethylcellulose, and silicon dioxide.

a See PRECAUTIONSInformation for the Patient/Phenylketonurics.

Each 5 mL of reconstituted 600 mg/42.9 mg per 5 mL oral suspension of AUGMENTIN ES-600 contains 0.23 mEq potassium.

CLINICAL PHARMACOLOGY

The pharmacokinetics of amoxicillin and clavulanate were determined in a study of 19 pediatric patients, 8 months to 11 years, given AUGMENTIN ES-600 Powder for Oral Suspension at an amoxicillin dose of 45 mg/kg q12h with a snack or meal. The mean plasma amoxicillin and clavulanate pharmacokinetic parameter values are listed in the following table.

Table 1. Mean (±SD) Plasma Amoxicillin and Clavulanate Pharmacokinetic Parameter Values Following Administration of 45 mg/kg of AUGMENTIN ES-600 Powder for Oral Suspension Every 12 Hours to Pediatric Patients
PARAMETER * AMOXICILLIN CLAVULANATE
*
Arithmetic mean ± standard deviation, except Tmax values which are medians (ranges).
Cmax (mcg/mL) 15.7 ± 7.7 1.7 ± 0.9
Tmax (hr) 2.0 (1.0 — 4.0) 1.1 (1.0 — 4.0)
AUC0-t (mcg⋅hr/mL) 59.8 ± 20.0 4.0 ± 1.9
T1/2 (hr) 1.4 ± 0.3 1.1 ± 0.3
CL/F (L/hr/kg) 0.9 ± 0.4 1.1 ± 1.1

The effect of food on the oral absorption of AUGMENTIN ES-600 Powder for Oral Suspension has not been studied.

Approximately 50% to 70% of the amoxicillin and approximately 25% to 40% of the clavulanic acid are excreted unchanged in urine during the first 6 hours after administration of 10 mL of 250 mg/5 mL suspension of AUGMENTIN.

Concurrent administration of probenecid delays amoxicillin excretion but does not delay renal excretion of clavulanic acid.

Neither component in AUGMENTIN ES-600 Powder for Oral Suspension is highly protein-bound; clavulanic acid has been found to be approximately 25% bound to human serum and amoxicillin approximately 18% bound.

Oral administration of a single dose of AUGMENTIN ES-600 Powder for Oral Suspension at 45 mg/kg (based on the amoxicillin component) to pediatric patients, 9 months to 8 years, yielded the following pharmacokinetic data for amoxicillin in plasma and middle ear fluid (MEF).

Table 2. Amoxicillin Concentrations in Plasma and Middle Ear Fluid Following Administration of 45 mg/kg of AUGMENTIN ES-600 Powder for Oral Suspension to Pediatric Patients
Timepoint Amoxicillin concentration in plasma (mcg/mL) Amoxicillin concentration in MEF (mcg/mL)
1 hour meanmedianrange 7.79.31.5 — 14.0(n = 5) 3.23.50.2 — 5.5(n = 4)
2 hour meanmedianrange 15.713.011.0 — 25.0( n= 7) 3.32.41.9 — 6(n = 5)
3 hour meanmedianrange 13.012.05.5 — 21.0(n = 5) 5.86.53.9 — 7.4(n = 5)

Dose administered immediately prior to eating.

Amoxicillin diffuses readily into most body tissues and fluids with the exception of the brain and spinal fluid. The results of experiments involving the administration of clavulanic acid to animals suggest that this compound, like amoxicillin, is well distributed in body tissues.

Microbiology:

Amoxicillin is a semisynthetic antibiotic with a broad spectrum of bactericidal activity against many gram-positive and gram-negative microorganisms. Amoxicillin is, however, susceptible to degradation by β-lactamases, and therefore, its spectrum of activity does not include organisms which produce these enzymes. Clavulanic acid is a β-lactam, structurally related to penicillin, which possesses the ability to inactivate a wide range of β-lactamase enzymes commonly found in microorganisms resistant to penicillins and cephalosporins. In particular, it has good activity against the clinically important plasmid-mediated β-lactamases frequently found responsible for transferred drug resistance.

The clavulanic acid component of AUGMENTIN ES-600 Powder for Oral Suspension protects amoxicillin from degradation by β-lactamase enzymes and effectively extends the antibiotic spectrum of amoxicillin to include many bacteria normally resistant to amoxicillin and other β-lactam antibiotics. Thus, AUGMENTIN ES-600 Powder for Oral Suspension possesses the distinctive properties of a broad-spectrum antibiotic and a β-lactamase inhibitor.

Amoxicillin/clavulanic acid has been shown to be active against most isolates of the following microorganisms, both in vitro and in clinical infections as described in the INDICATIONS AND USAGE section.

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