To reduce the development of drug-resistant bacteria and maintain the effectiveness of AMOXIL (amoxicillin) and other antibacterial drugs, AMOXIL should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.
DESCRIPTION
Formulations of AMOXIL contain amoxicillin, a semisynthetic antibiotic, an analog of ampicillin, with a broad spectrum of bactericidal activity against many gram-positive and gram-negative microorganisms. Chemically, it is (2
S,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. It may be represented structurally as:
The amoxicillin molecular formula is C16H19N3O5S•3H2O, and the molecular weight is 419.45.
Capsules and powder for oral suspension of AMOXIL are intended for oral administration.
Pediatric Drops for Oral Suspension:
Each mL of reconstituted suspension contains 50 mg amoxicillin as the trihydrate and 0.03 mEq (0.69 mg) of sodium.
Amoxicillin trihydrate for oral suspension 250 mg/5 mL (or 50 mg/mL), and 400 mg/5 mL are bubble-gum-flavored pink suspensions. Inactive ingredients: FD&C Red No. 3, flavorings, silica gel, sodium benzoate, sodium citrate, sucrose, and xanthan gum.
CLINICAL PHARMACOLOGY
Amoxicillin is stable in the presence of gastric acid and is rapidly absorbed after oral administration. The effect of food on the absorption of amoxicillin from the tablets and suspension of AMOXIL has been partially investigated. The 400-mg and 875-mg formulations have been studied only when administered at the start of a light meal. However, food effect studies have not been performed with the 200-mg and 500-mg formulations. Amoxicillin diffuses readily into most body tissues and fluids, with the exception of brain and spinal fluid, except when meninges are inflamed. The half-life of amoxicillin is 61.3 minutes. Most of the amoxicillin is excreted unchanged in the urine; its excretion can be delayed by concurrent administration of probenecid. In blood serum, amoxicillin is approximately 20% protein-bound.
Orally administered doses of 250-mg and 500-mg amoxicillin capsules result in average peak blood levels 1 to 2 hours after administration in the range of 3.5 mcg/mL to 5.0 mcg/mL and 5.5 mcg/mL to 7.5 mcg/mL, respectively.
Mean amoxicillin pharmacokinetic parameters from an open, two-part, single-dose crossover bioequivalence study in 27 adults comparing 875 mg of AMOXIL with 875 mg of AUGMENTIN® (amoxicillin/clavulanate potassium) showed that the 875-mg tablet of AMOXIL produces an AUC0-
∞ of 35.4 ± 8.1 mcg•hr/mL and a Cmax of 13.8 ± 4.1 mcg/mL. Dosing was at the start of a light meal following an overnight fast.
Orally administered doses of amoxicillin suspension, 125 mg/5 mL and 250 mg/5 mL, result in average peak blood levels 1 to 2 hours after administration in the range of 1.5 mcg/mL to 3.0 mcg/mL and 3.5 mcg/mL to 5.0 mcg/mL, respectively.
