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Distribution

Amoxicillin has a center volume of distribution of 27.7L. In serum, amoxicillin is 17 percent protein
bound. The mean clearance of amoxicillin is 21.3L/h. 125mg to 1g doses of amoxicillin are 70-78%
eliminated in the urine after 6 hours. Around 18% of total plasma amoxicillin is bound to protein, with
an apparent volume of distribution of 0.3 to 0.41/kg. Except when the meninges are inflamed,
amoxicillin diffuses rapidly into most human tissues and fluids, with the exception of brain and spinal
fluid. Amoxicillin is roughly 20% protein-bound in blood serum. Following a 1-gram dosage and using a
unique skin window approach to evaluate antibiotic levels, it was discovered that therapeutic amounts
of the antibiotic were identified in the interstitial fluid. Amoxicillin competes with penicillin binding
proteins, causing autolytic enzymes to be activated and cell wall production to be inhibited. Amoxicillin
has a lengthy duration of effect because it is often used twice daily. Because modest overdoses are not
linked with severe toxicity, amoxicillin has a broad therapeutic range. Patients should be advised about
the dangers of anaphylaxis, Clostridium difficile infections, and bacterial resistance.

Absorption

Amoxicillin is a stomach acid stable and readily absorbed after oral treatment. The effect of meals on
amoxicillin absorption from AMOXIL tablets and suspension has been researched in part; 400mg and
875mg formulations have only been evaluated when delivered at the outset of a light meal. Orally given
dosages of 250-mg and 500-mg amoxicillin capsules result in typical peak blood levels of 3.5 mcg/mL to
5.0 mcg/mL and 5.5 mcg/mL to 7.5 mcg/mL, respectively, 1 to 2 hours after administration. The 875-mg
pill of AMOXIL produced an AUC0- of 35.4 8.1 mcg•hr/mL and a Cmax of 13.8 4.1 mcg/mL in an open,
two-part, single-dose crossover bioequivalence study in 27 people comparing 875 mg of AMOXIL with
875 mg of AUGMENTIN® (amoxicillin/clavulanate potassium). The dose was given at the commencement
of a small meal after an overnight fast. Amoxicillin suspension dosages of 125 mg/5 mL and 250 mg/5 mL
result in typical peak blood levels of 1.5 mcg/mL to 3.0 mcg/mL and 3.5 mcg/mL to 5.0 mcg/mL,
respectively, 1 to 2 hours after delivery.

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