[Beta-lactam/beta-lactamase inhibitor combinations for oral administration]

Beta-lactamase inhibitors are compounds which are able to bind many beta-lactamase and to inactivate them irreversibly ("suicide inactivators"). Their intrinsic antimicrobial activity is weak. However, in combination with aminopenicillins they exhibit marked synergism both in vitro and in vivo against many beta-lactamase producing bacterial strains. At the achievable serum and tissue concentrations after oral administration, various aminopenicillin/beta-lactamase inhibitor combinations are active against many strains of beta-lactamase producing Haemophilus influenzae, Moraxella catarrhalis, Bacteroides fragilis and staphylococci. At levels achievable in the urine, they are also active against many strains of Escherichia coli, Proteus spp. and Klebsiella spp. Clinically, they have been shown to be effective in the treatment of various human infections of the urinary tract, airways, skin, soft tissues, ear and sinuses. Mild gastrointestinal disturbances are the most commonly encountered side effects. Aminopenicillin/beta-lactamase inhibitor combinations may be a suitable therapeutic option in treating mild to moderately severe infections, i.e. in an outpatient setting.