IMIPENEM CILASTATIN - AN UPDATE OF ITS ANTIBACTERIAL ACTIVITY, PHARMACOKINETICS AND THERAPEUTIC EFFICACY IN THE TREATMENT OF SERIOUS INFECTIONS/

The Prototype carbapenem antibacterial agent imipenem has a very broad spectrum of antibacterial activity, encompassing most Gram-negative a nd Gram-positive aerobes and anaerobes, including most beta-lactamase- producing species. It is coadministered with a renal dehydropeptidase inhibitor, cilastatin, in order to prevent its renal metabolism in cli nical use. Extensive clinical experience gained with imipenem/cilastat in has shown it to provide effective monotherapy for septicaemia, neut ropenic fever, and intra-abdominal, lower respiratory tract, genitouri nary, gynaecological, skin and soft tissue, and bone and joint infecti ons. In these indications, imipenem/cilastatin generally exhibits simi lar efficacy to broad-spectrum cephalosporins and other carbapenems an d is at least equivalent to standard aminoglycoside-based and other co mbination regimes. Imipenem/cilastatin is generally well tolerated by adults and children, with local injection site events, gastrointestina l disturbances and dermatological reactions being the most common adve rse events. Seizures have also been reported, occurring mostly in pati ents with impaired renal function or CNS pathology, or with excessive dosage. Although it is no longer a unique compound, as newer carbapene ms such as meropenem are becoming available, imipenem/cilastatin never theless remains an important agent with established efficacy as monoth erapy for moderate to severe bacterial infections. Its particular nich e is in treating infections known or suspected to be caused by multire sistant pathogens.