Chemical structure Linezolid is the first member of the group Oxazolidinone antibiotics. Oxazolidinones (sulfoxide 1) were first characterized for their use in treating plant diseases in 1978. Six years later antibacterial properties were discovered, with greatly improved antibacterial properties relative to their progenitor compounds. It is usually these two compounds, which are referred to as the first true lead compounds in the oxazolidinone family (lead compound - compound that exhibits pharmacological properties which suggest its value as a starting point for drug development). Further structural discussion led to piperazine derivatives.Those compounds were selected for further modification as they combined excellent activity with an …show more content…
In the initiation process,this site of inhibition comes prior to other protein synthesis inhibitors that inhibit elongation process.due to this unique site of inhibition,cross-resistance to other protein synthesis inhibitors has not been reported.[3] Summary of antibacterial …show more content…
also co-administration with antacids like magnesium hydroxide and aluminium hydroxide had no effect on oral absorption.[6] plasma protein binding level is 31% and the volume of distribution approximates to the total body water content of 40–50 L. Plasma elimination half-life is 3.4–7.4 h. Linezolid is metabolized to two inactive metabolites, an aminoethoxyacetic acid (metabolite A) and a hydroxyethyl glycine (metabolite B). The clearance rate (+SD) is 80+29 mL/min and by non-renal (65%) and renal mechanisms. Renal tubular reabsorption may occur.Aproportion of the dose is excreted unchanged in the urine. extensive work on the pharmacokinetics of linezolid at different doses and in different groups of patients have been done. A small degree of non-linearity has been observed, with a 30% decrease in clearance after a 5-fold increase in dose. The non-linearity is not relevant over the therapeutic dosage range. Plasma linezolid concentrations in elderly patients, patients with mild to moderate hepatic impairment or mild to severe renal impairment are similar to those achieved in young or healthy volunteers. Although women had higher concentrations in compare with men, dose adjustment is not needed. Patients with severe renal