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Determination of meropenem in plasma and filtrate-dialysate from patients under continuous veno-venous haemodiafiltration by SPE-LC.

Meropenem, a carbapenem antibiotic displaying a broad spectrum of antibacterial activity, is administered in Medical Intensive Care Unit to critically ill patients undergoing continuous veno-venous haemodiafiltration (CVVHDF). However, there are limited data available to substantial rational dosing decisions in this condition. In an attempt to refine our knowledge and propose a rationally designed dosage regimen, we have developed a HPLC method to determine meropenem after solid-phase extraction (SPE) of plasma and dialysate fluids obtained from patients under CVVHDF. The assay comprises the simultaneous measurement of meropenem's open-ring metabolite UK-1a, whose fate has never been studied in CVVHDF patients. The clean-up procedure involved a SPE on C18 cartridge. Matrix components were eliminated with phosphate buffer pH 7.4 followed by 15:85 MeOH-phosphate buffer pH 7.4. Meropenem and UK-1a were subsequently desorbed with MeOH. The eluates were evaporated under nitrogen at room temperature (RT) and reconstituted in phosphate buffer pH 7.4. Separation was performed at RT on a Nucleosil 100-5 microm C18 AB cartridge column (125 x 4 mm I.D.) equipped with a guard column (8 x 4 mm I.D.) with UV-DAD detection set at 208 nm. The mobile phase was 1 ml min(-1), using a step-wise gradient elution program: %MeOH/0.005 M tetrabutylammonium chloride pH 7.4; 10/90-50/50 in 27 min. Over the range of 5-100 microg ml(-1), the regression coefficient of the calibration curves (plasma and dialysate) were >0.998. The absolute extraction recoveries of meropenem and UK-1a in plasma and filtrate-dialysate were stable and ranged from 88-93 to 72-77% for meropenem, and from 95-104 to 75-82% for UK-1a. In plasma and filtrate-dialysate, respectively, the mean intra-assay precision was 4.1 and 2.6% for meropenem and 4.2 and 3.7% for UK-1a. The inter-assay variability was 2.8 and 3.6% for meropenem and 2.3 and 2.8% for UK-1a. The accuracy was satisfactory for both meropenem and UK-1a with deviation never exceeding 9.0% of the nominal concentrations. The stability of meropenem, studied in biological samples left at RT and at +4 degrees C, was satisfactory with < 5% degradation after 1.5 h in blood but reached 22% in filtrate-dialysate samples stored at RT for 8 h, precluding accurate measurements of meropenem excreted unchanged in the filtrate-dialysate left at RT during the CVVHDF procedure. The method reported here enables accurate measurements of meropenem in critically ill patients under CVVHDF, making dosage individualisation possible in such patients. The levels of the metabolite UK-1a encountered in this population of patients were higher than those observed in healthy volunteers but was similar to those observed in patients with renal impairment under hemodialysis.

Anti-Bacterial Agents↗

The stability of a novel carbapenem antibiotic, meropenem (SM-7338), in a solid state formulation for injection.

A formulation of meropenem, a novel carbapenem antibiotic for injection, was developed as a vial filled with a mixture of meropenem and dried sodium carbonate. During the design phase, we studied the effect of water in the formulation on the stability of meropenem in the solid state. Meropenem is obtained as trihydrate, whose moisture content is 12.35% and is nonhygroscopic. Dehydrated meropenem, whose moisture content was 3.4%, took up moisture quickly even under low humidity (33% RH). Also, the chemical stability of dehydrated meropenem was poor compared with that of untreated meropenem, which is quite stable. Degradation of meropenem by free water was considered as a possible cause of the poor stability. Degradation of meropenem due to liberation of its crystal water to free water was also observed when meropenem was micronized by pneumatic pulverization. Crystal water of meropenem was found to stay bound and to be almost inert in the formulation. Thus, meropenem injection formulation is stable for long time at room temperature.

Chemistry, Pharmaceutical↗

[Selection of resistance mutants and bacteriostatic and bactericidal activity of meropenem and imipenem against Acinetobacter spp].

BACKGROUND: To evaluate the inhibitory and bactericidal activity of meropenem and imipenem against multiresistant isolates of Acinetobacter spp and to compare the frequency of mutation for both antibiotics. METHODS: Minimum inhibitory concentrations were determined by the agar dilution method. Bactericidal activities were evaluated by killing curves method employing 8 times the MIC. One-step resistant mutant selection was performed by spreading more than 5 x 10(8) ufc/ml on agar Mueller Hinton plates containing 2, 4 and 8 times the MIC of meropenem or imipenem. RESULTS: In the group of sensitive strains (MIC < 4 mg/l for imipenem and meropenem) we detected lower MIC for imipenem than meropenem (61.5% of the strains). Strains with reduced susceptibility to imipenem (MIC = 4 mg/l) were more sensitive to meropenem with MICs equivalents to the sensitive group. Bactericidal activity was detected in 6 hs for imipenem and in 24 hs for meropenem. Meropenem was bactericidal in 4 clinical isolates with MICs = 4 mg/l for imipenem and imipenem was bactericidal in laboratory mutants resistant to meropenem. It was no possible to select mutants resistant to imipenem but for meropenem the rate of mutation was 1.4 x 10(-9) to 1.0 x 10(-8). Mutants resistant to meropenem were susceptible to imipenem and 57% of them were stable. CONCLUSIONS: From the laboratory point of view we consider that imipenem is more active than meropenem because it presents lower MICs, better bactericidal activity, and no risk to select resistance. However meropenem could be useful in some strains resistant to imipenem (MIC = 4 mg/l). Cross-resistance was no detected so we consider that both antibiotics should be tested against Acinetobacter spp. because they are not equivalents.

Acinetobacter↗

Pharmacokinetic properties and stability of continuous-infusion meropenem in adults with cystic fibrosis.

BACKGROUND: Meropenem is commonly used to treat lung infections in adults with cystic fibrosis (CF). Although continuous infusion is the ideal method to maximize the pharmacodynamic properties of this betalactam antibiotic, meropenem is stable for only approximately 4 to 6 hours at room temperature, and its pharmacokinetic (PK) properties, when administered by continuous infusion to patients with CF, are largely unknown. OBJECTIVE: This study was undertaken to determine the PK properties and stability of meropenem when administered to adults with CF by a continuous ambulatory drug-delivery infusion pump stored in a cold pouch between 2 freezer packs. METHODS: This open-label, multidose, randomized, crossover PK study was conducted at the Clinical Research Center at Hartford Hospital (Hartford, Connecticut). Adults aged > or = 18 years with CF were eligible. Study participants were randomized to receive meropenem 125 mg/h or 250 mg/h (equivalent to 3 g and 6 g, respectively, over 24 hours) by continuous IV infusion for 12 hours. Serum samples were collected throughout the infusion and then for 6 hours after infusion to determine the PK properties (volume of distribution [V(d)], elimination rate constant, total body clearance [CL], terminal half-life [t 1/2], and steady-state concentration [C(ss)]). Serum meropenem concentrations were assayed using high-performance liquid chromatography, and PK profiles were determined using compartmental analysis. Meropenem stability was ascertained by sampling the drug directly from the infusion pump at prespecified time points. Meropenem tolerability was assessed throughout the study by questioning subjects on how they felt. In addition, laboratory values of serum chemistries and liver enzymes were compared with baseline values. RESULTS: Seven adult volunteers with CF (4 women, 3 men; mean [SD] age, 27 [10] years [range, 19-46 years]) participated in the study. Mean (SD) C(ss) values were 8.31 (0.68) mg/L and 18.50 (3.31) mg/L for the 125-mg/h and 250-mg/h infusion rates, respectively. V(d), CL, and t 1/2 were dose independent and similar between the 2 infusion rates. Meropenem stability was maintained over 12 and 24 hours. Meropenem by continuous infusion was well tolerated. One patient complained of a headache during the study. CONCLUSIONS: In this study of adults with CF, meropenem infusion rates of 125 mg/h and 250 mg/h provided serum drug concentrations greater than the minimum inhibitory concentration for pathogens considered meropenem susceptible (< or =4 microg/mL) and intermediately resistant (8 microg/mL), respectively.

Adult↗

In-vitro studies of meropenem.

Meropenem, a new carbapenem, was compared with imipenem and seven other broad-spectrum antimicrobial agents against approximately 1000 clinical isolates. Meropenem was two- to four-fold more active than imipenem against Gram-negative organisms and its spectrum of antimicrobial activity was wider than those of all other drugs tested. However, imipenem was more potent than meropenem against the staphylococci, Streptococcus spp. and enterococci. Many rarely isolated organisms were more susceptible to the carbapenems than to other comparison compounds. All anaerobic bacteria were inhibited by meropenem at less than or equal to 8 mg/l and 50% of strains were inhibited by 0.25 mg/l. Meropenem MICs were not significantly influenced by high inocula and the drug was generally bactericidal. Strains producing various beta-lactamases remained susceptible to meropenem but some isolates producing high levels of chromosomally-mediated enzymes showed an inoculum effect only at 10(7) cfu/ml. Meropenem demonstrated antagonism with several other beta-lactams against strains producing Type I cephalosporinases. Susceptibility tests performed on agar and in broth produced very similar meropenem results. Imipenem and meropenem shared a high degree of cross-susceptibility as measured by dilution test methods. Disc diffusion (10-micrograms disc) regression-line correlations with meropenem MICs are reported with two possible sets of interpretive criteria, using meropenem breakpoints of less than or equal to 2 and less than or equal to 4 mg/l.

Anti-Bacterial Agents↗

Meropenem: clinical response in relation to in vitro susceptibility.

OBJECTIVE: To collate the clinical response and pathogen eradication rates for meropenem monotherapy with in vitro susceptibility of the causative pathogens. METHODS: Data were compiled from 17 randomized clinical studies that compared meropenem monotherapy with standard treatment options, often combinations. A total of 4906 pathogens from lower respiratory tract, intra-abdominal, obstetric/gynecological, skin/soft tissue, meningitis, or pediatric infections were assessed. Of these, 3713 pathogens (1963 meropenem, 1750 comparators) were evaluable. RESULTS: The overall rates of satisfactory clinical response (cure or improvement) and pathogen eradication (eradication or presumed eradication) at the end of therapy were similar with meropenem (93% for both responses) and the comparators (92%), as were the rates in each infection type. For each pathogen, the clinical response and eradication rates with meropenem were similar across the minimum inhibitory concentration (MIC) range of < or = 0.25 to 4 mg/L. Overall, a satisfactory clinical response occurred in 93% (1580 of 1708) of infections caused by nonfastidious pathogens with MICs < or = 4 mg/L and in 84% (16 of 19) of those with an MIC of 8 mg/L. Pathogen eradication rates were similar (93 and 79%, respectively). A similar profile was observed for fastidious pathogens. The high rates of satisfactory clinical response and pathogen eradication produced by meropenem in each type of infection were generally independent of the causative pathogen, whether Gram-positive or -negative aerobe or anaerobe or when occurring as mono- or polymicrobial infections. CONCLUSIONS: The attractive in vitro profile of meropenem translates into good clinical efficacy. The National Committee for Clinical Laboratory Standards has now defined meropenem MIC breakpoints for nonfastidious aerobes or anaerobes as < or = 4 (susceptible), 8 (intermediate) and > or = 16 mg/L (resistant), respectively. The susceptibility breakpoint for Streptococcus spp. (excluding Streptococcus pneumoniae) is < or = 0.5 mg/L and, since meropenem is indicated for the treatment of meningitis, the susceptibility breakpoint for S. pneumoniae and Haemophilus influenzae is < or = 0.25 and < or = 0.5 mg/L, respectively. Meropenem monotherapy is therefore a valid option for the initial empirical treatment of a range of serious infections caused by single or multiple bacterial pathogens.

Bacteria↗

Clinical and economic benefits of a meropenem dosage strategy based on pharmacodynamic concepts.

PURPOSE: The clinical and economic outcomes of a meropenem dosage strategy based on pharmacodynamic concepts are retrospectively reviewed. METHODS: The medical records of all patients receiving at least one day of meropenem at a large teaching hospital during 2002 were reviewed. Patients were included if they were clinically evaluable, had no prior successful antibiotic therapy, and received a meropenem dosage appropriate for renal function. Clinical outcomes were evaluated by the rate of response (days to normalization of temperature or lymphocyte count) and success rate. A cost-minimization analysis was performed from the hospital's perspective for level 1, 2, and 3 costs. The average wholesale price of meropenem for 2002 and the cost for one hospital day at our institution were used to calculate economic outcomes. RESULTS: Of the 136 patients identified as receiving at least one dose of meropenem, 85 met inclusion criteria, of whom 45 received meropenem 500 mg every six hours and 40 received meropenem 1000 mg every eight hours. No significant differences in demographics, site of infection, meropenem-related length of stay, or rate of response were found. Clinical success rates were similar between groups (p = 0.862). Patients taking the 500-mg regimen received less meropenem during treatment than those in the 1000-mg group (13 g versus 18 g, respectively) (p = 0.012). Median level 1 and 2 costs were significantly lower for the 500-mg regimen (p = 0.009 and p = 0.008, respectively). Level 3 costs were not significantly different. CONCLUSION: A pharmacodynamically designed meropenem dosage strategy of 500 mg every six hours yielded similar clinical outcomes to a regimen of 1000 mg every eight hours and reduced the daily drug acquisition costs associated with antibiotic therapy.

Adult↗

Meropenem: in-vitro activity and kinetics of activity against organisms of the Bacteroides fragilis group.

Meropenem was compared with imipenem and nine other antimicrobial agents, against 101 strains of the Bacteroides fragilis group. Meropenem was active against all strains tested, and its activity was similar to, and in many cases better than, that of imipenem. The activity of meropenem was similar to that of metronidazole, and greater than that of the other antimicrobial agents tested. The bactericidal activity of meropenem against B. fragilis was impressive, since the MBC to MIC ratios were no greater than two. The bactericidal activity was confirmed by time-killing curve assays with two strains which showed that meropenem was rapidly bactericidal and reduced the initial inoculum significantly during the first 4-6 h. The postantibiotic effect of meropenem (2-4 h) and a sub-inhibitory concentration of 1/4 x MIC suggested that meropenem interferes with the normal growth of B. fragilis, even when administered concentrations fall below the MIC. MICs of meropenem were affected minimally by the pH of the medium or by an increase in inoculum size. Meropenem continued to have good activity against a B. fragilis strain that had been induced for the production of cephalosporinase. The in-vitro data presented in this paper indicate that meropenem is a promising antimicrobial agent which may be useful in the treatment of problematic mixed infections.

Bacteroides fragilis↗

Meropenem versus cefuroxime plus gentamicin for treatment of serious infections in elderly patients.

In this multicenter study, the efficacy of and tolerability for meropenem were compared with those for the combination of cefuroxime-gentamicin (+/- metronidazole) for the treatment of serious bacterial infections in patients > or = 65 years of age. A total of 79 patients were randomized; thirty-nine received meropenem (1 g/8 h), and 40 received cefuroxime (1.5 g/8 h) plus gentamicin (4 mg/kg of body weight daily) for 5 to 10 days. Metronidazole (500 mg/6 h) could be added to the cefuroxime-gentamicin regimen for the treatment of intra-abdominal infections (n = 10). Seventy patients were evaluable for clinical efficacy; the primary diagnoses were as follows: pneumonia in 41 patients (20 treated with meropenem, 21 treated with cefuroxime-gentamicin), intra-abdominal infection in 10 patients (7 meropenem, 3 cefuroxime-gentamicin-metronidazole), urinary tract infection (UTI) in 11 patients (6 meropenem, 5 cefuroxime-gentamicin), sepsis syndrome in 7 patients (4 meropenem, 3 cefuroxime-gentamicin), and "other" in 1 patient (cefuroxime-gentamicin). The pathogens isolated from 18 patients with bacteremia were as follows: Staphylococcus spp. (n = 2), Streptococcus spp. (n = 2), members of the family Enterobacteriaceae (n = 11), and Bacteroides spp. (n = 3). A satisfactory clinical response at the end of therapy was achieved in 26 of 37 (70%) and 24 of 33 (73%) evaluable patients treated with meropenem and combination therapy, respectively. Clinical success was achieved in 23 of 31 (74%) and 21 of 28 (75%) evaluable patients with infections other than UTIs, respectively. A satisfactory microbiological response occurred in 15 of 22 (68%) patients in the meropenem group compared with 12 of 19 (63%) treated with combination therapy. Renal failure occurred during therapy in 2 of 39 (5%) meropenem recipients compared with 5 of 40 (13%) of those treated with combination therapy. The findings in this small study indicate that meropenem is as efficacious for and as well tolerated by elderly patients as the combination of cefuroxime-gentamicin (+/- metronidazole).

Aged↗

Beta-lactamase stability and inhibitory activity of meropenem combined with a potent antibacterial activity.

The affinity of meropenem for various known types of beta-lactamases and its stability to them were tested in comparison with other beta-lactams, including imipenem. Meropenem exhibited a marked stability to all beta-lactamases tested and was only hydrolyzed by Xanthomonas maltophilia beta-lactamase, as were other beta-lactams. This was responsible for the potent antibacterial activities of meropenem against beta-lactamase-producing strains. Meropenem and imipenem had almost the same, relatively high affinity for beta-lactamases; however, they had a lower affinity than clavulanic acid for penicillin beta-lactamases and cefoxitin for cephalosporin beta-lactamases. Meropenem also had higher beta-lactamase inhibitory activity than imipenem. Meropenem inhibited type III (TEM-1), Ia Citrobacter freundii and Ic Proteus vulgaris beta-lactamases in a progressive manner. Meropenem was thought to be a potent inhibitor of various beta-lactamase because of its ability to form stable enzyme-meropenem acyl-complexes. Meropenem generally exhibited a lower induction potential than imipenem against five clinical isolates of C. freundii, Enterobacter cloacae and Pseudomonas aeruginosa, but its induction potential was higher than that of ceftazidime. Meropenem induced beta-lactamases at concentrations above the MIC.

Bacteria↗

Meropenem: a new carbapenem antimicrobial.

OBJECTIVE: To describe and then compare an investigational carbapenem antibiotic, meropenem, with the only currently available antibiotic in this class, imipenem/cilastatin. DATA IDENTIFICATION: An English language search using MEDLINE (1988-1993); Abstracts of the 31st Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC), 1991; and Abstracts of the 32nd ICAAC, 1992. STUDY SELECTION: All current scientific publications were reviewed for study design and quality. Emphasis was placed on susceptibility and pharmacokinetic analysis. Phase 3 clinical trials are now being completed and have only been published in abstract form. Hence, conclusions derived regarding efficacy were tempered. RESULTS: Meropenem is active against a broad spectrum of gram-positive and -negative pathogens including beta-lactamase producers. Meropenem appears to be two- to fourfold less active than imipenem against gram-positive organisms. Meropenem is two- to fivefold more active against enterobacteriaceae. The two compounds appear to be equally active against Pseudomonas aeruginosa. Pharmacokinetic disposition is also similar for imipenem and meropenem. Meropenem may exhibit greater tissue penetration. Meropenem is not labile to renal hydrolysis and can be administered without a competitive antagonist of dihydropeptidase, such as cilastatin. In clinical trials, meropenem appears to be as safe and effective as imipenem/cilastatin or ceftazidime in the treatment of infections involving soft tissue, urinary tract, upper respiratory tract, abdominal processes, and febrile neutropenic episodes. CONCLUSIONS: Meropenem is comparable to imipenem in terms of in vitro susceptibility pattern and pharmacokinetic disposition. Overall, meropenem seems to offer promise as the second of the carbapenem class of antibiotics. Clinical data are preliminary, and further data are needed.

Clinical Trials as Topic↗

Pharmacokinetics of meropenem in patients with renal failure and patients receiving renal replacement therapy.

Meropenem is a well established carbapenem antibacterial with a wide spectrum of activity against Gram-positive and Gram-negative bacteria, including beta-lactamase producers and Pseudomonas aeruginosa. Because of its clinical and bacteriological efficacy, meropenem is an important antimicrobial drug in the treatment of serious infections in adults and in children. Meropenem is predominately excreted unchanged in the urine, and thus dosage adjustments are necessary in patients with renal insufficiency and those undergoing intermittent haemodialysis (IHD) or various forms of continuous renal replacement therapy (CRRT), such as continuous venovenous haemodialysis, continuous venovenous haemodiafiltration (CVVHDF), continuous venovenous haemofiltration (CVVHF) or continuous ambulatory peritoneal dialysis (CAPD). The half-life of meropenem (approximately 1 hour in healthy volunteers) is prolonged up to 13.7 hours in anuric patients with end-stage renal disease. In patients receiving renal replacement therapy, half-life is influenced by drug-specific factors as well by membrane and treatment modalities (IHD, CRRT or CAPD). Plasma meropenem concentrations reach a peak of between 53 and 62 mg/L after the administration of meropenem 1g intravenously to healthy volunteers, up to 53 mg/L after meropenem 0.5g in haemodialysis patients, and between 18 and 45 mg/L after meropenem 1g during CRRT in critically ill patients. Approximately 50% of meropenem is eliminated by IHD, 25 to 50% by CVVHF and 13 to 53% by CVVHDF. Such differences are not negligible and demonstrate the great influence of the treatment modality on the elimination of the drug during renal replacement therapy. Thus, physicians run the risk of underdosing with this antimicrobial drug because of the quite different recommendations in the literature. Because of the excellent tolerability profile of meropenem, such underadministration should be avoided.

Adult↗

The Meropenem Yearly Susceptibility Test Information Collection antimicrobial susceptibility program in Spain: a 5-year analysis.

The Meropenem Yearly Susceptibility Test Information Collection program is a global study providing in vitro surveillance data on antimicrobial susceptibility in centers prescribing meropenem. This study summarizes data on the activity of meropenem and 5 comparators against 4022 clinical isolates from 7 centers in Spain (1999-2003). Those bacteria intrinsically resistant to meropenem were excluded. Among Enterobacteriaceae, 100% of Enterobacter spp., Citrobacter spp., and Serratia spp. were susceptible to meropenem. Escherichia coli and Klebsiella pneumoniae susceptibilities to carbapenems were 100% and > or =98%, respectively. Extended-spectrum beta-lactamase-producing Enterobacteriaceae were 3.8% of isolates, and all of them were susceptible to meropenem. Ciprofloxacin resistance in E. coli was around 20%. Meropenem and piperacillin/tazobactam were the most active agents against Pseudomonas aeruginosa. Acinetobacter baumannii were 61-90% susceptible to carbapenems, but only 6-21% susceptible to ciprofloxacin. In this period, around 100% of oxacillin-susceptible staphylococci were susceptible to meropenem. There was no significant decrease in susceptibility to the carbapenems throughout the 5-year period. The clinical use of meropenem in 7 Spanish centers did not increase bacterial resistance to this agent in the microorganisms evaluated.

Academic Medical Centers↗

Meropenem versus imipenem/cilastatin as empirical monotherapy for serious bacterial infections in the intensive care unit.

OBJECTIVE: To compare the efficacy and tolerability of meropenem and imipenem/cilastatin as empirical monotherapy in intensive care unit (ICU) patients with serious bacterial infections. METHODS: A multicenter, open-label, randomized, parallel-group trial was conducted in Belgium, evaluating empirical monotherapy with meropenem or imipenem/cilastatin (both 1 g/8 h intravenously) in ICU patients with one or more of the following infections caused by sensitive pathogens: lower respiratory tract infection (LRTI) in ventilated patients, intra-abdominal infection or sepsis. RESULTS: The overall satisfactory clinical response rate at the end of randomized treatment was 77.0% (67/87) with meropenem and 68.1% (62/91) with imipenem/cilastatin (difference 8.9%; 95% confidence interval -4.2% to 21.9%; P = 0.185). The two drugs produced similar satisfactory clinical response rates against LRTIs: 68.3% (41/60) with meropenem versus 68.6% (35/51) with imipenem/cilastatin. Meropenem appeared to be slightly more effective against intra-abdominal infections: 95.5% (21/22) versus 76.7% (23/30), respectively. All five meropenem recipients with sepsis had a satisfactory clinical response, compared to 40.0% (4/10) of those who received imipenem/cilastatin. The overall satisfactory bacteriologic response rate was 67.1% (49/73) with meropenem and 60.3% (44/73) with imipenem/cilastatin (difference 6.9%; 95% confidence interval -8.7% to 22.4%; P = 0.389). The predominant pathogens were Escherichia coli, Enterobacter spp. and Pseudomonas aeruginosa. No incidences of drug-related nausea and vomiting were reported, but one probable drug-related seizure occurred in the imipenem/cilastatin group. CONCLUSIONS: Meropenem is at least as efficacious (clinically and bacteriologically) as imipenem/cilastatin for the empirical monotherapy of serious bacterial infections in ICU patients, and it can therefore be considered a useful option in this setting. Moreover, meropenem is well tolerated and offers several potential advantages, including greater in vitro activity against Gram-negative pathogens and the option of bolus administration.

Adult↗

In vitro activity of meropenem compared to nine other antimicrobial agents: importance of its stability when used in agar dilution systems.

The antibacterial activity of meropenem was tested against 426 clinical isolates representing a wide range of aerobic and anaerobic species. The in vitro activity of meropenem was compared with that of iminpenem, ceftazidime, cefotaxime, ciprofloxacin, piperacillin and tobramycin against aerobic isolates, and also compared with that of imipenem, metronidazole, cefoxitin, clindamycin and piperacillin against the anaerobic isolates. Meropenem exhibited an extended spectrum of activity with low minimal inhibitory concentrations (MIC) against Gram negative aerobes, anaerobes, Gram positive anaerobes and most of the Gram positive aerobes. The MIC90 of meropenem against the Enterobacteriaceae ranged from 0.03 mg/l to 0.125 mg/l. Meropenem was very active against extended spectrum beta lactamase producing Klebsiella pneumoniae, most Acinetobacter species, Pseudomonas aeruginosa, Clostridium difficile (MIC90 of 1.0 mg/l), Clostridium perfringens and other Clostridium species. Even though imipenem exhibited better activity against the coagulase negative staphylococci, meropenem still had MIC's which were less than the break point (8.0 mg/l). The stability of meropenem in agar was determined indirectly by plotting the geometric mean MIC of control strains over a period of two weeks. Mean MIC of six control strains for meropenem was 0.05 mg/l and remained constant over 10 days, whereas the mean MIC of imipenem rose to 0.24 mg/l after two days and to 3.4 mg/l after 10 days. Meropenem was therefore far more stable in agar than imipenem. This has implications for laboratories using agar dilution as it requires less frequent plate preparation and decreased labour costs.

Agar↗

Comparison of antibacterial activities of meropenem and six other antimicrobials against Pseudomonas aeruginosa isolates from North American studies and clinical trials.

The in vitro activity of meropenem was compared with those of six other antimicrobials against up to 1,182 clinical isolates of Pseudomonas aeruginosa from 16 North American centers by means of standardized controlled methods. Meropenem was the most active drug. These isolates were less frequently resistant to meropenem (4.2%) than to imipenem (12.5%), ceftazidime (15.6%), piperacillin (21%), ciprofloxacin (16%), tobramycin (26%), or gentamicin (29.8%). Of 147 imipenem-resistant P. aeruginosa isolates, 43.8% were susceptible to meropenem, and 26.9% additional isolates were moderately susceptible to meropenem. Of 49 meropenem-resistant (MIC, > or = 16 micrograms/mL) isolates, 85.7% were also imipenem-resistant, and 24% to 79% were resistant to other antimicrobials. Meropenem MICs were lower than imipenem and ceftazidime MICs for 92 P. aeruginosa isolates from meropenem clinical trials. Carbapenem MICs of > or = 16 micrograms/mL for selected P. aeruginosa isolates from meropenem clinical trials were associated with loss of the approximately 45-kD outer-membrane protein and/or production of type I beta-lactamases. No metallo-beta-lactamases (e.g., "efficient" carbapenemases) were detected.

Anti-Bacterial Agents↗

Activity of meropenem, against gram-positive bacteria.

A new carbapenem antibiotic, meropenem, was shown to be active against a large number of Gram-positive bacteria. The drug inhibited penicillinase-positive and -negative, methicillin-susceptible staphylococci equally well. Among the comparative antimicrobials examined, only N-formimidoyl-thienamycin (imipenem) was two to four times more active than meropenem. Compared with vancomycin or methicillin, meropenem was 10-20 times more active. Strains of 11 species of streptococci were highly susceptible to meropenem; the geometric mean MICs of the drug for these species ranged from 0.01 to 0.04 mg/l. The agent, however, only had moderate activity against Enterococcus faecalis (mean MIC 5 mg/l) and Ent. faecium (mean MIC 11.6 mg/l). Among Corynebacterium jeikeium, strains were encountered that showed susceptibility to meropenem but resistance to imipenem and other beta-lactams. Strains of other corynebacteria, Rhodococcus equi, Erysopelothrix rhusiopathiae, Listeria monocytogenes, and Bacillus spp. all were highly susceptible to meropenem (mean MICs 0.04-0.17 mg/l). Although methicillin-resistant staphylococci were inhibited by concentrations of 1-2 mg/l of meropenem in agar dilution tests, such strains showed heteroresistance in population studies, as is typical for all beta-lactam antibiotics. In addition, the biochemical correlate of methicillin-resistance, penicillin-binding protein 2', showed low affinity for meropenem, similar to that for imipenem. Meropenem was as bactericidal as imipenem and comparative bactericidal antimicrobials in killing-curve experiments. Strains of Ent. faecium, C. jeikeium, and L. monocytogenes were killed at a slower rate than streptococci or staphylococci.

Bacterial Proteins↗

Therapeutic activity of meropenem in experimental infections.

Meropenem and comparative antibiotics were evaluated in five models of infection. All antibiotics were administered parenterally; imipenem was used in combination with cilastatin but meropenem and other agents were given alone. Generalized infections in mice caused by Staphylococcus aureus, Streptococcus pneumoniae, Escherichia coli, Serratia marcescens, Proteus mirabilis or Pseudomonas aeruginosa all responded to low doses of meropenem or imipenem. Immunocompromised mice infected with Ps. aeruginosa responded to slightly higher doses of meropenem or gentamicin but required four to seven times the dose of other agents. Those given a greater challenge of Ps. aeruginosa were treated most successfully by meropenem. Treatment with meropenem, imipenem or ceftazidime caused significant reductions of E. coli in the urinary bladder and kidneys of mice challenged per urethram. Infection with Ps. (Xanthomonas) maltophilia localized to the subcutaneous neck tissue of guinea pigs was also treated successfully. Lung infections caused by Ps. aeruginosa in guinea pigs were treated effectively by meropenem, imipenem, and ceftazidime at the dose of 10 mg/kg but only meropenem eradicated bacteria from all the tissues examined. These results demonstrate that meropenem has excellent antibacterial activity in vivo in both normal and immunocompromised animals and in some models of infection is superior to imipenem.

Animals↗