Meronem powder for solution for intravenous administration vials 10 pcs
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Active ingredients
Meropenem
Release form
Powder
Composition
1 bottle contains: Meropenem trihydrate 1.14 g, which corresponds to the content of Meropenem 1 g. Excipients: sodium anhydrous carbonate - 208 mg.
Pharmacological effect
An antibiotic from the group of carbapenems for parenteral use, resistant to human dehydropeptidase-1 (BPH-1), does not require additional administration of the BPH-1 inhibitor. Meropenem has a bactericidal effect due to the effect on the synthesis of the bacterial cell wall. The potent bactericidal action of meropenem against a broad spectrum of aerobic and anaerobic bacteria is due to the high ability of bacteria to penetrate the cell wall, a high level of resistance to most β-lactamase, and significant affinity for penicillin-binding proteins (BSP). The minimum bactericidal concentrations (MBC) are usually the same as the minimum inhibitory concentrations (MIC). For 76% of the bacterial species tested, the MBC / MIC ratio was 2 or less. Meropenem is stable in pathogen sensitivity tests. In vitro tests show that meropenem acts synergistically with various antibiotics. It has been shown in vitro and in vivo that meropenem has a post-antibiotic effect. The only recommended criteria for susceptibility to meropenem are based on the pharmacokinetics of the drug and on the correlation of clinical and microbiological data — the diameter of the zone and the MIC determined for the respective pathogens. The spectrum of antibacterial activity of meropenem, determined in vitro, includes almost all clinically significant gram-positive and gram-negative aerobic and anaerobic microorganisms. The drug is active in the case of the aerobic . h. Staphylococcus saprophyticus, Staphylococcus capitis, Staphylococcus cohnii, Staphylococcus xylosus, Staphylococcus warneri, Staphylococcus hominis, Staphylococcus simulans, Staphylococcus intermedius, Staphylococcus sciuri, Staphylococcus lugdenensis, Streptococcus pneumoniae (sensitive and penicillin-resistant), Streptococcus agalactiae, Streptococcus pyogenes, Streptococcus equi, Streptococcus bovis, Streptococcus mitis, Streptococcus mitior, Streptococcus milleri, Streptococcus sanguis, Streptococcus viridans, Streptococcus salivarius, Streptococcus morbillorum, Streptococcus group G, group F, Rhodococcus equi; aerobic mangleCitro , Haegeen Proteus mirabilis, Proteus vulgaris, Proteus penneri, Providencia rettgeri, Providencia stuartii, Providencia alcalifaciens, Pasteurella multocida, Plesiomonas shigelloides, Pseudom onas aeruginosa, Pseudomonas putida, Pseudomonas alcaligenes, Pseudomonas cepacia, Pseudomonas fluorescens, Pseudomonas stutzeri, Pseudomonas pseudomallei, Pseudomonas acidovorans, Salmonella spp., including Salmonella enteritidis, Salmonella typhi, Serratia marcescens, Serratia liquefaciens, Serratia rubidaea, Shigella sonnei, Shigella flexneri, Shigella boydii, Shigella dysenteriae, Vibrio cholerae, Vibrio parahaemolyticus, Vibrio vulnificus, Yersinia enterocolitica; anaerobic bacteria: Actinomyces odontolyticus, Actinomyces meyeri, Bacteroides-Prevotella-Porphyromonas spp, Bacteroides fragilis, Bacteroides vulgatus, Bacteroides variabilis, Bacteroides pneumosintes, Bacteroides coagulans, Bacteroides uniformis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides eggerthii, Bacteroides capsillosis,. Prevotella buccalis, Prevotella corporis, Bacteroides gracilis, Prevotella melaninogenica, Prevotella intermedia, Prevotella bivia, Prevotella splanchnicus, Prevotella oralis, Prevotella disiens, Prevotella rumenicola, Prevotella ureolyticus, Prevotella oris, Prevotella buccae, Prevotella denticola, Prevotella levii, Porphyromonas asaccharolyticus, Bifidobacterium spp Bilophilia wadsworthia, Clostridium perfringens, Clostridium bifermentans, Clostridium ramosum, Clostridium sporogenes, Clostridium cadaveris, Clostridium sordellii, Clostridium butyricum, Clostridium clostridiiformis, Clostridium inno cuum, Clostridium subterminale, Clostridium tertium, Eubacterium lentum, Eubacterium aerofaciens, Fusobacterium mortiferum, Fusobacterium necrophorum, Fusobacterium nucleatum, Fusobacterium varium, Mobiluncus curtisii, Mobiluncus mulieris, Peptostreptococcus anaerobius, Peptostreptococcus micros, Peptostreptococcus saccharolyticus, Peptococcus saccharolyticus, Peptococcus asaccharolyticus, Peptostreptococcus magnus, Peptostreptococcus prevotii, Propionibacterium acnes, Propionibacterium avidium, Propionibacterium granulosum. Stenotrophomonas maltophilia, Enterococcus faecium and methicillin-resistant staphylococci are resistant to the drug. Meronem has shown efficacy as monotherapy or in combination with other antimicrobial agents in the treatment of polymicrobial infections.
Pharmacokinetics
Distribution: B / in the administration of a single dose of the drug to healthy volunteers within 30 minutes results in a Cmax of approximately 11 μg / ml for a dose of 250 mg, 23 μg / ml for a dose of 500 mg and 49 μg / ml for a dose of 1 g. However there is no absolute pharmacokinetic proportional dependence on the dose administered for either Cmax or AUC. Moreover, there was a decrease in plasma clearance from 287 to 205 ml / min for doses from 250 mg to 2 g. In / in a bolus injection for 5 min of a single dose of Meronem, healthy volunteers achieve a Cmax of about 52 μg / ml for a dose 500 mg and 112 mcg / ml - for a dose of 1 g. Cmax in plasma with intravenous injection of 1 g of the drug for 2 minutes, 3 minutes and 5 minutes was 110, 91 and 94 mcg / ml, respectively. Plasma protein binding is about 2%. Meropenem penetrates well into most tissues and body fluids, incl. into the cerebrospinal fluid of patients with bacterial meningitis, reaching concentrations in excess of those required to suppress most bacteria. 6 h after i / v administration of 500 mg, meropenem plasma level decreases to 1 μg / ml or less. With repeated doses with an interval of 8 hours in patients with normal renal function, meropenem does not accumulate. Metabolism and excretion: The only metabolite meropenem is microbiologically inactive. Approximately 70% of the administered dose is excreted in the urine in unchanged form within 12 hours, after which further excretion in the urine is insignificant.A concentration of meropenem in the urine exceeding 10 μg / ml is maintained for 5 hours after a dose of 500 mg. With the administration modes of 500 mg every 8 hours or 1 g every 6 hours, no accumulation of meropenem in plasma and urine was observed in volunteers with normal liver function. In patients with normal renal function, T1 / 2 is approximately 1 hour. Pharmacokinetics in special clinical situations: Meronem's pharmacokinetic parameters in children are the same as in adults. T1 / 2 meropenem in children under 2 years old is approximately 1.5-2.3 hours, and linear pharmacokinetics are observed in the dose range of 10–40 mg / kg. Studies of the pharmacokinetics of the drug in patients with renal insufficiency showed that clearance of meropenem correlates with creatinine clearance. In such patients, dose adjustment is necessary. Studies of the pharmacokinetics of the drug in elderly patients showed a decrease in clearance of meropenem, which correlated with a decrease in creatinine clearance associated with age. Studies of the pharmacokinetics of the drug in patients with liver disease have shown that liver disease does not affect the pharmacokinetics of meropenem.
Indications
Treatment of the following infections in children and adults caused by one or several pathogens sensitive to the drug: Pneumonia (including nosocomial). Urinary system infections. Abdominal infections. Gynecological infections (such as endometritis and pelvic inflammatory diseases). Skin infections and soft tissues. Meningitis. Septicemia. Empirical therapy for suspected bacterial infection in adult patients with febrile episodes on the background of neutropenia, as monotherapy or in combination with irusnymi or antifungal drugs.
Contraindications
Hypersensitivity to the drug. Precautions should be prescribed simultaneously with potentially nephrotoxic drugs, as well as patients with dyspepsia symptoms, especially those associated with colitis.
Precautionary measures
On the part of the digestive system: abdominal pain, nausea, vomiting, diarrhea; in some cases - a reversible increase in blood levels of bilirubin, transaminases, alkaline phosphatase and LDH individually or in combination; in some cases - pseudomembranous colitis.On the part of the hemopoietic system: reversible thrombocytosis, eosinophilia, thrombocytopenia, leukopenia and neutropenia (including very rare cases of agranulocytosis). Some patients may have a positive direct or indirect Coombs test; there are also reports of reduced partial thromboplastin time. From the side of the central nervous system and peripheral nervous system: headache, paresthesia; there are reports of the development of seizures, but a causal connection with the reception of Meronem has not been established.
Use during pregnancy and lactation
The safety of Meronema during pregnancy has not been studied. Experimental studies on animals did not show any adverse effects on the developing fetus. The only adverse event identified in the study of animals on the effect of the drug on the reproductive system was the increased frequency of abortions in monkeys when given a dose 13 times higher than recommended for humans. Meronem should not be used during pregnancy, unless the potential benefits of its use justify the possible risk to the fetus. In each case, the drug must be used under the direct supervision of a physician. Meropenem is determined in breast milk of animals in very low concentrations. Meronem should not be used during lactation (breastfeeding), unless the potential benefits of its use justifies the possible risk to the child. If necessary, the use of the drug during lactation should consider stopping breastfeeding.
Dosage and administration
For adults, the dosage regimen and duration of therapy are determined depending on the type and severity of the infection and the condition of the patient. Recommend the following daily doses. In the treatment of pneumonia, urinary tract infections, gynecological infections (endometritis and inflammatory diseases of the pelvic organs), infections of the skin and soft tissues - 500 mg i / v every 8 hours. In the treatment of nosocomial pneumonia, peritonitis, suspected bacterial infection in patients with neutropenia , as well as septicemia - 1 g intravenously every 8 hours. When treating meningitis - 2 g intravenously every 8 hours. In patients with impaired renal function with a CC of 50 ml / min or less, the doses should be reduced as follows.Creatinine clearance (ml / min) Dose based on dose unit (500 mg or 1 g or 2 g) Frequency of administration 50–26 one dose unit every 12 hours 25–10 half dose unit every 12 hours less than 10 half dose units every 24 hours Meropenem displayed during hemodialysis, therefore, if further treatment is required, it is recommended that the unit dose (determined depending on the type and severity of the infection) be administered at the end of the hemodialysis procedure in order to restore the effective plasma concentration. Experience with Meronema in patients undergoing peritoneal dialysis is absent. In patients with hepatic insufficiency, there is no need for dose adjustment. Elderly patients with normal renal function or CC more than 50 ml / min do not need to adjust the dose. For children aged 3 months to 12 years, the recommended dose for intravenous administration is 10–20 mg / kg every 8 hours, depending on the type and severity of the infection, the sensitivity of the pathogen and the patient’s condition. In children weighing more than 50 kg, the same doses should be used as in adults. For meningitis, the recommended dose is 40 mg / kg every 8 hours.
Side effects
Severe side effects are rare. The following side effects were reported: Allergic reactions rarely - angioedema, anaphylactic reactions. Dermatological reactions itching, rash, urticaria. rarely, erythema multiforme (exudative), Stevens-Johnson syndrome, and toxic epidermal necrolysis. From the digestive system, abdominal pain, nausea, vomiting, diarrhea. in some cases - a reversible increase in blood levels of bilirubin, transaminases, alkaline phosphatase and LDH individually or in combination. in some cases, pseudomembranous colitis. For the hematopoietic system, reversible thrombocytosis, eosinophilia, thrombocytopenia, leukopenia and neutropenia (including very rare cases of agranulocytosis). In some patients, a positive direct or indirect Coombs test is possible. there are also reports of cases of reduced partial thromboplastin time. For the central nervous system and peripheral nervous system, headache, paresthesia. there are reports of the development of seizures, however, a causal connection with the reception of Meronem has not been established. Local reactions are inflammation, thrombophlebitis, pain at the site of administration. Effects caused by the biological effect of oral candidiasis, vaginal candidiasis.
Overdose
Accidental overdose is possible during treatment, especially in patients with impaired renal function. Treatment: conduct symptomatic therapy.Normally, the drug is rapidly eliminated by the kidneys. In patients with renal impairment, hemodialysis effectively removes meropenem and its metabolites.
Interaction with other drugs
Probenecid competes with meropenem for active tubular secretion and, thus, inhibits renal excretion of meropenem, causing an increase in its half-life and plasma concentration. Since the effectiveness and duration of action of Meronem without probenecid are adequate; co-administration of probenecid with Meronem is not recommended. The possible effect of Meronema on metabolism and protein binding of other drugs has not been studied. However, given the low binding of meropenem to plasma proteins (about 2%), it can be assumed that there should be no interaction with other drugs. Meronem was administered while taking other medications, and no adverse pharmacological interactions were noted. Meronem can reduce serum valproic acid levels. In some patients, a lower therapeutic level may be reached. However, there are no specific data on possible drug interactions.
special instructions
As with other antibiotics, when using meropenem as monotherapy in critically ill patients with known or suspected lower respiratory tract infection caused by Pseudomonas aeruginosa, regular determination of the sensitivity of the pathogen is recommended. Pseudomembranous colitis occurs with virtually all antibiotics and can vary in intensity from mild to life-threatening forms. Therefore, antibiotics should be administered with caution to persons with gastrointestinal complaints, especially to patients with colitis. It is important to keep in mind the diagnosis of pseudomembranous colitis in the case of diarrhea while taking antibiotics. Although studies have shown that the toxin produced by Clostridium difficile is one of the main causes of colitis associated with antibiotics, however, other reasons need to be kept in mind. There are clinical and laboratory signs of partial cross-sensitivity between other carbapenems and beta-lactam antibiotics, penicillins and cephalosporins.Although allergic reactions with the use of beta-lactam antibiotics were quite common, hypersensitivity reactions were rarely reported during the administration of Meronem. Before starting therapy with meropenem, it is necessary to carefully interview the patient, paying particular attention to hypersensitivity reactions to beta-lactam antibiotics in history. Meronem should be used with caution in patients with a history of similar indications. If an allergic reaction to meropenem occurs, then it is necessary to stop administering the drug and take appropriate measures. The use of Meronema in patients with liver diseases should be carried out under careful control of the level of transaminases and bilirubin. As with other antibiotics, the prevailing growth of insensitive microorganisms is possible, and therefore constant monitoring of each patient is necessary. Use in case of infections caused by methicillin-resistant staphylococcus is not recommended. Use in pediatrics: The effectiveness and tolerability of Meronema in children under the age of 3 months have not been established, so the drug is not recommended for use in children younger than 3 months. There is no experience of using the drug in pediatric practice in patients with neutropenia or with primary or secondary immunodeficiency. Experience with Meronema in children with impaired liver and kidney is not. The efficacy and tolerability of Meronema in children under the age of 3 months have not been established, so the drug is not recommended for use in children under 3 months. Influence on ability to drive motor vehicles and control mechanisms: Meronem does not affect the ability to drive a car and other equipment.