Among the known beta-lactam antibiotics has the most highly active against most aerobic and anaerobic gram-positive and gram-negative bacteria. It is active against gram-positive aerobes: of Bacillus spp, of Corynebacterium diphtheriae, of Enterococcus liquifaciens, of Enterococcus avium, of Enterococcus faecalis, of Listeria monocytogenes, of Lactobacillus spp,.. asteroides Nocardia, dianabol side effects for men Staphylococcus aureus (including penitsillinazoprodutsiruyuschih), Staphylococcus spp . (coagulase-negative), including: S taphylococcus saprophyticus, Staphylococcus capitis, Streptococcus pneumoniae (including strains resistant to penicillin), Streptococcus agalactiae, Streptococcus pyogenes, Streptococcus equi, Streptococcus bovis, Streptococcus mitis, Streptococcus viridans, Streptococcus salivarius, Streptococcus morbillorum, Streptococcus spp. ( group G and the F), of Rhodococcus equi ; Gram-negative aerobes: Achromobacter xylosoxidans, of Acinetobacter anitratus, of Acinetobacter Iwoffii, of Acinetobacter baumannii, the Aeromonas hydrophila, the Aeromonas sorbria, the Aeromonas caviae, of Alcaligenes faecalis, of Bordetella bronchiseptica, of Brucella melitensis, of Campylobacter coli, of Campylobacter jejuni, Citrobacter freundii , Citrobacter diversus, Citrobacter amalonaticus, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae, Escherichia coli, Gardnerella vaginalis, Haemophilus influenzae (including beta-lactamase and ampicillin strains),Haemophilus parainfluenzae, Haemophilus ducreyi, Helicobacter pylori, Neisseria meningitidis, Neisseria gonorrhoeae (including strains of beta-lactamase are resistant to penicillins and spectinomycin), Hafhia alvei. Klebsiella pneumoniae, Klebsiella aerogenes, Klebsiella ozaenae, Klebsiella oxytoca, Moraxella catarrhalis, Morganella morganii, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Providencia alcalifaciens, Pasteurella multocida, Pseudomonas shigelloides, Pseudomonas aeruginosa , Pseudomonas putida, Pseudomonas alcaligenes, Burkholderia cepacia, Pseudomonas fluorescens, Pseudomonas stutzeri, Stenotrophomonas, Salmonella spp., including Salmonella typhi, Serratia marcescens, Serratia liquifaciens , Serratia spp., Shigella sonnei, Shigella flexneri, dysenteria of Shigella, of Vibrio cholerae, of Vibrio parahaemolyticus, of Vibrio vulnificus, of Yersinia enterocolitica ; anaerobic bacteria:of Actinomyces israelii, of Bacteroides spp. (including Bacteroides fragilis, Bacteroides vulgatus, Bacteroides variabilis , Bacteroides pneumosintes, Bacteroides coagulans, Bacteroides uniformis, Bacteroides distasonis , of Bacteroides ovatus, of Bacteroides thetaiotaomicron), Prevotella spp. (including Prevotella melaninogenica, Prevotella buccae, Prevotella denticola, Prevotella levii ), of Porphyromonas spp . (including Porphyromonas asaccharolyticus), Bifidobacterium spp., Clostridium perfringens, Clostridium difficile, Clostridium sporogenes, Clostridium cadaveris, Clostridium sordellii, Clostridium butyricum, Clostridium clostridiiformis, Clostridium tetani, Eubacter lentum, Eubacter aerofaciens, Fusobacterium mortiferum, Fusobacterium necrophorum, Mobiluncus curtisii, Mobiluncus mulieris, Peptostreptococcus anaerobius , Peptostreptococcus micros, Peptostreptococcus saccharolyticus, Peptococcus magnus, Peptococcus prevotii, Propionibacterium acne, Propionibacterium avidium, Propionibacterium granulosum.
For intravenous (i / v) administration of 250 mg for 30 minutes maximum concentration), C max – 11 ug / ml for a dose of 500 mg – 23 mg / ml, 1 g – 49 ug / ml (the absolute pharmacokinetic proportional to the introduced dose C max and AUC not). By increasing the dose from 0.25 to 2 g of the clearance decreases from 287 to 205 ml / min. The on / in a bolus over 5 min 500 mg C max – 52 ug / ml, 1 g – 112 mg / ml.Communication with 2% of the plasma proteins.
It penetrates in most tissues and body fluids including in the CSF of patients with bacterial meningitis, achieving concentrations in excess of the required majority for the suppression of sensitive bacteria (bactericidal concentrations are over 0.5-1.5 hours after start of infusion). In small amounts into breast milk.
Subject to an insignificant metabolism in the liver with the formation of a single inactive metabolite. The half-life (T ½ ) – 1 hour, children under 2 years -. 1.5-2.3 hours in the dose range 10-40 mg / kg for adults and children, there is a linear dependence of the pharmacokinetic parameters. Not accumulates.
Excreted by the kidneys 70% unchanged for 12 hours. The concentration of meropenem in urine exceeding 10 mcg / ml is maintained for 5 hours after administration of 500 mg. In patients with renal insufficiency clearance to correlate with creatinine clearance (CC). In elderly patients, a decrease in clearance of meropenem correlates with age-related decline in QC; T ½ -. 1.5 hours
is displayed in hemodialysis.
The infectious-inflammatory diseases caused by susceptible pathogens: lower respiratory tract infections (including pneumonia, including hospital, infections caused by Pseudomonas aeruginosa), abdominal infections (complicated appendicitis, peritonitis, pelvioperitonit). pyelonephritis, pyelitis, skin and soft tissue infections (including erysipelas, impetigo, dianabol side effects for men secondarily infected dermatoses), dysentery, endocarditis, bacterial meningitis, sepsis, inflammatory diseases of the pelvic organs (including endometritis), suspected bacterial infection in adults with febrile episodes of neutropenia (empirical treatment).
Hypersensitivity, including to other beta-lactam antibiotics; does not apply in children younger than 3 months. (efficacy and safety have not been established). Pregnancy and lactation Safety of use during pregnancy has not been determined. Breastfeeding should be discontinued at the time of treatment.
Dosing and dose
Meropenabol should be administered as an intravenous bolus injection for at least 5 minutes, or as an intravenous infusion over 15-30 minutes.
The dosage and duration of therapy should be set depending on the type and severity of the infection and condition of the patient.
The recommended daily doses: Adults 500 mg intravenously every 8 hours with the treatment of pneumonia, urinary tract infections, gynecological infections such as endometritis, and pelvic inflammatory disease, skin and soft tissue infections. 1 g intravenously every 8 hours with the treatment of nosocomial pneumonia, peritonitis, . suspected bacterial infection in neutropenic patients and septicemia in the treatment of meningitis the recommended dosage is 2 g every 8 hours. in chronic renal insufficiency the dose adjusted according to creatinine clearance (CC): with CC 26-50 ml / min at 0.5-1 g of 2 times swirls, 10-25 ml / min – 250-500 mg 2 times a day, less than 10 ml / min -. 500 mg 1 time per day Meropenem appear in hemodialysis. If required prolonged treatment is recommended that the unit dose (determined depending on the type and severity of infection) was administered at the end of hemodialysis, to restore effective concentration in plasma. Children For children aged 3 months to 12 years, the recommended dose for intravenous administration of 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 dosage should be used for adults. In meningitis the recommended dose is 40 mg / kg every 8 hours. Meropenabol not recommended for use in children younger than 3 months.There is no experience with children with impaired liver and kidney function.
Preparation of solutions
for intravenous bolus injection should Meropenabol divorce sterile water for injection (K) ml per 500 mg meropenem). This provides a solution concentration of 50 mg / ml.
For the intravenous infusion Meropepabol divorce sterile water for injection or infusion compatible liquid and then another compatible infusion fluid (50-200 mL).
Meropenabol compatible with infusion fluids following:
– 0.9% Sodium Chloride in / infusion;
– 10% or 5% dextrose / in infusion;
– 5% dextrose / in infusion with 0.02% sodium bicarbonate,
– 0.9% sodium chloride and 5% dextrose / in infusions;
– 5% dextrose with 0.225% sodium chloride solution for the on / in infusions;
– 5% dextrose with 0.15% potassium chloride to / in infusions;
– 2.5% mannitol and 10% w / w infusions.
Meropenabol not be mixed with solutions containing other drugs.
Side effect From the digestive system : epigastric pain, nausea, vomiting, diarrhea, cholestatic hepatitis, hyperbilirubinemia, increased activity of “liver” transaminases and alkaline phosphatase, lactate dehydrogenase, rarely – oral candidiasis, pseudomembranous colitis. Cardio-vascular system : tachy or bradycardia, decrease or increase in blood pressure, development or exacerbation of congestive heart failure, syncope, myocardial infarction, thromboembolism of pulmonary artery branches, cardiac arrest. From the urinary system : dysuria, edema, renal dysfunction (hypercreatininemia, increasing concentrations of urea plasma), hematuria. Allergic reactions : itching, skin rash, urticaria, erythema multiforme exudative, angioedema, anaphylactic shock. nervous system : headache, paresthesia, insomnia, irritability, anxiety, depression, impaired consciousness, hallucinations , epileptiform seizures, convulsions. From the laboratory parameters : eosinophilia, neutropenia, leukopenia, rarely – agranulocytosis, reversible thrombocytopenia, reduction in partial thromboplastin time. Local reactions : inflammation, thrombophlebitis, pain at the injection site. Other : a positive direct or indirect Coombs test, anemia, dyspnea, vaginal candidiasis.
Accidental overdose possible during treatment, especially in patients with impaired renal function. Treatment of an overdose should be symptomatic. Normally, there is a rapid elimination of the drug in hemodialysis.
Interaction with other medications
compatible with 0.9% sodium chloride, 5% or 10% dextrose solution, 5% dextrose and 0.02% sodium bicarbonate, 0.9% sodium chloride and 5% dextrose, 5 % dextrose solution with 0.225% sodium chloride, 5% dextrose solution with 0.15% potassium chloride, 2.5% and 10% mannitol solution.
meropenem compatibility with other drugs, other than the above is not installed. Therefore, meropenem and solutions should not be mixed or added to solutions containing other drugs.
Drugs that block tubular secretion, slow excretion and increase in the plasma concentration of meropenem.
Patients with a history of dianabol side effects for men hypersensitivity to carbapenems, penicillins or other. Beta-lactam antibiotics may demonstrate hypersensitivity to meropenem.
Treatment of patients with liver disease should be carried out under the close supervision of the activity of “liver” transaminases and bilirubin.
In the course of treatment may develop stability agents, and therefore the long-term treatment is carried out under the permanent control of the spread of drug-resistant strains. Individuals with complaints of the gastrointestinal tract, especially suffering from colitis, it is necessary to take into account the possibility of pseudomembranous colitis (a toxin produced by Clostridium difficile, is a major cause of colitis associated with antibiotics), the first symptom of which can serve the development of diarrhea pas a background of treatment.
Monotherapy known or suspected infections of the lower respiratory tract of heavy flow caused by Pseudomonas aeruginosa, recommended regular determination of susceptibility.