The minimum bactericidal concentration (MBC) and the minimum inhibitory concentration (MIC) are virtually indistinguishable. Interacts with receptors – specific penicillin binding proteins on the surface of the cytoplasmic membrane, inhibits the synthesis of peptidoglycan cell wall layer (as a result of structural similarity), inhibits the transferase, promotes the release of autolytic enzymes, buy deca durabolin cell wall, which ultimately can cause damage and death of bacteria. In vitro tests show meropenem synergistic effect with various antibiotics. In vitro and in vivo tests show the effect of post-antibiotic meropenem. The spectrum of antibacterial activity meropenem includes the majority of clinically significant Gram positive and Gram negative aerobic and anaerobic bacterial strains.
Gram-positive aerobes: of Enterococcus faecalis (including vancomycin-resistant strains), Staphylococcus aureus (penitsillinazoneprodutsiruyuschie and penitsillinazoprodutsiruyuschie [methicillin-sensitive]); Streptococcus agalactiae, Streptococcus pneumoniae (penicillin-susceptible only); Streptococcus pyogenes, Streptococcus spp. . viridans group of Gram-negative aerobes: Escherichia coli, Haemophilus influenzae (and penitsillinazoneprodutsiruyuschie penitsillinazoprodutsiruyuschie), Klebsiella pneumoniae, Neisseria meningitidis, Pseudomonas aeruginosa, Proteus mirabilis. Anaerobic bacteria: Bacteroides fragilis, Bacteroides thetaiotaomicron, Peptostreptococcus spr.
Meropenem is effective in vitro against the following microorganisms: Gram-positive aerobes: of Staphylococcus epidermidis (penitsillinazoneprodutsiruyuschie and penitsillinazoprodutsiruyuschie [methicillin-sensitive]). Gram-negative aerobes: of Acinetobacter spr, Aeromonas hydrophila, Campylobacter jejuni, Citrobacter diversus, Citrobacter freundii, Enterobacter cloacae, Haemophilus influenzae (. … of ampicillin-resistant, penitsillinazoneprodutsiruyuschie strains), Hafnia alvei, Klebsiella oxytoca, Moraxella catarrhalis ( penitsillinazoneprodutsiruyuschie and penitsillinazoprodutsiruyuschie), Morganella morganii, Pasteurella multocida, Proteus vulgaris, Salmonella spr, Serratia marcescens, Shigella spr, Yersinia enterocolitica Anaerobic bacteria: of Bacteroides distasonis , Bacteroides ovatus, Bacteroides uniformis, Bacteroides ureolyticus, Bacteroides vulgatus, Clostridium difficile, Clostridium perfringens, Eubacterium lentum, Fusobacterium spr., Prevotella bivia, Prevotella intermedia, Prevotella melaninogenica, Porphyromonas asaccharolytica, Propionibacterium acnes.
When administered intravenously, 250 mg for 30 minutes in the maximum concentration (C max ) is about 11 ug / ml for a dose of 500 mg of 23 ug / ml for a dose of 1000 mg about 49 mg / ml. Absolute pharmacokinetic proportional to the administered dose for the C max and AUC (area under the curve “concentration-time”) no. With increasing doses from 250 mg to 2000 mg of the plasma clearance decreases from 287 to 205 ml / min. For intravenous bolus over 5 min 500 mg C max of about 52 mg / ml, about 1000 mg 112 mg / ml. Communication with plasma proteins – 2%.
After 6 hours after intravenous administration of 500 mg meropenem plasma concentration falls below the 1 mg / ml or less.
When administered 500 mg every 8 hours and 1000 mg every 6 hours, the patient with the normal function of cumulative renal meropenem in urine and plasma was observed.
in patients with normal renal function, half-life (T?) is about 1 hour.
meropenem penetrates well in most tissues and body fluids including the cerebrospinal fluid of patients with bacterial meningitis, achieving concentrations sufficient to providing bactericidal activity against most bacteria. In small quantities into breast milk.
Meropenem undergoes slight metabolism in liver with only the inactive metabolite.
Excreted by the kidneys – 70% unchanged within 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 meropenem clearance correlates with creatinine clearance (CC). Such patients require dose adjustment. Older patients decline meropenem clearance correlates with a decrease in CC associated with age. T? -. 1.5 hours Write hemodialysis. Patients with liver pharmacokinetics meropenem unchanged.
Studies in children have shown that the pharmacokinetics of meropenem in children and in adults similar. T? Meropenem in children under 2 years of age is approximately 1.5-2.3 hours, in the dose range 10-40 mg / kg there is a linear relationship pharmacokinetic parameters.
Infectious-inflammatory diseases caused by susceptible to malaria infections, including polymicrobial infections when (as monotherapy or combination with other antibacterial, antiviral and antifungal drugs):
- lower respiratory infections (including pneumonia, including the hospital);
- Urinary tract infections (including pyelonephritis, pyelitis);
- infections of skin and soft tissue (including erysipelas, impetigo, secondarily infected dermatitis);
- intra-abdominal infections (complicated appendicitis, peritonitis, pelvioperitonit);
- pelvic infections (including endometritis);
- bacterial meningitis;
- suspected bacterial infection in adults with febrile neutropenia (empirical treatment alone or in combination buy deca durabolin with antiviral or antifungal agents).
: Hypersensitivity to any component of the drug.
Children under the age of 3 months (no data on the efficacy and tolerability).
– co-administration with nephrotoxic drugs;
– patients with colitis.
Pregnancy and lactation
Use of the drug during pregnancy is possible only when the intended benefits to the mother outweighs the potential risk to the fetus. If necessary, use during lactation should decide the issue of termination of breastfeeding.
Dosage and administration
. Intravenous Intravenous bolus: a dilution with sterile water for injection 10 ml 500 mg, 15 mg per 1000 ml for at least 5 minutes. Intravenous infusion: for 15-30 min, diluted to 50-200 mL . compatible infusion fluid Meropenem is compatible with the following fluids:
- 0.9% sodium chloride solution;
- 5-10% dextrose (glucose);
- Ekstrozy 5% solution (glucose) with 0.02% sodium bicarbonate solution;
- 5% dextrose (glucose) with 0.225% sodium chloride solution;
- 5% dextrose (glucose), with 0.15% potassium chloride;
- 2.5 and 10% mannitol solution.
Meropenem should not be mixed or added to other drugs. Dose and duration of therapy set depending on the severity of the infection and condition of the patient. The recommended dose: Adults:
- When pneumonia, urinary tract infections, pelvic infections, skin and soft tissue infections – IV, 500 mg every 8 hours;
- In nosocomial pneumonia, peritonitis, septicemia, suspected bacterial infection in neutropenic patients – intravenously at 1000 mg 3 times daily;
- When meningitis – to 2000 mg every 8 hours.meropenem.Children:
- from 3 months to 12 years (or weighing less than 50 kg) single dose intravenous – 10-20 mg / kg, 3 times a day;
- Children weighing more than 50 kg dose used for adults;
- meningitis 40 mg / kg every 8 hours.
Experience of application in children with impaired renal function is not available.
Side effects: Allergic reactions : skin rash (including erythematous rash), itching, erythema multiforme, a malignant exudative erythema multiforme (including Stevens-Johnson syndrome), urticaria, angioedema, anaphylactic shock. Nervous system : headache, dizziness, paresthesia, agitation, impaired consciousness, epileptiform seizures, convulsions. From the urinary system : dysuria, edema, renal dysfunction (hypercreatininemia, increasing urea concentration in plasma), hematuria. From the digestive system : pain in epigastric region, nausea, vomiting, diarrhea, constipation, anorexia, jaundice, candidiasis oral mucosa, pseudomembranous colitis. Laboratory findings : thrombocytosis, eosinophilia, thrombocytopenia, decreased hemoglobin, hematocrit, leukopenia, shortening of prothrombin and partial thromboplastin time, leukocytosis, hypokalemia ; hyperbilirubinemia, activity increase in alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), lactate dehydrogenase (LDH). Local reactions : inflammation, phlebitis, thrombophlebitis, pain at the injection site. Other: a positive direct or indirect Coombs test, anemia, . hypervolemia, vaginal candidiasis causal relationship with the reception of meropenem has not been established: fainting, hallucinations, depression, anxiety, irritability, insomnia, cholestatic hepatitis, heart failure, heart failure, tachycardia, bradycardia, myocardial infarction, decreased or increased blood pressure, thrombosis pulmonary embolism, dyspnoea.
In case of overdose, possible mainly in the treatment of patients with impaired renal function, symptomatic treatment. Perhaps hemodialysis.
Interaction with other drugs
Drugs that block tubular secretion, slows down and increases the concentration of meropenem in plasma.
Meropenem may reduce the concentration of valproic acid in the plasma.
Patients with a history buy deca durabolin of 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 treatment of possible development of resistance of pathogens, in this connection, long-term treatment is carried out under the permanent control of the spread of drug-resistant strains. Individuals with complaints from the gastrointestinal tract, especially in patients with colitis, you must 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 on background treatment.
monotherapy with known or suspected infections of the lower respiratory tract of heavy flow caused by Pseudomonas aeruginosa, recommended regular determination of susceptibility to meropenem.
Experience of the drug in children with neutropenia, with primary or secondary immunodeficiencies not.
During the period of treatment must be careful when driving and other lesson potentially dangerous activities which require high concentration and psychomotor speed reactions.