Antibiotic group of carbapenems, for parenteral use. It has bactericidal activity by inhibiting bacterial cell wall synthesis. The bactericidal action of meropenem against a broad range of aerobic and anaerobic bacteria due to the high capacity meropenem penetrate cell walls of bacteria, a high level of stability to most dianabol before and after beta-lactamases and substantial affinity for binding proteins penicillin.
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, cell wall, which ultimately can cause damage and destruction of the bacteria.
The bactericidal and bacteriostatic concentrations do not differ. The spectrum of activity of 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 (penitsillinazoneprodutsiruyuschie and penitsillinazoprodutsiruyuschie), Klebsiella pneumoniae, Neisseria meningitidis, Pseudomonas aeruginosa, Proteus mirabilis. Anaerobic bacteria: . Bacteroides fragilis, Bacteroides thetaiotaomicron, Peptostreptococcus spp Regarding following microorganisms meropenem effective in vitro, however, clinical efficacy in diseases caused by these pathogens, has not been proven:Gram-positive aerobes: of Staphylococcus epidermidis (penitsillinazoneprodutsiruyuschie and penitsillinazoprodutsiruyuschie [methicillin-sensitive]). Gram-negative aerobes: of Acinetobacter spp, the Aeromonas hydrophila, of Campylobacter jejuni, Citrobacter diversus, Citrobacter freundii, of Enterobacter. cloacae, Haemophilus influenzae (ampicillin-resistant, penitsillinazoneprodutsiruyuschie strains), Hafnia alvei, Klebsiella oxytoca, Moraxella catarrhalis (penitsillinazoneprodutsiruyuschie and penitsillinazoprodutsiruyuschie), Morganella morganii, Pasteurella multocida, Proteus vulgaris, Salmonella spp., Serratia marcescens, Shigella spp., Yersinia enterocolitica. Anaerobic bacteria: of Bacteroides distasonis, of Bacteroides ovatus, of Bacteroides uniformis, of Bacteroides ureolyticus, of Bacteroides vulgatus, of Clostridium difficile-, of Clostridium perfringens, Eubacterium lentum, by Fusobacterium spp, Prevotella bivia, Prevotella intermedia, Prevotella melaninogenica, of Porphyromonas asaccharolytica, of Propionibacterium acnes..
When administered intravenously, 250 mg for 30 minutes in the maximum concentration (C max ) is 11 micrograms / ml for a dose of 500 mg – 23 mg / ml for a dose of 1 g – 49 ug / ml. With increasing doses from 250 mg to 2 g of meropenem clearance decreases from 287 to 205 ml / min.
With intravenous bolus over 5 minutes 500 mg meropenem Sshah is 52 ug / ml, 1 g of -112 pg / ml. Contact with blood plasma proteins – 2%. It penetrates in most tissues and body fluids including in the cerebrospinal fluid of patients with bacterial meningitis, achieving concentrations in excess of the required to inhibit most 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 microbiologically inactive metabolite.
The half-life of 1 hour, for children up to 2 years – 1.5 – 2.3 hours pharmacokinetics of meropenem in children and adults are similar,. in the dose range of 10-40 mg / kg of a linear dependence of pharmacokinetic parameters.
excreted by the kidneys – 70% unchanged for 12 hours meropenem concentration in urine exceeding 10 mcg / ml is maintained for 5 to 500 hours after administration. mg.
In patients with renal insufficiency, dianabol before and after the clearance of meropenem correlates with creatinine clearance. Such patients require dose adjustment.
In elderly patients, a decrease in clearance of meropenem correlates with the age-related decrease in creatinine clearance. The half -. 1.5 hours Meropenem appear in hemodialysis.
Infectious-inflammatory diseases (monotherapy or in combination with other antimicrobial drugs) caused by susceptible pathogens to meropenem:
- lower respiratory tract infections (including pneumonia, including hospital);
- abdominal infections (complicated appendicitis, peritonitis, pelvioperitonit);
- urinary tract infection (pyelonephritis, pyelitis);
- infections of skin and soft tissue (including erysipelas, impetigo, secondarily infected dermatitis);
- pelvic infections (including endometritis);
- bacterial meningitis;
- empirical treatment (monotherapy or in combination with anti-viral or anti-fungal medicines) for suspected infection in adult patients with febrile neutropenia.
Hypersensitivity to meropenem or any other beta-lactam antibiotics in history, children up to 3 months. Precautions Concurrent administration of potentially nephrotoxic drugs. Persons with complaints from the gastrointestinal tract (including colitis). Pregnancy and lactation Meropenem should not be used during pregnancy except in cases where the potential benefit of its use justifies the potential risk to the fetus. Meropenem should not be used during lactation, except in cases where the potential benefit of its use justifies the potential risk to the child. If necessary, use during lactation should consider termination of breastfeeding.
Dosage and administration:
Intravenous bolus for at least 5 minutes or by intravenous infusion for 15-30 minutes, using the corresponding dilution infusion solutions. The dose and duration of therapy shall be established depending on the type and severity of the infection and the patient’s condition.
Adults: 500 mg every 8 hours for pneumonia, urinary tract infections, infectious and inflammatory diseases of the pelvic organs, skin and soft tissue infections. Meropenem appear in hemodialysis. If required prolonged treatment meropenem recommended administered dose (in accordance with the type and severity of the infection) after hemodialysis, to restore effective concentration in the blood plasma. In patients with hepatic failure there is no need to dose adjustment. In elderly patients with normal renal function or a creatinine clearance greater than 50 mL / min dose adjustment is required. 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 status patient. children under 12 years of age with a body weight over 50 kg should use the adult dose. in meningitis the recommended dose is 40 mg / kg every 8 hours.The experience of use in children with impaired renal function is not available. Preparation of solutions Meropenem intravenous bolus injection should be diluted sterile water for injection (20 ml for 1 g of meropenem), the solution concentration is about 50 mg / ml. The resulting solution is a clear liquid (colorless or light yellow). Meropenem for intravenous infusion can be diluted compatible infusion solution (50 to 200 ml). Meropenem suitable for infusion solutions:
- 0.9% sodium chloride solution
- 10% or 5% dextrose.
When breeding meropenem care should be taken aseptic and antiseptic. Divorced solution shaken before use. All vials are intended for single use only. Meropenem should not be mixed in one package with other drugs.
Side effect From the digestive system: epigastric pain, nausea, vomiting, diarrhea, constipation, anorexia, jaundice, cholestatic hepatitis, hyperbilirubinemia, increased activity of “liver” transaminases, alkaline phosphatase, lactate dehydrogenase; rarely – candidiasis of the oral mucosa, pseudomembranous colitis. Cardio-vascular system: development or exacerbation of congestive heart failure, cardiac arrest, tachy or bradycardia, decrease or increase in blood pressure, fainting, heart attack, embolism pulmonary artery branches. With urinary system: dysuria, edema, renal dysfunction (hypercreatininemia, increasing the concentration of urea in plasma), hematuria. Allergic reactions: itching, skin rash, urticaria, erythema multiforme exudative (Stevens-Johnson syndrome), angioedema, anaphylactic shock.From dianabol before and after the nervous system: headache, dizziness, paraesthesia, insomnia, drowsiness, irritability, agitation, anxiety, depression, impaired consciousness, hallucinations, epileptiform seizures, convulsions.Laboratory findings: eosinophilia, neutropenia, leukopenia, rarely – agranulocytosis, hypokalemia, leukocytosis, reversible thrombocytopenia, reduction in partial thromboplastin time, and anemia. Local reactions: inflammation, phlebitis, thrombophlebitis, pain at the injection site. Other: a positive direct or indirect Coombs test, hypervolemia, shortness of breath, vaginal candidiasis.
possible overdose during treatment, especially in patients with impaired renal function. Treatment: symptomatic therapy. Normally, there is a rapid elimination of the drug by the kidneys. In patients with impaired renal function hemodialysis effectively remove meropenem and its metabolite.
Interaction with other drugs
Drugs that block tubular secretion, slows down and increases the concentration of meropenem in plasma.
It can reduce the concentration of valproic acid in blood plasma.
Treatment of patients with liver disease should be carried out under the close supervision of the activity of “liver” transaminases and bilirubin. During treatment possible development of resistance of pathogens, and therefore the long-term treatment is carried out under the permanent control of the spread of drug-resistant strains.
In patients with gastrointestinal disease, particularly colitis, it is necessary to take into account the possibility of pseudomembranous colitis (a toxin produced by Clostridium difficile, is one a major cause of colitis associated with antibiotics), the first symptom of which can serve the development of diarrhea during treatment.
when using meropenem as monotherapy in patients who are in critical condition, with diagnosed infection of the lower respiratory tract, caused by Pseudomonas aeruginosa, or suspected it is recommended to regularly perform a test of the pathogen sensitivity to meropenem.
Experience of the drug in children with neutropenia, with primary or secondary immunodeficiencies not.
Effects on ability to drive the car and machinery
during treatment, to determine the individual response to meropenem, patients should refrain from driving motor vehicles and other activities that require high concentration and speed of psychomotor reactions. steroids for sale