Active substanceMeropenemMeropenem
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  • Dosage form: & nbsppowder for solution for intravenous administration
    Composition:

    Each vial contains:

    active substance: meropenem trihydrate 0.57 g, equivalent to 0.5 g of meropenem or 1.14 g, equivalent to 1.0 g of meropenem;

    adjuvant: sodium carbonate.

    Description:

    The powder is white or white with a yellowish hue.

    Pharmacotherapeutic group:Antibiotic carbapenem
    ATX: & nbsp

    J.01.D.H.02   Meropenem

    J.01.D.H   Carbapenems

    Pharmacodynamics:

    Antibiotic for parenteral use from the group of Karabapenems, has a bactericidal action (suppresses the synthesis of the bacterial cell wall), easily penetrates the bacterial cell wall, is resistant to the action of most beta-lactamases.

    Unlike imipenem, it practically does not break down in the renal tubules with dehydropeptidase-1 (it does not need to be combined with cilastatin, a specific inhibitor of dehydropeptidase-1) and, accordingly, no nephrotoxic degradation products are formed,has a high affinity for proteins that bind penicillin.

    Bactericidal and bacteriostatic concentrations practically do not differ.

    It interacts with receptors-specific penicillin-binding proteins on the surface of the cytoplasmic membrane, inhibits the synthesis of the peptidoglycan layer of the cell wall, suppresses transpeptidase, promotes the release of autolytic enzymes of the cell wall, which eventually causes its damage and death of bacteria.

    The spectrum of antibacterial activity of meropenem includes the majority of clinically significant Gram-positive and Gram-negative aerobic and anaerobic strains of bacteria:

    Gram-positive aerobes:

    Enterococcus faecalis (including vancomycin-resistant strains). Staphylococcus aureus(penicillinase-inducing and penicillinase-producing [methicillin-sensitive]); Streptococcus agalactiae, Streptococcus pneumoniae (only penicillin-sensitive); Streptococcus pyogenes. Streptococcus spp. groups viridans.

    Gram-negative aerobes:

    Escherichia coli, Haemophilus influenzae (penicillinase-inducing and penicillin-producing), Klebsiella pneumoniae, Neisseria meningitidis. Pseudomonas aeruginosa, Proteus mirabilis.

    Anaerobic bacteria:

    Bacteroides fragilis, Bacteroides thetaiotaomicron, Peptostreptococcus spp.

    Meropenem is effective in vitro with respect to the microorganisms listed below, however, its clinical effectiveness in diseases caused by these pathogens has not been proven:

    Gram-positive aerobes:

    Staphylococcus epidermidis (penicillinase-inducing and penicillinase-producing [methicillin-sensitive]).

    Gram-negative aerobes:

    Acinetobacter spp., Aeromonas hydrophila, Campylobacter jejuni, Citrobacter-diversus, Citrobacter ffeundii, Enterobacter cloacae, Haemophilus influenzae (ampicillin-resistant, penicillinase-sparing strains), Hafnia alvei, Klebsiella oxytoca, Moraxella catarrhalis (penicillinase-inducing and penicillin-producing), Morganella morganii, Pasteurella multocida, Proteus vulgaris. Salmonella spp., Serratia marcescens. Shigella spp., Yersinia enterocolitica.

    Anaerobic bacteria:

    Bacteroides distasonis, Bacteroides ovatus, Bacteroides uniformis, Bacteroides ureolyticus, Bacteroides vulgatus, Clostridium difficile, Clostridium perfringens, Eubacterium lentum, Fusobacterium spp., Prevotella bivia, Prevotella intermedia, Prevotella melaninogenica, Porphyromonas asaccharolytica, Propionibacterium acnes.

    Pharmacokinetics:

    When intravenous (iv) 250 mg for 30 minutes, the maximum concentration (Cmax) - 11 mcg / ml, for a dose of 500 mg - 23 mcg / ml, 1 g - 49 mcg / ml (absolute pharmacokinetic proportional dependence on the administered dose for Cmax and AUC (area under the pharmacokinetic curve "concentration-time")). When the dose is increased from 0.25 to 2 g, the clearance decreases from 287 to 205 ml / min. With iv bolus administration for 5 min 500 mg Cmax - 52 mcg / ml, 1 g -112 mcg / ml. Connection with plasma proteins - 2%.

    Well penetrates into most tissues and body fluids, incl.in cerebrospinal fluid of patients with bacterial meningitis, reaching concentrations exceeding those required for suppression of the majority of bacteria (bactericidal concentrations are created 0.5-1.5 hours after the start of infusion). In small amounts penetrates into breast milk.

    Exposed to a slight metabolism in the liver with the formation of a single inactive metabolite. The half-life (T1/2) - 1 h, in children under 2 years - 1.5-2.3 hours. In the dose range of 10-40 mg / kg in adults and children, a linear dependence of pharmacokinetic parameters is observed. Do not cumulate. It is excreted by the kidneys - 70 % unchanged for 12 hours. The concentration of meropenem in the urine, exceeding 10 μg / ml, is maintained for 5 hours after administration of 500 mg. In patients with renal failure, clearance is correlated with creatinine clearance (CC). In elderly patients, a decrease in the clearance of meropenem correlates with a decrease in QC associated with age. T1/2 - 1.5 hours. It is excreted during hemodialysis.

    Indications:Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation, including in case of polymicrobial infections (as monotherapy or combination with other antibacterial, antiviral and antifungal drugs):

    - intra-abdominal infections (incl.complicated appendicitis, peritonitis, pelvioperitonitis);

    - Lower respiratory tract infections(including pneumonia, including hospital);

    - urinary tract infection (in t.ch. pyelonephritis, pyelitis);

    - infections of the skin and soft tissues (incl. rye, impetigo, secondarily infected dermatoses);

    - infections of the pelvic organs (incl.endometritis);

    - bacterial meningitis;

    - septicemia;- empirical treatment (in the form of monotoneor in combination with an antiviralor antifungal medicines) withinfection in adultstov with febrile episodes with neutropeniction;

    - the effectiveness of the drug has been proven both in monotherapy mode and in combination with other antimicrobial agents in the treatment of polymicrobial infections.

    Contraindications:

    Hypersensitivity to meropenem or other drugs of the carbapene groupin the anamnesis.

    Severe hypersensitivity(anaphylactic reactions, chamild skin reactions) to any antibacterial agent having a beta-lactam structure (ie, to penicillins or cephalosporins). Children under 3 months.

    Carefully:

    - Simultaneous administration with nephrotoxic drugs;

    - patients with colitis.

    Pregnancy and lactation:

    The use of the drug during pregnancy is possible only in cases where the intended benefit to the mother exceeds the potential risk to the fetus. If you need to use the drug during lactation, you should decide whether to stop breastfeeding.

    Dosing and Administration:

    Intravenously.

    Solution of the drug meropenem introduced by intravenous bolus injection in a flownot less than 5 minutes or by intravenousinfusion of duration from 15 minutes to 30 minutes.

    A method of preparing a solution for whithIntroduction: for making racesfor intravenous bolus injectiondrug should be dissolved sterile(5 ml per 250 mg), with a solution concentration of 50 mg / ml. To prepare a solution for intravenous infusion, the drug should be dissolved with 0.9% sodium chloride solution or 5 % solution of dextrose, with the concentration of the solution should be from 1 to 20 mg / ml.

    The dose of the drug and the duration of therapy are determined depending on the severity of the infection and the patient's condition. The following doses are recommended.

    Adults:

    - with pneumonia, urinary tract infections paths, infectious-inflammatory diseases of the pelvic organs, skin and soft tissue infections - IV, 500 mg every 8 hours;

    >- with hospital pneumonia, peritonitis, suspected bacterial infection in patients with neutropenia, septicemia - in / in, 1 g 3 times a day;

    - when meningitis - 2 g every 8 hours.

    The safety of taking a dose of 2 g in the form of a bolus injection has not been sufficiently studied.

    If the renal function is impaired, the dose is adjusted depending on the creatinine clearance:

    Creatinine clearance (ml / min)

    Dose (depending on the type of infection)

    Periodicity of introduction

    26-50

    The recommended dose

    In 12 hours

    10-25

    Half the recommended dose

    In 12 hours

    <10

    Half the recommended dose

    In 24 hours

    Meropenem is excreted in hemodialysis and hemofiltration. If continuation of treatment is required, it is recommended that the dose unit (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 concentration in the plasma. The experience of using meropenem in patients undergoing peritoneal dialysis is absent.Patients with hepatic insufficiency do not need a dose adjustment. Elderly patients with normal renal function or QA more than 50 ml / min is required to adjust the dose.

    For children:

    - at the age of 3 months. and 12 (. weighing less than 50 kg) in single dose for / in - 10-20 mg / kg every 8 hours;

    - Children weighing more than 50 kg are given doses for adults;

    - with meningitis - IV, 40 mg / kg every 8 hours.

    The safety of taking a dose of 40 mg / kg as a bolus injection has not been sufficiently studied. There is no experience of using the drug in children with liver and kidney disorders.

    Patients with hepatic insufficiency do not have the need for dose adjustment.

    Side effects:

    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 - oral candidiasis, pseudomembranous colitis.

    From the cardiovascular system: development or exacerbation of heart failure, cardiac arrest, tachy- or bradycardia, a decrease or increase in blood pressure, fainting, myocardial infarction, thromboembolism of the branches of the pulmonary artery.

    From the urinary system: dysuria, edema, renal dysfunction (hypercreatininaemia, increased urea concentration in plasma), hematuria.

    Allergic reactions: itching of the skin, skin rash, urticaria, multiforme exudative erythema, malignant exudative erythema (Stevens-Johnson syndrome), angioedema, anaphylactic shock.

    From the nervous system: headache, dizziness, paresthesia, insomnia, drowsiness, increased excitability, agitation, anxiety, depression, impaired consciousness, hallucinations, epileptiform seizures, convulsions.

    Laboratory indicators: eosinophilia, neutropenia, leukopenia, rarely - agranulocytosis, hypokalemia, leukocytosis, reversible thrombocytopenia, reduction of partial thromboplastin time.

    Local reactions: inflammation, phlebitis, thrombophlebitis, tenderness at the injection site.

    Other: false positive direct or indirect samples of Coombs, anemia, hypervolemia, dyspnea, vaginal candidiasis.

    Overdose:

    In case of an overdose, which is possible mainly in the treatment of patients with impaired renal function, symptomatic treatment is performed.Hemodialysis is possible.

    Interaction:

    Probenecid competes with meropenem for active tubular secretion and, thatIn this way, it inhibits renal excretionmeropenem, causing an increase in half-life and concentration in plasma. Since the efficiency and durationthe effect of meropenem without probenecyyes are adequate, jointProbenecida with meropenem is not recoatedis melded.

    Meropenem should not be mixed or add to other medicinal productsparatam.

    Meropenem reduces plasma concentrationvalproic acid, which can lead to a decrease in anticonvulsant effect.

    Medicines blocking tubular secretion, slow down excretion and increase concentration in plasma.

    Indirect anticoagulants

    In patients receiving antibacterial drugs, the anticoagulant effect of simultaneously taken indirect anticoagulants, including warfarin. The risk of developing this effect varies depending on the type of infection, age and general condition of the patient, so the effect of antibiotics to increase the international normalized attitude (INR) is difficult to estimate.With the simultaneous use of antibiotics with indirect anticoagulants and some time after its termination, frequent monitoring of INR is recommended.

    Special instructions:

    Patients with a history of hypertensionsensitivity to carbapenems, finescillines or other beta-lactam ancan be hypersensitiveto the meropenem.

    Against the background of the use of carbapenems, in including meropenem, was rarely reported about occurrence of seizures, it is necessary to observecaution when applying prepain patients with a lowered threshold convulsive readiness.

    Treatment of patients with neonatal diseasesshould be conducted under careful control of the activity of "hepatic" transaminases and bilirubin concentrations.

    In the process of treatment, development is possible stability of pathogens, in connection with which long-term treatment is carried out under constantcontrol of the spread ofstent strains. Patients with a complaintmi from the gastrointestinal tractthat, especially with colitis, you need to teachto develop the possibility of developmentBranotic colitis (toxin produced Clostridium difficile, is one of thenew causes of colitis associated with antibiotic), the first symptom of which can serve as the development of diarrhea in the background treatment.

    With the development of pseudomembranous colitis should cancel the drug.

    Contraindicated use of drugs that inhibit intestinal peristalsis.

    In monotherapy of a known or suspected lower respiratory tract infection of severe course caused by Pseudomonas aeruginosa, a regular determination of the sensitivity of the pathogen is recommended.

    Experience in the use of the drug in children with neutropenia, with primary or secondary immunodeficiency is not.

    There are clinical and laboratory signs of cross-allergic reactions between other carbapenems and beta-lactam antibiotics, penicillins and cephalosporins. There are rare reports of cases of hypersensitivity reactions (including fatal outcome) when using the drug meropenem, as well as other beta-lactam antibiotics (see the "Side effect" section). Before starting therapy with meropenem, the patient should be thoroughly questioned, paying special attention to the history of hypersensitivity reactions to beta-lactam antibiotics. Meropenem should be used with caution in patients with a history of such events.If there was an allergic reaction to meropenem, it is necessary to stop the introduction of the drug and take appropriate measures.

    It is not recommended to take the drug together meropenem and preparations of valproic acid. The use of the drug for infections caused by methicillin-resistant staphylococcus is not recommended.

    Effect on the ability to drive transp. cf. and fur:During the period of treatment, care must be taken when driving vehicles, mechanisms and when engaging in other potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:

    Powder for the preparation of a solution for intravenous administration of 0.5 g and 1 g.

    Packaging:

    0.5 g of active substance into a vial of colorless glass (type IUSP) with a capacity of 10 or 20 ml or 1 g of active substance in a vial of colorless glass (type I USP) with a capacity of 30 ml, ukuporenny rubber stopper with aluminum obakkoy and plastic lid.

    1 bottle together with the instruction for use is placed in a pack of cardboard.

    Storage conditions:

    Store in a dry, dark place at a temperature of no higher than 30 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-007395/10
    Date of registration:30.07.2010 / 03.04.2018
    Expiration Date:Unlimited
    The owner of the registration certificate:M. J. Biofarm Pvt. Ltd.M. J. Biofarm Pvt. Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspM.J. BIOFARM Pvt. Ltd. division of the corporation MJ Group M.J. BIOFARM Pvt. Ltd. division of the corporation MJ Group India
    Information update date: & nbsp01.05.2018
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