Imipenem+Cilastatin, 500 mg+500 mg powder
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Pharmacotherapeutic group: Antibiotic, carbapenem
Pharmacological action
Beta-lactam antibiotic of broad spectrum. Inhibits the synthesis of the bacterial cell wall and has a bactericidal effect against a wide range of Gram-positive and Gram-negative microorganisms, aerobic and anaerobic.
Imipenem is a derivative of thienamycin and belongs to the group of carbapenems.
Cilastatin sodium inhibits dehydropeptidase, the enzyme that metabolizes imipenem in the kidneys, which significantly increases the concentration of unchanged imipenem in the urinary tract. Cilastin has no intrinsic antibacterial activity and does not inhibit the beta-lactamase of bacteria.
It is active against Pseudomonas aeruginosa, Staphylococcus aureus, Streptococcus faecalis and Bacteroides fragilis.
Resistant to degradation by bacterial beta-lactamase, making it effective against many microorganisms such as Pseudomonas aeruginosa, Serratia spp. and Enterobacter spp. which are resistant to most beta-lactam antibiotics.
The antibacterial spectrum includes virtually all clinically relevant pathogens.
Active against Gram-negative aerobic bacteria: Achromobacter spp, Acinetobacter spp. (formerly Mima – Herellea), Aeromonas hydrophila, Alcaligenes spp., Bordetella bronchicanis, Bordetella bronchiseptica, Bordetella pertussis, Brucella melitensis, Campylobacter spp., Capnocytophaga spp, Citrobacter spp. (including Citrobacter diversus, Citrobacter freundii), Eikenella corrodens, Enterobacter spp. Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae), Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae (including beta-lactamase producing strains), Haemophilus parainfluenzae, Hafnia alvei, Klebsiella spp. (including Klebsiella oxytoca, Klebsiella ozaenae, Klebsiella pneumoniae), Moraxella spp, Morganella morganii (formerly Proteus morganii), Neisseria gonorrhoeae (including penicillinase-producing strains), Neisseria meningitidis, Yersinia spp.Yersinia multocida, Yersinia enterocolitica, Yersinia pseudotuberculosis; Plesiomonas shigelloides, Proteus spp. (including Proteus mirabilis, Proteus vulgaris), Providencia spp. Providencia alcalifaciens, Providencia rettgeri (formerly Proteus rettgeri), Providencia stuartii), Pseudomonas spp. (including Pseudomonas aeruginosa, Pseudomonas fluorescens, Pseudomonas pseudomallei, Pseudomonas putida, Pseudomonas stutzeri), Salmonella spp. (including Salmonella typhi), Serratia spp. (including Serratia marcescens, Serratia proteamaculans), Shigella spp, Enterococcus faecalis, Erysipelothrix rhusiopathiae, Listeria monocytogenes, Nocardia spp., Pediococcus spp, Staphylococcus aureus (including penicillinase-producing strains), Staphylococcus epidermidis (including penicillinase-producing strains), Staphylococcus saprophyticus, Streptococcus agalactiae, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus group C, Streptococcus group G, green streptococci including alpha- and gamma-hemolytic strains); Gram-negative anaerobic bacteria: Bacteroides spp. (including Bacteroides distasonis, Bacteroides fragilis, Prevotella melaninogenica (formerly Bacteroides melaninogenicus), Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides uniformis, Bacteroides vulgatus), Bilophila wadsworthia, Fusobacterium spp, including (Fusobacterium necrophorum, Fusobacterium nucleatum), Porphyromonas asaccharolytica (previously Bacteroides asaccharolyticus), Prevotella bivia (previously Bacteroides bivius), Prevotella disiens (previously Bacteroides disiens), Prevotella intermedia (previously Bacteroides intermedius), Veillonella spp.; gram positive anaerobic bacteria: Actinomyces spp, Bifidobacterium spp., Clostridium spp. (including Clostridium perfringens), Eubacter spp., Lactobacillus spp, Microaerophilic streptococcus, Mobiluncus spp, Peptococcus spp, Peptostreptococcus spp, Propionibacterium spp. (including Propionibacterium acne); other microorganisms: Mycobacterium fortuitum, Mycobacterium smegmatis.Some Staphylococcus spp. (resistant to methicillin), Streptococcus spp. (group D), Stenotrophomonas maltophilia, Enterococcus faecium and some strains of Pseudomonas cepacia are not sensitive to imipenem.
It is effective against many infections caused by bacteria resistant to cephalosporins, aminoglycosides, penicillins. In vitro it acts synergistically with aminoglycosides against some strains of Pseudomonas aeruginosa.
Pharmacokinetics
The bioavailability of imipenem is 95% and that of cilastatin 75% when administered by injection.
The binding to plasma proteins of imipenem is 20%, that of cilastatin – 40%. Cmax of imipenem when administered v/v in a dose of 250, 500 or 1000 mg for 20 min is 14-24, 21-58 and 41-83 µg/mL, respectively; when administered v/m in 500 or 750 mg is 10 and 12 µg/mL, respectively. Cmax of cilastatin when administered v/v in a dose of 250, 500 or 1000 mg for 20 min is 15-25, 31-49 and 56-80 µg/mL; when administered v/v in 500 or 750 mg is 24 and 33 µg/mL, respectively.
It is rapidly and well distributed in most tissues and body fluids. The highest concentrations are achieved in pleural effusions, peritoneal and interstitial fluids, and reproductive organs. In low concentrations, it is found in CSF. Vd in adults is 0.23-0.31 l/kg, in children 2-12 years old – 0.7 l/kg, in newborns – 0.4-0.5 l/kg.
Blocking of tubular secretion of imipenem by cilastatin leads to inhibition of its renal metabolism and accumulation in the urine in unchanged form. Cilastatin is metabolized to N-acetyl compound.
When administered in m/m, the T1/2 of imipenem is 2-3 h. When administered intravenously, T1/2 of imipenem and cilastatin is 1 h in adults, 1-1.2 h in children 2-12 years old, in newborns T1/2 of imipenem is 1.7-2.4 h, cilastatin 3.8-8.4 h; in impaired renal function T1/2 imipenem 2.9-4 h, cilastatin 13.3-17.1 h.
Extracted primarily by the kidneys (70-76% within 10 h) by glomerular filtration (2/3) and active tubular secretion (1/3); 1-2% is eliminated through bile with feces and 20-25% by the extrarenal route (mechanism unknown).
Fast and efficient (73-90%) excretion by hemodialysis (a 3-hour session of intermittent hemofiltration removes 75% of the dose received).
Indications
Active ingredient
Composition
Powder – 1 fl.
How to take, the dosage
The drug formulation for intravenous administration should not be administered intramuscularly. The average therapeutic dose for adults with body weight greater than or equal to 70 kg and normal renal function (CK 70 ml/min/1.73 m or more) is -1-2 g/day (per imipenem) divided into 3-4 injections.
The maximum daily dose is 4t or 50 mg/kg, whichever is lower.
Depending on the severity of the infection, the following doses are recommended (imipenem dose calculation):
In mild infections and uncomplicated urinary tract infections, 250 mg 4 times daily (total daily dose 1 g).
In a moderate course, 500 mg 3 times a day or 1000 mg 2 times a day (a total daily dose of 1.5-2 g).
In a severe course and complicated urinary tract infections, 500 mg 4 times daily (total daily dose 2 g).
In case of a life-threatening infection it is 1000 mg 3-4 times a day (total daily dose is 3-4 g).
For prevention of postoperative infections, 1000 mg during anesthesia and 1000 mg after 3 hours. In case of surgical intervention with high risk of infection development (colorectal surgery) 500 mg is administered additionally 8 hours and 16 hours after general anesthesia.
In patients with a CKR less than 70 ml/min/1.73 m2 and/or a body weight less than 70 kg, the dose should be proportionally reduced (imipenem dosage calculation):
The maximum daily dose is 1.0 g.
Body weight kg Creatinine clearance, ml/min/1.73 m2.
>71 41-70 21-40 6-20.
>70 250 mg every 6 h 250 m g every 8 h 250 mg every 12 h 250 mg every 12 h.
60-69 250 mg every 8 h 125 m g every 6 h 250 mg every 12 h 125 mg every 12 h.
50-59 125 mg every 6 h 125 mg every 6 h 125 mg every 8 h 125 mg every 12 h.
40-49 125 mg every 6 h 125 mg every 8 h 125 mg every 12 h 125 mg every 12 h.
30-39 125 mg every 8 h 125 mg every 8 h 125 mg every 12 h 125 mg every 12 h.
The maximum daily dose is 1.5 g.
Body weight kg Creatinine clearance, ml/min/1.73 m2.
>71 41-70 21-40 6-20.
>70 500 mg every 8 h 250 mg every 6 h 250 mg every 8 h 250 mg every 12 h.
60-69 250 mg every 6 h 250 mg every 8 h 250 mg every 8 h 250 mg every 12 h.
50-59 250 mg every 6 h 250 mg every 8 h 250 mg every 12 h 250 mg every 12 h.
40-49 250 mg every 8 h 125 mg every 6 h 125 mg every 8 h 125 mg every 12 h.
30-39 125 mg every 6 h 125 mg every 8 h 125 mg every 8 h 125 mg every 12 h.
The maximum daily dose is 2.0 g.
Body weight kg Creatinine clearance, ml/min/1.73 m2.
>71 41-70 21-40 6-20.
>70 500 mg every 6 h 500 mg every 8 h 250 mg every 6 h 250 mg every 12 h.
60-69 500 mg every 8 h 250 mg every 6 h 250 mg every 8 h 250 mg every 12 h.
50-59 250 mg every 6 h 250 mg every 6 h 250 mg every 8 h 250 mg every 12 h.
40-49 250 mg every 6 h 250 mg every 8 h 250 mg every 12 h 250 mg every 12 h.
30-39 250 mg every 8 h 125 mg every 6 h 125 mg every 8 h 125 mg every 12 h.
The maximum daily dose is 3.0 g.
Body weight kg Creatinine clearance, ml/min/1.73 m2.
>71 41-70 21-40 6-20.
>70 1000 mg every 8 h 500 mg every 6 h 500 mg every 8 h 500 mg every 12 h.
60-69 750 mg every 8 h 500 mg every 8 h 500 mg every 8 h 500 mg every 12 h.
50-59 500 mg every 6 h 500 mg every 8 h 250 mg every 6 h 250 mg every 12 h.
40-49 500 mg every 8 h 250 mg every 6 h 250 mg every 8 h 250 mg every 12 h.
30-39 250 mg every 6 h 250 mg every 8 h 250 mg every 8 h 250 mg every 12 h.
In patients with a CKR less than 5 ml/min/1.73 m, the drug should only be administered if hemodialysis is to be performed at least 48 h later.
In patients with a KC less than 5 ml/min/1.73 m who are on hemodialysis, the drug should be administered at doses recommended for patients with a KC of 6-20 ml/min/1.73 m2 immediately after the hemodialysis session and at 12-hour intervals from the completion of the procedure. Patients on hemodialysis, especially if they have diseases of the central nervous system, should be closely monitored. The use of the drug in patients on hemodialysis is recommended only in cases when the benefit of treatment exceeds the potential risk of seizures. At present, there are insufficient data to recommend the use of the drug in patients on peritoneal dialysis. In children from 3 months of age, with body weight up to 40 kg, the single dose is 15 mg/kg administered every 6 hours. The maximum daily dose is 2 g. Children with a body weight of 40 kg or more are prescribed the same doses as adults.
The duration of infusion depends on the selected dose: 250-500 mg is administered for 20-30 minutes; over 500 mg for 40-60 minutes. Patients who experience nausea during the infusion should reduce the rate of administration of the drug. Ready solutions for infusion (imipenem concentration 5 mg/ml) can be stored for 4 h at room temperature or for 24 h in the refrigerator.
Interaction
Pharmaceutically incompatible with lactic acid salt, other antibacterial drugs.
In concomitant use with penicillins and cephalosporins cross-allergy is possible; shows antagonism to other beta-lactam antibiotics (penicillins, cephalosporins and monobactams).
Hanciclovir increases the risk of generalized seizures.
Drugs that block tubular secretion slightly increase plasma and T1/2 concentrations of imipenem (if high concentrations of imipenem are required, concomitant use of these drugs is not recommended).
Special Instructions
It is not recommended for the treatment of meningitis.
It stains the urine a reddish color.
The drug formulation for intravenous administration should not be used for intravenous and vice versa.
A thorough history of previous allergic reactions to beta-lactam antibiotics should be taken before starting therapy.
People with a history of gastrointestinal disease (especially colitis) have an increased risk of pseudomembranous enterocolitis.
The therapy with antiepileptic drugs in patients with a history of brain injury or seizures must be continued for the duration of treatment (to avoid CNS side effects).
Please note that elderly patients may have age-related renal dysfunction, which may require dose reduction.
Impact on driving and operating ability
With regard to the possibility of CNS side effects, caution should be exercised when driving vehicles and engaging in other potentially dangerous activities requiring increased concentration and quick psychomotor reactions.
Contraindications
Hypersensitivity (including to carbapenems and other beta-lactam antibiotics); pregnancy (only for “vital” indications); early childhood (under 3 months); in children – severe renal failure (serum creatinine concentration more than 2 mg/dL).
For the suspension in case of intravenous injection prepared with lidocaine hydrochloride as a solvent: hypersensitivity to local anesthetics of amide structure (shock, intracardiac conduction disorders).
Cautions
. CNS disorders, history of seizures, high seizure activity, anticonvulsant therapy with valproic acid (decreased effectiveness of therapy), chronic renal failure (CK less than 70 ml/min), patients on hemodialysis, advanced age, patients with history of gastrointestinal disorders (includingpseudomembranous colitis).
Side effects
CNS and peripheral nervous system disorders: myoclonia, psychiatric disorders, hallucinations, confusion, epileptic seizures, paresthesias.
Urinary system disorders: oliguria, anuria, polyuria, acute renal failure (rare).
In the digestive system: nausea, vomiting, diarrhea, pseudomembranous enterocolitis, hepatitis (rare).
Hematopoietic and hemostatic system disorders: eosinophilia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, thrombocytosis, monocytosis, lymphocytosis, basophilia, decrease of hemoglobin, prolongation of prothrombin time, positive Coombs reaction.
Laboratory tests: increase of liver transaminases and alkaline phosphatase activity, hyperbilirubinemia, hypercreatininemia, increased concentration of urea nitrogen; direct positive Coombs test.
Allergic reactions: skin rash, pruritus, urticaria, erythema multiforme (including Stevens-Johnson syndrome), angioedema, toxic epidermal necrolysis (rare), exfoliative dermatitis (rare), fever, anaphylactic reactions.
Local reactions: skin hyperemia, painful infiltration at the injection site, thrombophlebitis.
Others: candidiasis, taste disorders.
Pregnancy use
It is used in pregnancy only if the estimated benefit to the mother exceeds the potential risk to the fetus.
The drug penetrates in small amounts through the breast milk, therefore it is necessary to consider stopping breastfeeding during treatment.
Weight | 0.027 kg |
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Manufacturer | Kraspharma PJSC, Russia |
Medication form | Powder for preparation of solution for infusion |
Brand | Kraspharma PJSC |
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