Imipenem cilastatin is a medication with an antibacterial effect, which has a beta-lactam property and is included in the pharmacological group of drugs with an antibacterial effect - carbapenems.
This agent of the antibiotic group acts on numerous pathogenic microbes.
general information
Combined medication, which has an antibacterial effect, contains two active ingredients. This substance is imipenem, as well as the component cilastatin.
The substance imipenem is an antibacterial beta-lactom drug. The active substance belongs to the modern medicines of the thienamycin group. The drug is an inhibitor of the synthesis of the bacterial cell membrane.
The drug affects the suppression of the vital activity of gram-positive microbes, and also affects gram-negative bacteria.
Among the microorganisms that are sensitive to the drug Imipenem cilastatin, there is a group of aerobic bacteria and a group of anaerobic microbes.
The component in the preparation cilastatin sodium is an enzyme that does not have its own antibacterial effect on microorganisms.
It does not inhibit them at the cellular membrane level, but it is a means that slows down the metabolism of the active component imipenem in the cells of the renal organ, which significantly increases the concentration of unchanged imipenem in bladder and the urethral canal.
The drug affects the suppression of the vital activity of gram-positive microbes The sensitivity of microorganisms to the drug
The antibacterial agent Imipenem cilastatin is resistant to the resistance of microorganisms, which gives it a high degree of effect on many types of microbes, including those bacilli that are not sensitive to many antibiotics.
These microbes include Pseudomonas aeruginosa, Serratia spp. Bacillus, and Enterobacter spp.
Sensitivity to the antibacterial drug Imipenem cilastatin has the following gram-positive bacilli, of the aerobic type:
- Aerobic microbes Enterococcus faecium;
- Bacillus Staphylococcus aureus (a strain that produces penicillin);
- Group of streptococcal bacilli - Streptococcus pneumoniae, as well as Streptococcus agalactiae;
- Streptococcus pyogenes, as well as Staphylococcus epidermidis (a strain that produces penicillin);
Sensitivity of aerobic-type gram-negative bacilli to the drug Imipenem cilastatin:
- Aerobic microbes Citrobacter spp. and Acinetobacter spp. as well as Enterobacter spp .;
- Gardnerella vaginalis infections and Escherichia coli microbe;
- Haemophilus parainfluenzae and the microbe Haemophilus influenza;
- Morganella morganii bacteria and Klebsiella spp.
Sensitivity to the agent Imipenem cilastatin of gram-positive bacilli, anaerobic type:
- Propionibacterium spp. and the bacillus Clostridium spp .;
- Peptostreptococcus spp. and the bacteria Peptococcus spp.
Sensitivity of gram-negative bacilli of the anaerobic type to the drug Imipenem cilastatin:
- Alcaligenes spp. and the microorganism Aeromonas hydrophila;
- Neisseria gonorrhoeae as well as Providencia stuartii (the strain that forms penicillin);
- Prevotella disiens and bacillus Prevotella bivia.
Pharmacology
The antibacterial drug Imipenem cilastatin has the following properties on the body:
- The highest concentration of active components in the composition of the blood plasma, after injection inside, occurs in 20 - 30 minutes and reaches from 0.0210 to 0.0580 milligrams per milliliter - this is the concentration of the imipenem component;
- The concentration of the cilastatin component for 20- 30 minutes reaches 0.0210 - 0.0550 milligrams per milliliter;
- After 6 hours, the concentration of the imipenem component decreases to 0.0010 milligram per milliliter;
- Half-life of active ingredients within 60 minutes;
- The process of binding components to proteins - substance imipenem- 20.0%, cilastatin up to 40.0%;
- For 10 hours from the moment of injection, up to 70.0% of the drug is excreted outside the body with the help of the renal organ;
- In urine, the concentration is no more than 0.010 milligrams per milliliter, and the drug can be in urine for 8 - 10 hours.
Indications for use
In accordance with the manufacturer's proposed instructions for use, this group of antibiotics is prescribed as part of drug therapy. infectious diseases, as well as during the period of inflammation.
Appointments for intravenous drip are such infections in the body that cause a severe course of the disease:
- Respiratory system infections;
- Diseases of the urinary system and organs excreting urine from the body;
- Bone cells;
- Infections on skin as well as subcutaneous inflammation.
By the drip method, the drug Imipenem cilastatin is prescribed for gynecological pathologies, infections of the abdominal digestive system, for pathology of septicemia, as well as for endocarditis caused by the invasion of bacilli.
Prescriptions for the administration of the drug Imipenem cilastatin by injection into the muscle tissue are the same as for the drip injection of the drug into the body.
Antibacterial agent Imipenem cilastatin is resistant to microorganisms Directions for use and dosage
Imipenem cilastatin is prescribed for injection into the body by drip into a vein, or by injection into muscle tissue.
With the drip technique, the dosage for the adult population from 12 years old is from 1.0 grams to 4.0 grams. The frequency of drip injection is after 6 hours.
For children, the dosage is calculated based on the weight of the baby - 60.0 milligrams per kilogram. Imipenem cilastatin can be used from three months of age if the child has a body weight higher than 4.0 kilograms.
The dosage of the introduction of the drug into the muscle tissue per day should not exceed 1.0 - 1.5 grams. The frequency of administration of the drug is 2 times a day.
For elderly people over 65 years old, the drug is used with caution, constantly monitoring the work of the renal organ.
Duration of the drip procedure for drug administration:
- Within 20 minutes - 30 minutes when infused from 250.0 milligrams to 500.0 milligrams of an injection solution of the drug Imipenem cilastatin;
- 40 minutes - 1 hour for the introduction of a volume of 500.0 milliliters of medication.
If the patient feels an attack of nausea, then it is necessary to reduce the rate of drug delivery by the drip method. Injections of the drug are made into large muscle tissues (buttocks).
After a complete cure of the body from infection has been determined in laboratory diagnostics, the drug Imipenem cilastatin is administered for another 2 to 3 days.
Antibacterial medication Imipenem cilastatin is not available in tablets, and the release form is only a powder for the preparation of solutions for the drip method of administration and a suspension for excretion of muscle fibers.
The antibacterial drug Imipenem cilastatin is not available in tablets How to prepare a solution for oral administration by the drip technique?
A solution is being prepared for the drip method of administration in the following stages:
- It is necessary to pour a dextrose solution of 5.0%, or 10.0%, into the vial containing the powder of the drug; a solution of sodium chloride 0.90% can also be used. The volume of the solution should not exceed 10.0 - 20.0 milliliters;
- It is necessary to mix thoroughly by shaking until a homogeneous suspension;
- This suspension must be combined with a solvent and the total volume of the drug for the dropper should be 100.0 milliliters;
- If a suspension remains on the walls of the vial, then you can add 10.0 - 20.0 milliliters of solution and shake thoroughly to clean the walls;
- Pour the rest of the suspension into a general container.
This solution for the drip technique of administration becomes transparent and has a concentration of the active ingredient Imipenem cilastatin of 5.0 milligrams per milliliter.
The finished solution can be stored for no more than 4 hours in a room, and with the help of a refrigerator - no longer than one day.
How to make Imipenem cilastatin injection solution?
In order to independently prepare a solution for injection into muscle fibers, the following rules must be observed:
- Take a bottle containing the powder of an antibacterial agent, pour in a solution of sodium chloride 0.90%, or lidocaine 1.0%, you can also use water for injection to make a solution;
- Mix everything thoroughly until smooth by long shaking. It turns out a suspension of white or yellow hue;
- Draw up the suspension into a syringe and inject the drug into large muscle tissue.
Solution for injection into muscle fibers Side effects
The antibacterial agent Imipenem cilastatin has a number of negative effects on all systems of the human body, provoking such symptoms in the organs.
In the nerve fibers of the system, the following symptoms of side effects appear:
- Soreness in the head;
- Sleepiness during the day and sleeplessness at night;
- Whirling in the head;
- Limb tremor;
- Convulsive condition in the limbs;
- Encephalopathy of brain cells;
- Disturbance in the mental state of the patient;
- Disorientation of consciousness.
Violations in the organs of human sensitivity:
- Blurred vision;
- Hearing loss;
- Change in taste references.
The urinary system and its organs also feel the negative effect of the antibiotic Imipenem cilastatin:
- Urine turns red;
- The daily volume of urine excreting by the body increases - the pathology of polyuria;
- Pathology of anuria - urine does not leave the body;
- Oliguria develops - the production of urine slows down;
- Improper functioning of the renal organ.
An antibacterial agent negatively affects the entire digestive system:
- Severe diarrhea;
- Nausea that provokes vomiting;
- Produced a large number of oral fluid (saliva);
- Inflammation in areas of the intestine - colitis pathology;
- Inflammation of liver cells - hepatitis;
- Insufficiency of the hepatic organ.
Disturbances in the hemostatic system under the influence side effects medication Imipenem cilastatin:
- Eosinophilia pathology;
- Blood disease - leukopenia;
- Pathology of neuropenia;
- An increase in platelet molecules in the blood - thrombocytosis, and their decrease - thrombocytopenia;
- Anemia of the hemolytic type.
Side effects in the bloodstream system:
- Rapid heartbeat - tachycardia;
- Hypotension.
Allergic processes can also develop at the local level - redness of the injection site, as well as skin allergies, in the form of a rash and severe itching... Edema may appear, and also quite rarely, but still, there is a possibility of anaphylactic shock.
There are frequent cases of pain in the joints, weakness of the body and the development of candidiasis pathology in the genitals.
Photo Gallery: Side Effects
Contraindications
In accordance with the given annotation to this medication, it is impossible to prescribe its administration inside in these situations:
- If the body is unable to transfer one of the active components of the medication;
- Infants who are less than 3 months old from the date of birth (drip in a vein);
- The method of introduction into the muscle tissue is prohibited under 12 years of age for a child;
- Insufficiency of the renal organ;
- A woman's period, when carrying a baby.
The drug is prescribed under the strict supervision of a doctor in such cases:
- Diseases in the organs of the central nervous system;
- With pathology, colitis;
- When there is a history of damage to the digestive tract;
- With increased creatinine;
- With valproic acid already taken;
- Feeding the baby with breast milk;
- When used in the treatment of kidney hemodialysis;
- Advanced age.
Overdose
With the wrong regimen of use, or with an increased dosage, the following symptoms appear in the body:
- Severe nausea, which causes vomit to separate from the body;
- Confusion and disorientation
- A sharp decrease in the blood pressure index;
- Slow heartbeat - bradycardia;
- Tremors in the limbs.
Treat an overdose with Imipenem with cilastatin:
- It is necessary to stop the administration of the drug inside;
- Carry out the procedure for cleaning the kidneys by the method of hemodialysis;
- To relieve the symptoms of an antibiotic overdose.
Interaction with other medications
Imipenem cilastatin is not used simultaneously with antibiotics, which contain lactic acid-based substances. If you apply Imipenem together with Ganciclovir, then the body will inevitably have a convulsive state.
When using Imipenem with penicillin antibiotics, then there is a great risk of allergies and anaphylactic shock.
Do not use the medication Imipenem with cilastatin when taking calcium channel blockers, because there is a high risk of an increase in the blood plasma composition of the consistency of the antibacterial agent.
With the combined administration of dehydropeptidase inhibitors and the antibacterial drug Imipenem, the active component of imipenem accumulates in an increased concentration in urine.
Analogues and price
An antibacterial drug with the trade name Imipenem cilastatin has many analogues of foreign manufacturers and domestic pharmaceutical companies.
There are analogs:
- Tienam drug;
- Antibiotic Aquapenem;
- Medication Grimipenem;
Typical clinical and pharmacological article 1
Pharmaceutical action. and Bacteroides fragilis. and Enterobacter spp., (previously (incl. (incl. (incl. (previously (previously Pasteurella), incl. (incl. (incl. (previously (incl. (incl. (incl. (including strains that form penicillinase), Staphylococcus epidermidis(including strains that form penicillinase), group C, Streptococcus Bacteroides spp.(incl. (previously incl. (previously (previously (previously (previously (incl. (including Propionibacterium acne); other microorganisms: Some Staphylococcus spp.(methicillin resistant), Streptococcus spp.(group D), and some strains Pseudomonas cepacia In vitro Pseudomonas aeruginosa.
Pharmaceutical action. Broad-spectrum beta-lactam antibiotic. Suppresses the synthesis of the cell wall of bacteria and has a bactericidal effect against a wide range of gram-positive and gram-negative microorganisms, aerobic and anaerobic. Imipenem is a thienamycin derivative, belongs to the carbapenem group. Cilastatin sodium inhibits dehydropeptidase, an enzyme that metabolizes imipenem in the kidneys, which significantly increases the concentration of unchanged imipenem in the urinary tract. Cilastatin does not have its own antibacterial activity, does not inhibit the beta-lactamase of bacteria. Active in relation to Pseudomonas aeruginosa, Staphylococcus aureus, Streptococcus faecalis and Bacteroides fragilis. Resistant to destruction by bacterial beta-lactamase, which makes 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 almost all clinically significant pathogenic microorganisms. Active against gram-negative aerobic bacteria: Achromobacter spp., Acinetobacter spp.(previously Mima-Herellea), Aeromonas hydrophila, Alcaligenes spp., Bordetella bronchicanis, Bordetella bronchiseptica, Bordetella pertussis, Brucella melitensis, Campylobacter spp., Capnocytophaga spp., Citrobacter spp.(incl. Citrobacter diversus, Citrobacter freundii), Eikenella corrodens, Enterobacter spp.(incl. Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae), Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae(including strains that form beta-lactamase), Haemophilus parainfluenzae, Hafnia alvei, Klebsiella spp.(incl. Klebsiella oxytoca, Klebsiella ozaenae, Klebsiella pneumoniae), Moraxella spp., Morganella morganii(previously Proteus morganii), Neisseria gonorrhoeae(including strains that form penicillinase), Neisseria meningitidis, Yersinia spp.(previously Pasteurella), incl. Yersinia multocida, Yersinia enterocolitica, Yersinia pseudotuberculosis; Plesiomonas shigelloides, Proteus spp.(incl. Proteus mirabilis, Proteus vulgaris), Providencia spp.(incl. Providencia alcalifaciens, Providencia rettgeri(previously Proteus rettgeri), Providencia stuartii), Pseudomonas spp.(incl. Pseudomonas aeruginosa, Pseudomonas fluorescens, Pseudomonas pseudomallei, Pseudomonas putida, Pseudomonas stutzeri), Salmonella spp.(incl. Salmonella typhi), Serratia spp.(incl. Serratia marcescens, Serratia proteamaculans), Shigella spp.; gram-positive aerobic bacteria: Bacillus spp., Enterococcus faecalis, Erysipelothrix rhusiopathiae, Listeria monocytogenes, Nocardia spp., Pediococcus spp., Staphylococcus aureus(including strains that form penicillinase), Staphylococcus epidermidis(including strains that form penicillinase), 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.(incl. Bacteroides distasonis, Bacteroides fragilis, Prevotella melaninogenica(previously Bacteroides melaninogenicus), Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides uniformis, Bacteroides vulgatus), Bilophila wadsworthia, Fusobacterium spp. incl. (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.(incl. 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.(methicillin resistant), Streptococcus spp.(group D), Stenotrophomonas maltophilia, Enterococcus faecium and some strains Pseudomonas cepacia are insensitive to imipenem. Effective against many infections caused by bacteria resistant to cephalosporins, aminoglycosides, penicillins. In vitro acts synergistically with aminoglycosides against certain strains Pseudomonas aeruginosa.
Pharmacokinetics. When administered intramuscularly, the bioavailability of imipenem is 95%, cilastatin is 75%. Communication with plasma proteins of imipenem - 20%, cilastatin - 40%. C max of imipenem with intravenous administration at a dose of 250, 500 or 1000 mg for 20 minutes - 14-24, 21-58 and 41-83 μg / ml, respectively; with an intramuscular injection of 500 or 750 mg - 10 and 12 μg / ml, respectively. C max of cilastatin with intravenous administration at a dose of 250, 500 or 1000 mg for 20 minutes - 15-25, 31-49 and 56-80 μg / ml; with intramuscular administration of 500 or 750 mg - 24 and 33 μg / ml, respectively. It is quickly and well distributed in most tissues and body fluids. The highest concentrations are found in pleural effusion, peritoneal and interstitial fluids, and reproductive organs. It is found in low concentrations in CSF. The volume of distribution 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 the tubular secretion of imipenem with cilastatin leads to inhibition of its renal metabolism and accumulation in the urine unchanged. Cilastatin is metabolized to the N-acetyl compound. With intramuscular administration of T 1/2 imipenem - 2-3 hours With intravenous administration of T 1/2 imipenem and cilastatin in adults - 1 hour, in children 2-12 years old - 1-1.2 hours, in newborns T 1/2 imipenem - 1.7-2.4 hours, cilastatin - 3.8-8.4 hours; with impaired renal function T 1/2 imipenem - 2.9-4 hours, cilastatin - 13.3-17.1 hours. It is excreted mainly by the kidneys (70-76% within 10 hours) by glomerular filtration (2/3) and active tubular secretion (1/3); 1-2% is excreted through the bile in the feces and 20-25% - by the extracurricular route (the mechanism is unknown). It is quickly and efficiently (73-90%) excreted by hemodialysis (as a result of a 3-hour session of intermittent hemofiltration, 75% of the dose received is removed).
Indications. Intra-abdominal infections, lower infections respiratory tract, genitourinary system, bones and joints, skin and soft tissues, pelvic organs, sepsis, bacterial endocarditis, prevention of postoperative infections, mixed infections, nosocomial infections, etc.
Contraindications Hypersensitivity (including carbapenems and other beta-lactam antibiotics), pregnancy (only for "vital" indications), early childhood(up to 3 months); in children - severe renal failure (serum creatinine concentration more than 2 mg / dL). For a suspension for intramuscular injection prepared using lidocaine hydrochloride as a solvent - hypersensitivity to local anesthetics amide structure (shock, impaired intracardiac conduction).
Carefully. Diseases of the central nervous system, lactation period, old age.
Dosing. Intravenous drip and intramuscular The doses given below are calculated for a body weight of 70 kg or more and a CC of 70 ml / min / 1.73 m2 or more. For patients with CC less than 70 ml / min / 1.73 m2 and / or less body weight, the dose should be reduced proportionally. The intravenous route of administration is preferable to use at the initial stages of therapy for bacterial sepsis, endocarditis, and other severe and life-threatening infections, incl. lower respiratory tract infections caused by Pseudomonas aeruginosa, and in case of severe complications.
To prepare the infusion solution, 100 ml of solvent is added to the vial (0.9% NaCl solution, 5% aqueous dextrose solution, 10% aqueous dextrose solution, 5% dextrose solution and 0.9% NaCl, etc.). The concentration of imipenem in the resulting solution is 5 mg / ml.
The average therapeutic dose for adults with intravenous administration is 1-2 g / day, divided into 3-4 injections; maximum daily dose- 4 g or 50 mg / kg, whichever is the smaller dose. Patients with a mild severity of infection - 250 mg 4 times a day, an average degree - 500 mg 3 times a day or 1 g 2 times a day, a severe degree - 500 mg 4 times a day, with an infection that threatens the patient's life - 1 g 3-4 times a day. Every 250-500 mg is injected intravenously for 20-30 minutes, and every 1 g for 40-60 minutes.
For the prevention of postoperative infections - 1 g during induction anesthesia and 1 g after 3 h ...
The maximum daily doses for intravenous administration in patients with renal insufficiency, depending on the severity of the infection and the CC values (ml / min / 1.73 m2):
with a mild course of infection and CC 41-70 ml / min - 250 mg after 8 hours, CC 21-40 ml / min - 250 mg after 12 hours, CC 6-20 ml / min - 250 mg after 12 hours;
with moderate infection and CC 41-70 ml / min - 250 mg after 6 hours, CC 21-40 ml / min - 250 mg after 8 hours, CC 6-20 ml / min - 250 mg after 12 hours;
in severe cases (highly sensitive strains) and CC 41-70 ml / min - 500 mg after 8 hours, CC 21-40 ml / min - 250 mg after 6 hours, CC 6-20 ml / min - 250 mg after 12 hours; in severe cases (moderately sensitive strains, incl. Pseudomonas aeruginosa) and CC 41-70 ml / min - 500 mg after 6 hours, CC 21-40 ml / min - 500 mg after 8 hours, CC 6-20 ml / min - 500 mg after 12 hours; in severe life-threatening infection and CC 41-70 ml / min - 750 mg after 8 hours, CC 21-40 ml / min - 500 mg after 6 hours, CC 6-20 ml / min - 500 mg after 12 hours
Patients with CC less than 5 ml / min are prescribed only if hemodialysis is performed every 48 hours, followed by administration after 12 hours (from the moment the procedure is completed).
For the prevention of postoperative infections in adults - 1 g each with induction anesthesia and again after 3 hours; for surgical interventions with a high degree of risk (on the colon and rectum) - in addition, another 500 mg is administered 8 and 16 hours after the start of general anesthesia. Currently, there is no sufficient data on the dosage regimen for preoperative prophylaxis in patients with CC less than 70 ml / min / 1.73 sq. M.
Children weighing 40 kg or more - the same doses as adults; with a body weight of less than 40 kg - 15 mg / kg 4 times a day; the maximum daily dose is 2 g.
IM administration can be used as an alternative to IV formulation for the treatment of infections in which IM administration is preferred. Depending on the severity of the infection, the sensitivity of pathogenic microorganisms and the patient's condition, 500-750 mg is administered every 12 hours. The total daily dose is not more than 1500 mg. If there is a need for large doses of the drug, it is necessary to use intravenous administration.
IM administration in patients with CC less than 20 ml / min / 1.73 m2, as well as in children, has not been studied.
For the treatment of urethritis and cervicitis caused by Neisseria gonorrhoeae, 500 mg is administered once, intramuscularly. The powder is mixed with 2 ml of 1% lidocaine hydrochloride solution (without epinephrine), water for injection or 0.9% NaCl solution until a homogeneous suspension (white or slightly yellow) is formed.
Side effect. From the nervous system: myoclonus, mental disorders, hallucinations, confusion, epileptic seizures, paresthesias.
From the urinary system: oliguria, anuria, polyuria, acute renal failure (rarely).
From the digestive system: nausea, vomiting, diarrhea, pseudomembranous enterocolitis, hepatitis (rarely).
On the part of the hematopoietic and hemostatic system: eosinophilia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, thrombocytosis, monocytosis, lymphocytosis, basophilia, decreased Hb, prolongation of prothrombin time, positive Coombs' reaction.
Laboratory indicators: increased activity of "hepatic" transaminases and alkaline phosphatase, hyperbilirubinemia, hypercreatininemia, increased concentration of urea nitrogen; direct positive Coombs test.
Allergic reactions: skin rash, pruritus, urticaria, exudative erythema multiforme (including Stevens-Johnson syndrome), angioedema, toxic epidermal necrolysis (rare), exfoliative dermatitis (rare), fever, anaphylactic reactions.
Local reactions: skin flushing, painful infiltration at the injection site, thrombophlebitis.
Others: candidiasis, taste disturbance.
Interaction. Pharmaceutically incompatible with lactic acid salt, other antibacterial drugs.
With simultaneous use with penicillins and cephalosporins, cross-allergy is possible; shows antagonism towards other beta-lactam antibiotics (penicillins, cephalosporins and monobactams).
Ganciclovir increases the risk of developing generalized seizures.
Drugs that block tubular secretion slightly increase the plasma concentration and T 1/2 of imipenem (if high concentrations of imipenem are required, it is not recommended to use these drugs at the same time).
Stains urine reddish.
The dosage form for intramuscular administration should not be used for intravenous administration and vice versa.
Before starting therapy, a thorough history should be collected for previous allergic reactions to beta-lactam antibiotics. Individuals with a history of gastrointestinal diseases (especially colitis) have an increased risk of developing pseudomembranous enterocolitis.
Therapy with antiepileptic drugs in patients with a history of brain injury or seizures should be continued for the entire period of drug treatment (in order to avoid side effects from the side of the central nervous system).
It should be borne in mind that in elderly patients, age-related renal dysfunction is likely, which may require a dose reduction.
State Register of Medicines. Official edition: in 2 volumes - M .: Medical Council, 2009. - V.2, part 1 - 568 p .; Part 2 - 560 p.
5R, 6S) -6 - [(1R) -1-hydroxyethyl] -3 - ((2 - [(iminomethyl) amino] ethyl) thio) -7-oxo-1-azabicyclohept-2-ene-2-carboxylic acid
Chemical properties
This antibiotic belongs to the group of carbapenems, beta-lactamate antibacterial agents. In general, substances of this kind are more resistant to beta-lactamazam , have a wide spectrum of action. This substance is a derivative thienamycin ... It is often used in combination with other medicines. Molecular mass chemical compound = 299.3 grams per mole. Release form Imipenem - solution (lyophilisate for preparation of solution) for intravenous or intramuscular administration.
pharmachologic effect
Bactericidal , antibacterial , antimicrobial .
Pharmacodynamics and pharmacokinetics
Imipenem inhibits the synthesis of bacterial cell walls. The substance is active towards aerobic and anaerobic microorganisms , however, does not affect the mushroom kingdom in any way. Antibiotic cannot break down bacterial beta-lactamase enzymes , cephalosporinases and penicillinase therefore it is effective in cases where other drugs of the same kind are powerless.
This substance has an effect on staphylococcus , Listeria monocytogenes , streptococci groups B, C and G , Enterococci , Bacillus spp. , Nocardia spp. , green streptococci that belong to the group Viridans , Citrobacter spp. , Acinetobacter spp ... and some resistant to action strains.
Also, gram-positive anaerobic bacteria are sensitive to the action of the agent - Eubacterium spp. , Bifidobacterium spp. , Peptococcus spp. , Clostridium spp. , Propionibacterium spp ... and gram-negative anaerobes - Bacteroides spp. , Prevotella disiens , Prevotella bivia , Fusobacterium spp. , Prevotella melaninogenica , VeiIlonella spp. The antibiotic does not affect the life cycle in any way mycoplasma , chlamydia , Enterococcus faecium , Xanthomonas maltophilia , mushrooms , strains P. cepacia , viruses , methicillin-resistant staphylococci.
Intravenous injections of Imipenem allow reaching the maximum plasma concentration of the drug within 15-20 minutes after administration. The drug continues to work for 5 hours after infusion. With intramuscular injections, the bioavailability of the drug is about 95%, and the half-life is 60 minutes. The drug has a relatively low degree of binding to blood plasma proteins - up to 20%.
Substance metabolism occurs in the kidneys with the help of an enzyme dehydropeptidases , which cleaves the beta-lactam ring. Then the drug is quickly and completely distributed over most tissues, organs and fluids (intraocular fluid, vitreous humor, sputum, bile, cerebrospinal fluid, myometrium, skin, etc.). About 72% of Imipenem administered intravenously is excreted from the body within 10 hours.
Indications for use
The drug is prescribed:
- for the treatment of infections of the genitourinary system, organs abdominal cavity, respiratory tract;
- in gynecological practice;
- at septicemia ;
- for the treatment of infections of the joints and bones;
- with infectious;
- in diseases of the skin and soft tissues caused by microorganisms sensitive to the action of the antibiotic;
- for the prevention of complications after surgery.
Contraindications
The medicine is contraindicated:
- if available on active substance, penicillins, cephalosporins , other beta-lactam antibiotics ;
- children under 3 months old (intravenously) and up to 12 years old (intramuscularly);
- while breastfeeding;
- children with renal failure.
Side effects
May develop:
- skin rashes eosinophilia ;
- vomiting, distortion of taste, an increase in the activity of liver enzymes, pseudomembranous colitis , nausea;
- increased seizure activity, epileptic seizures ;
- lesions of the skin and mucous membranes by a fungus of the genus Candida , anaphylactic reactions ;
- pain and discomfort at the injection site, with intravenous use of the drug.
Imipenem, application instruction (Way and dosage)
The dosage and route of administration depend on the severity of the disease, height, weight and individual characteristics of the patient's body. The medicine is prescribed intravenously or intramuscularly, as recommended by the attending physician.
Intravenous infusion is performed slowly, drip. Most often, this method of administration is used at the beginning sepsis , endocarditis or other life-threatening infections, with physiological disorders (for example, shocked ).
Intravenously, adults and children over 12 years of age are prescribed 1-4 grams of the drug per day. Infusions are made every 6 hours. For babies from 3 months who weigh more than 4 kg, daily dosage calculated on the basis of 60 mg per kg of body weight.
Intramuscular injections are prescribed from the age of 12 years. The medicine is injected deep into the muscle at 1-1.5 grams per day (for 2 doses).
The maximum daily dosage for adults is 4 grams intravenously and 1.5 grams intramuscularly. Children should not be administered more than 2 grams of the drug intravenously during the day.
In patients over 65 years of age, the function of the kidneys, liver is reduced, and the work is impaired of cardio-vascular system... Therefore, the treatment of this group of patients must be carried out with extreme caution, prescribing the minimum active and effective dosages. Careful monitoring of kidney function is also necessary.
Overdose
There are no data on cases of drug overdose. It is recommended to cancel the medication and prescribe supportive therapy. Imipenem is supposed to be outputted using .
Interaction
Combination Imipenem + Cilastatin or can lead to the development of seizures.
Terms of sale
On prescription.
special instructions
Particular care should be taken when prescribing the drug to patients with diseases of the central nervous system or kidneys. It is recommended to adjust the dosage.
It should be remembered and taken into account that if the patient has previously experienced allergic reactions to beta-lactam antibiotics , you may develop an allergy to Imipenem.
When using this medication and , the latter is a renal inhibitor dehydropeptidases ... This combination can lead to accumulation of imipenem in the urine.
During treatment with the drug, a false positive Coombs reaction .
For children
In pediatric practice antibiotic used as intravenous injection. It is necessary to adjust the daily dosage.
Elderly
During pregnancy and lactation
For pregnant women, the drug is prescribed only if the intended benefit will significantly outweigh the risk to the fetus. It is best to stop breastfeeding during treatment.
Preparations that contain (Imipenem's analogs)
Matching ATX level 4 code:Combination Imipenem + Cilastatin is a part of the following drugs: Aquapenem , Imipenem and Cilastatin , , Imipenem and cilastatin sodium , Imipenem +Cilastatin-Vial , Tsilapenem ,Grimipenem , Cilaspen , Tiepenem .
Kraspharma OJSCCountry of origin
RussiaProduct group
Antibacterial drugsAntibiotic, carbapenem + dehydropeptidase inhibitor
Forms of issue
- ind / pack
Description of the dosage form
- Powder for solution for infusion of white or white with a yellowish tinge.
Pharmacokinetics
The maximum concentration (Cmax) of imipenem with intravenous (iv) administration at a dose of 250 mg, 500 mg, 1000 mg for 20 minutes is 14-24 μg / ml, 21-58 μg / ml, 41-83 μg / ml, respectively ... Cmax of cilastatin with intravenous administration at a dose of 250 mg, 500 mg, 1000 mg for 20 minutes - 15-25 μg / ml, 31-49 μg / ml, 56-80 μg / ml, respectively. 20% of the administered dose of imipenem and 40% of cilastatin reversibly bind to blood plasma proteins. Imipenem is well and quickly distributed in most tissues and body fluids. The highest concentrations are achieved in pleural effusion, peritoneal and interstitial fluids, and reproductive organs. It is found in low concentrations in cerebrospinal fluid (CSF). The volume of distribution 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. Both components of the drug are excreted mainly by the kidneys (70-76% within 10 hours) by glomerular filtration (2/3) and active tubular secretion (1/3): 1-2% is excreted through the intestine and 20-25% - by the extrarenal route ( mechanism unknown). With intravenous administration, the half-life (T1 / 2) of imipenem and cilastatin in adults -1 hour, in children 2-12 years old - 1-1.2 hours, in newborns T1 / 2 imipenem - 1.7- 2.4 hours, cilastatin -3.8-8.4 h; in case of impaired renal function T1 / 2 imipenem - 2.9-4 hours cilastatin - 13.3-17.1 hours Imipenem and cilastatin are quickly and effectively (73-90%) excreted by hemodialysis (as a result of a 3-hour session of intermittent hemofiltration is removed 75% of the administered dose).Special conditions
Not recommended for the treatment of meningitis. Strict adherence to the recommended dosage and dosage regimen is urgently required, especially in patients prone to seizure activity. Anticonvulsant therapy in patients with a history of epilepsy should be continued for the entire period of drug treatment. If local tremor, myoclonus, or seizures are observed, patients should undergo neurologic evaluation and anticonvulsant therapy. The dosage of the drug in this case should be reviewed to determine if it should be reduced or the drug should be canceled. The dosage form contains 37.56 mg (1.63 meq) sodium. Before starting therapy, a thorough history should be collected for previous allergic reactions to beta-lactam antibiotics. If an allergic reaction develops, the drug should be discontinued immediately. Individuals with a history of gastrointestinal diseases (especially colitis) have an increased risk of developing pseudomembranous colitis. When using the drug, both during administration and after 2-3 weeks. after stopping treatment, diarrhea caused by Clostridium difficile (pseudomembranous colitis) may develop. In mild cases, it is sufficient to discontinue treatment and use ion-exchange resins (cholestyramine, colestipol), in severe cases, it is indicated to compensate for the loss of fluid, electrolytes and protein, the appointment of vancomycin and metronidazole. Cannot be applied medicines, inhibiting intestinal peristalsis. As with other beta-lactam antibiotics, Pseudomonas aeruginosa can quickly develop drug resistance during treatment. Therefore, during the treatment of Pseudomonas aeruginosa infections, it is recommended to carry out periodic antibiotic susceptibility tests according to the clinical situation. In elderly patients, age-related renal impairment is likely, which may require a dose reduction. Stains urine reddish. Impact on the ability to manage vehicles and work with mechanisms Care should be taken when driving a car and engaging in other potentially hazardous activities that require increased attention and speed of psychomotor reactions.Compound
- 1 fl.
- imipenem (in the form of monohydrate) 500 mg
- cilastatin (in the form of cilastatin sodium) 500 mg
- Excipients: sodium bicarbonate 20 mg.
Imipenem + Cilastatin indications for use
- Infectious and inflammatory diseases caused by microorganisms sensitive to the drug:
- - lower respiratory tract infections;
- - urinary tract infections;
- - intra-abdominal infections;
- - gynecological infections;
- - bacterial septicemia;
- - infections of bones and joints;
- - infections of the skin and soft tissues;
- - bacterial endocarditis.
- Prevention of postoperative infectious complications
Imipenem + Cilastatin contraindications
- - hypersensitivity to one of the components of the drug, as well as to other carbapenems, beta-lactam antibiotics, penicillins and cephalosporins;
- - chronic renal failure with CC less than 5 ml / min / 1.73 m2 without hemodialysis;
- - early childhood (up to 3 months);
- - in children - severe renal failure (serum creatinine concentration more than 2 mg / dl).
- Carefully
- Diseases of the central nervous system (CNS), pseudomembranous colitis, patients with gastrointestinal diseases in history, with CC less than 70 ml / min / 1.73 m2, patients on hemodialysis, anticonvulsant therapy with valproic acid (decreased effectiveness of therapy), old age.
- Application during pregnancy and lactation
- Use during pregnancy is permissible only if the potential benefit of the treatment to the mother outweighs the potential risk to the fetus.
- Imipenem and cilastatin pass into breast milk in small amounts, so the question of stopping breastfeeding should be decided
Imipenem + Cilastatin dosage
- 500 mg + 500 mg
Imipenem + Cilastatin side effects
- From the side of the central nervous system: dizziness, drowsiness, myoclonus, mental disorders, hallucinations, confusion, convulsions, paresthesia, encephalopathy, tremor, headache, vertigo.
- From the senses: hearing loss, ringing in the ears, taste disturbance.
- From the urinary system: oliguria, anuria, polyuria, acute renal failure, changes in the color of urine.
- From the digestive system: nausea, vomiting, diarrhea, pseudomembranous colitis, hemorrhagic colitis, hepatitis (including fulminant), liver failure, jaundice, gastroenteritis, abdominal pain, glossitis, hypertrophy of the papillae of the tongue, staining of the teeth or tongue, pain in the pharynx, hypersalivation , heartburn.
- Respiratory system: chest discomfort, shortness of breath, hyperventilation.
- From the side of the hematopoietic organs: eosinophilia. leukopenia, neutropenia, agranulocytosis, thrombocytopenia, thrombocytosis, monocytosis, lymphocytosis, leukocytosis, basophilia, pancytopenia, inhibition of bone marrow hematopoiesis, hemolytic anemia.
- Laboratory indicators: increased activity of "hepatic" transaminases and alkaline phosphatase, lactate dehydrogenase, hypercreatininemia, hyperbilirubinemia, increased concentration of urea nitrogen; false positive direct Coombs' test; decrease in hemoglobin and hematocrit, lengthening of prothrombin time; increased concentration of low density lipoproteins; hyponatremia, hyperkalemia, hypochloremia; the appearance of protein, erythrocytes, leukocytes, cylinders, an increase in the concentration of bilirubin in the urine.
- Allergic reactions: skin rash, itching, urticaria, exudative erythema multiforme, Stevens-Johnson syndrome, angioedema, toxic epidermal necrolysis, exfoliative dermatitis, fever, anaphylactic reactions.
- From the side of the cardiovascular system: lowering blood pressure, palpitations, tachycardia.
- Local reactions: skin flushing, painful infiltration at the injection site, phlebitis / thrombophlebitis.
- Others: candidiasis, vaginal itching, cyanosis, hyperhidrosis, polyarthralgia, asthenia, burning sensation behind the breastbone, pain in the thoracic spine.
Drug interactions
Pharmaceutical incompatible with lactic acid salt, solutions of other antibiotics. With simultaneous use with penicillins and cephalosporins, cross-allergy is possible; shows antagonism to other beta-lactam antibiotics (penicillins, cephalosporins and monobactams). With simultaneous use with ganciclovir, the risk of developing generalized seizures increases. These drugs should not be used concomitantly, unless the potential benefits outweigh the potential risks. Drugs that block tubular secretion slightly increase the plasma concentration and T1 / 2 of imipenem (if high concentrations of imipenem are required, it is not recommended to use these drugs simultaneously). When using the drug, the serum concentration of valproic acid decreases, which leads to a decrease in the effectiveness of the anticonvulsant therapy, therefore, it is recommended to monitor the serum concentration of valproic acid during the treatment period.Overdose
In case of overdose, it is recommended to cancel the drug, prescribe symptomatic and supportive therapy. Imipenem is excreted by hemodialysis.Storage conditions
- keep away from children
- store in a dark place
International name
Imipenem + [Cilastatin] (Imipenem +)Group affiliation
Antibiotic carbapenem + dehydropeptidase inhibitorDosage form
Powder for preparation of solution for intramuscular administration, powder for preparation of solution for infusion, powder for preparation of solution for intravenous administrationpharmachologic effect
Broad-spectrum beta-lactam antibiotic. Suppresses the synthesis of the cell wall of bacteria and has a bactericidal effect against a wide range of gram-positive and gram-negative microorganisms, aerobic and anaerobic.
Imipenem is a thienamycin derivative, belongs to the carbapenem group.
Cilastatin sodium inhibits dehydropeptidase, an enzyme that metabolizes imipenem in the kidneys, which significantly increases the concentration of unchanged imipenem in the urinary tract. Cilastatin does not have its own antibacterial activity, does not inhibit the beta-lactamase of bacteria.
Sensitive in vivo: gram-positive aerobes - Enterococcus faecalis, Staphylococcus aureus, including penicillinase-forming strains, Staphylococcus epidermidis, including penicillinase-forming strains, Streptococcus agalactiae (Streptococcus group B), Streptococcus pneumoniae, Streptococcus pneumoniae, Streptococcus pneumoniae.
Gram-negative aerobes: Acinetobacter spp., Citrobacter spp., Enterobacter spp., Escherichia coli, Gardnerella vaginalis, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella spp., Morganella morganas, S. marcescens.
Gram-positive anaerobes: Bifidobacterium spp., Clostridium spp., Eubacterium spp., Peptococcus spp., Peptostreptococcus spp., Propionibacterium spp.
Gram-negative anaerobes: Bacteroides spp., Including B. fragilis, Fusobacterium spp.
Sensitive in vitro (clinical efficacy has not been established): gram-positive aerobes - Bacillus spp., Listeria monocytogenes, Nocardia spp., Staphylococcus saprophyticus, Streptococcus spp. groups C, G and viridans.
Gram-negative aerobes: Aeromonas hydrophila, Alcaligenes spp., Capnocytophaga spp., Haemophilus ducreyi, Neisseria gonorrhoeae, including penicillinase-forming strains, Pasteurella spp., Providencia stuartii.
Gram-negative anaerobes: Prevotella bivia, Prevotella disiens, Prevotella melaninogenica, Veillonella spp.
Insensitive: Enterococcus faecium, methicillin-resistant Staphylococcus spp., Xanthomonas maltophilia, Pseudomonas cepacia.
In vitro acts synergistically with aminoglycosides against certain strains of Pseudomonas aeruginosa.
Indications
For intravenous administration - treatment of severe infections caused by sensitive microorganisms: infections of the lower respiratory tract, urinary tract (complicated and uncomplicated), intra-abdominal and gynecological infections, septicemia, infections of bones and joints, skin and subcutaneous tissues, endocarditis, super- and co -infections.
For intramuscular administration - treatment of lungs and moderate severity of infections caused by sensitive microorganisms: lower respiratory tract infections, intra-abdominal and gynecological infections, infections of the skin and subcutaneous tissues.
Contraindications
Hypersensitivity (including carbapenems and other beta-lactam antibiotics), pregnancy (only for "vital" indications); CRF (CC less than 5 ml / min without hemodialysis), CRF in children weighing less than 30 kg, CNS infections in children.
For a suspension for intramuscular injection, prepared using lidocaine as a solvent - hypersensitivity to local anesthetics of the amide structure (shock, impaired intracardiac conduction).
Additionally for intramuscular injection: children under 12 years of age.
Side effects
From the nervous system: myoclonus, mental disorders, hallucinations, confusion, convulsions, paresthesia, dizziness, drowsiness, encephalopathy, tremor, headache, vertigo.
From the senses: hearing loss, tinnitus, taste disturbance.
From the urinary system: oliguria, anuria, polyuria, acute renal failure (rare), changes in the color of urine.
From the digestive system: nausea, vomiting, diarrhea, pseudomembranous colitis, hemorrhagic colitis, hepatitis (rarely), liver failure, jaundice, gastroenteritis, abdominal pain, glossitis, hypertrophy of the papillae of the tongue, staining of the teeth or tongue, pain in the pharynx, hypersalivation.
From the side of hematopoiesis: eosinophilia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, thrombocytosis, monocytosis, lymphocytosis, basophilia, pancytopenia, inhibition of bone marrow hematopoiesis, hemolytic anemia.
Laboratory indicators: increased activity of "hepatic" transaminases and alkaline phosphatase, LDH, hyperbilirubinemia, hypercreatininemia, increased concentration of urea nitrogen; direct false positive Coombs' test; decrease in Hb and hematocrit, lengthening of prothrombin time; hyponatremia, hyperkalemia, hyperchloremia; the appearance of protein, erythrocytes, leukocytes, cylinders in the urine.
Allergic reactions: skin rash, itching, urticaria, exudative erythema multiforme, Stevens-Johnson syndrome, angioedema, toxic epidermal necrolysis (rare), exfoliative dermatitis (rare), fever, anaphylactic reactions.
From the CVS: lowering blood pressure, palpitations, tachycardia.
Local reactions: skin flushing, painful infiltration at the injection site, thrombophlebitis.
Others: candidiasis, vaginal itching, cyanosis, hyperhidrosis, polyarthralgia, asthenia, burning behind the breastbone.
Application and dosage
Intravenous drip and intramuscular Doses are expressed in terms of imipenem.
The intravenous route of administration is preferable to use at the initial stages of therapy for bacterial sepsis, endocarditis, and other severe and life-threatening infections, incl. lower respiratory tract infections caused by Pseudomonas aeruginosa and in the case of severe complications.
To prepare the infusion solution, 100 ml of solvent (0.9% NaCl solution, 5% aqueous dextrose solution, 10% aqueous dextrose solution, 5% dextrose and 0.9% NaCl solution, etc.) are added to the vial. The concentration of imipenem in the resulting solution is 5 mg / ml.
Every 250-500 mg is injected intravenously for 20-30 minutes, and every 750-1000 mg is injected for 40-60 minutes. If nausea occurs during administration, the rate of administration of the drug is reduced.
The doses given below are calculated for a body weight of 70 kg or more and a CC of 70 ml / min / 1.73 m2 or more. For patients with CC less than 70 ml / min / 1.73 m2 and / or less body weight, the dose should be reduced proportionally.
Dosing regimen in patients weighing 70 kg or more and CC 71 (ml / min / 1.73 sq.m.): with high sensitivity of pathogens, including gram-positive and gram-negative aerobes and anaerobes: mild severity - 250 mg every 6 hours ( total daily dose 1 g); medium degree - 500 mg every 6 or 8 hours (total daily dose 2 g or 1.5 g); life-threatening infections - 500 mg every 6 hours (total daily dose 1 g); uncomplicated urinary tract infections - 250 mg every 6 hours (total daily dose 1 g); complicated urinary tract infections - 500 mg every 6 hours (total daily dose 2 g).
With moderate sensitivity of pathogens, mainly some strains of Pseudomonas aeruginosa: mild severity - 500 mg every 6 hours (total daily dose 2 g); medium degree - 500 mg every 6 hours (total daily dose 2 g) or 1000 mg every 8 hours (total daily dose 3 g); life-threatening infections - 1000 mg every 6 or 8 hours (total daily dose 4 g or 3 g); uncomplicated urinary tract infections - 250 mg every 6 hours (total daily dose 1 g); complicated urinary tract infections - 500 mg every 6 hours (total daily dose 2 g).
In view of the high antimicrobial activity of the drug, the dose should not be administered more than 50 mg / kg / day or 4 g / day. Patients over 12 years old with cystic fibrosis were prescribed up to 90 mg / kg / day, but not more than 4 g / day.
Adults weighing less than 70 kg or with CC less than 71 (ml / min / 1.73 sq.m.): first, it is necessary to determine the total daily dose appropriate for patients weighing 70 kg and in the absence of chronic renal failure. When used in a total daily dose of 1 g / day: with a CC of more than 71 ml / min / 1.73 m2 and a body weight of more than 70 kg - 250 mg every 6 hours; with CC more than 71 and body weight 60 kg - 250 mg every 8 hours; with CC more than 71 and body weight 40-50 kg - 125 mg every 6 hours; with CC more than 71 and body weight 30 kg - 125 mg every 8 hours. With CC 41-70 and body weight more than 70 kg - 250 mg every 8 hours; with CC 41-70 and body weight 50-60 kg - 125 mg every 6 hours; with CC 41-70 and body weight 50-60 kg - 125 mg every 8 hours. With CC 21-40 and body weight more than 60 kg - 250 mg every 12 hours; with CC 21-40 and body weight 50 kg - 125 mg every 8 hours; with CC 21-40 and body weight 30-40 kg - 125 mg every 12 hours. With CC 6-20 and body weight more than 70 kg - 250 mg every 12 hours; with CC 6-20 and body weight 30-60 kg - 125 mg every 12 hours.
When prescribed in a total daily dose of 1.5 g / day: with a CC of more than 71 and a body weight of more than 70 kg - 500 mg every 8 hours; with CC more than 71 and body weight 50-60 kg - 250 mg every 6 hours; with CC more than 71 and body weight 40 kg - 250 mg every 8 hours; with CC more than 71 and body weight 30 kg - 125 mg every 6 hours. With CC 41-70 and body weight more than 70 kg - 250 mg every 6 hours; with CC 41-70 and body weight 50-60 kg - 250 mg every 8 hours; with CC 41-70 and body weight more than 40 kg - 125 mg every 6 hours; with CC 41-70 and body weight 30 kg - 125 mg every 8 hours. With CC 21-40 and body weight more than 60 kg - 250 mg every 8 hours; with CC 21-40 and body weight 50 kg - 250 mg every 12 hours; with CC 21-40 and body weight 30-40 kg - 125 mg every 8 hours. With CC 6-20 and body weight more than 50 kg - 250 mg every 12 hours; with CC 6-20 and body weight 30-40 kg - 125 mg every 12 hours.
When prescribed in a total daily dose of 2 g / day: with a CC of more than 71 and a body weight of more than 70 kg - 500 mg every 6 hours; with CC more than 71 and body weight 60 kg - 500 mg every 8 hours; with CC more than 71 and body weight 40-50 kg - 250 mg every 6 hours; with CC more than 71 and body weight 30 kg - 250 mg every 8 hours. With CC 41-70 and body weight more than 70 kg - 500 mg every 8 hours; with CC 41-70 and body weight 50-60 kg - 250 mg every 6 hours; with CC 41-70 and body weight 40 kg - 250 mg every 8 hours; With CC 41-70 and body weight 30 kg - 125 mg every 6 hours. With CC 21-40 and body weight over 70 kg - 250 mg every 6 hours; with CC 21-40 and body weight 50-60 kg - 250 mg every 8 hours; with CC 21-40 and body weight 40 kg - 250 mg every 12 hours; with CC 21-40 and body weight 30 kg - 125 mg every 8 hours. With CC 6-20 and body weight more than 40 kg - 250 mg every 12 hours; with CC 6-20 and body weight 30 kg - 125 mg every 12 hours.
When prescribed in a total daily dose of 3 g / day: with a CC of more than 71 and a body weight of more than 70 kg - 1000 mg every 8 hours; with CC more than 71 and body weight 60 kg - 750 mg every 8 hours; with CC more than 71 and body weight 50 kg - 500 mg every 6 hours; with CC more than 71 and body weight 40 kg - 500 mg every 8 hours; with CC more than 71 and body weight 30 kg - 250 mg every 6 hours. With CC more than 41-70 and body weight more than 70 kg - 500 mg every 6 hours; with CC more than 71 and body weight 50-60 kg - 500 mg every 8 hours; with CC more than 71 and body weight 40 kg - 250 every 6 hours; with CC more than 71 and body weight 30 kg - 250 mg every 8 hours. With CC 21-40 and body weight more than 60 kg - 500 mg every 8 hours; with CC 21-40 and body weight 50 kg - 250 mg every 6 hours; with CC 21-40 and body weight 30-40 kg - 250 mg every 8 hours. With CC 6-20 and body weight more than 60 kg - 500 mg every 12 hours; with CC 6-20 and body weight 30-50 kg - 250 mg every 12 hours.
When prescribed in a total daily dose of 4 g / day: with a CC of more than 71 and a body weight of more than 70 kg - 1000 mg every 6 hours; with CC more than 71 and body weight 60 kg - 1000 mg every 8 hours; with CC more than 71 and body weight 50 kg - 750 mg every 8 hours; with CC more than 71 and body weight 40 kg - 500 mg every 6 hours; with CC more than 71 and body weight 30 kg - 500 mg every 8 hours. With CC 41-70 and body weight more than 60 kg - 750 mg every 8 hours; with CC 41-70 and body weight 50 kg - 500 mg every 6 hours; with CC 41-70 and body weight 40 kg - 500 mg every 8 hours; with CC 41-70 and body weight 30 kg - 250 mg every 6 hours. With CC 21-40 and body weight more than 70 kg - 500 mg every 6 hours; with CC 21-40 and body weight 50-60 kg - 500 mg every 8 hours; with CC 21-40 and body weight 40 kg - 250 mg every 6 hours; with CC 21-40 and body weight 30 kg - 250 mg every 8 hours. With CC 6-20 and body weight more than 50 kg - 500 mg every 12 hours; with CC 6-20 and body weight 30-40 kg - 250 mg every 12 hours.
Patients with CC 6-20 in most cases are prescribed 125-250 mg every 12 hours, because with the appointment of 500 mg every 12 hours, the risk of seizures increases.
For patients with CC less than 6 ml / min / 1.73 m2, the drug is prescribed if hemodialysis is performed within 48 hours, while the doses correspond to those prescribed for patients with CC 6-20 ml / min / 1.73 m2. Imipenem and cilastatin are removed during hemodialysis, therefore the drug is administered after the procedure and further with an interval of 12 hours. Patients with CNS infections on hemodialysis are prescribed the drug if the expected benefit outweighs the risk.
Children older than 3 months are prescribed at a dose of 15-25 mg / kg every 6 hours (with the exception of CNS infections). With a high sensitivity of pathogens, the total daily dose should not exceed 2 g, with a moderate sensitivity of the pathogen - 4 g. Doses of more than 90 mg / kg / day are prescribed for cystic fibrosis.
Children under 3 months of age (with a body weight of more than 1500 g): in the early neonatal period (up to 7 days) - 25 mg / kg every 12 hours; in the late neonatal period (8-28 days) - 25 mg / kg every 8 hours; at the age of 1-3 months - 25 mg / kg every 6 hours. A dose of up to 500 mg is administered within 15-30 minutes, more than 500 mg - within 40-60 minutes.
Children with infections of the central nervous system or chronic renal failure (with a body weight of less than 30 kg) the drug is not prescribed.
When administered intramuscularly to patients with infections of the lower respiratory tract, skin and subcutaneous tissues and gynecological infections with mild and moderate severity of the disease, depending on the severity, 500-750 mg is prescribed every 12 hours. For intra-abdominal infections, 750 mg is prescribed every 12 hours. The drug is injected deep into a large muscle with a needle at least 21 in size and diameter 2. The powder is mixed with 2 ml of 1% lidocaine hydrochloride solution (without epinephrine), water for injection or 0.9% NaCl solution until a homogeneous suspension (white or slightly yellow) is formed. ...
The maximum daily dose is 1500 mg.
Treatment should be continued for another 2 days after symptoms resolve. The efficacy and safety of treatment after 14 days of use, as well as in patients with CC less than 20 ml / min / 1.73 m2, has not been studied.
special instructions
Stains urine reddish.
The dosage form for intramuscular administration should not be used for intravenous administration and vice versa.
Before starting therapy, a thorough history should be collected for previous allergic reactions to beta-lactam antibiotics.
Individuals with a history of gastrointestinal diseases (especially colitis) have an increased risk of developing pseudomembranous colitis.
Therapy with antiepileptic drugs in patients with a history of brain injury or seizures should be continued for the entire period of drug treatment (in order to avoid side effects from the central nervous system).
It should be borne in mind that in elderly patients, age-related renal dysfunction is likely, which may require a dose reduction.
Interaction
Pharmaceutically incompatible with lactic acid salts, other antibacterial drugs.
With simultaneous use with penicillins and cephalosporins, cross-allergy is possible; shows antagonism towards other beta-lactam antibiotics (penicillins, cephalosporins and monobactams).
Ganciclovir increases the risk of developing generalized seizures.
Significantly reduces the concentration of vaplproic acid in the blood, which can reduce the effectiveness of anticonvulsant therapy.
Drugs that block tubular secretion insignificantly increase the plasma concentration and T1 / 2 of imipenem (if high concentrations of imipenem are required, it is not recommended to use these drugs at the same time).