INSTRUCTIONS FOR MEDICAL USE
Trade name of the drug: Reacin
Active substance (INN): Amikacin
Dosage form: Solution for injection
2 ml of the solution (1 ampoule) contains:
Active ingredient: Amikacin (as sulfate): 100 mg and 500 mg.
Excipients: sodium citrate two aqueous, sodium metabisulfite, sulfuric acid 35%, water for injection.
Description: clear, colorless or slightly yellowish liquid.
Pharmacotherapeutic group: antibiotic of aminoglycoside group.
ATX code: J01GB06
It is a broad-spectrum antibiotic. It actively penetrates through cell membrane and irreversibly binds with specific receptor proteins on 30S ribosome subunit. Disrupts the formation of a complex between matrix (informational) RNA and the 30S subunit of the ribosome. This results in the misreading of information from RNA and the formation of incomplete proteins. Polyribosomes disintegrate and lose the ability to synthesize protein, which leads to the death of the microbial cell.
Highly active against most gram-negative and some gram-positive microorganisms: Pseudomonas aeruginosa, including those resistant to gentamicin, tobramycin, sizomycin and netilmicin, Escherichia coli, Klebsiella spp. Serratia spp., Providencia spp., Enterobacter spp., Salmonella spp., Shigella spp., Streptococcus spp., Staphylococcus spp. including those resistant to penicillin, methicillin and some cephalosporins. It has bacteriostatic effect on Mycobacterium tuberculosis resistant to streptomycin, isoniazid, PASK and other anti-tuberculosis drugs. Anaerobic microorganisms are resistant to the drug.
Amikacin does not lose activity under the action of enzymes inactivating other aminoglycosides and may remain active against strains of Pseudomonas aeruginosa resistant to tobramycin, gentamicin and netilmicin.
It is practically not absorbed from the gastrointestinal tract. It is administered i / v or i/m. Cmax is reached 1 h and 0.5 h after administration of 7.5 mg/kg i / v and is 21 and 38 µg/ml, respectively. Therapeutic concentration (15-25 mcg/ml) is maintained for 10-12 hours after v/m and v/v administration. Binding to plasma proteins is 4-11%. Distribution volume is 0.2-0.4 l/kg, in newborns up to 0.68 l/kg. It easily crosses histohematic barriers, penetrates into the tissue of lungs, liver, myocardium, spleen, bone tissue, is selectively accumulated in the cortical layer of kidneys and distributed in extracellular fluid, including serum, lymph, pleural, pericardial and peritoneal exudate, synovial fluid, abscess fluid. Determined in low concentrations in bile, bronchial secretion, muscle and fatty tissue. It is not metabolized. T1/2 is 2-4 hours in adults and 5-8 hours in newborns. Renal clearance is 79-100 ml/min; in patients with impaired renal function T1/2 is increased to 70-100 hours. It is excreted mainly by kidneys (65-94%) in unchanged form by glomerular filtration, forms high concentrations in urine; a small amount is excreted with bile.
Indications for use
Infectious-inflammatory diseases caused by Gram-negative microorganisms (resistant to gentamicin, sisomycin and kanamycin) or by associations of Gram-positive and Gram-negative microorganisms:
- Respiratory tract infections (bronchitis, pneumonia, pleural empyema, pulmonary abscess);
- septic endocarditis;
- CNS infections (including meningitis);
- Abdominal infections (including peritonitis);
- Infections of the urogenital tract (pyelonephritis, cystitis, urethritis);
- purulent skin and soft tissue infections (including infected burns, infected ulcers and bedsores of various genesis);
- biliary tract infections;
- Bone and joint infections (including osteomyelitis);
- wound infection;
- postoperative infections.
- neuritis of the auditory nerve;
- Severe chronic renal failure with azotemia and uremia;
- Hypersensitivity to the components of the drug;
- hypersensitivity to other aminoglycosides in anamnesis.
The drug should be used with caution in myasthenia gravis, parkinsonism, botulism (aminoglycosides may cause neuromuscular transmission failure, which leads to further weakening of skeletal muscles), dehydration, renal failure, during neonatal period, in premature children, in elderly patients, during lactation.
Digestive system: increased liver transaminase activity, hyperbilirubinemia, nausea, vomiting.
Allergic reactions: skin rash, itching, fever, rarely – Quincke’s edema.
Blood system: anemia, leukopenia, granulocytopenia, thrombocytopenia.
CNS and peripheral nervous system: headache, somnolence, impaired neuromuscular transmission, decreased hearing, up to permanent deafness, vestibular disorders.
Urinary system: oliguria, proteinuria, microhematuria, rarely – renal failure.
Dosage and administration
I/m, i/m (by jetting for 2 min or by dropwise at a rate of 60 drops per minute). Adults and children: 5 mg/kg every 8 hours or 7.5 mg/kg every 12 hours; the maximum dose is 15 mg/kg/day, the course dose is not more than 15 g. In premature infants: the initial dose is 10 mg/kg and then 7.5 mg/kg every 18-24 hours; in newborns the initial dose is 10 mg/kg and then 7.5 mg/kg every 12 hours. The duration of treatment by intravenous injection is 3-7 days, by intravenous injection – 7-10 days. Patients with renal insufficiency need to correct the dosage regimen according to creatinine clearance.
Symptoms: toxic reactions, neuromuscular block up to respiratory arrest, CNS depression (lethargy, coma, deep respiratory depression) in infants.
Treatment: calcium chloride IV, anticholinesterase agents (neostigmine p/k), m-choline blockers (atropine), symptomatic therapy. Hemodialysis and peritoneal dialysis are effective in impaired renal function, and exchange blood transfusion is performed in newborns.
Interaction with other drugs
Risk of nephrotoxic action increases when concomitant use of amikacin with amphotericin B, vancomycin, methoxiflurane, enflurane, NSAIDs, X-ray contrast agents, cephalothin, cyclosporine, cisplatin, polymyxins.
The risk of ototoxicity increases when concomitant use of amikacin with diuretics (furosemide, etacrynic acid), cisplatin.
When concomitant use with penicillins (in renal insufficiency) antimicrobial effect is reduced.
Concomitant use with ethyl ether and neuromuscular transmission blockers increases the risk of respiratory depression.
Amikacin is incompatible in solution with penicillins, cephalosporins, amphotericin B, chlorothiazide, erythromycin, heparin, nitrofurantoin, thiopentone as well as, depending on solution composition and concentration, with tetracyclines, B vitamins, vitamin C and potassium chloride.
Before use, the sensitivity of the isolated pathogens is determined using disks containing 30 µg amikacin. If the diameter of the growth-free zone is 17 mm or more, the microorganism is considered sensitive, 15 to 16 mm – moderately sensitive, less than 14 mm – resistant.
Plasma concentration of amikacin should not exceed 25 µg/ml (therapeutic concentration is 15-25 µg/ml).
Kidney, auditory nerve and vestibular function should be monitored at least once a week during treatment.
The probability of nephrotoxicity is higher in patients with impaired renal function, as well as when prescribing high doses or for a long time (daily monitoring of renal function may be required in this category of patients).
In case of unsatisfactory audiometric tests, the drug dose is reduced or the treatment is discontinued.
Patients with infectious inflammatory diseases of the urinary tract are recommended to take increased amount of fluid with adequate diuresis.
In the absence of positive clinical dynamics, it should be remembered about the possibility of development of resistant microorganisms. In such cases, it is necessary to cancel the treatment and initiate appropriate therapy. Sodium disulfite contained in the drug may cause allergic complications (up to anaphylactic reactions) in patients, especially in patients with allergic history.
Administration during pregnancy and lactation
The drug is contraindicated in pregnancy.
In case of vital indications the drug may be used in lactating women. It should be kept in mind that aminoglycosides are excreted with breast milk in small amounts. They are poorly absorbed from the gastrointestinal tract, and related complications in infants have not been recorded.
Use in patients with impaired renal function
It is contraindicated in severe chronic renal failure with azotemia and uremia.
Correction of dosage regimen is required in case of impaired renal excretory function.
Administration in elderly patients
Caution should be exercised when using in elderly patients.
Form of production
Solution for injection 500 mg/2 ml and 100 mg/2 ml in 2 ml ampoules 1 ml.
Store in a dry, dark place at a temperature not exceeding 25°C. Keep out of the reach of children!
2 years. Do not use after the expiration date.
Conditions of dispensing from pharmacies
Released by a doctor’s prescription