CostaU

1 ampules of 2 and 4 ml

Active substance: Amicacin, in the form of amikacin sulfate - 500 (1000) mg. Restfarms: sodium citrate; sodium metabisulphite; sulphuric acid; water for injections.

ATH / PBX Code:J01GB06.

Pharmacotherapeutic group

Antibacterial agents for systemic use. Aminoglycosidic antibiotics. Other aminoglycosides.

Description

Transparent colorless or slightly yellowish solution.

Pharmacological properties

Pharmacodynamics

Amicacin sulfate is an aminoglycosidic antibiotic, which is active against a wide range of gram-negative microorganisms, including Pseudomonas. sPP., Escherichia. coli., indole positive and indole negative microorganisms Proteus. sPP., Klebsiella- Enterobacter.- Serratia. sPP., Salmonella, Shigella, Minea.- Herellae., Citrobacter. Freundii. andProvidencia. sPP..

Many strains of these gram-negative organisms resistant to gentamicin and tobramycin, show sensitivity to amikacin iN. vitro.. The main gram-positive organism sensitive to amikacin is Staphylococcus aureus., Including strains resistant to meticillin. Amicacin has some activity against other gram-positive organisms, including certain strains Streptococcus pyogenes, Enterprocci. and Diplococcus pneumoniae..

Pharmacokinetics

Amikacin after intramuscular administration (in / m) quickly absorbed. An hour after the introduction in a dose of 250 mg or 500 mg, the maximum serum concentration is about 11 mg / l and 23 mg / l, respectively; And 10 hours after injection - about 0.3 mg / l and 2.1 mg / l, respectively.

Twenty percent or less associated serum or free drug proteins have a bactericidal effect to microorganisms sensitive to it within 10-12 hours.

Amicacin is freely distributed in extracellular fluid, is displayed mainly by glomerular filtration without changing, with urine. The half-life in patients with normal renal function is two to three hours.

With the normal function of the kidneys in the first 6 hours, it is removed with the urine unchanged about 65% of the dose entered and 91% in 24 hours. The average concentration in the urine for 6 hours is 563 μg / ml and 163 mg / l for 6-12 hours. The average concentration in the urine after the dose of 500 mg entered in / m is 832 mg / l in the first six hours.

The maximum concentration of amikacin in serum after one-time intravenous infusion healthy patients at a dose of 500 mg, for 30 minutes, at the end of the infusion is 38 mg / l. Repeated administration The drug does not hold to its accumulation.

After parenteral administration, amikacin is found in the spinal, pleural and amniotic fluidsas well as in the abdominal cavity.

Multicenter data clinical studies show that healthy children in spinal fluid The concentration of amikacin is about 10-20% of its concentration in serum and can reach 50% when meningitis. In newborns and, especially in premature babies, the removal of amikacin kidneys is reduced during its intramuscular or intravenous administration.

In a single center study, a newborn (1-6 days after childbirth) grouped by weight (<2000, 2000-3000 и > 3000 g) administered amikacin intramuscularly and / or intravenously at a dose of 7.5 mg / kg. Clearance in newborns with a weight\u003e 3000 g was 0.84 ml / min / kg, and the half-life was about 7 hours. In this group, the initial volume of the distribution and the volume of the distribution at an equilibrium state was 0.3 ml / kg and 0.5 mg / kg, respectively. In groups of newborns with a lower weight, the clearance / kg of amikacin was less, and the half-life - longer period. Repeated administration of the drug every 12 hours in all of the above groups did not demonstrate the accumulation of the drug for 5 days.

Indications for use

Amicacin is used in short-term treatment of serious infections caused by gram-negative bacteria sensitive to the drug.

The drug can also be used to treat diseases caused by staphylococcal or with suspected staphylococcal infection. Official recommendations should be taken into account on the proper use of antibacterial agents.

Method of application and dose

Amicacin Do not pre-mix with others drugs, And should be administered separately in accordance with the recommended dose and the method of administration.

For most infections, intramuscular administration is preferred. But with infections, threatening life, or at the impossibility of intramuscular administration, they are prescribed slowly intravenously inkjet (2-3 minutes), or an infusion (0.25% solution for 30 minutes).

Intramuscular and intravenous administration

Amikacin can be introduced intramuscularly and intravenously.

When prescribed in the recommended doses with non-complicated infections caused by microorganisms sensitive to amikaccin, the therapeutic response can be obtained within 24-48 hours. If a clinical response is not received within 3-5 days, it is necessary to assign alternative therapy.

For proper calculation of the dose:

Weigh the patient; evaluate the function of the kidneys, measuring creatinine concentration in blood serum or having calculated the level of creatinine clearance; During treatment with amikacin, periodic monitoring of the kidney function is recommended.

If it is possible, it is necessary to determine the concentration of amikacin in serum (maximum and minimal serum concentration periodically during therapy).

The maximum serum concentration of amikacin (30-90 minutes after injection) should be avoided (30 μg / ml, minimal serum concentration (immediately before the introduction of the next dose) is more than 10 μg / ml. In patients with normal kidney function, amikacin can be prescribed 1 time per day, in this case the maximum serum concentration May exceed 35 μg / ml. Usually the duration of therapy is 7-10 days.

The total dose independently of the path of administration should not exceed 15-20 mg / kg / day.

With complicated infections, when a course of treatment is needed for more than 10 days, the kidney function should be carefully monitored, auditory and vestibular touch system, as well as the level of serum amikacin.

If there is no clinical improvement for 3-5 days, the use of amikacin needs to stop and double-check the sensitivity of microorganisms to amikacin.

Dose Calculation

Adults and children over 12 years old: with normal kidney function (clearance creativenina≥ 50 ml / min) per / m or in / at 15 mg / kg / day 1 time per day or 7.5 mg / kg every 12 hours. The total daily dose should not exceed 1.5 g. With endocarbage and febrile neutropenia - the daily dose must be divided into 2 administrations, because There is not enough data on the introduction of 1 time per day.

Children from 4 weeks – 12 years: with normal kidney function (creatinine clearance≥ 50 ml / min) V / m or V / B (intravenously slowly infusionally) 15-20 mg / kg / day 1 time per day or 7.5 mg / kg every 12 hours. With endocarditis and febrile neutropenia - the daily dose must be divided into 2 administrations, because There is not enough data on the introduction of 1 time per day.

Newborn children: The initial load dose is 10 mg / kg, then 7.5 mg / kg every 12 hours.

Premature newborns: 7.5 mg / kg every 12 hours.

Special recom ndations for intravenous administration

Adults and children, a solution of amikacin, as a rule, is introduced infusion for 30-60 minutes.

For up to 2 years old, infusion should be introduced within 1 - 2 hours.

Solution for intravenous application Prepare by adding the desired dose to 100 ml or 200 ml of sterile diluent: normal saline or 5% dextrose in water.

In children, the amount of diluent used will depend on the amount of amikacin carried by the patient.

Elderly patients

Amicacin is excreted by the kidneys. The kidney function should be estimated and prescribed a dose as in violation of the excretory function of the kidneys.

Infections, threatening life and / or causedPseudomonas.

The dose in adults can be increased to 500 mg every 8 hours, but do not introduce amikacin at a dose of more than 1.5 g per day, and not more than 10 days. The total maximum term dose should not exceed 15 grams.

Infection urinary tract (Other not causedPseudomonas.). Dose equal to 7.5 mg / kg / day divided into 2 equal doses (that adults are equivalent to 250 mg 2 times a day). Since the activity of amiccin increases by increasing the pH, a means to simultaneously applied to the urine.

Calculation of the dose of amikacin in violation of the excretory function of the kidneys (creatinine clearance<50 мл/мин)

Patients with violation of the excretory function of the kidneys:

Or increase the interval between the introduction of the recommended single dose; Or reduce the one-time recommended dose - at a fixed interval between the introductions of amikacin.

Both methods are based on the determination of creatinine clearance or creatinine concentration in the patient's serum.

In the event of an increase in the interval between the introductions (if the clearance level of creatinine is not known, the patient's condition is stable), the interval between the drugs is established as follows:

interval (clock) \u003d Creatine concentration in blood serum (in mg / 100 ml) × 9. For example, the concentration of creatinine in serum 2 mg / 100 ml, then a single dose (7.5 mg / kg) is recommended to enter every 18 hours.

Creatinine concentration in blood serum (mg / 100 ml)		Interval between Introduction Games in a dose of 7.5 mg / kg (clock)
1,5	× 9.	13,5
2,0		18
2,5		22,5
3,0		27
3,5		31,5
4,0		36
4,5		40,5
5,0		45
5,5		49,5
6,0		54

Determination of a reduced one-time dose at a fixed interval between the introduction of amikacin

When the renal function is broken and the administration of sulfate amiccin is preferably at a fixed time interval, a dose should be reduced. In these patients, it is desirable to determine the concentration of amikacin in the blood serum to avoid exceeding the serum concentration. If the determination of serum amicacine concentration is impossible, and the patient's condition is stable, the values \u200b\u200bof the clearance of whey creatinine and creatinine are the most affordable indicators of the degree of renal failure for use as a guide to reduce the dose of the drug.

Initial (load dose) in violation of the excretory function of the kidneys - 7.5 mg / kg

The calculation of the maintenance dose is made by the formula:

Supporting dose (mg) (introduced every 12 hours) \u003d

creatinine clearance (ml / min) × Calculated initial (load dose) (mg) Creatinine clearance normal (ml / min)

An alternative method for calculating a reduced dose of amikacin at 12 o'clock intervals between administration (in patients with a known value of equilibrium (stationary) concentration of creatinine in plasma): divide the conventional recommended dose to the patient's serum creatinine value.

Due to the fact that the kidney function can change significantly during the use of amiccin, the creatinine of blood serum should be regularly monitored, and if necessary, adjust the dosing mode.

Side effect

Side effects are presented with an indication of the class of the system of organs and indicating the frequency of the occurrence: very often (≥1 / 10), often (≥1 / 100,<1/10), нечасто (≥1/1000, <1/100), редко (≥1/10000, <1/1000), очень редко (<1/10000) и частота неизвестна (не может быть оценена на основе имеющихся данных).

Blood violations and lymphatic system: seldom - anemia, eosinophilia;

immunuted violations: frequency unknown - anaphylactic reactions (anaphylactic reactions, anaphylactic shock and anaphylactoid reactions), hypersensitivity;

violations of metabolism and nutrition: seldom - hypomagnation;

violations from the nervous system: seldom - Tremor, Paresthesia, Headache, Equilibrium Disorder; frequency unknown - paralysis;

violations of the organ of vision: seldom - blindness, mesh infarction;

violations by the organ of hearing and the labyrinth: seldom - ringing in the ears, hearing loss; unknown - deafness, deafness neurosensory;

vessel violations: seldom - hypotension;

violations by the respiratory system, chest and mediastinal organs: frequency unknown - apnea, bronchospasm;

gastrointestinal disorders: seldom - nausea, vomiting;

disorders from the skin and subcutaneous fabrics: seldom - rash, skin itching, urticaria;

violations from muscular, skeletal and connective tissue: seldom - arthralgia, muscular twitching;

disorders from the kidneys and urinary tract: reco-Oliguria, an increase in creatinine in the blood, albuminuria, azotemia, red blood cells in the urine, white blood cells in the urine; frequency unknown - acute renal failure, toxic nephropathy, cells in the urine;

general disorders and reactions at the injection site: seldom - fever.

Soosuggestion about unwanted reactions

It is important to report suspects of unwanted reactions after registering the drug in order to ensure continuous monitoring of the ratio of "benefits - risk" of the drug. It is recommended to report any suspects of unwanted drug reactions through national communication systems about unwanted reactions and non-efficiency of medicines.

If a patient has any unwanted reactions, it is recommended to consult with the doctor. This recommendation applies to any possible unwanted reactions, including those not listed in the liner. You can also report unwanted reactions to the information database of unwanted reactions (actions) for drugs, including messages about the ineffectiveness of medicines. By informing unwanted reactions, you help get more information about the safety of the drug.

Contraindications

Increased sensitivity to amikacin, other aminoglycosides and auxiliary components of the drug (see section "Composition"), Miasthenia Gravis, Near Hearing Nerva, Heavy Chronic Renal Insufficiency with Azotemia and Uremia.

With caution: Parkinsonism, botulism (aminoglycosides can cause a disruption of neuromuscular transmission, which leads to a further weakening of skeletal muscles), dehydration, renal failure, a period of newborn, the presence of children, an elderly age.

Patients receiving aminoglycosides must be under constant clinical observation due to their associated potential altoxicity and nephrotoxicity.

Amicacin safety for a 14-day treatment period is not shown.

Overdose

In the event of an overdose, there is a risk of developing nephro-, and neurotoxic (neuromuscular blockade) of reactions.

The neuromuscular blockade with a respiratory stop requires appropriate treatment, including the use of calcium preparations (for example, 10-20% solution of gluconate or lactobionate).

In the event of an overdose or toxic reaction, peritoneal dialysis or hemodialysis will help reduce the concentration of amikacin in the blood.

The level of amikacin is also reduced with continuous arteriovenous hemofiltration.

Newborn babies can use blood transfusion.

Interaction with other drugs and other types of mutualaction

It should be avoided either systemic or local use of amikacin with other neurotoxic, withdochetic or nephrotoxic drugs, in particular bacitracycling, cisplatin, amphotericin AT,cIKlenosporin, torolimus, cephaloridine, paromomycin, viomycin, polymixin AT,berissistine, vancomycin or others aminoglycosides Due to the possible total effect. It has been reported an increase in the risk of nephrotoxicity while simultaneously parenteral administration aminoglycosides Antibiotics and cephalosporins. Recognizing appointment cephalosporins It may falsely increase the level of creatinine in serum. If possible, carefully control.

The risk of isotoxicity increases with the use of amikacin in combination with fast-acting diuretics, especially with intravenous administration of the diuretic. Diuretics can enhance the toxicity of aminoglycoside, changing the concentration of antibiotics in serum and tissue. These drugs include furosemid and stacrinovaya acid, Which in itself is a cast-toxic drugs. As a result, irreversible deafness can develop.

The use of amikacin is not recommended in patients receiving anesthetics or myelorelaxants (including ether,galotan, d.- tubokuran, succinylcholine deboiming, atrakuria, rocuroni, centurian Or in patients receiving massive blood transfusion with citrate preservatives), as neuromuscular blockade may occur and the subsequent stop of the respiratory. If blockade occurs, calcium salts can remove this action.

Indomethacin may increase the concentration of amikacin in plasma in newborns.

In patients with disturbed kidney function, the decrease in the activity of aminoglycosides can occur while using drugs penicillin.

In the study iN. vitro. It is shown that the interaction of aminoglycosides with beta-lactam antibiotics (penicillins or cephalosporins) It can lead to a significant decrease in mutual activity. Reducing the activity of amikacin in blood serum is also observed with separate administration iN. vivo aminoglycoside or penicillin. The inactivation of aminoglycoside is clinically significant was observed only in patients with serious impaired kidney function. Inactivation can continue in samples of organism fluids collected for analysis, which leads to inaccurate readings of aminoglycoside. Such samples should be properly handled (analyze quickly, freeze or processed beta lactamase).

With the introduction of amikacin with bisphosphonate Increased risk of hypocalcemia.

With the introduction of aminoglycoside with platinum compounds An increased risk of nephrotoxicity may arise and, possibly, output.

Simultaneous administration with amikacin thiamine (vitamin B1) It can lead to the destruction of thiamine metabisulfite sodium composite of sulfate amikacin.

Precautionary measures

All aminoglycosides are capable of inducing the isotoxicity, renal toxicity and neuromuscular blockade. These toxicity occur more often in patients with renal failure, in patients receiving other differentoxic or nephrotoxic drugs, and in patients receiving amikacin treatment for longer periods of time and / or with higher doses than recommended.

Care should be exercised in patients with previously existing renal failure or previously existing auditory or vestibular disorders. Cautions for dispensing and conduct adequate hydration should be observed.

In patients with impaired kidney function or reduced glomerular filtration, the kidney function should be estimated by conventional methods to therapy and periodically during therapy. To avoid abnormally high levels of amikacin in the blood and minimize the risk of isotoxicity, daily doses and / or elongated the interval between doses in accordance with the concentrations of creatinine serum should be reduced. Regular monitoring of the concentration of the drug in serum and kidney function is especially important in elderly patients who may have a reduced kidney function, which is not manifested by the results of conventional screening tests, i.e. Concentration of urea and creatinine in serum. If it is expected that therapy will continue seven days or more in patients with renal failure or 10 days from other patients, it is recommended to make an audiogram before treatment and control it during therapy. Amikacin should be canceled if noise is developing in ears or subjective hearing loss or if the control audiograms show a significant loss of response to the sound of high frequency.

Changes to the kidney function are usually reversible when the use of the drug stopped.

Toxic effects on the eighth cranopy brain nerve can lead to a loss of hearing, loss of equilibrium or to the other. Amikacin, first of all, affects the auditory function. Cochlear neuritis auditory nerve includes high-frequency deafness and usually occurs before the clinical loss of hearing can be detected by audiometric testing.

The risk of toxicity caused by aminoglycoside is higher in patients with impaired renal function and in those who receive high doses, or those whose therapy lasts more than 5-7 days. The first may happen high-frequency deafness. A dizziness may be observed, which indicates vestibular disorders. Other symptoms of neurotoxicity, manifest to vestibular and / or hearing output, may include numbness, feeling tingling on the skin, twitching muscles and convulsions. The risk of aminoglycosides is increased with an increase in the degree of exposure as a result of either the persistence of high peak concentrations, or a constantly high level in serum. Patients who develop cochlearic or vestibular disorders may not have symptoms during therapy, on the basis of which it would be possible to prevent the development of toxic damage to the eighth pair of nerves. Full or partial irreversible double-sided deafness or dizziness can be observed after the use of the drug. Usually ototoxich nosta induced aminoglycoside , irreversible.

Application of amiccin in patients with allergies on aminoglycosides or in patients who may have subclinical signs of violation of the kidney function or damage to the eighth pair of nerves caused by the preceding appointment of nephrotoxic and / or over-cells, such as streptomycin, dihydrosthydomycin, gentamicin, tobramycin, kanamycin, biscanicin, Neomycin, Polymixin B, Kolistin, Cephaloridin or Biomycin should be considered with caution, since toxicity can be summed up. In these patients, amikacin should be applied only if, according to a doctor, therapeutic advantages outweigh potential risks.

A macular infarction has been reported, sometimes leading to constant loss of vision, after intraocular administration (injection in the eye) of amikacin.

Under the recommended precautions and doses of amikacin, the frequency of toxic reactions, such as noise in ears, dizziness and partial reversible deafness, skin rash, fever, headache, paresthesia, nausea and vomiting are low.

The urinary signs of kidney irritation (albumin, red or white cells), azotemia and Oliguria, although they are rarely found.

Before appointment of amikacin, the sensitivity of the selected pathogens is determined using discs containing 30 μg of amikacin. When the diameter of the height-free zone is 17 mm and more microorganism is considered sensitive, from 15 to 16 mm - moderately sensitive, less than 14 mm - stable.

The concentration of amikacin in the plasma should not exceed 25 μg / ml (therapeutic concentration of 15-25 μg / ml).

Cases of neuromuscular blockade and respiratory paralysis are recorded after parenteral injection, local instillation (with orthopedic and abdominal irrigation or with local treatment of empynesses), oral use of aminoglycosides. The ability of respiratory paralysis should be considered if the aminoglycosides were administered in any way, especially in patients receiving anesthetics, neuromuscular blockers, or in patients who received massive curtain blood transfuses. If neuromuscular blockade occurs, it is recommended to introduce calcium salts that can eliminate respiratory paralysis, but mechanical respiratory assistance can still be required. Nervous muscular blockade and muscle paralysis have been demonstrated in laboratory animals at high amikacin doses.

Amikacin should not be used in patients with Miastenia Gravis. Aminoglycosides should be used with caution in patients with muscle disorders, such as Parkinsonism, since these drugs may aggravate the weakness of the muscles due to their potential strip-like effect on the neuromuscular compound.

During the treatment period, it is necessary at least 1 time a week to control the function of the kidneys, auditory nerve and the vestibular apparatus.

The likelihood of the development of nephrotoxicity is higher in patients with impaired kidney function, as well as when prescribing high doses or its use for a long time\u003e 5-7 days (this category of patients may require daily control of the kidney function).

Renal toxicity does not depend on maximum (peak) plasma concentrations (WITHtAX) amikacin. Patients should be well hydrated during treatment and renal function should be estimated by conventional methods prior to the start of therapy and daily during the course of treatment. Reducing the dosage is required if there are signs of renal dysfunction, such as the presence of pathological changes in the urine, reduced clearance of creatinine, reduced urine specific weight, increase blood urea, creatinine in blood serum or oliguria. If nitotemia increases or if the diurea reduction progresses, treatment should be discontinued.

Elderly patients can reduce the renal function, which can manifest itself in conventional screening tests, such as urea concentration or serum creatinine. At the same time, the determination of creatinine clearance can be more useful. Monitoring renal function in elderly patients during the treatment of aminoglycosides is especially important.

The functions of the kidneys and the eighth pair of cranial nerves should be carefully monitored, especially in patients with well-known or alleged renal failure at the beginning of therapy, as well as those whose renal function is initially normal and in which signs of renal dysfunction develop during therapy. When it is possible, it is recommended to control the concentration of amikacin in serum to provide adequate concentrations and to prevent potentially toxic levels. It is recommended to regularly monitor the overall urine analysis, the concentration of urea and creatinine in blood serum or creatinine clearance. If it is possible to do audiograms especially in patients with high risk of toxicity. Evidence of the isotoxicity (dizziness, including vestibular dizziness, the noise in the ears, ringing in the ears and loss of hearing) or nephrotoxicity requires the abolition of a drug or a dose adjustment. Parallel and / or consistent systemic, oral or local use of other neurotoxic or nephrotoxic drugs, in particular bacitracycling, cisplatin, amphotericin, cephaloridine, ferryomycin, vyomycin, polymixine, colorsine, vancomycin or other aminoglycosides should be avoided. Other factors that can increase the risk of toxicity is an elderly age and dehydration.

Aminoglycosides should be used with caution in premature and newborn children due to the immaturity of the kidneys in these patients and, as a result, lengthening the half-life of these medicines.

With unsatisfactory audiometric tests, the dose of the drug reduce or cease treatment.

Patients with infectious inflammatory diseases of the urinary tract it is recommended to receive an increased amount of fluid during adequate diurea.

In the absence of positive clinical dynamics, it should be remembered for the possibility of the development of resistant microorganisms. In such cases, it is necessary to cancel the treatment and start conducting appropriate therapy.

Amicacin contains sodium metabisulphite, which may occasionally cause severe hypersensitivity reactions and bronchospasm.

Amicacine in 2 ml dosage contains 0.504 mmol or 11.54 mg of sodium, into a dosage of 4 ml - 1.008 mmol or 23.08 mg of sodium, which must be taken into account patients on a diet with a limited flow of sodium.

Application during pregnancy or breastfeeding

Pregnancy

The use of amikacin during pregnancy and in newborns is possible only by life indications and under the supervision of the doctor.

The literature meets limited information on the use of aminoglycosides during pregnancy. Aminoglycosides can cause damage to the fetus. Amikacin penetrates through the placenta, and can lead, as reported, to the full of irreversible bilateral congenital deafness in children whose mothers received streptomycin During pregnancy. Although the side effects on the fruit or newborns were not observed in pregnant women who received other aminoglycosides, there is a chance to harm them. If amikacin is used during pregnancy or if the patient gets pregnant when taking this drug, the patient must be informed about the potential danger to the fetus.

Lactation

It is not installed, amikacin penetrates in breast milk. It is necessary to make a decision or to stop breastfeeding or termination of therapy. Fertility

In preclinical research of reproductive toxicity, they did not reveal the influence of amikacin for fertility or the development of the fetus in mice and rats.

Impact on the ability to control vehicles and other mechanisms

Not studied the effects of amikacin on the ability to control vehicles or other mechanisms. Due to the advent of some adverse reactions (see Side Activity), the ability to control vehicles and work with other mechanisms can be broken.

Shelf life

Storage conditions

In the light-protected place at a temperature not higher than 25 ° C. Keep out of the reach of children.

Conditions of vacation from pharmacies

Recommended by a doctor's prescription.

Packaging

2 ml or 4 ml in ampoules made of colorless glass. 5 ampoules into the liner from the film polyvinyl chloride. 2 liners along with the instructions for use in a pack of cardboard box (if necessary with a knife for opening an ampoules).

Packaging for hospitals.

10 contour cellular packs with ampoules along with instructions for use are placed in a box of cardboard for consumer packaging.

Manufacturer

Amicacin sulfate 1000mg

pharmachologic effect

Pharmacodynamics
Amicacin is a semi-synthetic antibiotic of a wide range of action, a bactericidal acts. By binding to the 30s ribosom subunit, prevents the formation of a complex of transport and matrix RNA, blocks protein synthesis, and also destroys cytoplasmic membranes of bacteria. Highly active in relation to aerobic gram-negative microorganisms - Pseudomonas Aeruginosa, Escherichia Coli, Klebsiella SPP., Serratia SPP., Providencia SPP., Enterobacter SPP., Salmonella SPP., Shigella SPP.; Some gram-positive microorganisms are Staphylococcus SPP. (including Penicillin resistant, some cephalosporins); Moderately active with respect to Streptococcus SPP. With a simultaneous purpose with benzylpenicillin, a synergistic effect has a synergistic effect on the Enterococcus Faecalis strains. Does not act on anaerobic microorganisms. Amikacin does not lose activity under the action of enzymes inactivating other aminoglycosides, and may remain active with respect to Pseudomonas Aeruginosa strains, resistant to drawramycin, gentamicin and neutylmicin.

Pharmacokinetics
After intramuscular administration is absorbed quickly and completely. Maximum concentration (Cmax) with intramuscular administration of 7.5 mg / kg - 21 μg / ml, after 30 minutes of a non-rated infusion of 7.5 mg / kg - 38 μg / ml. The time to achieve maximum concentration (TCMAX) is about 1.5 hours after intramuscular administration. Communication with plasma proteins is 4-11%. Well distributed in extracellular liquid (the contents of abscesses, pleural effusion, ascitic, pericardial, synovial, lymphatic and peritoneal liquid); In high concentrations, it is found in the urine; In low - in bile, breast milk, water wrapped in the eyes, bronchial secrete, sputter and spinal cord fluid (SMG). It penetrates well into all the tissues of the body, where it accumulates intracellular; High concentrations are noted in organs with good blood supply: light, liver, myocardium, spleen, and especially in the kidneys, where it accumulates in the cortical matter, lower concentrations - in muscles, adipose tissue and bones.

When presulting in the mid-merate doses (normally), adults amicacin does not penetrate the hematophephalic barrier (BGB), with inflammation of the brain shells, permeability increases slightly. Newborns achieved higher concentrations in the CMF than adults; It passes through the placenta - it is found in the blood of the fetus and amniotic fluid. The volume of distribution in adults - 0.26 l / kg, in children - 0.2-0.4 l / kg, in newborns - aged less than 1 week and body weight less than 1500 g - to 0.68 l / kg, aged less than 1 week and body weight 1500 g - to 0.58 l / kg, in patients with fibrosis - 0.3-0.39 l / kg. The average therapeutic concentration at a / in or per / m administration is preserved for 10-12 hours. Not metabolized.

Half-life (T1 / 2) in adults - 2-4 hours, in newborns - 5-8 hours, in older children - 2.5-4 h. The final value of T1 / 2 is more than 100 hours (release from intracellular depot). It is excreted by the kidneys by glomerular filtration (65-94%) mainly unchanged. Kidney clearance - 79-100 ml / min. T1 / 2 in adults in violation of the kidney function varies depending on the degree of violation - up to 100 hours, in patients with fibrosis - 1-2 hours, in patients with burns and hyperthermia T1 / 2 may be shorter compared to the average indicators due to increased clearance . It is derived during hemodialysis (50% in 4-6 h), peritoneal dialysis is less effective (25% in 48-72 h).

Indications

Infectious-inflammatory diseases caused by gram-negative microorganisms (resistant to gentamicin, cozyomycin and canamicin) or associations of gram-positive and gram-negative microorganisms:

• respiratory tract infections (bronchitis, pneumonia, empty pleura, lung abscess),
• sepsis,
• septic Endocarditis,
• infections of the central nervous system (CNS) (including meningitis),
• infections of the abdominal cavity (incl. peritonitis),
• urinary tract infections (pyelonephritis, cystitis, urethritis),
• purulent infections of the skin and soft tissues (including infected burns, infected ulcers and breakdowns of different genes),
• infections of biliary tract, bones and joints (including osteomyelitis),
• wound infection
• postoperative infections.

Contraindications

• Hypersensitivity (incl. To other aminoglycosides in history),
• neuritis the auditory nerve
• severe chronic renal failure with azotemia and uremia,
• pregnancy.

With caution - Miasthenia, Parkinsonism, botulism (aminoglycosides can cause a non-muscular transmission impairment, which leads to a further weakening of skeletal muscles), dehydration, renal failure, period of newborn, prematurity of children, elderly age, lactation period.

special instructions

Before use, the sensitivity of the selected pathogens is determined using discs containing 30 μg of amikacin. When the diameter of the height-free zone is 17 mm and more microorganism is considered sensitive, from 15 to 16 mm - moderately sensitive, less than 14 mm - stable. The concentration of amikacin in the plasma should not exceed 25 μg / ml (therapeutic concentration of 15-25 μg / ml).

During the treatment period, it is necessary at least 1 time a week to control the function of the kidneys, auditory nerve and the vestibular apparatus. The probability of the development of nephrotoxicity is higher in patients with impaired kidney function, as well as when prescribing high doses or for a long time (this category of patients may require daily kidney function control). With unsatisfactory audiometric tests, the drug dose reduce or cease treatment.

Patients with infectious inflammatory diseases of the urinary tract it is recommended to receive an increased amount of fluid. In the absence of positive clinical dynamics, it should be remembered for the possibility of the development of resistant microorganisms. In such cases, it is necessary to cancel the treatment and start conducting appropriate therapy. In the presence of life indications, the drug can be used in nursing women (aminoglycosides penetrate into breast milk in small quantities, however, they are weakly absorbed from the gastrointestinal tract, and there were no complications associated with them).

Structure

Active substance: Amicacin sulfate (in terms of amikacin) - 1000 mg.

Method of application and dose

Intramuscularly, intravenously (stove, for 2 minutes, or drip), adults and children over 6 years old - 5 mg / kg every 8 hours or 7.5 mg / kg every 12 hours; Bacterial infections of urinary tract (uncomplicated) - 250 mg every 12 hours; After the hemodialysis session, an additional dose can be assigned - 3-5 mg / kg.
Maximum doses for adults - 15 mg / kg / day, but not more than 1.5 g / day for 10 days.
The duration of treatment with in / in the introduction is 3-7 days, at a / m - 7-10 days.
Premature newborn initial dose - 10 mg / kg, then 7.5 mg / kg every 18-24 hours; Newborn and children up to 6 years old, the initial dose is 10 mg / kg, then 7.5 mg / kg every 12 hours for 7-10 days.

Patients with burns may be required to dose 5-7.5 mg / kg every 4-6 hours due to the shorter T1 / 2 (1-1.5 h) in these patients.
For intramuscular injection, a solution prepared by adding 250 mg or 500 mg of 2-3 ml of water for injection to the contents of the vial 250 mg.
Intravenously amikacin is injected droplet for 30-60 minutes, if necessary - intensity

For intravenous administration (stream), a solution prepared by adding 250 mg or 5-3 ml of water for injection or 0.9% solution of sodium chloride or 5% dextrose sodium solution is used.
For intravenous administration (drip), the contents of the vial are dissolved in 200 ml of 5% dextrose solution or 0.9% sodium chloride solution.
The concentration of amikacin in the solution for intravenous administration should not exceed 5 mg / ml.

Side effects

From the digestive system: nausea, vomiting, violation of the liver function (increase in the activity of "liver" transaminases, hyperbilirubinemia).

On the part of the blood formation organs: anemia, leukopenia, granulocyptopenia, thrombocytopenia.

From the side of the nervous system: headache, drowsiness, neurotoxic effect (twitching muscles, feeling of numbness, tingling, epileptic seizures), disruption of neuromuscular transmission (respiratory stop).

From the sides of the senses: Ostotoxicity (decrease in hearing, vestibular and labyrinth disorders, irreversible deafness), toxic effect on the vestibular apparatus (disincordination of movements, dizziness, nausea, vomiting).

From the urinary system: nephrotoxicity - impaired kidney function (oliguria, proteinuria, microhematuria).

Allergic reactions: skin rash, itching, hyperemia of the skin, fever, swelling of quinque.

Local: soreness at the injection site, dermatitis, phlebitis and perifelibate (with intravenous administration).

Medicinal interaction

Pharmaceutically incompatible with penicillins, heparin, cephalosporins, capeomycin, amphotericin, hydrochlorothiazide, erythromycin, nitrofurantine, vitamins of the group B and C, potassium chloride. Exhibits synergism when interacting with carbenicillin, benzylpenicillin, cephalosporins (in patients with severe chronic renal failure, with joint use with beta-lactam antibiotics, it is possible to reduce the effectiveness of aminoglycosides).

Nalidix Acid, Polymixin B, Cisplatin and Vancomycin increase the risk of developing and nephrotoxicity. Diuretics (especially furosemid), cephalosporins, penicillins, sulfalosporins and non-steroidal anti-inflammatory drugs, competing for active secretion in the tube nephron, block the elimination of aminoglycosides, increase their serum concentration, enhancing nephro- and neurotoxicity. Enhances the myarlaxizing effect of stripping drugs.

Methoxyfluran, polymixins for parenteral administration, cappeomycin and other drugs blocking neuromuscular transmission (halogenated hydrocarbons as drugs for inhalation anesthesia, opioid analgesics), transfusion of large amounts of blood with citrate preservatives increase the risk of respiratory stop. The parenteral administration of Indomethacin increases the risk of the development of the toxic actions of aminoglycosides (an increase in the half-life and reduction of clearance). Reduces the effect of antimaistical medicines.

Overdose

Symptoms: Toxic reactions (hearing loss, ataxia, dizziness, urination disorders, thirst, decline in appetite, nausea, vomiting, ringing or feeling of laundry in ears, respiratory impairment).

Treatment: To remove the blockade of neuromuscular transmission and its consequences - hemodialysis or peritoneal dialysis; Anticholinesterase products, calcium salts (CA2 +), artificial ventilation of the lungs, other symptomatic and supporting therapy.

Storage conditions Amikacin sulfate

In a dry, light-protected place at a temperature not higher than 25 ° C. Store in places inaccessible to children.

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Dosage form: & nbsppowder for the preparation of the solution for intravenous and intramuscular administration Structure:

Active substance : Amikacin Sulphate 500 mg (in terms of amikacin)

Description:

White or almost white powder.

Pharmacotherapeutic Group:Antibiotic aminoglycoside ATH: & NBSP

J.01.G.B.06 Amicacin

Pharmacodynamics:

A semi-synthetic antibiotic of a wide range of action from the group of aminoglycosides of the 3rd generation, acts bactericidally. Binding S.30 S. the ribosome subunit, prevents the formation of a complex of transport and matrix RNA, blocks protein synthesis, and also destroys the cell membranes of bacteria.

Highly active in aerobic gram-negative microorganisms -Pseudomonas Aeruginosa, Escherichia Coli, Klebsiella SPP., Serratia SPP., Providencia SPP., Enterobacter SPP., Salmonella SPP., Shigella SPP.; some gram-positive microorganisms- Staphylococcus SPP. (including penicillin resistant, some cephalosporins); moderately active in relationSREPTOCOCCUS SPP.

With simultaneous appointment with benzylpenicillin, a synergistic effect has a synergistic effect on strainsEnterococcus faecalis. Does not act on aerobic microorganisms.

Amikacin does not lose activity under the action of enzymes inactivating other aminoglycosides, and may remain active in relation to strainsPseudomonas Aeruginosa, resistant to drawramycin, gentamicin and nonylmicin.

Pharmacokinetics:

After intramuscular administration (in / m) is absorbed quickly and completely. The maximum concentration of the drug in the blood (with M ah ) At the I / M administration at a dose of 7.5 mg / kg - 21 μg / ml, after 30 minutes in / in infusion at a dose of 7.5 mg / kg - 38 μg / ml. The time to achieve the maximum concentration of the drug in the blood (T with M ah ) - about 1.5 hours after the introduction. Communication with plasma proteins - 4-11%.

Well distributed in extracellular liquid (the contents of abscesses, pleural effusion, ascitic, pericardial, synovial, lymphatic and peritoneal liquid); In high concentrations, it is found in the urine; In low - in bile, breast milk, water moisture, bronchial secrete, wet and spinal fluid (SMG). Well penetrates all tissues of the body, where accumulate intracellular; High concentrations are noted in organs with good blood supply: light, liver, myocardium, spleen, and especially in the kidneys, where the cortical substance accumulates, lower concentrations - in muscles, adipose tissue and bones.

When appropriate in the mid-therapeutic doses (normally), adults do not penetrate the hematorencephalic barrier (GEB), during the inflammation of the brain shells, permeability increases slightly. Newborns achieved higher concentrations in the CMF than adults; It passes through the placenta - it is found in the blood of the fetus and amniotic fluid. The volume of distribution in adults is 0.26 l / kg, in children - 0.2-0.4 l / kg, in newborns - aged less than 1 week. and body weight less than 1.5 kgup to 0.68 l / kg, aged less than 1 week. And the body weight is more than 1.5 kg - up to 0.58 l / kg, in patients with cystic acids - 0.3-0.39 l / kg. The average therapeutic concentration with / in or in / m was preserved for 10-12 hours.

Not metabolized. Half-life from blood (T 1/2. ) in adults - 2-4 hours, in newborns - 5-8 hours, in older children - 2.5-4 hours. The final valueT 1/2. more than 100 hours (release from intracellular depot).

It is excreted by the kidneys by glomerular filtration (65-94%) mainly unchanged. Kidney clearance - 79-100 ml / min.

T 1/2. in adults, in violation, the kidney function varies depending on the degree of violation - up to 100 hours, in patients with cystic fibrosis - 1-2 hours, in patients with burns and hyperthermiaT 1/2. it may be shorter compared to the average indicators due to increased clearance.

It is derived during hemodialysis (50% in 4-6 h), peritoneal dialysis is less effective (25% in 48-72 h).

Indications:

Infectious-inflammatory diseases caused by gram-negative microorganisms (resistant to gentamicin, cozyomycin and canamycin) or associations of gram-positive and gram-negative microorganisms: respiratory tract infection (bronchitis, pneumonia, empty of pleura, abscess light), sepsis, septic endocarditis, central nervous infection (CNS ) (including meningitis), abdominal infection (including peritonitis), urinary tract infections (pyelonephritis, cystitis, urethritis, prostatitis, gonorrhea), purulent skin infections and soft tissues (including infected burns, infected ulcers and the breakdown of various origins), infections of the biliary tract, bones and joints (including approxitomyelitis), wound infection, postoperative infections.

Contraindications:

Hypersensitivity (including to other aminoglycosides in history), neuritis auditory nerves, chronic renal failure (CPN) with azotemia and uremia, pregnancy.

Carefully:Miastations, Parkinsonism, botulism (aminoglycosides can cause a neuromuscular transmission impairment, which leads to a further weakening of skeletal muscles), dehydration, renal failure, a period of newborn, prematurity of children, elderly age, lactation period. Pregnancy and lactation:

In the presence of "life", indications can be used during lactation (aminoglycosides penetrate into breast milk in small quantities, but they are poorly absorbed from the gastrointestinal tract, and there were no complications associated with them).

Method of use and dose:

Intramuscularly or intravenously (inkjano, for 2 minutes or drip). Adults and children over 6 years old - 5 mg / kg every 8 hours or 7.5 mg / kg every 12 hours; Bacterial infections of urinary tract (uncomplicated) - 250 mg every 12 hours; After the hemodialysis session, an additional dose can be assigned - 3-5 mg / kg. Maximum doses for adults - up to 15 mg / kg / day, but not more than 1.5 g / day for 10 days.

The duration of treatment with in / in the introduction is 3-7 days, at a / m - 7-10 days.

Premature newborn initial dose - 10 mg / kg, then 7.5 mg / kg every 18-24 hours; Newborn and children up to 6 years old, the initial dose is 10 mg / kg, then 7.5 mg / kg every 12 hours for 7-10 days.

Patients with renal failure requires correction of the dosing mode: a decrease in dose or an increase in the interval between the introductions is necessary. Treatment should be carried out under the control of the content of the drug in the plasma (the therapeutic concentration of 15-25 μg / ml).

Patients with burns may be required to dose 5-7.5 mg / kg every 4-6 hours due to shorterT 1/2 (1-1.5 h) in these patients.

For a / m administration, a solution preparedex Tempore. from the powder with the addition of 2-3 ml of water for injection to the contents of the bottle. For in / in inkjet administration, 4-5 ml of water for injection, 0.9% solution of sodium chloride or 5% dextrose solution are added to the contents of the vial. For B / in drip administration, the same solutions are used as for in / m, pre-diluting them with 200 ml of 5% declaration solution or 0.9% sodium chloride solution. The concentration of amikacin in the solution for C / in administration should not exceed 5 mg / ml.

With violation of the excretory function of the kidneys A decrease in doses or an increase in the intervals between the introductions is necessary.

In the case of an increase in the interval between the introductions (if the cryatinine clearance level is not known, and the patient's condition is stable), the interval between the drugs is established as follows:

Interval (clock) = creatinine concentration in blood serum * 9.

If the concentration of creatinine in serum 2 mg / 100 ml, then the recommended one-time dose (7.5 mg / kg) must be administered every 18 hours. With an increase in the interval, the one-time dose do not change.

In the case of a decrease in a single dose with a constant dosing mode, the first dose of patients with renal failure is 7.5 mg / kg. To calculate the following doses, it is necessary to divide the value of the clearance (ml / min) in patients with creatinine clearance normally, then the obtained figure is multiplied by the value of the initial dose in mg:

subsequent dose (mg) \u003dclementine clearance identified in a patient (ml / min) / creatinine clearance normally (ml / min) H. initial dose (mg).

Side effects:

From the digestive system: Nausea vomiting, violation of the liver function (increase in the activity of "liver" transaminases, hyperbilirubinemia).

From the blood formation organs : anemia, leukopenia, granulocyptopenia, thrombocytopenia.

From the nervous system: Headache, drowsiness, neurotoxic effect (twitching muscles, feeling of numbness, tingling, epileptic seizures), disruption of neuromuscular transmission (respiratory stop).

From the senses: Overtoon (Hearing reduction, vestibular and labyrinth disorders, irreversible deafness), toxic effect on the vestibular apparatus (disincordination of movements, dizziness, nausea, vomiting).

From the urinary system : nephrotoxicity is a violation of the kidney function (oliguria, proteinuria, microhematuria).

Allergic reactions: Skin rash, itching, hyperemia of the skin, fever, swelling of quinque.

Local: soreness at the injection site, dermatitis, phlebitis and perifelhibit (with intravenous administration).

Overdose:

Symptoms: Toxic reactions (hearing loss, ataxia, dizziness, urination disorders, thirst, decline in appetite, nausea, vomiting, ringing or feeling of laying in ears, respiratory impairment).

Treatment: to remove the blockade of neuromuscular transmission and its consequences - hemodialysis or peritoneal dialysis; Anticholinesterase drugs, calcium salts, artificial lung ventilation, other symptomatic and supporting therapy.

Interaction:

Pharmaceutically incompatible with penicillins, heparin, cephalosporins, capeomycin, amphotericin, hydrochlorothiazide, erythromycin, nitrofurantine, vitamins of the group B and C, potassium chloride.

Exhibits synergism when interacting with carbenicillin,benzylpenicillin, cephalosporins (in patients with severe chronic renal failure (CPN), beta-lactam antibiotics can reduce the effect of aminoglycosides).

Nalidix Acid, B, and increase the risk of developing and nephrotoxicity.

Diuretics (especially), cephalosporins, penicillins, sulfonamides and nonspecific anti-inflammatory drugs, competing for active secretion in the tube of nephron, block the elimination of aminoglycosides, increase their serum concentration, enhancing nephro- and neurotoxicity.

Enhances the myarlaxing effect of stripping medicines.

Metoxifluran, polymixins for parenteral administration, etc. Medicinal products blocking neuromuscular transmission (halogenated hydrocarbons as medicines for inhalation anesthesia, narcotic analgesics), the transfusion of large amounts of blood with citrate preservatives increase the risk of respiratory stop.

The parenteral administration of indomethacin increases the risk of developing the toxic effect of aminoglycosides (increase T 1/2. and reduced clearance).

Reduces the effectiveness of antimaistical medicines.

Special instructions:

Before use, the sensitivity of the selected pathogens is determined using discs containing 30 μg of amikacin. When the diameter of the height-free zone is 17 mm and more microorganism is considered sensitive, from 15 to 16 mm - moderately sensitive, less than 14 mm - stable.

The concentration of amikacin in the plasma should not exceed 25 μg / ml (therapeutic concentration of 15-25 μg / ml).

During the treatment period, it is necessary at least 1 time a week to control the function of the kidneys, auditory nerve and the vestibular apparatus.

The probability of the development of nephrotoxicity is higher in patients with impaired kidney function, as well as when prescribed in high doses or for a long time (this category of patients may require daily control of the kidney function).

With unsatisfactory audiometric tests, the drug dose reduce or cease treatment.

Patients with infectious inflammatory diseases of the urinary tract it is recommended to receive an increased amount of fluid.

In the absence of positive clinical dynamics, it should be remembered for the possibility of the development of resistant microorganisms. In such cases, it is necessary to cancel the treatment and start conducting appropriate therapy.

Release form / Dosage:Powder for the preparation of a solution for intravenous and intramuscular administration. Packaging:

In bottles of 500 mg.The bottle with instructions for use is placed in a cardboard pack.

10 bottles with the drug, along with instructions for use, are placed in a pack.

50 bottles with the drug together with instructions for use are placed in a box of cardboard (for hospitals).

Storage conditions:

In the dry place protected from light, at a temperature not higher than 25 ° C.

Keep out of the reach of children.

Shelf life: 2 years. Do not use after the expiration date indicated on the package. Conditions of vacation from pharmacies:On prescription Registration number:LSR-008632/08 Registration date:10/30/2008 Instructions

active substance:amikacin;

1 ml of solution contains sulfate amikacin in terms of amikacin 50 mg or 250 mg;

excipients:sodium metabisulphite (E 223), sodium citrate, water for injection.

Dosage form. Injection.

Basic physico-chemical properties:transparent, colorless or slightly yellowish liquid.

Pharmacotherapeutic group.Antimicrobial means for systemic use.

Aminoglycosides. Amikacin. ATH code J01G B06.

Pharmacological properties

Pharmacodynamics.

Amicacin is a semi-synthetic aminoglycosoid antibiotic of a wide range of action. Amicacin actively penetrates through the membrane of the bacterial cell. Combining with a 30s subunit ribosoma, interferes with the formation of a complex of transport and matrix RNA, blocks protein synthesis, and also disrupts the synthesis of cytoplasmic membrane of bacteria.

Active relative to aerobic gram-negative microorganisms: Pseudomonas Aeruginosa, Escherichia Coli, Shigella SPP., Salmonella SPP., Klebsiella SPP., Enterobacter SPP., Providencia SPP., Proteus SPP. (indolence and indolencestricative strains), Serratia SPP., Acinetobacter Species, Citrobacter Freundii.

Active relative to some gram-positive microorganisms: Staphylococcus SPP.., incl. Staphylococci, resistant to penicillin, meticillin, some cephalosporins and some strains Streptococcus Pyogenes, Streptococcus Pneumoniae, Enterococcus. Amikacin under certain conditions can be used as basic therapy with a prescribed diagnosis or suspected of a disease caused by sensitive stamps of staphylococci in patients with allergies to other antibiotics and with mixed staphylococcal gram-negative infections. Amikacin is inactive relative to the anaerobic pathogens.

Pharmacokinetics.

After intramuscular administration, amikacin is absorbed quickly and completely. The maximum concentration is achieved in 0.5-1.5 hours after intramuscular administration and 0.5 hours after intravenous administration. The therapeutic concentration of amikacin is preserved for 10-12 hours.

Distribution.Blood proteins binding is 4-11%. The amikacin is well distributed in the extracellular substance (the content of abscesses, pleural effusion, ascitic, pericarordial, synovial, lymphatic and peritoneal fluid). Amikacin in high concentrations is in the urine, in low - in bile, breast milk, watery moisture, bronchial secrete, wet and spinal fluid. Amicacin penetrates well into all the tissues of the body, where it is accumulated intracellularly. The high concentration of amikacin is determined in the organs with enhanced blood supply: lungs, liver, myocardium, spleen and especially in the kidneys, where accumulates in the cortical layer; Lower concentration - in muscles, adipose tissue and bones.

In adults, in medium therapeutic doses, amikacin practically does not penetrate through the blood hematcinetic barrier, the penetration suddenly increases with brain-shells. Newborns achieved higher concentrations in the spinal fluid than adults.

Amicacin penetrates through the placental barrier and is determined in the blood of the fetus and amniotic fluid.

Deletion.Amicacin is not metabolized, is excreted by kidneys by glomerular filtration (65-94%) unchanged, forming high concentrations in the urine. Kidney clearance - 79-100 ml / min. The speed of excretion depends on the age, the functions of the kidneys and the concomitant pathology of the patient. In patients with fever, it increases, with a decrease in the function of the kidneys and in older people, slows down significantly.

The half-life in adults with a normal kidney function is 2-4 hours, in newborns - 5-8 hours, in older children - 2.5-4 hours. In renal failure, the half-life can reach 70 hours and more, with fiberglass - 1-2 hours. The ultimate duration of the half-life is more than 100 hours (exemption from intracellular depot).

In hemodialysis, 50% is excreted in 4-6 hours, with peritoneal dialysis - 25% in 48-72 hours.

Clinical characteristics.

Indications

Infections caused by amicacin-sensitive strains of microorganisms resistant to other aminoglycosides.

Contraindications

• Renal failure;
• neuritis the auditory nerve;
• increased sensitivity to amikacin or to any other antibiotic aminoglycoside group and their derivatives;
• increased sensitivity to any of the auxiliary substances included in the preparation;
• miasthenia gravis;
• violation of the function of the vestibular apparatus;
• azotemia (residual nitrogen above 150 mg%);
• preliminary treatment with reference or nephrotoxic drugs.

Interaction with other medicines and other types of interactions.

The simultaneous administration of amikacin sulfate with anesthetics and muscle relaxants can cause a blockade of neuromuscular transmission and palsy of respiratory muscles.

The risk of nephrotoxic action increases with simultaneous use with amphotericin B, cephalotin, polymyxin and furosemide. The risk of the development of a isotoxic action increases with the simultaneous use of the preparation with a furosemide, a stacry acid or cisplatin.

Amicacine sulfate is incompatible in a solution with penicillins, cephalosporins, amphotericin, hydrochlorodiazide, erythromycin, heparin, nitrofurantoin, thiopenthine, warfarin, tetracycles, vitamins of group B, vitamin C and potassium chloride.

Indomethacin, phenylbutazone and other NSAIDs, violating the renal blood flow, can slow the speed of the sulfate amikacin. When the sulfate amikacin is used by premature babies simultaneously with intravenous injection of indomethacin, there is an increase in the concentration of blood plasma and the risk of toxicity occurs.

Combinations of antibiotics amicacin + Ceftazidim and amicacin + Cefotaxim detect the most addive and synergistic effect on Pseudomonas Aeruginosa..

Features of application

Due to the potential overoxy and nephrotoxicity of aminoglycosides, patients should be under the special observation of the doctor.

Caution should be taken by sick Miastenia and Parkinsonism, as well as elderly people, patients who have neuromuscular conduction disorders due to the possibility of a strip-like effect.

In the presence of infections, severe treatment, or complicated infections in 10 days, it is necessary to evaluate the treatment with the drug and before appointing the next course to check the function of the kidneys, hearing, the vestibular apparatus and the concentration of the drug in serum. If there is no expected clinical effect in 3-5 days, treatment should be discontinued and determining the sensitivity of the pathogen to antibiotics.

Patients with disturbed kidney function need to adjust the dosing mode depending on the clearance of creatinine. The risk of solidoxic and nephrotoxic action increases with the introduction of large doses of the drug. For the prevention of from and nephrotoxic complications and reducing the amount of their development, when applying the drug, it is recommended to monitor the functions of the kidneys, hearing and the vestibular apparatus at least 1 time per week.

The main toxic effect of the drug during parenteral administration is its action on VIII a pair of brain brain nerves, which is first manifested by deafness in the range of high frequency sounds. In patients with impaired kidney function, the risk of developing output complications is significantly higher. Before the start of treatment, it is necessary to correct the water and electrolyte balance in the patient. During the treatment of amikacin sulfate, it is necessary to use a sufficient amount of fluid, often determine the concentration of creatinine in blood plasma and, if necessary, adjust the dosing circuit.

Elderly patients need to be reduced by the dose of sulfate amikacin due to the decrease in the functional activity of the kidneys and a possible decrease in body weight. The functional activity of the kidneys should be regularly evaluated. It is necessary to carry out urine analysis before or during treatment. Periodic examination and recording of the audiogram must be determined by the vestibular function. If the renal, vestibular or hearing failure is observed, doses should be reduced or stop the use of sulfate amiccin.

Patients with impairment of kidney function Daily dose It is necessary to reduce and / or the interval between doses to increase according to the concentration of creatinine in serum to prevent the accumulation of the drug in the blood and the minimum of the risk of dysotoxicity. If there are signs of kidney lesion (for example, albuminuria, microhematuria, leukocyturia), hydration should be increased and reduced dosing. These manifestations usually disappear after the end of treatment. If there are signs of ototoxicity (for example, dizziness, ringing, noise in ears or a decrease in hearing) or nephrotoxicity (for example, a decrease in creatinine clearance, oliguria), the use of sulfate amiccin must be discontinued or reduced dose. However, if the manifestations of azotemia arise or Oliguria is increasing, treatment should be stopped.

Ototoxicity caused by aminoglycosidic antibiotics can develop and after the end of the use of the drug and is usually irreversible. The risk of the development of isotoxicity is increased in patients with impaired kidney function, as well as when using high doses or with prolonged treatment with a drug.

In patients with dehydration of the body, the risk of toxicity increases due to an increase in the concentration of the drug in blood serum.

The simultaneous use of rapid sulfate amiccin and diuretics, for example, precipitous acid derivatives, furosemide, manita (especially, if the diuretic is administered intravenously), may lead to the development of a thorough deafness.

It is impossible to prescribe two aminoglycoside simultaneously or replace one drug to others if the first aminoglycoside was used for 7-10 days. Repeated course can be carried out no earlier than 6 weeks.

The drug contains sodium metabisulphite, which can cause an allergic type reactions, including symptoms of anaphylaxis and varying severity of asthmatic seizures, especially in bronchial asthma patients.

With simultaneous use with cephalosporins, it is advisable to introduce them to different places (with intramuscular administration) with an interval of at least 1 hour.

The use of sulfate amikacin can change such laboratory indicators: serum alanine-bellows, aspartatenotransferase, bilirubin, lactate dehydrogenase, alkalinophosphate, urinary nitrogen, creatinine, calcium, magnesium, potassium ions, sodium.

Application during pregnancy or breastfeeding.

The drug is contraindicated during pregnancy and breastfeeding.

The ability to influence the reaction rate when managing motor vehicles or other mechanisms.

The experience of using the drug suggests that it does not affect the ability to drive a car or work with mechanisms, but the likelihood of such side effects on the part of the central nervous system, as drowsiness, neuromuscular transmission disorders should be taken into account.

Method of application and dose

The drug is prescribed intramuscularly or intravenously (inkidino or drip). The dose and method of administering the drug are determined individually for each patient depending on the severity of the disease, the sensitivity of the pathogen, the functions of the kidneys and the mass of the patient's body. Adults and children aged 12 are prescribed 10-15 mg / kg per day. Daily dose is distributed to 2 administration. The maximum daily dose for adults is 1.5 g. The duration of treatment during intravenous administration is 3-7 days, with intramuscular administration - 7-10 days.

With uncomplicated infections of the organs of the urinary system (except for infections caused by a blue rod), the drug is injected intramuscularly 250 mg 2 times a day for 5-7 days.

In case of infections caused by a blue rod, and in infections, threatening life, the drug is prescribed at a dose of 15 mg / kg per day, separated by 3 administration.

For newborn and premature babies, the initial load dose is 10 mg / kg per day, followed by the introduction of a daily dose of 15 mg / kg, divided into 2 administrations within 7-10 days.

Patients with impaired kidney function The daily dose should be reduced or increasing the interval between the introductions to avoid the cumulation of the antibiotic. It is necessary to adjust the dispensing scheme depending on the clearance of creatinine.

Clematinine clearance, mg / ml	Number of administration	Dose, mg / kg
	1 time in 24 hours
	1 time in 48 hours

For the preparation of an infusion solution, an isotonic sodium chloride solution is used, a 5% glucose solution, a ringer solution. The concentration of the amiccin solution during intravenous administration should not exceed 5 mg / ml. The duration of infusion is 30-90 minutes. Intravenous injection should be carried out slowly for 7 minutes.

Children.The drug is used in pediatric practice.

Amicacine sulfate is used with caution for the treatment of premature and docking babies, because through the underdevelopment of the excretory system, the removal of aminoglycosides can be extended, causing the phenomena of toxicity.

Overdose

It is possible that the appearance of the referee and nephrotoxic effects of the drug and the signs of the neuromuscular blockade are possible: noise in ears, auditory disorders, skin rashes, headache, dizziness, fever, paresthesia, reduction of kidney function (before renal failure), depression or respiratory paralysis.

If necessary, the preparation is derived from the body by parenteral dialysis or hemodialysis. Reduce the level of the drug with continuous arteriovenomous hemofiltration. Also apply exchange hemotransphus to remove the drug from the body in newborns.

At the first signs of the blockade of neuromuscular conductivity, it is necessary to stop the introduction of sulfate amikacin and immediately introduce intravenously calcium calcium chloride or subcutaneously sampling and atropine. If necessary, the patient is transferred to the controlled breathing.

Adverse reactions

From the digestive tract: Nausea, vomiting, diarrhea.

From the side of the hearing organs:partially revolt or non-deafness, noise in the ears.

From the central nervous system: Headache, drowsiness, it is possible to reduce hearing, vestibular disorders, dizziness, paresthesia, tremor, convulsions, encephalopathy; In isolated cases, disorders of neuromuscular conductivity, the occurrence of neuromuscular blockade (muscle paralysis, inhibition of breathing).

From the hematopopitation system: Anemia, leukopenia, granulocyptopenia, hematuria, thrombocytopenia, eosinophilia.

From the urinary system: nephrotoxicity - disorders of the kidney function (oliguria, albuminuria, cylindruria, hyperazotemia, proteinuria, microhematuria, hematuria, improving the level of creatinine); Rarely - acute necrosis, interstitial jade, acute renal failure.

From the side of the cardiovascular system:vasculitis, arterial hypotension.

From the endocrine system and metabolism: Hypomania.

From the musculoskeletal system: arthralgia.

Allergic reactions: skin rashes, itching, fever; In isolated cases - swelling of quinque.

Others: Pain in the place of administration, hyperemia, swelling, hyperthermia, hyperbilirubinemia, increase blood transaminase level.

Shelf life

Storage conditions

Store in the original packaging at a temperature not higher than 25 ° C.

Keep out of the reach of children.

Packaging

Injection solution 50 mg / ml - 2 ml in ampoules.

Injection solution 250 mg / ml - 2 ml or 4 ml in ampoules.

1 ampoule in a bundle.

5 ampoules in a blister, 1 or 2 blisters in a pack.

On prescription.

Manufacturer

Private joint-stock company LEKKHIM-Kharkov.

The location of the manufacturer and its address of the activities of the activity.

Ukraine, 61115, Kharkiv region, city Kharkov, Severina Pototsky Street, house 36.

One bottle of the drug Amicacin contains 1000, 500 or 250 mg amicacin sulfate in the form of powder.

Additional substances: edetat Dinatry, Sodium Hydrophosphate , water.

One ampoule of amicacin contains in 1 ml of a solution of 250 mg amicacin sulfate .

Amicacin release form

Powder for the manufacture of a solution intended for intravenous or intramuscular administration is always white or close to white color, hygroscopic.

1000, 500 or 250 mg of such powder in a bottle of 10 ml; 1, 5, 10 or 50 of such bottles in a pack of paper.

The solution (intravenous, intramuscular administration) is usually transparent, straw color or colorless.

Forms of release in tablets do not exist.

pharmachologic effect

Bactericidal, bacteriostatic (Depending on the administered dose).

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Amicacin (the name in the recipe on Latin Amikacin) is a semi-synthetic aminoglycoside (), acting on a wide range of pathogens. Possessed bactericidal action. Quickly penetrates through the cell wall of the pathogen, it is firmly associated with the closure of the bacterium ribosomes, and the protein biosynthesis is inhibited.

Provided with respect to gram-negative aerobic pathogens: Salmonella SPP., Enterobacter SPP., Escherichia Coli, Klebsiella SPP., Pseudomonas Aeruginosa, Shigella SPP., Serratia SPP., Providencia Stuartii.

Moderately active in relation to grampotive bacteria: Staphylococcus SPP. (including steady meticular resistant strains), row of strains Streptococcus SPP.

Aerobic bacteria are insensitive to amikacin.

Pharmacokinetics

After intramuscular administration is actively absorbed in the full volume. Penetrates all the fabrics and through histohematic barriers. Bonding with blood proteins is up to 10%. Not exposed to transformation. Examined through the kidneys unchanged. The half-life approaches 3 o'clock.

Indications for the use of amikacin

Indications for the use of amicacin are infectious and inflammatory diseases caused by gramnegative microorganisms (resistant to, or sizomycin ) or at the same time grampositive and gramnegative microorganisms:

• respiratory system infections ( , Empiama pleura, lungs );
• sepsis ;
• infectious;
• brain infections (including);
• urinary tract infections ( , );
• abdominal infections (including peritonitis );
• infections of soft tissues, subcutaneous fiber and purulent skin (including infected ulcers, burns,);
• hepato-biliary system infections;
• infections of joints and bones (including);
• infected wounds;
• infectious postoperative complications.

Contraindications

Severe kidney lesions, pregnancy, hearing nerve inflammation, to drugs from the group aminoglycoside .

Side effects

• Allergic reactions: ,.
• Reactions from the digestive system: hyperbilirubiney Activation hepatic transaminaz , nausea, vomiting.
• Reactions from the hematopoietic system: leukopenia, granulocyptopenia, anemia, thrombocytopenia .
• Reactions from the nervous system: change in neuromuscular transmission, reduced hearing (deafness possible), vestibular disorders.
• From the urogenital system: , oliguria, microhematuria , renal failure.

Assessment of amikacin (method and dosage)

AMICACIN injections Instructions for use permits to introduce the drug intramuscularly either intravenously.

Such a dosage form, as pills for oral administration does not exist.

Before injection, it is necessary to produce an intracutaneous sample on the sensitivity to the drug, if there are no contraindications for its execution.

How and how to breed Amicacin? The solution of the preparation is prepared before administration by administering to the contents of the vial 2-3 ml of distilled water intended for injection. The solution is administered immediately after cooking.

Standard doses for adults and children from one month - 5 mg / kg three times a day or 7.5 mg / kg twice a day for 10 days.

The maximum daily dose for adults is 15 mg / kg, divided into two administrations. In extremely severe cases and for diseases caused by Pseudomonas, the daily dose is divided into three administrations. The largest introduced dose for the entire course of treatment should not be more than 15 grams.

The newborn is first prescribed by 10 mg / kg, then turning to 7.5 mg / kg for 10 days.

The therapeutic effect usually occurs after 1-2 day, if after 3-5 days after the start of therapy, the effect of the drug is not marked, it should be canceled and change the tactics of treatment.

Overdose

Signs: ataxia , loss of hearing, thirst, urination disorders, vomiting, nausea, ringing in ears, breathing disruption.

Treatment: to relieve neuro-muscular transmission disorders; Sololi. calcium , anticholinesterase products , IVL as well as symptomatic therapy.

Interaction

Nephrotoxic effect is possible while using , methoxyphluran, radiocontrase agents, nonsteroidal anti-inflammatory agents, enflouran, Cefalotin, .

Outlook action is possible while simultaneously use with stacry acid, cisplatin .

When co-use with (with kidney damage), antimicrobial effects decreases.

When sharing with neuro muscular transmission blockers and ethyl ether The possibility of oppression of breathing increases.

Amicacin is forbidden to mix in solution with cephalosporins, penicillins, amphotericin B, chlorothiazide,

Analogs of amikacin

Coincidences on the ATX 4 level code:

Analogs: Amikacin Sulfat. Ambiotic (injection), Amikacin-Kredopharm (powder for the preparation of the solution) Lorikatin (injection), F.lexelett (injection).

Due to bad suction all aminoglycoside From the intestines in tablets analogues of amikacin are not produced.

Children

Children under 6 years old are prescribed an initial dose of 10 mg / kg, then twice a day at 7.5 mg / kg.

Newborn

Premature newborn children first prescribe 10 mg / kg, then go to 7.5 mg / kg once a day; 10 mg / kg are also prescribed a duplicate newborn, and then go to the introduction of 7.5 mg / kg twice a day.

With alcohol

During pregnancy (and lactation)

- Strict contraindication for the introduction of amikacin. Since Amicacin stands out with breast milk in minor quantities and is almost not absorbed from the intestine, it is allowed to use it by strict testimony.