Active material: Amikacin
When ATH: J01GB06
CCF: Antibiotics aminoglycoside
ICD-10 codes (testimony): A39, A40, A41, G00, i33, J15, J20, J42, J85, J86, K65.0, K81.0, K81.1, K83.0, L01, L02, L03, L08.0, L89, M00, M86, N10, N11, N30, N34, N41, T79.3, Z29.2
When CSF: 06.05.01
Manufacturer: Synthesis of {Russia}
Solution for in / and the / m clear, colorless or slightly colored.
| 1 ml | 1 amp. | |
| amikacin (in sulphate form) | 250 mg | 500 mg |
Excipients: sodium bisulfite (sodium metabisulfite), sodium citrate d/and (sodium citrate pentaseskvigidrat), sulfuric acid divorced, water d / and.
2 мл – ампулы стеклянные (5) – упаковки контурные ячейковые (1) – пачки картонные.
2 мл – ампулы стеклянные (5) – упаковки контурные ячейковые (2) – пачки картонные.
2 мл – ампулы стеклянные (10) – упаковки контурные ячейковые (1) – пачки картонные.
2 мл – ампулы стеклянные (10) – коробки картонные.
Solution for in / and the / m clear, colorless or slightly colored.
| 1 ml | 1 amp. | |
| amikacin (in sulphate form) | 250 mg | 1 g |
Excipients: sodium bisulfite (sodium metabisulfite), sodium citrate d/and (sodium citrate pentaseskvigidrat), sulfuric acid divorced, water d / and.
4 мл – ампулы стеклянные (5) – упаковки контурные ячейковые (1) – пачки картонные.
4 мл – ампулы стеклянные (5) – упаковки контурные ячейковые (2) – пачки картонные.
4 мл – ампулы стеклянные (10) – упаковки контурные ячейковые (1) – пачки картонные.
4 мл – ампулы стеклянные (10) – коробки картонные.
Powder for solution for I / O, and the / m white or nearly white, hygroscopic.
| 1 fl. | |
| amikacin (in sulphate form) | 1 g |
Vials 10 ml (1) – пачки картонные.
Vials 10 ml (5) – пачки картонные.
Vials 10 ml (10) – пачки картонные.
Polusinteticeski antibiotic broad-spectrum from aminoglycoside, bactericidal effect. Communicating with the 30S subjedinica ribosom, prevents the formation of complex transport and messenger RNA, blocking protein synthesis, as well as destroying zitoplazmaticalkie membranes of bacteria.
Vsokoakteven against 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. (incl. resistant to penicillin, some zefalosporynam).
Moderately active against Streptococcus spp.
Together with the appointment of benzilpenitsillinom shows synergies action against strains of Enterococcus faecalis.
No effect on anaerobic microorganisms.
Amikacin does not lose activity under the action of enzymes, inaktiviruûŝih other aminoglycosides, and may remain active against strains of Pseudomonas aeruginosa, resistant to tobramicinu, gentamicin and netilmicinu.
Absorption
After the/m of rapidly and completely absorbed. Cmax in plasma with the/m in a dose of 7.5 мг/кг – 21 ug / ml, after 30 min on/in infusions in the dose 7.5 мг/кг – 38 ug / ml. After the/m of tmax - About 1.5 no.
The average therapeutic concentration in/in or/m introduction maintained for a period of 10-12 no.
Distribution
Plasma protein binding is 4-11%. Vd у взрослых – 0.26 l / kg, у детей – 0.2-0.4 l / kg, in newborn: at the age of less than 1 weeks and weighing less than 1500 г – до 0.68 l / kg, at the age of less than 1 weeks and weighing more than 1500 г – до 0.58 l / kg, у больных муковисцидозом – 0.3-0.39 l / kg.
It is distributed in the extracellular fluid (contents of abscesses, pleural effusion, ascite, pericardial, synovial, lymphatic and peritoneal fluid); in high concentrations detected in the urine; в низких – в желчи, breast milk, the aqueous humor of the eye, bronchial secretions, sputum and cerebrospinal fluid. It penetrates into all body tissues, where accumulated intracellularly; high concentrations are observed in organs with a good blood supply: lungs, liver, myocardial, spleen, and particularly in the kidneys, where is accumulated in the cortical substance, более низкие концентрации – в мышцах, adipose tissue and bones.
When you assign in sredneterapevtičeskih doses (normal) adults not to cross the Geb amikacin, When brain nerve membrane permeability increases slightly. The newborn is achieved higher concentrations in cerebrospinal fluid, than in adults. It penetrates through the placental barrier: detected in the blood of the fetus and amniotic fluid.
Metabolism
Do not metabolized.
Deduction
T1/2 у взрослых – 2-4 no, in newborns - 5-8 no, у детей более старшего возраста – 2.5-4 no. The final T1/2 – more 100 no (release from intracellular depots).
Report kidneys by clubockova filtering (65-94 %) mainly unchanged. Почечный клиренс – 79-100 ml / min.
Pharmacokinetics in special clinical situations
T1/2 у взрослых при нарушении функции почек варьирует в зависимости от степени нарушения – до 100 no, у пациентов с муковисцидозом – 1-2 no, patients with burns and hyperthermia T1/2 may be shorter than average due to increased ground clearance.
Displayed in hemodialysis (50% for 4-6 no), peritoneal dialysis is less effective (25% for 48-72 no).
Infectious-inflammatory diseases, caused by Gram-negative microorganisms (resistant to gentamicin, sizomicinu and kanamycin) or associations of grampolaugitionah and gramotricationah microorganisms:
- Respiratory tract infections (bronchitis, pneumonia, empyema, lung abscess);
- Sepsis;
- Bacterial endocarditis;
-CNS infections (including meningitis);
- Infections of the abdominal cavity (incl. peritonitis);
-urinary tract infection (pyelonephritis, cystitis, uretrit);
-fatigue infections of the skin and soft tissues (incl. infected burns, infected sores and decubitus different Genesis);
- Infection of the biliary tract;
- Bone and joint infections (incl. osteomyelitis);
-wound infection;
- Postoperative infections.
The drug is introduced into / m, I / (spray, during 2 minutes or drip) adults and children over 6 years - By 5 mg / kg every 8 or h 7.5 mg / kg every 12 no. At bacterial infections of the urinary tract (uncomplicated) - By 250 mg every 12 no; после сеанса гемодиализа может быть назначена дополнительная доза – 3-5 mg / kg.
The maximum dose for Adult – 15 mg / kg / day, but not more 1,5 g / day for 10 days. Продолжительность лечения при в/в введении – 3-7 days, при в/м – 7-10 days.
To preterm infants initial single dose of 10 mg / kg, then 7.5 mg / kg every 18-24 no; to infants and children up to 6 years начальная доза – 10 mg / kg, then 7.5 mg / kg every 12 h for 7-10 days.
At infected Burns may require dose 5-7.5 mg / kg every 4-6 h in connection with shorter T1/2 (1-1.5 no) This category of patients.
In/in drip for misleading amikacin 30-60 m, в случае необходимости – струйно.
For i / v administration (drop) the drug previously diluted 200 ml 5% dextrose (Glucose) or 0.9% sodium chloride solution. Amikaczina concentration in the solution for the on/in the introduction should not exceed 5 mg / ml.
At violation excretory functions of the kidneys It is necessary to reduce the dose or increase the interval between wvedeniami. In the event of an increase the interval between wvedeniami (If the value CC is unknown, and the patient's condition stable) the interval between the introduction of the preparation set according to the following formula:
interval (no) = concentration of whey creatinine × 9.
If the concentration of serum creatinine is 2 mg / dL, the recommended single dose (7.5 mg / kg) You must enter every 18 no. When you increase the single dose interval does not change.
If a single dose with an unmodified first dose dispensing mode for patients with renal insufficiency is 7.5 mg / kg. Calculation of subsequent doses is as follows:
Subsequent dose (mg), you enter every 12 h = QC (ml / min) patient × initial dose (mg)/QA OK (ml / min).
From the digestive system: nausea, vomiting, abnormal liver function (повышение активности “печеночных” трансаминаз, giperʙiliruʙinemija).
From the hematopoietic system: anemia, leukopenia, granulocytopenia, thrombocytopenia.
From the central and peripheral nervous system: headache, drowsiness, neurotoxic effects (clonus, benumbed sensation, tingling, seizures), violation of neuromuscular transmission (respiratory arrest).
From the senses: ototoxicity (hearing loss, vestibular and labyrinth disorders, irreversible deafness), a toxic effect on the vestibular system (discoordination movements, dizziness, nausea, vomiting).
From the urinary system: нефротоксичность – нарушение функции почек (oligurija, proteinuria, mikrogematuriâ).
Allergic reactions: skin rash, itch, dermahemia, fever, angioedema.
Local reactions: soreness at the injection site, dermatitis, phlebitis and periphlebitis (at / in the introduction).
-Neuritis of the auditory nerve;
-severe chronic renal insufficiency with azotemia and uremyei;
- Pregnancy;
- Hypersensitivity to the drug;
-hypersensitivity to other aminoglikozidam history.
FROM caution the drug should be used when myasthenia, parkinsonizme, botulizme (aminoglycosides can cause a violation of neuromuscular transmission, which leads to a further weakening of the skeletal muscles), degidratacii, renal failure, in the newborn, in preterm infants, in elderly patients, lactation.
The drug is contraindicated in pregnancy.
In the presence of the living testimony of the drug can be used in lactating women. It will be appreciated, that aminoglikozida stand out with breast milk in small amounts. They are poorly absorbed from the digestive tract, and related complications in infants is not registered.
Before using the define sensitivity of selected pathogens, using disks, containing 30 micrograms amikaczina. In diameter growth-free zone 17 mm or more is considered a sensitive organism, from 15 to 16 мм – умеренно чувствительным, less 14 мм – устойчивым.
Amikaczina concentration in the plasma should not exceed 25 ug / ml (therapeutic concentration is 15-25 ug / ml).
During the period of treatment should be not less than 1 times per week to monitor kidney function, the auditory nerve and the vestibular apparatus.
The likelihood of higher Nephrotoxicity in patients with impairment of renal function, as well as in the appointment of high doses or for a long time (This category of patients may require daily monitoring of renal function).
When poor audiometric test dose reduce or stop treatment.
Patients with infectious and inflammatory diseases of the urinary tract are advised to take an increased amount of fluid with adequate diureze.
In the absence of positive clinical Dynamics should be mindful of the possible development of resistant microorganisms. In such cases, it is necessary to cancel treatment and initiate appropriate therapy.
Contained in the composition of sodium disul′fit may lead to the development of patients with allergic complications (until the anaphylactic reactions), especially in patients with allergological history.
Symptoms: токсические реакции – потеря слуха, ataxia, dizziness, urination disorders, thirst, decreased appetite, nausea, vomiting, or ringing sensation in the ears laying, respiratory failure.
Treatment: для снятия блокады нервно-мышечной передачи и ее последствий – гемодиализ или перитонеальный диализ; anticholinesterase agents, calcium salt, IVL, other symptomatic and supportive therapy.
Shows high synergy with karbenicillinom, benzilpenicillinom, cephalosporins (in patients with severe chronic renal insufficiency when coupled with the use of beta-lactam antibiotics may decrease the effectiveness of aminoglycosides).
Nalidixic acid, polymyxin b, cisplatin, Vancomycin increases the risk of development of OTO- and nephrotoxicity.
Diuretic (especially furosemide), cephalosporins, penicillins, sulfonamides and NSAIDS, competing for the active secretion in bone nefrona, block eliminatiu aminoglycosides, increase their concentration in the serum, reinforcing nefro- and neurotoxicity.
Amikacin enhances miorelaksirutee kurarepodobnykh drugs.
Together with amikacin methoxyflurane, Parenteral polymyxin, capreomycin and other medicines, blocking neuromuscular transmission (галогенизированные углеводороды – средства для ингаляционной анестезии, opioid analgesics), a large number of blood transfusions citratnymi preservatives to increase the risk of breathing stops.
Injecting a indometacin increases the risk of toxic effects aminoglikozidov (the increase in T1/2 and reduced ground clearance).
Amikacin reduces the effectiveness antimiasteniceskih drugs.
Pharmaceutical interaction
Farmatsevticeski incompatible with penitsillinami, geparinom, cephalosporins, capreomycin, amphotericin B, hydrochlorothiazide, Erythromycin, nitrofurantoinom, vitamins b and c, potassium chloride.
The drug is released under the prescription.
List B. The drug should be stored out of reach of children, dry, the dark place at a temperature between 5° c to 25° c. Shelf life - 2 year.
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