Amitsil

General characteristics. Structure:

Active ingredient: amikacin;
1 bottle contains 250 mg of amikacin of sulfate (1:1,8) in terms of amikacin.
excipients: mannitol (Е 421).

Pharmacological properties:

Pharmacodynamics. Amikacin - a semi-synthetic antibiotic of a broad spectrum of activity of group of aminoglycosides. Has bactericidal effect. Actively getting through a cell wall of bacteria, it is irreversible communicates with 30S in subunit of bacterial ribosomes and by that microorganism protein synthesis oppresses that finally leads to his death.
Has high bactericidal activity concerning gram-positive microorganisms: Staphylococcus spp. (including penitsillinazoustoychivy); gram-negative microorganisms: Citrobacter freundii, Enterobacter spp.; Escherichia coli, Haemorhilus influenzae, Klebsiella spp., Proteus spp. (indolpositive and indolnegative), Rgovidencia of spp., Pseudomonas aeruginosa, Salmonella spp., Shigella spp., Yersinia enterocolitica. On activity exceeds gentamycin concerning Klebs_ella spp. and Rgov_dens_a of spp. It is inactive concerning anaerobic bacteria.

Pharmacokinetics. At intramuscular introduction it is quickly and completely soaked up. It is distributed in extracellular liquid, including blood serum, liquid of abscesses, a pleural exudate, ascitic, pericardiac, synovial, lymphatic and peritoneal liquids. High concentration are found in urine. Low concentration are noted in bile, breast milk, a bronchial secret, a phlegm and liquor. At an inflammation of a meninx penetration into liquor increases. Gets into all body tissues where collects intracellularly. High concentration are noted in bodies with good blood supply, in such as liver, lungs, especially kidneys where drug collects in cortical substance. Elimination half-life: adults – 2 - 4 hours; children are newborns – 5 - 8 hours, more advanced age – 2,5 – 4 hours. It is brought by kidneys in not changed view by glomerular filtering to 75 – 95%. Pharmaceutical characteristics. Main physical and chemical properties: porous mass of color, white or white with a yellowish shade.

Indications to use:

The heavy infections caused by microorganisms, sensitive to drug.

Route of administration and doses:

The mode of dosing is set individually taking into account weight of a current and localization of an infection, and also sensitivity of the activator. The usual dose for adults and children is more senior than 12 years:
intramusculary or by intravenous infusion on 15 mg/kg of body weight in 2 – 3 receptions a day within 7 – 10 days. The maximum doses for adults no more than 1,5 g a day. Maximum duration
uses of drug are made by 10 days. At a renal failure (clearance of creatinine less than 50 mg/ml) the introduction mode two or three times a day with definition of concentration of amikacin in blood serum and a korregirovaniye of a dose or a dose decline, or decrease in an interval between administrations of drug is recommended. Not to administer to a sutochnuyudoz the drug for once. At a renal failure the dose decline of drug and introduction in 8-12 hours is recommended. For confirmation of correctness of selection of a dose and prevention of excess concentration of amikacin in blood serum it is necessary if there is an opportunity, periodically to check concentration of the last in a blood plasma.
Treatment begin with drug with a load single dose 7,5 mg/kg. Then depending on decrease in clearance of creatinine calculate a maintenance dose as it is defined below.
Interval between introductions of 12 h.

                                                                Real clearance   x  Dose, theoretically
                                                                  creatinine at              necessary for the patient
                                                                sick (ml/min.)      
Korregirovanny
maintenance dose =              --------------------------------------------------------------------------
                                                            Normal clearance of creatinine (theoretically) for
                                                                                 this sick (ml/min.)

Other way of definition of a dose by the patient (interval between introductions of 12 hours) at a stable state and with the known value of creatinine of serum - to divide the recommended dose into value of creatinine of serum.
Doses for children: premature newborns – in the beginning 10 mg/kg, then 7,5 mg/kg each 18 – 24 hours within 7 – 10 days; newborn – in the beginning 10 mg/kg, then on 7,5 mg/kg each 12 hours within 7 – 10 days; age from 1 to 12 years – 15 mg/kg by 2 – 3 times a day within 7 – 10 days. Amitsil's solution is prepared just before use. For intramuscular injections contents of a bottle are dissolved in 2 – 3 ml of water for injections and entered deeply into an upper outside quadrant of a buttock. At introduction of an antibiotic of more than 0,5 g, an amount of water for injections increase to multiply above-stated quantity. For intravenous infusions contents of a bottle dissolve 0,9% of solution of sodium of chloride or 5% of solution of glucose in 100 – 200 ml. Infusion is carried out kapelno with a speed of 60
thaw in a minute. Concentration of solution at introduction to a vein should not exceed 5 mg/ml. The intravenous jet injection of Amitsil should be carried out slowly, within about 7 minutes. At uncomplicated infections of urinogenital ways (except the infections caused by a pyocyanic stick) Amitsil enter 250 mg 2 times a day intramusculary within 5 – 7 days. For strengthening of action concerning a pyocyanic infection perhaps combined use with cephalosporins ІІІ-go generations (a ceftazidime, цефоперазон), at the same time the amikacin combination with a ceftazidime is the most effective.

Features of use:

The main toxic effect of Amitsil at parenteral administration is its action on the VIII couple of cranial nerves. Usually at the beginning deafness in the range of sounds of high frequency is noted that can be revealed at an audiometric research. At patients with renal failures the risk of development of ototoksichesky complications is considerably increased. If during treatment progressing of a renal failure is observed, it is recommended to conduct audiometric researches and, in case of need, to stop drug use. With care Amitsil patients with a myasthenia and parkinsonism, and also elderly people have to apply. Patients with disturbance of secretory function of kidneys need correction of the mode of dosing depending on clearance of creatinine. As Amitsil is brought with urine, prior to treatment it is necessary to carry out correction of water and electrolytic balance. At emergence of signs of nephrotoxicity (frequent desires to an urination, detection of leukocytes, erythrocytes or albumine in urine) administration of liquid should be increased, and the dose of drug is recommended to be lowered. The specified symptoms usually disappear by the end of a course of treatment. However in case of development of a hyperazotemia or an oliguria treatment should be stopped. At combined use with cephalosporins it is desirable to enter them into different places (at intramuscular introduction) with an interval not less than 1 hour.
Ability to influence speed of response at control of motor transport or work with other mechanisms. It is necessary to take with caution drug to patients whose activity demands speed of psychomotor reactions (management of transport, work with potentially dangerous mechanisms), considering risk of emergence of possible undesirable reactions from a nervous system.

Side effects:

At Amitsil's use are possible:
- from the alimentary system: nausea, vomiting, hyperbilirubinemia, increase in activity of hepatic transaminases;
- allergic reactions: skin rash, an itch, fever, it is rare - a Quincke's edema;
- from system of a hemopoiesis: anemia, leukopenia, granulocytopenia, thrombocytopenia, eosinophilia;
- from TsNS and a peripheral nervous system: a headache, drowsiness, neuromuscular transmission disturbance, decrease in hearing up to development of irreversible deafness, vestibular frustration, a sonitus, arterial hypotension;
- from an urinary system: oliguria, proteinuria, albuminuria, cylindruria, hyperazotemia, microhematuria; seldom - a renal failure.

Interaction with other medicines:

Amitsil is incompatible in solution with penicillin, cephalosporins, Amphotericinum In, hlortiazidy, erythromycin, heparin, nitrofurantoin, thiopental, and also depending on structure and concentration of solution – with tetracyclines, group B vitamins, vitamin C and potassium chloride. At simultaneous use of Amitsil with Amphotericinum In, Vancomycinum, metoksiflurany, enflurany, NPVS, X-ray contrast means, cefalotin, cyclosporine, Cisplatinum, polymyxins the risk of development of nephrotoxic action increases. At simultaneous use of Amitsil with loopback diuretics (furosemide, Acidum etacrynicum) or with Cisplatinum the risk of development of ototoksichesky action increases. At simultaneous use with ethyl ether and blockers of neuromuscular transmission the risk of respiratory depression increases.

Contraindications:

- Hypersensitivity to amikacin, other components of drug and antibiotics of group of aminoglycosides;
- neuritis of an acoustical nerve;
- myasthenia гравис;
- heavy renal failures;
- pregnancy;
- breastfeeding period.

Overdose:

At Amitsil's use in high doses the risk of development of ototoksichesky or nephrotoxic action increases.
At parenteral administration it is necessary to consider a possibility of neuromuscular blockade.
Treatment: at toxic reactions – peritoneal dialysis or a hemodialysis.
In case of blockade and respiratory depression enter прозерин with atropine; if necessary artificial ventilation of the lungs is shown.
Use during pregnancy or feeding by a breast. Amikacin gets through a placenta and can have ototoksichesky effect on a fruit therefore its use during pregnancy is contraindicated. Drug is contraindicated for use for the women nursing therefore in need of its use breastfeeding follows прекратить.Дети. With extra care it is necessary to use drug at children up to 3 years.

Storage conditions:

Period of validity 2 years. To store in the place, unavailable to children, in original packaging, at a temperature not over 25 ºС.

Issue conditions:

According to the recipe

Packaging:

On 250 mg in bottles.