Amikacin sulfate 500mg bottle №1

Mechanism of action

Antibiotic aminoglycoside group. It has a wide range of antibacterial action. Active against gram-positive bacteria: Staphylococcus spp. (including strains resistant to penicillin and methicillin); Gram-negative bacteria: Escherichia coli Proteus spp. Providencia spp. Serratia spp. Klebsiella spp. Enterobacter spp. Citrobacter spp. Salmonella spp. Shigella spp., sizomycin).
Amikacin Sulfate moderately active against Streptococcus spp. (including Streptococcus pneumoniae), Enterococcus spp.
To drug are resistant non-spore-forming gram-negative anaerobic bacteria, protozoa.

Suction
Rapidly absorbed after i / m administration. C_max Achieved 1 hour after drug administration, therapeutic concentrations of amikacin sulfate are maintained for 10-12 hours.
With intravenous drip, the concentration of amikacin sulfate in the blood plasma exceeds that observed with intramuscular administration, C_max reached in 30 minutes The dynamics of the decrease in concentration is similar to that with i / m administration, the therapeutic concentration of amikacin sulfate is maintained for 10–12 h.
Distribution
Amikacin sulfate is distributed in the lungs, liver, myocardium, spleen, bone tissue, pleural and peritoneal exudates, synovial fluid, bronchial secretions, bile. Selectively accumulates in the cortical layer of the kidneys. Amikacin sulfate penetrates through the BBB. With the inflammation of the meningeal membranes, the penetration of Amikacin Sulfate into the cerebrospinal fluid increases. Amikacin sulfate penetrates the placental barrier and is found in the blood of the fetus and amniotic fluid.
Removal
It is excreted unchanged by the kidneys by glomerular filtration, creating a high concentration in the urine.
Pharmacokinetics in special clinical situations
In patients with impaired renal excretory function, the elimination of amikacin sulfate is slowed down, which leads to an increase in its concentration in the blood plasma.

Indications and usage

Acute and chronic infections of the severe course caused by gram-negative bacteria resistant to other antibiotics (incl.to Gentamicin, sizomycin and kanamycin), or by associations of gram-positive and gram-negative bacteria:
-sepsis;
-meningitis;
-peritonitis;
- septic endocarditis;
-infectious-inflammatory diseases of the respiratory system (pneumonia, empyema, lung abscess);
-infection of the kidneys and urinary tract, especially complicated and often recurrent (pyelonephritis, urethritis, cystitis);
-infected burns.

Assign IM or IV (drip).
Adults and teenagers with normal renal function, 15 mg / kg of body weight (7.5 mg / kg every 12 hours or 5 mg / kg every 8 hours) are prescribed.
For children the initial single dose is 10 mg / kg, in the future - 7.5 mg / kg every 12 hours.
The duration of treatment is 7-10 days.
The maximum daily dose of the drug - 1.5 g, the total exchange rate dose - 15 g. In the absence of the effect, within 5 days they are transferred to treatment with other drugs.
Patients with impaired renal excretory function The first dose is 7.5 mg / kg. Subsequent doses should be reduced or the interval should be increased.
The interval is set as follows: the interval (h) is equal to the serum creatinine concentration, multiplied by 9.
With an increase in the interval of a single dose does not change.
With dose adjustment, the interval does not change (12 hours). To calculate subsequent doses applied every 12 hours, it is necessary to divide the CC value (ml / min) in patients per CC (ml / min) in the normal state, then multiply the resulting figure by the initial dose (mg).
Rules of preparation of the solution
The solution for parenteral administration is prepared immediately before administration and is used immediately after preparation.
For intramuscular administration to the contents of the vial (250 mg or 500 mg of powder), add 2-3 ml of water for injection.
For iv administration, the same solutions are used as for intramuscular administration, having previously diluted them with 200 ml of 5% glucose solution or isotonic sodium chloride solution. The concentration of the drug in the solution for iv administration should not exceed 5 mg / ml.

Urogenital: increase in residual nitrogen in blood serum, reduced QA, oliguria, proteinuria, cylindruria.
Nervous system: rarely, neuromuscular blockade; decrease in hearing (decrease in perception of high tones), disorders of the vestibular apparatus (dizziness). The incidence of vestibular and auditory disorders increases in patients with renal failure.
Allergic reactions: skin rash, fever, headache.
Local reactions: with the on / in the introduction of possible development of phlebitis and periphlebites.

Contraindications

- unhealthy auditory nerve;
- dysfunction of the vestibular apparatus;
-azotemia (residual nitrogen above 150 mg%);
- myasthenia;
-pregnancy;
- increased sensitivity to amikacin sulfate or other aminoglycosides.

Pregnancy and breastfeeding

The drug is contraindicated for use in pregnancy.
If necessary, the use of the drug during lactation should decide on the termination of breastfeeding.

Before using the drug, determine the sensitivity of isolated pathogens using discs containing 30 μg of amikacin sulfate. With a zone diameter of 17 mm and more, the pathogen is considered sensitive, from 15 mm to 16 mm is moderately sensitive, less than 14 mm is stable.
Oto- and nephrotoxic reactions are usually reversible. To prevent complications and reduce the frequency of their development, it is recommended to use the drug under the control of kidney function, hearing and the vestibular apparatus (at least 1 time per week).
In patients with hypersensitivity to other aminoglycosides, cross-allergic reactions to amikacin sulfate are possible.
With the development of allergic reactions, the drug is canceled and desensitization therapy is prescribed (dimedrol, Calcium chloride).
The mechanism of development of the neuromuscular blockade is similar to the action of muscle relaxants of anti-depolarizing type. At the first signs of a blockade of neuromuscular conduction, it is necessary to stop the administration of amikacin sulfate and immediately introduce iv / into the solution of calcium chloride or the subcutaneous solution of Prozerin and atropine. If necessary, the patient is transferred to controlled breathing.
Control of laboratory parameters
Due to the variability of pharmacokinetics (especially in cases of impaired renal function), treatment should be carried out with constant monitoring of the content of amikacin in the blood plasma (the concentration should not exceed 30 μg / ml).

Overdosage

Perhaps increased oto-and nephrotoxic effects of the drug.

Drug Interactions

With simultaneous use of amikacin sulfate with drugs that cause oto- and nephrotoxic action (streptomycin, kanamycin, monomitsin, gentamicin, tobramycin, vibromycin, polymyxin B), as well as diuretics (furosemide, ethacrynic acid), increases the risk of ot-and nephrotoxic effects.Therefore, these combinations are not recommended for use.
Pharmaceutical Interaction
Due to the possible pharmaceutical incompatibility, Amikacin Sulfate cannot be mixed in the same syringe with other drugs.

Storage conditions

List B. The drug should be stored in a dry, dark place at room temperature. Shelf life - 2 years.