Universal reference book for medicines
Product name: SELEMYCIN (SELEMYCIN)

Active substance: amikacin

Type: Antibiotic of the aminoglycoside group

Manufacturer: MEDOCHEMIE (Cyprus)
Composition, form of production and packaging
The solution for intravenous and / or injection is
clear, colorless or slightly yellowish in color.

1 ml of 1 fl.

amikacin (in the form of sulfate) 250 mg 500 mg

[PRING] sodium citrate, sodium metabisulfite, sulfuric acid concentrated, water d / u.

2 ml - bottles (100) - packs of cardboard.

INSTRUCTION FOR THE SPECIALIST.

The description of the drug was approved by the manufacturer for the 2006 print edition.

PHARMACHOLOGIC EFFECT

Antibiotic of the aminoglycoside group.
Semisynthetic antibiotic of a wide spectrum of action, acts bactericidal. Linking to the 30S-subunit of ribosomes, prevents the formation of a complex of transport and matrix RNA, blocks the synthesis of protein, and also destroys the cytoplasmic membranes of bacteria. Highly active 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. (including those resistant to penicillin and some cephalosporins).
The drug is moderately active against Streptococcus spp.

At simultaneous appointment with benzilpenitsillinom shows a synergy with respect to strains Enterococcus faecalis.

Amikacin does not lose its activity by enzymes that inactivate other aminoglycosides, and can remain active against Pseudomonas aeruginosa strains resistant to tobramycin, gentamicin, and netilmicin.

Amikacin is not active against anaerobic microorganisms.

PHARMACOKINETICS

Suction

After the / m introduction is absorbed quickly and completely.
C max in blood plasma with a / m administration of the drug at a dose of 7.5 mg / kg - 21 μg / ml, after intravenous infusion at a dose of 7.5 mg / kg for 30 minutes - 38 μg / ml. The time to reach C max after the / m administration is about 1.5 h.
Distribution

Binding to plasma proteins is 4-11%.

It is well distributed in the extracellular fluid (the contents of abscesses, pleural effusion, ascitic, pericardial, synovial, lymphatic and peritoneal fluid);
in high concentrations is found in the urine; in low - in bile, breast milk, watery eye moisture, bronchial secretion, sputum and cerebrospinal fluid. Well penetrates into all tissues of the body, where it accumulates intracellularly; high concentrations are noted in organs with good blood supply - lungs, liver, myocardium, spleen, and especially in the kidneys, where it accumulates in the cortex; lower concentrations - in muscles, adipose tissue and bones.
In adults, when applied at moderate therapeutic doses (normal), amikacin does not penetrate the BBB, while the permeability of the meninges increases somewhat.
In newborns, higher concentrations are achieved in CSF than in adults.
Amikacin penetrates the placental barrier - it is found in the fetal blood and amniotic fluid.

V d in adults - 0.26 l / kg, in children - 0.2-0.4 l / kg, in newborns less than 1 week old and weighing less than 1.5 kg - up to 0.68 l / kg, age less than 1 week and body weight more 1.5 kg - up to 0.58 l / kg, in patients with cystic fibrosis - 0.3-0.39 l / kg.

The average therapeutic concentration with IV or IM injection is maintained for 10-12 hours.

Metabolism

It is not metabolized.

Excretion

T 1/2 in the terminal (?) Phase in adults is 2-4 hours, in newborns 5-8 hours, in older children 2.5-4 hours. The final value of T 1/2 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.
Pharmacokinetics in special clinical cases

If the kidney function in adults T 1/2 varies depending on the degree of impairment - up to 100 hours, in patients with cystic fibrosis - 1-2 hours. In patients with burns and hyperthermia, T 1/2 may be shorter compared with the average increased clearance.

It is excreted in hemodialysis (50% in 4-6 hours), peritoneal dialysis is less effective (25% for 48-72 hours).

INDICATIONS

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

- respiratory tract infections (bronchitis, pneumonia, pleural empyema, lung abscess);

- sepsis;

- septic endocarditis;

- CNS infections (including meningitis);

- infection of the abdominal cavity (including peritonitis);

- urinary tract infections (pyelonephritis, cystitis, urethritis, prostatitis, gonorrhea);

- Purulent infections of the skin and soft tissues (including infected burns, infected ulcers and bedsores of various origins);

- biliary tract infections;

- infections of bones and joints (including osteomyelitis);

- wound infection;

- postoperative infections;

- Otitis.

DOSING MODE

In / m, iv (5 minutes / drip for 5 minutes / drop) every 8 hours or 7.5 mg / kg every 12 hours. For bacterial infections of the urinary tract (uncomplicated) , 250 mg every 12 hours;
after the hemodialysis session, an additional dose of 3-5 mg / kg may be prescribed. The maximum dose for adults is up to 15 mg / kg / day, but not more than 1.5 g / day for 10 days.
Duration of treatment with IV introduction - 3-7 days, with / m - 7-10 days.

Preterm neonates with an initial dose of 10 mg / kg, then 7.5 mg / kg every 18-24 hours;
newborns the initial dose is 10 mg / kg, then 7.5 mg / kg every 12 hours for 7-10 days.
Patients with renal failure require a correction of the dosing regimen.

Patients with burns may need a dose of 5-7.5 mg / kg every 4 to 6 hours due to a shorter T 1/2 (1-1.5 h) in these patients.

For IV introduction, the same solutions as for IM are used, previously diluted with 200 ml of a 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 EFFECT

On the part of the digestive system: nausea, vomiting, impaired liver function (increased activity of hepatic transaminases, hyperbilirubinemia).

On the part of the hematopoiesis system: anemia, leukopenia, granulocytopenia, thrombocytopenia.

From the side of the central nervous system and peripheral nervous system: headache, drowsiness, neurotoxic effect (muscle twitching, numbness, tingling, epileptic seizures), violation of neuromuscular transmission (respiratory arrest).

From the senses: ototoxicity (hearing loss, vestibular and labyrinthine disorders, irreversible deafness), toxic effect on the vestibular apparatus (discoordination of movements, dizziness, nausea, vomiting).

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

Allergic reactions: skin rash, itching, skin hyperemia, fever, angioedema.

CONTRAINDICATIONS

- neuritis of the auditory nerve;

- severe renal failure with azotemia and uremia;

- Pregnancy;

- Hypersensitivity to the components of the drug (including other aminoglycosides) in the anamnesis.

With caution apply the drug with myasthenia gravis, parkinsonism, botulism (aminoglycosides can cause a violation of neuromuscular transmission, which leads to further weakening of skeletal muscles), dehydration, renal failure, in newborns (especially premature babies), in old age, during lactation breastfeeding).

PREGNANCY AND LACTATION

The use of Selemicin in pregnancy and during lactation is possible with life indications (aminoglycosides penetrate breastmilk in small amounts, but their absorption from the gastrointestinal tract is low, and complications in infants associated with their use are not documented).

APPLICATION FOR FUNCTIONS OF THE LIVER

Contraindicated in severe renal failure, patients with renal insufficiency require a correction of the dosing regimen.

APPLICATION FOR CHILDREN

With caution apply the drug in newborns (especially premature babies).

Preterm neonates with an initial dose of 10 mg / kg, then 7.5 mg / kg every 18-24 hours;
newborns the initial dose is 10 mg / kg, then 7.5 mg / kg every 12 hours for 7-10 days.
APPLICATION IN ELDERLY PATIENTS

The drug is administered with caution in the elderly.

SPECIAL INSTRUCTIONS

Before using the drug, the sensitivity of the isolated pathogens is determined using discs containing 30 μg of amikacin.
With a diameter of a growth free zone of 17 mm or more, the microorganism is considered sensitive, from 15 to 16 mm - moderately sensitive, less than 14 mm - resistant.
The concentration of amikacin in plasma should not exceed 25 mcg / ml (the therapeutic concentration is 15-25 mcg / ml).

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

The likelihood of developing nephrotoxicity is higher in patients with impaired renal function, as well as in the administration of the drug in high doses or for a long time (this category of patients may require daily monitoring of kidney function).

When unsatisfactory audiometric tests, the dose of the drug is reduced or discontinued.

Patients with infectious inflammatory diseases of the urinary tract are advised to take an increased amount of fluid.

In the absence of positive clinical dynamics should be remembered the possibility of developing resistant microorganisms.
In such cases, it is necessary to cancel treatment and begin appropriate therapy.
The metabase, contained in ampoules of sodium, can cause the development of allergic complications in patients (up to anaphylactic reactions), especially in patients with an allergic anamnesis.

OVERDOSE

Symptoms: toxic reactions (hearing loss, ataxia, dizziness, urination disorders, thirst, loss of appetite, nausea, vomiting, ringing or feeling in the ears, respiratory failure).

Treatment: to remove the blockade of the neuromuscular transmission and its consequences - hemodialysis or peritoneal dialysis;
anticholinesterase drugs, calcium salts, artificial ventilation, and other symptomatic and supportive therapies.
DRUG INTERACTION

Pharmaceutically incompatible with penicillins, heparin, cephalosporins, capreomycin, amphotericin B, hydrochlorothiazide, erythromycin, nitrofurantoin, vitamins of group B and C, potassium chloride.

Amikacin shows a synergism in the interaction with carbenicillin, benzylpenicillin, cephalosporins (in patients with severe chronic renal failure, when combined with beta-lactam antibiotics, a decrease in the effectiveness of aminoglycosides is possible).

Nalidixic acid, polymyxin B, cisplatin and vancomycin increase the risk of oto and nephrotoxicity.

Diuretics (especially furosemide), cephalosporins, penicillins, sulfonamides and NSAIDs, competing for active secretion in the tubules of the nephron block the elimination of aminoglycosides, increase their concentration in the serum, enhancing nephro- and neurotoxicity.

Strengthens the muscle relaxant effect of curare-like drugs.

Methoxyflurane, polymyxins for parenteral administration, capreomycin and other drugs that block neuromuscular transmission (halogenated hydrocarbons as inhalation anesthetics, opioid analgesics), transfusion of large amounts of blood with citrate preservatives - increase the risk of respiratory arrest (especially with intraperitoneal administration of amikacin ).

Parenteral administration of indomethacin increases the risk of toxic effects of aminoglycosides (an increase in T 1/2 and a decrease in clearance).

Amikacin reduces the effectiveness of drugs for the treatment of myasthenia gravis.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. The drug should be stored in a dry, protected from light and out of reach of children, at a temperature of no higher than 25 ° C.
Shelf life - 3 years.
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