TEGASIN [Amicacin] 500 mg Solution for intramuscular injection, intravenous injection

TEGASIN

instructions for medical use of the medicinal product

Tradename

Tegasin, Тегасин

International non-proprietary name

Amikacin, Амикацин

Composition

Tegasin 100 mg

Each vial (2 ml solution) contains:

active ingredient: amikacin   (as sulfate) USP 100 mg

excipients: sodium citrate, sodium bisulfite, disodium edetate, water for injection.

Tegasin 500 mg

Each vial (2 ml solution) contains:

active ingredient: amikacin   (as sulfate) USP 500 mg

excipients: sodium citrate, sodium bisulfite, disodium edetate, water for injection.

Dosage form

Solution for injection .

Pharmacotherapeutic group

Aminoglycoside antibiotic.

Pharmacological properties

Tegasin is an antibiotic of the aminoglycoside group . Semi-synthetic broad-spectrum antibiotic, bactericidal. The active substance is amikacin.

Pharmacodynamics

Amikacin, binding to the 30 S subunit of ribosomes, prevents the formation of a complex of transport and messenger RNA, blocks protein synthesis, and also destroys the cytoplasmic membranes of bacteria. Highly active against gram-negative microorganisms: Klebsiella   spp , Pseudomonas   aeroginosa , E. coli , Proteus , Enterobacter   spp , Serratia   spp , Shigella   spp , Salmonella , Providencia   stuartii , Mima - Herelea , Citobacter   freundii (including strains resistant to kanamycin, gentamicin, tobramycin), as well as some gram-positive microorganisms: Staphylococcus   spp (including strains resistant to penicillin, methicillin, some cephalosporins), some strains of Streptococcus   spp .

Not active against anaerobes.
With simultaneous appointment with benzylpenicillin, synergism is manifested in relation to strains of Enterococcus   faecalis .

Pharmacokinetics

Absorption is fast and complete with intramuscular and topical application. Peak concentrations of amikacin with intramuscular injection of a dose of 7.5 mg / kg - 21 μg / ml (reached one hour after a dose of 500 mg, decreasing to 2 μg / ml 10 hours after injection), with intravenous administration over 30 minutes of a dose 7, 5 mg/kg - 38 mcg/ml (decreased to 18 mcg/ml 1 hour after IV infusion).

In critically ill patients, intramuscular absorption may be reduced [especially in conditions leading to impaired perfusion (shock) as a result of reduced plasma concentrations]. High concentrations in urine, low - in bile, sputum, CSF.

Communication with plasma proteins 0-10%. Found in therapeutic concentrations in the liver, kidneys, lungs, pleural, pericardial, synovial, peritoneal, ascitic and lymphatic fluids, urine, wound discharge, pus, granulations. Low concentrations are noted in adipose tissue, muscles, bones, bile, breast milk, aqueous humor of the eye, bronchial secretions, sputum and cerebrospinal fluid. Aminoglycosides diffuse well into the perilymph of the inner ear. Elimination by the kidneys 75-80% unchanged (glomerular filtration), in small amounts by bile. In patients with normal renal function, 70-95% is excreted in the first day, while concentrations of more than 100 μg / ml are created in the urine. The half-life in adults is 2-4 hours, in children aged 1 week to 6 months - 3-3.5 hours, in newborns and premature babies weighing more than 2 kg - 5.5 hours, with body weight less than 1, 5 kg - 11.5 hours, up to 2 kg - 8 hours, with renal failure - up to 100 hours. They are removed during hemodialysis (for every 4-6 hours the concentration of aminoglycosides decreases by 50%), peritoneal dialysis is less effective (removes ~ 25% doses for 48-72 hours).

Indications for use

Infectious and inflammatory diseases caused by gram-negative microorganisms (resistant to gentamicin, sisomycin 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),
- infections of the abdominal cavity (including peritonitis),
- Complicated urinary tract infections (pyelonephritis, cystitis, urethritis),

- purulent infections of the skin and soft tissues (including infected burns, infected ulcers and bedsores of various origins),
- infections of the biliary tract, bones and joints (including osteomyelitis),
- wound infection
- postoperative infections

Contraindications

- Hypersensitivity (including to other aminoglycosides in history),

- neuritis of the auditory nerve,

- severe chronic renal failure with azotemia and uremia.

Dosage and administration

In / m, in / in (stream, for 2 minutes, or drip, at a rate of 60 drops per minute).

The dose is set individually, taking into account the severity of the course and localization of the infection, the sensitivity of the pathogen.

Adults and children: 5 mg/kg every 8 hours or 7.5 mg/kg every 12 hours; the maximum dose is 15 mg / kg / day, the course dose is not more than 15 g.

Premature newborns: at the initial dose - 10 mg / kg, then 7.5 mg / kg every 18-24 hours; newborns: initial dose - 10 mg / kg, then 7.5 mg / kg every 12 hours.

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

Patients with renal insufficiency require correction of the dosing regimen in accordance with creatinine clearance.

Special instructions and precautions

Use with caution in patients with myasthenia gravis, parkinsonism, renal failure, as well as in the elderly. It is not recommended to use amikacin in patients with hypersensitivity to other aminoglycosides due to the risk of cross-allergy.

Use during pregnancy and during breastfeeding

Use during pregnancy and during breastfeeding is contraindicated.

Interaction with other drugs

The risk of developing nephrotoxicity increases with the simultaneous use of amikacin with amphotericin B , vancomycin, methoxyflurane, enflurane, NSAIDs, radiopaque agents, cephalothin, cyclosporine, cisplatin, polymyxins. The risk of developing an ototoxic effect increases with the simultaneous use of amikacin with "loop" diuretics (furosemide, ethacrynic acid), cisplatin. With simultaneous use with penicillins (with renal failure), the antimicrobial effect decreases. With simultaneous use with ethyl ether and neuromuscular blockers, the risk of respiratory depression increases. Amikacin is incompatible in solution with penicillins, cephalosporins, amphotericin B , chlorothiazide, erythromycin, heparin, nitrofurantoin, thiopentone, and also, depending on the composition and concentration of the solution, with tetracyclines, B vitamins, vitamin C and potassium chloride.

Side effect

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

From the nervous system: headache, drowsiness, neurotoxic effect (muscle twitching, numbness, tingling, epileptic seizures), impaired neuromuscular transmission (respiratory arrest).

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

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

Allergic reactions: skin rash, itching, skin flushing, fever, Quincke's edema.

Overdose

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

Treatment: to remove the blockade of neuromuscular transmission and its consequences - hemodialysis or peritoneal dialysis; anticholinesterase agents, calcium salts (Ca “+), mechanical ventilation, other symptomatic and supportive therapy.

Storage conditions

Store in a cool and dry place, at a temperature not exceeding 25 ⁰ C.

Keep out of the reach of children!

Best before date

3 years. Do not use after the expiry date stated on the packaging.

Holiday conditions

Released by prescription.

Release form

1 bottle of 2 ml together with instructions for use in a cardboard box.