Selemicin, 250 mg/ml 2 ml 100 pcs

Pharmacological properties

Semi-synthetic broad-spectrum antibiotic, acts bactericidally. It binds with 30S ribosome subunit, prevents formation of transport and matrix ribonucleic acid (RNA) complex, blocks protein synthesis and destroys 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, some cephalosporins); moderately active against Streptococcus spp.

In concomitant administration with benzylpenicillin it has a synergistic effect against strains of Enterococcus faecalis.

It has no effect on anaerobic microorganisms.

Amicacin does not lose activity under the action of enzymes that inactivate other aminoglycosides and may remain active against strains of Pseudomonas aeruginosa resistant to tobramycin, gentamicin and netilmicin.

Pharmacokinetics

After intramuscular (i.m.) administration, absorption is rapid and complete. Maximum concentration (Cmax) with 7.5 mg/kg intramuscular administration is 21 µg/ml, after 30 min intravenous (IV) infusion of 7.5 mg/kg is 38 µg/ml. Time of reaching maximum concentration (TCmax) is about 1.5 h after intravenous administration. Binding to plasma proteins is 4-11%.

It is well distributed in extracellular fluid (contents of abscesses, pleural effusion, ascitic fluid, pericardial, synovial, lymphatic and peritoneal fluid); in high concentration it is found in urine; in low concentration – in bile, breast milk, aqueous humor of eyes, bronchial secretion, sputum and cerebrospinal fluid (CSF). It penetrates well into all body tissues, where it accumulates intracellularly; high concentrations are noted in organs with good blood supply: lungs, liver, myocardium, spleen, and especially in kidneys, where it accumulates in cortical substance, lower concentrations – in muscles, adipose tissue and bones.

When administered in medium therapeutic doses (normal) in adults, amikacin does not penetrate the blood-brain barrier (BBB); in inflammation of the brain membranes permeability increases slightly. Neonates reach higher concentrations in the CSF than adults; it passes through the placenta and is detected in fetal blood and amniotic fluid. Distribution volume in adults is 0.026 l/kg, in children – 0.2-0.4 l/kg, in newborns – less than 1 week old and weighing less than 1500 g – up to 0.68 l/kg, in those less than 1 week old and weighing more than 1500 g – up to 0.58 l/kg, in cystic fibrosis patients – 0.3-0.39 l/kg. Average therapeutic concentration when administered by IV or IM is maintained for 10-12 hours.

It is not metabolized. Elimination half-life (T1/2) in adults is 2-4 hours, in infants – 5-8 hours, in older children – 2.5-4 hours. Final value of T1/2 is more than 100 hours (release from intracellular depots).

Extracted by the kidneys by glomerular filtration (65-94%), mainly unchanged. Renal clearance is 79-100 ml/min.

The T1/2 in adults with impaired renal function varies depending on the degree of impairment – up to 100 h, in patients with cystic fibrosis – 1-2 h, in patients with burns and hyperthermia T1/2 may be shorter compared to the average figures due to increased clearance.

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

Indications

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

Active ingredient

Composition

1 ml contains:

The active ingredient:

Amicacin sulfate equivalent to amikacin base – 250 mg;

Associates:

Sodium citrate dihydrate – 25.10 mg,

Sodium disulfite – 6.60 mg,

Sulfuric acid concentrated to pH 3.5-5.5,

Injection water up to 1 ml.

How to take, the dosage

I/m, v/v (by jetting for 2 minutes or by drip) 5 mg/kg every 8 hours or 7.5 mg/kg every 12 hours. In case of bacterial urinary tract infections (uncomplicated) – 250 mg every 12 hours; an additional dose of 3-5 mg/kg may be prescribed after a hemodialysis session. Maximum doses for adults are up to 15 mg/kg/day, but no more than 1.5 g/day for 10 days.

The duration of treatment when administered intravenously is 3-7 days, when administered intravenously is 7-10 days.

In premature infants the initial dose is 10 mg/kg, then 7.5 mg/kg every 18-24 hours; in newborns the initial dose is 10 mg/kg, then 7.5 mg/kg every 12 hours for 7-10 days.

Patients with renal insufficiency require adjustment of the dosing regimen.

Patients with burns may require a dose of 5-7.5 mg/kg every 4-6 h due to the shorter T1/2 (1-1.5 h) in these patients.

Interaction

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

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

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

Diuretics (especially furosemide), cephalosporins, penicillins, sulfonamides and nonsteroidal anti-inflammatory drugs, competing for active secretion in nephron tubules, block elimination of aminoglycosides and increase their serum concentrations, increasing nephro- and neurotoxicity.

It enhances the myorelaxant effect of nondepolarizing myorelaxants.

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

Parenteral administration of indomethacin increases the risk of aminoglycoside toxic effects (increased elimination half-life and decreased clearance).

Decreases the effect of antimiasthenic drugs.

Special Instructions

The sensitivity of isolated pathogens is determined before use using discs containing 30 µg amikacin. When the diameter of the growth-free zone is 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 µg/ml (therapeutic concentration is 15-25 µg/ml).

The renal, auditory nerve and vestibular function should be monitored at least once a week during treatment.

The likelihood of nephrotoxicity is greater in patients with impaired renal function and when high doses are prescribed or for prolonged periods (daily monitoring of renal function may be necessary in this category of patients).

In case of unsatisfactory audiometric tests, the drug dose is reduced or treatment is stopped.

Patients with infectious inflammatory diseases of the urinary tract are advised to take increased amounts of fluids.

In the absence of positive clinical dynamics, it is necessary to remember about the possibility of development of resistant microorganisms. In such cases, treatment should be stopped and appropriate therapy should be initiated.

The sodium disulfite in the ampoule can cause allergic complications (up to and including anaphylactic reactions) in patients, especially in those with a history of allergy.

The concomitant use of ototoxic and nephrotoxic drugs is to be avoided.

Impact on the ability to drive vehicles and operate moving machinery

Persons experiencing sensory side effects (dizziness) should refrain from driving or operating other potentially dangerous machinery.

Contraindications

Hypersensitivity to amikacin (including other aminoglycosides in anamnesis) and other components of the drug, auditory neuritis, severe chronic renal failure with azotemia and uremia, pregnancy.

With caution

Myasthenia gravis, parkinsonism, botulism (aminoglycosides may cause disruption of neuromuscular transmission, leading to further weakening of the skeletal musculature), dehydration, renal failure, newborn period, premature children, advanced age.

Side effects

Allergic reactions: skin rash, itching, skin hyperemia, fever, Quincke’s edema.

In the digestive system: nausea, vomiting, liver function disorders (increased activity of “liver” transaminases – aspartate aminotransferase (AST), alanine aminotransferase (ALT), hyperbilirubinemia).

Nervous system disorders: headache, somnolence, neurotoxic effect (muscle twitching, numbness, tingling sensation, convulsions), violation of neuromuscular transmission (respiratory arrest).

More urinary system disorders: nephrotoxicity – renal dysfunction (oliguria, proteinuria, microhematuria).

Hematopoietic organs: anemia, leukopenia, granulocytopenia, thrombocytopenia, hypercreatininemia, azotemia, eosinophilia.

Senses: ototoxicity (decreased hearing, vestibular and labyrinthine disorders, irreversible deafness), toxic effects on the vestibular system (discoordination of movements, dizziness, nausea, vomiting).

Motor system disorders: arthralgia.

Local reactions: soreness at the injection site, dermatitis.

Overdose

Symptoms:

Toxic reactions (hearing loss, ataxia, dizziness, urinary disorders, thirst, decreased appetite, nausea, vomiting, ringing or tinnitus, respiratory disorders).

Treatment:

To relieve neuromuscular transmission blockade and its consequences, hemodialysis or peritoneal dialysis; anticholinesterase agents, calcium salts, artificial lung ventilation, other symptomatic and supportive therapy.

Pregnancy use

The drug is contraindicated in pregnancy.

If it is necessary to prescribe the drug during lactation, it is necessary to decide whether to stop breastfeeding.