Гентамицин-Ферейн®

General characteristics. Structure:

Active ingredient: 40 mg of Gentamycini sulfas in 1 ampoule.

Excipients: sodium disulphite (sodium pyrosulphite); dinatrium эдетат (disodium salt of ethylene diamine tetraacetic acid, Trilonum of B); water for injections.

Pharmacological properties:

Pharmacodynamics. A bactericidal antibiotic of a broad spectrum of activity from group of aminoglycosides. Communicates with 30S in subunit of ribosomes and breaks protein synthesis, interfering with formation of a complex of transport and information RNA, at the same time there is a wrong reading of a genetic code and formation of nonfunctional proteins.

Gram-negative microorganisms - Proteus spp are highly sensitive to gentamycin (the minimum overwhelming concentration (MOC) less than 4 mg/l). (including indolpositive and indole negative strains), Escherichia coli, Klebsiella spp., Salmonella spp., Shigella spp., Campylobacter spp.; gram-positive microorganisms - Staphylococcus spp. (including penitsillinorezistentny); are sensitive at MPK of 4-8 mg/l - Serratia spp., Klebsiella spp., Pseudomonas spp. (including Pseudomonas aeruginosa), Acinetobacter spp., Citrobakter spp., Providencia spp. Rezistentna (MPK more than 8 mg/l) - Neisseria meningitides, Treponema pallidum, Streptococcus spp. (including Streptococcus pneumoniae and strains of group D), Bacteroides spp., Clostridium spp., Providencia rettgeri.

Resistance of microorganisms to gentamycin develops slowly, however the strains steady against Neomycinum and Kanamycinum can show stability as well to gentamycin (incomplete cross stability). Does not affect mushrooms, viruses, the elementary.

Pharmacokinetics. After intramuscular introduction (in oil) it is soaked up quickly and completely. Time of achievement of the maximum concentration (TCmax) after introduction in oil - 0,5-1,5 h, after 30 min. intravenous (in/in) infusion - 30 min., after 60 min. in/in infusion - 15 min.; the maximum concentration (Cmax) after in oil or in/in introductions of 1,5 mg/kg makes 6 mkg/ml.

Communication with proteins of plasma - low (to 10%). Distribution volume adults - 0,26 l/kg, at children have 0,2-0,4 l/kg. It is found in therapeutic concentration in a liver, kidneys, lungs, in pleural, pericardiac, synovial, peritoneal, ascitic and lymphatic liquids, urine, in separated wounds, pus, granulations. Low concentration are noted in fatty tissue, muscles, bones, bile, breast milk, watery moisture of eyes, a bronchial secret, a phlegm and cerebrospinal fluid (SMZh).

In therapeutic concentration at adults practically does not get through a blood-brain barrier (GEB), at meningitis its concentration in SMZh increases. Gets through a placenta.

Is not exposed to metabolism. An elimination half-life of drug (T1/2) at adults - 2-4 h, at children aged from 1 иед up to 6 months - 3-3,5 h.

It is removed generally by kidneys in an invariable look; in insignificant quantities - with bile. At patients with normal function of kidneys for the first days 70-95% are removed, at the same time in urine concentration more than 100 mkg/ml are created. At patients with reduced glomerular filtering removal considerably decreases.

It is removed at a hemodialysis - in each 4-6 h concentration decreases by 50%. Peritoneal dialysis is less effective - for 48-72 h 25% of a dose are removed.

At repeated introductions it kumulirutsya, mainly in lymphatic space of an inner ear and in proximal departments of renal tubules.

Indications to use:

The bacterial infections caused by sensitive microflora: infections of upper and lower respiratory tracts (including bronchitis, pneumonia, a pleura empyema), the complicated urogenital infections (including pyelonephritis, cystitis, an urethritis, prostatitis, gonorrhea, an endometritis), infections of bones and joints (including osteomyelitis), infections of skin and soft tissues, abdominal infections (peritonitis, a pelviperitonitis), infections of the central nervous system (meningitis, etc.), sepsis, a wound fever, a burn infection, otitis.

Route of administration and doses:

The drug is administered intramusculary and intravenously.

Daily dose at moderately severe diseases for adults with normal function of kidneys - 3 mg/kg/days. Frequency rate of introduction - 2-3 times a day.

At the heavy course of diseases a daily dose - 5 mg/kg, frequency rate - 3-4 times a day; after improvement of a state the dose is reduced to 3 mg/kg. To patients with infectious and inflammatory diseases of urinary tract and normal function of kidneys appoint 1 time a day in a dose of 120-160 mg within 7-10 days; at gonorrhea - 240-280 mg once. To children is more senior appoint 6-7 mg/kg/days in 3 introductions 1 month (2-2,5 mkg/kg each 8 h).

The average duration of treatment is 7-10 days.

At a renal failure the scheme of introduction of Gentamycini sulfas is adjusted by reduction of doses or lengthening of intervals between introductions. In this case the single dose of drug for patients with body weight higher than 60 kg makes 1 mg/kg, it is less than 60 kg - 0,8 mg/kg. For calculation of intervals between administrations of drug by the patient with disturbance of secretory function of kidneys the following formula can be recommended: an interval between introductions in hours = to the content of creatinine in blood (mg / 100 ml) x 8.

Gentamycini sulfas dose at such patients should be calculated according to the provided table.

The dose has to be picked up so that Cmax did not exceed 12 mkg/ml (decrease in risk of development nefro-, from - and a neurotoxicity).

At hypostases, ascites, obesity the dose is defined on "ideal" or Sukhoi to body weight. At a renal failure and carrying out a hemodialysis the recommended doses after the session adult - 1-1,7 mg/kg (depending on weight of an infection), to children - 2-2,5 mg/kg.

In/in kapelno, during 1,5-2 h in 0,9% solution of sodium of chloride or 5% dextrose solution, the entered volume - 50-300 ml; children have to have a smaller volume of the entered liquid (concentration should not exceed 1 mg/ml = 0,1%).

Features of use:

The disulphite which is contained in sodium ampoules can cause development in sick allergic reactions, especially at patients with allergic diseases.

Patients with infectious and inflammatory diseases of urinary tract are recommended to accept the increased amount of liquid.

During treatment it is necessary to determine by aminoglycosides concentration of drug in blood serum (for the prevention of purpose of low inefficient doses or, on the contrary, drug overdose), and also to carry out control the clearance of creatinine (CC), especially at elderly people.

The probability of development of nephrotoxicity is higher at patients with an impaired renal function, and also at appointment in high doses or for a long time therefore regularly (1 or 2 times a week, and at the patients receiving high doses or being on treatment more than 10 days - daily) should be controlled функцшо kidneys.

In order to avoid development of a hearing disorder it is recommended regularly (1 or 2 times a week) to conduct a research of vestibular function for definition of a hearing loss at high frequencies (at unsatisfactory audiometric tests the dose of drug is reduced or stop treatment).

On the foyer of treatment resistance of microorganisms can develop. In similar cases it is necessary to cancel drug and to appoint treatment on the basis of data of an antibiotikogramma.

Side effects:

From digestive tract: nausea, vomiting, increase in activity of "hepatic" transaminases, hyperbilirubinemia.

From bodies of a hemopoiesis: anemia, leukopenia, granulocytopenia, thrombocytopenia.

From a nervous system: twitching of muscles, paresthesias, feeling of numbness, epileptic seizures, a headache, drowsiness, children have a psychosis.

From an urinary system: nephrotoxicity - a renal failure (an oliguria, a proteinuria, a microhematuria), in rare instances - a renal tubular necrosis.

From sense bodys: ototoxicity - a sonitus, decrease in hearing, vestibular and labyrinth disturbances, irreversible deafness.

Allergic reactions: skin rash, itch, fever, Quincke's disease, eosinophilia.

Laboratory indicators: children have a hypocalcemia, a hypopotassemia, a hypomagnesiemia. Other: fever, development of superinfection.

Interaction with other medicines:

Pharmaceutical it is incompatible (it is impossible to mix in one syringe) with other medicines (M) (including with other aminoglycosides, Amphotericinum In, heparin sodium, ampicillin, benzylpenicillin, kloksatsilliny, karbenitsilliny, kapreomitsiny).

Increases myorelaxation effect of kurarepodobny medicines. Reduces effect of anti-myasthenic medicines.

Metoksifluran, polymyxins for parenteral administration, etc. the medicines blocking neuromuscular transmission (galogenizyrovanny hydrocarbons as medicinal, means for inhalation anesthesia, narcotic analgetics, transfusion of large amounts of blood with nitrate preservatives), increase risk of emergence of nefroksichesky action and an apnoea (as a result of strengthening of neuromuscular blockade).

"Loopback" diuretics strengthen from - and nephrotoxicity (decrease in canalicular secretion of gentamycin).

Toxicity amplifies at joint appointment with Cisplatinum, etc. from - and nefrotoksichny medicines.

Antibiotics of a penicillinic row (ampicillin, карбенициллин) strengthen antimicrobic action due to expansion of a range of activity.

Parenteral administration of an itsdometatsin increases risk of development of toxic effects of aminoglycosides (increase in T1/2 and decrease in clearance).

Contraindications:

Hypersensitivity (including to other aminoglycosides in the anamnesis), neuritis of an acoustical nerve, the heavy chronic renal failure (CRF) with an azotemia and uraemia, pregnancy, the lactation period, newborn, including premature children (in connection with high risk of development of ototoksichesky and nephrotoxic action).

With care. A myasthenia, parkinsonism, botulism (aminoglycosides can cause neuromuscular transmission disturbance that leads to further weakening of skeletal muscles), dehydration, a renal failure, advanced age.

Overdose:

Symptoms: decrease in neuromuscular conductivity (apnoea).

Treatment: the adult intravenously enter antikholinesterazny medicines (прозерин), and also calcium drugs (Calcium chloratum of 10% 5-10 ml, calcium a gluconate of 10% 5-10 ml).

Before introduction of a prozerin previously intravenously enter atropine in a dose of 0,5-0,7 mg, expect increase of pulse and in 1,5-2 min. enter intravenously 1,5 mg (3 ml of 0,05% of solution) of a prozerin. If the effect of this dose was insufficient, enter repeatedly the same dose of a prozerin (at emergence of bradycardia do an additional injection of atropine). To children administer the drugs of calcium ions. In hard cases of respiratory depression artificial ventilation of the lungs is necessary. It can be removed by means of a hemodialysis (is more effective) also peritoneal dialysis.

Storage conditions:

List B. In the place protected from light at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 2 years. Not to use after the date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for intravenous and intramuscular administration, 40 mg/ml. Packaging: on 1 or 2 ml in ampoules of neutral glass. On 5, 10 ampoules in a blister strip packaging from a film polyvinyl chloride. On 5, 10 ampoules in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished or a packing material. On 1, 2 blister strip packagings together with the application instruction and a knife ampoule or the scarificator ampoule in a pack from a cardboard. On 5, 10 ampoules together with the application instruction and a knife ampoule or the scarificator ampoule in a pack with an insert with cells for ampoules in 1 or 2 rows from a cardboard. When using ampoules with a point, a break ring the knife ampoule or the scarificator ampoule is not put.