Gentamicin-Ferein - instructions for use, dose, side effects, contraindications

Pharmacodynamics:Bactericidal broad-spectrum antibiotic from the group of aminoglycosides. It binds to the 30S subunit of the ribosomes and disrupts protein synthesis, preventing the formation of a complex of transport and information RNA, with an erroneous reading of the genetic code and the formation of non-functional proteins. Highly sensitive to gentamicin (minimal inhibitory concentration (MIC) less than 4 mg / l), gram-negative microorganisms - Proteus spp. (including indol-positive and indole negative strains), Escherichia coli, Klebsiella spp., Salmonella spp., Shigella spp., Campylobacter spp .; Gram-positive microorganisms -Staphylococcus spp. (including penicillin-resistant); sensitive with MPC 4-8 mg / l - Serratia spp., Klebsiella spp., Pseudomonas spp. (including Pseudomonas aeruginosa), Acinetobacter spp., Citrobakter spp., Providencia spp. Resistant (MIC of 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 gentamicin develops slowly, however, strains resistant to neomycin and kanamycin,can exhibit resistance also to gentamicin (incomplete cross-resistance). Does not affect mushrooms, viruses, protozoa.

Pharmacokinetics:

After intramuscular (IM injection) absorbed quickly and completely. The time to reach the maximum concentration (TCmax) after IM is 0.5-1.5 hours, after 30 minutes intravenous (IV) infusion - 30 minutes, after 60 minutes IV infusion - 15 minutes; the maximum concentration (Cmax) after IM or IV injection of 1.5 mg / kg is 6 μg / ml.

The connection with plasma proteins is low (up to 10%). The volume of distribution in adults is 0.26 l / kg, in children 0.2-0.4 l / kg. It is found in therapeutic concentrations in the liver, kidneys, lungs, pleural, pericardial, synovial, peritoneal, ascitic and lymphatic fluids, urine, in segregated wounds, pus, granulation. Low concentrations are found in adipose tissue, muscles, bones, bile, breast milk, watery eyes, bronchial secretion, sputum and cerebrospinal fluid (CSF).

In therapeutic concentrations in adults, almost does not penetrate the blood-brain barrier (BBB), with meningitis, its concentration in CSF increases. Penetrates through the placenta.

Not exposed to metabolism. The half-life of the drug (T1 / 2) in adults is 2-4 hours, in children from 1 week to 6 months - 3-3.5 hours.

It is excreted mainly by the kidneys in an unchanged form; in small quantities - with bile. In patients with normal renal function, 70-95% is excreted in the first 24 hours, while concentrations of more than 100 μg / ml are created in the urine. In patients with reduced glomerular filtration, excretion is significantly reduced.

It is excreted by hemodialysis - every 4-6 hours the concentration decreases by 50%. Peritoneal dialysis is less effective - for 48-72 hours, 25% of the dose is excreted.

With repeated administration, it is cumulated, mainly in the lymphatic space of the inner ear and in the proximal sections of the renal tubules.

Indications:Bacterial infections caused by sensitive microflora: infections of the upper and lower respiratory tract (including bronchitis, pneumonia, pleural empyema), complicated urogenital infections (including pyelonephritis, cystitis, urethritis, prostatitis, gonorrhea, endometritis), infections bones and joints (including osteomyelitis), skin and soft tissue infections, abdominal infections (peritonitis, pelvioperitonitis), central nervous system infections (meningitis, etc.), sepsis, wound infection, burn infection, otitis media.

Contraindications:Hypersensitivity (incl. To dr.aminoglycosides in the history), neuritis of the auditory nerve, severe chronic renal failure (CRF) with azotemia and uremia, pregnancy, lactation, newborns, including premature infants (due to a high risk of ototoxic and nephrotoxic action).

Carefully:Myasthenia gravis, parkinsonism, botulism (aminoglycosides can cause disruption of neuromuscular transmission, which leads to further weakening of skeletal muscles), dehydration, renal insufficiency, and advanced age.

Dosing and Administration:

The drug is administered intramuscularly and intravenously.

The daily dose for moderate diseases for adults with normal renal function is 3 mg / kg / day. Multiplicity of administration - 2-3 times a day.

In severe cases, the daily dose - 5 mg / kg, multiplicity - 3-4 times a day; after improving the condition, the dose is reduced to 3 mg / kg. Patients with infectious and inflammatory diseases of the urinary tract and normal kidney function are prescribed once a day at a dose of 120-160 mg for 7-10 days; with gonorrhea - 240-280 mg once. Children over 1 month. prescribe 6-7 mg / kg / day in 3 injections (2-2.5 μg / kg every 8 hours).

The average duration of treatment is 7-10 days.

In renal failure, the gentamycin sulfate administration regimen is adjusted by decreasing the doses or extending the intervals between the administrations. In this case, a single dose of the drug for patients with a body weight above 60 kg is 1 mg / kg, less than 60 kg - 0.8 mg / kg. To calculate the intervals between the administration of the drug to a patient with impaired renal excretory function, the following formula can be recommended: interval between administrations in hours = creatinine content in blood (mg / 100 ml) x 8.

The dose of gentamicin sulfate in such patients should be calculated according to the table below.

Content serum creatinine, mg / 100 ml	Creatinine clearance, ml / min / 1,73 m²	The magnitude of the dose, % from injected with normal kidney function
<1,0	> 100	100
1,1-1,3	70-100	80
1,4-1,6	55-70	65
1,7-1,9	45-55	55
2,0-2,2	40-45	50
2,3-2,5	35-40	40
2,6-3,0	30-35	35
3,1-3,5	20-30	30
3,6-4,0	20-25	25
4,1-5,1	15-20	20
5,2-6,6	10-15	15
6,7-8,0	< 10	10

The dose should be selected so that Cmax does not exceed 12 μg / ml (reduced risk of developing nephro-, oto- and neurotoxicity).

With edema, ascites, obesity, the dose is determined by the "ideal" or "dry" mass of the body. In case of kidney failure and hemodialysis, the recommended dose after the adult session is -1-1.7 mg / kg (depending on the severity of the infection), children - 2-2.5 mg / kg.

In / in drip, for 1.5-2 hours in a 0.9% solution of sodium chloride or 5% solution of dextrose, injected volume - 50-300 ml; in children, the volume of the injected fluid should be less (concentration should not exceed 1 mg / ml = 0.1%).

Side effects:

From the gastrointestinal tract: nausea, vomiting, increased activity of "liver" transaminases, hyperbilirubinemia.

From the hematopoiesis: anemia, leukopenia, granulocytopenia, thrombocytopenia.

From the nervous system: twitching of muscles, paresthesia, sensation of numbness, epileptic seizures, headache, drowsiness, in children - psychosis.

From the urinary system: nephrotoxicity - a violation of kidney function (oliguria, proteinuria, microhematuria), in rare cases - renal tubular necrosis.

From the sense organs: ototoxicity - noise in the ears, hearing loss, vestibular and labyrinthine disorders, irreversible deafness.

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

Laboratory indicators: in children - hypocalcemia, hypokalemia, hypomagnesemia. Other: fever, development of superinfection.

Overdose:

Symptoms: decrease in neuromuscular conduction (respiratory arrest).

Treatment: adults are injected intravenously with anticholinesterase drugs (proserin), as well as calcium preparations (calcium chloride 10% 5-10 ml, calcium gluconate 10% 5-10 ml).

Before the introduction of proserine, intravenously atropine in a dose of 0.5-0.7 mg, the pulse is expected to accelerate and 1.5 mg (3 ml 0.05% solution) of prozerol is injected 1.5-2 minutes intravenously. If the effect of this dose was insufficient, re-inject the same dose of prosirin (with the appearance of bradycardia, an additional injection of atropine). Children are given preparations of calcium ions. In severe cases of respiratory depression, artificial ventilation is necessary. Can be excreted by hemodialysis (more effective) and peritoneal dialysis.

Interaction:

It is pharmaceutically incompatible with other drugs (including other aminoglycosides, amphotericin B, sodium heparin, ampicillin, benzylpenicillin, cloxacillin, carbenicillin, capreomycin).

Increases the muscle relaxant effect of curare-like medicines.Reduces the effect of antimiasthenic drugs.

Methoxyflurane, polymyxins for parenteral administration, and other drugs that block neuromuscular transmission (halogenated hydrocarbons as medicines, agents for inhalation anesthesia, narcotic analgesics, transfusion of large amounts of blood with nitrate preservatives) increase the risk of nephroxia and respiratory arrest as a result of increased neuromuscular blockade).

"Loop" diuretics increase oto and nephrotoxicity (decrease in tubular secretion of gentamicin).

Toxicity is enhanced when co-administered with cisplatin and other oto- and nephrotoxic drugs.

Antibiotics of the penicillin series (ampicillin, carbenicillin) enhance the antimicrobial effect by expanding the spectrum of activity.

Parenteral administration of iodomethacin increases the risk of toxic actions of aminoglycosides (an increase in T1 / 2 and a decrease in clearance).

Special instructions:

The disulfite contained in ampoules of sodium can cause development of allergic reactions in patients, especially in patients with allergic diseases.

Patients with infectious and inflammatory diseases of the urinary tract is recommended to take an increased amount of liquid.

During the treatment with aminoglycosides, the serum concentration of the drug should be determined (to prevent the administration of low ineffective doses or, conversely, drug overdose), and to monitor the clearance of creatinine (CC), especially in the elderly.

The probability of developing nephrotoxicity is higher in patients with impaired renal function, as well as in appointments in high doses or for a long time, so regularly (1 or 2 times a week, and in patients receiving high doses or being treated for more than 10 days - daily), kidney function should be monitored.

To avoid the development of hearing impairment, it is recommended that a regular (1 or 2 times a week) study of the vestibular function be performed to determine hearing loss at high frequencies (with poor audiometric tests, the dose of the drug is reduced or discontinued).

Against the background of treatment, resistance of microorganisms can develop. In such cases, you must stop the drug and prescribe treatment based on antibiogram data.

Form release / dosage:Solution for intravenous and intramuscular administration, 40 mg / ml.

Packaging:

1 or 2 ml into neutral glass ampoules.

5, 10 ampoules per contour cell pack of polyvinyl chloride film.

5, 10 ampoules per contour cell packaging made of polyvinylchloride film and aluminum foil printed lacquered, or packaging material.

For 1, 2 contour mesh packages together with the instructions for use and a vial ampoule or scarifier ampullum in a pack of cardboard.

For 5, 10 ampoules, together with the instruction for use and a knife ampoule or scarifier ampullum in a pack with an insert with cells for ampoules in 1 or 2 rows of cardboard.

If you use ampoules with a point, a ring of a fracture, an ampoule knife or an ampoule scapegrator is not inserted.

Storage conditions:

List B. In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:2 years. Do not use after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N001205 / 01

Date of registration:10.09.2008

Expiration Date:Unlimited

The owner of the registration certificate:BRYNTSALOV-A, CJSC BRYNTSALOV-A, CJSC Russia

Manufacturer: & nbsp

BRYNTSALOV-A, CJSC Russia

Information update date: & nbsp23.03.2017

Illustrated instructions

Instructions

Gentamicin-Ferein® (Gentamicin-Ferein)