Gentamicin - instructions for use, doses, side effects, contraindications

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. Has a bactericidal action - in high concentrations reduces the barrier functions of cytoplasmic membranes and causes the death of microorganisms.

Highly sensitive to gentamycin (minimum inhibitory concentration less than 4 mg / l), gram-negative microorganisms - Proteus spp. (including indol-positive and indolotricate strains), Escherichia coli, Klebsiella spp., Salmonella spp., Shigella spp., Campylobacter spp .; Gram-positive microorganisms - Staphylococcus spp. (including penicillin-resistant); sensitive with a minimum inhibitory concentration of 4-8 mg / l - Serratia spp., Klebsiella spp., Pseudomonas spp. (incl.Pseudomonas aeruginosa), Acinetobacter spp., Citrobacter spp., Providencia spp.

Resistant (the minimum suppressive concentration is more than 8 mg / l) - Neisseria meningitidis, Treponema pallidum, Streptococcus spp. (including Streptococcus pneumoniae and strains of group D), Bacteroides spp., Clostridium spp., Providencia rettgeri.

In combination with penicillins (including benzylpenicillin, ampicillin, carbenicillin, oxacillin), acting on the synthesis of the cell wall of microorganisms, shows activity against Enterococcus faecalis, Enterococcus faecium, Enterococcus durans, Enterococcus avium, almost all strains of Streptococcus faecalis and their varieties (including Streptococcus faecalis liquifaciens, Streptococcus faecalis zymogenes), Streptococcus faecium, Streptococcus durans. Resistance of microorganisms to gentamicin develops slowly, however, strains resistant to neomycin and kanamycin can also show resistance to gentamicin (incomplete cross-resistance). Does not affect mushrooms, viruses, protozoa.

Pharmacokinetics:

After intramuscular injection absorbed quickly and completely. The time to reach the maximum concentration (TCmax) after intramuscular injection is 0.5-1.5 hours, after 30 minutes of intravenous infusion - 30 minutes, after 60 minutes of intravenous infusion - 15 minutes; the maximum concentration (C max) after intramuscular or intravenous administration 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 the cerebrospinal fluid 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 unchanged form, in small amounts - with bile. In patients with normal renal function, 70 to 95% are excreted in the first 24 hours, while concentrations of more than 100 μg / ml are produced in the urine. In patients with reduced glomerular filtration, excretion is significantly reduced.

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

With repeated administration cumulates, 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 uregenital infections (including pyelonephritis, cystitis, urethritis, prostatitis, gonorrhea, endometritis), infections of 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 (including other aminoglycosides in the anamnesis), 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 developing 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 intravenous and intramuscular administration in cases of moderate severity 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 older than 1 month are prescribed 6-7 mg / kg / day in 3 injections (2-2.5 mg / kg every 8 hours).

The average duration of treatment is 7-10 days.

In renal failure, the gentamicin sulfate administration regimen is adjusted by decreasing the doses or extending the intervals between 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.

Creatinine content in serum, mg / 100 ml	Creatinine clearance, ml / min / 1.73 m²	Dose value,% of administered 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	25-30	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 in such a way that the maximum concentration does not exceed 12 μg / ml (reduced risk of developing nephro-, oto- and neurotoxicity)

With edema, ascites, obesity, the dose is calculated by "ideal" or "dry" body weight. If the kidney function is disrupted and hemodialysis is performed, 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.

Intravenously drip, in the flow1.5-2 hours in a 0.9% solution of sodium chloride or 5% dextrose solution administered volume - 50-300 ml; in children, the volume of the liquid should be less (concentration should not exceed 1 mg / ml = 0.1%)

Side effects:

From the digestive system: 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 to 0.7 mg, the pulse is expected to increase and 1.5 mg (3 ml of 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:

Pharmaceutically incompatible (it is impossible to mix in one syringe) with other medicines (including with other aminoglycosides, amphotericin B, 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 drugs for inhalation anesthesia, narcotic analgesics, transfusion of large amounts of blood with citrated preservatives) increase the risk of nephroxia and respiratory arrest (as a result strengthening 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 indomethacin increases the risk of toxic actions of aminoglycosides (increased half-life and decreased clearance).

Special instructions:

The disulfite contained in ampoules of sodium can cause development of allergic reactions in patients, especially in patients with allergic anamnesis. Patients with infectious and inflammatory diseases of the urinary tract is recommended to take an increased amount of liquid.

During 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, especially in the elderly.

The likelihood of developing nephrotoxicity is higher in patients with impaired renal function, as well as in the administration of high doses or for a long time,therefore, regular kidney function should be monitored regularly (1 or 2 times a week, and in patients receiving high doses or being treated for more than 10 days - every day).

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, it is necessary to cancel the drug and prescribe a treatment based on the antibioticogram.

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

Packaging:

2 ml per ampoule of neutral glass.

5 ampoules per contour cell packaging made of polyvinyl chloride film.

2 contour squares with instructions for use and a vial ampoule or scarifier amputated in a pack of cardboard.

When packing ampoules with notches, dots or rings knife ampoule or scarifier Do not invest.

Storage conditions: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 expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-007788/09

Date of registration:05.10.2009

Expiration Date:Unlimited

The owner of the registration certificate:Company DEKO, LLC Company DEKO, LLC Russia

Manufacturer: & nbsp

Company DEKO, LLC Russia

Information update date: & nbsp23.03.2017

Illustrated instructions

Instructions

Gentamicin (Gentamicin)