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

Bactericidal broad-spectrum antibiotic from the group of aminoglycosides. It binds to the 30S subunit of ribosomes and disrupts the synthesis of the protein, preventing the formation of a complex of transport and information ribonucleic acid, with an erroneous reading of the genetic code and the formation of non-functional proteins. Has bactericidal action - in high concentrations reduces the barrier functions of cell membranes and causes the death of microorganisms.

Highly sensitive to gentamicin (minimal inhibitory concentration (MIC) less than 4 mg / l), gram-negative microorganisms - Proteus spp. (including indole-fat and indolentric 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., Citrobacter spp., Providencia spp.
Resistant (MIC of 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, is active against Enterococcus faecalis, Enterococcus faecium, Enterococcus durans, Enterococcus avium, almost all strains of Streptococcus faecalis and their varieties including Streptococcus faecalis liguifaciens, 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:

Absorbed quickly and completely. The time required to reach a maximum concentration of 0.5-1.5 hours, the maximum concentration after intramuscular injection of 1.5 mg / kg is 6 μg / ml, the therapeutic concentrations in the blood persist for 8-12 hours.

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 pus from the wounds, granulation.Low concentrations are found in adipose tissue, muscles, bones, bile, breast milk, watery eyes, bronchial secretion, sputum and cerebrospinal fluid.

In therapeutic concentrations in adults, virtually does not penetrate the blood-brain barrier, with meningitis, its concentration in the cerebrospinal fluid increases. Penetrates through the placenta.

Not exposed to metabolism. The half-life 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 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 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, empyema of the pleura);

- complicated urogenital infections (including pyelonephritis, cystitis, urethritis, prostatitis, gonorrhea, endometritis);

- infections of bones and joints (including osteomyelitis);

- skin and soft tissue infections;

- abdominal infections (peritonitis, pelvioperitonitis);

- infections of the central nervous system (including meningitis);

- sepsis;

- wound infection, burn infection;

- otitis media.

Contraindications:Hypersensitivity to gentamicin (including other aminoglycosides in history), neuritis of the auditory nerve, severe chronic renal failure with azotemia and uremia, newborns (up to 1 month).

Carefully:Myasthenia gravis, parkinsonism, botulism (aminoglycosides can cause a violation of neuromuscular transmission, which leads to further weakening of skeletal muscles), dehydration, renal insufficiency, advanced age, pregnancy, lactation period, prematurity of children.

Pregnancy and lactation:The use of the drug during pregnancy and during breastfeeding is possible if the expected benefit for the mother exceeds the potential risk to the fetus and the baby.

Dosing and Administration:

Intramuscularly.For intramuscular injection, the contents of the vial are dissolved in 2 ml of water for injection.

The daily dose for diseases of moderate severity for adults with normal renal function is 3 mg / kg / day: The rate of administration is 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.

Premature - 6 mg / kg / day, the frequency of administration - 2 times; children from 1 month to 2 years -6 mg / kg / day, the frequency of administration - 3 times; Children over 2 years are prescribed 3-5 mg / kg / day, the frequency of administration is 3 times.

Patients with impaired renal excretory function and elderly patients, as well as with severe burn disease, need to determine the concentration of gentamicin in plasma for an adequate choice of dosing regimen.

The interval between the administration of medium doses of gentamicin (in hours) is determined by the formula: interval (h) = creatinine concentration (mg / 100 ml) x 8.

In severe infections, an appointment is recommendedsmaller single doses with a higher multiplicity; the reduction in the single dose should be a multiple of the ratio of the interval calculated according to the above formula to the value of the normal interval between administrations (8 h). 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 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.

Side effects:

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

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

From the urinary system: nephrotoxicity - renal dysfunction (oliguria, proteinuria, microhematuria, renal failure), renal tubular necrosis.

From the digestive system: nausea, vomiting, increased activity of "liver" transaminases, hyperbilirubinemia.

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

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

Laboratory indicators: in children - hypocalcemia, hypokalemia, hypomagnesemia.

Other: fever, development of superinfection.

Overdose:

Symptoms: decrease in neuromuscular conduction (respiratory arrest).

Treatment: adults are intravenously injected with cholinesterase inhibitors (neostigmine methyl sulfate), as well as calcium preparations (5-10 ml of 10% calcium chloride solution, 5-10 ml of 10% calcium gluconate solution). Before the introduction of neostigmine methyl sulfate, intravenously atropine in a dose of 0.5-0.7 mg, the pulse is expected to increase and 1.5 mg (3 ml of a 0.05% solution) of neostigmine methyl sulfate is injected 1.5-2 minutes intravenously. If the effect of this dose is insufficient, re-inject the same dose of methyl isosulfate neostigmine (with the appearance of bradycardia, an additional injection of atropine). Children are given calcium preparations. In severe cases of respiratory depression, artificial ventilation of the lungs is necessary. Can be excreted by hemodialysis, (more effective) and peritoneal dialysis.

Interaction:

It is pharmaceutically incompatible with other medicines (including 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 citrate 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:

Before using the drug should be convinced of the absence of hypovolemia and the presence of adequate diuresis.

In the presence of "vital" evidence can be used in pregnant and lactating women.

Aminoglycosides penetrate into breast milk in small amounts. However, they are poorly absorbed from the gastrointestinal tract, and complications associated with them in infants have not been reported.

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 when administered at high doses or for a long time, therefore, 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.

Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:Powder for solution for intramuscular injection 80 mg.

Packaging:

80 mg of active substance in bottles with a capacity of 10 ml.

5 bottles are placed in a contour mesh package.

1, 5 or 10 vials or 1-2 contour packs with instructions for use are placed in a pack of cardboard.

For 50 bottles with 5 instructions for use are placed in a box of cardboard for delivery to hospitals.

Storage conditions:

In the dark place at a temperature of 10 to 25 ° C.

Keep out of the reach of children.

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

Terms of leave from pharmacies:On prescription

Registration number:LS-001598

Date of registration:04.08.2011

Expiration Date:Unlimited

The owner of the registration certificate:SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Information update date: & nbsp23.03.2017

Illustrated instructions

Instructions

Gentamicin (Gentamicin)