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

Excipients: sodium metabisulphite (sodium disulfite) - 3.2 mg, edetate disodium (ethylenediaminetetraacetic acid disodium salt) - 0.1 mg, water for injection - up to 1 ml.

Description:Colorless or slightly colored transparent liquid.

Pharmacotherapeutic group:Antibiotic - aminoglycoside

ATX: & nbsp

J.01.G.B.03 Gentamicin

Pharmacodynamics:

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

Absorption when taken orally - low (almost not absorbed, therefore only applied parenterally).

After intramuscular injection absorbed quickly and completely. Time to reach the maximum concentration 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 plasma concentration 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, in newborns under the age of 1 week. and body weight less than 1.5 kg - up to 0.68 l / kg, at the age of up to 1 week. and a body weight of more than 1.5 kg - up to 0.58 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.

In therapeutic concentrations in adults, virtually does not penetrate the blood-brain barrier, with meningitis, its concentration in the cerebrospinal fluid increases. Newborns have higher concentrations in the cerebrospinal fluid than in adults. Penetrates through the placenta. Not exposed to metabolism. The half-life in adults is 2-4 hours, in children aged 1 week. up to 6 months. - 3-3,5 h, in newborns and premature infants with a body weight of more than 2 kg - 5.5 h, with a body weight of less than 1.5 kg - 11.5 h, up to 2 kg - 8 h.

It is excreted mainly by the kidneys in unchanged form; in small amounts-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, 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), sepsis, wound infection, burn infection, otitis media.

Contraindications:Increased sensitivity to gentamicin (including other aminoglycosides in the anamnesis),hypersensitivity to other components of the drug, neuritis of the auditory nerve, severe chronic renal failure with azotemia and uremia, pregnancy, the period of breastfeeding, newborns (up to 1 month), 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.

Pregnancy and lactation:Use during pregnancy is contraindicated; If it is necessary to use the drug during lactation, breastfeeding should be abolished (due to a high risk of ototoxic and nephrotoxic action).

Dosing and Administration:

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

Intravenously 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%).

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 from 1 month. up to 2 years - 6 mg / kg / day, multiplicity of administration - 3 times; children older than 2 years -3-5 mg / kg / day, the frequency of administration - 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 average doses of gentamicin (in hours) is determined by the formula; interval (h) = creatinine concentration (mg / 100 ml) x 8.

In severe infections, the recommended use of smaller 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 in the plasma does not exceed 12 μg / ml (reduced risk of nephro-, oto- and neurotoxicity). With edema, ascites, obesity, the dose is determined by the "ideal" or "dry" mass of the body.

If the kidney function is violated and hemodialysis is carried out, the recommended dose after the adult session is 1-1.7 mg / kg (depending on the severity of the infection), children from 1 month. - 2-2.5 mg / kg.

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), 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 calcium preparations. 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 (it should not be mixed in one syringe) 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 of increased neuromuscular blockade).

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

Toxicity is enhanced when combined 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 (an increase in the half-life of the drug and a decrease in clearance).

Special instructions:

The metabase contained in ampoules of sodium can cause the development of allergic complications 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 creatine, especially in the elderly.

The likelihood of developing nephrotoxicity is higher in patients with impaired renal function, as well as in appointing 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 - every day ), 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, it is necessary to cancel the drug and prescribe a treatment based on the antibioticogram.

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.

Effect on the ability to drive transp. cf. and fur:Care must be taken when managing vehicles, mechanisms and engaging in other potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Form release / dosage:Solution for intravenous and intramuscular administration 40 mg / ml in ampoules of 1 ml or 2 ml.

Packaging:

For 10 ampoules with instructions for use, with an ampoule or ampoule ampoule knife in a pack or box of cardboard.

When packing ampoules that have a break ring or a point for dissection, the ampoule knife or scarifier does not insert.

5 ampoules in a cassette outline package. 2 cassette contour packs with instructions for use in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of 18 to 25 ° C.

Keep out of the reach of children.

Shelf life:2 years. Do not use after the time specified on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N000108 / 01

Date of registration:22.01.2008 / 16.07.2014

Expiration Date:Unlimited

The owner of the registration certificate:MICROGEN FGUP Scientific and Production Association MICROGEN FGUP Scientific and Production Association Russia

Manufacturer: & nbsp

MICROGEN FGUP NGO Russia

Information update date: & nbsp23.03.2017

Illustrated instructions

Instructions

Gentamicin (Gentamicin)