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 ribonucleic acid (RNA), 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 indol-positive and indolotricate strains), Escherichia coli, Klebsiella spp., Salmonella spp., Shigella spp., Campylobacter spp .; Gram-positive microorganisms - Staphylococcus spp. (incl.penicillin-resistant); sensitive for MPC 4-8 mg / l -Serratia spp., Klebsiella spp., Pseudomonas spp. (including Pseudomonas aeruginosa), Acinetobacter spp., Citrobacter spp., Providecia 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, 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:

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 (C max) 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, in newborns under 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 (CSF). In therapeutic concentrations in adults, almost does not penetrate the blood-brain barrier (BBB), with meningitis, its concentration in CSF increases. In newborns, higher concentrations are achieved in CSF than in adults. Penetrates through the placenta.

Not exposed to metabolism. The half-life period (T1 / 2) in adults is 2-4 hours, in children from 1 week to 6 months of age - 3-3.5 hours, in newborns and premature infants with a body weight of more than 2 kg, 5.5 hours, 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 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, 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 (CNS) infections (meningitis - etc.), sepsis, wound infection, burn infection , otitis media.

Contraindications:Hypersensitivity (including to other aminoglycosides in the anamnesis), neuritis of the auditory nerve, severe chronic renal failure (CRF) with azotemia and uremia, pregnancy and lactation (due to a high risk of ototoxic and nephrotoxic action), newborns up to 1 month) and premature babies.

Carefully:With caution appoint gentamicin Parkinsonism, myasthenia gravis, renal dysfunction, botulism (aminoglycosides can cause a breakdown of the neuromuscular transmission, which leads to further weakening of the skeletal muscles), to the elderly.

Pregnancy and lactation:The use of the drug during pregnancy and lactation, newborns and premature babies is contraindicated.

Dosing and Administration:

Intramuscularly, intravenously drip. The daily dose for intravenous (intravenous) and intramuscular (IM) administration for diseases of moderate severity is the same for adults with normal renal function - 3 mg / kg / day. Multiplicity of administration 2-3 times a day. In / in drip, for 1.5-2 hours in a 0.9% solution of sodium chloride (NaCl) or 5% solution of dextrose, injected volume of 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 over 2 years are prescribed 3-5 mg / kg / day; multiplicity of administration - 3 times; children from 1 month to 2 years - 6 mg / kg with the frequency of administration 3 times a day.

Patients with impaired renal excretory function and elderly patients, and also, in severe burn disease for an adequate choice of dosing regimen, a determination of the concentration of gentamicin in plasma is required.

The interval between the administration of average doses of gentamicin (in hours) is determined by the formula: interval (h) = creatinine concentration (mg / 100 ml) * 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 from the above formula to the value of the normal interval between administrations (8h). The dose should be selected in such a way that Cmax does not exceed 12 μg / ml (reduced risk of developing nephro-, oto- and neurotoxicity).

With edema, ascites, obesity, the dose is calculated by the "ideal" or "dry" body weight. If the renal function is impaired 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.

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 - renal dysfunction (oliguria, proteinuria, microhematuria), 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, Quincke's edema, eosinophilia, bronchospasm.

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

Overdose:

Symptoms: decrease in neuromuscular conduction (respiratory arrest).

Treatment: adults in / in injected anticholinesterase drugs (neostigmine methylsulfate), as well as calcium preparations (calcium chloride 10% 5-10 ml, calcium gluconate 10% 5-10 ml).Before the introduction of neostigmine methyl sulfate, pre-IV injection atropine in a dose of 0.5-0.7 mg, the pulse is expected to increase more rapidly, and 1.5 mg (3 ml, 0.05% solution) of neostigmine methyl sulfate is injected 1.5-2 minutes later. 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). In severe cases of respiratory depression, artificial ventilation is necessary. Can be excreted by hemodialysis (more effective) and peritoneal dialysis.

Interaction:

Pharmaceutically incompatible with other drugs (including other aminoglycosides, amphotericin B, heparin, ampicillin, benzylpenicillin, cloxacillin, carbenylcillin, capreomycin).

Increases the muscle relaxant effect of curare-like drugs.

Reduces the effect of antimiasthenic drugs.

Methoxyflurane, polymyxins for parenteral administration, etc. 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 of 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 T1 / 2 and a decrease in clearance).

Special instructions:

The sodium bisulfite contained in the 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 carry out monitoring of creatinine clearance (CC), especially in the elderly.

The likelihood of nephrotoxicity was higher in patients with impaired renal function, as well as in high doses or for a long time, so a regular basis (1 or 2 times a week, and in patients receiving high doses or in treatment for more than 10 days - every day ), kidney function should be monitored.

To avoid development of hearing impairment to regularly (1 or 2 times a week) To study the vestibular function to determine the hearing loss at high frequencies (at unsatisfactory audiometrycheskih test dose reduce or discontinue treatment).

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.

Gentamicin can not be mixed in one syringe with other medicines!

Effect on the ability to drive transp. cf. and fur:So far, cases of drug influence on the performance of potentially hazardous activities that require attention and speed of reaction (road management, work with moving machinery) have been reported.

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

Packaging:2 ml per ampoule. 10 ampoules per box of cardboard along with instructions for use and a scarifier ampoule. 5 ampoules per contour pack of PVC film. 1-2 contour mesh packages together with a scarifier ampoule and instructions for use in a pack of cardboard. When using ampoules with a dot or a ring of fracture, the scarifier is not embedded.

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 the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N003962 / 01

Date of registration:22.12.2009

Expiration Date:Unlimited

The owner of the registration certificate:MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC Russia

Manufacturer: & nbsp

MOSHIMFARM PREPARATES them. NA Semashko OJSC Russia

Information update date: & nbsp23.03.2017

Illustrated instructions

Instructions

Gentamicin (Gentamicin)