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. It has a bactericidal action at high concentrations that 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 in-dolotricative 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., Pseudomonas spp. (including 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:

Absorption when taken orally - low (almost not absorbed, therefore only applied parenterally). After intramuscular injection absorbed quickly and completely. The time to reach the maximum concentration (TCmax) after intramuscular injection is 0.5 to 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. 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 period (T1 / 2) in adults is 2-4 hours, in children with a body weight of more than 2 kg, 5.5 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.Displays when 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, 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, pelvic inflammation), central nervous system infections (CNS) (meningitis), sepsis, wound infection, burn infection, otitis media.

Contraindications:Hypersensitivity (including to other. Aminoglycosides history), neuritis of the acoustic nerve, severe chronic renal failure with azotemia, and uremia, pregnancy, lactation, neonatal period (up to 1 month), preterm infants (weight less than 1.5 kg), hypersensitivity to sulfites, especially in patients with a history of allergic anamnesis, bronchial asthma.

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:

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

In case of severe disease, the daily dose is 5 mg / kg, the multiplicity is 3-4 times a day, after the condition is improved, 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 are prescribed 6-7.5 mg / kg / day (2-2.5 mg / kg every 8 hours).

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: a 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.

Multiplicity of administration - 2 - 3 times a day. Intravenous drip, for 1.5-2 hours in a 0.9% solution of sodium chloride or 5% solution of dextrose, the volume administered is 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 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, bronchospasm.

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 (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, intravenously atropine in a dose of 0.5 to 0.7 mg, the pulse is expected to increase and 1.5 mg (1.5 ml of 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 is necessary. Can be excreted by hemodialysis (more effective) and peritoneal dialysis.

Interaction:

Pharmaceutically compatible (can not be mixed in the same syringe) with others. Medicines (including with others. 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 others. Medicaments that block neuromuscular transmission (halogenated hydrocarbons as medicaments for inhalation anesthetic, narcotic analgesics, transfusion of large amounts of blood to citrate preservatives), increase the risk of nefroksicheskogo action and respiratory arrest (in by enhancing 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 sodium disulfite contained in the ampoules (sodium metabisulphite) can cause the development of allergic complications in patients, especially in patients with a history of 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 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 audiometry at high frequencies be performed regularly (1 or 2 times a week) 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:A solution for intravenous and intramuscular administration of 40 mg / ml in neutral glass ampoules of 1 ml or 2 ml.

Packaging:

For 10 ampoules, together with the instruction for use and the ampoule opening opener or ampoule scarifier, is placed in a cardboard box.

5 ampoules into the contour cell package. 2 contour squeeze packs with instructions for use and a knife for opening ampoules or a scarifier ampullum are placed in a pack of cardboard.

When using ampoules with break points or rings, the ampoule scaler or knife for opening ampoules is not inserted.

Storage conditions:

List B. 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 expiry date.

Terms of leave from pharmacies:On prescription

Registration number:P N003879 / 01

Date of registration:03.11.2009

Expiration Date:Unlimited

The owner of the registration certificate:DALHIMFARM, OJSC DALHIMFARM, OJSC Russia

Manufacturer: & nbsp

DALHIMFARM, OJSC Russia

Information update date: & nbsp23.03.2017

Illustrated instructions

Instructions

Gentamicin (Gentamicin)