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

active substance: gentamycin (in the form of gentamycin sulfate) -40 mg; Excipients: sodium disulfite - 3.2 mg, disodium edetate dihydrate - 0.1 mg, water for injection - up to 1 ml.

Description:Colorless or greenish shade transparent solution.

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 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. (including penicillin-resistant); sensitive with MPC 4-8 mg / l -Serratia spp., Klebsiella spp .. Pseudomonas spp. (incl.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, 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. After intramuscular or intravenous administration, therapeutic concentrations in the blood are created after about 0.5-1.5 hours and remain for 8-12 hours.

Pharmacokinetics:

Absorption when taken orally - low (almost not absorbed, therefore only applied parenterally). After intramuscular injection absorbed quickly and completely. The maximum concentration in the blood serum 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 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, adults practically do not penetrate the blood-brain barrier (BBB), with meningitis concentrating it in CSF increases. Penetrates through the placenta. Not exposed to metabolism. The half-life in adults is 2-4 hours, in children from 1 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, 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 and others), sepsis, wound infection, burn infection, otitis media.

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

Carefully:Myasthenia gravis, parkinsonism, botulism (aminoglycosides can cause a breakdown of neuromuscular transmission,which leads to a further weakening of skeletal muscles), dehydration, renal failure, elderly age.

Pregnancy and lactation:Contraindicated use of the drug during pregnancy and breastfeeding.

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 (NaCl) 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 diseases 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-inflammatory diseases of the urinary tract and normal kidney function is prescribed once a day at a dose of 120-160 mg for 7-10 days; with gonorrhea - 240-280 mg once.

Children prescribe 6-7,5 mg / kg / day (2-2,5 mg / kg every 8 hours).

Patients with impaired renal excretion and elderly patients, as well as with severe burn disease For an adequate choice of the 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) x8.

In severe infections recommended the appointment 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 so that the maximum concentration in the serum 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.

When the kidney function is disturbed and hemodialysis 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, angioedema, eosinophilia.

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

Other: bronchospasm, fever, development of superinfection.

Overdose:

Symptoms: decrease in neuromuscular conduction (respiratory arrest).

Treatment: adults are intravenously injected with cholinesterase inhibitors (neostigmine methylsulfate), as well as preparations of Ca²⁺ (CaCl₂ 10% 5-10 ml, calcium gluconate 10% 5-10 ml). Before the introduction of neostigmine methyl sulfate, intravenously atropine in a dose of 0.5-0.7 mg, the pulse is expected to increase and 1.5 mg (3 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 drugs Sa²⁺. In severe cases of respiratory depression, artificial ventilation is necessary (IVL). 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 citrated preservatives) increase the risk of nephrotoxic action 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 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 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, regularly (1 or 2 times a week, and in patients receiving high doses or being treated for more than 10 days), monitor kidney function.

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:Persons experiencing side effects from the nervous system (headache, drowsiness, imbalance, etc.) should refrain from driving or other potentially dangerous mechanisms.

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

Packaging:

2 ml per ampoule.

For 10 ampoules, together with the instructions for use and the scapegrator, the ampoule is placed in a box of cardboard.

5 ampoules are placed in a contour mesh package.

For 1 or 2 contour mesh packages together with the instruction for use and the ampoule scarifier are placed in a pack of cardboard.

When using ampoules with a break ring, it is allowed to pack ampoules without an ampoule scarifier.

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:П N016270 / 01

Date of registration:07.07.2010 / 10.02.2015

Expiration Date:Unlimited

The owner of the registration certificate:OMELA, LTD. OMELA, LTD. Russia

Manufacturer: & nbsp

BELMEDPREPARATY, RUP Republic of Belarus

Information update date: & nbsp23.03.2017

Illustrated instructions

Instructions

Gentamicin (Gentamicin)