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

Composition:Active substance: Gentamycin sulfate (in terms of gentamicin) - 0.04 g in 1 ml. Excipients: sodium pyrosulfite, disodium ethylenediaminetetraacetic acid, water for injection.

Description:Transparent colorless or slightly greenish 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 protein synthesis, preventing the formation of a complex of transport and information RNA, with erroneous reading of RNA and the formation of non-functional proteins. Has a bactericidal action - in high concentrations reduces the barrier functions of cytoplasmic membranes and causes the death of microorganisms.

Highly sensitive to gentamycin (MIC of 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. (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 with benzylpenicillin, ampicillin, carbenicillin, oxacillin) acting on the cell wall synthesis microorganisms is active against Enterococcus faecalis, Enterococcus faecium, Enterococcus durans, Enterococcus avium, virtually all strains of Streptococcus faecalis and varieties (including Str.faecalis liguifaciens, Str.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 the / m administration is 0.5-1.5 h, after 30 min intravenous (IV) infusion - 30 min, after 60 min IV infusion - 15 min; the value of Cmax after IM or IV 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 in body weight less than 1.5 kg, up to 0.68 l / kg, up to 1 week and body weight of more than 1.5 kg 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 the separated wounds, pus, granulations. 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 - 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 less than 1.5 kg - 11.5 h, up to 2 kg - 8 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), 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, lactation, newborns, including premature infants, children (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.

Dosing and Administration:

Parenteral. The daily dose for intravenous and / or intramuscular injection for moderate to severe diseases is the same for adults with normal renal function - 3 mg / kg / day. Multiplicity of administration - 2-3 times a day. In / in the drip, for 1.5-2 hours in 0.9% NaCl solution or 5% dextrose solution, the injected volume is 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; premature and newborn (age less than 1 week) is prescribed in a daily dose of 6 mg / kg; multiplicity - 2 times; children under 2 years - 6 mg / kg with the frequency of administration 3 times a day.

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, 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 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. 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:

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.

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 (proserin), as well as calcium preparations (calcium chloride 10% 5-10 ml, calcium gluconate 10% 5-10 ml). Before the introduction of proserine, I / atropine in a dose of 0.5-0.7 mg, the pulse is expected to accelerate, and 1.5 mg (3 ml of 0.05% solution) of prozerol is injected 1.5-2 minutes later.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). 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 with other drugs (including other aminoglycosides, amphotericin B, heparin, ampicillin, benzylpenicillin, cloxacillin, carbenicillin, capreomycin).

Increases the muscle relaxant effect of curare-like drugs.

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 enhancement neuromuscular blockade).

"Loop" diuretics increase oto and nephrotoxicity (decrease in tubular secretiongentamycin).

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 (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 the 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 (CC), especially in the elderly.

The likelihood of developing nephrotoxicity is higher in patients with impaired renal function, as well as in the administration of 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, you must stop the drug and prescribe treatment based on antibiogram data.

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

Packaging:1 or 2 ml in ampoules. For 10 ampoules together with the instruction for use and a knife for opening ampoules or a scarifier ampoule in a box of cardboard.

Storage conditions:

List B. 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 expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N012010 / 01

Date of registration:19.12.2007 / 11.09.2012

Expiration Date:Unlimited

The owner of the registration certificate:BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Manufacturer: & nbsp

BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Information update date: & nbsp23.03.2017

Illustrated instructions

Instructions

Gentamicin (Gentamicin)