Gentamicin Sulfate (Gentamicin sulfate)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
Read on
Active substanceGentamicinGentamicin
Similar drugsTo uncover
  • Gentamicin
    drops d / eye 
    MOSCOW ENDOCRINE FACTORY, FSUE     Russia
  • Gentamicin
    solution w / m in / in 
    Promomed Rus, Open Company     Russia
  • Gentamicin
    powder w / m 
    SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products     Russia
  • Gentamicin
    solution w / m in / in 
    OMELA, LTD.     Russia
  • Gentamicin
    solution w / m in / in 
    MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC     Russia
  • Gentamicin
    drops d / eye 
    Warsaw Pharmaceutical Plant Polfa, JSC     Poland
  • Gentamicin
    solution w / m in / in 
    DALHIMFARM, OJSC     Russia
  • Gentamicin
    solution w / m in / in 
    Company DEKO, LLC     Russia
  • Gentamicin
    solution w / m in / in 
    PHARMSTANDART-UFIM VITAMIN FACTORY, OJSC     Russia
  • Gentamicin
    ointment externally 
    NIZHFARM, JSC     Russia
  • Gentamicin
    solution w / m in / in 
    MICROGEN FGUP Scientific and Production Association     Russia
  • Gentamicin
    solution w / m in / in 
    BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC     Republic of Belarus
  • Gentamycin-AKOS
    ointment externally 
    SYNTHESIS, OJSC     Russia
  • Gentamicin-K
    solution w / m in / in 
    KRKA, dd, Novo mesto, AO    
  • Gentamicin-Ferein®
    drops d / eye 
    BRYNTSALOV-A, CJSC     Russia
  • Gentamicin-Ferein®
    solution w / m in / in 
    BRYNTSALOV-A, CJSC     Russia
  • Gentamicin Sulfate
    solution w / m in / in 
    Mapichem AG     Switzerland
    • Dosage form: & nbspsolution for intravenous and intramuscular administration
    Composition:

    1 ml of the preparation contains:

    Active substance: gentamycin sulfate (in terms of gentamicin) - 40 mg; Excipients: sodium sulfite anhydrous - 3 mg, water for injection - up to 1 ml.

    2 ml of the preparation contains:

    Active substance: gentamycin sulfate (in terms of gentamicin) - 80 mg; Excipients: sodium sulfite anhydrous - 6 mg, water for injection - up to 2 ml.

    Description:Transparent colorless or slightly yellowish 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 indolotric, strains), Escherichia coli, Klebsiella spp., Salmonella spp., Shigella spp., Campylobacter spp .; Salmonella spp., Shigella spp., Campylobacter spp .; Gram-positive microorganisms -Staphylococcus spp. (including penicillin-resistant); sensitive for 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 strains of group D), Bacteroides-spp., Clostridiumspp., Providencia rettgeri.

    In combination with penicillins (including benzylpenicillin, ampicillin, carbenicillin, oxacillin), acting on the synthesis of the cell wall of microorganisms, shows activity with respect to 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. Time to reach the maximum concentration (TCmax) after intramuscular (intramuscular) administration - 0.5-1.5 hours, after 30 minutes intravenous (IV) infusion - 30 minutes, after 60 minutes IV infusion -15 minutes; the quantity Cmax after in / m or in / in the introduction of 1.5 mg / kg is 6 mcg / 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 purulent discharge, granulation. Low concentrations are found in adipose tissue, muscles, bones, bile, breast milk, watery eyes, bronchial sputum secretion and cerebrospinal fluid (CSF). In therapeutic concentrations in adults, virtually does not penetrate the blood-brain barrier (BBB) ​​with meningitis, its concentration in the CSF -increases. In newborns, higher concentrations are achieved in CSF; than in adults. Penetrates through the placenta.

    Not exposed to metabolism. The half-life (T1/2) in adults - 2-4 hours, in children aged 1 weeks to 6 months - 3-3.5 hours, in newborns and premature babies with a body weight of more than 2 kg - 5.5 hours, with a body weight of less than 1.5 kg-11.5.ch , 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:Infectious-inflammatory diseases caused by microorganisms sensitive to gentamicin: upper and lower respiratory tract infections (including bronchitis, pneumonia, pleural empyema), complicated urogenital infections (including pyelonephritis, cystitis, urethritis, prostatitis, gonorrhea, endometritis), infections of 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 others, 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 a violation 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 a normal kidney function of 3 mg / kg / day. Multiplicity of administration -2-3 times a day. In / in the 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 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, 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 chosen so 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 respiratory system: bronchospasm.

    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: 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 accelerate, 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:

    It is pharmaceutically incompatible with other drugs (including other aminoglycosides, amphotericin B, heparin, ampicillin, benzylpenicillin, cloxacillin, carbenicillin, capreomycin) (it should not be mixed in one syringe).

    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 nitrate preservatives) increase the risk of nephroxia and respiratory arrest 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 reduced clearance).

    Special instructions:

    Contained. in ampoules of sodium disulfite can cause development in patients with allergic complications, 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 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 fordetermination of 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.

    Effect on the ability to drive transp. cf. and fur:Considering the side effects of the drug, care must be taken when driving vehicles or potentially dangerous mechanisms.
    Form release / dosage:Solution for intravenous and intramuscular injection 40 mg / ml in ampoules of 2 ml.
    Packaging:10 ampoules are placed in a contour mesh package made of a polyvinyl chloride film. 1 circuit cell pack together with the instruction for use is placed in a cardboard box.
    Storage conditions:In a dry, protected from light 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:LS-002216
    Date of registration:19.09.2011
    Expiration Date:Unlimited
    The owner of the registration certificate: Mapichem AG Mapichem AG Switzerland
    Manufacturer: & nbsp
    Representation: & nbspMapichem AGMapichem AG
    Information update date: & nbsp23.03.2017
    Illustrated instructions
      Instructions
      Up