Gentamicin sulfate
Gentamicin sulfate: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. Use in the elderly
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Gentamicin sulfate
ATX code: J01GB03
Active ingredient: gentamicin (gentamicin)
Manufacturer: SHANDONG WEIFANG PHARMACEUTICAL FACTORY, Co. Ltd. (China), JSC Borisov Plant of Medical Preparations (Belarus), Pharmaceutical company DOSFARM (Kazakhstan), CJSC Pharmaceutical Firm Darnitsa (Ukraine)
Description and photo update: 2018-25-10
Gentamicin sulfate is an antibacterial drug with a bactericidal effect from the aminoglycoside group.
Release form and composition
The dosage form of Gentamicin sulfate is a solution for injection: transparent, with a slight yellowish tinge or colorless [in glass ampoules of 2 ml, in a plastic cell package 5 or 10 ampoules or in a cardboard box 1 pack of 10 ampoules or 2 packs of 5 ampoules (in depending on the manufacturer)].
Composition of 1 ml solution:
- active substance: gentamicin (in the form of gentamicin sulfate) - 40 mg;
- auxiliary substances (depending on the manufacturer): sodium metabisulfite, disodium salt of ethylenediaminetetraacetic acid, water for injection; or anhydrous sodium sulfite and water for injection.
Pharmacological properties
Pharmacodynamics
Gentamicin sulfate is an aminoglycoside antibiotic with a broad spectrum of action. By penetrating the bacterial cell membrane and irreversibly binding to the 30S subunits of bacterial ribosomes, it disrupts the protein synthesis of the pathogen. Gentamicin prevents the formation of a complex of tRNA (transport ribonucleic acid) and mRNA (template ribonucleic acid), therefore, the genetic code is erroneously read from the mRNA and non-functional proteins are formed.
The antibiotic in high concentrations helps to reduce the barrier functions of plasma membranes in the cells of microorganisms, causing their death. This is responsible for the bactericidal effect of gentamicin.
In vitro tests confirm the activity of gentamicin sulfate against the following types of gram-negative and gram-positive microorganisms: Proteus spp. (indolegative and indole positive), Escherichia coli, Salmonella spp., Klebsiella spp., Campylobacter spp., Shigella spp., Staphylococcus spp. (including penicillin- and methicillin-resistant strains), Pseudomonas spp. (including Pseudomonas aeruginosa), Serratia spp., Providencia spp., Citrobacter spp., Acinetobacter spp.
Resistant to gentamicin, as a rule, the following microorganisms: Streptococcus pneumoniae, most other species of streptococci, enterococci, Neisseria meningitides, Treponema pallidum and anaerobic microorganisms such as Clostridium spp., Bacteroides spp., Providencia rettgeri.
Gentamicin in combination with penicillins (including benzylpenicillin, ampicillin, oxacillin, carbenicillin), which affect the cell wall of microorganisms, is active against Enterococcus faecium, Enterococcus faecalis, Enterococcus avium, Enterococcus durans, including almost all strains faecalis zymogenes, Streptococcus faecalis liquefaciens), Streptococcus durans, Streptococcus faecium.
The development of resistance of microorganisms to gentamicin is slow. Strains showing resistance to kanamycin and neomycin, due to incomplete cross-resistance, may be resistant to gentamicin. The antibiotic also does not act on viruses, fungi, protozoa.
After intravenous (intravenous) or intramuscular (intramuscular) administration, therapeutic concentrations of gentamicin in the blood are reached in approximately 0.5–1.5 hours and persist from 8 to 12 hours.
Pharmacokinetics
- absorption: gentamicin is practically not absorbed in the gastrointestinal tract, therefore it is not used for oral administration. After i / m administration, it is absorbed quickly and completely. The time of the onset of the maximum plasma concentration (C max) after i / m administration is 30–90 minutes, after i / v infusion lasting 30 minutes - 30 minutes, after i / v infusion lasting 60 minutes - 15 minutes. The value of C max after i / m or i / v administration of gentamicin sulfate at a dose of 1.5 mg / kg - 6 μg / ml;
- distribution: up to 10% of the substance binds to blood plasma proteins. The volume of distribution (V d) in adult patients is 0.26 l / kg, in children - from 0.2 to 0.4 l / kg, in newborns up to 1 week and weighing less than 1.5 kg - up to 0.68 l / kg, s weighing more than 1.5 kg - up to 0.58 l / kg. Gentamicin in therapeutic concentrations is observed in the kidneys, liver, lungs, urine, synovial, pericardial, pleural, lymphatic, ascitic and peritoneal fluids, in wounds, granulations, pus. In low concentrations, the substance is found in muscles, adipose tissue, breast milk, bile, bones, aqueous humor of the eye, CSF (cerebrospinal fluid), sputum and bronchial secretions. In adults, gentamicin practically does not pass through the BBB (blood-brain barrier) at therapeutic concentrations, but penetrates the placental barrier. With meningitis, its concentration in the CSF increases. In newborns, the concentration of the substance in the CSF is higher,than in adults;
- metabolism: gentamicin is not metabolized in the body;
- elimination: T 1/2 (half-life) in adults - from 2 to 4 hours, in children from 1 week to 6 months - 3-3.5 hours, in newborns and premature babies weighing more than 2 kg - 5.5 hours, with a weight of 1.5 to 2 kg - 8 hours, with a weight of less than 1.5 kg - 11.5 hours. It is excreted mainly by the kidneys unchanged, with bile - in small quantities. With normal kidney function, 70–95% of gentamicin is excreted in the first 24 hours, while urine concentrations above 100 μg / ml are observed. In patients with glomerular filtration disorders, excretion is significantly slowed down.
Gentamicin is excreted during hemodialysis, while its concentration decreases by 50% every 4-6 hours. During peritoneal dialysis, 25% of the dose is excreted in 48-72 hours.
With repeated injections, the active substance accumulates mainly in the proximal segments of the renal tubules and in the lymphatic space of the inner ear.
Indications for use
According to the instructions, Gentamycin sulfate should be used to treat severe systemic infections in cases where the microorganisms that caused the disease are resistant to safer antibiotics.
The drug is indicated for bacterial infections caused by pathogens sensitive to gentamicin:
- infectious and inflammatory diseases of the upper and lower respiratory tract (including pneumonia, bronchitis, lung abscess, pleural empyema);
- sepsis, septic endocarditis;
- infectious diseases of the kidneys and urinary tract (including pyelonephritis, endometritis, prostatitis, urethritis, cystitis, gonorrhea);
- central nervous system infections (including meningitis);
- abdominal infections (peritonitis, pelvioperitonitis);
- infectious diseases of soft tissues and skin, infected burns;
- joint and bone infections (including osteomyelitis).
Contraindications
Absolute:
- severe chronic renal dysfunction with uremia and azotemia;
- acute form of renal failure;
- neuritis of the auditory nerve;
- otitis media, including those transferred earlier;
- diabetes;
- myasthenia gravis;
- joint therapy with loop diuretics, as well as with other ototoxic and nephrotoxic drugs;
- pregnancy, lactation period;
- increased individual sensitivity to gentamicin or other aminoglycosides (including a history).
Relative (diseases / conditions in which the use of Gentamicin sulfate requires caution):
- botulism, parkinsonism (aminoglycoside antibiotics can lead to impaired neuromuscular conduction and further weakening of skeletal muscles);
- dehydration;
- prematurity of children and the neonatal period;
- elderly age.
Instructions for the use of Gentamicin sulfate: method and dosage
Gentamicin sulfate is administered intramuscularly or intravenously.
For intravenous infusion, the dose of the drug is diluted with a solvent (sterile saline or 5% glucose solution). For adults, the usual volume of solvent is 50–300 ml, for children it should be reduced accordingly. In solution, the concentration of gentamicin should not exceed 0.1% (1 mg / ml). Duration of intravenous infusion of Gentamicin sulfate - 1-2 hours.
The route of administration and dosage regimen of Gentamicin sulfate depend on the patient's condition and the severity of the disease. The dose is calculated depending on the patient's weight.
Due to the fact that gentamicin is distributed in the extracellular fluid and does not accumulate in adipose tissue, in obesity, its dose must be reduced. The dose should be calculated on PMT (actual body weight) if the patient is not overweight [ie, no more than 20% additional to BMI (ideal body weight)]. If overweight is 20% or more to BMI, the dose for this body weight (DMT) is calculated using the formula: DMT = BMI + 0.4 (FMI - BMI).
Recommended dosage regimen:
- for adults and children over 14 years of age: for moderate to severe infections, the usual daily dose of gentamicin is 3 mg / kg body weight, divided into 2-3 injections. The maximum daily dose is 5 mg / kg, divided into 3-4 injections;
- for children: up to 3 years old Gentamicin sulfate is prescribed exclusively for health reasons. The daily dose for newborns and infants is 2-5 mg / kg, for children from 1 to 5 years old - 1.5-3 mg / kg, for children from 6 to 14 years old - 3 mg / kg. The maximum daily dose for children of all age groups is 5 mg / kg. The drug is administered 2-3 times a day. In all children, regardless of age, it is recommended to check the concentration of gentamicin in serum daily (1 hour after injection, it should be approximately 4 μg / ml);
- for patients with impaired renal function: the dosage regimen should be selected so that it provides the therapeutic adequacy of the antibiotic. Before starting and during the entire period of treatment, it is necessary to control the serum concentration of gentamicin. The initial single dose for patients with stable chronic renal failure is 1–1.5 mg / kg. In 30-60 minutes after i / m administration, the concentration of the drug in the blood serum should be 5-10 mcg / ml. In the future, the dose and the interval between injections are determined depending on the CC (creatinine clearance).
The usual duration of the course of therapy with Gentamicin sulfate for all patients is from 7 to 10 days. If necessary, in the case of severe and complicated infectious diseases, the course of treatment can be extended. Since the toxicity of the antibiotic appears after 10 days of its use, it is recommended to control the functioning of the kidneys, vestibular apparatus and hearing with a longer course of therapy.
If dialysis is necessary, adult patients with infectious diseases are prescribed 1–1.5 mg / kg of gentamicin at the end of each procedure.
Side effects
The following side effects from systems and organs are possible when using Gentamicin sulfate:
- digestive system: nausea / vomiting, hyperbilirubinemia, increased enzymatic activity of hepatic transaminases;
- hematopoietic organs: leukopenia, anemia, thrombocytopenia, granulocytopenia;
- nervous system: paresthesias, muscle twitching, drowsiness, headache, convulsions, epileptic seizures, numbness, psychosis (in children);
- urinary system: due to nephrotoxicity - renal dysfunction (microhematuria, proteinuria, oliguria); rarely - OTN (acute tubular necrosis);
- organs of hearing and vestibular apparatus: due to ototoxicity - hearing loss, tinnitus, irreversible deafness, labyrinth and vestibular disorders;
- allergic reactions: itching, skin rash, fever, eosinophilia, angioedema;
- laboratory tests: in children - hypokalemia, hypocalcemia, hypomagnesemia; very rarely - an increase in the number of reticulocytes;
- others: development of superinfection, fever; very rarely - loss of appetite, increased salivation, weight loss, pain in muscles, joints, laryngeal edema, hypotension, respiratory depression, blockade of neuromuscular transmission;
- reactions at the injection site: with intramuscular injection - soreness, hyperemia, skin tightening, atrophy / necrosis of subcutaneous tissue; with intravenous infusion - the development of phlebitis and periphlebitis.
Overdose
In case of administration of high doses of Gentamicin sulfate, the following symptoms may appear: nausea / vomiting, ototoxic and nephrotoxic manifestations, impaired neuromuscular transmission (respiratory arrest).
In case of an overdose of the drug, it is recommended for adults to intravenously administer anticholinesterase drugs (for example, proserin), as well as calcium preparations (10% calcium chloride - 5-10 ml, 10% calcium gluconate - 5-10 ml). Before the introduction of neostigmine methyl sulfate (proserin), 0.5–0.7 mg of atropine is injected intravenously, 1.5–2 minutes after the heart rate increases, 1.5 mg (0.05% solution - 3 ml) proserin. In case of insufficient effect of this dose, the same dose of neostigmine methyl sulfate is administered again (with the development of bradycardia, an injection of atropine is additionally made).
Children with an overdose of gentamicin should receive calcium supplements. In cases of respiratory failure, mechanical ventilation is required (artificial ventilation of the lungs).
Gentamicin sulfate can be eliminated by hemodialysis and peritoneal dialysis. Hemodialysis is more effective.
special instructions
Since Gentamicin sulfate has a wide spectrum of action, it can be used for mixed infections, as well as in cases where the causative agent of the infection has not been identified, as a rule, in combination with semi-synthetic penicillins (carbenicillin, ampicillin).
Gentamicin therapy can only be carried out for medical purposes and under strict clinical supervision due to the potential toxicity of the drug.
During the entire period of treatment, it is necessary to regularly monitor the concentration of the antibiotic in the blood plasma to ensure adequate therapy and to avoid toxic levels of the drug in the blood.
During therapy, a sufficient amount of liquid should be consumed.
When using Gentamicin sulfate, it is necessary to check the functioning of the kidneys 1 or 2 times a week, and in patients on treatment for more than 10 days or receiving high doses of patients - daily. To avoid the ototoxic effect of the antibiotic, it is recommended to examine the vestibular function 1 or 2 times a week and to determine the hearing loss at high frequencies.
In some cases, hearing impairment occurred after the end of treatment.
If you experience symptoms such as ringing or tinnitus, a feeling of any degree of hearing loss, impaired coordination of movements, dizziness, tingling of the skin, numbness, muscle cramps, twitching, at any time during the entire period of treatment, you must inform your doctor about this, so how symptoms may indicate the manifestation of neurological adverse reactions.
The development of impaired renal function, damage to the hearing or vestibular apparatus requires the abolition of Gentamicin sulfate and only in exceptional cases - correction of the antibiotic dose.
Gentamicin sulfate should be taken with caution in hypocalcemia, dehydration, reduced renal function, obesity. It is not recommended (due to the lack of clinical experience) to administer the entire daily dose of the drug to patients with cystofibrosis, ascites, endocarditis, sepsis, burns with an area of more than 20%, chronic renal failure during hemodialysis. Rapid administration of an antibiotic may initially lead to an increase in gentamicin concentration to neurotoxic levels. It is important to administer the daily dose of the drug at the recommended time intervals.
Among the antibiotics of the aminoglycoside group, cross-hypersensitivity is likely.
Antibiotic resistance may develop against the background of gentamicin therapy. In such cases, gentamicin sulfate should be discontinued and the sensitivity of microorganisms should be investigated.
Influence on the ability to drive vehicles and complex mechanisms
You should refrain from driving and all types of activities that require increased attention and rapid motor / mental reactions, since Gentamicin sulfate affects the speed of neuromuscular transmission.
Application during pregnancy and lactation
The drug is contraindicated for use during pregnancy, since gentamicin crosses the placental barrier and may have a nephrotoxic effect on the fetus.
Gentamicin sulfate tends to penetrate into breast milk, therefore, if it is necessary to use it in a woman during lactation, breastfeeding should be stopped.
Pediatric use
The use of Gentamicin sulfate in children is possible according to the dosage regimen.
With impaired renal function
In patients with severe chronic impairment of renal function with uremia and azotemia, as well as in patients with acute renal failure, the use of the drug is contraindicated.
The risk of developing nephrotoxic side effects with gentamicin treatment is increased in the case of impaired renal function. Therefore, before starting and during the entire course of therapy, it is necessary to control the concentration of gentamicin in the blood, as well as to check the kidney function.
Apply Gentamicin sulfate in renal failure according to the dosage regimen.
Use in the elderly
Prescribing the drug to elderly patients requires caution.
Drug interactions
It should be borne in mind that gentamicin has pharmaceutical incompatibility (it cannot be mixed in one syringe) with other drugs (including other aminoglycosides, heparin, amphotericin B, ampicillin, cloxacillin, benzylpenicillin, capreomycin, carbenicillin).
The use of gentamicin concurrently with some drugs can lead to the development of the following effects:
- curariform drugs: enhancement of their muscle relaxant action;
- methoxyflurane, polymyxins for parenteral administration and other drugs that block neuromuscular conduction (narcotic analgesics, halogenated hydrocarbons with inhalation anesthesia, transfusion of large portions of blood with citrate preservatives): increased risk of nephrotoxic effect and respiratory arrest (due to aggravation of neuromuscular blockade);
- anti-myasthenic drugs: reducing their effect;
- loop diuretics: increased otoxicity and nephrotoxicity (due to a decrease in the tubular secretion of gentamicin);
- antibiotics of the penicillin series (carbenicillin, ampicillin): increased antimicrobial action due to the expansion of the spectrum of activity;
- indomethacin (parenteral administration): increased risk of developing the toxic effects of gentamicin (due to an increase in T 1/2 of the drug and a decrease in clearance);
- cisplatin and other oto- and nephrotoxic drugs: increased toxicity;
- streptomycin, tobramycin, kanamycin, neomycin, polymyxin B, biomycin, paromomycin, cephaloridin, vancomycin, amikacin, colistin and other neuro- or nephrotoxic antibiotics: their combined use with gentamicin should be avoided;
- amphotericin B, cyclosporine, foscarnet, methoxyflurane, piperacillin, clindamycin, radiocontrast agents for intravenous administration, cisplatin: increased risk of renal dysfunction, vestibular and hearing aids.
Analogs
Analogues of Gentamicin sulfate are: Gentamicin, Gentamicin-K, Gentamicin-Ferein.
Terms and conditions of storage
Store in a dark place at a temperature not exceeding 25 ° C.
Keep out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Gentamicin sulfate
In reviews of Gentamicin sulfate, users note that this is a very strong drug in terms of its effect on almost all common infectious diseases. Its use in the dosage regimen recommended by the instruction guarantees a positive result of therapy. However, side effects can be quite serious, therefore medical supervision and regular appropriate laboratory tests are necessary.
Price for Gentamicin sulfate in pharmacies
The average price for Gentamicin sulfate is approximately 33 rubles per pack of 10 ampoules.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
