Gentamicin sulfate is an aminoglycoside broad-spectrum antibiotic, which has antibacterial and bactericidal effects on a variety of gram-negative and positive bacteria. It has a strong effect on Gram-negative bacteria such as Pseudomonas aeruginosa, Aerobacter, Pneumoniae, Salmonella, Escherichia coli and Proteus, and Staphylococcus aureus.
BALLYA provides a gentamicin test to tell you if there are gentamicin residues in dairy products you eat every day.
2. Pharmacology and Toxicology
This product is an aminoglycoside antibiotic. It has a good antibacterial effect on various gram-negative bacteria and gram-positive bacteria. It has good antibacterial effects on various Enterobacteriaceae such as Escherichia coli, Klebsiella, Proteus, Salmonella, Shigella, Enterobacter, Serratia, and Pseudomonas aeruginosa.
Neisseria and Haemophilus influenzae are moderately sensitive to this product. It also has a certain effect on Brucella, Yersinia pestis, Acinetobacter and Campylobacter fetus. It has a good antibacterial effect on about 80% of methicillin-sensitive strains in Staphylococcus (including Staphylococcus aureus and coagulase-negative Staphylococcus), but most of the methicillin-resistant strains are resistant to this product.
The effect on Streptococcus and Streptococcus pneumoniae is poor, and most of the Enterococcus is resistant to the product. When this product is used in combination with β-lactams, most of them can obtain synergistic antibacterial effects.
The mechanism of action of this product is to combine with the 30S subunit of the bacterial ribosome to inhibit bacterial protein synthesis. In recent years, the number of gram-negative bacilli resistant to gentamicin has increased significantly.
After intramuscular injection, the product is absorbed rapidly and completely, reaching peak plasma concentration (Cmax) within 0.5 to 1 hour. The blood elimination half-life (t1/2b) is about 2 to 3 hours, and it can be significantly prolonged in patients with reduced renal function. The protein binding rate is low.
It can be distributed in various tissues and body fluids in the body, accumulate in renal cortex cells, and can also enter the fetus through the placental barrier, but cannot easily enter the brain tissue and cerebrospinal fluid through the blood-cerebrospinal fluid barrier. It is not metabolized in the body, and is excreted in urine as a prototype through glomerular filtration, and excretes 50% to 93% of the dose within 24 hours after administration.
Hemodialysis and peritoneal dialysis can remove a considerable amount of medicine from the blood and significantly shorten the half-life.
What is gentamicin sulfate used for?
The mechanism of action of this product is to firmly bind to the specific protein on the bacterial riboprotein body subunit, interfere with the function of the riboprotein body, prevent protein synthesis, and cause the error of the code on the translation messenger ribonucleic acid (mRNA) to synthesize non-functional protein.
It is clinically used for sepsis, respiratory tract infection, biliary tract infection, purulent peritonitis, intracranial infection, urinary tract caused by Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, Shigella, Klebsiella, Proteus and other sensitive bacteria Diseases such as infection and dysentery.
It is suitable for the treatment of serious infections caused by sensitive gram-negative bacilli, such as Escherichia coli, Klebsiella, Enterobacter, Proteus, Serratia, Pseudomonas aeruginosa and Staphylococcus methicillin sensitive strains, such as sepsis, lower respiratory tract infection, intestinal infection, pelvic infection, abdominal cavity infection, skin and soft tissue infection, complicated urinary tract infection, etc. The treatment of abdominal infection and pelvic infection should be combined with anti-anaerobic drugs, and gentamicin and other antibacterial drugs are often used in clinical practice. Penicillin (or ampicillin) with gentamicin sulfate can treat Enterococcus infections.
For central nervous system infections caused by sensitive bacteria, such as meningitis and ventriculitis, intrathecal injection of this product can be used as an adjuvant treatment.
3. Usage and Dosage
Adult intramuscular injection or intravenous drip after dilution, 80 mg (80,000 units) once, or 1～1.7 mg/kg according to body weight once, once every 8 hours; or once 5 mg/kg, once every 24 hours. The course of treatment is 7 to 14 days. During intravenous infusion, add a dose of 50～200ml of 0.9% sodium chloride injection or 5% glucose injection. The amount of liquid added during intravenous infusion once a day should not be less than 300ml so that the concentration of the drug solution does not exceed 0.1 %, the solution should be instilled slowly within 30 to 60 minutes to avoid neuromuscular blockade.
Pediatric intramuscular injection or intravenous drip after dilution, 2.5 mg/kg once, once every 12 hours; or 1.7 mg/kg once, once every 8 hours. The course of treatment is 7 to 14 days, during which the blood concentration should be monitored as much as possible, especially for newborns or infants.
Intrathecal and intracerebroventricular administration doses are 4-8 mg once for adults, and 1-2 mg once for children (over 3 months), once every 2 to 3 days. During injection, dilute the drug solution to a concentration of not more than 0.2%, and pump it into a 5ml or 10ml sterile syringe. After lumbar puncture, first make a considerable amount of cerebrospinal fluid flow into the syringe and push while pumping to remove all the drug slowly inject within 3 to 5 minutes.
Dosage for patients with impaired renal function: once every 8 hours for patients with normal renal function, a normal dose of 1～1.7 mg/kg, and a creatinine clearance rate of 10～50ml/min, once every 12 hours It is 30 to 70% of the normal dose; when the creatinine clearance rate is less than 10ml/min, 20-30% of the normal dose is given every 24 to 48 hours.
What are the side effects of gentamicin sulfate effects?
1. Gentamicin Sulfate Side Effects
Similar to kanamycin, it has a greater impact on the vestibule of the ear, but less damage to the cochlea. The main manifestations are dizziness and tinnitus. For people with renal insufficiency or children, more attention should be paid to toxic reactions. In severe cases, it can cause hearing loss or even deafness.
Because the product has a blocking effect on the neuromuscular junction, it is not suitable for intravenous injection or high-dose rapid intravenous infusion to prevent respiratory depression. People who are allergic to this product or other aminoglycosides should ban this drug.
2. Adverse Reaction
The medication may cause hearing loss, tinnitus, or ear fullness and other ototoxic reactions. Unsteady walking and dizziness may occur when the vestibular function is affected. Nephrotoxic reactions such as hematuria, significant reduction in the frequency and output of urination, loss of appetite, and extreme thirst may also occur. Those with a lower incidence have dyspnea, lethargy, and weakness due to neuromuscular blockade or nephrotoxicity. Occasionally, skin rash, nausea, vomiting, decreased liver function, leukopenia, neutropenia, anemia, hypotension can be seen.
A few patients may experience ototoxic symptoms such as hearing loss, tinnitus or fullness of the ears after stopping the drug, so attention should be paid.
Systemic administration combined with intrathecal injection may cause leg twitching, skin rash, fever, and body spasm.
The product can pass through the placental barrier and enter the fetal tissue, which may cause fetal hearing damage. Pregnant women should fully weigh the pros and cons before using the product. The product is secreted very little in milk, but usually breastfeeding women should stop breastfeeding during the medication period.
Gentamicin is an aminoglycoside. It should be used with caution in pediatrics, especially for premature infants and newborns. Because their kidney tissue is not fully developed, the half-life of this type of drug is prolonged, and it is easy to accumulate in the body and cause toxic reactions.
The renal function of elderly patients has a certain degree of physiological decline. Even if the measured value of renal function is within the normal range, a small amount of treatment should be used. Elderly patients are more likely to have various toxic reactions after applying this product, and blood drug concentration should be monitored as much as possible during the course of treatment.
Sufficient water should be given to patients to reduce the damage to renal tubules.
Long-term application may lead to overgrowth of resistant bacteria.
Not suitable for subcutaneous injection.
The product has the effect of inhibiting respiration, so intravenous injection is not allowed.
The product should be used with caution in the following situations: patients with dehydration, damage to the cranial nerves, myasthenia gravis or Parkinson's disease and renal impairment.
Cross allergy. Patients who are allergic to an aminoglycoside antibiotic such as streptomycin and amikacin may be allergic to this product.
Routine urine and renal function tests should be performed regularly before and during medication to prevent serious nephrotoxic reactions. If necessary, do audiometry or audiogram, especially high-frequency audiometry and temperature stimulation test, to detect vestibular toxicity.
4. Drug Interactions
Combined use with other aminoglycosides or successive local or systemic applications may increase the possibility of ototoxicity, nephrotoxicity and neuromuscular blockade.
Combined use with neuromuscular blockers can aggravate the neuromuscular blockade, resulting in muscle weakness, respiratory depression and other symptoms.
Combining with capreomycin, cisplatin, ethanilic acid, furosemide, or vancomycin (or norvancomycin), or succcessive local or systemic application, may increase ototoxicity and nephrotoxicity.
Local or systemic combination with cefalotin and cefazolin may increase nephrotoxicity.
Combined use with polymyxin injections or successive local or systemic applications can increase nephrotoxicity and neuromuscular blockade.
Other nephrotoxic and ototoxic drugs should not be used in combination with this product or applied successively, so as not to aggravate nephrotoxicity or ototoxicity.
Aminoglycosides and β lactams (cephalosporins and penicillins) can cause mutual inactivation when mixed. This product must be instilled in separate bottles when combined with the above antibiotics.
Gentamicin sulfate is suitable for a variety of infectious diseases and central nervous system infections, but it has a great impact on hearing and kidneys. Patients must follow the doctor's arrangements when using this drug, especially pregnant women and lactating women.