What Is Gentamicin I?
Gentamicin is one of the few thermostable antibiotics, and is therefore widely used in media configuration. China has independently developed a broad-spectrum antibiotic, which is one of the great scientific and technological achievements since the founding of New China. It started development in 1967 and was successfully identified at the end of 1969. It was named "gentamicin", meaning to celebrate the "Nineth Congress" and to celebrate the greatness of the working class. Gentamicin [gentamycin] is obtained from the fermentation broth of Actinomycetes monosporum. It is a basic compound and is a commonly used aminoglycoside antibiotic. It is mainly used to treat bacterial infections, especially those caused by Gram-negative bacteria. Gentamicin can bind to the 30s subunit of bacterial ribosomes and block bacterial protein synthesis.
- Drug Name
- Gentamicin
- Foreign name
- Gentamicin
- Whether prescription drugs
- prescription
- Main indications
- Treating bacterial infections
- Main medication contraindications
- For people with renal insufficiency or long-term medication
- Whether to include health insurance
- Incorporate
- Gentamicin is one of the few thermostable antibiotics, and is therefore widely used in media configuration. China has independently developed a broad-spectrum antibiotic, which is one of the great scientific and technological achievements since the founding of New China. It started development in 1967 and was successfully identified at the end of 1969. It was named "gentamicin", meaning to celebrate the "Nineth Congress" and to celebrate the greatness of the working class. Gentamicin [gentamycin] is obtained from the fermentation broth of Actinomycetes monosporum. It is a basic compound and is a commonly used aminoglycoside antibiotic. It is mainly used to treat bacterial infections, especially those caused by Gram-negative bacteria. Gentamicin can bind to the 30s subunit of bacterial ribosomes and block bacterial protein synthesis.
Introduction to Gentamicin Compounds
Gentamicin Basic Information
- Chinese name gentamicin
- Chinese alias: Zhengtaimycin; Baole; Pediatric Libao; Gentamycin; Qingda
- English name: Gentamicin
- English alias: GENTAMYCINE; Gentavet; Gentacycol; Ampullen; Cidomycin; Genmycin; Gentalin
- CAS number: 1403-66-3
- Molecular formula: C 60 H1 23 N 15 O 21
- Molecular weight: 1390.71000
- Exact mass: 1389.90000 PSA: 627.17000
Physiochemical Properties of Gentamicin
- Appearance and properties: transparent amber liquid
- Density: 1.3 g / cm 3
- Boiling point: 669.4ºC at 760 mmHg
- Flash point: 358.6ºC
- Vapor pressure: 8.85E-21mmHg at 25 ° C
Gentamicin Safety Information
- Customs Code: 3004909090
- China Customs Code: 3004909090 [1]
History of Gentamicin Discovery
- Wang Yue, Ru Mingzhong Wu, was born in Minhou County, Fujian Province (now Fuzhou City), Fujian Province. He was born in August 1915 at Tongming Lane, Shangdu. Business in the last century, opened Wang Dasheng smoke shop, has a history of more than 200 years. His father, Lulu, was a scholar in the late Qing Dynasty, known for his writings and calligraphy. He was a well-known literati in Fuzhou. He participated in the 1911 Revolution in his early years and served as the secretary of the Provincial Construction Department and the Finance Department after his recovery. Wang Yueyou was taught by his father, with integrity and sincerity, being sincere, hard-working, and aggressive. He was 12 years old (1927) studying at Fuzhou Yinghua Middle School, and transferred to Fuzhou Trinity Middle School in 1929. He studied hard and ranked among the best.
- In August 1941, he was recommended by the US Ambassador to China, Stuart, to go to graduate school at Rutgers University in New Jersey, USA. Under the guidance of Professor Wagsman, a well-known Nobel Prize winner, pioneer in antibiotic research, and discoverer of streptomycin and neomycin, he completed all research topics after three years of hard work and achieved outstanding results in 1943. PhD in Microbiology, received the Golden Key Award from the SIGMX Institute, and was employed as a researcher at the Merck Institute for Chemotherapy in the United States. During his studies in the United States, his instructor, Professor Wagersmann, valued him and advised him to stay in the United States Engaged in microbiological research and provided him with favorable employment and scientific research conditions. However, he believes that despite poverty and backwardness, China is, after all, its own motherland, and it is its responsibility and obligation to return to the motherland and dedicate itself to the development of the scientific cause of the motherland. In particular, driven by the tide of anti-Japanese and national salvation of the overseas Chinese in the United States in September 1943, he returned home with enthusiasm for serving the motherland in 1944.
- From April 1944 to December 1948, he was employed as a technician at the Central Health Laboratory. In 1947, he published a series of discussions on the changes in the process of biogas production from faeces under anaerobic conditions, the first of its kind in China. He also published academic papers introducing various new antibiotics, hoping to promote and conduct experiments to develop the antibiotics industry in China. However, his enthusiasm did not get the attention of the government at the time, and he failed to provide the necessary research conditions, which disappointed him. As early as a student, he was concerned about sanitation in rural China and began to systematically study the scientific treatment of rural feces in China. Later, in addition to teaching, he often conducted in-depth investigations and studies in rural areas; after studying abroad, he continued to conduct research on rural health and agricultural development, and put forward many suggestions and opinions. In 1947, he first published a series of studies on the chemical changes in the process of manure producing biogas under anaerobic conditions, the first of its kind in China. However, the Kuomintang authorities did not pay much attention to his research results, and his ideals and ambitions of saving the country through science were lost. He lamented that his ten-year cold window eventually "did nothing."
- In January 1949, he was hired as a researcher at the Fujian Research Institute, and in March he was transferred to the professor and dean of the Department of Chemistry of Xiehe University. In April 1950, he served as a professor at Fujian Normal University, and later served as the director of the Microbiology Laboratory of the East China Institute of Subtropical Botany, Chinese Academy of Sciences. In the early days of liberation, imperialism imposed a comprehensive blockade on China, using antibiotics as combat preparation materials, and imposing an embargo on China. At that time was the golden age of antibiotic research and production in various countries in the world, but there was an extreme shortage of antibiotic drugs in China. At this critical moment, Wang Yue felt that he had a responsibility to share the concerns for the country and the people, and determined to fill the gap in the motherland s medicine.
- With the support and help of the party and the people's government, in 1953 he pioneered the antibiotic laboratory under the rudimentary conditions of the Fujian Normal University and began research on screening antibiotics. In 1954, he was employed as a researcher and director of the Microbiology Laboratory of the Chinese Academy of Sciences. In the early days, he overcame all kinds of difficulties because of simplification, and insisted on using medical antibiotics as a long-term research direction. After hard work, I finally found the actinomycetin "23-21" producing bacteria with a certain curative effect on cancer from Streptomyces, and extracted the crystalline samples, and then made a detailed analysis at the first national antibiotic academic conference. Report. His discovery found the first antibiotic drug for China and immediately went into production. He attached importance to identifying research projects based on actual conditions, and worked hard to develop new areas of antimicrobial research. In 1965, he first proposed a research field to find new antibiotics from Micromonas in China.
- In 1966, he and his assistant isolated a well-known gentamicin-producing bacterium from Micromonas and officially put it into production on the 20th anniversary of the founding of the People's Republic of China in 1969. According to statistics, from the start of production to 1985, there were 40 factories in the country with an output of 868 tons and an output value of more than 1 billion yuan. The discovery of gentamicin has pushed the research and production of antibiotics in China to a new stage and made a significant contribution to the Chinese medical community.
- He was persecuted during the Cultural Revolution. In the face of adversity, he still couldn't shake his loyalty to the motherland. He said, "I deeply understand that Marxism itself is a great science, and Marxists believe in science the most." "Thirty years of scientific research practice has proved that scientific research must be led by the party. Only in accordance with the party's guidelines and policies, scientific research, combined with the needs of the country and the people, will not lose direction in scientific research." Therefore, he is still diligently translating his works in the predicament, grasping the dynamics and development trends of microbial research at home and abroad. After smashing the Jiang Qing Counter-Revolutionary Group, the Fujian Provincial Party Committee and the Provincial Government of the Communist Party of China invited him to work. He proposed a strategic idea for studying new areas of microbiology, and translated and published more than 200,000 words of "Physic Chemistry of Biologists". Highly appraised by the industry.
- In 1978, he participated in the review of the book "Physicochemical Properties of Antibiotics" and the research results of gentamicin won the National Science Congress Award. On October 11, he was elected to the Central Committee of the Revolutionary Committee. In January 1979, he was elected to the Standing Committee of the Fifth Fujian Provincial Committee of the Revolutionary Committee, and shortly after, he was elected to the CPPCC National Committee. After the Third Plenary Session of the Eleventh Central Committee of the Party, Wang Yue was in a good mood and invigorated. He became the first director of the Fujian Institute of Microbiology and concurrently a professor of Fujian Normal University and Huaqiao University. He is also a member of the Fujian Provincial Society of Microbiology and the Chairman of the Provincial Microbiology Society.
- Wang Yue is engaged in both scientific research and teaching. Under his leadership, the Fujian Institute of Microbiology has continuously created a new situation in scientific research. He firmly believes that "scientific research must be reformed before there is a way out", he often goes to relevant factories inside and outside the province, finds scientific research topics in production practice, puts forward reform opinions, and signed more than 30 technical collaboration projects. He also trains graduate students and advanced students, teaches them according to their aptitude, focuses on cultivating students' professionalism in scientific research, and stimulates their creativity. He is rigorous in his studies and attaches importance to the continuous updating of knowledge. Under his careful teaching and careful guidance, many students have become the backbone of domestic scientific research, teaching and construction.
- In 1980, Wang Yue and his assistants successfully prepared the single-component national standards of the gentamicin group C. In 1981, he first advocated and organized the scientific research work of dry fermentation to produce biogas in China, and achieved great achievements, which has now become a new process widely used in rural areas in northern China. In 1982, he led the Institute of Microbiology to isolate a new aminosugar antibiotic with higher efficacy and safety against infection from Micromonospora, which are the bacteria producing perillomycin and Wuyimycin. At the same time, he also proposed the idea of opening up a new field of enzyme inhibitor physiologically active substances research, and organized implementation soon. That year, he attended the thirteenth annual meeting of the International Society of Microbiology in the United States, visited the American Space Research Center, scientific research institutions, universities, pharmaceutical factories, etc., signed an agreement on academic exchanges and the selection of graduate students, and brought back many valuable Information and samples. He also made a report on his research work and achievements on the forum of the Wagsman Institute of the International Center for Microbiology Research, which shocked American scientists. His alma mater, Rutgers University, awarded him the "R" medal. That year he was named a model worker in Fujian Province.
- In 1983, Wang Yue and his assistants found a new type of immunosuppressant, cyclosporin-producing bacteria for organ transplantation, and later found several pepsin inhibitor-producing bacteria. These new discoveries caused national medicine The strong response from the industry has greatly promoted the development of basic research in organ transplantation and immunology in China, pushed the research on antibiotics in China to a new field, and had a profound impact. In January 1955, the Fujian Provincial Political Consultative Conference held the first session of the committee. As a member of the scientific and technological circles, he attended the meeting. In 1959 and 1964, he was elected as a member of the second and third provincial CPPCC and actively participated in the negotiation of major issues of the party and state. In October 1983, he was elected to the Standing Committee of the Sixth Central Committee of the Revolutionary Committee. In June 1984, he was elected as Vice Chairman of the Fujian Provincial Committee of the Revolutionary Committee. In November of the following year, he attended the "Double First" Congress of the Democratic Parties serving the four modernizations in the province and made a typical speech at the meeting. Just this year, he found himself suffering from advanced gastric cancer. He believed that birth, old age, sickness, and death were objective laws. He put forward the motto of "exhausting, struggling" and took time to do more work. More than a month after the operation in the hospital, he went to the institute to listen to the work report, revise the work summary, and formulate a work plan, showing a tenacious spirit.
- In 1985, he was recommended by the National Revolutionary Committee to attend the National "Recognition Conference for Advanced Collectives and Advanced Individuals of the Four Democratic Parties and the Federation of Industry and Commerce for the Service of the Four Modernizations." He died in Fuzhou on September 7 at the age of 70.
- He has published more than 60 (department) scientific research articles and translations, and edited the book "Antibiotics". He is enthusiastic in assisting local research in production issues related to microbial fermentation. In order to commemorate his contribution to the cause of microbiology, Fujian Institute of Microbiology selected 67 papers and published "Professor Wang Yue's Thesis".
Gentamicin Drug Description
Gentamicin Classification
- Antibiotics> Aminoglycosides
Gentamicin dosage form
- 1. Tablet: 20mg, 40mg;
- 2. Injection: 20mg (1ml), 40mg (1ml), 80mg (1ml);
- 3. Sustained-release tablets 40mg;
- 4. Granules: 10mg, 40mg;
- 5. Eye drops: 40,000 U (8ml).
Gentamicin pharmacological action
- Gentamicin is an aminoglycoside. Its mechanism of action is to act on ribosomes in bacteria, inhibit bacterial protein synthesis, and destroy the integrity of bacterial cell membranes. Gentamicin can first pass through the outer membrane porin through passive diffusion, and then enter the cell through the cell membrane through the transport system. It does not reversibly bind to the isolated ribosomal 30S subunit, leading to the destruction of the A site, and further:
- 1. Prevent the correct localization of ammonia tRNA at the A position, especially prevent the binding of methionyl tRNA, thus interfere with the assembly of functional ribosomes and inhibit the formation of 70S initiation complexes.
- 2. Induced mismatch of tRNA and mRNA code triplet, causing the 30S subunit of the complete ribosome to misread the genetic code, causing the wrong amino acid to be inserted into the protein structure, leading to abnormal, nonfunctional protein synthesis.
- 3. Blocking the termination factor from binding to the A site, preventing the synthesized peptide from being released, and preventing the 70S intact ribosome from dissociating.
- 4. Impede the depolymerization and assembly process of polyribosomes, resulting in depletion of ribosomes in bacteria. Gentamycin against Pseudomonas aeruginosa, Proteus (indole positive and negative), E. coli, Klebsiella, Enterobacteria, Serratia, Shigella, Citrobacter , Neisseria, Staphylococcus aureus (excluding methicillin-resistant strains) have strong antibacterial activity. Gentamicin is not effective against Streptococcus (including Streptococcus pyogenes, Pneumococcus, Streptococcus faecalis, etc.), anaerobic bacteria (Bacteroides), Mycobacterium tuberculosis, Rickettsia, viruses and fungi.
Gentamicin pharmacokinetics
- Absorption is rapid and complete after intramuscular injection. After local rinsing or topical application, a certain amount can also be absorbed through the body surface. After absorption, it is mainly distributed in extracellular fluid, of which 5 to 15% is redistributed into tissues, accumulated in renal cortical cells, and the product can pass through the placenta. The distribution volume is 0.2 to 0.25 L / kg (0.06 to 0.63 L / kg). High drug concentration in urine. Bronchial secretions, cerebrospinal fluid, subarachnoid space, ocular tissues, and aqueous humor are low. Low or very low protein binding. Peak blood concentration reaches 30 to 60 minutes after intramuscular injection or intravenous infusion. The peak blood concentration (g / ml) in adults after intramuscular injection is generally 4 times the intramuscular dose (mg / kg) by body weight. Intravenous After completion, it can reach 4-6 g / ml, and the baby can reach 3-6 g / ml after a single 2.5mg / kg administration. In patients with fever or large-scale burns, the blood concentration may be reduced. T1 / 2 adults are 2 to 3 hours, and those with renal function decline are 40 to 50 hours. T1 / 2 may be shortened in patients with fever, anemia, severe burns, or in combination with carbenicillin; however, there are significant differences among patients with gynecology, surgery, and burns. Pediatric T1 / 2 is 5 to l1.5 hours, and lighter T1 / 2 is longer. The product is not metabolized in the body and is excreted through glomerular filtration. The concentration in urine can exceed 100 g / ml, and it is excreted in 50 to 93% within 24 hours. For neonates within 3 days of birth, 10% are excreted within 12 hours of administration; for neonates 5 to 40 days after birth, 40% are excreted within 12 hours of administration. Hemodialysis and peritoneal dialysis can clear a considerable amount of drug from the blood, and shorten T1 / 2 significantly.
Gentamicin indications
- 1. Suitable for the treatment of neonatal sepsis and sepsis caused by sensitive bacteria.
- 2. Suitable for the treatment of respiratory infections, peritonitis, and biliary infections caused by sensitive bacteria.
- 3. Suitable for the treatment of genitourinary system infections caused by sensitive bacteria (except the initial treatment of simple urinary tract infections).
- 4. Suitable for the treatment of skin and soft tissue infections and burn infections caused by sensitive bacteria.
- 5. Oral can be used for intestinal infection or preparation before colon surgery
- 6. Intramuscular injection with clindamycin or metronidazole can be used to reduce the incidence of infection after colon surgery.
- 7. Intrathecal injection can be used as an adjuvant treatment for severe central nervous system infection (acute suppurative meningitis, ventriculitis) caused by Pseudomonas aeruginosa or staphylococcus.
- 8. Gentamicin can also be used to treat listeriosis.
- 9. Gentamicin eye drops are suitable for conjunctivitis, keratitis, tears caused by coagulase-negative and positive staphylococci, Pseudomonas aeruginosa, Escherichia coli, pneumoniae and other Gram-negative bacteria and gonococci Bursitis, blepharitis, meibomitis, etc.
Gentamicin dosage
- 1. (1) For intestinal infection or preoperative preparation, 80 to 160 mg each time, 3 to 4 times a day. (2) Intramuscular injection: General dose: 80mg (80,000 units) each time, 2 to 3 times a day, with an interval of 8h; or 1 to 1.7mg / kg, once every 8 hours; a total of 7 to 14 days. Simple urinary tract infection: weight less than 60mg, 3mg / kg each time, once a day; weight over 60mg, 160mg each time, once a day; or 1.5mg / kg each time, once every 12 hours. (3) Intravenous infusion: the dose is the same as that of intramuscular injection; each dose is added to 50% to 200ml of 0.9% physiological saline or 5% glucose solution, so that the drug concentration does not exceed 1g / L (base) (equivalent to 0.1% Solution), slowly dripping within 30 to 60 minutes. (4) Intrathecal or intraventricular injection: 4 to 8 mg each time, once every 2 to 3 days. Each dose (concentration: 2g / L) is drawn into a 5ml or 10ml sterile syringe for lumbar puncture. After the cerebrospinal fluid sample is taken for laboratory examination, the syringe with gentamicin Connect the lumbar puncture needle, make a considerable amount of cerebrospinal fluid flow into the syringe, push while pulling, and then slowly inject all the medicinal fluid in the syringe within 3 to 5 minutes, and tilt the lumbar puncture needle slightly upwards, such as cerebrospinal fluid. When purulent and difficult to flow out, gentamicin can also be diluted with saline injection. (5) Dose for renal insufficiency: After the first saturated dose (1 to 2 mg / kg) is given, the maintenance amount for renal insufficiency can be adjusted as follows: Each dose is unchanged (1 to 2 mg / kg), Extend the dosing interval. Dosage interval = patient's serum creatinine value (mg / 100ml) × 8; Do not change the administration interval (administration once every 8 hours), reduce the maintenance dose; the maintenance amount can be calculated as follows: each dose = Patient weight (kg) × conventional dosage (mg / kg) / patient blood creatinine (mg / 100ml). The dosage can also be adjusted according to the creatinine clearance rate of patients: creatinine clearance rate> 100ml per minute, using 100% of the usual amount for adults; creatinine clearance rate of 70-100ml per minute, using 85% of the usual amount for adults; creatinine clearance rate of 55 per minute 70ml, 65% of the usual amount of adult; creatinine clearance of 45 55ml / min, 55% of the usual amount of adult; creatinine clearance of 40 45ml / min, 50% of the amount of adult commonly used; creatinine clearance per minute 35 40ml, using 40% of the usual amount of adults; creatinine clearance rate of 30 35ml per minute, using 35% of the amount commonly used by adults; creatinine clearance rate of 25 30ml per minute, using 30% of the amount commonly used by adults; creatinine clearance rate per 20 to 25 ml per minute, 25% of the usual amount for adults; creatinine clearance of 15 to 20 ml per minute, 20% of the usual amount for adults; creatinine clearance of 10 to 15 ml per minute, 15% of the usual amount for adults; creatinine clearance <10ml per minute, 10% of the usual amount for adults. (6) Dose during dialysis: After hemodialysis, according to the severity of infection, a dose of 1 to 1.7 mg / kg can be replenished according to the weight of the infection.
- 2. Children: (1) Oral administration: for intestinal infection or preoperative preparation, 10 to 15 mg / kg per day, divided into 3 to 4 times. (2) Intramuscular injection: Premature infants or term neonates born within 1 week: 2.5mg / kg each time, once every 12-24 hours for a total of 7-14 days. Newborns or infants over 1 week: 2.5mg / kg each time, once every 12 hours for a total of 7 to 14 days. Children: 2 2.5mg / kg each time, once every 8 hours for 7-12 days. (3) Intravenous infusion: the dose is the same as that of intramuscular injection; each dose is added to 50% to 200ml of 0.9% physiological saline or 5% glucose solution, so that the drug concentration does not exceed 1g / L (base) (equivalent to 0.1% Solution), slowly dripping within 30 to 60 minutes. (4) Intrathecal or intraventricular injection: 1 to 2 mg for infants and children over 3 months, once every 2 to 3 days. (5) Dose during dialysis: After hemodialysis, according to the severity of the infection, children (more than 3 months) should be replenished with a dose of 2 2.5mg / kg once per body weight.
Gentamicin considerations
- (1) Blood concentration should be monitored, especially in newborns, the elderly and patients with renal insufficiency
- Blood drug concentration test
- (2) When the blood concentration cannot be measured, the dose should be adjusted based on the measured creatinine clearance.
- (3) After the first saturation dose (1 to 2 mg / kg) is given, the maintenance amount for patients with renal insufficiency and vestibular function or hearing loss should be reduced as appropriate: the dose is unchanged and the interval between administrations is prolonged; or It is unchanged, each dose is reduced or gentamicin is maintained. The maintenance amount can be calculated according to the following formula: Extend the administration interval (hours), each dose is unchanged (1 ~ 2mg / kg), between administrations Period = Patient's serum creatinine value (mg / 100ml) × 8 or Reduce the maintenance dose, administered every 8 hours: each dose = patient weight (kg) × conventional dose (mg / kg) / patient's blood creatinine value (mg / 100ml). Because gentamicin is not metabolized in the body and is mainly excreted in the urine, patients with impaired renal function may cause drug accumulation to a toxic concentration.
- (4) Patients should be given sufficient water to reduce renal tubular damage.
- (5) Long-term application may lead to excessive growth of drug-resistant bacteria.
- (6) Inhibition of breathing, no intravenous bolus. Ineffective against streptococcal infections. Upper respiratory tract infections caused by streptococci should not be used.
Gentamicin adverse reactions
- (1) It has been reported that gentamicin caused by systemic application combined with intrathecal injection
- Large doses can easily cause edema
- (2) Those who have a higher incidence have hearing loss, tinnitus or ear fullness (ototoxicity), hematuria, a significant decrease in the number of urination or decreased urine output, decreased appetite, extreme thirst (nephrotoxicity), unstable walking, dizziness (Ototoxicity, affecting vestibular; renal toxicity). The lower incidence was dyspnea, drowsiness, and extreme weakness (neuromuscular block or renal toxicity).
- (3) If you have hearing loss, tinnitus, or a feeling of fullness in your ears after you stop taking the drug, you need to be careful. Adverse reactions are similar to kanamycin, and the reaction is lighter when the dosage is small. If the dosage is large, the treatment period is long, and occasionally the intestinal flora is disturbed. Once the drug is stopped, it can return to normal. Leukopenia, hearing and kidney damage Individual cases have skin numbness, dizziness, and tinnitus around the mouth, face, and limbs. Occasionally anaphylactic shock, the main symptoms are respiratory tract obstruction and circulatory disorders, and more than half of the cases died after rescue failure, so some people think that the product is the most serious The adverse reaction is rapid-onset anaphylactic shock. It can cause Romberg's disease (difficult to close eyes, unstable in the dark and when washing the face) poisoning symptoms.
- Large doses can easily cause edema
- Large-dose use may have urinary occlusion, acute renal failure, and neurological symptoms. Allergic reactions may occur in inhalation, asthma. Eye drops may have edema, toxic conjunctivitis. This product can cause respiratory depression, both at home and abroad. The product can occasionally cause multiple neuropathy and toxic encephalopathy. Allergic reactions are rare, and occasionally skin itching and urticaria may occur. Generally, it does not affect the continued application of the drug, and the rash quickly subsides after stopping the drug. This product also causes occasional allergic leukopenia and neutropenia. The product can cause anemia, leukopenia, granulocytopenia, thrombocytopenia, and hypotension. This product can cause nausea, loss of appetite, vomiting, abdominal distension and other symptoms of gastrointestinal tract discomfort. A small number of patients may have liver function changes, such as elevated serum aminotransferases and positive turbidity reactions. There are also cases of double infection.
Gentamicin contraindications
- 1. Those who are allergic to gentamicin or other aminoglycosides;
- 2. Pregnant women (especially during the first 3 months of pregnancy).
Gentamicin Drug Interactions
- See streptomycin sulfate. This product is combined with penicillin G and has a synergistic effect on almost all Streptococcus faecalis and its variants, such as Streptococcus faecium species and Streptococcus perseverance. When this product is combined with Junbeicillin in sufficient amount, it has a synergistic effect on some sensitive strains of Pseudomonas aeruginosa. ). The problem of increased renal toxicity when this product is used in combination with cephalosporins has been reported differently. Authoritative scholars believe that there is no conclusive conclusion, but from clinical experience and related monographs, the combination of the two can cause increased renal toxicity. It is advisable to fully weigh the pros and cons and treat it carefully before selecting it for clinical use. Aminoglycoside interactions:
- (1) Combined with strong diuretics (such as furosemide, itanilic acid, etc.) can strengthen ototoxicity.
- (2) Combined with other ototoxic drugs (such as erythromycin), the possibility of ear poisoning may be strengthened.
- Dextran combined with nephrotoxicity
- (3) Combined application with cephalosporins can increase renal toxicity. Dextran can enhance the renal toxicity of this class of drugs.
- (4) Combined application with muscle relaxants or drugs with such effects (such as diazepam, etc.) can lead to enhanced neuro-muscular blockade. Neostigmine or other anticholinesterase drugs can antagonize neuro-muscular blockade.
- (5) The combined use of this class of drugs and alkaline drugs (such as sodium bicarbonate, aminophylline, etc.) can enhance the antibacterial efficacy, but at the same time, the toxicity is also increased accordingly, so you must be cautious.
- (6) The antibacterial effect of penicillins on certain streptococci can be strengthened by the combination of aminoglycosides. For example, it is currently recognized that streptococcus grass green endocarditis and enterococcal infection can be added with penicillin Mycin (or other aminoglycoside). However, it is not certain whether other bacteria have synergistic effects. There are even reports of treatment failure caused by the combination of two drugs. Therefore, the combination of these two drugs must follow its indications and not be used at will.
Gentamicin substance toxicity
|
|
|
|
|
|
|---|---|---|---|---|---|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
2. Behavioral toxicity-convulsions or seizure thresholds affected 3. Behavioral toxicity-ataxia |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
2. Behavioral toxicity-ataxia 3. Lung, chest or respiratory toxicity-irritating the respiratory tract |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
2. Kidney, ureter and bladder toxicity-changes in urine components 3. Hematological toxicity-changes in serum components (such as TP, bilirubin, cholesterol) |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
2. Kidney, ureter and bladder toxicity-increased urine output 3. Kidney, ureter and bladder toxicity-changes in bladder weight |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
2. Biochemical toxicity-Inhibition or induction of dehydrogenase 3. Biochemical toxicity-Inhibition or induction of other enzymes |
|
|
|
|
|
2. Kidney, ureter and bladder toxicity-other changes 3. Hematological toxicity-other changes |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
2. Kidney, ureter and bladder toxicity-changes in bladder weight 3. Chronic disease-related toxicity-death |
|
|
|
|
|
|
|
|
|
|
|
3. Chronic disease-related toxicity-death |
|
|
|
|
|
2. Kidney, ureter and bladder toxicity-changes in bladder weight 3. Hematological toxicity-changes in serum composition (eg TP, bilirubin, cholesterol) |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
2. Kidney, ureter and bladder toxicity-changes in urine components 3. Biochemical toxicity-inhibition or induction of enzymes |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| ||
|
|
|
| ||
|
|
|
| ||
|
|
|
| ||
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
Gentamicin poisoning
- Gentamicin resistance to bacteria is severe, limiting its application. The drug is poorly absorbed orally, and is absorbed quickly and completely by intramuscular and intravenous drip administration, rarely binding to plasma proteins, and has a half-life of 2 to 3 hours. Clinically, it is often combined with piperacillin and other semi-synthetic penicillins or cephalosporins to treat severe Gram-negative bacterial infections. The effective therapeutic concentration range is from 4 to 10 g / ml, and the blood concentration of poisoning persists> 12 g / ml. Elevated blood concentration can easily induce ototoxicity. In the application, the toxicity to the 8th neurons and kidneys was mainly analyzed. Clinical analysis of 3370 cases showed that renal toxicity occurred in about 4.1% and ototoxicity was 2.3%. The maximum dose on the 1st day was 5 mg / kg, given in two divided doses.
- Clinical manifestation
- 1. Common adverse reactions include nausea, vomiting, loss of appetite, abdominal distension and other gastrointestinal discomforts. A few patients have liver function changes and cause double infection.
- 2. Renal toxicity is manifested as non-oliguria kidney injury or oliguria with acute renal failure, the former manifested as polyuria, hematuria, proteinuria, etc. Individuals with severe kidney damage can die from uremia.
- 3. Ototoxicity manifests as dizziness, dizziness, tinnitus, ataxia, etc. Sometimes nystagmus can be seen, in severe cases can not walk, can not afford bed, can progress to deafness.
- 4. This drug causes rare allergic reactions, occasionally skin itching, urticaria, occasionally leukopenia, neutropenia, and anaphylactic shock.
- 5. This medicine can cause neuromuscular transmission function to be inhibited and cause respiratory depression. Occasionally, there are multiple neuropathy and toxic encephalopathy, such as psychiatric symptoms and epileptic seizures.
- treatment
- The main points of treatment for gentamicin poisoning are:
- 1. Symptomatic and supportive treatment is mainly used when overdose or poisoning, such as the treatment of uremia and epilepsy.
- 2. Hemodialysis or peritoneal dialysis can effectively clear gentamicin.
- 3. When early kidney damage occurs, discontinue the drug in time. Most kidney damage is reversible. If oliguria and renal insufficiency occur, the drug should be discontinued in time. After about 10 days, the patient has a polyuria, and the recovery of renal function takes several weeks to several months.
- 4. Early detection of ototoxic symptoms, timely withdrawal can be recovered, and generally no longer exacerbated.
- 5. Immediately discontinue the medication when an allergic reaction occurs and treat it accordingly [51] .
Gentamicin Expert Review
- Gentamicin is a multi-component mixture produced by Micromonas and is one of the main antibiotics currently used in clinical resistance to various gram-negative bacteria infections. Due to the wide application of gentamicin, there are now a certain number of Drug-resistant strains exist. Clinically used for systemic or local infections caused by Gram-negative bacteria such as E. coli, dysentery, Klebsiella pneumoniae, Proteus, Pseudomonas aeruginosa [52] .