What Is Kanamycin Resistance?
Kanamycin is an inhibitor of protein biosynthesis that causes misreading of the mRNA code by binding to the 30S ribosome. If an enzyme that destroys kanamycin is produced in bacteria, it can become a resistant strain. Kanamycin-resistant plasmids are often used in molecular cloning as selection or marker genes.
- Chinese name
- Kanamycin
- Foreign name
- Kanamycin
- Species
- Kanamycin hydrochloride and kanamycin sulfate
- Molecular formula
- C18H38N4O15S
- Molecular weight
- 582.58
- CAS No
- 133-92-6
- Nature
- Protein biosynthesis inhibitor
- Use
- Used as a marker gene in molecular cloning
- Kanamycin is an inhibitor of protein biosynthesis that causes misreading of the mRNA code by binding to the 30S ribosome. If an enzyme that destroys kanamycin is produced in bacteria, it can become a resistant strain. Kanamycin-resistant plasmids are often used in molecular cloning as selection or marker genes.
- It can be used for oral and intravenous injections, is effective against a variety of bacterial infections, and is isolated from Streptomyces kanamyceticus .
Kanamycin Basic Information
- Kanamycin hydrochloride and kanamycin sulfate
- Drug name:
- Kanamycin [1]
- English abbreviation: Kana
- English alias KANAMYCIN A; KANAMYCIN BASE; 4))-2-deoxy-y-alpha-d-glucopyranosyl- (; 4,6-diamino-2-hydroxy-1,3-cyclohexane3,6'diamino-3,6 ' -dideoxydi-alpha-d-gluc; 4,6-diamino-2-hydroxy-1,3-cyclohexane3,6'diamino-3,6'-dideoxydi-alpha-d-glucos; d-deoxydi; d-streptamine, o-3-amino-3-deoxy-alpha-d-glucopyranosyl- (1.fwdarw.6) -o- [6-amin; Kanamycin Monosulfate
- Molecular formula: C18H38N4O15S
- Molecular weight: 582.58
- Structural formula: see right
- CAS No .: 133-92-6
- EINECS 200-411-7
- Description Kanamycin sulfate for injection: 0.5g per bottle; 1g.
- Injection (containing kanamycin monosulfate): 500mg (2ml) each.
- Eye drops: 8ml (40mg).
- Compound kanamycin injection: Each contains 360 mg of kanamycin sulfate and 18 mg of trimethoprim (2 ml).
Kanamycin function
- Some strains of E. coli, Klebsiella, Enterobacter, Proteus, Mycobacterium tuberculosis and Staphylococcus aureus are sensitive to this product
- Glomerular filtration metabolizes drugs
- Intramuscular injection of 0.5g, peak blood concentration at about 1 hour, about 20 g / ml, t1 / 2 of about 2.5 hours, plasma protein binding rate is very low, distribution volume (Vd) is 0.26 ± 0.05L / kg, 24 hours after administration Ninety percent of the drug is excreted from the urine in its original form within hours. This product easily penetrates into pleural fluid and ascites. Effective concentrations cannot be achieved in cerebrospinal fluid.
- Orally used to treat intestinal infections caused by sensitive bacteria and used as preparations for intestinal surgery, and has the effect of reducing ammonia production by intestinal bacteria, and has a certain prevention effect on liver coma in patients with cirrhosis and gastrointestinal bleeding.
- Intramuscular injection is used for systemic infections caused by sensitive bacteria, such as pneumonia, sepsis, and urinary tract infections.
- Kanamycin diluted to a certain concentration and sprayed on cotton leaves can be used to identify whether it is Bt transgenic insect-resistant cotton. The leaves are yellow and not resistant to cotton bollworm, and the color is insect-resistant cotton [2]
Kanamycin dosage
- 1. Adults usually use intramuscular injection or intravenous drip, 0.5g once (based on kanamycin, the same below), 1 to 1.2g a day. Or by weight 5mg / kg,
- Creatinine clearance
- 3. Other usages: 0.25% of this product solution can be used to wash the lesions, this product injection can be used for gas-soluble inhalation.
- Creatinine clearance
- (1) Blood concentration should be monitored, especially for neonates, elderly and patients with renal insufficiency. The effective therapeutic concentration range of kanamycin is 15-30 g / ml. It should be avoided that the peak plasma concentration is continuously above 30-35 g / ml and the trough concentration exceeds 5 g / ml.
- (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 (5 to 7.5 mg / kg) is given, the maintenance amount used in patients with renal insufficiency and vestibular function or hearing loss should be reduced, that is, the dose is unchanged, and the interval between administrations is prolonged; or The drug interval is unchanged, and kanamycin is reduced or discontinued with each dose. Its maintenance amount can be calculated as follows:
- Extend the interval between administrations (hours), with each dose unchanged (7.5mg / kg), the interval between administrations = the patient's blood creatinine value (mg / 100ml) × 9
- Reduce the dosage per administration, once every 12 hours: each dosage = patient's blood creatinine clearance (mg / min) × 7.5 (mg / kg) / normal human creatinine clearance (mg / min). Because kanamycin 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 enough water to reduce renal tubular damage.
- (5) Long-term medication may lead to excessive growth of drug-resistant bacteria.
- (6) Preparation of Kanamycin Sulfate Intravenous Infusion Solution: Kanamycin sulfate injection without dilution cannot be directly injected intravenously. Take kanamycin sulfate injection and dilute it with sodium chloride injection or 5% glucose injection; or take kanamycin sulfate for injection and dissolve it with sterilized water for injection first, add 200 1 g of kanamycin 400ml sodium chloride injection or 5% glucose injection or other appropriate sterilized diluent: The solution should be dripped within 30 to 60 minutes after preparation. Pediatric patients should reduce the amount of diluent accordingly. This product is only allowed for intramuscular injection and intravenous drip, not static push.
Kanamycin precautions
- (1) Use with caution in patients with renal insufficiency.
- (2) The toxicity of aminoglycosides is closely related to their blood concentration. In order to prevent the blood concentration from rising suddenly, this product is only for intramuscular injection and intravenous drip. It has a breath-suppressing effect. It cannot be pushed quietly to prevent accidents.
Kanamycin kinetics
- After intramuscular injection, the product is quickly absorbed, and a certain amount of drug can be absorbed from the body surface after local irrigation or topical application. It is mainly distributed in extracellular fluid. The concentration in normal infants' cerebrospinal fluid can reach 10-20% of the plasma concentration of the same period, and when the meninges are inflamed, it can reach 50% of the plasma concentration of the same period. 5 to 15% of the drug is redistributed to various tissues, which can accumulate in renal cortical cells and pass through the placenta. The synovial fluid has a blood concentration of more than 50%, and the concentrations of bronchial secretions, bile and aqueous humor are low. The accumulation of drugs in the pleural fluid is slow, but it can gradually reach a level close to the blood concentration. The distribution volume is 0.26L / kg. After intramuscular injection, the blood concentration reached a peak in 1 to 2 hours, and the concentration in bile reached a peak about 6 hours after intramuscular injection.
- Glomerular filtration metabolizes drugs
- After a single administration of 7.5 mg / kg, the average peak plasma concentration is 22 g / ml, which may be lower in patients with fever or severe burns. The concentration in urine is 10 to 20 times the blood concentration. T1 / 2 adults are 2 to 4 hours, those with impaired renal function are 27 to 80 hours; premature babies are 18 hours, and term newborns are generally 6 to 8.6 hours (inversely proportional to body weight and age at birth). This product is not metabolized in the body and is mainly filtered through the glomerulus. It is excreted in about 50% within 4 hours after administration, and the concentration in urine can reach 800 g / ml. It is excreted in about 80 to 90% within 24 hours. 1%; a small amount can also be excreted in milk, blood and peritoneal dialysis can remove a considerable amount of blood from the blood, thereby greatly reducing the half-life of the drug.
Kanamycin adverse reactions
- Those with higher rates have hearing loss, tinnitus, or fullness in the ears (ototoxicity), hematuria, decreased urination or decreased urine output, decreased appetite, extreme
- Adverse reactions-erythema rash
- Degree of thirst (renal toxicity), erratic walking, dizziness (ototoxicity, affecting vestibular), nausea or vomiting (ototoxicity, affecting vestibular, renal toxicity). Less frequent cases have difficulty breathing, lethargy, or weakness (neuromuscular block, nephrotoxicity). Hearing loss, tinnitus, or fullness in the ears after discontinuation of the drug indicates that ototoxicity may be needed and attention should be paid. May have hearing and kidney damage. Can cause gastrointestinal reactions: nausea, vomiting, loss of appetite, bloating, diarrhea. Occasionally allergic reactions, rashes, heat of medicine, etc. In severe cases, there may be shock death. Neurological symptoms, Myocardial depression, respiratory failure, etc.
Kanamycin allergic reaction
- Drug fever and rash are uncommon, and their incidence is between 1% and 3%; however, eosinophilia is quite common, up to 10%, especially when the course of treatment exceeds 1 week. Anaphylactic shock is occasionally seen. One case of anaphylactic shock caused by kanalomycin perforation due to ulcerative perforation was reported in China. After rescue, the patient switched to gentamicin without adverse reactions.
Kanamycin nervous system
- The most important adverse reaction in the application of this product is to affect the cochlear nerve. The patient's high-frequency hearing is damaged first, and then the hearing loss gradually develops to the ear.
- Cochlear nerve
- According to statistics: the incidence of clinical ototoxicity when treated with kanamycin is about 5%. Ototoxicity is rare in neonates and premature infants after application of kanamycin. It is reported that the commonly used adult dose (15mg / kg / day) often fails to reach effective blood concentrations in children. Therefore, it is advocated that the dosage of children should be increased to each time 10 mg / kg intramuscularly every 8 hours. Nevertheless, kanamycin should be used with caution in children. The cochlear nerve damage caused by this product can continue to develop after discontinuation of the drug. Kanamycin has greater ototoxicity than streptomycin and gentamicin, but lower than neomycin.
- It is rare for this product to cause vestibular damage during the course of treatment. This product is the same as streptomycin and neomycin. It can also block neuromuscular junctions and cause respiratory depression. It is more likely to occur in intraperitoneal administration under ether anesthesia. It also occurs after intramuscular or intravenous injection. Neuromuscular junction block can still cause
- Calcium gluconate may relieve respiratory depression
Kanamycin Urinary System
- This product can also cause kidney damage, its toxicity to the kidney is lower than neomycin but greater than streptomycin. There can be clear casts and granular casts in the urine, sometimes there are a small amount of red and white blood cells, proteinuria is occasionally seen, and most of them are transient. A few patients, especially the elderly, can develop renal dysfunction; there are also individual cases of oliguria and acute kidney Report of necrosis. The renal lesions caused by kanamycin are reversible and can be recovered quickly after stopping the treatment. In severe cases, the recovery is slower or partial.
Kanamycin digestive system
- Oral can cause nausea, vomiting, diarrhea, even after long-term use can cause malabsorption, fat diarrhea and so on. [Others] This product has a higher incidence of local pain by intramuscular injection and is generally more tolerant. May cause leukopenia, prolonged prothrombin time, decreased fibrinogen, and hypertension. Secondary infections (caused by Pseudomonas aeruginosa or other Gram-negative bacteria, drug-resistant Staphylococcus aureus, Bacteroides, etc.) are occasionally seen.
Kanamycin contraindications
- Renal dysfunction should be used with caution.
Kanamycin
- See streptomycin sulfate. 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.
- (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. Neosmin
- Dextran increases or decreases the renal toxicity of this product
- (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.
Kanamycin
Kanamycin eye drops
- Pharmacological action
- Kanamycin is an aminoglycoside antibiotic. For most Enterobacteriaceae bacteria, such as Escherichia coli, Klebsiella, Proteus, intestine
- The drug enters the fetal circulation through the placenta
- dynamics
- This product is rarely absorbed into the eye tissues or into the systemic blood circulation after eye drops.
- Indication
- Eye drop preparation for meibomitis
- Suitable for the treatment of infections caused by bacteria such as sensitive Escherichia coli, Klebsiella, Proteus, Neisseria gonorrhoeae and Staphylococcus, keratitis, dacryocystitis, eyelid inflammation, meibomitis .
- Dosage
- Drop into the conjunctival sac of the eye, 1 to 2 drops at a time, 3 to 5 times a day.
- Adverse reactions
- Occasionally mild eye irritation and discomfort, no systemic adverse reactions.
- Taboo
- Those who are allergic to this product or other aminoglycosides are contraindicated.
- Precautions
- 1. This product should not be injected directly under the bulbous conjunctiva or into the anterior chamber of the eye. 2. Lacrimal sac infection (dacryocystitis) often occurs in children with lacrimal duct occlusion. In addition to using this product for eye drops, it can be supplemented with local hot compresses.
- 3 Do not touch the mouth of the bottle during eye drops. Tighten the bottle cap after use to avoid contaminating the liquid medicine. Although this product is rarely absorbed into the whole body's blood circulation after eye drops, pregnant women and lactating women should still pay attention not to overdose, so as not to affect the growth and development of the fetus and infant.
- interaction
- This product should not be used in combination with capreomycin
- 1. Combined with other aminoglycosides or applied topically, it can increase ototoxicity, renal toxicity, and neuromuscular blockade. 2. Combined with capreomycin, cisplatin, itanilic acid, furosemide, or vancomycin (or norvancomycin), or continuous topical application may increase ototoxicity and renal toxicity.
- 3 Topical concomitant use with cefotaxime or cefazolin may increase renal toxicity.
- 4 Other nephrotoxic drugs and ototoxic drugs should be used with this product in combination or successively, so as not to aggravate nephrotoxicity or ototoxicity.
- preparation
- 1, 8ml: 40mg
Kanamycin veterinary medicine treatment direction
- Swine asthma, also known as porcine endemic pneumonia, is a chronic lung disease in pigs. The main symptoms are cough and asthma.
- Combined with cefazolin sodium increases renal toxicity
- 2. Symptoms. The main symptoms are cough and asthma, while the body temperature and appetite are generally normal; the elderly with disease course show debilitating, thin body, rough coat, slow growth, and increased feed-to-meat ratio.
- 3. Post-mortem. The lesions were limited to the lymph nodes in the lungs and abdominal cavity, and the lung lobes on both sides were symmetrically "pancreatic."
- 4. Differential diagnosis. Mainly different from swine influenza, swine pneumonia, and infectious pleurisy. Influenza: sudden outbreak, rapid spread, pigs
- Kanamycin eye drops
- 5. Preventive measures. While strengthening the daily management work, inoculate the epidemic area (field) with attenuated vaccine against swine asthma, breed males and sows twice a year, and immunize piglets 15 to 18 days old. Intramuscular injection with kanamycin sulfate, 30,000 to 50,000 units / kg body weight, twice a day.
Kanamycin injection
Kanamycin pharmacological action
- Kanamycin sulfate is an aminoglycoside antibiotic. This product is for most Enterobacteriaceae bacteria such as Escherichia coli, Klebsiella, Enterobacter
- Kanamycin injection
Kanamycin kinetics
- After intramuscular injection of this product, it is quickly absorbed and reaches the peak drug concentration in 1 to 2 hours. After a single intramuscular injection of 0.5 g, the average peak plasma concentration (Cmax) was 20 mg / L. The blood elimination half-life (T1 / 2a) is 2 to 4 hours, and the serum protein binding rate is low. Renal hypofunction can be prolonged significantly. Kanamycin can be distributed to various tissues in the body, accumulated in renal cortical cells, and has high concentrations of pleural fluid and ascites fluid, which can pass through the placenta and enter the fetus. Concentrations in bile and feces are lower. This product rarely enters the cerebrospinal fluid. This product is not metabolized in the body, mainly excreted by the urine after glomerular filtration, and 80% to 90% is excreted in the urine within 24 hours after administration. Hemodialysis and peritoneal dialysis can clear considerable doses.
Kanamycin indications
- This product is suitable for severe infections caused by sensitive Enterobacteriaceae bacteria such as Escherichia coli, Klebsiella, Proteus, Enterobacter aerogenes, Shigella, etc., such as pneumonia, sepsis, abdominal infections, etc., often Need to be combined with other antibacterial drugs.
Kanamycin dosage
- 1. Adults usually use intramuscular injection or intravenous drip, 0.5g once every 12 hours; or 7.5mg / kg once every 12 hours, the daily dosage for adults should not exceed 1.5g, and the course of treatment should not exceed 14 days. The dose should be appropriately reduced in patients over 50 years of age. 2. Children usually use intramuscular injection or intravenous drip, divided into two doses according to the weight of 15-25mg / kg a day.
- 3 Kanamycin sulfate 0.25% solution can be used as a rinse. 0.1% solution can also be used for aerosol inhalation. 2.5% injection can be used for intraperitoneal administration.
- 4 Dosage for renal insufficiency: 60% to 90% of normal dose when creatinine clearance is 50-90mg / min, once every 12 hours (normal dose is 7.5mg / kg each time, once every 12 hours); creatinine When the clearance rate is 10 to 50ml / min, 30% to 70% of the normal dose is used every 12 to 18 hours; when the creatinine clearance rate is <10mg / min, 20% to 30% of the normal dose is used, every 24 to 48 hours. Times.
Kanamycin adverse reactions
- 1. Hearing loss, tinnitus or ear fullness may occur during the course of treatment, which is caused by affecting the cochlear nerves. A small number of patients, especially those with previous renal dysfunction, can occur after discontinuation of the drug and require attention. Dizziness and instability can occur when affecting vestibular nerve function, but it is rare. 2. Nephrogenic reactions such as hematuria, decreased urination or decreased urine output, decreased appetite, nausea, vomiting, and extreme thirst may occur.
- 3 Occasionally, there may be neuromuscular blockade such as dyspnea, drowsiness or weakness.
- 4 Other adverse reactions include headache, rash, drug fever, numbness around the mouth, decreased white blood cells, increased eosinophils, and local pain caused by intramuscular injection.
Kanamycin contraindications
- Those with a history of allergies to this product or other aminoglycosides are contraindicated.
Other requirements for kanamycin
- 1. Patients allergic to an aminoglycoside antibiotic, such as streptomycin, gentamicin, amikacin, etc., may also be allergic to this product.
- Adverse Reactions-Leukopenia
- 2. The following inspections should be performed during the medication: (1) Routine urine tests and renal function tests to prevent severe renal toxicity. (2) Hearing test or electrogram, especially high-frequency audiometry, is more important for the elderly. 3 Blood conditions should be monitored when possible, especially in neonates, the elderly and patients with impaired renal function. When administered once every 12 hours, the peak plasma concentration should be maintained at 15-30 mg / ml, and the trough concentration should be 5-10 mg / ml. The peak plasma concentration should be maintained at 56-64 mg / ml when administered once every 24 hours. Concentration <1mg / ml.
- 4 This product should be used with caution in the following cases: (1) loss of water can increase blood drug concentration and increase the possibility of toxic reactions. (2) The eighth pair of brain nerve damage, because this product can cause damage to the auditory nerve and vestibular function. (3) Myasthenia gravis or Parkinson's disease, because this product can cause neuromuscular blockade, resulting in skeletal muscle weakness. (4) Those with impaired renal function may cause renal toxicity due to this product.
- 5. Interference to diagnosis: can increase the measured values of alanine aminotransferase (ALT), aspartate aminotransferase (AST), serum bilirubin concentration and serum lactate dehydrogenase concentration; blood calcium, magnesium, The measured values of potassium and sodium concentrations may decrease.
- 6. Aminoglycosides and -lactams (cephalosporins and penicillins) can cause mutual inactivation when mixed. When kanamycin is used in combination with the above antibiotics, it must be administered in divided bottles. Kanamycin should not be instilled in the same bottle with other drugs.
- The drug enters the fetal circulation through the placenta
- 7. This product may cause ototoxicity and nephrotoxicity, so it should not be used for long-term treatment (such as mycobacterium disease), usually the treatment course does not exceed 14 days. This product
- Routine urine test during medication
Kanamycin overdose
- Due to the lack of specific antagonists, when kanamycin is excessive or causes toxic reactions, symptomatic therapy and supportive therapy are mainly used, and a large amount of water is added at the same time. Hemodialysis or peritoneal dialysis helps to clear kanamycin from the blood.
Kanamycin interaction
- 1. Combined with other aminoglycosides or applied locally or systemically, it can increase ototoxicity, renal toxicity, and neuromuscular blockade. 2. Combined with neuromuscular blocking drugs, it can aggravate neuromuscular blockade, resulting in muscle weakness and respiratory depression.
- 3 Combined with capreomycin, cisplatin, itanilic acid, furosemide, or vancomycin (or norvancomycin), or successive local or systemic applications may increase ototoxicity and renal toxicity.
- Combined with cefazolin sodium increases renal toxicity
- 4 Local or systemic use with cefotaxime or cefazolin may increase renal toxicity. 5. Combined with polymyxin injections, or successive local or systemic applications, can increase renal toxicity and neuromuscular blockade.
- 6. Other nephrotoxic drugs and ototoxic drugs should not be combined with this product or applied in order to avoid aggravating nephrotoxicity or ototoxicity.
Kanamycin preparation
- (1) 0.5g (500,000 units) (2) 1g (1 million units)