Analysis and application of β-lactam antibiotic combination preparation
2019-09-13 16:04:37
Beta-lactam antibiotics are a class of antibacterial agents with good anti-infective effects. However, the resistance of bacteria to such drugs has become a serious problem. One of the mechanisms of bacterial resistance is that bacteria destroy the β-lactam ring by producing enzymes, which makes the antibiotics inactive.
The main resistance mechanism of bacteria to β-lactam drugs is as follows: (1) Inactivated enzymes are produced, so that the antibacterial drugs are destroyed before they act on the cells. 2 antibiotic osmotic barrier, due to bacterial cell wall barrier or bacterial cytoplasmic membrane permeability changes, so that drugs can not enter the bacteria. 3 changes in the target position or the production of new targets, the conformational change of the bacterial penicillin-binding protein, so that its binding ability to the antibacterial agent is reduced. 4 Overexpression of the target site. 5 active efflux system, the bacteria produce an active efflux mechanism, increasing the active discharge of antibiotics from the bacteria to the body. Among them, the * mechanism is the main reason for the spread of drug-resistant strains.
One of the methods for solving the drug resistance problem is to develop a β-lactamase inhibitor, which inactivates the β-lactamase by an enzyme inhibitor to protect the β-lactam ring, thereby allowing these antibiotics to exert their original antibacterial effects. The results of in vitro tests showed that the effect of BRL4271 was obvious, tazobactam, potassium clavulanate was second, and sulbactam was weak. These enzyme inhibitors must be combined with antibiotics to function better. Therefore, many pharmaceutical companies at home and abroad produce a batch of compound preparations for clinical use. These antibacterial compound preparations are now analyzed for reference by clinical and drug research and development departments.
1. Compound preparation containing enzyme inhibitor
1.1 Compound preparation containing sulbactam (see Table 1)
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1.1.1 Ampicillin / sulbactam. Its antibacterial spectrum is the same as that of ampicillin, but due to the presence of sulbactam, it has a strong inhibitory effect on β-lactamase produced by drug-resistant strains. Therefore, this strain has a good effect on strains resistant to ampicillin. The pharmacokinetics of ampicillin and sulbactam in parallel are beneficial to the synergistic antibacterial effect of the two drugs in the body. Because the sulbactam in this product penetrates the cell membrane weakly, the product is produced. The extracellular enzyme of S. aureus works well.
Note when using: 1 penicillin allergy is disabled. 2 Penicillin skin test should be performed before administration. 3 Shuxinxin powder injection was 0.75g (ampicillin sodium 0.5g + sulbactam sodium 0.25g), and sulbaccilin oral tablet was 187.5mg, 375mg. 4 Some adverse reactions of ampicillin can occur in this product. 5 patients who receive allopurinol or disulfiram should not use this product. 6 patients with mononucleosis, combined with ampicillin susceptible to rash.
1.1.2 Amoxicillin / sulbactam. For compound tablets or injections. Tablets 500 mg per tablet (containing amoxicillin 250 mg, sulbactam 250 mg). Injection 750 mg per capsule (containing amoxicillin 500 mg, sulbactam 250 mg). Sulbactam is a β-lactamase inhibitor that rapidly passes through the bacterial cell wall and irreversibly destroys the β-lactamase, thereby maintaining the sensitivity of amoxicillin to bacteria and effectively killing bacteria. After oral administration of 500 mg, the Tmax was about 90 min, and after intramuscular injection of 750 mg, the Tmax was about 45 min. This product is mainly discharged from the urine.
Note when using: 1 For those who are allergic to penicillin, it is not recommended for pregnant women and lactating women. 2 Excessive poisoning can be removed by hemodialysis. 3 Intramuscular injection or intravenous injection at least 3.5ml of water for injection to dissolve a bottle of powder, the solution must be used within 60min after preparation, the solution should be discarded after this time. 4 intravenous injection should be prepared according to different dilutions. The high concentration of the drug zui in the solution and the long time of the drug solution zui are shown in Table 2.
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1.1.3 cefoperazone / sulbactam. The main ingredients are cefoperazone sodium and sulbactam sodium. Cefoperazone is a third-generation cephalosporin that achieves bactericidal action by inhibiting the synthesis of bacterial cell walls. In addition to its antibacterial activity against Neisseria gonorrhoeae and Acinetobacter, sulbactam has no other antibacterial activity, but has irreversible inhibition on various β-lactamases produced by drug-resistant strains, and can enhance cefoperazone. The ability to resist the degradation of various β-lactamases has a significant synergistic effect on cefoperazone.
Note when using [3]: 1 Disable allergy to any component of this product. 2 Skin allergy test should be done before use. 3 pregnant women, lactating women with caution with this product. 4 should avoid starting with Lactate Ringer's solution or 2% lidocaine solution to prepare injections, because of mixing can cause incompatibility. 5 can not be directly mixed with aminoglycoside injection, due to physical compatibility contraindications. 6 There have been individual patients who used cefoperazone to cause Vitamin K deficiency. 7 Prohibition of alcohol and alcoholic beverages during the period of cefoperazone use and within 5 days of withdrawal. 8 The function of the liver, kidney and hematopoietic system should be checked regularly during longer treatment periods. 9 Due to the broad-spectrum antibacterial activity of this product, the use of this product alone is sufficient to treat most infections, and if necessary, in combination with other antibiotics, such as with aminoglycosides, the renal function of patients should be monitored during treatment.
1.1.4 Ceftriaxone / sulbactam. Ceftriaxone is a third-generation cephalosporin with broad-spectrum antibacterial activity and is effective against many G+ and G-bacteria. Sulbactam is an enzyme inhibitor that inhibits the β-lactamase produced by drug-resistant bacilli and ensures cephalosporins. The anti-drug effect of Qusong. This product also has good antibacterial activity against ampicillin-resistant Haemophilus influenzae and resistance to cephalosporin and penicillin-resistant Staphylococcus aureus.
Note when using: 1 Ceftriaxone can enter the milk through the placenta, pregnant women and lactating women should use this product with caution. 2 newborns with symptoms of jaundice should not use this product. 3 elderly patients, in addition to weakness, malnutrition and renal function decline, generally do not need to adjust the dose. 4 mild to moderate liver and kidney dysfunction can be adjusted without dose adjustment, severe patients adjust the dose according to the monitoring results. 5 for a cephalosporin or allergic to penicillin, may also be allergic to this product, should pay attention. 6 The test of urine sugar by copper sulfate method may give a false positive reaction (glucose method is not disturbed).
1.1.5 cefotaxime / sulbactam. Cefotaxime is a semi-synthetic third-generation cephalosporin, which has a similar or weaker effect on Gram-positive bacteria than the first-generation cephalosporin, and has strong antibacterial activity against Gram-negative bacteria. It has strong antibacterial activity against streptococcus (except enterococcus). This product does not absorb the intestines. Intramuscular injection of 1g, 0.5h blood drug concentration peaked. The distribution in the body is wide, the concentration in the bile is high, and it is not easy to pass through the normal meninges. However, when the meninges have inflammation, the amount of penetration can be increased to achieve an effective concentration in the cerebrospinal fluid. Its metabolites and some prototypes are excreted in the urine, and the concentration of the drug in the urine is high. Sulbactam is a β-lactamase inhibitor that inhibits the destruction of penicillins and cephalosporins by β-lactamase. At the same time, it has a good effect on Neisseria (Neisseria gonorrhoeae, meningococcus). The inhibition rate of the enzyme by 4.8 μg/ml was 100%. The cefotaxime and sulbactam were prepared in a 1:1 formula, and the effective rate was 86%. The bacteriological clearance rate was 82%, and the adverse reaction rate was 10%. The main symptoms were gastrointestinal symptoms and light. Degree of ALT increased. This product can cause allergic reactions, caution for those who are allergic to penicillin.
1.2 Compound preparation containing potassium clavulanate (clavulanic acid) (see Table 3)
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1.2.1 Amoxicillin / Clavulanate potassium [3]. It is a compound preparation of amoxicillin (amoxycillin) and potassium clavulanate. The clavulanic acid inhibits the β-lactamase produced by the bacteria, protects amoxicillin from the destruction of the enzyme and exerts an antibacterial effect, thereby increasing the antibacterial efficacy of amoxicillin. This product has a strong bactericidal effect on ampicillin and amoxicillin resistant bacteria. Sensitive pathogens include: Staphylococcus aureus, Streptococcus pyogenes, Schonococcus, Influenza, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, and Bacteroides fragilis.
Note when using: 1 This product is not suitable for intramuscular injection. 2 penicillin allergy is disabled. A penicillin skin allergy test is required before use. 3 Dissolved product should be administered immediately, any remaining liquid should be discarded and should not be stored frozen. 4 This product will reduce its stability in a solution containing glucose, dextran or bicarbonate, so this product solution can not be mixed with the solution containing the above substances. 5 This product solution should not be mixed with blood products or protein-containing liquids in vitro, nor mixed with intravenous fat emulsion. 6 If this product is combined with aminoglycoside antibiotics, they should not be mixed in the same bottle, because this product will inactivate the latter. 7 pregnant women should not be used. 8 patients with severe liver dysfunction should be used with caution. 9 patients with moderate or severe renal dysfunction should adjust the dose of this product.
1.2.2 ticarcillin sodium / potassium clavulanate. Ticarcillin has an antibacterial effect on some G-aerobic pathogens, but it is not resistant to enzymes. Potassium clavulanate is a β-lactamase inhibitor that inhibits the β-lactamase of most bacteria, thereby blocking the hydrolysis of penicillins by enzymes and expanding and enhancing the antibacterial range and activity of penicillins.
Note when using: 1 Allergic to β-lactam antibiotics (such as penicillin, cephalosporin). A penicillin skin allergy test should be performed before using this product. 2 pregnant women are banned. 3 patients with severely impaired liver function should use this product with caution. 4 patients with moderate to severe renal insufficiency need to adjust medication. 5 very few patients with high-dose ticarcillin after coagulation dysfunction, bleeding occurred. Most patients with renal insufficiency, unless the doctor believes that no other drugs can be replaced, should be promptly discontinued and appropriate treatment. 6 Because this product is a sodium-containing preparation, the sodium content of this product should be included in the total sodium intake for patients with sodium-restricted diet.
1.3 Compound preparation containing tazobactam (see Table 4)
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Piperacillin / tazobactam. Piperacillin is an anti-Pseudomonas penicillin, and the main antibacterial spectrum includes G-bacteria and certain anaerobic bacteria. Tazobactam is an enzyme inhibitor that inhibits the destruction of piperacillin by β-lactamase produced by bacteria and is suitable for infection caused by enzyme-producing strains.
Note when using: 1 This product can cause anaphylactic shock, and penicillin skin test should be performed before use. 2 During treatment, patients with diarrhea should consider whether it is pseudomembranous colitis. If the diagnosis is established, appropriate measures should be taken. 3 This product contains sodium. Patients who need to control salt intake should check the serum electrolyte level regularly. For patients who are treated with cytotoxic drugs or diuretics, be alert to the possibility of hypokalemia. 4 pregnant women, lactating women with caution. 5 Regularly check the hematopoietic function, especially for patients with a course longer than 21d. 6 This product cannot be mixed with other drugs in syringes or bottles. If it is used together with other antibiotics, it must be given separately. 7 Solutions containing sodium lactate and sodium bicarbonate should not be compatible with this product. 8 patients with renal insufficiency should adjust the dose.
1.4 Combination preparation containing specific enzyme inhibitor (cilastatin) (see Table 5)
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Imipenem/cilastatin sodium. Is an equivalent compound of imipenem and cilastatin sodium. Imipenem is a broad-spectrum carbapenem ring of thimycin antibiotics. G+ bacteria G-bacteria and anaerobic bacteria are killed by inhibiting the synthesis of bacterial cell walls. Since imipenem can be destroyed by renal peptidase in the kidney, cilastatin sodium is added to the preparation. It is a specific enzyme inhibitor that blocks the metabolism of imipenem in the kidney to ensure the effectiveness of the drug.
This product has strong stability to β-lactamase produced by bacteria, and has broad spectrum of antibacterial activity. The concentration of less than 8μg/ml can kill almost all common pathogenic bacteria in clinical practice. The MIC90 of most pathogenic bacteria is less than 1μg/ml. . Intravenous injection of this product 1g, Cmax is 65μg / ml, effective antibacterial concentration can be maintained for 4-6h, half-life of 1h, mainly through the kidney, 24h urine discharge of 70% of the dose.
Note when using: 1 For those who are allergic to any component of this product, before using this product, you should carefully ask about the history of allergic reactions to penicillin, cephalosporins, other β-lactam antibiotics and other allergens. If you have an allergic reaction to this product, you should stop the drug immediately and do the treatment. 2 pregnant women and lactating women with caution, pediatric patients with infants and renal insufficiency should not be used. 3 patients with epilepsy should also be used with caution. 4 overdose use of this product may have neurotoxic effects, such as muscle cramps, confusion or seizures, especially in patients with severe renal impairment and epilepsy. 5 have nausea, vomiting, diarrhea, and severe cases of pseudomembranous colitis. 6 Intravenous infusion can not be mixed with other antibiotics or directly added to other antibiotics. 7 intramuscular injection of this product suspension, used within 1h after preparation. 8 This product can be combined with infusion containing sodium lactate
2. Compound preparation containing probenecid (see Table 6)
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Ampicillin / probenecid. Ampicillin is a semi-synthetic broad-spectrum antibiotic. Its effect on G+ bacteria is similar to that of penicillin. It is not effective against penicillin-resistant Staphylococcus aureus. It is effective against some G-bacteria, but it is easy to produce drug resistance. The serum concentration of this product was 2h peaked, and the serum concentration was 0.5-1h after intramuscular injection. The body was widely distributed, 80% of the original drug was excreted by urine, and the half-life was less than 1h. This product can be used for urinary system caused by sensitive bacteria, respiratory system, biliary tract, intestinal infection and meningitis, endocarditis and so on. Probenecid can interfere with the metabolism of enzymes by reversible action, thereby inhibiting the excretion rate of renal tubules to penicillin and semi-synthetic penicillin, so as to increase and prolong the concentration of the above drugs in plasma, so that the above drugs can prolong the effect. According to this principle, the combination of ampicillin and probenecid can enhance the therapeutic effect.
Note when using: 1 The toxicity of this product is extremely low, so a larger dose can be used, but it can cause gastrointestinal discomfort after oral administration. 2 Must be tested for penicillin skin allergy before use. 3 The incidence of rash is higher than other penicillins, up to 10% or higher, and sometimes medicinal fever occurs.
3. Combination preparation containing trimethoprim (see Table 7)
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Each capsule contains cephalexin 125 mg and trimethoprim 25 mg. The drug inhibits the synthesis of bacterial cell walls by inhibiting bacterial transpeptidase, inhibiting or killing bacteria. The combination of cephalexin and trimethoprim improves the antibacterial ability, delays the development of drug resistance, and reduces the oral dose.
Note when using: 1 disabled for cephalosporin antibiotics and pregnant women. 2 for penicillin allergy and liver and kidney dysfunction are used with caution. 3 occasional loss of appetite, rash, itching, medicinal fever, can disappear after stopping the drug.
4. a combination of two antibiotics
4.1 Amoxicillin / flucloxacillin (new sterilization). A composite antibiotic consisting of amoxicillin and flucloxacillin in a 1:1 ratio. Flucloxacillin mainly kills β-lactamase-resistant Staphylococcus aureus and other positive bacteria, and has an inhibitory effect on β-lactamase. Amoxicillin has a highly effective bactericidal effect on G-bacteria. Therefore, the combination of the two enhances the bactericidal ability and expands the antibacterial spectrum. This product is acid and resistant to enzymes. Oral absorption is good, its bioavailability is greater than 90%, the body is widely distributed, and there is a high concentration in body fluids. This product can be used for respiratory, urinary, bone and joint, oral and otolaryngology, skin and soft tissue, digestive tract and other infections.
Note when using: 1 Disabled for allergic to penicillin. 2 Penicillin should be used for skin allergy test before use. 3 After the product is dissolved, the liquid may turn red, but it does not affect the curative effect.
4.2 Amoxicillin / dicloxacillin sodium (cocci injection). The antibacterial spectrum of amoxicillin is the same as that of ampicillin, but the bactericidal effect is better than that of ampicillin. It is not effective against enzyme-resistant Staphylococcus aureus and enzyme-resistant negative bacilli and Pseudomonas aeruginosa. Diclocillin is resistant to staphylococcus penicillin and has good antibacterial activity against strains of Staphylococcus aureus. The in vitro antibacterial activity is strong in diclocillin. The combination of the two drugs makes the antibacterial properties complementary.
Note when using: 1 Disabled for allergic to penicillin or cephalosporin. 2 Need to be tested for penicillin allergy before use.
4.3 ampicillin / cloxacillin sodium (Erosu powder injection, etc.). It is an equal mixture of ampicillin sodium and cloxacillin sodium. Ampicillin has broad-spectrum antibacterial properties, but is not resistant to enzymes. Cloxacillin is resistant to the penicillinase properties produced by S. aureus, and the combination of the two complements the antibacterial properties. It has an antibacterial effect on the enzyme-producing Staphylococcus aureus and some other G+ bacteria and a few G-bacteria.
Note during use: 1 The penicillin skin allergy test should be done before use. 2 newborns with symptoms of jaundice should use this product with caution. 3 This product may have mild bloating, nausea, vomiting, loss of appetite and other gastrointestinal symptoms, can also cause rash, urticaria, and even anaphylactic shock. 4 This product should not use sodium bicarbonate or other alkaline liquid as a solvent.
The main resistance mechanism of bacteria to β-lactam drugs is as follows: (1) Inactivated enzymes are produced, so that the antibacterial drugs are destroyed before they act on the cells. 2 antibiotic osmotic barrier, due to bacterial cell wall barrier or bacterial cytoplasmic membrane permeability changes, so that drugs can not enter the bacteria. 3 changes in the target position or the production of new targets, the conformational change of the bacterial penicillin-binding protein, so that its binding ability to the antibacterial agent is reduced. 4 Overexpression of the target site. 5 active efflux system, the bacteria produce an active efflux mechanism, increasing the active discharge of antibiotics from the bacteria to the body. Among them, the * mechanism is the main reason for the spread of drug-resistant strains.
One of the methods for solving the drug resistance problem is to develop a β-lactamase inhibitor, which inactivates the β-lactamase by an enzyme inhibitor to protect the β-lactam ring, thereby allowing these antibiotics to exert their original antibacterial effects. The results of in vitro tests showed that the effect of BRL4271 was obvious, tazobactam, potassium clavulanate was second, and sulbactam was weak. These enzyme inhibitors must be combined with antibiotics to function better. Therefore, many pharmaceutical companies at home and abroad produce a batch of compound preparations for clinical use. These antibacterial compound preparations are now analyzed for reference by clinical and drug research and development departments.
1. Compound preparation containing enzyme inhibitor
1.1 Compound preparation containing sulbactam (see Table 1)
1.1.1 Ampicillin / sulbactam. Its antibacterial spectrum is the same as that of ampicillin, but due to the presence of sulbactam, it has a strong inhibitory effect on β-lactamase produced by drug-resistant strains. Therefore, this strain has a good effect on strains resistant to ampicillin. The pharmacokinetics of ampicillin and sulbactam in parallel are beneficial to the synergistic antibacterial effect of the two drugs in the body. Because the sulbactam in this product penetrates the cell membrane weakly, the product is produced. The extracellular enzyme of S. aureus works well.
Note when using: 1 penicillin allergy is disabled. 2 Penicillin skin test should be performed before administration. 3 Shuxinxin powder injection was 0.75g (ampicillin sodium 0.5g + sulbactam sodium 0.25g), and sulbaccilin oral tablet was 187.5mg, 375mg. 4 Some adverse reactions of ampicillin can occur in this product. 5 patients who receive allopurinol or disulfiram should not use this product. 6 patients with mononucleosis, combined with ampicillin susceptible to rash.
1.1.2 Amoxicillin / sulbactam. For compound tablets or injections. Tablets 500 mg per tablet (containing amoxicillin 250 mg, sulbactam 250 mg). Injection 750 mg per capsule (containing amoxicillin 500 mg, sulbactam 250 mg). Sulbactam is a β-lactamase inhibitor that rapidly passes through the bacterial cell wall and irreversibly destroys the β-lactamase, thereby maintaining the sensitivity of amoxicillin to bacteria and effectively killing bacteria. After oral administration of 500 mg, the Tmax was about 90 min, and after intramuscular injection of 750 mg, the Tmax was about 45 min. This product is mainly discharged from the urine.
Note when using: 1 For those who are allergic to penicillin, it is not recommended for pregnant women and lactating women. 2 Excessive poisoning can be removed by hemodialysis. 3 Intramuscular injection or intravenous injection at least 3.5ml of water for injection to dissolve a bottle of powder, the solution must be used within 60min after preparation, the solution should be discarded after this time. 4 intravenous injection should be prepared according to different dilutions. The high concentration of the drug zui in the solution and the long time of the drug solution zui are shown in Table 2.
1.1.3 cefoperazone / sulbactam. The main ingredients are cefoperazone sodium and sulbactam sodium. Cefoperazone is a third-generation cephalosporin that achieves bactericidal action by inhibiting the synthesis of bacterial cell walls. In addition to its antibacterial activity against Neisseria gonorrhoeae and Acinetobacter, sulbactam has no other antibacterial activity, but has irreversible inhibition on various β-lactamases produced by drug-resistant strains, and can enhance cefoperazone. The ability to resist the degradation of various β-lactamases has a significant synergistic effect on cefoperazone.
Note when using [3]: 1 Disable allergy to any component of this product. 2 Skin allergy test should be done before use. 3 pregnant women, lactating women with caution with this product. 4 should avoid starting with Lactate Ringer's solution or 2% lidocaine solution to prepare injections, because of mixing can cause incompatibility. 5 can not be directly mixed with aminoglycoside injection, due to physical compatibility contraindications. 6 There have been individual patients who used cefoperazone to cause Vitamin K deficiency. 7 Prohibition of alcohol and alcoholic beverages during the period of cefoperazone use and within 5 days of withdrawal. 8 The function of the liver, kidney and hematopoietic system should be checked regularly during longer treatment periods. 9 Due to the broad-spectrum antibacterial activity of this product, the use of this product alone is sufficient to treat most infections, and if necessary, in combination with other antibiotics, such as with aminoglycosides, the renal function of patients should be monitored during treatment.
1.1.4 Ceftriaxone / sulbactam. Ceftriaxone is a third-generation cephalosporin with broad-spectrum antibacterial activity and is effective against many G+ and G-bacteria. Sulbactam is an enzyme inhibitor that inhibits the β-lactamase produced by drug-resistant bacilli and ensures cephalosporins. The anti-drug effect of Qusong. This product also has good antibacterial activity against ampicillin-resistant Haemophilus influenzae and resistance to cephalosporin and penicillin-resistant Staphylococcus aureus.
Note when using: 1 Ceftriaxone can enter the milk through the placenta, pregnant women and lactating women should use this product with caution. 2 newborns with symptoms of jaundice should not use this product. 3 elderly patients, in addition to weakness, malnutrition and renal function decline, generally do not need to adjust the dose. 4 mild to moderate liver and kidney dysfunction can be adjusted without dose adjustment, severe patients adjust the dose according to the monitoring results. 5 for a cephalosporin or allergic to penicillin, may also be allergic to this product, should pay attention. 6 The test of urine sugar by copper sulfate method may give a false positive reaction (glucose method is not disturbed).
1.1.5 cefotaxime / sulbactam. Cefotaxime is a semi-synthetic third-generation cephalosporin, which has a similar or weaker effect on Gram-positive bacteria than the first-generation cephalosporin, and has strong antibacterial activity against Gram-negative bacteria. It has strong antibacterial activity against streptococcus (except enterococcus). This product does not absorb the intestines. Intramuscular injection of 1g, 0.5h blood drug concentration peaked. The distribution in the body is wide, the concentration in the bile is high, and it is not easy to pass through the normal meninges. However, when the meninges have inflammation, the amount of penetration can be increased to achieve an effective concentration in the cerebrospinal fluid. Its metabolites and some prototypes are excreted in the urine, and the concentration of the drug in the urine is high. Sulbactam is a β-lactamase inhibitor that inhibits the destruction of penicillins and cephalosporins by β-lactamase. At the same time, it has a good effect on Neisseria (Neisseria gonorrhoeae, meningococcus). The inhibition rate of the enzyme by 4.8 μg/ml was 100%. The cefotaxime and sulbactam were prepared in a 1:1 formula, and the effective rate was 86%. The bacteriological clearance rate was 82%, and the adverse reaction rate was 10%. The main symptoms were gastrointestinal symptoms and light. Degree of ALT increased. This product can cause allergic reactions, caution for those who are allergic to penicillin.
1.2 Compound preparation containing potassium clavulanate (clavulanic acid) (see Table 3)
1.2.1 Amoxicillin / Clavulanate potassium [3]. It is a compound preparation of amoxicillin (amoxycillin) and potassium clavulanate. The clavulanic acid inhibits the β-lactamase produced by the bacteria, protects amoxicillin from the destruction of the enzyme and exerts an antibacterial effect, thereby increasing the antibacterial efficacy of amoxicillin. This product has a strong bactericidal effect on ampicillin and amoxicillin resistant bacteria. Sensitive pathogens include: Staphylococcus aureus, Streptococcus pyogenes, Schonococcus, Influenza, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, and Bacteroides fragilis.
Note when using: 1 This product is not suitable for intramuscular injection. 2 penicillin allergy is disabled. A penicillin skin allergy test is required before use. 3 Dissolved product should be administered immediately, any remaining liquid should be discarded and should not be stored frozen. 4 This product will reduce its stability in a solution containing glucose, dextran or bicarbonate, so this product solution can not be mixed with the solution containing the above substances. 5 This product solution should not be mixed with blood products or protein-containing liquids in vitro, nor mixed with intravenous fat emulsion. 6 If this product is combined with aminoglycoside antibiotics, they should not be mixed in the same bottle, because this product will inactivate the latter. 7 pregnant women should not be used. 8 patients with severe liver dysfunction should be used with caution. 9 patients with moderate or severe renal dysfunction should adjust the dose of this product.
1.2.2 ticarcillin sodium / potassium clavulanate. Ticarcillin has an antibacterial effect on some G-aerobic pathogens, but it is not resistant to enzymes. Potassium clavulanate is a β-lactamase inhibitor that inhibits the β-lactamase of most bacteria, thereby blocking the hydrolysis of penicillins by enzymes and expanding and enhancing the antibacterial range and activity of penicillins.
Note when using: 1 Allergic to β-lactam antibiotics (such as penicillin, cephalosporin). A penicillin skin allergy test should be performed before using this product. 2 pregnant women are banned. 3 patients with severely impaired liver function should use this product with caution. 4 patients with moderate to severe renal insufficiency need to adjust medication. 5 very few patients with high-dose ticarcillin after coagulation dysfunction, bleeding occurred. Most patients with renal insufficiency, unless the doctor believes that no other drugs can be replaced, should be promptly discontinued and appropriate treatment. 6 Because this product is a sodium-containing preparation, the sodium content of this product should be included in the total sodium intake for patients with sodium-restricted diet.
1.3 Compound preparation containing tazobactam (see Table 4)
Piperacillin / tazobactam. Piperacillin is an anti-Pseudomonas penicillin, and the main antibacterial spectrum includes G-bacteria and certain anaerobic bacteria. Tazobactam is an enzyme inhibitor that inhibits the destruction of piperacillin by β-lactamase produced by bacteria and is suitable for infection caused by enzyme-producing strains.
Note when using: 1 This product can cause anaphylactic shock, and penicillin skin test should be performed before use. 2 During treatment, patients with diarrhea should consider whether it is pseudomembranous colitis. If the diagnosis is established, appropriate measures should be taken. 3 This product contains sodium. Patients who need to control salt intake should check the serum electrolyte level regularly. For patients who are treated with cytotoxic drugs or diuretics, be alert to the possibility of hypokalemia. 4 pregnant women, lactating women with caution. 5 Regularly check the hematopoietic function, especially for patients with a course longer than 21d. 6 This product cannot be mixed with other drugs in syringes or bottles. If it is used together with other antibiotics, it must be given separately. 7 Solutions containing sodium lactate and sodium bicarbonate should not be compatible with this product. 8 patients with renal insufficiency should adjust the dose.
1.4 Combination preparation containing specific enzyme inhibitor (cilastatin) (see Table 5)
Imipenem/cilastatin sodium. Is an equivalent compound of imipenem and cilastatin sodium. Imipenem is a broad-spectrum carbapenem ring of thimycin antibiotics. G+ bacteria G-bacteria and anaerobic bacteria are killed by inhibiting the synthesis of bacterial cell walls. Since imipenem can be destroyed by renal peptidase in the kidney, cilastatin sodium is added to the preparation. It is a specific enzyme inhibitor that blocks the metabolism of imipenem in the kidney to ensure the effectiveness of the drug.
This product has strong stability to β-lactamase produced by bacteria, and has broad spectrum of antibacterial activity. The concentration of less than 8μg/ml can kill almost all common pathogenic bacteria in clinical practice. The MIC90 of most pathogenic bacteria is less than 1μg/ml. . Intravenous injection of this product 1g, Cmax is 65μg / ml, effective antibacterial concentration can be maintained for 4-6h, half-life of 1h, mainly through the kidney, 24h urine discharge of 70% of the dose.
Note when using: 1 For those who are allergic to any component of this product, before using this product, you should carefully ask about the history of allergic reactions to penicillin, cephalosporins, other β-lactam antibiotics and other allergens. If you have an allergic reaction to this product, you should stop the drug immediately and do the treatment. 2 pregnant women and lactating women with caution, pediatric patients with infants and renal insufficiency should not be used. 3 patients with epilepsy should also be used with caution. 4 overdose use of this product may have neurotoxic effects, such as muscle cramps, confusion or seizures, especially in patients with severe renal impairment and epilepsy. 5 have nausea, vomiting, diarrhea, and severe cases of pseudomembranous colitis. 6 Intravenous infusion can not be mixed with other antibiotics or directly added to other antibiotics. 7 intramuscular injection of this product suspension, used within 1h after preparation. 8 This product can be combined with infusion containing sodium lactate
2. Compound preparation containing probenecid (see Table 6)
Ampicillin / probenecid. Ampicillin is a semi-synthetic broad-spectrum antibiotic. Its effect on G+ bacteria is similar to that of penicillin. It is not effective against penicillin-resistant Staphylococcus aureus. It is effective against some G-bacteria, but it is easy to produce drug resistance. The serum concentration of this product was 2h peaked, and the serum concentration was 0.5-1h after intramuscular injection. The body was widely distributed, 80% of the original drug was excreted by urine, and the half-life was less than 1h. This product can be used for urinary system caused by sensitive bacteria, respiratory system, biliary tract, intestinal infection and meningitis, endocarditis and so on. Probenecid can interfere with the metabolism of enzymes by reversible action, thereby inhibiting the excretion rate of renal tubules to penicillin and semi-synthetic penicillin, so as to increase and prolong the concentration of the above drugs in plasma, so that the above drugs can prolong the effect. According to this principle, the combination of ampicillin and probenecid can enhance the therapeutic effect.
Note when using: 1 The toxicity of this product is extremely low, so a larger dose can be used, but it can cause gastrointestinal discomfort after oral administration. 2 Must be tested for penicillin skin allergy before use. 3 The incidence of rash is higher than other penicillins, up to 10% or higher, and sometimes medicinal fever occurs.
3. Combination preparation containing trimethoprim (see Table 7)
Each capsule contains cephalexin 125 mg and trimethoprim 25 mg. The drug inhibits the synthesis of bacterial cell walls by inhibiting bacterial transpeptidase, inhibiting or killing bacteria. The combination of cephalexin and trimethoprim improves the antibacterial ability, delays the development of drug resistance, and reduces the oral dose.
Note when using: 1 disabled for cephalosporin antibiotics and pregnant women. 2 for penicillin allergy and liver and kidney dysfunction are used with caution. 3 occasional loss of appetite, rash, itching, medicinal fever, can disappear after stopping the drug.
4. a combination of two antibiotics
4.1 Amoxicillin / flucloxacillin (new sterilization). A composite antibiotic consisting of amoxicillin and flucloxacillin in a 1:1 ratio. Flucloxacillin mainly kills β-lactamase-resistant Staphylococcus aureus and other positive bacteria, and has an inhibitory effect on β-lactamase. Amoxicillin has a highly effective bactericidal effect on G-bacteria. Therefore, the combination of the two enhances the bactericidal ability and expands the antibacterial spectrum. This product is acid and resistant to enzymes. Oral absorption is good, its bioavailability is greater than 90%, the body is widely distributed, and there is a high concentration in body fluids. This product can be used for respiratory, urinary, bone and joint, oral and otolaryngology, skin and soft tissue, digestive tract and other infections.
Note when using: 1 Disabled for allergic to penicillin. 2 Penicillin should be used for skin allergy test before use. 3 After the product is dissolved, the liquid may turn red, but it does not affect the curative effect.
4.2 Amoxicillin / dicloxacillin sodium (cocci injection). The antibacterial spectrum of amoxicillin is the same as that of ampicillin, but the bactericidal effect is better than that of ampicillin. It is not effective against enzyme-resistant Staphylococcus aureus and enzyme-resistant negative bacilli and Pseudomonas aeruginosa. Diclocillin is resistant to staphylococcus penicillin and has good antibacterial activity against strains of Staphylococcus aureus. The in vitro antibacterial activity is strong in diclocillin. The combination of the two drugs makes the antibacterial properties complementary.
Note when using: 1 Disabled for allergic to penicillin or cephalosporin. 2 Need to be tested for penicillin allergy before use.
4.3 ampicillin / cloxacillin sodium (Erosu powder injection, etc.). It is an equal mixture of ampicillin sodium and cloxacillin sodium. Ampicillin has broad-spectrum antibacterial properties, but is not resistant to enzymes. Cloxacillin is resistant to the penicillinase properties produced by S. aureus, and the combination of the two complements the antibacterial properties. It has an antibacterial effect on the enzyme-producing Staphylococcus aureus and some other G+ bacteria and a few G-bacteria.
Note during use: 1 The penicillin skin allergy test should be done before use. 2 newborns with symptoms of jaundice should use this product with caution. 3 This product may have mild bloating, nausea, vomiting, loss of appetite and other gastrointestinal symptoms, can also cause rash, urticaria, and even anaphylactic shock. 4 This product should not use sodium bicarbonate or other alkaline liquid as a solvent.
Food Ingredients, some natural raw materials can be widely used in food, drink etc. for human's health care.
Powder, oil, pigment etc.
Fish Oil EE/TG
Evening primrose oil
CLA oil
Krill oil
Borage oil
COQ 10
Chitosan
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Food Ingredients
Food Ingredients,Health Ingredients,Fish Oil,Natural Health Ingredients,Seabuckthorn Fruit Oil
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