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vancomycin

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Vancomycin is a kind of Glycopeptide antibiotics , used to treat bacterial infections.
Chinese name
vancomycin
Foreign name
Vancomycin
Molecular formula
C sixty-six H seventy-five Cl two N nine O twenty-four
molecular weight
one thousand four hundred and forty-nine point two five
CAS login number
1404-90-6
EINECS login number
215-772-6
Appearance
Almost white powder
Density
1.65 g/cm³

Compound Introduction

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essential information

Chinese name: vancomycin
English name: Vancomycin
CAS No.: 1404-90-6
Molecular formula: C sixty-six H seventy-five Cl two N nine O twenty-four
Molecular weight: 1449.25
PSA:530.49000
LogP:4.73460

Physicochemical properties

Appearance and properties: almost white powder
Density: 1.65 g/cm three

purpose

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1. Kill bacteria by inhibiting their growth and reproduction. This drug interferes with the Key components Peptidoglycan interferes with the synthesis of cell wall and inhibits the production of phospholipids and polypeptides in cell wall.
2. Vancomycin is mainly used in four aspects of infection treatment: first Drug resistant bacteria Treatment of infection; It is also used for antibiotics produced by clostridium difficile Drug resistance Treatment of pseudomembranous enteritis.
3. Vancomycin can also be used to treat colitis and intestinal inflammation; Vancomycin is also often used to prevent infection when installing cardiac catheters, venous catheters and other devices. Vancomycin can be used alone or in combination.
4. It can inhibit the synthesis of bacterial cell wall Staphylococcus aureus , suppuration streptococcus , Streptococcus pneumoniae, etc Bacillus anthracis Diphtheria And so on.
5. None with other antibiotics Cross resistance , rarely Drug resistant bacteria Strains. It is mainly used for endocarditis, septicemia, pseudomembranous enteritis, etc.
6. The drug is not absorbed after oral administration, and must be dissolved with water for injection before intravenous drip. The drip time shall not be less than 1 hour. If the intravenous drip is too fast, there will be skin reaction, and if the concentration is too high, it may cause Thrombophlebitis Intramuscular injection can cause severe pain, so intramuscular injection is not allowed; Severe ototoxicity and Nephrotoxicity , so it is only suitable for short-term rescue.

Pharmacology and toxicology:

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This product has good antibacterial effect on most gram-positive bacteria, such as methicillin sensitive and drug-resistant strains of staphylococcus including Staphylococcus aureus and coagulase negative staphylococcus, various streptococci, Streptococcus pneumoniae and Enterococcus.

Pharmacokinetics:

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This product is not absorbed after oral administration. A single intravenous drip of 400mg will reach the peak concentration of the drug in the blood after the drip( c max )25.18mg/L, the average 8-hour blood concentration is 1.90mg/L, and the effective blood concentration can be maintained for 6-8 hours. The average peak blood concentration was 50.07mg/L after a single intravenous drip of 800mg. This product can be widely distributed in all kinds of body tissues and body fluids, but it is not easy to enter brain tissues, and its amount in bile is also very small. After intravenous drip, it was mainly excreted by the kidney, with a single intravenous drip of 400mg. The average total excretion rate in 24 hours' urine was 81.1%; The average total excretion rate in 24 hours urine was 85.9% after a single intravenous drip of 800 mg.

indication:

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This product is limited to systemic infection caused by methicillin resistant Staphylococcus aureus (MRSA) and intestinal infection and systemic infection caused by Clostridium difficile; Penicillin allergic patients cannot use penicillin or cephalosporins, or patients with severe staphylococcal infection who are ineffective in the treatment of the above antibiotics can use norvancomycin. This product is also used for the treatment of enterococcal endocarditis and corynebacterium (diphtheria like bacillus) endocarditis in penicillin allergic patients. Treatment of arteriovenous shunt infection caused by Staphylococcus in hemodialysis patients with or without penicillin allergy.

Specifications:

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(1) 0.5g (500000 units) (according to C sixty-six H seventy-five Cl two N nine O twenty-four Count)

Usage and dosage:

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Vancomycin hydrochloride is usually used with 2g (potency) every day, which can be divided into 500mg every 6 hours or 1g every 12 hours. Each intravenous drip is more than 60 minutes, which can be increased or decreased moderately according to age, weight and symptoms. The elderly should drip 500mg every 12 hours or 1g every 24 hours for more than 60 minutes each time. 40 mg/kg/day for children and infants, divided into 2-4 intravenous drip, each intravenous drip should be more than 60 minutes. The dosage of each dose for newborns is 10-15mg/kg. The dose is given every 12 hours for newborns within one week of birth, and every 8 hours for newborns from one week to one month of birth. Each intravenous drip is more than 60 minutes.
The preparation method is to add 10mL of water for injection into the vial containing 0.5g of the product to dissolve it, and dilute it with at least 100mL of normal saline or 5% glucose injection. The intravenous drip time is more than 60 minutes.

Adverse reactions:

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(1) Rashes, nausea and phlebitis may occur.
(2) This product can also cause tinnitus, hearing loss and renal function damage.
(3) Some patients may also have transient peripheral leukopenia, serum aminotransferase, etc.
(4) Rapid injection can lead to anaphylactoid reaction, decreased blood pressure, even cardiac arrest, wheezing, dyspnea, rash, upper body redness (red neck syndrome), chest and back muscle spasm, etc.

Taboos:

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It is forbidden for those allergic to vancomycin antibiotics.

matters needing attention:

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1. This product is not suitable for intramuscular injection or intravenous injection.
2. The intravenous drip speed should not be too fast. Each dose (0.4~0.8g) should be dissolved with at least 200mL 5% glucose injection or sodium chloride injection and then slowly drip. The drip time should be more than 1 hour.
3. Patients with renal insufficiency should use this product with caution. If there are indications for use, it should be used in a reduced amount according to the degree of renal function decline under the monitoring of therapeutic drug concentration (TDM).
4. Interference to diagnosis: blood urea nitrogen may increase.
5. During the treatment, the hearing, protein in urine, tube type, cell number and urine relative density should be checked regularly.

Drugs for pregnant and lactating women:

Patients during pregnancy should avoid using this product. Use with caution for lactating women.

Children's medication:

There is a lack of data on the application of this product in newborns and infants.

Medication for the elderly:

This product may cause ototoxicity and nephrotoxicity in elderly patients (hearing loss or hearing loss). Since the renal function of elderly patients declines with age, even if the renal function measurement of elderly patients is within the normal range, a smaller therapeutic dose should be used.

Expert comments

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Vancomycin is an effective and safe antibiotic for the treatment of severe infections caused by methicillin-resistant Staphylococcus aureus, methicillin-resistant coagulase negative Staphylococcus and enterococci, including septicemia, lung infection, skin and soft tissue infection. Vancomycin is the first choice for hospital pulmonary infection caused by methicillin-resistant Staphylococcus aureus. In China, 32 patients with severe infection caused by methicillin resistant Staphylococcus aureus (MRSA), methicillin resistant coagulase negative Staphylococcus (MR-CON) and enterococci were given vancomycin 500mg every 8 or 6 hours for at least one week. The results showed that the total clinical effective rate of vancomycin in the treatment of severe gram-positive bacterial infections was 84.38%, the bacterial clearance rate was 79.10%, and the incidence of adverse reactions was 9.38%. The adverse reactions returned to normal after drug withdrawal. Vancomycin is an effective and safe antibiotic for the treatment of severe infections caused by MRSA/MRCON and enterococci, including septicemia, lung infection, skin and soft tissue infection. This drug has a strong bactericidal effect on gram-positive cocci, and oral administration has an excellent effect on the treatment of clostridium difficile pseudomembranous colitis.

Coping with superbugs

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1. In India and other South Asian countries“ Superbug ”NDM-1 has spread to the United Kingdom, the United States, Canada, Australia, the Netherlands and other countries, with 170 people infected worldwide. American media analysis said that although this superbug is scary, there is no way to control its spread. Domestic experts also believe that the superbug will not be as fierce as swine flu, and there is no need to panic. A Belgian man who had a car accident in Pakistan and received temporary treatment there died in June 2010. The doctor did not reveal the identity of the deceased, but said that he was infected with bacteria containing the super drug resistance gene NDM-1 when he was hospitalized in Pakistan. The doctor said that he was in a car accident and injured his leg. He was hospitalized for major surgery and then returned to Belgium, but he was infected with this superbug when he returned home. Doctors used powerful antibiotics Myxin Treatment of this patient, but still unable to save his life, this Belgian man is the first person to die of superbug. Another Belgian man was infected with this superbug due to a car accident in Montenegro, and then received treatment and recovered in Belgium.
2. He Jianfeng, director of the Institute of Epidemic Prevention and Control of Guangdong CDC, said that NDM-1 is actually an enzyme gene change, which is easily mixed with bacteria and becomes a carrier of bacteria, which can be replicated and spread. Superbugs have many antibiotics Drug resistance However, according to the research, vancomycin is still effective for it. All major hospitals have reserves and can use it when necessary. However, although vancomycin is effective in the treatment of multi drug resistant bacteria, it is unknown how effective it is. Wang Guiqiang, director of the Department of Infectious Diseases of Peking University Hospital, also said that NDM-1 is an infectious bacterium, not an infectious disease like SARS or swine flu, so it will not cause a pandemic, and we need not panic too much. Wang Guiqiang It is pointed out that it is not known what effective method is to prevent NDM-1, but it is necessary to do well in personal hygiene protection such as washing hands frequently. [1]