What Is Vancomycin Toxicity?

Vancomycin's chemical name is (S)-(3S, 6R, 7R, 22R, 23S, 26S, 36R, 38R) -44- [[2-O- (3-amino-2, 3, 6- Trideoxy-3-C-methyl--L-lyso-hexapyranosyl) --D-glucopyranosyl] oxy] -3- (carbamoylmethyl) -10,19 -Dichloro-2,3,4,5,6,7,23,24,25,26,36,37,38,38-tetradecane-7,22,28,30,32-pentahydroxy-6 -[(2R) -4-methyl-2- (amino) valeramido-2,5,24,38,39-pentaoxo-22H-8,11: 18,21-divinylene-23 , 36- (iminomethylene) -13,16: 31,35-dimethylene-1H, 16H- [1,6,9] oxadiazacyclohexadecyl [4,5-m] [10,2,16] -Benzoxadiazepine docosatratin-26-carboxylic acid, white powder, molecular formula C66H76Cl3N9O24, molecular weight 1485.71000, density 1.65 g / cm3

Chinese name: Vancomycin
Foreign name: Vancomycin

CAS number: 1404-90-6
Molecular formula: C66H76Cl3N9O24

Vancomycin compounds

Vancomycin Basic Information

Chinese name: Vancomycin

English name: Vancomycin

English alias: Vancomycin

CAS number: 1404-90-6

Molecular formula: C ₆₆ H ₇₆ Cl ₃ N ₉ O ₂₄

Molecular weight: 1485.71000

Structural formula:

Exact mass: 1483.41000

PSA: 530.49000 ^[1]

LogP: 4.73460

Vancomycin physical and chemical properties

Appearance and properties: almost white powder

Density: 1.65 g / cm ³ ^[1]

Vancomycin uses

1. ^[2] Kill bacteria by inhibiting their growth and reproduction. The drug interferes with cell wall synthesis by interfering with peptidoglycan, a key component in the bacterial cell wall structure, and inhibits the production of phospholipids and polypeptides in the cell wall.

2. Vancomycin is mainly used in the treatment of four aspects of infection: the first is the treatment of resistant bacteria infections; the other is also used in the treatment of antibiotic-resistant pseudomembranous enteritis caused by Clostridium difficile.

Vancomycin

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 walls, and has a strong effect on Staphylococcus aureus, Streptococcus pyogenes, and Streptococcus pneumoniae. It also has a good effect on Bacillus difficile, Bacillus anthracis and Diphtheria.

5, no cross-resistance with other antibiotics, very few resistant strains. Mainly used for endocarditis, sepsis, pseudomembranous enteritis, etc.

6. The drug is not absorbed orally. It must be dissolved with water for injection before intravenous drip. The drip time should not be less than 1 hour. Intravenous drips have skin reactions too quickly, and excessive concentrations can cause thrombophlebitis; intramuscular injection can cause severe pain, so it should not be injected intramuscularly; severe ototoxicity and nephrotoxicity should be used only for short-term rescue.

Vancomycin pharmacology and toxicology:

This product has a good antibacterial effect on most gram-positive bacteria such as methicillin-sensitive and resistant strains in Staphylococcus, including Staphylococcus aureus and coagulase-negative Staphylococcus, various Streptococci, Streptococcus pneumoniae and Enterococcus. ^[3]

Vancomycin pharmacokinetics:

This product is not absorbed orally. A single dose of intravenous infusion of 400mg will reach the peak blood concentration (Cmax) of 25.18mg / L after the infusion. The average blood concentration of 8 hours is 1.90mg / L. The effective blood concentration can be maintained for 6-8 hours . A single intravenous infusion of 800 mg resulted in an average peak blood concentration of 50.07 mg / L. This product can be widely distributed in various tissues and fluids of the body, but it is not easy to enter the brain tissue, and the amount in bile is also very small. After intravenous infusion, it is mainly excreted through the kidney. A single intravenous infusion of 400 mg has an average total excretion rate of 81.1% in 24 hours; a single intravenous infusion of 800 mg has an average total excretion rate of 85.9% in 24 hours. ^[3]

Vancomycin indications:

This product is limited to systemic infections caused by methicillin-resistant Staphylococcus aureus (MRSA) and intestinal infections and systemic infections caused by Clostridium difficile; penicillins or cephalosporins cannot be used in penicillin allergies For patients with severe staphylococcal infections that have not been treated with the above antibiotics, norvancomycin can be selected. This product is also used for the treatment of enterococcal endocarditis and coryneform (diphtheria) endocarditis in people who are allergic to penicillin. Treatment of staphylococcus-induced, venous shunt infections in hemodialysis patients allergic to penicillin and non-allergic to penicillin. ^[3]

Vancomycin specifications:

(1) 0.5g (500,000 units) (based on C65H73Cl2N9O24) ^[3]

Vancomycin Usage and Dosage:

Vancomycin hydrochloride is usually used at 2g (titer) per day, which can be divided into 500mg every 6 hours or 1g every 12 hours. Each intravenous drip is more than 60 minutes. It can be increased or decreased according to age, weight and symptoms. The elderly are 500mg every 12 hours or 1g every 24 hours, and each intravenous drip is more than 60 minutes. For children and infants, 40 mg / kg per day is divided into 2 to 4 intravenous drips, each drip is more than 60 minutes. The dose for each newborn is 10-15mg / kg. The newborn is administered once every 12 hours within one week of birth. The newborn is administered once every eight hours from one week to one month. Each intravenous drip is more than 60 minutes.
The preparation method is to add 10 mL of water for injection to a vial containing this product to dissolve it, and dilute it with at least 100 mL of physiological saline or 5% glucose injection, and the intravenous drip time is more than 60 minutes. ^[3]

Vancomycin adverse reactions:

(1) Rash, nausea, and phlebitis may occur.

(2) This product can also cause tinnitus, hearing loss, and impaired renal function.

(3) Transient peripheral blood leukopenia and elevated serum aminotransferase may occur in some patients.

(4) Rapid injection can cause allergic reactions, such as reduced blood pressure, and even cardiac arrest, as well as wheezing, dyspnea, rash, redness in the upper body (red neck syndrome), and spasms of the chest and back. ^[3]

Vancomycin contraindications:

Those who are allergic to vancomycin antibiotics are prohibited. ^[3]

Vancomycin precautions:

1. This product cannot be injected intramuscularly, and it is not suitable for intravenous injection.

2. The intravenous drip rate should not be too fast. Each dose (0.4-0.8g) should be slowly dripped after dissolving with at least 200ml 5% glucose injection or sodium chloride injection. The drip time should be more than 1 hour.

3 This product should be used with caution in patients with renal insufficiency. If there is an indication of application, it should be applied under the monitoring of the concentration of therapeutic drug (TDM) according to the degree of renal dysfunction.

4 Disturbance to diagnosis: Blood urea nitrogen may increase.

5. During the treatment, hearing, urine protein, cast, cell number, and relative urine density should be checked regularly. ^[3]

Vancomycin medication for pregnant and lactating women:

Avoid using this product during pregnancy. Use with caution in lactating women.

Vancomycin for children:

There is no data on the application of this product in newborns and infants. ^[3]

Vancomycin for the elderly:

This product is used in elderly patients with the risk of causing ototoxicity and renal toxicity (hearing or loss of hearing). As the renal function of elderly patients declines with age, even if the renal function measurement is within the normal range in elderly patients, a smaller therapeutic dose should be used. ^[3]

Vancomycin expert review

Vancomycin is a safe and effective antibiotic for the treatment of severe infections caused by methicillin-resistant Staphylococcus aureus, methicillin-resistant coagulase-negative staphylococci, and enterococci, including sepsis, lung infections, and skin and soft tissue infections. For nosocomial pulmonary infections with methicillin-resistant Staphylococcus aureus, vancomycin is the drug of choice. In China, Vancomycin 500mg was administered to 32 patients with severe infections caused by methicillin-resistant Staphylococcus aureus (MRSA), methicillin coagulase-negative staphylococcus (MR-CON), and enterococci every 8 hours or Once every 6 hours for at least 1 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 discontinuation. Vancomycin is an accurate and safe antibiotic for the treatment of severe infections caused by MRSA / MRCON and Enterococcus, including sepsis, lung infections, and skin and soft tissue infections. This medicine has a strong bactericidal effect on Gram-positive cocci, and oral administration has an excellent effect on the treatment of Clostridium difficile pseudomembranous colitis. ^[4]

Vancomycin fights superbugs

1. The "superbug" NDM-1, which has appeared in South Asian countries such as India, has spread to Britain, the United States, Canada, Australia, the Netherlands and other countries, and 170 people have been infected worldwide. According to US media analysis, although this super bacteria is terrifying, it is not impossible to control its spread. Domestic experts also believe that the super germs will not be as fierce as a stream, without excessive panic. A Belgian man who had a car accident in Pakistan and received short treatment there died in June 2010. The doctor did not confess the identity of the deceased, but only said that he was infected with bacteria containing the super-resistant gene NDM-1 when he was hospitalized in Pakistan. The doctor said that he was involved in a car accident, injured his leg, was admitted to hospital for major surgery, and then returned to Belgium, but was infected with the super bacteria when he returned home. The doctor had treated the patient with the powerful antibiotic colistin, but still could not save his life. The Belgian man was the first person to die from a super germ. Another Belgian man was infected with the super bacteria in a car accident in Montenegro. He was subsequently treated in Belgium and recovered last month.

2. He Jianfeng, director of the Institute for Epidemic Prevention and Control of the Guangdong Provincial Center for Disease Control and Prevention, said that the super pathogen NDM-1 is actually an enzyme gene change, which is easily mixed with bacteria and becomes a carrier for bacteria, which can be replicated and transmitted. Superbugs are resistant to many antibiotics, but according to research, vancomycin is still effective against it, and major hospitals have reserves that can be used when necessary. However, although vancomycin is effective in treating multi-drug resistant bacteria, it is unknown how effective it is. Director of the Department of Infectious Diseases, Peking University Hospital, Wang Guiqiang also said that NDM-1 is an infectious bacterium and is not an infectious disease like SARS or influenza A, so it will not cause a pandemic, so you don't have to be too panic. Wang Guiqiang pointed out that it is not known what special effects can be prevented by NDM-1, but it is necessary to protect personal hygiene such as washing hands frequently.

3. While the super germs caused global panic, some related pharmaceutical stocks were also sought after by the market. According to experts, superbugs are resistant to almost all antibiotics. The best antibiotics currently available are tigecycline and vancomycin. If the germ really spreads, pharmaceutical stocks could benefit.