Antibiotic Chloramphenicol Powder chloramphenicol
Product Description
Product Details
| Product Name |
Chloramphenicol |
| CAS No. |
56-75-7 |
| MF |
C11H12Cl2N2O5 |
| MW |
323.12938 |
| Appearance and shape |
White Powder |
chloramphenicol is an antibiotic with the chemical formula C11H12Cl2N2O5, ethanol, propanol, slightly soluble in ether, insoluble in benzene. Chloramphenicol is extremely stable and its aqueous solution does not fail even after boiling for 5h. Because chloramphenicol has two asymmetric carbon atoms in the molecule, chloramphenicol has four optical isomers, of which only the left-handed isomer has antibacterial properties.
Application&Function
Pharmacological properties
Chloramphenicol is a broad spectrum bacteriostatic agent. It can be diffused into bacterial cells through fat solubility, mainly acting on the 50s subunit of bacterial 70s ribosomes, inhibiting the transeptidase, blocking the growth of peptide chain, inhibiting the formation of peptide chain, and thus preventing protein synthesis. High concentrations or bacteria that are highly sensitive to this product are also bactericidal.
Chloramphenicol is generally more effective against gram-negative bacteria than Gram-positive bacteria. Sensitive bacteria are enterobacteriaceae bacteria (such as Escherichia coli, Enterobacter aerogenes, Klebsiella, Salmonella, etc.) and anthrax bacteria, pneumococcus, streptococcus, Listeria, staphylococcus and so on. Chlamydia, leptospira, Rickettsia are also sensitive to this product. This product on anaerobic bacteria such as clostridium tetanus, perfringens bacteria, actinobacteria and lactobacillus, clostridium also has considerable effect. However, it has no effect on pseudomonas aeruginosa, tuberculosis bacillus, viruses, fungi and so on.
Bacteria have slowly developed resistance to chloramphenicol and mainly produce acetyltransferase. Obtained by plasmid delivery. Some strains of certain bacteria (pseudomonas aerosa, Proteus, Klebsiella, etc.) also change the permeability of the bacterial cell wall, so that chloramphenicol can not enter the bacteria and become resistant.
pharmacokinetics
After intravenous administration, this product is widely distributed in the whole body tissues and body fluids, with high concentration in liver and kidney tissues, followed by lung, spleen, myocardium, intestine and brain tissues. It can enter the cerebrospinal fluid through the blood-cerebrospinal fluid barrier. When there is no inflammation of the meninges, the concentration of the cerebrospinal fluid is 21% to 50% of the blood concentration, when there is inflammation of the meninges, it can reach 45% to 89% of the blood concentration, and the newborn and infant patients can reach 50% to 99%. It can also enter the fetal circulation through the placental barrier, and the fetal blood concentration can reach 30% to 80% of the maternal blood concentration. It can also enter aqueous humor and vitreous fluid through the blood-eye barrier, and can reach therapeutic concentrations. It can also be secreted into milk, saliva, ascites, pleural fluid and synovial fluid.
The apparent volume of distribution (Vd) is 0.6 to 1L/kg. The protein binding rate is about 50% ~ 60%. Blood elimination half-life (t1/2b) is 1.5 ~ 3.5 hours for adults, 3 ~ 4 hours for patients with renal function impairment, the blood elimination half-life (t1/2b) is extended (4.6 ~ 11.6 hours) for patients with severe liver function impairment, the neonatal blood elimination half-life (t1/2b) within 2 weeks of birth is 24 hours, and the neonatal blood elimination half-life (T1/2B) is 12 hours for patients with 2 ~ 4 weeks. 4 hours for infants older than 1 month. 90% of the free drugs in the liver are combined with glucuronic acid to form inactive chloramphenicol monoglucuronic ester. Within 24 hours, 5% to 10% are excreted by glomerular filtration in their original form, and 80% are excreted by renal tubules as inactive metabolites. Dialysis had no obvious effect on the clearance of this product.
Specification
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