药品详细
Kanamycin (卡那霉素 )
化学结构式图
中文名
卡那霉素
英文名
Kanamycin
分子式
Not Available
化学名
(2R,3S,4S,5R,6R)-2-(aminomethyl)-6-{[(1R,2R,3S,4R,6S)-4,6-diamino-3-{[(2S,3R,4S,5S,6R)-4-amino-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy}-2-hydroxycyclohexyl]oxy}oxane-3,4,5-triol
分子量
Average: 484.4986
Monoisotopic: 484.238058014
Monoisotopic: 484.238058014
CAS号
8063-07-8
ATC分类
A07A 未知;J01G 未知;S01A 抗感染药
药物类型
small molecule
阶段
商品名
Bekanamycin;Kanamycin A;Kanamycin B;Kenamycin A;Klebcil;
同义名
Aminodeoxykanamycin;KAN;Kanamycin Base;Kanamycin Sulfate;Nebramycin Factor 5;
基本介绍
Antibiotic complex produced by Streptomyces kanamyceticus from Japanese soil. Comprises 3 components: kanamycin A, the major component, and kanamycins B and C, the minor components. [PubChem]
生产厂家
- Abraxis pharmaceutical products
- Apothecon inc div bristol myers squibb
- App pharmaceuticals llc
- Baxter healthcare corp anesthesia and critical care
- International medication systems ltd
- King pharmaceuticals inc
- Loch pharmaceuticals inc
- Pharmafair inc
- Solopak laboratories inc
- Warner chilcott div warner lambert co
- Watson laboratories inc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
| Form | Route | Strength |
|---|---|---|
| Injection, solution | Intramuscular | |
| Injection, solution | Intravenous | |
| Tablet | Oral |
规格
| Unit description | Cost | Unit |
|---|---|---|
| Kanamycin sulfate powder | 25.2 USD | g |
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
antibacterials 抗细菌;
药理
| Indication | For treatment of infections where one or more of the following are the known or suspected pathogens: E. coli, Proteus species (both indole-positive and indole-negative), E. aerogenes, K. pneumoniae, S. marcescens, and Acinetobacter species. | ||||||
| Pharmacodynamics | Kanamycin is an aminoglycoside antibiotic. Aminoglycosides work by binding to the bacterial 30S ribosomal subunit, causing misreading of t-RNA, leaving the bacterium unable to synthesize proteins vital to its growth. Aminoglycosides are useful primarily in infections involving aerobic, Gram-negative bacteria, such as Pseudomonas, Acinetobacter, and Enterobacter. In addition, some mycobacteria, including the bacteria that cause tuberculosis, are susceptible to aminoglycosides. Infections caused by Gram-positive bacteria can also be treated with aminoglycosides, but other types of antibiotics are more potent and less damaging to the host. In the past the aminoglycosides have been used in conjunction with penicillin-related antibiotics in streptococcal infections for their synergistic effects, particularly in endocarditis. Aminoglycosides are mostly ineffective against anaerobic bacteria, fungi and viruses. | ||||||
| Mechanism of action | Aminoglycosides like kanamycin "irreversibly" bind to specific 30S-subunit proteins and 16S rRNA. Specifically Kanamycin binds to four nucleotides of 16S rRNA and a single amino acid of protein S12. This interferes with decoding site in the vicinity of nucleotide 1400 in 16S rRNA of 30S subunit. This region interacts with the wobble base in the anticodon of tRNA. This leads to interference with the initiation complex, misreading of mRNA so incorrect amino acids are inserted into the polypeptide leading to nonfunctional or toxic peptides and the breakup of polysomes into nonfunctional monosomes. | ||||||
| Absorption | Kanamycin is rapidly absorbed after intramuscular injection and peak serum levels are generally reached within approximately one hour. Poor oral and topical absorption except with severe skin damage. | ||||||
| Volume of distribution | Not Available | ||||||
| Protein binding | Not Available | ||||||
| Metabolism | |||||||
| Route of elimination | Not Available | ||||||
| Half life | 2.5 hours | ||||||
| Clearance | Not Available | ||||||
| Toxicity | Mild and reversible nephrotoxicity may be observed in 5 - 25% of patients. Amikacin accumulates in proximal renal tubular cells. Tubular cell regeneration occurs despite continued drug exposure. Toxicity usually occurs several days following initiation of therapy. May cause irreversible ototoxicity. Otoxocity appears to be correlated to cumulative lifetime exposure. Drug accumulation in the endolymph and perilymph of the inner ear causes irreversible damage to hair cells of the cochlea or summit of ampullar cristae in the vestibular complex. High frequency hearing is lost first with progression leading to loss of low frequency hearing. Further toxicity may lead to retrograde degeneration of the 8th cranial (vestibulocochlear) nerve. Vestibular toxicity may cause vertigo, nausea, vomiting, dizziness and loss of balance. Oral LD50 is 17500 mg/kg in mice, over 4 g/kg in rats, and over 3 g/kg in rabbits. | ||||||
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理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | Not Available | ||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Bumetanide | Increased ototoxicity |
| Cefotaxime | Increased risk of nephrotoxicity |
| Cefotetan | Increased risk of nephrotoxicity |
| Cefoxitin | Increased risk of nephrotoxicity |
| Ceftazidime | Increased risk of nephrotoxicity |
| Ceftriaxone | Increased risk of nephrotoxicity |
| Ethacrynic acid | Increased ototoxicity |
| Furosemide | Increased ototoxicity |
| Ticarcillin | Ticarcillin may reduce the serum concentration of Kanamycin. Ticarcillin may inactivate Kanamycin in vitro and the two agents should not be administered simultaneously through the same IV line. |
食物相互作用
Not Available
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