药品详细
Neomycin(新霉素)
化学结构式图
中文名
新霉素
英文名
Neomycin
分子式
C23H46N6O13
化学名
(2R,3S,4R,5R,6R)-5-amino-2-(aminomethyl)-6-{[(1R,2R,3S,4R,6S)-4,6-diamino-2-{[(2S,3R,4S,5R)-4-{[(2R,3R,4R,5S,6S)-3-amino-6-(aminomethyl)-4,5-dihydroxyoxan-2-yl]oxy}-3-hydroxy-5-(hydroxymethyl)oxolan-2-yl]oxy}-3-hydroxycyclohexyl]oxy}oxane-3,4-diol
分子量
Average: 614.6437
Monoisotopic: 614.312285588
Monoisotopic: 614.312285588
CAS号
1404-04-2
ATC分类
A01A 未知;A07A 未知;B05C 未知;D06A 未知;J01G 未知;R02A 未知;S01A 抗感染药;S02A 未知;S03A 未知;D09A 未知;S01A 抗感染药
药物类型
small molecule
阶段
approved
商品名
Biosol;Bykomycin;Endomixin;Fradiomycin;Fradiomycin Sulfate;Fraquinol;Lidamycin Creme;Myacine;Myacyne;Mycifradin;Mycifradin-N;Myciguent;Neo-Fradin;Neo-Mantle Creme;Neo-Rx;Neobiotic;Neobrettin;Neofracin;Neolate;Neomix;Neosulf;Nivemycin;Tuttomycin;Vonamycin Powder V;
同义名
Caswell No. 595;Neomycin B Sulfate;Neomycin Sulfate;Neomycin Sulphate;Neomycin trisulfate salt hydrate;USAF CB-19;
基本介绍
A component of neomycin that is produced by Streptomyces fradiae. On hydrolysis it yields neamine and neobiosamine B. (From Merck Index, 11th ed). Neomycin is a bactericidal aminoglycoside antibiotic that binds to the 30S ribosome of susceptible organisms. Binding interferes with mRNA binding and acceptor tRNA sites and results in the production of non-functional or toxic peptides.
生产厂家
- Bristol myers squibb co
- Eli lilly and co
- Lannett co inc
- Oman pharmaceutical products co llc
- Pfizer laboratories div pfizer inc
- Pharmacia and upjohn co
- Roxane laboratories inc
- Sandoz inc
- Teva pharmaceuticals usa inc
- X gen pharmaceuticals inc
封装厂家
- Akorn Inc.
- Amend
- Bausch & Lomb Inc.
- Dispensing Solutions
- Draxis Specialty Pharmaceuticals Inc.
- Hi Tech Pharmacal Co. Inc.
- Major Pharmaceuticals
- Murfreesboro Pharmaceutical Nursing Supply
- Nucare Pharmaceuticals Inc.
- Pharmedix
- Physicians Total Care Inc.
- Southwood Pharmaceuticals
- Teva Pharmaceutical Industries Ltd.
- UDL Laboratories
- X-Gen Pharmaceuticals
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
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适应症
antibacterials 抗细菌;
药理
| Indication | Topical uses include treatment for superficial eye infections caused by susceptible bacteria (used in combination with other antiinfectives), treatment of otitis externa caused by susceptible bacteria, treatment or prevention of bacterial infections in skin lesions, and use as a continuous short-term irrigant or rinse to prevent bacteriuria and gram negative rod bacteremia in abacteriuric patients with indwelling catheters. May be used orally to treat hepatic encephalopathy, as a perioperative prophylactic agent, and as an adjunct to fluid and electrolyte replacement in the treatment of diarrhea caused to enteropathogenic E. coli (EPEC). | ||||||
| Pharmacodynamics | Neomycin 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 neomycin "irreversibly" bind to specific 30S-subunit proteins and 16S rRNA. Specifically neomycin 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 | Poorly absorbed from the normal gastrointestinal tract. Although only approximately 3% of neomycin is absorbed through intact intestinal mucosa, significant amounts may be absorbed through ulcerated or denuded mucosa or if inflammation is present. | ||||||
| Volume of distribution | Not Available | ||||||
| Protein binding | Protein binding studies have shown that the degree of aminoglycoside protein binding is low and, depending upon the methods used for testing, may be between 0% and 30%. | ||||||
| Metabolism |
Neomycin undergoes negligible biotransformation after parenteral administration.
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| Route of elimination | The small absorbed fraction is rapidly distributed in the tissues and is excreted by the kidney in keeping with the degree of kidney function. | ||||||
| Half life | 2 to 3 hours | ||||||
| Clearance | Not Available | ||||||
| Toxicity | LD50 = 200 mg/kg (rat). Because of low absorption, it is unlikely that acute overdosage would occur with oral neomycin. However, prolonged administration could result in sufficient systemic drug levels to produce neurotoxicity, ototoxicity and/or nephrotoxicity. Nephrotoxicity occurs via drug accumulation in renal proximal tubular cells resulting in cellular damage. Tubular cells may regenerate despite continued exposure and nephrotoxicity is usually mild reversible. Neomycin is the most toxic aminoglycoside agent, which is thought to be due to its large number of cationic amino groups. Otoxocity occurs via drug accumulation in the endolymph and perilymph of the inner ear causing irreversible damage to hair cells in the cochlea or summit of ampullar cristae in the vestibular complex. High frequency hearing loss is followed by low frequency hearing loss. Further toxicity may cause retrograde degeneration of the auditory nerve. Vestibular toxicity may result in vertigo, nausea and vomiting, dizziness and loss of balance. | ||||||
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理化性质
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| State | solid | ||||||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| 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 |
| Colistimethate | Aminoglycosides may enhance the nephrotoxic effect of Colistimethate. Aminoglycosides may enhance the neuromuscular-blocking effect of Colistimethate. Due to the potential for additive or synergistic toxicities (including both nephrotoxicity and neuromuscular blockade) between colistimethate and the aminoglycoside antibiotics, this combination should be avoided whenever possible. If these agents must be used together, patients' renal and neuromuscular function should be monitored closely. |
| Tacrolimus | Additive renal impairment may occur during concomitant therapy with aminoglycosides such as Neomycin. Use caution during concomitant therapy. |
| Ticarcillin | Ticarcillin may reduce the serum concentration of Neomycin. Ticarcillin may inactivate Neomycin 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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