药品详细
Streptomycin(链霉素)
化学结构式图
中文名
链霉素
英文名
Streptomycin
分子式
C21H39N7O12
化学名
1-[(1S,2R,3R,4S,5R,6R)-3-carbamimidamido-6-{[(2R,3R,4R,5S)-3-{[(2S,3S,4S,5R,6S)-4,5-dihydroxy-6-(hydroxymethyl)-3-(methylamino)oxan-2-yl]oxy}-4-formyl-4-hydroxy-5-methyloxolan-2-yl]oxy}-2,4,5-trihydroxycyclohexyl]guanidine
分子量
Average: 581.5741
Monoisotopic: 581.265669747
Monoisotopic: 581.265669747
CAS号
57-92-1
ATC分类
A07A 未知;J01G 未知;S01A 抗感染药
药物类型
small molecule
阶段
approved
商品名
Kantrex;
同义名
Streptomycin a Sulfate;Streptomycin Sesquisulfate Hydrate;Streptomycin Sulfate;Streptomycin Sulphate;Streptomycin, Sulfate Salt;
基本介绍
Streptomycin is an aminoglycoside antibiotic produced by the soil actinomycete Streptomyces griseus. It acts by binding to the 30S ribosomal subunit of susceptible organisms and disrupting the initiation and elongation steps in protein synthesis. It is bactericidal due to effects that are not fully understood.
生产厂家
- Eli lilly and co
- John d copanos and co inc
- Pfizer laboratories div pfizer inc
- X gen pharmaceuticals inc
封装厂家
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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| Substructures |
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适应症
antibacterials 抗细菌;
药理
| Indication | For the treatment of tuberculosis. May also be used in combination with other drugs to treat tularemia (Francisella tularensis), plague (Yersia pestis), severe M. avium complex, brucellosis, and enterococcal endocarditis (e.g. E. faecalis, E. faecium). | ||||||
| Pharmacodynamics | Streptomycin 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 Streptomycin "irreversibly" bind to specific 30S-subunit proteins and 16S rRNA. Specifically Streptomycin 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 | Rapidly absorbed after intramuscular injection with peak serum concentrations attained after 1 - 2 hours. Not absorbed in the GI tract. | ||||||
| Volume of distribution | Not Available | ||||||
| Protein binding | Not Available | ||||||
| Metabolism |
Not Available
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| Route of elimination | Small amounts are excreted in milk, saliva, and sweat. Streptomycin is excreted by glomerular filtration. | ||||||
| Half life | 5 - 6 hours in adults with normal renal function | ||||||
| Clearance | Not Available | ||||||
| Toxicity | Nephrotoxic and ototoxic potential. Nephrotoxicity is caused by accumulation of the drug in proximal renal tubular cells, which results in cellular damage. Tubular cells may regenerate despite continued exposure and nephrotoxicity is usually mild and reversible. Streptomycin is the least nephrotoxic of the aminoglycosides owing to the small number of cationic amino groups in its structure. Otoxocity occurs via drug accumulation in the endolymph and perilymph of the inner ear. Accumulation causes irreversible damage to hair cells of the cochlea or summit of the ampullar cristae of the vestibular complex. High frequency hearing loss precedes low frequency hearing loss. Further toxicity may result in retrograde degeneration of the auditory nerve. Vestibular toxicity may result in vertigo, nausea and vomiting, dizziness and loss of balance. LD50=430 mg/kg (Orally in rats with Streptomycin Sulfate); Side effects include nausea, vomiting, and vertigo, paresthesia of face, rash, fever, urticaria, angioneurotic edema, and eosinophilia. | ||||||
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理化性质
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| State | solid | ||||||||||||||||||||||||||||||||||||||||||
| Experimental 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 |
| 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. |
| Ethacrynic acid | Increased ototoxicity |
| Furosemide | Increased ototoxicity |
| Tacrolimus | Additive renal impairment may occur during concomitant therapy with aminoglycosides such as Streptomycin. Use caution during concomitant therapy. |
| Ticarcillin | Ticarcillin may reduce the serum concentration of Streptomycin. Ticarcillin may inactivate Streptomycin 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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