药品详细
Gentamicin (庆大霉素 )
化学结构式图
中文名
庆大霉素
英文名
Gentamicin
分子式
Not Available
化学名
2-{[4,6-diamino-3-({3-amino-6-[1-(methylamino)ethyl]oxan-2-yl}oxy)-2-hydroxycyclohexyl]oxy}-5-methyl-4-(methylamino)oxane-3,5-diol
分子量
Average: 477.5954
Monoisotopic: 477.316248755
Monoisotopic: 477.316248755
CAS号
1403-66-3
ATC分类
D06A 未知;J01G 未知;S01A 抗感染药;S02A 未知;S03A 未知
药物类型
small molecule
阶段
商品名
Alcomicin;Apogen;Bristagen;G-Mycin;G-Myticin;Garamycin;Garamycin Otic Solution;Genoptic Liquifilm;Genoptic S.O.P.;Gentacidin;Gentafair;Gentak;Gentamar;Gentamcin Sulfate;Jenamicin;Ocu-Mycin;Spectro-Genta;U-gencin;
同义名
基本介绍
A complex of three different closely related aminoglycoside sulfates, Gentamicins C1, C2, and C1, obtained from Micromonospora purpurea and related species. They are broad-spectrum antibiotics, but may cause ear and kidney damage. They act to inhibit protein synthesis (genetic translation). [PubChem]
生产厂家
- Abbott laboratories pharmaceutical products div
- Akorn inc
- Alcon universal ltd
- Allergan
- Alpharma us pharmaceuticals division
- Altana inc
- App pharmaceuticals llc
- B braun medical inc
- Bausch and lomb pharmaceuticals inc
- Baxter healthcare corp
- Baxter healthcare corp anesthesia and critical care
- Bristol laboratories inc div bristol myers co
- E fougera div altana inc
- Falcon pharmaceuticals ltd
- Hospira inc
- International medication systems ltd
- Kalapharm inc
- King pharmaceuticals inc
- Novartis pharmaceuticals corp
- Paco research corp
- Perrigo new york inc
- Pharmaceutical specialist assoc
- Pharmacia and upjohn co
- Pharmaderm div altana inc
- Pharmafair inc
- Schering corp sub schering plough corp
- Solopak laboratories inc
- Taro pharmaceuticals usa inc
- Teva parenteral medicines inc
- Watson laboratories inc
- Wyeth ayerst laboratories
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
| Form | Route | Strength |
|---|---|---|
| Cream | Topical | |
| Liquid | Ophthalmic | |
| Ointment | Ophthalmic | |
| Ointment | Topical | |
| Solution | Auricular (otic) | |
| Solution | Intravenous | |
| Solution | Ophthalmic | |
| Solution / drops | Auricular (otic) | |
| Solution / drops | Ophthalmic |
规格
| Unit description | Cost | Unit |
|---|---|---|
| Gentak 0.3% Ointment 3.5 gm Tube | 19.99 USD | tube |
| Gentamicin Sulfate 0.1% Cream 15 gm Tube | 12.99 USD | tube |
| Gentamicin Sulfate 0.1% Ointment 15 gm Tube | 11.99 USD | tube |
| Gentamicin Sulfate 0.3% Solution 5ml Bottle | 11.99 USD | bottle |
| Gentamicin sulfate powder | 5.05 USD | g |
| Gentamicin Sulfate 10 mg/ml Solution 2ml Vial | 5.0 USD | vial |
| Gentamicin 40 mg/ml | 2.82 USD | ml |
| Gentamicin ped 10 mg/ml vial | 2.4 USD | ml |
| Gentak 3 mg/ml eye drops | 1.91 USD | ml |
| Gentamicin 3 mg/ml eye drops | 1.89 USD | ml |
| Gentamicin 10 mg/ml vial | 1.29 USD | ml |
| Garamycin 0.3 % Ointment | 1.2 USD | g |
| Sandoz Gentamicin Sulfate 0.3 % Ointment | 1.2 USD | g |
| Garamycin 0.3 % Solution | 0.75 USD | ml |
| Sandoz Gentamicin Sulfate 0.3 % Solution | 0.75 USD | ml |
| Gentamicin 40 mg/ml vial | 0.45 USD | ml |
| Ratio-Gentamicin Sulfate 0.1 % Cream | 0.43 USD | g |
| Ratio-Gentamicin Sulfate 0.1 % Ointment | 0.37 USD | g |
| Gentamicin 0.1% cream | 0.16 USD | g |
| Iso gentamicin 120 mg/100 ml | 0.09 USD | ml |
| Gentamicin 90 mg/ns 100 ml pb | 0.05 USD | ml |
| Isoton gentamicin 40 mg/100 ml | 0.05 USD | ml |
| Gentamicin 60 mg/ns 100 ml pb | 0.04 USD | ml |
| Gentamicin 100 mg/ns 100 ml | 0.03 USD | ml |
| Gentamicin 80 mg/ns 100 ml pb | 0.03 USD | ml |
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 serious infections caused by susceptible strains of the following microorganisms: P. aeruginosa, Proteus species (indole-positive and indole-negative), E. coli, Klebsiella-Enterobactor-Serratia species, Citrobacter species and Staphylococcus species (coagulase-positive and coagulase-negative). | ||||||
| Pharmacodynamics | Gentamicin is a broad spectrum 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 gentamicin "irreversibly" bind to specific 30S-subunit proteins and 16S rRNA. Specifically gentamicin 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 | Injections lead to peak serum concentrations in 30-60 minutes. Topical gentamicin is readily absorbed from large burned, denuded, or granulating areas but not through intact skin. Absorption of gentamicin is faster and greater with the cream compared to the ointment. Gentamicin is absorbed in small quantities following topical application to the eye. Gentamicin is also absorbed in small amounts following topical application to the ear (especially if the eardrum is perforated or if tissue damage is present). Gentamicin is very poorly absorbed orally. | ||||||
| Volume of distribution | Not Available | ||||||
| Protein binding | Low (between 0 and 30%) | ||||||
| Metabolism | |||||||
| Route of elimination | Not Available | ||||||
| Half life | 3-3½ hours in infants one week to six months of age; this increases to 5½ hours in full-term and large premature infants less than one week old. | ||||||
| Clearance | Not Available | ||||||
| Toxicity | Mild and reversible nephrotoxicity may be observed in 5 - 25% of patients. Gentamicin accumulates in proximal renal tubular cells and causes cell damage. 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. Mouse, intravenous LD50: 52 mg/kg; rat, intravenous LD50: 96 mg/kg. | ||||||
| Affected organisms |
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| Pathways |
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理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | 105°C (218-237°C as sulfate salt) | ||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Atracurium | The agent increases the effect of muscle relaxant |
| Bumetanide | Increased ototoxicity |
| Cefamandole | Increased risk of nephrotoxicity |
| Cefazolin | Increased risk of nephrotoxicity |
| Cefonicid | Increased risk of nephrotoxicity |
| Cefoperazone | Increased risk of nephrotoxicity |
| Ceforanide | Increased risk of nephrotoxicity |
| Cefotaxime | Increased risk of nephrotoxicity |
| Cefotetan | Increased risk of nephrotoxicity |
| Cefoxitin | Increased risk of nephrotoxicity |
| Cefradine | Increased risk of nephrotoxicity |
| Ceftazidime | Increased risk of nephrotoxicity |
| Ceftizoxime | Increased risk of nephrotoxicity |
| Ceftriaxone | Increased risk of nephrotoxicity |
| Cefuroxime | Increased risk of nephrotoxicity |
| Cephalothin Group | Increased risk of nephrotoxicity |
| Cephapirin | Increased risk of nephrotoxicity |
| Cisplatin | Increased risk of nephrotoxicity |
| Doxacurium | The agent increases the effect of muscle relaxant |
| Ethacrynic acid | Increased ototoxicity |
| Furosemide | Increased ototoxicity |
| Gallamine Triethiodide | The agent increases the effect of muscle relaxant |
| Metocurine | The agent increases the effect of muscle relaxant |
| Mivacurium | The agent increases the effect of muscle relaxant |
| Pancuronium | The agent increases the effect of muscle relaxant |
| Pipecuronium | The agent increases the effect of muscle relaxant |
| Rocuronium | The agent increases the effect of muscle relaxant |
| Succinylcholine | The agent increases the effect of muscle relaxant |
| Tacrolimus | Additive renal impairment may occur during concomitant therapy with aminoglycosides such as Gentamicin. Use caution during concomitant therapy. |
| Thalidomide | Thalidomide increases the renal toxicity of the aminoglycoside |
| Ticarcillin | Ticarcillin may reduce the serum concentration of Gentamicin. Ticarcillin may inactivate Gentamicin in vitro and the two agents should not be administered simultaneously through the same IV line. |
| Torasemide | Increased ototoxicity |
| Tubocurarine | The agent increases the effect of muscle relaxant |
| Vecuronium | The agent increases the effect of muscle relaxant |
食物相互作用
Not Available
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