药品详细
Tetracycline(四环素)
化学结构式图
中文名
四环素
英文名
Tetracycline
分子式
C22H24N2O8
化学名
(4S,4aS,5aS,6S,12aS)-4-(dimethylamino)-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide
分子量
Average: 444.4346
Monoisotopic: 444.153265754
Monoisotopic: 444.153265754
CAS号
60-54-8
ATC分类
A01A 未知;D06A 未知;J01A 未知;S01A 抗感染药;S02A 未知;S03A 未知;A01A 未知;S01A 抗感染药;J01A 未知;J01A 未知;S01A 抗感染药;G01A 未知;D06A 未知;D06A 未知;J01A 未知
药物类型
small molecule
阶段
approved
商品名
Abramycin;Abricycline;Achromycin;Achromycin V;Actisite;Agromicina;Ambramicina;Ambramycin;Amycin;Bio-Tetra;Biocycline;Bristaciclin;Bristaciclina;Bristacycline;Cefracycline;Ciclibion;Copharlan;Criseociclina;Cyclopar;Cytome;Democracin;Deschlorobiomycin;Dumocyclin;Enterocycline;Hostacyclin;Lexacycline;Limecycline;Liquamycin;Medocycline;Mericycline;Micycline;Neocycline;Oletetrin;Omegamycin;Orlycycline;Panmycin;Polycycline;Polyotic;Purocyclina;Resteclin;Retet;Robitet;Roviciclina;SK-Tetracycline;Solvocin;Sumycin;TAC;Tetra-CO;Tetrabon;Tetrachel;Tetracycl;Tetracycline II;Tetracyn;Tetradecin;Tetrafil;Tetramed;Tetraverine;Tetrex;Topicycline;Tsiklomistsin;Tsiklomitsin;Veracin;Vetacyclinum;
同义名
Anhydrotetracycline;TC;Tetracycline HCl;
基本介绍
Tetracycline is a broad spectrum polyketide antibiotic produced by the Streptomyces genus of Actinobacteria. It exerts a bacteriostatic effect on bacteria by binding reversible to the bacterial 30S ribosomal subunit and blocking incoming aminoacyl tRNA from binding to the ribosome acceptor site. It also binds to some extent to the bacterial 50S ribosomal subunit and may alter the cytoplasmic membrane causing intracellular components to leak from bacterial cells.
生产厂家
- Angus chemical co
- Apothecon inc div bristol myers squibb
- Bristol laboratories inc div bristol myers co
- Heritage pharmaceuticals inc
- Ivax pharmaceuticals inc sub teva pharmaceuticals usa
- Lederle laboratories div american cyanamid co
- On site therapeutics inc
- Par pharmaceutical
- Par pharmaceutical inc
- Pfipharmecs div pfizer inc
- Pfizer laboratories div pfizer inc
- Pharmacia and upjohn co
- Shire development inc
- Solvay pharmaceuticals
- Storz ophthalmics inc sub american cyanamid co
- Warner chilcott div warner lambert co
- Wyeth ayerst laboratories
封装厂家
- Advanced Pharmaceutical Services Inc.
- Aidarex Pharmacuticals LLC
- Apotheca Inc.
- A-S Medication Solutions LLC
- Axcan Pharma Inc.
- Barr Pharmaceuticals
- Belgomex Sprl
- Blenheim Pharmacal
- Bryant Ranch Prepack
- C.O. Truxton Inc.
- Central Texas Community Health Centers
- Comprehensive Consultant Services Inc.
- Coupler Enterprises Inc.
- Direct Dispensing Inc.
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Draxis Specialty Pharmaceuticals Inc.
- E.R. Squibb and Sons LLC
- Gallipot
- Global Pharmaceuticals
- Golden State Medical Supply Inc.
- Goldline Laboratories Inc.
- Group Health Cooperative
- H and H Laboratories
- H.J. Harkins Co. Inc.
- Heartland Repack Services LLC
- Ivax Pharmaceuticals
- Kaiser Foundation Hospital
- Laboratorios Atral Sarl
- Liberty Pharmaceuticals
- Major Pharmaceuticals
- Medisca Inc.
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Nucare Pharmaceuticals Inc.
- Palmetto Pharmaceuticals Inc.
- Par Pharmaceuticals
- Patient First Corp.
- PCA LLC
- PD-Rx Pharmaceuticals Inc.
- Pharmedix
- Physicians Total Care Inc.
- Preferred Pharmaceuticals Inc.
- Prepackage Specialists
- Prepak Systems Inc.
- Prometheus Laboratories Inc.
- Proter SPA
- Qualitest
- Rebel Distributors Corp.
- Remedy Repack
- Sandhills Packaging Inc.
- Sino American Shanghai Squibb Pharmaceutical Ltd.
- Southwood Pharmaceuticals
- Talbert Medical Management Corp.
- Tya Pharmaceuticals
- Veratex Corp.
- Warner Chilcott Co. Inc.
- Watson Pharmaceuticals
参考
剂型
规格
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 | Used to treat bacterial infections such as Rocky Mountain spotted fever, typhus fever, tick fevers, Q fever, rickettsialpox and Brill-Zinsser disease. May be used to treat infections caused by Chlamydiae spp., B. burgdorferi (Lyme disease), and upper respiratory infections caused by typical (S. pneumoniae, H. influenzae, and M. catarrhalis) and atypical organisms (C. pneumoniae, M. pneumoniae, L. pneumophila). May also be used to treat acne. Tetracycline may be an alternative drug for people who are allergic to penicillin. | ||||||
Pharmacodynamics | Tetracycline is a short-acting antibiotic that inhibits bacterial growth by inhibiting translation. It binds to the 30S ribosomal subunit and prevents the amino-acyl tRNA from binding to the A site of the ribosome. It also binds to some extent to the 50S ribosomal subunit. This binding is reversible in nature. Additionally tetracycline may alter the cytoplasmic membrane of bacteria causing leakage of intracellular contents, such as nucleotides, from the cell. | ||||||
Mechanism of action | Tetracycline passively diffuses through porin channels in the bacterial membrane and reversibly binds to the 30S ribosomal subunit, preventing binding of tRNA to the mRNA-ribosome complex, and thus interfering with protein synthesis. | ||||||
Absorption | Bioavailability is less than 40% when administered via intramuscular injection, 100% intravenously, and 60-80% orally (fasting adults). Food and/or milk reduce GI absorption of oral preparations of tetracycline by 50% or more. | ||||||
Volume of distribution | Not Available | ||||||
Protein binding | 20 - 67% protein bound | ||||||
Metabolism |
Not metabolized
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Route of elimination | They are concentrated by the liver in the bile and excreted in the urine and feces at high concentrations in a biologically active form. | ||||||
Half life | 6-12 hours | ||||||
Clearance | Not Available | ||||||
Toxicity | LD50=808mg/kg (orally in mice) | ||||||
Affected organisms |
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Pathways |
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理化性质
Properties | |||||||||||||||||||||||||||||||||||||||||||
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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 |
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Acenocoumarol | Tetracycline may increase the anticoagulant effect of acenocoumarol. |
Acitretin | Increased risk of intracranial hypertension |
Aluminium | Formation of non-absorbable complexes |
Amoxicillin | Possible antagonism of action |
Ampicillin | Possible antagonism of action |
Anisindione | Tetracycline may increase the anticoagulant effect of anisindione. |
Atovaquone | Tetracycline may decrease the effect of atovaquone. |
Attapulgite | Formation of non-absorbable complexes |
Azlocillin | Possible antagonism of action |
Aztreonam | Possible antagonism of action |
Bacampicillin | Possible antagonism of action |
Bexarotene | Tetracycline may enhance the adverse/toxic effect of Retinoic Acid Derivatives. Due to the risk of developing pseudotumor cerebri (also known as intracranial hypertension), avoid this combination of drugs if possible. If used concomitantly, monitor for evidence of this interaction (eg, dizziness, diplopia, headache). |
Bismuth Subsalicylate | Formation of non-absorbable complexes |
Calcium | Formation of non-absorbable complexes |
Calcium Acetate | Calcium salts such as calcium acetate may decrease the serum concentration of tetracycline derivatives such as tetracycline. In general, the coadministration of oral calcium salts and oral tetracycline derivatives should be avoided. Interactions may be able to be minimized by administering oral calcium preparations several hours before or after the dose of the oral tetracycline derivatives. Even with dose separation, therapy may still be compromised. Monitor for decreased therapeutic effect of oral tetracycline derivatives. |
Calcium Chloride | Calcium salts such as calcium chloride may decrease the serum concentration of tetracycline derivatives such as tetracycline. In general, the coadministration of oral calcium salts and oral tetracycline derivatives should be avoided. Interactions may be able to be minimized by administering oral calcium preparations several hours before or after the dose of the oral tetracycline derivatives. Even with dose separation, therapy may still be compromised. Monitor for decreased therapeutic effect of oral tetracycline derivatives. |
Carbenicillin | Possible antagonism of action |
Clavulanate | Possible antagonism of action |
Cloxacillin | Possible antagonism of action |
Colesevelam | Bile acid sequestrants such as colesevelam may decrease the absorption of Tetracycline Derivatives. Monitor for decreased therapeutic effects of tetracycline derivatives if coadministered with a bile acid sequestrant. If these agents are used concomitantly, separate doses 2 or more hours to minimize the interaction. The manufacturer of colesevelam suggests that drugs should be administered at least 1 hour before or 4 hours after colesevelam. |
Cyclacillin | Possible antagonism of action |
Dicloxacillin | Possible antagonism of action |
Dicumarol | Tetracycline may increase the anticoagulant effect of dicumarol. |
Dihydroxyaluminium | Formation of non-absorbable complexes |
Ethinyl Estradiol | This anti-infectious agent could decrease the effect of the oral contraceptive |
Etretinate | Increased risk of intracranial hypertension |
Flucloxacillin | Possible antagonism of action |
Hetacillin | Possible antagonism of action |
Iron | Formation of non-absorbable complexes |
Iron Dextran | Formation of non-absorbable complexes |
Isotretinoin | Increased risk of intracranial hypertension |
Magnesium | Formation of non-absorbable complexes |
Magnesium salicylate | Formation of non-absorbable complexes |
Mestranol | This anti-infectious agent could decrease the effect of the oral contraceptive |
Methicillin Acyl-Serine | Possible antagonism of action |
Methotrexate | Tetracycline may increase methotrexate toxicity. |
Methoxyflurane | Tetracycline may increase the renal toxicity of methoxyflurane. |
Mezlocillin | Possible antagonism of action |
Nafcillin | Possible antagonism of action |
Oxacillin | Possible antagonism of action |
Penicillin G | Possible antagonism of action |
Penicillin V | Possible antagonism of action |
Piperacillin | Possible antagonism of action |
Pivampicillin | Possible antagonism of action |
Pivmecillinam | Possible antagonism of action |
Quinapril | Quinapril may decrease the absorption of tetracycline. |
Tamsulosin | Tetracycline, a CYP3A4 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Tetracycline is initiated, discontinued, or dose changed. |
Tazobactam | Possible antagonism of action |
Ticarcillin | Tetracycline may reduce the effect of Ticarcillin by inhibiting bacterial growth. Ticarcillin exerts its effects on actively growing bacteria. To achieve synergism, Ticarcillin should be administered at least 2 hours prior to using Tetracycline. |
Tolterodine | Tetracycline may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity. |
Tramadol | Tetracycline may increase Tramadol toxicity by decreasing Tramadol metabolism and clearance. |
Trazodone | The CYP3A4 inhibitor, Tetracycline, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Tetracycline is initiated, discontinued or dose changed. |
Tretinoin | Demeclocycline may increase the adverse effects of oral Tretinoin. Increase risk of pseudotumour cerebri. Concurrent therapy should be avoided. |
Trisalicylate-choline | Formation of non-absorbable complexes |
Warfarin | Tetracycline may increase the anticoagulant effect of warfarin. |
Zinc | Formation of non-absorbable complexes |
食物相互作用
- Avoid milk, calcium containing dairy products, iron, antacids, or aluminium salts 2 hours before or 6 hours after using antacids while on this medication.
- Take on empty stomach: 1 hour before or 2 hours after meals.
- Take with a full glass of water.