药品详细
Moxifloxacin (莫西沙星 )
化学结构式图
中文名
莫西沙星
英文名
Moxifloxacin
分子式
Not Available
化学名
7-[(4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridin-6-yl]-1-cyclopropyl-6-fluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
分子量
Average: 401.4314
Monoisotopic: 401.175084476
Monoisotopic: 401.175084476
CAS号
354812-41-2
ATC分类
J01M 未知;S01A 抗感染药
药物类型
small molecule
阶段
商品名
Avelox;Avelox I.V.;Vigamox;
同义名
BAY 12-8039;moxifloxacin;Moxifloxacin HCl;Moxifloxacin hydrochloride;
基本介绍
Moxifloxacin is a synthetic fluoroquinolone antibiotic agent. Bayer AG developed the drug (initially called BAY 12-8039) and it is marketed worldwide (as the hydrochloride) under the brand name Avelox (in some countries also Avalox) for oral treatment.
生产厂家
- Alcon inc
- Bayer Healthcare Pharmaceuticals
- Bayer healthcare pharmaceuticals inc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference |
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剂型
| Form | Route | Strength |
|---|---|---|
| Solution | Intravenous | |
| Solution | Ophthalmic | |
| Tablet | Oral |
规格
| Unit description | Cost | Unit |
|---|---|---|
| Vigamox 0.5% Solution 3ml Bottle | 90.72 USD | bottle |
| Vigamox 0.5% eye drops | 27.22 USD | ml |
| Avelox 400 mg tablet | 16.68 USD | tablet |
| Avelox abc pack 400 mg tablet | 16.35 USD | tablet |
| Avelox iv 400 mg/250 ml | 0.17 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 the treatment of sinus and lung infections such as sinusitis, pneumonia, and secondary infections in chronic bronchitis. Also for the treatment of bacterial conjunctivitis (pinkeye). |
| Pharmacodynamics | Moxifloxacin is a quinolone/fluoroquinolone antibiotic. Moxifloxacin can be used to treat infections caused by the following bacteria: Aerobic Gram-positive microorganisms: Corynebacterium species, Micrococcus luteus, Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus warneri, Streptococcus pneumoniae, and Streptococcus viridans group. Aerobic Gram-negative microorganisms: Acinetobacter lwoffii, Haemophilus influenzae, and Haemophilus parainfluenzae. Other microorganisms: Chlamydia trachomatis. Moxifloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase, which allows the untwisting required to replicate one DNA double helix into two. Notably the drug has 100 times higher affinity for bacterial DNA gyrase than for mammalian. Moxifloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. |
| Mechanism of action | The bactericidal action of moxifloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV. DNA gyrase is an essential enzyme that is involved in the replication, transcription and repair of bacterial DNA. Topoisomerase IV is an enzyme known to play a key role in the partitioning of the chromosomal DNA during bacterial cell division. |
| Absorption | Well absorbed from the gastrointestinal tract. Absolute oral bioavailability is approximately 90%. Food has little effect on absorption. |
| Volume of distribution |
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| Protein binding | 50% bound to serum proteins, independent of drug concentration. |
| Metabolism |
Approximately 52% or oral or intravenous dose is metabolized via glucuronide and sulphate conjugation. The cytochrome P450 system is not involved in metabolism. The sulphate conjugate accounts for 38% of the dose, and the glucuronide conjugate accounts for 14% of the dose. |
| Route of elimination | Approximately 45% of an oral or intravenous dose of moxifloxacin is excreted as unchanged drug (~20% in urine and ~25% in feces). |
| Half life | 11.5-15.6 hours (single dose, oral) |
| Clearance |
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| Toxicity | Symptoms of overdose include CNS and gastrointestinal effects such as decreased activity, somnolence, tremor, convulsions, vomiting, and diarrhea. The minimal lethal intravenous dose in mice and rats is 100 mg/kg. |
| Affected organisms |
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| Pathways | Not Available |
理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | 238-242 oC | ||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Acenocoumarol | The quinolone antibiotic, moxifloxacin, may increase the anticoagulant effect of acenocoumarol. |
| Aluminium | Formation of non-absorbable complexes |
| Amiodarone | Increased risk of cardiotoxicity and arrhythmias |
| Anisindione | The quinolone antibiotic, moxifloxacin, may increase the anticoagulant effect of anisindione. |
| Artemether | Additive QTc-prolongation may occur. Concomitant therapy should be avoided. |
| Bepridil | Increased risk of cardiotoxicity and arrhythmias |
| Bretylium | Increased risk of cardiotoxicity and arrhythmias |
| Calcium | Formation of non-absorbable complexes |
| Dicumarol | The quinolone antibiotic, moxifloxacin, may increase the anticoagulant effect of dicumarol. |
| Dihydroquinidine barbiturate | Increased risk of cardiotoxicity and arrhythmias |
| Disopyramide | Increased risk of cardiotoxicity and arrhythmias |
| Erythromycin | Increased risk of cardiotoxicity and arrhythmias |
| Iron | Formation of non-absorbable complexes |
| Iron Dextran | Formation of non-absorbable complexes |
| Josamycin | Increased risk of cardiotoxicity and arrhythmias |
| Lumefantrine | Additive QTc-prolongation may occur. Concomitant therapy should be avoided. |
| Magnesium | Formation of non-absorbable complexes |
| Magnesium oxide | Formation of non-absorbable complexes |
| Quinidine | Increased risk of cardiotoxicity and arrhythmias |
| Quinidine barbiturate | Increased risk of cardiotoxicity and arrhythmias |
| Quinupristin | This combination presents an increased risk of toxicity |
| Sotalol | Increased risk of cardiotoxicity and arrhythmias |
| Sucralfate | Formation of non-absorbable complexes |
| Tacrolimus | Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. |
| Thiothixene | May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration. |
| Tizanidine | Moxifloxacin may decrease the metabolism and clearance of Tizanidine. Consider alternate therapy or use caution during co-administration. |
| Toremifene | Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration. |
| Trimipramine | Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. |
| Voriconazole | Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). |
| Vorinostat | Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). |
| Warfarin | The quinolone antibiotic, moxifloxacin, may increase the anticoagulant effect of warfarin. |
| Zinc | Formation of non-absorbable complexes |
| Ziprasidone | Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated. |
| Zuclopenthixol | Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). |
食物相互作用
- Take without regard to meals. Drink liberally. Absorption is not affected by lipid-rich meals or yogourt.
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