Tìm theo
Gatifloxacin
Các tên gọi khác (6 ) :
  • 1-Cyclopropyl-1,4-dihydro-6-fluoro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
  • 1-Cyclopropyl-6-fluoro- 8-methoxy-7-(3-methylpiperazin-1-yl)- 4-oxo-quinoline-3-carboxylic acid
  • AM 1155
  • Gatifloxacine
  • Gatifloxacino
  • Gatifloxacinum
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 112811-59-3
ATC: S01AE06, J01MA16
ĐG : Allergan Inc. , http://www.allergan.com
CTHH: C19H22FN3O4
PTK: 375.3941
Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. Bristol-Myers Squibb introduced Gatifloxacin in 1999 under the proprietary name Tequin® for the treatment of respiratory tract infections, having licensed the medication from Kyorin Pharmaceutical Company of Japan. Allergan produces an eye-drop formulation called Zymar®. Gatifloxacin is available as tablets and in various aqueous solutions for intravenous therapy. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H22FN3O4
Phân tử khối
375.3941
Monoisotopic mass
375.159434412
InChI
InChI=1S/C19H22FN3O4/c1-10-8-22(6-5-21-10)16-14(20)7-12-15(18(16)27-2)23(11-3-4-11)9-13(17(12)24)19(25)26/h7,9-11,21H,3-6,8H2,1-2H3,(H,25,26)
InChI Key
InChIKey=XUBOMFCQGDBHNK-UHFFFAOYSA-N
IUPAC Name
1-cyclopropyl-6-fluoro-8-methoxy-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
Traditional IUPAC Name
gatifloxacin
SMILES
COC1=C2N(C=C(C(O)=O)C(=O)C2=CC(F)=C1N1CCNC(C)C1)C1CC1
Độ tan chảy
182-185 °C
Độ hòa tan
60 mg/mL (at pH 4)
logP
2.6
logS
-2.8
pKa (strongest acidic)
5.69
pKa (Strongest Basic)
8.73
PSA
82.11 Å2
Refractivity
98.82 m3·mol-1
Polarizability
38.29 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
7
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Dược Lực Học : Gatifloxacin is a synthetic broad-spectrum 8-methoxyfluoroquinolone antibacterial agent for oral or intravenous administration. 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. Gatifloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. It should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.
Cơ Chế Tác Dụng : Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. Bristol-Myers Squibb introduced Gatifloxacin in 1999 under the proprietary name Tequin® for the treatment of respiratory tract infections, having licensed the medication from Kyorin Pharmaceutical Company of Japan. Allergan produces an eye-drop formulation called Zymar®. Gatifloxacin is available as tablets and in various aqueous solutions for intravenous therapy. [Wikipedia] The bactericidal action of Gatifloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV, which are required for bacterial DNA replication, transcription, repair, and recombination.
Dược Động Học :
▧ Absorption :
Well absorbed from the gastrointestinal tract after oral administration with absolute bioavailability of gatifloxacin is 96%
▧ Protein binding :
20%
▧ Metabolism :
Gatifloxacin undergoes limited biotransformation in humans with less than 1% of the dose excreted in the urine as ethylenediamine and methylethylenediamine metabolites
▧ Half Life :
7-14 hours
Chỉ Định : For the treatment of bronchitis, sinusitis, community-acquired pneumonia, and skin infections (abscesses, wounds) caused by S. pneumoniae, H. influenzae, S. aureus, M. pneumoniae, C. pneumoniae, L. pneumophila, S. pyogenes
Tương Tác Thuốc :
  • Aluminium Formation of non-absorbable complexes
  • Amiodarone Increased risk of cardiotoxicity and arrhythmias
  • Bepridil Increased risk of cardiotoxicity and arrhythmias
  • Bretylium Increased risk of cardiotoxicity and arrhythmias
  • Chlorpromazine Increased risk of cardiotoxicity and arrhythmias
  • Digoxin Gatifloxacin increases the effect of digoxin
  • Dihydroquinidine barbiturate Increased risk of cardiotoxicity and arrhythmias
  • Disopyramide Increased risk of cardiotoxicity and arrhythmias
  • Fluphenazine Increased risk of cardiotoxicity and arrhythmias
  • Iron Formation of non-absorbable complexes
  • Iron Dextran Formation of non-absorbable complexes
  • Magnesium Formation of non-absorbable complexes
  • Magnesium oxide Formation of non-absorbable complexes
  • Magnesium salicylate Formation of non-absorbable complexes
  • Mesoridazine Increased risk of cardiotoxicity and arrhythmias
  • Methotrimeprazine Increased risk of cardiotoxicity and arrhythmias
  • Perphenazine Increased risk of cardiotoxicity and arrhythmias
  • Prochlorperazine Increased risk of cardiotoxicity and arrhythmias
  • Promazine Increased risk of cardiotoxicity and arrhythmias
  • Promethazine Increased risk of cardiotoxicity and arrhythmias
  • Propiomazine Increased risk of cardiotoxicity and arrhythmias
  • 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.
  • Thiethylperazine Increased risk of cardiotoxicity and arrhythmias
  • Thioridazine Increased risk of cardiotoxicity and arrhythmias
  • 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.
  • 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.
  • Trifluoperazine Increased risk of cardiotoxicity and arrhythmias
  • Triflupromazine Increased risk of cardiotoxicity and arrhythmias
  • 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).
  • Zinc Formation of non-absorbable complexes
  • Ziprasidone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
Liều Lượng & Cách Dùng : Solution - Ophthalmic
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Tequin
  • Công ty :
    Sản phẩm biệt dược : Zymar
  • Công ty :
    Sản phẩm biệt dược : ZYMAXID
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01044
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5379
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506159
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07661
ChemSpider
http://www.chemspider.com/Chemical-Structure.5186.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0023-9218-05
PharmGKB
http://www.pharmgkb.org/drug/PA449738
Wikipedia
http://en.wikipedia.org/wiki/Gatifloxacin
RxList
http://www.rxlist.com/cgi/generic3/gatifloxacin.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/zym1676.shtml
Drugs.com
http://www.drugs.com/cdi/gatifloxacin-drops.html
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