Tìm theo
Lomefloxacin
Các tên gọi khác (6 ) :
  • (+-)-1-Ethyl-6,8-difluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
  • 1,4-Dihydro-6,8-difluoro-1-ethyl-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
  • LFLX
  • Lomefloxacine
  • Lomefloxacino
  • Lomefloxacinum
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 98079-51-7
ATC: J01MA07, S01AE04
ĐG : GD Searle LLC
CTHH: C17H19F2N3O3
PTK: 351.3479
Lomefloxacin is a fluoroquinolone antibiotic, used to treat bacterial infections including bronchitis and urinary tract infections. It is also used to prevent urinary tract infections prior to surgery.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H19F2N3O3
Phân tử khối
351.3479
Monoisotopic mass
351.139447899
InChI
InChI=1S/C17H19F2N3O3/c1-3-21-8-11(17(24)25)16(23)10-6-12(18)15(13(19)14(10)21)22-5-4-20-9(2)7-22/h6,8-9,20H,3-5,7H2,1-2H3,(H,24,25)
InChI Key
InChIKey=ZEKZLJVOYLTDKK-UHFFFAOYSA-N
IUPAC Name
1-ethyl-6,8-difluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
Traditional IUPAC Name
lomefloxacin
SMILES
CCN1C=C(C(O)=O)C(=O)C2=CC(F)=C(N3CCNC(C)C3)C(F)=C12
Độ tan chảy
239-240.5 °C
Độ hòa tan
27.2 mg/mL
logP
-0.30
logS
-3.5
pKa (strongest acidic)
5.64
pKa (Strongest Basic)
8.7
PSA
72.88 Å2
Refractivity
90.11 m3·mol-1
Polarizability
34.8 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
6
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Lomefloxacin is a fluoroquinolone antibiotic used to treat chronic bronchitis, as well as complicated and uncomplicated urinary tract infections. It is also used as a prophylactic or preventative treatment to prevent urinary tract infections in patients undergoing transrectal or transurethral surgical procedures. Flouroquinolones such as lomefloxacin possess excellent activity against gram-negative aerobic bacteria such as E.coli and Neisseria gonorrhoea as well as gram-positive bacteria including S. pneumoniae and Staphylococcus aureus. They also posses effective activity against shigella, salmonella, campylobacter, gonococcal organisms, and multi drug resistant pseudomonas and enterobacter.
Cơ Chế Tác Dụng : Lomefloxacin is a fluoroquinolone antibiotic, used to treat bacterial infections including bronchitis and urinary tract infections. It is also used to prevent urinary tract infections prior to surgery. Lomefloxacin is a bactericidal fluoroquinolone agent with activity against a wide range of gram-negative and gram-positive organisms. The bactericidal action of lomefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited.
Dược Động Học :
▧ Absorption :
Rapid and nearly complete with approximately 95% to 98% of a single oral dose being absorbed.
▧ Protein binding :
10%
▧ Metabolism :
Minimally metabolized although 5 metabolites have been identified in human urine. 65% appears as the parent drug in urine and 9% as the glucuronide metabolite.
▧ Route of Elimination :
The urinary excretion of lomefloxacin was virtually complete within 72 hours after cessation of dosing, with approximately 65% of the dose being recovered as parent drug and 9% as its glucuronide metabolite.
▧ Half Life :
8 hours
▧ Clearance :
* 271 mL/min/1.73 m2 [creatinine clearance of 110 mL/min/1.73 m2] * 31 mL/min/1.73 m2 [creatinine clearance of 0 mL/min/1.73 m2]
Độc Tính : Adverse reactions include peripheral neuropathy, nervousness, agitation, anxiety, and phototoxic events (rash, itching, burning) due to sunlight exposure.
Chỉ Định : For the treatment of bacterial infections of the respiratory tract (chronic bronchitis) and urinary tract, and as a pre-operative prophylactic to prevent urinary tract infection caused by: S.pneumoniae, H.influenzae, S.aureus, P.aeruginosa, E. cloacae, P. mirabilis, C. civersus, S. asprphyticus, E.coli, and K.pneumoniae.
Tương Tác Thuốc :
  • Calcium Formation of non-absorbable complexes
  • Calcium Acetate Calcium salts such as calcium acetate may decrease the absorption of quinolone antibiotics such as lomefloxacin. Of concern only with oral administration of both agents. Interactions can be minimized by administering oral quinolone at least 2 hours before, or 6 hours after, the dose of an oral calcium supplement. Monitor for decreased therapeutic effects of oral quinolones if administered with oral calcium supplements.
  • Iron Dextran Formation of non-absorbable complexes
  • Magnesium Formation of non-absorbable complexes
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Bareon
  • Công ty :
    Sản phẩm biệt dược : Maxaquin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00978
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3948
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508499
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07078
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02318
ChemSpider
http://www.chemspider.com/Chemical-Structure.3811.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50240373
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0025-5501-01
PharmGKB
http://www.pharmgkb.org/drug/PA164749165
Wikipedia
http://en.wikipedia.org/wiki/Lomefloxacin
RxList
http://www.rxlist.com/cgi/generic2/lomefloxacin.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/max1249.shtml
Drugs.com
http://www.drugs.com/cdi/lomefloxacin.html
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