Tìm theo
Gemifloxacin
Các tên gọi khác (3) :
  • Factiv
  • Gemifloxacin mesilate
  • gemifloxacin mesylate
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 175463-14-6
ATC: J01MA15
ĐG : Cornerstone Pharmacy , http://www.cpsrx.com
CTHH: C18H20FN5O4
PTK: 389.3809
Gemifloxacin is an oral broad-spectrum quinolone antibacterial agent used in the treatment of acute bacterial exacerbation of chronic bronchitis and mild-to-moderate pneumonia. Gemifloxacin acts by inhibiting DNA synthesis through the inhibition of both DNA gyrase and topoisomerase IV, which are essential for bacterial growth.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C18H20FN5O4
Phân tử khối
389.3809
Monoisotopic mass
389.149932358
InChI
InChI=1S/C18H20FN5O4/c1-28-22-14-8-23(6-9(14)5-20)17-13(19)4-11-15(25)12(18(26)27)7-24(10-2-3-10)16(11)21-17/h4,7,9-10H,2-3,5-6,8,20H2,1H3,(H,26,27)/b22-14+
InChI Key
InChIKey=ZRCVYEYHRGVLOC-HYARGMPZSA-N
IUPAC Name
7-[(4Z)-3-(aminomethyl)-4-(methoxyimino)pyrrolidin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid
Traditional IUPAC Name
gemifloxacin
SMILES
CO\N=C1/CN(CC1CN)C1=NC2=C(C=C1F)C(=O)C(=CN2C1CC1)C(O)=O
Độ hòa tan
Freely soluble at neutral pH (350 mg/mL at 37 °C, pH 7.0).
logP
2.3
logS
-3.3
pKa (strongest acidic)
5.53
pKa (Strongest Basic)
9.53
PSA
121.35 Å2
Refractivity
99.74 m3·mol-1
Polarizability
39.3 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
9
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Dược Lực Học : Gemifloxacin is a quinolone/fluoroquinolone antibiotic. Gemifloxacin 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. Gemifloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria.
Cơ Chế Tác Dụng : Gemifloxacin is an oral broad-spectrum quinolone antibacterial agent used in the treatment of acute bacterial exacerbation of chronic bronchitis and mild-to-moderate pneumonia. Gemifloxacin acts by inhibiting DNA synthesis through the inhibition of both DNA gyrase and topoisomerase IV, which are essential for bacterial growth. The bactericidal action of gemifloxacin 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 :
Rapidly absorbed from the gastrointestinal tract. The absolute bioavailability averages approximately 71%.
▧ Volume of Distribution :
* 1.66 to 12.12 L/kg
▧ Protein binding :
60-70%
▧ Metabolism :
Gemifloxacin is metabolized to a limited extent by the liver. All metabolites formed are minor (<10% of the administered oral dose); the principal ones are N-acetyl gemifloxacin, the E-isomer of gemifloxacin and the carbamyl glucuronide of gemifloxacin.
▧ Route of Elimination :
Gemifloxacin and its metabolites are excreted via dual routes of excretion.Following oral administration of gemifloxacin to healthy subjects, a mean (± SD) of 61 ± 9.5% of the dose was excreted in the feces and 36 ± 9.3% in the urine as unchanged drug and metabolites. The mean (± SD) renal clearance following repeat doses of 320 mg was approximately 11.6 ± 3.9 L/hr (range 4.6-6 L/hr), which indicates active secretion is involved in the renal excretion of gemifloxacin.
▧ Half Life :
7 (± 2) hours
▧ Clearance :
* renal cl=11.6+/- 3.9 L/hr [Healthy subjects receiving repeat doses of 320 mg orally]
Chỉ Định : For the treatment of bacterial infection caused by susceptible strains such as S. pneumoniae, H. influenzae, H. parainfluenzae, or M. catarrhalis, S. pneumoniae (including multi-drug resistant strains [MDRSP]), M. pneumoniae, C. pneumoniae, or K. pneumoniae.
Tương Tác Thuốc :
  • Aluminium Formation of non-absorbable complexes
  • Calcium Acetate Calcium salts such as calcium acetate may decrease the absorption of quinolone antibiotics such as gemifloxacin. 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 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
  • Sucralfate Formation of non-absorbable complexes
  • Zinc Formation of non-absorbable complexes
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Factive
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01155
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02471
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/67707-320-05
PharmGKB
http://www.pharmgkb.org/drug/PA10088
Wikipedia
http://en.wikipedia.org/wiki/Gemifloxacin
RxList
http://www.rxlist.com/cgi/generic3/factive.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/fac1662.shtml
Drugs.com
http://www.drugs.com/cdi/gemifloxacin.html
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