Tìm theo
Ceftaroline fosamil
Các tên gọi khác (4 ) :
  • (6R,7R)-7-[(2Z)-2-ethoxyimino-2-[5-(phosphonoamino)-1,2,4-thiadiazol-3-yl]acetyl]amino]-3-[4-(1-methylpyridin-1-ium-4-yl)-1,3-thiazol-2-yl]sulfanyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
  • Ceftaroline
  • PPI 0903
  • Teflaro
cephalosporins, antibiotics
Thuốc Gốc
Small Molecule
CAS: 400827-46-5
ATC: J01DI02
CTHH: C22H21N8O8PS4
PTK: 684.685
Ceftaroline fosamil is a cephalosporin antibacterial indicated for the treatment of the following infections caused by designated susceptible bacteria: Acute bacterial skin and skin structure infections. Community-acquired bacterial pneumonia.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C22H21N8O8PS4
Phân tử khối
684.685
Monoisotopic mass
684.01027896
InChI
InChI=1S/C22H21N8O8PS4/c1-3-38-26-13(16-25-21(43-28-16)27-39(35,36)37)17(31)24-14-18(32)30-15(20(33)34)12(9-40-19(14)30)42-22-23-11(8-41-22)10-4-6-29(2)7-5-10/h4-8,14,19H,3,9H2,1-2H3,(H4-,24,25,27,28,31,33,34,35,36,37)/b26-13+/t14-,19-/m1/s1
InChI Key
InChIKey=ZCCUWMICIWSJIX-XHNDKCDBSA-N
IUPAC Name
4-(2-{[(6R,7R)-2-carboxylato-7-[(2E)-2-(ethoxyimino)-2-[5-(phosphonoamino)-1,2,4-thiadiazol-3-yl]acetamido]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]sulfanyl}-1,3-thiazol-4-yl)-1-methylpyridin-1-ium
Traditional IUPAC Name
4-(2-{[(6R,7R)-2-carboxylato-7-[(2E)-2-(ethoxyimino)-2-[5-(phosphonoamino)-1,2,4-thiadiazol-3-yl]acetamido]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]sulfanyl}-1,3-thiazol-4-yl)-1-methylpyridin-1-ium
SMILES
[H][C@]12SCC(SC3=NC(=CS3)C3=CC=[N+](C)C=C3)=C(N1C(=O)[C@H]2NC(=O)C(=N\OCC)\C1=NSC(NP(O)(O)=O)=N1)C([O-])=O
Độ hòa tan
>100 mg/ml
logP
-3.7
logS
-4.5
pKa (strongest acidic)
1.8
pKa (Strongest Basic)
0.39
PSA
223.24 Å2
Refractivity
171.63 m3·mol-1
Polarizability
63.77 Å3
Rotatable Bond Count
11
H Bond Acceptor Count
13
H Bond Donor Count
4
Physiological Charge
-2
Number of Rings
5
Bioavailability
0
MDDR-Like Rule
true
Dược Lực Học : The time that unbound plasma concentration of ceftaroline exceeds the minimum inhibitory concentration (MIC) of the infecting organism has been shown to best correlate with efficacy in a neutropenic murine thigh infection model with S. aureus and S. pneumoniae. No significant effect on QTc (corrected QT interval) interval was detected at peak plasma concentration or at any other time.
Cơ Chế Tác Dụng : Ceftaroline fosamil is a cephalosporin antibacterial indicated for the treatment of the following infections caused by designated susceptible bacteria: Acute bacterial skin and skin structure infections. Community-acquired bacterial pneumonia. Ceftaroline fosamil is an antibacterial drug.
Dược Động Học :

▧ Volume of Distribution :
Median 20.3 L (18.3-21.6 L).
▧ Protein binding :
approximately 20%.
▧ Metabolism :
Ceftaroline fosamil is converted into bioactive ceftaroline in plasma by a phosphatase enzyme. Hydrolysis of the beta-lactam ring of ceftaroline occurs to form the microbiologically inactive, open-ring metabolite ceftaroline M-1.
▧ Route of Elimination :
primarily eliminated by the kidneys (6% in feces within 48 hours).
▧ Half Life :
1.60 hours (600 mg dose).
Độc Tính : LD50/LC50: Draize test, rabbit, eye: 100 mg/24H Moderate; Oral, mouse: LD50 = 300 mg/kg; Oral, rabbit: LD50 = 3200 mg/kg; Oral, rat: LD50 = 980 mg/kg.
Chỉ Định : Ceftaroline fosamil is indicated for the treatment of patients with the following infections caused by susceptible isolates of the designated microorganisms.
Liều Lượng & Cách Dùng : Injection, powder, for solution - Intravenous - 600 mg or 400 mg of sterile Ceftaroline fosamil powder in single-use 20 mL vials.
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06590
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D08884
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0456-0600-01
Wikipedia
http://en.wikipedia.org/wiki/Ceftaroline_fosamil
RxList
http://www.rxlist.com/teflaro-drug.htm
PDRhealth
http://www.pdr.net/MedMerck-full-prescribing-information/teflaro?druglabelid=158
Drugs.com
http://www.drugs.com/teflaro.html
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