Tìm theo
Imipenem
Các tên gọi khác (11 ) :
  • (5R,6S)-3-((2-(Formimidoylamino)ethyl)thio)-6-((R)-1-hydroxyethyl)-7-oxo-1-azabicyclo(3.2.0)hept-2-ene-2-carboxylic acid
  • (5R,6S)-3-(2-Formimidoylamino-ethylsulfanyl)-6-((R)-1-hydroxy-ethyl)-7-oxo-1-aza-bicyclo[3.2.0]hept-2-ene-2-carboxylic acid
  • (5R,6S)-6-((R)-1-Hydroxyethyl)-3-(2-(iminomethylamino)ethylthio)-7-oxo-1-azabicyclo(3.2.0)hept-2-ene-2-carbonsaeure
  • Imipemide
  • Imipenem
  • Imipenem anhydrous
  • Imipenem, n-formimidoyl thienamycin
  • Imipenemum
  • IMP
  • N-Formimidoyl thienamycin
  • N-formimidoylthienamycin
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 74431-23-5
ĐG : Cardinal Health , http://www.cardinal.com
CTHH: C12H17N3O4S
PTK: 299.346
Semisynthetic thienamycin that has a wide spectrum of antibacterial activity against gram-negative and gram-positive aerobic and anaerobic bacteria, including many multiresistant strains. It is stable to beta-lactamases. Clinical studies have demonstrated high efficacy in the treatment of infections of various body systems. Its effectiveness is enhanced when it is administered in combination with cilastatin, a renal dipeptidase inhibitor. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H17N3O4S
Phân tử khối
299.346
Monoisotopic mass
299.093976737
InChI
InChI=1S/C12H17N3O4S/c1-6(16)9-7-4-8(20-3-2-14-5-13)10(12(18)19)15(7)11(9)17/h5-7,9,16H,2-4H2,1H3,(H2,13,14)(H,18,19)/t6-,7-,9-/m1/s1
InChI Key
InChIKey=ZSKVGTPCRGIANV-ZXFLCMHBSA-N
IUPAC Name
(5R,6S)-3-({2-[(E)-(aminomethylidene)amino]ethyl}sulfanyl)-6-[(1R)-1-hydroxyethyl]-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid
Traditional IUPAC Name
imipenem
SMILES
[H][C@]12CC(SCC\N=C\N)=C(N1C(=O)[C@]2([H])[C@@H](C)O)C(O)=O
Độ hòa tan
1E+004 mg/L
logP
-3.9
logS
-2.6
pKa (strongest acidic)
3.63
pKa (Strongest Basic)
10.88
PSA
116.22 Å2
Refractivity
75.84 m3·mol-1
Polarizability
31.1 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
6
H Bond Donor Count
3
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
pKa
3.2
Dược Lực Học : Imipenem is a beta-lactam antibiotic belongings to the subgroup of carbapenems. Imipenem has a broad spectrum of activity against aerobic and anaerobic Gram positive as well as Gram negative bacteria. It is particularly important for its activity against Pseudomonas aeruginosa and the Enterococcus species. Imipenem is rapidly degraded by the renal enzyme dehydropeptidase when administered alone, and is always co-administered with cilastatin to prevent this inactivation.
Cơ Chế Tác Dụng : Semisynthetic thienamycin that has a wide spectrum of antibacterial activity against gram-negative and gram-positive aerobic and anaerobic bacteria, including many multiresistant strains. It is stable to beta-lactamases. Clinical studies have demonstrated high efficacy in the treatment of infections of various body systems. Its effectiveness is enhanced when it is administered in combination with cilastatin, a renal dipeptidase inhibitor. [PubChem] Imipenem acts as an antimicrobial through the inhibition of cell wall synthesis of various gram-positive and gram-negative bacteria. This inhibition of cell wall synthesis in gram-negative bateria is attained by binding to pencillin binding proteins (PBPs). In E. coli and selected strains of P. aeruginosa, imipenem has shown to have the highest affinity to PBP-2, PBP-1a, and PBP-1b. This preferential binding to PBP-2 and PBP-1b results in the direct conversion of the individual cell to a spheroblast, which leads to rapid cell lysis and death without filament formation.
Dược Động Học :
▧ Absorption :
Imipenem is not effectively absorbed from the gastrointestinal tract and therefore must be administered parenterally.
▧ Protein binding :
20% binds to plasma proteins
▧ Metabolism :
Renal.
▧ Half Life :
1 hour
Chỉ Định : For the treatment of bacterial infections caused by susceptible bacteria.
Tương Tác Thuốc :
  • Cyclosporine Imipenem increases the effect and toxicity of cyclosporine
  • Valganciclovir Generalized convulsions have been reported in patients taking Ganciclovir and Imipenem-cilastatin. Concomitant therapy should be avoided. (Note: Valganciclovir is converted to Ganciclovir in vivo)
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Tienamycin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01598
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=104838
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505744
ChemSpider
http://www.chemspider.com/Chemical-Structure.94631.html
PharmGKB
http://www.pharmgkb.org/drug/PA449968
Wikipedia
http://en.wikipedia.org/wiki/Imipenem
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