エルタペネム HYDROCHLORIDE

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H302：飲み込むと有害

  H315：皮膚刺激

  H319：強い眼刺激

  H335：呼吸器への刺激のおそれ

• 注意書き

  P261：粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

エルタペネム HYDROCHLORIDE 価格

エルタペネム HYDROCHLORIDE 化学特性,用途語,生産方法

• 効能

  抗生物質, 細胞壁合成阻害薬

• 説明

  Ertapenem is another synthetic carbapenem with a rather complex side chain at C-3. It is used once daily parenterally, with special application against anaerobes. As with meropenem, the 4-β-methyl group confers stability toward dehydropeptidase-1 It is not active against pseudomonads or acinetobacteria and, therefore, should not be substituted for imipenem or meropenem. It is relatively strongly bound to serum proteins, so it has a prolonged half-life, making it more convenient to use than the other carbapenems when its spectrum warrants this. Its reported indications include complicated intra-abdominal and complicated skin/skin structure infections caused by sensitive organisms (for intra-abdominal: Escheri chia coli, Clostri di um clostri doforme, Bacteroi des fragilis, and Peptostreptococcus sp; for skin/skin structures: Staphylococcus aureus (methicillin-susceptible strains), Streptococcus pyogenes, E.coli, or Peptostreptococcus sp.). It can be administered once daily.

• 使用

  Ertapenem is a long-acting parenteral cabapenem. Ertapenem has bactericidal activity against a variety of gram-negative pathogens, some gram positive strains, and Haemopilus influenzae. Ertapenem has shown to inactivate L,D-transpeptidase, an enzyme responsible for in vitro cross-linking of Mycobacterium tuberculosis peptidoglycan.

• 定義

  ChEBI: Meropenem in which the one of the two methyl groups attached to the amide nitrogen is replaced by hydrogen while the other is replaced by a 3-carboxyphenyl group. The sodium salt is used for the treatment of moderate to severe susceptible infections includ ng intra-abdominal and acute gynaecological infections, pneumonia, and infections of the skin and of the urinary tract.

• 抗菌性

  Activity against aerobic and anaerobic pathogens is comparable to that of imipenem: MIC values for Gramnegative bacilli (with the exception of Ps. aeruginosa) are generally lower and those for Gram-positive cocci higher.
  Ertapenem is stable to most serine β-lactamases, but is hydrolyzed by serine carbapenemases and metallo- β-lactamases.

• 一般的な説明

  Ertapenem (Invanz, for injection) is a synthetic 1-β-methylcarbapenem that is structurally related to β-lactam antibiotics,particularly the thienamycin group. Its mechanism ofaction is the same as that of other β-lactam antibiotics. Thestructure resists β-lactamases and dehydropeptidases.
  Ertapenem is indicated for the treatment of moderate tosevere infections caused by susceptible strains causing complicatedintra-abdominal infections such as Escherichia,Clostridium, Peptostreptococcus, and Bacteroides. Theantibiotic is also indicated for complicated skin and skinstructure infections including diabetic foot infections (withoutosteomyelitis). Treatable strains include Staphylococcus(MSSA), Streptococcus, Escherichia, Klebsiella, Proteus,and Bacteroides. Ertapenem is also indicated for community-acquired pneumonia caused by S. pneumoniae,Haemophilus infljuenzae, and M. catarrhalis. Complicatedurinary tract infections and acute pelvic infections round outthe indications for ertapenem.

• 薬物動態学

  C_max 1 g intramuscular: c. 67 mg/L after 2 h
  1 g intravenous infusion (30 min): c. 155 mg/L end infusion
  Plasma half-life: c. 4 h
  Volume of distribution: c. 0.12 L/kg (steady state)
  Plasma protein binding: 85–95%
  Absorption after intramuscular injection is essentially complete with 90% bioavailability. The modestly extended plasma half-life allows once-daily dosing.
  Excretion is predominantly by the renal route, about 80% being recovered in the urine within 24 h. About 40% is eliminated unchanged, the rest as a biologically inactive ringopened metabolite. Dosage should be reduced in severe renal impairment.

• 臨床応用

  Complicated intra-abdominal infections
  Complicated skin and skin structure infections, including diabetic foot
  infections without osteomyelitis
  Community acquired pneumonia
  Complicated urinary tract infections including pyelonephritis
  Acute pelvic infections including postpartum endomyometritis, septic
  abortion and postsurgical gynecologic infections
  Prophylaxis of surgical site infection following elective colorectal surgery

• 副作用

  Ertapenem appears to be generally well tolerated. The most common drug-related adverse experiences are diarrhea (5.5%), infused vein complication (3.7%), nausea (3.1%), headache (2.2%), vaginitis (2.1%), phlebitis/thrombophlebitis (1.3%) and vomiting (1.1%). Seizures have occasionally been reported (0.5%) in patients with a history of disorders of the CNS.

エルタペネム HYDROCHLORIDE 生産企業

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