メロペネム三水和物 化学特性,用途語,生産方法
外観
白色〜うすい黄色, 結晶性粉末〜粉末
溶解性
水にやや溶けにくく、エタノール(95)及びジエチルエーテルにほとんど溶けない。
用途
合タンパク質に結合し、細胞壁
の合成阻害作用を示します。抗菌スペクトル
は広く、緑膿菌にも強い抗菌力を示します。
また、β ラクタマーゼに対しても安定です。
用途
カルバペネム系抗生物質です。
ペニシリン結合タンパクに結合し、細胞壁の
合成阻害作用を示します。抗菌スペクトルは
広く、緑膿菌にも強い抗菌力を示します。ま
た、β ラクタマーゼに対しても安定です。
効能
抗生物質, 細胞壁合成阻害薬
商品名
メロペン (大日本住友製薬)
使用上の注意
不活性ガス封入
化学的特性
White or slight-yellow crystalline powder LOD ≤0.5% Heavy Metals ≤20 ppm
使用
Meropenem trihydrate is a carbapenem antibiotic with wide spectrum of antibacterial. It is an ultra-broad spectrum beta-lactam antibiotic and has antibacterial activity against Gram-negative and Gram-positive bacteria as well as anaerobic microorganisms such as Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae, Enterobacter species, Serratia marcescens, Streptococcus pyogenes, Streptococcus agalactiae and Citrobacter sp. Meropenem trihydrate is indicated for the treatment of serious bacterial infection including complicated skin infections, complicated intra-abdominal infections, urinary tract infections, severe pneumonia, broncho-pulmonary infections and bacterial meningitis.
主な応用
Meropenem trihydrate is a thienamycin derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of bacterial infections, including infections in immunocompromised patients.
Meropenem trihydrate has also been used in the
antibiotic susceptibility testing of E coli isolates from harbor estuary sediment samples.
in the bacterial killing assay and for screening antibiotic resistance of cystic fibrosis patient′s sputum based Staphylococcus aureus transformed macrophages in phagocyte infection.
for screening Enterococcus faecalis from human bile.
抗菌性
The unique side chain at C-2 is associated with increased activity against Gram-negative bacteria, including H. influenzae. It is slightly less active than imipenem against Gram-positive organisms. It is active against anaerobes and more active against some strains that are less susceptible to imipenem. Its excellent activity against Gram-negative organisms is due to high affinity for multiple penicillin-binding proteins. Activity is little affected by inoculum size or the presence of serum. It is bactericidal at concentrations close to the MIC.
Stability to β-lactamases is similar to that of other carbapenems: it is highly resistant to most serine β-lactamases, including extended-spectrum enzymes, but can be hydrolyzed by metallo-β-lactamases and by serine carbapenemases.
一般的な説明
Meropenem trihydrate (MRP) belongs to the carbapenem group of compounds. It is susceptible to degradation at high temperature and humidity. It is soluble in methanol-water or acetone-water combinations. It is used as an antibacterial agent for treating meningitis and pneumonia.
薬物動態学
C
max 500 mg intravenous (30-min
infusion): 23 mg/L end infusion
1 g intravenous (30-min infusion): 49 mg/L end infusion
Plasma half-life: 1 h
Volume of distribution: c. 0.3 L/kg
Plasma protein binding: 2%
Absorption and distribution
Meropenem is not absorbed after oral administration. It
penetrates well into most body fluids and tissues, including
CSF, achieving concentrations matching or exceeding those
required to inhibit most susceptible bacteria. In pediatric
patients (1 month to 15 years) with inflamed meninges it
achieves CSF levels of 0.9–6.5 mg/L after a single intravenous
infusion (40 mg/kg) over 30 min. After a single intravenous
dose, the highest mean concentrations of meropenem were
found in tissues and fluids at 1 h (0.5–1.5 h) after the start
of infusion.
Metabolism and excretion
The mean recovery of unchanged meropenem is approximately
70%. The remainder consists of the microbiologically
inactive open-ring form. Renal excretion is greater than
70% of unchanged drug over 12 h. Co-administration with
probenecid prolongs the half-life 38%, but peak concentrations
are not greatly affected. In patients with renal impairment
the dose should be adjusted. Parent drug and metabolite
are removed by hemodialysis.
臨床応用
Meropenem is a second-generation carbapenem that, todate, has undergone the most extensive clinical evaluation.It has recently been approved as Merrem for the treatmentof infections caused by multiply-resistant bacteria and forempirical therapy for serious infections, such as bacterialmeningitis, septicemia, pneumonia, and peritonitis.Meropenem exhibits greater potency against Gram-negativeand anaerobic bacteria than does imipenem, but it is slightlyless active against most Gram-positive species. It is not effectiveagainst MRSA. Meropenem is not hydrolyzed byDHP-I and is resistant to most β-lactamases, including a fewcarbapenemases that hydrolyze carbapenem.
適応症
Intra-abdominal infections
Bacterial meningitis (pediatric patients >3 months)
Complicated skin and skin structure infections
副作用
Seizures and other CNS adverse experiences have been
reported in 0.7% of all adult patients, most commonly those
with pre-existing CNS disorders. Pseudomembranous colitis
has been reported. Other reactions include diarrhea (4.8%),
nausea and vomiting (3.6%), inflammation at the site of
injection (2.4%) and headache (2.3%). Moniliasis occurs in
1.9–3.1% of pediatric patients.
Patients with a history of hypersensitivity reactions to other
β-lactam agents should be treated cautiously.
メロペネム三水和物 上流と下流の製品情報
原材料
準備製品