ロラカルベフ 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
Loracarbef is a synthetic C-5 “carba” analogue of cefaclor. The smaller methylene moiety (as compared to
sulfur) would be expected to make loracarbef more reactive/potent, and this seems to be the case. It is more
stable chemically, however, and this adds to its virtues.
使用
An antibiotic, a synthetic carbacephem analogue of cefaclor, and is more stable chemically.
定義
ChEBI: A synthetic "carba" analogue of cefaclor, with carbon replacing sulfur at position 1. Used to treat a wide range of infections caused by both gram-positive and gram-negative bacteria.
抗菌性
An oral carbacephem, with carbon replacing sulfur in the
fused ring structure. Its structure and properties are otherwise
closely related to those of cefaclor, but it has improved
chemical stability. Activity and stability to β-lactamases correspond
closely to those of cefaclor.
It is almost completely absorbed by the oral route, but
food delays absorption. A 500 mg oral dose achieves a serum
concentration of around 16 mg/L after 1.3 h. Adequate concentrations
are achieved for the treatment of upper respiratory
tract infection. Sputum concentrations have been found
to be around 2% of the corresponding plasma level. The
plasma half-life is about 1 h and protein binding is 25%.
Most of the dose is excreted unchanged in the urine, 60%
within 12 h. The elimination half-life is increased in patients
with impaired renal function. Probenecid delays excretion.
Diarrhea is the most prominent side effect, occurring in
about 4% of patients. Other gastrointestinal upsets are also
reported. It has been used for the oral treatment of upper
respiratory tract infection, skin and soft-tissue infections, and
uncomplicated urinary tract infection caused by sensitive
organisms, but is not widely available.
臨床応用
Loracarbef (Lorabid) is the first of a series of carbacephemsprepared by total synthesis to be introduced. Carbacephemsare isosteres of the cephalosporin (or △ 3-cephem) antibioticsin which the 1-sulfur atom has been replaced by a methylene(CH2) group. Loracarbef is isosteric with cefaclor and hassimilar pharmacokinetic and microbiological properties.Thus, the antibacterial spectrum of activity resembles thatof cefaclor, but it has somewhat greater potency againstH. influenzae and M. catarrhalis, including β-lactamase–producing strains. Unlike cefaclor, which undergoes degradationin human serum, loracarbef is chemically stable inplasma. It is absorbed well orally. Oral absorption is delayedby food. The half-life in plasma is about 1 hour.
副作用
Diarrhea is the most common adverse effect with
loracarbef and, along with certain other adverse effects, is seen more frequently with children, so this
lessens enthusiasm for the drug in patients younger than 12 years.
ロラカルベフ 上流と下流の製品情報
原材料
準備製品