クロルゾキサゾン 化学特性,用途語,生産方法
外観
白色～うすい黄色, 結晶～粉末又は塊
溶解性
エタノール及びアセトンに溶け、水にほとんど溶けない。
効能
骨格筋弛緩薬
使用上の注意
不活性ガス封入
説明
Chlorzoxazone is a muscle relaxant. It acts by blocking nerve
impulses or pain sensations that are sent to brain. Typically, it
is used together with rest and physical therapy to treat skeletal
muscle conditions such as pain or injury. Chlorzoxazone,
5-chloro-2-benzoxazolione, is synthesized by a heterocyclization
reaction of 2-amino-4-chlorophenol with phosgene.
Skeletal muscle relaxants have conventionally been classified
into one group; however, they are actually a heterogeneous
group of medications commonly used to treat two different
types of underlying conditions – spasticity from upper motor
neuron syndromes and muscular pain or spasms from
peripheral musculoskeletal conditions. Medications classified
as skeletal muscle relaxants are baclofen, carisoprodol,
chlorzoxazone, cyclobenzaprine, dantrolene, metaxalone,
methocarbamol, orphenadrine, and tizanidine. These drugs
may impair mental and/or physical abilities required for
driving vehicles. As a class, skeletal muscle relaxants have
central nervous system (CNS)-related side effects: drowsiness,
dizziness, decreased alertness, blurred vision, and ataxia.
Their use has been associated with a twofold increase in the
risk for motor vehicle crashes. Muscle relaxants are included
in the ‘Beers List’ of potentially inappropriate medications
in older adults. Most muscle relaxants are poorly tolerated by
elderly patients because they cause anticholinergic adverse
effects, sedation, and weakness. Although extremely uncommon,
this compound may yield to idiosyncratic and
unpredictable type of liver toxicity. The concomitant use of
alcohol or other CNS depressants may have an additive effect.
Individuals on chlorzoxazone containing drugs should be
monitored for abnormal liver enzymes (e.g., aspartate transaminase
(AST), alanine transaminase (ALT), alkaline phosphatase,
bilirubin, etc.).
化学的特性
White to Off-White Solid
使用
Chlorzoxazone is a benzoxazolone derivative that causes skeletal muscle relaxation and blocks spasticity in clinical studies. Chlorzoxazone enhances small and intermediate conductance calcium-activated potassium channels (EC50s = 87 and 98 μM for KCa2.2 and KCa3.1, respectively). The cytochrome P450 isoform CYP2E1 converts chlorzoxazone to 6-hydroxy chlorzoxazone . The urinary excretion of this 6-hydroxy metabolite is often used as a probe of CYP2E1 activity in studies of hepatotoxicity.
定義
ChEBI: A member of the class of 1,3-benzoxazoles that is 1,3-benzoxazol-2-ol in which the hydrogen atom at position 5 is substituted by chlorine. A centrally acting muscle relaxant with sedative properties, it is used for the symptomatic treatment of painful mus
le spasm.
一般的な説明
Chlorzoxazone is a centrally active muscle relaxant used to treat painful muscle spasms linked to musculoskeletal disorders, such as fibrositis, bursitis, myositis, spondylitis, etc.
Pharmaceutical secondary standard for application in quality control. Provides pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards.
環境運命予測
Chlorzoxazone ismetabolized by the CYP1A2 and CYP2E1 microsomal
enzymes to a toxic metabolite 6-hydroxychlorzoxazone.
クロルゾキサゾン 上流と下流の製品情報
原材料
準備製品