2-プロピル吉草酸

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Danger

• 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

• 注意書き

  P201：使用前に取扱説明書を入手すること。

  P302+P352：皮膚に付着した場合：多量の水と石鹸で洗うこと。

  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。

  P308+P313：暴露または暴露の懸念がある場合：医師の診断/手当てを 受けること。

2-プロピル吉草酸 価格

MSDS Information

• Valproic acid

2-プロピル吉草酸 化学特性,用途語,生産方法

• 外観

  無色～黄褐色, 澄明の液体

• 溶解性

  エタノールに易溶, 水に難溶。水に難溶、有機溶媒に可溶。水に微溶。

• 解説

  バルプロ酸(CH3CH2CH2)2CHCOOHは各種癲癇発作およびそれに伴う性格行動障害の治療に用いられる。そのほか，抗不安薬であるジアゼパムなどベンゾジアゼピン系薬物も癲癇治療に用いられるようになり，この領域で重要な薬物となっている。

• 用途

  薬理研究用。

• 用途

  医薬原料

• 効能

  抗けいれん薬

• 説明

  Valproic acid and its salts are a new group of antiepileptic drugs that differs from the known drugs both structurally and in terms of its mechanism of action. It is believed that it acts on the metabolism of the GABA system. Valproic acid has been shown to elevate the level of GABA in the brain by means of competitive inhibition of GABA transaminase and the dehydrogenase of succinic semialdehyde.
  This drug not only exhibits anticonvulsant action, but also betters the mental condition of the patient.

• 化学的特性

  Colorless Liquid

• 使用

  2-Propylpentanoic acid has been used as a supplement in mouse embryonic fibroblast - conditioned medium (MEF-CM)?to feed the cells.

• 定義

  ChEBI: A branched-chain saturated fatty acid that comprises of a propyl substituent on a pentanoic acid stem.

• 生物学の機能

  Although it is marketed as both valproic acid (Depakene) and as sodium valproate (Depakote), it is the valproate ion that is absorbed from the gastrointestinal tract and is the active form.
  As with several other AEDs, it is difficult to ascribe a single mechanism of action to valproic acid.This compound has broad anticonvulsant activity, both in experimental studies and in the therapeutic management of human epilepsy.Valproic acid has been shown to block voltage-dependent sodium channels at therapeutically relevant concentrations. In several experimental studies, valproate caused an increase in brain GABA; the mechanism was unclear.There is evidence that valproate may also inhibit T-calcium channels and that this may be important in its mechanism of action in patients with absence epilepsy.

• 一般的な説明

  Clear colorless liquid.

• 空気と水の反応

  Insoluble in water.

• 火災危険

  2-Propylpentanoic acid is combustible.

• 薬物動態学

  Valproate undergoes rapid and complete absorption, which is only slightly slowed by food. It is 90% protein bound, and its clearance is dose-dependent because of an increase in the free fraction of the drug at higher doses. It is metabolized almost entirely by the liver, with 30 to 50% of an orally administered dose being eliminated in the urine as its acyl glucuronide conjugate, 40% from mitochondrial β-oxidation, approximately 15 to 20% by ω-oxidation, and less than 3% is excreted unchanged in urine. Its major active metabolite is (E)-2-ene valproate (trans 2-ene valproate). Its 4-ene metabolite has been proposed to be a reactive metabolite responsible for the hepatotoxicity of valproate. Other metabolites found in the urine include 3-oxo- and 4-hydroxyvalproate. The elimination half-life for valproate ranged from 9 to 16 hours following oral dosing regimens of 250 to 1,000 mg. Patients who are not taking enzyme-inducing AEDs (carbamazepine, phenytoin, and phenobarbital) will clear valproate more rapidly; therefore, monitoring of AED plasma concentrations should be intensified whenever concurrent AEDs are introduced or withdrawn.

• 臨床応用

  Valproic acid is well absorbed from the gastrointestinal tract and is highly bound (~90%) to plasma protein, and most of the compound is therefore retained within the vascular compartment.Valproate rapidly enters the brain from the circulation; the subsequent decline in brain concentration parallels that in plasma, indicating equilibration between brain and capillary blood. A large number of metabolites have been identified, but it is not known whether they play a role in the anticonvulsant effect of the parent drug. Valproic acid inhibits the metabolism of several drugs, including phenobarbital, primidone, carbamazepine, and phenytoin, leading to an increased blood level of these compounds. At high doses, valproic acid can inhibit its own metabolism. It can also displace phenytoin from binding sites on plasma proteins, with a resultant increase in unbound phenytoin and increased phenytoin toxicity. In this instance, the dosage of phenytoin should be adjusted as required. These examples reinforce the need to determine serum anticonvulsant levels in epileptic patients when polytherapy is employed.
  Valproic acid has become a major AED against several seizure types. It is highly effective against absence seizures and myoclonic seizures. In addition, valproic acid can be used either alone or in combination with other drugs for the treatment of generalized tonic– clonic epilepsy and for partial seizures with complex symptoms.

• 副作用

  The most serious adverse effect associated with valproic acid is fatal hepatic failure. Fatal hepatotoxicity is most likely to occur in children under age 2 years, especially in those with severe seizures who are given multiple anticonvulsant drug therapy. The hepatotoxicity is not dose related and is considered an idiosyncratic reaction; it can occur in individuals in other age groups, and therefore, valproic acid should not be administered to patients with hepatic disease or significant hepatic dysfunction or to those who are hypersensitive to it. Valproic acid administration has been linked to an increased incidence of neural tube defects in the fetus of mothers who received valproate during the first trimester of pregnancy. Patients taking valproate may develop clotting abnormalities.
  Valproic acid causes hair loss in about 5% of patients, but this effect is reversible. Transient gastrointestinal effects are common, and some mild behavioral effects have been reported. Metabolic effects, including hyperglycemia, hyperglycinuria, and hyperammonemia, have been reported. An increase in body weight also has been noted. Valproic acid is not a CNS depressant, but its administration may lead to increased depression if it is used in combination with phenobarbital, primidone, benzodiazepines, or other CNS depressant agents.

• Solubility in organics

  soluble in most organic solvents, including methanol, chloroform, and ether, solubility in water: 1.27 mg/mL.

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