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オクスカルバゼピン

オクスカルバゼピン 化学構造式
28721-07-5
CAS番号.
28721-07-5
化学名:
オクスカルバゼピン
别名:
10-オキソ-10,11-ジヒドロ-5H-ジベンゾ[b,f]アゼピン-5-カルボアミド;オキスカルバゼピン;オキサカルバマゼピン;オクスカルバゼピン;10,11-ジヒドロ-10-オキソ-5H-ジベンゾ[b,f]アゼピン-5-カルボアミド;オキシカルバマゼピン;10(11H)-オキソ-5H-ジベンゾ[b,f]アゼピン-5-カルボアミド;オクスカルバゼピン, 98%;オキサカルバゼピン;オクスカルバゼピン (JAN)
英語化学名:
Oxcarbazepine
英語别名:
Aurene;Oxetol;Oxecarb;gp47680;TRILEPTAL;Ocarbazepine;OXCARBAZEPINE;Oxcarbapezine;OXACARBAZEPINE;OXCARBAMAZEPINE
CBNumber:
CB9238172
化学式:
C15H12N2O2
分子量:
252.27
MOL File:
28721-07-5.mol

オクスカルバゼピン 物理性質

融点 :
215-216°C
沸点 :
457.2±55.0 °C(Predicted)
比重(密度) :
1.329±0.06 g/cm3(Predicted)
闪点 :
230.3±31.5 °C
貯蔵温度 :
Sealed in dry,Room Temperature
溶解性:
DMSO: ~9 mg/mL
外見 :
solid
酸解離定数(Pka):
13.73±0.20(Predicted)
色:
white
水溶解度 :
Soluble in DMSO, methanol, water, ethanol and acetone.
Merck :
14,6929
CAS データベース:
28721-07-5(CAS DataBase Reference)
EPAの化学物質情報:
5H-Dibenz[b,f]azepine-5-carboxamide, 10,11-dihydro-10-oxo- (28721-07-5)
安全性情報
  • リスクと安全性に関する声明
  • 危険有害性情報のコード(GHS)
主な危険性  Xn,F
Rフレーズ  22-36-20/21/22-11
Sフレーズ  16-36/37
RIDADR  UN 1648 3 / PGII
WGK Germany  3
RTECS 番号 HN8445000
HSコード  29339900
有毒物質データの 28721-07-5(Hazardous Substances Data)
絵表示(GHS)
注意喚起語 Danger
危険有害性情報
コード 危険有害性情報 危険有害性クラス 区分 注意喚起語 シンボル P コード
H225 引火性の高い液体および蒸気 引火性液体 2 危険 P210,P233, P240, P241, P242, P243,P280, P303+ P361+P353, P370+P378,P403+P235, P501
H302 飲み込むと有害 急性毒性、経口 4 警告 P264, P270, P301+P312, P330, P501
H319 強い眼刺激 眼に対する重篤な損傷性/眼刺激 性 2A 警告 P264, P280, P305+P351+P338,P337+P313P
注意書き
P210 熱/火花/裸火/高温のもののような着火源から遠ざ けること。-禁煙。
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。
P337+P313 眼の刺激が続く場合:医師の診断/手当てを受けること。
P403+P235 換気の良い場所で保管すること。涼しいところに 置くこと。

オクスカルバゼピン 価格 もっと(27)

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入
富士フイルム和光純薬株式会社(wako) W01TRCO869250 オクスカルバゼピン
Oxcarbazepine
28721-07-5 10mg ¥12500 2021-03-23 購入
富士フイルム和光純薬株式会社(wako) W01TRCO869250 オクスカルバゼピン
Oxcarbazepine
28721-07-5 25mg ¥21300 2021-03-23 購入
東京化成工業 O0363 オクスカルバゼピン >98.0%(HPLC)(N)
Oxcarbazepine >98.0%(HPLC)(N)
28721-07-5 5g ¥9800 2021-03-23 購入
東京化成工業 O0363 オクスカルバゼピン >98.0%(HPLC)(N)
Oxcarbazepine >98.0%(HPLC)(N)
28721-07-5 25g ¥28300 2021-03-23 購入
Sigma-Aldrich Japan Y0001576 European Pharmacopoeia (EP) Reference Standard
European Pharmacopoeia (EP) Reference Standard
28721-07-5 ¥35200 2021-03-23 購入

オクスカルバゼピン 化学特性,用途語,生産方法

外観

白色~うすい黄色~うすい黄赤色粉末~結晶

効能

抗けいれん薬, 抗てんかん薬

説明

Oxcarbazepine is a new antiepileptic carbamazepine derivative, reportedly better tolerated than carbamazepine. It appears to be most effective in partial epilepsy with complex seizures.

化学的特性

Pale Yellow Powder

Originator

Ciba-Geigy (Switzerland)

使用

The keto derivative of Carbamazepine. Used as an anticonvulsant

使用

A metabolite of Eslicarbazepine acetate, (BIA 2-093), a novel central nervous system drug.

使用

beta-adrenergic blocker

使用

Oxcarbazepine is a sodium channel protein inhibitor. It is an anticonvulsant and mood-stab.

定義

ChEBI: A dibenzoazepine derivative, having a carbamoyl group at the ring nitrogen, substituted with an oxo group at C-4 of the azepeine ring which is also hydrogenated at C-4 and C-5. It is a anticholinergic anticonvulsant and mood stabilizing drug, used primaril in the treatment of epilepsy.

brand name

Trileptal (Novartis).

生物学の機能

Oxcarbazepine is chemically and pharmacologically closely related to carbamazepine, but it has much less capacity to induce drug-metabolizing enzymes. This property decreases the problems associated with drug interactions when oxcarbazepine is used in combination with other drugs. The clinical uses and adverse effect profile of oxcarbazepine appear to be similar to those of carbamazepine.

一般的な説明

Oxcarbazepine, marketed under the trade name Trileptal?, is an anticonvulsant developed and prescribed for treatment of epilepsy. In recent years, Oxcarbazepine has shown efficacy in treatment of mood disorders. This certified solution standard is suitable as starting material for the preparation of calibrators and controls in oxcarbazepine testing by GC/MS or LC-MS/MS.

生物活性

Anticonvulsant; protects mice and rats against generalized tonic-clonic seizures induced by electroshock. Thought to act via inhibition of sodium channel activity.

Biochem/physiol Actions

Anticonvulsant, antineuralgic. Inhibits veratrine-induced transmitter release.

作用機序

Although oxcarbazepine is less potent that CBZ, its mechanism of action is similar. The majority of the pharmacological activity for oxcarbazepine is attributed to its primary metabolite, 10-monohydroxycarbazepine (MHD), the plasma levels of which may be ninefold higher than those for CBZ. Both oxcarbazepine and MHD produce a blockade of voltagedependent sodium channels, thus decreasing repetitive firing and spread of electrical activity. An additional action on calcium and potassium channels may contribute to the therapeutic effect. Like carbamazepine, oxcarbazepine may worsen juvenile myoclonic or absence seizures.

薬物動態学

Oxcarbazepine is completely absorbed, and food has no effect on its absorption. Unlike CBZ, it does not cause autoinduction of its own metabolism. The metabolism of oxcarbazepine is different from that of CBZ. Oxcarbazepine is reduced by cytosolic enzymes to MHD before its O-glucuronidation. More than 95% of its oral dose is excreted as conjugated metabolites, with approximately 4% of the drug converted to inactive 10,11-dihydroxy CBZ. Unlike CBZ, no epoxide nor aromatic hydroxylation metabolites are formed. The half-life is 2 hours for oxcarbazepine and 9 hours for the active 10-monohydroxy metabolite. In patients with impaired renal function, the half-life for MHD is prolonged to 19 hours, with a doubling in its area under the plasma concentration curve. Peak plasma concentration following an oral dose occurs at approximately 4.5 hours.
Oxcarbazepine induces CYP3A4/5 and UTP, and it also inhibits CYP2C19, producing significant effects on the plasma concentration of other drugs. Therefore, oxcarbazepine decreases felodipine bioavailability and lowers plasma levels for lamotrigine, CBZ, CBZ epoxide, calcium channel blockers, and oral contraceptives. Oxcarbazepine increases plasma levels of phenobarbital and phenytoin. Unlike carbamazepine, oxcarbazepine has no effect on plasma levels of risperidone or olanzepine. The plasma levels for oxcarbazepine or MHD are decreased by CBZ, phenobarbital, phenytoin, valproate, and verapamil. Serum MHD may decrease during pregnancy but increase following delivery. Oxcarbazepine clearance is decreased in renal impairment and the elderly. In children, a higher dose/kg for oxcarbazepine than in adults is required to obtain an effective plasma concentration.

臨床応用

Oxcarbazepine (Trileptal?) is the 10-keto analogue of carbamazepine. It is indicated as monotherapy or adjunctive therapy for partial seizures in adults with epilepsy, as monotherapy for the treatment of partial seizures in children 4 years of age or older, and as adjunct therapy in children 2 to 4 years of age.

副作用

Patients with hypersensitivity reactions to carbamazepine can be expected to show cross-sensitivity (e.g., rash) or related problems to oxcarbazepine. The improved toxicity profile for oxcarbazepine when compared to CBZ may result from absence of the epoxide or CBZ-iminoquinone metabolites. The most common side effects are headache, dizziness, nystagmus, blurred vision, somnolence, nausea, ataxia, and fatigue. The incidence of adverse effects has been related to elevated serum MHD concentrations. Adverse effects on cognitive status, hyponatremia, and serious dermatological reactions have been reported, as has hyponatremia.

オクスカルバゼピン 上流と下流の製品情報

原材料

準備製品


オクスカルバゼピン 生産企業

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28721-07-5(オクスカルバゼピン)キーワード:


  • 28721-07-5
  • 10,11-DIHYDRO-10-OXO-5H-DIBENZ[B,F]AZEPINE-5-CARBOXAMIDE
  • 10,11-DIHDYRO-10-OXO-5H-DIBENZ[B,F]AZEPINE-5-CARBOXAMIDE
  • 5H-DIBENZ[B,F]AZEPINE-5-CARBOXAMIDE, 10,11-DIHYDRO-10-OXO-
  • TRILEPTAL
  • Aurene
  • Oxecarb
  • Oxetol
  • Oxcarbazepine 10,11-Dihydro-10-oxo-5H-dibenz[b,f]azepine-5-carboxamide
  • Oxcarbazepine solution
  • Oxcarbazepine, 100ppm
  • Oxcarbazepine impurity
  • f)azepine-5-carboxamide,10,11-dihydro-10-oxo-5h-dibenz(
  • gp47680
  • OXCARBAMAZEPINE
  • OXCARBAZEPINE
  • OXACARBAZEPINE
  • 10,11-Dihdyro-10-oxo-5H-dibenz[b,f]azepine-5-carboxamide, Trileptal
  • OXCARBAZEPINE(SUBJECTTOPATENTFREE)
  • Ocarbazepine
  • 10,11-Dihydro-10-oxo-5h-dibenz[b,f]azepine-5-carboxamide, Oxacarbazepine
  • Oxcarbazepine (100 mg)
  • 1H-azepin-2-ylMethanol
  • Oxcarbapezine
  • 10-Oxo-10,11-dihydro-5H-dibenzo[b,f]azepine-5-carboxamide
  • Oxycarbamazepine
  • Eslicarbazepine Acetate 10,11-Dihydro-10-Oxo-5h-Dibenz [b,f] Azepine-5-Carboxamide
  • 10,11-Dihydro-10-oxo-5H-dibenzo[b,f]azepine-5-carboxamide
  • 10,11-Dihydro-10-oxo-5H-dibenzo(Z)[b,f]azepine-5-carboxamide
  • Oxcarbazepine,10,11-Dihydro-10-oxo-5h-dibenz[b,f]azepine-5-carboxamide, Oxacarbazepine
  • Oxcarbazepine>
  • 10-オキソ-10,11-ジヒドロ-5H-ジベンゾ[b,f]アゼピン-5-カルボアミド
  • オキスカルバゼピン
  • オキサカルバマゼピン
  • オクスカルバゼピン
  • 10,11-ジヒドロ-10-オキソ-5H-ジベンゾ[b,f]アゼピン-5-カルボアミド
  • オキシカルバマゼピン
  • 10(11H)-オキソ-5H-ジベンゾ[b,f]アゼピン-5-カルボアミド
  • オクスカルバゼピン, 98%
  • オキサカルバゼピン
  • オクスカルバゼピン (JAN)
  • 抗痙攣薬
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