您当前所在的位置:首页 > 产品中心 > 产品信息
Oxcarbazepine_分子结构_CAS_28721-07-5)
点击图片或这里关闭

Oxcarbazepine

产品号 DB00776 公司名称 DrugBank
CAS号 28721-07-5 公司网站 http://www.ualberta.ca/
分子式 C15H12N2O2 电 话 (780) 492-3111
分子量 252.26798 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 656

产品价格信息

请登录

产品别名

标题
Oxcarbazepine
IUPAC标准名
9-oxo-2-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,12,14-hexaene-2-carboxamide
IUPAC传统名
9-oxo-2-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,12,14-hexaene-2-carboxamide
商标名
Trileptal
别名
Oxcarbamazepine

产品登记号

PubChem CID 34312
PubChem SID 46507580
CAS号 28721-07-5

产品性质

疏水性(logP) 1.5
溶解度 308 mg/L at 25 oC (SRC PhysProp estimated -- MEYLAN,WM et al. (1996))

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved
Description Oxcarbazepine is structurally a derivative of carbamazepine, adding an extra oxygen atom to the benzylcarboxamide group. This difference helps reduce the impact on the liver of metabolizing the drug, and also prevents the serious forms of anemia occasionally associated with carbamazepine. Aside from this reduction in side effects, it is thought to have the same mechanism as carbamazepine - sodium channel inhibition - and is generally used to treat partial seizures in epileptic children and adults.
Indication For use as monotherapy or adjunctive therapy in the treatment of partial seizures in adults with epilepsy and as adjunctive therapy in the treatment of partial seizures in children ages 4-16 with epilepsy.
Pharmacology Oxcarbazepine is structurally a derivative of carbamazepine, adding an extra oxygen atom to the benzylcarboxamide group. This difference helps reduce the impact on the liver of metabolizing the drug, and also prevents the serious forms of anemia occasionally associated with carbamazepine. Aside from this reduction in side effects, it is thought to have the same mechanism as carbamazepine - sodium channel inhibition - and is generally used to treat the same conditions.
Toxicity Isolated cases of overdose with oxcarbazepine have been reported. The maximum dose taken was approximately 24,000 mg. All patients recovered with symptomatic treatment.
Affected Organisms
Humans and other mammals
Biotransformation Oxcarbazepine is completely absorbed and extensively metabolized to its pharmacologically active 10-monohydroxy metabolite (MHD). MHD is metabolized further by conjugation with glucuronic acid.
Absorption Completely absorbed following oral administration. Food has no effect on the rate and extent of absorption of oxcarbazepine.
Half Life The half-life of the parent is about 2 hours, while the half-life of MHD is about 9 hours, so that MHD is responsible for most anti-epileptic activity.
Protein Binding Approximately 40% of the active 10-monohydroxy metabolite (MHD) is bound to serum proteins, predominantly to albumin. Neither oxcarbazepine nor its MHD binds with alpha-1–acid blycoprotein.
Elimination Oxcarbazepine is cleared from the body mostly in the form of metabolites which are predominantly excreted by the kidneys. Fecal excretion accounts for less than 4% of the administered dose.
Distribution * 49 L
References
Mazza M, Della Marca G, Di Nicola M, Martinotti G, Pozzi G, Janiri L, Bria P, Mazza S: Oxcarbazepine improves mood in patients with epilepsy. Epilepsy Behav. 2007 May;10(3):397-401. Epub 2007 Feb 14. [Pubmed]
External Links
Wikipedia
RxList
PDRhealth
Drugs.com

参考文献

  • Mazza M, Della Marca G, Di Nicola M, Martinotti G, Pozzi G, Janiri L, Bria P, Mazza S: Oxcarbazepine improves mood in patients with epilepsy. Epilepsy Behav. 2007 May;10(3):397-401. Epub 2007 Feb 14. Pubmed