Primidone

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Chemical Structure| 125-33-7 同义名 : 扑米酮;去氧苯比妥;扑痫酮;密苏林;美速林 ;NSC 41701; NCI-C56360; XcelBrand of Primidone; Sertan; Sanofi-Synthelabo Brand of Primidone; Resimatil; Mysoline; Mizodin; Mylepsinum; Primaclone
CAS号 : 125-33-7
货号 : A538446
分子式 : C12H14N2O2
纯度 : 99%
分子量 : 218.25
MDL号 : MFCD00038662
存储条件：

Pure form Sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(229.09 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • Sodium Channel
描述 Primidone is a minor first-generation antiepileptic drug, and also remains a first-line treatment of essential tremor. Although it is metabolized in phenyl-ethyl-malondamide and phenobarbital, active metabolites that contribute also to its action, primidone is not a prodrug and is active by itself. Generally accepted therapeutic range for primidone is between 5 and 10 mg/L (23-46 mmol/L)[3]. Primidone, 50 to 1,000 mg/d, reduced the amplitude of essential tremor in both untreated and propranolol-treated patients. Low doses were as effective as high doses. Primidone decreased tremor more than propranolol. A single oral dose (250 mg) decreased tremor by 60% 1 to 7 hours after ingestion, with stable serum primidone levels. Tremor control was lost when phenobarbital was substituted for primidone shows primidone is an effective agent for the treatment of essential tremor[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01771523 Goiter Not Applicable Completed - Turkey ... 展开 >> Maltepe University School of Medicine, General Surgery Department İstanbul, Turkey, 34843 收起 <<
NCT01816568 Acute Appendicitis Not Applicable Completed - -
NCT01772745 Gallbladder Disease Not Applicable Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.58mL

0.92mL

0.46mL

22.91mL

4.58mL

2.29mL

45.82mL

9.16mL

4.58mL
参考文献

[1]Macdonald RL, Kelly KM. Antiepileptic drug mechanisms of action. Epilepsia. 1995;36 Suppl 2:S2-12.

[2]Calzetti S, Findley LJ, et al. Phenylethylmalonamide in essential tremor. A double-blind controlled study. J Neurol Neurosurg Psychiatry. 1981 Oct;44(10):932-4.

[3]Bentué-Ferrer D, Verdier MC, Tribut O. Suivi thérapeutique pharmacologique de la primidone et du phénobarbital [Therapeutic drug monitoring of primidone and phenobarbital]. Therapie. 2012 Jul-Aug;67(4):381-90. French.

[4]Koller WC, Royse VL. Efficacy of primidone in essential tremor. Neurology. 1986 Jan;36(1):121-4.