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Relationship between plasma concentration and effect of dantrolene sodium in man.

作者信息

Meyler W J, Mols-Thürkow H W, Wesseling H

出版信息

Eur J Clin Pharmacol. 1979 Sep;16(3):203-9. doi: 10.1007/BF00562062.

DOI:10.1007/BF00562062
PMID:499321
Abstract

Dantrolen sodium is a muscle relaxant, which is used in the treatment of spasticity. Although it is given chronically, little is known about its pharmacokinetic behaviour. The relationship between the effect of a single oral dose of dantrolene sodium and its plasma concentration in healthy volunteers was studied by measuring the effect on the twitch tension, and in spastic patients on the decrease in muscle hypertonia. On the twitch tension dantrolene gave a depression of 49.1 +/- 9.4% (+/- DS) within 1.15 and 3.45 h after ingestion of 100 mg. The mean maximal plasma concentration was 1.24 +/- 0.32 microgram/ml (+/- SD). The effect and the plasma concentration were correlated. No relationship between the plasma concentration of dantrolene sodium and its effect could be established in patients, although definite activity in 6 out of 7 patients was observed after a single oral dose of 100 mg, and plasma concentration of dantrolene sodium greater than 0.3 microgram/ml were consistenly associated with better results than placebo treatment in 6 out of 7 patients.

摘要

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Relationship between plasma concentration and effect of dantrolene sodium in man.
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PRELIMINARY TRIAL OF CARISOPRODOL IN MULTIPLE SCLEROSIS.卡立普多治疗多发性硬化症的初步试验
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The effect of dantrolene sodium in relation to blood levels in spastic patients after prolonged administration.长期给药后丹曲林钠对痉挛患者血药浓度的影响。
J Neurol Neurosurg Psychiatry. 1981 Apr;44(4):334-9. doi: 10.1136/jnnp.44.4.334.
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Dantrolene. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in malignant hyperthermia, the neuroleptic malignant syndrome and an update of its use in muscle spasticity.丹曲林。对其药效学、药代动力学特性以及在恶性高热、抗精神病药物恶性综合征中的治疗用途的综述,并更新其在肌肉痉挛中的应用。
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含有药物相关代谢物的生物样本中丹曲林的测定。
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Clinical pharmaco--physiology of dantrolene sodium.丹曲林钠的临床药理生理学
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7
Effect of dantrolene sodium on calcium movements in single muscle fibres.丹曲林钠对单根肌纤维钙转运的影响。
Nature. 1974 Dec 20;252(5485):728-30. doi: 10.1038/252728a0.
8
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Actions of dantrolene sodium on contractions of the tibialis anterior and soleus muscles of cats under chloralose anaesthesia.丹曲林钠对氯醛糖麻醉下猫胫骨前肌和比目鱼肌收缩的作用。
Clin Exp Pharmacol Physiol. 1974 Mar-Apr;1(2):113-22. doi: 10.1111/j.1440-1681.1974.tb00532.x.
10
Studies on the mechanism of action of dantrolene sodium. A skeletal muscle relaxant.丹曲林钠作用机制的研究。一种骨骼肌松弛剂。
Naunyn Schmiedebergs Arch Pharmacol. 1972;275(1):83-94. doi: 10.1007/BF00505069.