药品详情:
【苏沃雷生片Belsomra(Suvorexant) 简述】
苏沃雷生片Belsomra(Suvorexant)是个别食欲素受体拮抗剂。
【苏沃雷生片Belsomra(Suvorexant) 适应症】
苏沃雷生片Belsomra(Suvorexant)用于治疗失眠症。
【苏沃雷生片Belsomra(Suvorexant) 规格】
本品为片剂,分为10mg/15mg/20mg三种规格,每瓶100片。
【苏沃雷生片Belsomra(Suvorexant) 服用方法】
成人;每天服用一次,每次20毫克剂。
老年人;每天服用一次,每次15毫克。即可在睡前服用。
【苏沃雷生片Belsomra(Suvorexant) 注意事项】
1.作用机制
suvorexant的选择性是高度可逆的拮抗剂食欲素受体,人食欲肽-1(OX1)受体和食欲肽-2(OX2)对受体(Ki值)的亲和力分别为0.55和0.35纳米。
suvorexant,通过可逆地抑制OX1和OX2的结合受体食欲素A和B是促进觉醒的神经肽,到大脑从清醒到睡眠转变被认为诱导睡眠。
suvorexant的γ-氨基丁酸(GABA),没有表现出血清素,多巴胺,去甲肾上腺素,褪黑激素,组胺,乙酰胆碱和阿片样物质受体(KI>10μM)的亲和力。
2.对睡眠的影响
suvorexant大鼠正常活性相(10,30和100毫克/千克),狗(1和3mg / kg的)中,当口服给予猴子(10毫克/千克),唤醒时间减少,非REM睡眠和REM睡眠时间增加了。
【苏沃雷生片Belsomra(Suvorexant) 生产厂家】
苏沃雷生片Belsomra(Suvorexant)是由美国默沙东MSD制药公司生产。
Belsomra(Suvorexant)
Suvorexant, sold under the trade name Belsomra, is a medication for the treatment of insomnia. It is effective for insomnia, at least for four weeks and as compared to a placebo.
Suvorexant is a selective, dual orexin receptor antagonist (DORA) made by Merck & Co. It was approved for sale by the U.S. Food and Drug Administration (FDA) on August 13, 2014.The U.S. Drug Enforcement Administration (DEA) has placed it on the list of schedule IV controlled substances,]as it may lead to limited physical dependence or psychological dependence relative to the drugs or other substances in schedule III. The potential for psychological dependence is similar to that of zolpidem.[5]
The drug was initially released November 2014 in Japan, then later reached the United States in February 2015and Australia in November 2016.
Medical uses
Suvorexant is used for the treatment of insomnia, characterized by difficulties with sleep onset and/or sleep maintenance.
It is unclear how the medication compares to others used for insomnia as no comparisons have been done.It is also unclear if this medication is safe among people with a history of addiction, as they were excluded from the clinical trials of suvorexant.
Contraindications
This drug is not recommended in people with liver impairment.Suvorexant pregnancycategory is currently classified as Category C. Based on animal testing, this medication may cause fetal harm during pregnancy and should only be given in pregnancy if the potential benefit justifies the potential harm to the fetus. Evidence is inconclusive about whether using this medication while breastfeeding puts the infant at risk of harm.
Suvorexant is contraindicated in people diagnosed with narcolepsy.
Mechanism of action
Suvorexant exerts its therapeutic effect in insomnia through antagonism of orexin receptors. The orexin neuropeptide signaling system is a central promoter of wakefulness. Blocking the binding of wake-promoting neuropeptides orexin A and orexin B to receptors orexin receptor type 1 (OX1) and orexin receptor type 2 (OX2) is thought to suppress wake drive.Animal studies report the binding affinities for OX1 (0.55 nM) and OX2 (0.35 nM).
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