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    • 5. 发明申请
    • TOLERABILITY OF MIRTAZAPINE AND A SECOND ACTIVE BY USING THEM IN COMBINATION
    • 米他宁的耐受性和使用它们在组合中的第二活性
    • US20100160294A1
    • 2010-06-24
    • US12637465
    • 2009-12-14
    • Srinivas RaoJay KranzlerJeffery J. Anderson
    • Srinivas RaoJay KranzlerJeffery J. Anderson
    • A61K31/55A61K31/5375A61K31/435A61K31/4402A61K31/4164A61K31/135A61K31/138A61P25/18A61P25/24A61P25/22A61P25/06
    • A61K31/4402A61K31/55A61K45/06A61K2300/00
    • A reduction in the side effects of treating with an agent having combined 5HT2/5HT3 and alpha-2 antagonistic activity is obtained by administering an agent having selective norepinephrine reuptake inhibitory or histamine H1 agonist activity. A combined dosage form comprising an agent having 5HT2/5HT3 and alpha-2 antagonistic activity and an agent having selective norepinephrine reuptake inhibitory or histamine H1 agonist activity is presented. Some embodiments of the combined dosage form comprise an immediate release component comprising an agent having 5HT2/5HT3 and alpha-2 antagonistic activity and a delayed release component comprising an agent having selective norepinephrine reuptake inhibitor or histamine H1 agonist activity. Some embodiments of the combined dosage form comprise a delayed release component comprising an agent having 5HT2/5HT3 and alpha-2 antagonistic activity and an immediate release component comprising an agent having selective norepinephrine reuptake inhibitor or histamine H1 agonist activity. Methods of treatment comprising administration of such a dosage form after waking are also provided. Also provided are kits for administration of the first therapeutic agent having 5HT2/5HT3 and alpha-2 antagonistic activity and the second therapeutic agent having selective norepinephrine reuptake inhibitory or histamine H1 agonist activity. The kits include instructions for the administration of the first therapeutic agent having 5HT2/5HT3 and alpha-2 antagonistic activity prior to bed and the second agent having selective norepinephrine reuptake inhibitory activity or histamine H1 agonist activity after waking. In some embodiments, the invention provides synergistic combinations of 5HT2/5HT3 antagonist/alpha-2 antagonist and selective norepinephrine reuptake inhibitor or histamine H1 agonist.
    • 通过施用具有选择性去甲肾上腺素再摄取抑制剂或组胺H1激动剂活性的药物,可以减少用具有组合的5HT 2 / 5HT 3和α-2拮抗活性的药物治疗的副作用。 提供了包含具有5HT2 / 5HT3和α-2拮抗活性的药剂和具有选择性去甲肾上腺素再摄取抑制剂或组胺H1激动剂活性的药剂的组合剂型。 组合剂型的一些实施方案包括立即释放组分,其包含具有5HT 2 / 5HT 3和α-2拮抗活性的试剂和包含具有选择性去甲肾上腺素再摄取抑制剂或组胺H1激动剂活性的试剂的延迟释放组分。 组合剂型的一些实施方案包括包含具有5HT 2 / 5HT 3和α-2拮抗活性的试剂的延迟释放组分和包含具有选择性去甲肾上腺素再摄取抑制剂或组胺H1激动剂活性的试剂的速释组分。 还提供了包括在醒来后施用这种剂型的治疗方法。 还提供了用于施用具有5HT2 / 5HT3和α-2拮抗活性的第一治疗剂的试剂盒,以及具有选择性去甲肾上腺素再摄取抑制或组胺H1激动剂活性的第二治疗剂。 试剂盒包括在睡眠前施用具有5HT2 / 5HT3和α-2拮抗活性的第一种治疗剂的说明书,以及在唤醒后具有选择性去甲肾上腺素再摄取抑制活性或组胺H1激动剂活性的第二药剂。 在一些实施方案中,本发明提供5HT2 / 5HT3拮抗剂/α-2拮抗剂和选择性去甲肾上腺素再摄取抑制剂或组胺H1激动剂的协同组合。