| 药品名称 | Flunarizine |
|---|---|
| 分子靶点 | Voltage-dependent T-type calcium channel subunit alpha-1G;Voltage-dependent T-type calcium channel subunit alpha-1H;Voltage-dependent T-type calcium channel subunit alpha-1I;Histamine H1 receptor;Calmodulin |
| 酶 | Cytochrome P450 2D6;Cytochrome P450 2C9;Cytochrome P450 1A1;Cytochrome P450 1A2;Cytochrome P450 2A6;Cytochrome P450 3A4 |
| 药物类型 | Small Molecule |
| 研发阶段 | Approved |
| 药物描述 | Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy. |
| 结构式 |
 |
| 药物别名 | 1-[bis(4-fluorophenyl)methyl]-4-[(2E)-3-phenylprop-2-en-1-yl]piperazine;Flunarizina;Flunarizine;Flunarizinum |
| 治疗类别 | Agents causing hyperkalemia;Antiarrhythmic agents;Anticonvulsants;Antimigraine Agents, Miscellaneous;Antivertigo Preparations;Bradycardia-Causing Agents;Calcium Channel Blockers;Cardiovascular Agents;Central Nervous System Agents;Central Nervous System Depressants;Cytochrome P-450 CYP1A2 Substrates;Cytochrome P-450 CYP2A6 Substrates;Cytochrome P-450 CYP2C9 Substrates;Cytochrome P-450 CYP2D6 Substrates;Cytochrome P-450 CYP3A Substrates;Cytochrome P-450 CYP3A4 Substrates;Histamine Agents;Histamine Antagonists;Histamine H1 Antagonists;Membrane Transport Modulators;Nervous System;Neurotransmitter Agents;Piperazine Derivatives;Piperazines;Vasodilating Agents |
| UNII号 | R7PLA2DM0J |
| CAS号 | 52468-60-7 |
| 分子量 | 404.4948 |
| 分子式 | C26H26F2N2 |
| 适应症 | Used in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy. |
| 药效学 | Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. |
| 作用机制 | Flunarizine inhibits the influx of extracellular calcium through myocardial and vascular membrane pores by physically plugging the channel. The decrease in intracellular calcium inhibits the contractile processes of smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload. |
| 吸收 | 85% following oral administration. |
| 蛋白结合 | 99% bound to plasma proteins |
| 代谢 | Hepatic, to two metabolites via N-dealylation and hydroxylation. |
| 半衰期 | 18 days |
| 毒理 | -Flunarizine should be used with care in patients with depression or those being prescribed other agents, such as phenothiazines, concurrently, which may cause extrapyramidal side-effects.-Acute overdosage has been reported and the observed symptoms were sedation, agitation and tachycardia.-Treatment of acute overdosage consists of charcoal administration, induction of emesis or gastric lavage, and supportive measures. No specific antidote is known. |
| ATC代码 | N07CA03 |
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