| 简介：
部份中文阿雷地平处方资料（仅供参考）
Sapresta（Aranidipine）阿雷地平
别名
阿拉尼地平，阿雷地平；Sapresta；Bec
剂型
每包250mg中含阿拉尼地平5mg；每包500mg中含阿拉尼地平10mg。
药理作用
阿拉尼地平是在硝苯地平的结构中引入碳基的二氨吡啶类钙拮抗剂。它对正常血压的每天规律性变化无明显影响，每天口服1次便可稳定地控制血压。阿拉尼地平具有硝苯地平类的药理作用。
药代动力学
健康人口服阿拉尼地平颗粒5mg、10mg、20mg时，原形药物与代谢物M-1的血药峰浓度及药时曲线下面积与服用剂量成正比，且不受食物影响。给原发性高血压患者服用阿拉尼地平颗粒剂10mg后，原形药物与其代谢M-1的血药峰浓度及药时曲线下面积，比健康人的测出值大3～4倍。高血压合并慢性肾功能不全者每天服用阿拉尼地平颗粒剂10mg，连用8天未见有蓄积性。
适应证
高血压。
禁忌证
1.对阿拉尼地平或二氢吡啶类过敏者禁用。
2.重症肝损害者忌用或停用。
3.阿拉尼地平有致畸性和致死胎作用，孕妇禁用。哺乳期妇女忌用或及时停止哺乳。
注意事项
1.突然停药可使病情加重，故须停用阿拉尼地平前，应逐渐减量，仔细观察；
2.极少数人出现血压过度下降，应酌情减量或停药，并对症处理；
3.服阿拉尼地平者不得高空作业、驾车等机械操作，以免因降压而发生意外；
4.老年人防止过度降压，以免引起脑梗死，应从小剂量每天5mg开始，慎重用药；
5.小儿不宜用。
不良反应
1.少数患者偶有转氨酶、脱氢酶等升高；皮疹；尿酸、尿素氨、肌酸酐升高；白细胞、红细胞减少等，出现异常应停药。
2.有时出现颜面潮红、热感、头昏眼花、倦怠、水肿、心慌、心率加快。有时头痛、头重、步态蹒跚、麻木感等。尚偶有眼痛、结膜充血、异味感、多汗、尿频以及尿激酶、肌酐激酶、总胆固醇和血糖值升高等。
用法用量
口服，首次5mg，每天1次。以后每次5～10mg，每天1次。可酌情增减剂量。若效果不充分时可增量至每天20mg，或遵医嘱。
药物的相互作用
1.与其他降压药如中枢性降压药利血平、甲基多巴、哌唑嗪等或β-受体阻滞如普萘洛尔等并用可使降压作用增强。
2.同类药硫氮酮可使阿拉尼地平血中浓度升高。
3.西咪替丁可使阿拉尼地平血中浓度升高。
4.与地高辛合用，阿拉尼地平可使地高辛血中浓度升高。
5.利福平、苯巴比妥、苯妥英钠等可使阿拉尼地平血中浓度降低。
6.与红霉素伍用，可使其他钙拮抗剂作用增强。
专家临床研究
阿拉尼地平对原发性高血压的降压作用是通过降低全身外周血管阻力11%～16%实现的。与同类药硝苯地平缓释胶囊、硫氮酮等常规剂量的降压作用无显著性差别，也未见有不良反应。
包装
胶囊剂
5mg：PTP包装：100胶囊（10粒×10）
10毫克：PTP包装：100胶囊（10粒×10）
制造厂商
大鹏药业有限公司
完整处方资料附件：http://www.info.pmda.go.jp/go/pack/2149038D1044_1_04/
A package insert
Name of drug classification
Persistent Ca antagonist
Sales name
Suppressor capsule 5 mg
common name
Alanidipine (Aranidipine: JAN)
Chemical name
(±) -Methyl 2-oxopropyl 1,4-dihydro-2,6-dimethyl-4- (2-nitrophenyl) -3,5- pyridinedicarboxylate
Molecular formula
C19 H20 N 2 O 7
Molecular weight
388.37
Melting point
148 - 151 ° C
Distribution coefficient
3 × 102 (1-octanol / aqueous solvent, pH 2 to 9)
Property
It is a yellow crystal or a crystalline powder, it has no odor.
Dissolved in acetone, dichloromethane or 1,4-dioxane, slightly soluble in methanol, less soluble in ethanol (99.5), very insoluble in diethyl ether, hardly soluble in water.
It changes with light.
1,4-Dioxane solution (1 → 50) does not exhibit optical rotatory power
composition
Component · Content
Among 1 capsule, alanidipine 5 mg
Additive
Purified sucrose, methacrylic acid copolymer S, talc, aminoalkyl methacrylate copolymer RS, macrogol 6000
Capsule body: Hypromellose, carrageenan, potassium chloride, dimethylpolysiloxane, sorbitan fatty acid ester, polysorbate 80, titanium oxide, yellow No. 5, carnauba wax, magnesium stearate
Contraindications
Pregnant women or lactating women who may be pregnant (see "Administration to pregnant women, maternity women, lactating women, etc.")
Patients with a history of hypersensitivity to the components of this drug
Indication or effect
high blood pressure
The initial dose as alanidipine is 5 mg, and usually 5 to 10 mg is orally administered to adults once a day.
Incidentally, depending on age and symptoms, it will increase or decrease accordingly, but if the effect is insufficient, it can be increased to 20 mg once a day.
Careful Administration
Patient with liver dysfunction [easy to show side effects]
Patients with kidney dysfunction [easy to show side effects]
Patients with a history of hypersensitivity to dihydropyridine compounds
Elderly (see "Administration to the elderly" section)
Medicinal pharmacology
Antihypertensive effect
By administering once daily to patients with hypertension, stable antihypertensive effect was observed until the following day without affecting daily blood pressure fluctuation.
A dose-dependent antihypertensive effect was observed in a single oral administration using spontaneously hypertensive rats, renal hypertension rats, deoxycorticosterone acetate salt-loaded hypertensive rats and renal hypertensive dogs.
In addition, in 22 weeks feeding diet using spontaneously hypertensive rats with cerebral apoplexy, suppression of blood pressure rise, and suppression of hypertensive organ disorder (stroke, myocardial fibrosis, proliferative and necrotizing arteritis, malignant nephrosclerosis etc. ), And prolonged life effect was recognized.
Action on circulation dynamics
As a result of examining the circulatory dynamics of patients with light and moderate hypertension, it was found that the hypotensive effect was mainly due to a decrease in total peripheral vascular resistance (11 to 16%).
Renal blood flow, urine volume, urine Na + and K + excretion increased in oral administration using spontaneously hypertensive rats.
Hypotensive action mechanism
Inhibition of calcium ions into cells in the aortic specimen of guinea pig was suppressed and concentration of the binding of nitrendipine to the receptor was inhibited in porcine aorta specimen in a concentration dependent manner. We also suppressed the inward calcium ion current in a concentration dependent manner in guinea pig isolated ventricular myocytes.
The main mechanism of action of this drug acts on calcium channels in vascular smooth muscle cells and relaxes the vascular smooth muscle by suppressing the inflow of calcium ions from outside the cell into the cell to expand the blood vessel It is thought that it exerts antihypertensive effect. |
