中文药名: 硝苯地平

药品名称
通用名称：硝苯地平
英文名：Nifedipine
其它中文名：利心平、尼非地平、硝苯吡啶、硝苯啶
其它英文名：Nifelat、Procardia

规格
硝苯地平胶囊10mg, 20mg；硝苯地平缓释片 30mg, 60mg, 90mg。

药理作用
药效学
本品为一仲钙离子内流阻滞剂或慢通道阻滞剂，阻滞钙离子经过心肌或平滑肌细胞膜面的通道而进入细胞内，由此引起周身血管，包括冠状动脉(正常供血区或缺血区)的血管张力减低而扩张，因而可以降低血压，增加冠状动脉血供。并能抑制自发或麦角新碱所引起的冠状动脉痉挛。另一方面能抑制心肌收缩，使心肌作工减低，耗氧量减少，缓解心绞痛。治疗用量时对窦房结与房室结功能影响小。给本品后血压下降时可有反射性心率加速。心功能正常者给药后心脏指数略增，左心室喷血分数(LVEF)、左室舒张期末压(LVEDP) 及左室舒张期末容积(LVEDV)不变; 心功能不良者则给药后LVEF 略增而左室充盈压减低。
药动学
口服胃肠道吸收良好, 达90％左右，舌下含服吸收也快。蛋白结合率约90％, 口服30分钟血药浓度达高峰, 舌下或嚼碎服达峰时间提前。在10～30mg剂量范围内随剂量而增高, 但不受剂型与给药途径的影响。口服15分钟起效, 1～2小时作用达高峰, 作用持续4～8小时; 舌下给药2～3分钟起效, 20分钟达高峰。半衰期呈双相,半衰期α2.5～3小时, 半衰期β为5小时,半衰期受剂量影响。在肝脏代谢,产生无活性代谢产物, 80％以肾排出, 20％随粪便排出。

适应症　　
用于治疗高血压、心绞痛。包括冠状动脉痉挛所致的心绞痛和变异型心绞痛、冠状动脉阻塞所致的典型心绞痛或劳力性心绞痛。
本品适用于各种类型高血压病及肾性高血压的治疗，对顽固性、重度高血压及伴心力衰竭的高血压患者也有较好疗效。本品也适用于防治心绞痛，特别是变异型心绞痛和冠状动脉痉挛所致心绞痛。由于本品对呼吸功能无不良影响，故适用于患有呼吸道阻塞性疾病的心绞痛患者。对这两类疾病本品目前均为首选良药，尤其是缓释制剂产生反射性心动过速的不良反应较轻，1日服药1～2次，更为患者带来方便。此外，本品亦可用于治疗尿道梗阻或防治运动性哮喘。

用法用量　
成人常用量口服，开始一次 10mg，每日 3次，渐增至最大疗效而能耐受，剂量的增加每隔 1—2周进行 1次。住院患者可每隔 4～6小时增加 1次，每次 10mg。若按症状的发生次数和严重程度作为衡量疗效的标准，则剂量调整可以在 3天内完成，但必须严密观察监护。成人单剂最大量为 30mg，1日内总量不超过 120mg。
硝苯地平缓释片[用法用量]：
用于心绞痛，每日二次，每次一片。必要时可增加至每日二次，每次二片。
用于高血压。每日二次，每次一片。必要时可增加至每日二次，每次二片。最好在饭前或饭后服用，每次服用时间间隔不得少于 4小时。对肝、肾功能不全的病人，所开处方应谨慎，剂量应有所减少。
任何疑问，请遵医嘱！

禁用/慎用　
(1)啮齿类动物实验发现有致畸胎作用，人体研究尚不充分，在孕妇应用必须权衡利弊。
(2)在乳母的临床研究尚不够充分，服用本品者最好不授乳。
(3)在老年人本品的半衰期可能延长，应用须加注意。
(4)严重主动脉瓣狭窄、肝或肾功能不全患者须慎用。
心功能减退患者应慎用，孕妇、心源性休克者忌用。
对乙酰水杨酸和其它合成前列腺素抑制剂有过敏反应的病人，应慎用此药。
严重低血压者慎用。

给药说明　　
①长期给药不宜骤停，以避免发生停药综合征而出现反跳现象，如心绞痛发作；
②用药后注意是否有降压后出现反射性交感兴奋而心率加快以致加剧心绞痛；
③用药后，后负荷降低，也被用于治疗心力衰竭，但仅适用于高血压、冠心病所致的左心衰竭，用时还得注意有否心肌抑制的表现；
④与西咪替丁同用时本品的血药浓度峰值增高，须注意调节剂量。
服药期间必须经常测血压和做心电图检查，在开始用药而决定剂量的过程中以及从维持量加大用量时尤须注意。
少数患者初次服用本品后有首剂现象，表现为头痛、眩晕 心绞痛或心肌梗死、急性尿潴留等，故对心功能减退患者应慎用，一旦发生心肌缺血症状应立即停药。
日剂量大于120mg时，突然停药会产生撤药综合征，主要表现为心绞痛的复发或频繁发作。其原因与心肌细胞长期缺钙后对钙处于高敏状态，一旦停药，正常量钙离子进入细胞内即可产生过量的反应。
长期服药宜与利尿剂合用。

不良反应　
(1)反应短暂而较多见的是踝、足与小腿肿胀，用利尿药可消退；较少见的是呼吸困难、咳嗽、哮鸣、心跳快而重(由于降压后交感活性反射性增强；罕见的是胸痛(可出现于用药后 30分钟左右)、昏厥(血压过低所致)、胆石症、过敏性肝炎。
(2)反应持续出现而须加注意的有；眩晕、头昏、脸红及热感、头痛、恶心。
(3)逾量时可出现低血压，此时应停药观察，必要时用血管收缩药。
白细胞减少, 颜面或皮肤潮红, 心悸, 心动过速。个别病例舌根或口周麻木, 口干, 出汗, 头痛, 恶心, 浮肿, 男性乳房增大,视物模糊。个别病例出现心肌梗塞, 皮肤坏死, 局部组织损伤。可引起肝损害。
一般较轻，主要有头痛、乏力、颜面潮红、心悸、嗜睡、眩晕、恶心、呕吐、口干、便秘、食欲减退、腿部痉挛、舌根麻木、牙龈肿胀等。长期服用可能引起水钠潴留，水肿，多发生于踝部，偶见于脸部及眶周；剂量过大时可引起心动过缓及低血压。
也有报告发生暂时性视网膜缺血者。有报告发生易激动、震颤、好斗、抑郁、小腿及手部肌肉严重挛缩、恶梦及幻视。
此药可致肝脏损害。有报告此药可致肾功能不全、粒细胞减少者。
有报告发生末梢水肿，特别是小腿。有发生红斑伴疼痛及水肿、对光敏感及周身大疱疹。
有报告此药使患者在运动时出现双眼视物不清。有发生牙龈增生者，它与环孢素(Ciclosporin)合用则牙龈增生的发生率更高。有发生味觉及嗅觉异常者，停药24小时内即恢复正常。

药物相互作用
(1)与其他降压药同用可致极度低血压。
(2)与 β阻滞剂同用可导致血压过低、心功能抑制，心力衰竭发生的机会增多。
(3)突然停用 β阻滞剂治疗而启用本品，偶可发生心绞痛，须逐步递减前者用量。
(4)与蛋白结合率高的药物如双香豆素、洋地黄苷类、苯妥英钠、奎尼丁、奎宁、华法林等同用，这些药的游离浓度常发生改变。
(5)与硝酸酯类同用，可使心绞痛作用增强。本品与多数降压药物合用具协同降压作用，但一般不与哌唑嗪合用以免引起血压过度下降，也不与β受体阻滞药合用以防过度抑制心肌，出现心力衰竭或加重心绞痛及产生严重低血压。地尔硫卓可抑制本品氧化代谢，使硝苯地平血药浓度增加。本品可能增加地高辛血药浓度，故与地高辛合用时，应注意调整地高辛剂量。
它也使苯妥英浓度升高。它使奎尼丁排除增多，使奎尼丁的抗心律失常作用减低。它与哌唑嗪合用可导致急性低血压症。
有些药物(抗凝血剂、血小板凝聚抑制剂、胰岛素和口服抗糖尿病药)不应与本药合用。
本品可与其它抗高血压药物合用，有协同作用，应注意有时造成血压过低。
与心得安、洋地黄甙类、甲腈咪胍、利福平、苯妥英钠及葡萄柚汁等同服，可改变血药浓度及降压效果，应注意。

【原产地英文商品名】NIFEDICAL XL TABLET SA SR OSM(PROCARDIA XL OSM GENERIC)60mg/tab 30tabs/box
【原产地英文药品名】NIFEDIPINE
【原产地英文商品名】
注：以下产品是不同的规格和不同的价格，购买时请以电话咨询为准！
·NIFEDICAL XL OSM缓释片(PROCARDIA XL OSM仿制药)60毫克/片 30片/盒
·NIFEDICAL XL OSM缓释片(PROCARDIA XL OSM仿制药)30毫克/片 30片/盒

·硝苯地平ER OSM缓释片(PROCARDIA XL OSM仿制药)90毫克/片 30片/盒
·硝苯地平ER OSM缓释片(PROCARDIA XL OSM仿制药)60毫克/片 30片/盒
·硝苯地平ER OSM缓释片(PROCARDIA XL OSM仿制药)30毫克/片 30片/盒
【中文参考药品译名】硝苯地平

GENERIC NAME: nifedipine

BRAND NAMES: Adalat, Procardia, Afeditab, Nifediac

DRUG CLASS AND MECHANISM: Nifedipine belongs to a class of medications called calcium channel blockers (CCBs) that are used to treat angina (heart pain), high blood pressure, and abnormal heart rhythms. Other drugs in the same class include amlodipine (Norvasc), diltiazem (Cardizem LA, Tiazac), felodipine (Plendil), isradipine (Dynacirc), nicardipine (Cardene), nimodipine (Nimotop), and verapamil (Covera-HS, Veralan PM, Calan). Like other CCBs, nifedipine works by blocking the flow of calcium into the muscle cells surrounding the arteries that supply blood to the heart (coronary arteries) as well as other arteries of the body. Since the inflow of calcium is what causes the muscle cells to contract, blocking the entry of calcium relaxes the muscles and dilates (widens) the arteries. By dilating coronary arteries, nifedipine increases the flow of blood to the heart. This treats and prevents angina which occurs when the flow of blood to the heart is not adequate to supply the heart with enough oxygen necessary to pump blood. Relaxing the muscles surrounding other arteries of the body lowers blood pressure and thereby reduces the pressure against which the heart must pump blood and function. This reduces the demand of the heart for oxygen--another mechanism by which CCBs treat and prevent angina. In addition, nifedipine slows conduction of the electrical current that travels through the heart that causes the muscle of the heart to contract. This effect can be used to correct abnormally rapid heartbeats.

PRESCRIPTION: Yes

GENERIC AVAILABLE: Yes

PREPARATIONS: Capsules:10 and 20 mg. Tablets: 30, 60, and 90 mg

STORAGE: Tablets should be stored at room temperature 15-25 C (59-77 F). They should be protected from light, moisture, and humidity.

PRESCRIBED FOR: Nifedipine is used for the treatment and prevention of angina resulting from either an increased workload on the heart (as with exercise) or spasm of the coronary arteries. It is used in the treatment of high blood pressure, to treat abnormally fast heart rhythms such as atrial fibrillation, and in the prevention of episodes of rapid heart rhythm originating from the atria of the heart.

It also is used to dilate blood vessels that go into spasm such as those causing Raynaud's phenomenon, a painful condition of the hands caused by spasm of the arteries supplying blood to the hands. Non-FDA approved uses include anal fissures (applied to the fissures), prevention of migraine headaches in adults, ureteral stones (as secondary therapy) and wound healing (applied to the skin).

DOSING: The usual dose for nifedipine capsules is 10 to 20 mg three times daily. It is important to swallow capsules whole. For extended release tablets, the usual dose is 30 or 60 mg once daily. The tablets should be swallowed whole and not bitten or cut in half. Nifedipine can be taken with or without food.

DRUG INTERACTIONS: In rare instances, congestive heart failure has been associated with nifedipine, usually in patients already on a beta blocker, for example, propranolol (Inderal), metoprolol (Lopressor), etc. Excessive lowering of blood pressure (hypotension) during initiation of nifedipine treatment can occur, especially in patients already taking another blood pressure lowering drug.
Generally, nifedipine is avoided in children.

Nifedipine decreases the elimination of digoxin (Lanoxin) by the kidneys which can increase digoxin blood levels in the blood and give rise to digoxin toxicity. It is important, therefore, to monitor blood levels of digoxin in order to avoid toxicity.

Nifedipine interferes with the breakdown of tacrolimus (Prograf) by the liver, which in turn causes elevated blood levels of tacrolimus and may increase the risk of toxicity from tacrolimus.

Nifedipine reduces the blood levels of quinidine (Quinaglute, Quinidex, Quinora) which may reduce the effectiveness of quinidine. Conversely, blood levels of nifedipine are increased by quinidine and may lead to side effects from nifedipine.

Cimetidine (Tagamet) interferes with breakdown by the liver of nifedipine and increases nifedipine blood levels. Therefore, cautious dosing is necessary when both medications are administered concurrently.

Nifedipine should not be taken with grapefruit juice since grapefruit juice (one glass, approximately 200 ml) inhibits the breakdown of nifedipine by the liver and increases the levels of nifedipine in the blood.

PREGNANCY: There are no adequate studies of nifedipine in pregnant women, and in general, it is avoided during pregnancy.

NURSING MOTHERS: Nifedipine is excreted in human breast milk. Generally, nifedipine is avoided in nursing mothers.

SIDE EFFECTS: Side effects of nifedipine are generally mild, and reversible. Most side effects are expected consequences of the dilation of the arteries. The most common side effects include headache, dizziness, flushing, and edema (swelling) of the lower extremities. Less common side effects include dizziness, nausea and constipation.