英文药名: Dixarit(Clonidine Tablets)

中文药名: 可乐定片

生产厂家: Boehringer Ingelheim

药品名称

通用名: 盐酸可乐定片
英文名: CLONIDINE HYDROCHLORIDE TABLETS
药品类别: 抗高血压药
性状: 本品为白色片
药理毒理

药理作用
1. 可乐定是α受体激动剂。
2. 可乐定直接激动下丘脑及延脑的中枢突触后膜α2受体，使抑制性神经元激动，减少中枢交感神经冲动传出，从而抑制外周交感神经活动。可乐定还激动外周交感神经突触前膜α2受体，增强其负反馈作用，减少末梢神经释放去甲肾上腺素，降低外周血管和肾血管阻力，减慢心率，降低血压。肾血流和肾小球滤过率基本保持不变。直立性症状较轻或较少见，很少发生体位性低血压。
3. 盐酸可乐定使卧位心输出量中度（15%~20%）减少，而不改变周围血管阻力；45°倾斜时轻度减少心输出量和周围血管阻力。长期治疗后心输出量趋于正常，但周围血管阻力持续降低。使用可乐定的患者大部分有心率减慢，但药物对血液动力学无影响。
4. 临床研究证实可乐定降低血浆肾素活性、减少醛固酮及儿茶酚胺分泌，但这些药理作用与抗高血压作用的确切关系并不完全清楚。
5. 急性使用盐酸可乐定刺激儿童和成人的生长激素释放，但长期使用不引起生长激素水平持续增高。
6. 可乐定可以治疗偏头疼、痛经及绝经期潮热，但其治疗机制不明，可能通过稳定周围血管发挥作用。可能通过抑制脑内α受体活性戒阿片瘾。致癌、致突变及生殖毒性 小鼠服用32至46倍人体最大推荐剂量的盐酸可乐定132周，无致癌事件。3倍于人体最大推荐剂量的盐酸可乐定对兔子无致畸作用，无红细胞毒性作用。盐酸可乐定150mcg/kg或约3倍于人体最大推荐剂量时不影响雄性或雌性小鼠的繁殖能力；但500~2000mcg/kg或10~40倍人体最大推荐剂量，影响雌性小鼠繁殖能力。
 
药代动力学
本品口服后70%~80%吸收，并很快分布到各器官，组织内药物浓度比血浆中高，能通过血脑屏障蓄积于脑组织。蛋白结合率为20%~40%。口服本品后半小时到1小时发挥降压作用，3~5小时血药浓度达峰值，一般为1.35ng/ml，作用持续时间6~8小时。消除半衰期为 12.7（6~23）小时，肾功能不全时延长。表观分布容积为2.1±0.4L/kg。肌酐清除率 3.1±1.2ml/(min.kg)。在肝脏代谢，约50%吸收的剂量经肝内转化。40%~60%以原形于24 小时内经肾排泄，20%经肝肠循环由胆汁排出。

适应症
1. 高血压（不作为第一线用药）
2. 高血压急症。
3. 偏头痛、绝经期潮热、痛经，以及戒绝阿片瘾毒症状。
 
用法用量
1. 降低血压
口服，起始剂量0.1 mg，一日2次；需要时隔2~4天递增，每日0.1~0.2mg。常用维持剂量为0.3~0.9mg/日，分2~4次口服。严重高血压需紧急治疗时开始口服 0.2mg，继以每小时0.1mg，直到舒张压控制或总量达 0.7mg，然后用维持剂量。
2. 绝经期潮热
一次0.025~0.075mg，每日2次。
3. 严重痛经
口服 0.025mg，每日2次，在月经前及月经时，共服14日。
4. 偏头痛
一次 0.025mg，每日2~4次，最多为 0.05mg，每日3次。
5. 极量
一次0.6mg，一日2.4mg。
任何疑问，请遵医嘱！

不良反应
大部分不良反应轻微，并随用药过程而减轻。常见：最常见口干（与剂量有关），昏睡，头晕，精神抑郁，便秘和镇静，性功能降低和夜尿多，瘙痒，恶心、呕吐，失眠，荨麻疹、血管神经性水肿和风疹，疲劳，直立性症状，紧张和焦躁，脱发，皮疹，厌食和全身不适，体重增加，头痛，乏力，戒断综合征，短暂肝功能异常。少见：肌肉关节痛，心悸、心动过速、心动过缓，下肢痉挛， 排尿困难，男性乳房发育，尿潴留， 更少见有多梦、夜游症、烦躁不安、兴奋、幻视幻听、谵妄、雷诺现象、心力衰竭，心电图异常如传导紊乱、心律失常、乙醇过敏、发烧、短暂血糖升高、血清肌酸磷酸激酶升高、肝炎和腮腺炎等。

禁忌症
对可乐定过敏者。
 
注意事项
1. 长期用药由于液体潴留及血容量扩充，可产生耐药性，降压作用减弱，但加利尿剂可纠正。
2. 治疗时突然停药或连续漏服数剂，可发生血压反跳性增高。多于12-48小时出现，可持续数天，其中5%-20%的病人伴有神经紧张、胸痛、失眠、脸红、头痛、恶心、唾液增多、呕吐、手指颤动等症状。日剂量超过1.2mg或与β受体阻滞剂合用时，突然停药后发生反跳性高血压的机会增多。因此，停药必须在1-2周内逐渐减量，同时加以其他降压治疗。血压过高时可给二氮嗪或α阻滞剂，或再用本品。若手术必须停药，应在术前 4-6小时停药，术中静滴降压药，术后复用本品。
3. 为保证控制夜间血压，每天末次服药宜在睡前。
4. 下列情况慎用：脑血管病、冠状动脉供血不足、精神抑郁史、近期心肌梗死、雷诺病、慢性肾功能障碍、窦房结或房室结功能低下、血栓闭塞性脉管炎。
5. 对诊断的干扰：应用本品时可使直接抗球蛋白（Coombs）实验弱阳性，尿儿茶酚胺和香草杏仁酸（VMA）排出减少。
 
孕妇及哺乳期妇女用药

动物研究发现对胎仔有害，人体研究尚不充分。本品可通过乳汁分泌。此药只有必要时方可应用于妊娠及哺乳期妇女。
老年患者用药

老年人对降压作用较敏感，肾功能随年龄增长降低，应用时须减量，并注意防止体位性低血压。
 
药物相互作用

1. 与乙醇、巴比妥类或镇静药等中枢神经抑制药合用，可加强中枢抑制作用。
2. 与其他降压药合用可加强降压作用。
3. 与β受体阻滞剂合用后停药，可增加可乐定的撤药综合征危象，故宜先停用β受体阻滞剂，再停可乐定。
4. 与三环类抗抑郁药合用，减弱可乐定的降压作用。可乐定须加量。
5. 与非甾体类抗炎药合用，减弱可乐定的降压作用。

药物过量

过量的症状和体征包括低血压、心动过缓、嗜睡、烦躁、乏力、困倦、反射减低或丧失、恶心、呕吐和通气不足。过大剂量可有可逆性心脏传导障碍或心律失常，短暂高血压。低血压时应平卧，抬高床脚，必要时静脉输液，给多巴胺升血压。高血压时静脉给呋噻米、二氮嗪、酚妥拉明或硝普钠对症治疗。

规格：0.025mg *112 片

Clonidine Hydrochloride Solution for injection

What is this medicine?

CLONIDINE (KLOE ni deen) is used for relief of severe pain that is not controlled by other pain medications.
 
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•heart or blood vessel disease
•injection site infection
•kidney disease
•recent heart attack or stroke
•an unusual or allergic reaction to clonidine, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

This medicine is for infusion into the spine. It is given by a health care professional in a hospital or clinic setting.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What if I miss a dose?

If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses. If you take only one dose a day and forget to take it that day, do not take a double dose the next day.

What may interact with this medicine?

Do not take this medicine with any of the following medications:
•guanethidine
•MAOIs like Carbex, Eldepryl, Marplan, Nardil, and Parnate

This medicine may also interact with the following medications:
•barbiturates, like phenobarbital
•beta blockers
•heart medicines such as digoxin or digitoxin
•fluphenazine
•medicine for mental depression
•prescription pain medicines

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Your condition will be monitored carefully while you are receiving this medicine.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may increase this effect. Avoid alcoholic drinks.

Your mouth may get dry. Chewing sugarless gum or sucking hard candy, and drinking plenty of water may help. Contact your doctor if the problem does not go away or is severe.

If you have an epidural catheter, report any pain or redness at the catheter site to your doctor or health care professional as soon as possible.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•anxiety, nervousness
•chest pain
•dizziness or fainting spells
•fever, chills
•increased sweating
•fast, irregular heartbeat
•pain or difficulty passing urine
•swelling of feet or legs

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•constipation
•difficulty sleeping
•headache
•unusually weak or tired

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.