阿那格雷 Anagrelide
中文别名：	阿那格雷、氯喹咪唑酮、盐酸阿那格利
英文别名：	Agrylin、Anagrelide Hydrochloride
生产企业：
药品类别：	抗凝血药及溶栓药

适 应 症
	1.Anagrelide lowers the number of blood clotting cells (called platelets) in the body. This helps to prevent blood clots from forming. 2.Anagrelide is used to treat essential thrombocytosis (too many blood clotting cells in the body). 3.Anagrelide may also be used for purposes other than those listed in this medication guide.

用法用量

1.Take anagrelide exactly as directed by your doctor. If you do not understand these instructions, ask your pharmacist, nurse, or doctor to explain them to you. 2.Take each dose with a full glass of water. 3.Your doctor will need to monitor your blood with blood tests before starting treatment with anagrelide, every 2 days for the first week of treatment, and at least weekly thereafter until the desired maintenance dosage is reached. 4.Store anagrelide at room temperature away from moisture and heat.

不良反应

1.If you experience any of the following serious side effects, stop taking anagrelide and seek emergency medical attention or notify your doctor immediately: *an allergic reaction (difficulty breathing; closing of your throat; swelling of your lips, tongue, or face; or hives); *fast, slow, or irregular heartbeat; *chest pain; *swelling of the hands, feet, or legs; *shortness of breath or difficulty in breathing; *seizures; *bloody or black vomit or stools; *abdominal pain; *unusual, prolonged, or severe bleeding or bruising; or *a bleeding nose. 2.Other, less serious side effects may also occur. Continue to take anagrelide and talk to your doctor if you experience *headache; *diarrhea; *tingling or numbness in the hands or feet; *upset stomach, nausea, or vomiting; *dizziness; *gas; *fever; *a rash or itching; *loss of appetite; *sore throat; *cough; or *back pain. 3.Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome.

注意事项

1.Your doctor will need to monitor your blood with blood tests before starting treatment with anagrelide, every 2 days for the first week of treatment, and at least weekly thereafter until the desired maintenance dosage is reached. 2.Tell your doctor and dentist that you are taking this medication before undergoing any surgical procedures. If Miss a Dose: 1.Take the missed dose as soon as you remember. However, if it is almost time for your next dose, skip the missed dose and take only your next regularly scheduled dose. Do not take a double dose of this medication. Contraindications: 1.Before taking anagrelide, tell your doctor if you have * heart disease, *kidney disease, or *liver disease. 2.You may not be able to take anagrelide, or you may require a dosage adjustment or special monitoring during treatment if you have any of the conditions listed above. 3.Anagrelide is in the FDA pregnancy category C. This means that it is not known whether it will harm an unborn baby. Do not take this medication without first talking to your doctor if you are pregnant. 4.It is not known whether anagrelide passes into breast milk. Do not take this medication without first talking to your doctor if you are breast feeding a baby. 5.Anagrelide is not approved for use by children younger than 16 years old. Special Concerns: 1.Tell your doctor and dentist that you are taking this medication before undergoing any surgical procedures.

药物相互作用
	1.There are no known interactions between anagrelide and other medicines. Talk to your doctor and pharmacist before taking any prescription or over-the-counter medicines.

药品过量
	1.Seek emergency medical attention. 2.Symptoms of a anagrelide overdose are unknown but might include bleeding and blood in the vomit or stool.

口服抗血小板药物阿那格雷(ana鄄grelide)选择性强，副作用少，主要用于治疗原发性血小板增多症及其他骨髓增生性疾病引起的血小板增多。
■作用机制
阿那格雷主要作用于巨核细胞，可抑制环磷腺苷(cAMP)磷酸二酯酶的活性，增加血小板内cAMP水平，从而抑制血小板的聚集及形态变化，抑制巨核细胞的成熟。大量研究结果发现，阿那格雷在体内外都能影响巨核细胞的成熟，导致细胞体变小和形态特征的变化，并认为阿那格雷减少血小板的数量主要是因为干预巨核细胞的成熟。体外实验发现，阿那格雷可以通过减少巨核细胞的大小和倍性而抑制巨核细胞克隆的发展或者是破坏和阻止巨核细胞的成熟，这些作用出现在巨核细胞发展的后一阶段、非分裂期。
■药动学特点
阿那格雷吸收迅速，并在体内广泛分布。大部分在肝脏中代谢，代谢产物主要经肾脏排出，不到1％以原形从尿中排出。一次口服阿那格雷1毫克，0.9小时后达最大血浆浓度，消除半衰期约为7.6小时。
■临床应用评价
一项对546例原发性血小板增多症且血小板计数高于900×109/升的病人进行的非对照性研究发现，本品平均治疗65周后，70%以上的病人血小板计数降至治疗前的50%或低于600×109/升，且疗效持续4年。对12例慢性粒细胞性白血病患者在常规治疗的基础上联合应用阿那格雷进行研究，所有的患者使用羟基脲治疗，其中一些使用α-干扰素(单独或联用羟基脲)、白消安或美法仑治疗。使用阿那格雷前血小板为(970~3600)×109/升(平均为2000×109/升)，7例患者有出、凝血并发症。治疗后所有的患者血小板数下降至小于600×109/升(中位数为343×109/升)，出、凝血症状消失。阿那格雷的中位剂量为每日1.9毫克。结果表明，阿那格雷的抗血小板效果显著。对于慢性粒细胞性白血病患者，在传统治疗不能控制血小板增多时，阿那格雷是一种有益的辅助用药。对942例血小板增多患者使用阿那格雷进行治疗，其中真性红细胞增多症患者113例，平均用药剂量为每日2.4毫克，总有效率达74％，其中完全缓解66％，部分缓解8％，完全缓解的时
间在17～25天之间。对48例原发性血小板增多症患者进行阿那格雷的临床疗效观察，其中41例患者有血栓史或有出血并发症，16例未经任何治疗，15例使用羟基脲治疗，另17例使用多种药物治疗。在阿那格雷治疗前患者血小板数为（850~3100）×109/升，经治疗完全缓解87％，部分缓解或无效13％，约10％的患者因不良反应而停止治疗，大多数患者已治疗7年(平均用药剂量为每日2.5毫克)。结果表明，阿那格雷在降低血小板数量的同时，也减少了血栓并发症的发生。
■药物安全性
阿那格雷治疗中约有25％~37％的患者有不同程度的不良反应，主要包括头痛、低血压、腹泻、体液潴留、心悸、心律失常、咳嗽、恶心及呕吐等。但反应轻微，大多发生在早期且能自行缓解。约有10％的患者因严重不良反应而停止治疗。长期治疗有轻微短暂的贫血出现，偶有发生严重过敏性肺炎和充血性心力衰竭的报道。阿那格雷产生抗凝作用需要的剂量比抗血小板时使用的剂量大约高10倍，因此，常规使用的抗血小板剂量对血小板的凝血功能没有影响。