Balduini C L, Bertolino G, Noris P, Ascari E
Dipartimento di Medicina Interna, Università di Pavia, Italy.
Haematologica. 1992 Jan-Feb;77(1):40-3.
Anagrelide is a quinazolin compound developed initially as an inhibitor of platelet aggregation. Since "in vivo" studies demonstrated that it was responsible for thrombocytopenia in humans, anagrelide has been used recently in a small number of patients with thrombocytosis and myeloproliferative disorders. Platelet count was well controlled in the large majority of patients, and only minimal side effects were observed.
Eight patients (5 with essential thrombocythemia, 2 with chronic granulocytic leukemia, and 1 with idiopathic myelofibrosis) received anagrelide (induction dose 4 mg/die; mean maintenance dose 2 mg/die; mean observation time 26 weeks). Complete blood counts were determined 4 times during the first month, and subsequently every month. "In vivo" and "ex vivo" platelet function was studied before anagrelide and after 4 and 10 days of therapy.
Platelet count was reduced and maintained below 500 x 10(9)/L in 5 of 8 patients. Headache, palpitation/tachycardia, gastrointestinal symptoms and a decrease in hemoglobin were the side effects. Anagrelide did not modify the leukocyte count or "in vivo"/"ex vivo" platelet function.
Anagrelide may control thrombocytosis in patients with myeloproliferative disorders, even when traditional drugs have failed. When required, anti-aggregating drugs may be associated with anagrelide, since it has no effect on platelet function.
阿那格雷是一种喹唑啉化合物，最初作为血小板聚集抑制剂开发。由于“体内”研究表明它是导致人类血小板减少的原因，阿那格雷最近已用于少数血小板增多症和骨髓增殖性疾病患者。大多数患者的血小板计数得到了良好控制，仅观察到极少的副作用。
8例患者（5例原发性血小板增多症、2例慢性粒细胞白血病和1例特发性骨髓纤维化）接受了阿那格雷治疗（诱导剂量4毫克/日；平均维持剂量2毫克/日；平均观察时间26周）。在第一个月内进行4次全血细胞计数测定，随后每月进行一次。在使用阿那格雷之前以及治疗4天和10天后研究“体内”和“体外”血小板功能。
8例患者中有5例血小板计数降低并维持在500×10⁹/L以下。副作用包括头痛、心悸/心动过速、胃肠道症状和血红蛋白降低。阿那格雷未改变白细胞计数或“体内”/“体外”血小板功能。
阿那格雷可控制骨髓增殖性疾病患者的血小板增多症，即使传统药物治疗失败。如有需要，抗聚集药物可与阿那格雷联合使用，因为它对血小板功能无影响。
