Coleman M D
Mechanisms of Drug Toxicity Group, Pharmaceutical Sciences Institute, Aston University, Aston Triangle, Birmingham, B4 7ET, UK.
Toxicology. 2001 Apr 12;162(1):53-60. doi: 10.1016/s0300-483x(01)00360-2.
Agranulocytosis is a rare, severe and unpredictable idiosyncratic reaction associated with drug therapy that can lead to life-threatening illness. Typically, the patient presents with a fever and evidence of infection 1-3 months after initiation of drug administration with a neutrophil count below 0.5x10(9) l. Of the drugs linked with this disease, aminopyrine, dipyrone, clozapine, anti-thyroid agents, sulphonamides and dapsone are the best documented. Generally, agranulocytosis is associated with older individuals (>60 years) and those of non-Caucasian descent. The incidence of agranulocytosis in subjects taking oral dapsone in combination with maloprim for malaria is 1 -- 10-20,000 while leprosy patients treated with dapsone exhibit virtually zero risk of agranulocytosis. However, dapsone is unusual in that during the rare but severe inflammatory disease, dermatitis herpetiformis (DH), the risk of agranulocytosis is multiplied between 25 and 33 fold compared with normal patients. It is conceivable that dapsone might exhibit a similar risk in coeliac disease, a condition related to DH. As dapsone plasma levels in DH subjects can be high (2-10 microg/ml) the increased risk of agranulocytosis could be related to drug dosage, or increased immune responsiveness. The high risks in DH patients probably necessitate monitoring of neutrophil cell population in the first 3 months of therapy, while topical usage of the drug in acne treatment in otherwise healthy patients predominantly below the age of 25 is at the opposite end of the risk scale, probably as low as 1 in 10-20,000 patients.
粒细胞缺乏症是一种与药物治疗相关的罕见、严重且不可预测的特异反应,可导致危及生命的疾病。通常,患者在开始用药1 - 3个月后出现发热和感染迹象,中性粒细胞计数低于0.5×10⁹/L。与该疾病相关的药物中,氨基比林、安乃近、氯氮平、抗甲状腺药物、磺胺类药物和氨苯砜的记录最为详尽。一般来说,粒细胞缺乏症与老年个体(>60岁)及非白种人有关。服用口服氨苯砜联合乙胺嘧啶治疗疟疾的患者中粒细胞缺乏症的发生率为1/10000 - 20000,而接受氨苯砜治疗的麻风病患者粒细胞缺乏症的风险几乎为零。然而,氨苯砜的特殊之处在于,在罕见但严重的炎症性疾病疱疹样皮炎(DH)中,与正常患者相比,粒细胞缺乏症的风险增加了25至33倍。可以想象,氨苯砜在与DH相关的乳糜泻中可能也会表现出类似风险。由于DH患者的氨苯砜血浆水平可能较高(2 - 10μg/ml),粒细胞缺乏症风险增加可能与药物剂量或免疫反应性增强有关。DH患者的高风险可能需要在治疗的前3个月监测中性粒细胞数量,而在主要为25岁以下健康患者痤疮治疗中局部使用该药物的风险则处于相反的极端,可能低至1/10000 - 20000患者。