Golusin Z, Poljacki M, Preveden R, Stojanović S, Rajić N
Klinika za kozno-venericne bolesti, Medicinski fakultet, Klinicki centar, Novi Sad.
Med Pregl. 2000 Jul-Aug;53(7-8):369-72.
Diaminodiphenylsulfone or dapsone is a chemical analogue of sulfapyridine, synthesized in 1908. Dapsone is a bacteriostatic agent that proved to be efficient in treating leprosy and malaria, but today it is used in treating dermatologic noninfectious inflammatory diseases.
Dapsone is orally used in a dose of 50-400 mg per day in treatment of dermatologic diseases, and also in a dose of 50-100 mg per day in leprosy treatment. Dapsone is mainly eliminated from the body by urine and smaller part by faeces. Pharmacological interaction was reported when it is used with rifampicin and probenecid.
The bacteriostatic effect of dapsone is well known. It involves inhibition of folic acid synthesis in susceptible organisms. The anti-inflammatory effect of dapsone, which proves to be efficient in treating noninfectious inflammatory diseases, has not been explained completely yet. There are some pieces of evidence that anti-inflammatory action is not connected with its antibacteriological action.
Based on previous studies about therapy efficiency of dapsone in treating some diseases, there are two groups of diseases: the group responding well to dapsone (leprosy, malaria, DH, linear IgA-dermatosis, erythema elevatum diutinum, bullous systemic lupus erythematosus) and a group responding with average good response to dapsone (pyoderma gangrenosum, bullous and cicatricial pemphigoid, acne conglobata, discoid cutaneous lupus erythematosus, subcorneal pustulosis dermatosis, granuloma faciale, rheumatoid arthritis, polychondritis, leucocytoclastic vasculitis).
Adverse effects depend on the dose and they rarely occur at doses less than 100 mg per day. They are mainly shown on skin, nervous system, digestive system, hepatobiliary system, and kidney and hematologic system. The most important adverse effects are hemolytic anaemia and methemoglobinemia. Hemolysis usually occurs at doses of 200 mg and more per day. In patients with glucose-6-phosphate dehydrogenase deficiency, hemolysis may be provoked by a dose less than 50 mg per day. For prevention, before using dapsone in therapy, clinical examination with history, blood parameters, liver and renal parameters and determination of glucose-6-phosphate dehydrogenase level are recommended.
The use of dapsone is absolutely indicated in DH treatment and erythema elevatum diutinum. Because of anti-inflammatory effects, dapsone can also be used in treating other inflammatory noninfectious dermatoses when one should take care about "therapy efficiency/adverse effect" balance using the correct dose, monitoring relevant clinical and laboratory parameters and educating patients.
二氨基二苯砜或氨苯砜是磺胺吡啶的化学类似物，于1908年合成。氨苯砜是一种抑菌剂，已被证明对治疗麻风病和疟疾有效，但如今它被用于治疗皮肤非感染性炎症性疾病。
氨苯砜用于治疗皮肤病时口服剂量为每日50 - 400毫克，用于治疗麻风病时口服剂量为每日50 - 100毫克。氨苯砜主要通过尿液从体内排出，少量通过粪便排出。与利福平及丙磺舒合用时会出现药物相互作用。
氨苯砜的抑菌作用众所周知，它涉及抑制易感生物体中叶酸的合成。氨苯砜在治疗非感染性炎症性疾病中被证明有效的抗炎作用尚未完全阐明。有一些证据表明抗炎作用与其抗菌作用无关。
基于先前关于氨苯砜治疗某些疾病疗效的研究，有两组疾病：对氨苯砜反应良好的一组疾病（麻风病、疟疾、疱疹样皮炎、线状IgA大疱性皮病、持久性隆起性红斑、大疱性系统性红斑狼疮）和对氨苯砜反应一般良好的一组疾病（坏疽性脓皮病、大疱性和瘢痕性类天疱疮、聚合性痤疮、盘状皮肤红斑狼疮、角层下脓疱性皮肤病、面部肉芽肿、类风湿关节炎、多软骨炎、白细胞破碎性血管炎）。
不良反应取决于剂量，每日剂量低于100毫克时很少发生。主要表现在皮肤、神经系统、消化系统、肝胆系统、肾脏及血液系统。最重要的不良反应是溶血性贫血和高铁血红蛋白血症。溶血通常发生在每日剂量200毫克及以上时。对于葡萄糖 - 6 - 磷酸脱氢酶缺乏的患者，每日剂量低于50毫克时也可能引发溶血。为预防起见，在治疗中使用氨苯砜前，建议进行病史、血液参数、肝肾功能参数的临床检查以及葡萄糖 - 6 - 磷酸脱氢酶水平的测定。
氨苯砜在疱疹样皮炎和持久性隆起性红斑的治疗中绝对适用。由于其抗炎作用，氨苯砜也可用于治疗其他炎症性非感染性皮肤病，但此时应使用正确剂量，监测相关临床和实验室参数并对患者进行教育，以关注“治疗效果/不良反应”的平衡。
