| 简介：
部份中文 氨苯砜处文资料（仅供参考）
中文别名： 氨苯砜、对位氨基双苯砜、二氨苯砜、二氨二苯砜
英文别名：
Avelisulphone、Avlcsulphone、Avlosulfon、Avlosulphone、Diaminodiphenylsulfone、Diaphenylsulfone、Diphone、Disulone、Dubronax、Eporal、Novophone、Protogan、Reconan、Sulphonyldianiline、Udolac、Vdolac
药品类别： 抗结核、麻风分支杆菌
类药理药动
药效学
本品为砜类抑茵剂，对麻风杆菌有较强的抑制作用。作用机制与磺胺药相似，两者的抗菌谱相似，均可为氨基苯甲酸拮抗。氨苯砜亦可用作双氢叶酸还原酶抑制剂。抑制疱疹样皮炎的作用机制尚未阐明，但与其抑菌作用无关。氨苯砜可能作为酶抑制剂或氧化剂。此外，本品尚具有免疫抑制作用，可能与抑制疱疹样皮炎的作用有关。
药动学
本品口服后吸收迅速而完全。蛋白结合率50～90％。吸收后广泛分布于全身组织(如肝、肾、皮肤、肌肉等)和体液中。在肝脏中经N—乙酰转移酶代谢。患者可分氨苯砜慢乙酰化型和快酰化型，前者服药后较易产生不良反应，尤其血液系统的不良反应，其血药峰浓度亦较高，但临床疗效未见增加。快酰化型患者用药时可能需调整剂量。口服后数分钟可在血液中测得氨苯砜，1～3小时可达血浆浓度峰值，有时需4～8小时，Ｔ1/2为10～50小时(平均28小时)。约
70～85％以原形和代谢产物(主要为葡萄醛酸甙和硫酸盐)由尿中逐渐排泄。游离药物从胆道排出后重新进入肠肝循环，因此停药后氨苯砜在血浆中仍可持续存在数周之久。
适 应 症
氨苯砜单独或与其他抑制麻风药联合用于由麻风分枝杆菌引起的各种类型麻风，和疱疹样皮炎的治疗。氨苯砜也可用于脓疱性皮肤病、类天疱疮、坏死性脓皮病、复发性多软骨炎、放线菌性足分枝菌病及聚会性痤疮的治疗。氨苯砜可与甲氧苄啶联合治疗卡肺孢子虫肺炎；与乙嘧啶联合用于预防氯喹耐药性疟疾；亦可与乙胺嘧啶和氯喹三者联合用于预防间日疟。
用法用量
1．抑制麻风口服，与一种或多种其他抗麻风药合药。成人每 日 100mg，一次顿肠或每日按体重0.9一1.4mg/kg，一次顿服；小儿每日按体重 0.9一 1.4mg/kg，一次顿服。成人最高量每日 200mg。
2．疱疹样皮炎口服，成人起始每日 50mg，如症状未完全抑制，每日剂量可增加至300mg，成人最高量每日500mg，以后尽早减少至最低有效维持量。 3．预防疟疾本品100mg与乙胺嘧啶 12.5mg联合，一次顿服，每 7天服药一次。
口服.
麻风病:一日12.5-25mg,后渐增至日100mg,儿童一日1.4mg/kg. 红般狼疮:一日100mg,连用3-6月.
痤疮:一日50mg. 银屑病和变应性血管炎:一日100-150mg. 带状庖疹:一次25mg,一日3次,连服3-14日.
糜烂性扁平苔癣:一日50mg,连用月. 上述均服6日停一日,服10周停2周.
不良反应
①发生率较高者有：背、腿痛，胃痛，食欲减退；皮肤苍白、溶血性贫血；发热(较常见于溶血性贫血，较少见于粒细胞缺乏症)；皮疹(过敏)；异常乏力或软弱(较常见于溶血性贫血，较少见于变性血红蛋白血症)；
②发生率极低者有：指甲、唇或皮肤青紫，呼吸困难(变性血红蛋白血症)，皮肤瘙痒、干燥、发红、脱痂或脱皮、脱发(剥脱性皮炎)、精神改变；麻木、针刺感、烧灼感、手或足软弱(周围神经炎)；咽痛(粒细胞缺乏症)、眼或皮肤黄染(肝脏损害)。
③下列症状如持续存在需引起注意：如眩晕、头痛、恶心、呕吐。
可引起胃肠道反应：恶心,呕吐,食欲不振,腹胀,腹泻.白细胞和粒细胞减少,溶血性贫血,头痛,失眠,周围神经炎,中毒性精神病.
剥脱性皮炎,中毒性肝炎. 个别病例有再生障碍性贫血,甚至死亡.
不良反应的特点
最常见的不良反应为恶心、呕吐及食欲不振，也常出现皮疹。可发生麻风结节病加重或麻风性结节性红斑反应，这类反应考虑是Herxheimer氏型。“砜综合征”(sulphonesyndrome)与麻风结节病变加重很不一样，它表现为发热、欲呕、剥脱性皮炎、黄疸伴有肝坏死、淋巴结肿大、正铁血红蛋白症及贫血，后者的发生率为25％，常发生在开始治疗后5～6周。麻风性结节性红斑伴有虹膜睫状体炎、神经炎、睾丸炎、突然发热及出现皮疹，则需改用其他药治疗。溶血可见于红细胞缺乏6-磷酸葡萄糖脱氢酶之病人，或合并其他疾病的病人。可出现过敏性皮炎。
* 神经系统：
表现为头痛、失眠、神经过敏、因轴突变性所引起的可逆性末梢神经病变。因之有些病人需要减量。偶尔发生精神抑郁。有报告用本品治疗麻风病人2891例，其中2例出现精神障碍。
* 消化系统： 最常见的为恶心、呕吐及食欲不振。较罕见有肝炎或黄疸。以前或现在有肝脏疾患者，用药应严密观察。
* 造血系统：
最常见的毒性反应为不同程度的溶血与发绀。本品的剂量为200～300mg/日时，几乎每个病人都可发生这种反应。
* 过敏反应：
常见有瘙痒及皮疹。砜综合征主要发生于营养不良的病人，也常可引起麻风结节性红斑，但仅见于麻风结节型病人。
砜类还可引起瘤形麻风发作加剧(有称“麻风反应”的)，常在治疗开始后5～6周开始，营养不良者尤易发生，表现为发热，全身不适、剥脱性皮炎、黄疸并伴有肝坏死、淋巴结肿大、正铁血红蛋白血症及贫血等，此时各种麻风症状加重与病变发展，如结节性红斑、发热、急性麻风性神经炎、多发性红斑、坏死性红斑、急性虹膜睫状体炎、睾丸肿大和血尿等。
禁忌症
(1)交叉过敏：对一种砜类过敏的患者可能对其他砜类亦过敏。对呋塞米、噻嗪类利尿药、磺酰脲类、碳酸酐酶抑制剂或其他磺胺药过敏的患者可能对本品亦敏感。
(2)氨苯砜可在乳汁中达有效浓度，对新生儿具预防作用。但砜类药物在G-6-PD(葡萄糖-6-磷酸脱氢酶)缺乏的新生儿中可能引起溶血性贫血。
(3)下列情况应慎用：严重贫血、G-6-PD(葡萄糖-6-磷酸脱氢酶)缺乏、肝功能减退、变性血红蛋白还原酶缺乏症、肾功能减退。
(4)葡萄糖- 6-磷酸脱氢酶缺乏患者用本品时需减量。
严重肝肾及造血系统疾病禁用. 药物相互作用
(1)对氨基苯甲酸(PABA)不宜与本品合用治疗麻风，因 PABA更易为细菌吸收而对砜类的抑菌作用产生拮抗，但PABA并不拮抗氨苯砜对于疱疹样皮炎的作用。
(2)丙磺舒与氨苯砜合用可减少肾小管分泌砜类，使砜类药血浓度高而持久，或发生毒性作用。因此在应用丙磺舒的同时或以后需调整砜类的剂量。
(3)合用利福平可减低氨苯砜的作用，因利福平可刺激肝脏微粒体酶的活性，使氨苯砜血浓度降低至 1/7一1/10；故服用利福平的同时或以后应用氨苯砜时，后者的剂量应调整。
(4)本品不宜与骨髓抑制药合用，因可加重白细胞和血小板减少的程度，必须合用时应密切观察对骨髓的毒性。
(5)本品如与其他溶血合用可加重其溶血不良反应。
Dapsone
Generic Name: dapsone (DAP sone)
Brand Name:
What is dapsone?
Dapsone is an anti-infective medicine that fights bacteria.
Dapsone is used to treat dermatitis herpetiformis (a skin condition) and leprosy.
Dapsone may also be used for purposes not listed in this medication guide.
Important Information
Follow all directions on your medicine label and package. Tell each of your healthcare providers about all your medical conditions, allergies, and all medicines you use.
Before taking this medicine
You should not use dapsone if you are allergic to it.
To make sure dapsone is safe for you, tell your doctor if you have:
•a genetic enzyme deficiency called glucose-6-phosphate dehydrogenase (G6PD) deficiency;
•methemoglobin reductase deficiency (hemoglobin M);
•liver disease;
•heart disease; or
•lung disease.
FDA pregnancy category C. It is not known whether dapsone will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication.
Dapsone can pass into breast milk and may harm a nursing baby. You should not breast-feed while using this medicine.
How should I take dapsone?
Follow all directions on your prescription label. Your doctor may occasionally change your dose to make sure you get the best results. Do not take this medicine in larger or smaller amounts or for longer than recommended.
Dapsone may be only part of a complete program of treatment that may also include a special diet. Follow the diet plan created for you by your doctor or nutrition counselor. Get familiar with the list of foods you must avoid to help control your condition.
Your doctor will need to check your progress while you are using dapsone.
Store at room temperature away from moisture, heat, and light.
What happens if I miss a dose?
Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.
What happens if I overdose?
Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.
Overdose symptoms may vomiting, feeling restless or excited, and a pale or blue-colored appearance.
What should I avoid while taking dapsone?
Avoid exposure to sunlight or tanning beds. Dapsone can make you sunburn more easily. Wear protective clothing and use sunscreen (SPF 30 or higher) when you are outdoors.
Dapsone side effects
Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.
Call your doctor at once if you have:
•worsening or no improvement in your symptoms;
•jaundice (yellowing of the skin or eyes);
•numbness or tingling in your hands or feet;
•unusual thoughts or behavior;
•new or worsening cough, fever, trouble breathing;
•swelling, rapid weight gain, little or no urinating;
•signs of abnormal blood cell counts--sudden weakness or ill feeling, fever, chills, sore throat, mouth sores, red or swollen gums, trouble swallowing, pale skin, easy bruising, purple or red pinpoint spots under your skin;
•pancreas problems--severe pain in your upper stomach spreading to your back, nausea and vomiting, fast heart rate;
•an autoimmune disorder--joint pain or swelling with fever, headaches, confusion, chest pain, shortness of breath, and butterfly-shaped skin rash on your cheeks and nose that worsens in sunlight; or
•severe skin reaction--fever, sore throat, swelling in your face or tongue, burning in your eyes, skin pain, followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling.
Common side effects may include:
•stomach pain, nausea, vomiting;
•headache;
•dizziness or spinning sensation;
•blurred vision, ringing in your ears; or
•sleep problems (insomnia).
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
See also: Side effects (in more detail)
Dasone dosing information
Usual Adult Dose for Leprosy -- Lepromatous:
50 to 100 mg orally once a day for 2-5 years.
Usual Adult Dose for Leprosy -- Tuberculoid:
100 mg orally once a day for 6 months. Rifampin is additionally recommended to reduce the incidence of dapsone resistance. If the disease relapses, this regimen should be repeated.
Usual Adult Dose for Dermatitis Herpetiformis:
50 mg orally once a day continued on a life-long basis. Dosage may be advanced to 300 mg/day. Dosage reduction to a minimum maintenance level as soon as possible is recommended.
Usual Adult Dose for Pneumocystis Pneumonia:
100 mg orally once a day for 14 to 21 days. Used in combination with trimethoprim.
Usual Adult Dose for Pneumocystis Pneumonia Prophylaxis:
100 mg orally twice a week. Therapy should be continued on a life-long basis. The addition of pyrimethamine appears to significantly increase the activity of dapsone for PCP prophylaxis.
Usual Adult Dose for Toxoplasmosis -- Prophylaxis:
100 mg orally twice a week continued on a life-long basis.
Usual Pediatric Dose for Leprosy:
1 to 2 mg/kg (up to 100 mg) orally once a day.
Usual Pediatric Dose for Pneumocystis Pneumonia Prophylaxis:
> 1 month:
2 mg/kg/day (up to 100 mg) orally once a day.
Alternate dosing:
> 1 month:
4 mg/kg orally once weekly. Maximum dose = 200 mg.
Usual Pediatric Dose for Toxoplasmosis -- Prophylaxis:
> 1 month:
2 mg/kg/day (or 15 mg/m2) orally once a day. Maximum dose = 25 mg. Dapsone should be administered as part of combination therapy for prophylaxis of toxoplasmosis.
What other drugs will affect dapsone?
Other drugs may interact with dapsone, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.
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