金諾芬
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通用名稱：金諾芬
英文名稱：Auranofin
英文別名：Aurothioglycolanilide
本品性質穩定，含金約29％，微溶於水，易溶於類脂體中。
目錄 |
藥理及應用
有抗炎作用，起效慢。口服後所含金的25％被吸收，其中60％與血漿蛋白結合，40％與細胞結合。本品主要由糞便排出。長期服用本品，金血漿濃度12周達高峰，並可保持穩定狀態。主用於活動性類風濕性關節炎，亦用於對非甾體抗炎藥效果不顯或無法耐受患者，可延緩類風濕性關節炎病變發展，改善症状，耐受好。
用法
口服：成人量1日mg，於早飯後服，或早、晚飯後各服3mg。初始劑量1日mg，2周後增至 1日／6mg。如服6個月後療效不顯，可增至一日mg，分3次服。若此量連服3個月效果仍不顯，應停藥。
注意
(1)常見副作用有腹瀉，腹痛、噁心、胃腸不適。尚可見皮疹、瘙癢。口腔炎、結膜炎少見。國外報導有白細胞、血小板減少、紫癜、單純紅細胞發育不全、暫時性蛋白尿、血尿等及肝功能短時異常。
(2)對金過敏、壞死性小腸結腸炎、肺纖維化、剝脫性皮炎、骨髓再生障礙、進行性腎炎、嚴重肝病患者以及孕婦、哺乳婦女慎用。
[製劑] 片劑：每片3mg。膠囊劑：每膠囊3mg。薄膜片：每片3mg(含金0．87mg)。
藥理作用
Classification: Antiarthritic,oral gold compound
Action/Kinetics: Auranofin is agold-containing (29%) compound for PO administration. It has fewer side effects thaninjectable gold products. Although the mechanism is not known, auranofin will improvesymptoms of rheumatoid arthritis; it is most effective in the early stages of activesynovitis and may act by inhibiting sulfhydryl systems. Other possible mechanisms includeinhibition of phagocytic activity of macrophages and polymorphonuclear leukocytes,alteration of biosynthesis of collagen, and alteration of the immune response. Gold willnot reverse damage to joints caused by disease. Approximately 25% of an oral dose isabsorbed. Plasma t1/2 of auranofin gold: 26 days. Onset: 3-4 months(up to 6 months in certain clients). Approximately 3 months are required for steady-stateblood levels to be achieved. The drug is metabolized and excreted in both the urine andfeces.
適應症
Adults and children withrheumatoid arthritis that have not responded to other drugs. Up to 6 months may berequired for beneficial effects to occur. Auranofin should be part of a total treatmentregimen for rheumatoid arthritis, including nondrug treatments.
用法用量
Capsules Rheumatoid arthritis. Adults, initial: Either 6 mg/day or 3 mg b.i.d. If response is unsatisfactory after6 months, increase to 3 mg t.i.d. If response is still inadequate after 3 additionalmonths, discontinue the drug. Dosages greater than 9 mg/day are not recommended. Children, initial: 0.1 mg/kg/day; maintenance: 0.15 mg/kg/day, not to exceed0.2 mg/kg/day. Transfer from injectable gold. Discontinue injectable gold and begin auranofin at a dose of 6 mg/day.
注意事項
Pregnancy Category: C
Contraindications: History ofgold-induced disorders including necrotizing enterocolitis, pulmonary fibrosis,exfoliative dermatitis, bone marrow aplasia, or other hematologic severe disorders. Useduring lactation.
Special Concerns: Use withextreme caution in renal or hepatic disease, skin rashes, marked hypertension, compromisedcerebral or CV circulation, or history of bone marrow depression (e.g., agranulocytopenia,anemia). Gold dermatitis may be aggravated by exposure to sunlight. Although used inchildren, a recommended dosage has not been established. Tolerance to gold is oftendecreased in geriatric clients.
不良反應
GI: N&V, diarrhea (common), abdominal pain, metallic taste, stomatitis, glossitis,gingivitis, anorexia, constipation, flatulence, dyspepsia, dysgeusia, melena. Rarely,dysphagia, GI bleeding, ulcerative enterocolitis. Dermatologic: Skin rashes, pruritus, alopecia, urticaria, angioedema, actinic rash. Hematologic: Leukopenia, anemia, thrombocytopenia (with or without purpura), neutropenia,agranulocytosis, eosinophilia, pancytopenia, hypoplastic anemia, aplasticanemia pure red cell aplasia. Renal: Proteinuria, hematuria. Hepatic: Jaundice (with or without cholestasis, hepatitis with jaundice, toxichepatitis intrahepatic cholestasis. Other: Conjunctivitis,cholestatic jaundice, fever, interstitial pneumonia and fibrosis, peripheral neuropathy.
藥物過量
Symptoms: Rapid appearance of hematuria, proteinuria, thrombocytopenia, granulocytopenia. Also,N&V, diarrhea, fever, urticaria, papulovesicular lesions, urticaria, exfoliativedermatitis, pruritus. Treatment: Discontinue promptly and give dimercaprol.Supportive therapy should be provided for renal and hematologic symptoms. Treat moderatelysevere skin and mucous membrane symptoms with topical corticosteroids, oralantihistamines, and anesthetic lotions. Treat severe stomatitis or dermatitis withprednisone, 10-40 mg daily. Treat serious renal, hematologic, pulmonary, and enterocoliticcomplications with prednisone, 40-100 mg daily in divided doses. The duration of treatmentvaries, depending on the severity of symptoms and the response to steroids. In acuteoverdosage, induce emesis or perform gastric lavage immediately.
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