
Allopurinol
3,5,7,8-tetrazabicyclo[4.3.0] nona-3,5,9-trien-2-one
抗痛風:初始劑量--口服,100mg,一天一次。維持劑量--口服,100至200mg,一天二至三次,或300mg單一劑量,一天一次。在輕度痛風者的一般維持劑量為每天200mg至300mg。
一般孩童劑量:年齡及於6歲的孩童:口服,50mg,一天三次。
年齡6至12歲的孩童:口服,100mg,一天三次;或300mg當作一個單一劑量,一天一次。
Absorption
About 90% absorbed from GI tract. T max is 1.5 h (allopurinol) and 4.5 h (oxipurinol). C max is 3 mcg/mL (allopurinol 300 mg) and 6.5 mcg/mL (oxipurinol).
Metabolism
Rapidly oxidized to oxipurinol.
Elimination
About 20% is excreted in the feces. Allopurinol is essentially cleared by glomerular filtration, whereas oxipurinol is reabsorbed in the kidney tubules. T 1/2 , plasma is about 1 to 2 h (allopurinol) and about 15 h (oxipurinol).
Onset
Uric acid decreases in about 2 to 3 days.
Peak
May require a week or more of treatment.
Duration
Xanthine oxidase inhibition is maintained over 24 h; however, uric acid levels may not return to pretreatment levels until 7 to 10 days following cessation of therapy.
Aluminum salts, uricosuric agents
May lessen effectiveness of allopurinol.
Ampicillin
May increase incidence of ampicillin-induced skin rash.
Cyclophosphamide
May enhance bone marrow suppression.
Theophyllines
Theophylline Cl may be decreased, leading to toxicity.
Thiopurines (eg, azathioprine, mercaptopurine)
Toxicity of these drugs may be increased.
Drugs that are physically incompatible in solution with allopurinol sodium for injection are the following
amikacin; amphotericin B; carmustine; cefotaxime; chlorpromazine; cimetidine; clindamycin; cytarabine; dacarbazine; daunorubicin; diphenhydramine; doxorubicin; doxycycline; droperidol; floxuridine; gentamicin; haloperidol; hydroxyzine; idarubicin; imipenem plus cilastatin; mechlorethamine; meperidine; metoclopramide; methylprednisolone sodium succinate; minocycline; nalbuphine; netilmicin; ondansetron; prochlorperazine edisylate; promethazine; sodium bicarbonate; streptozocin; tobramycin; vinorelbine tartrate.
1.每天至少要飲用2000ml的液體,而且要鹼化尿液,防止尿酸的沉積和可能造成的腎損壞。
2.要告訴病人allopurinol的效力可能要花好幾個星期才會產生,並且警告病人,除非醫師有指示,否則不要改變劑量。
1.立即停用本品。2.減低吸收-如已攝取非常大的量,則洗胃。3.增加排除-雖然Allopurinol與Oxipurinol都是可以透析的,但是,血液透析或腹膜透析在Allopurinol超劑量的處理上尚未確立。4.監測-可能包括觀察病人並治療所觀察到的症狀。5.支持性照護-維持水分。對已知或疑其為意圖超劑量的病人,最好照會精神科醫師會診。
1. 限使用於痛風症、痛風性關節炎、尿酸結石、癌症或經化學治療產生之高尿酸血症之治療。
2. 本藥品可能發生嚴重藥物不良反應,故不得使用於非核准之適應症。且須充分提醒病人相關不良反應症狀及後續作為。




