物质信息
ID:320
名称和标识
别名
AllopurinolAllopurinol SodiumAlopurinol [INN-Spanish]Allopurinolum [INN-Latin]
IUPAC传统名
ALLO
IUPAC标准名
1H,2H,4H-pyrazolo[3,4-d]pyrimidin-4-one
商标名
AllopurAlluralAnoprolinTakanaruminUrbolUricemilUritasUrosinZyloprimDabrosonEpidropalGichtexRemidSigapurolSuspendolAiluralAllo-PurenAloralAlulineCaplenalCellidrinMonarchRiballUrobenylUrtiasXanturatZyloricBloxanthEpuricFoliganHPPHexanuretLedopurUriprimUrolitUrtias 1007HPAloprimApo-AllopurinolGotaxLopurinMiluritNektrohanProgoutPurinolApulongaApurolAtisurilBleminolDabrosinGeapurAdenockAllozymAlositolAnziefKetobun-ALysuronMiniplanorUripurinolAllohexalApurinCosuricDura AlEmbarinHamarinKetanrift
化合物性质
理化性质
疏水性(logP)
-1
溶解度
569 mg/L
描述信息
Drug Groups
approved
Description
A xanthine oxidase inhibitor that decreases uric acid production. It also acts as an antimetabolite on some simpler organisms. [PubChem]
Indication
For the treatment of hyperuricemia associated with primary or secondary gout. Also indicated for the treatment of primary or secondary uric acid nephropathy, with or without the symptoms of gout, as well as chemotherapy-induced hyperuricemia and recurrent renal calculi.
Pharmacology
Allopurinol, a structural analog of the natural purine base hypoxanthine, is used to prevent gout and renal calculi due to either uric acid or calcium oxalate and to treat uric acid nephropathy, hyperuricemia, and some solid tumors.
Toxicity
LD50=214 mg/kg (in mice)
Affected Organisms
Humans and other mammals
Biotransformation
Hepatic
Absorption
Approximately 80-90% absorbed from the gastrointestinal tract.
Half Life
1-3 hours
Protein Binding
Allopurinol and oxypurinol are not bound to plasma proteins
Elimination
Approximately 20% of the ingested allopurinol is excreted in the feces.
References
•
Pacher P, Nivorozhkin A, Szabo C: Therapeutic effects of xanthine oxidase inhibitors: renaissance half a century after the discovery of allopurinol. Pharmacol Rev. 2006 Mar;58(1):87-114.
[Pubmed]
•
Schlesinger N: Diagnosing and treating gout: a review to aid primary care physicians. Postgrad Med. 2010 Mar;122(2):157-61.
[Pubmed]
•
Suzuki I, Yamauchi T, Onuma M, Nozaki S: Allopurinol, an inhibitor of uric acid synthesis--can it be used for the treatment of metabolic syndrome and related disorders? Drugs Today (Barc). 2009 May;45(5):363-78.
[Pubmed]
•
Terkeltaub R: Update on gout: new therapeutic strategies and options. Nat Rev Rheumatol. 2010 Jan;6(1):30-8.
[Pubmed]
•
George J, Struthers AD: Role of urate, xanthine oxidase and the effects of allopurinol in vascular oxidative stress. Vasc Health Risk Manag. 2009;5(1):265-72. Epub 2009 Apr 8.
[Pubmed]
External Links
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参考文献
• Schlesinger N: Diagnosing and treating gout: a review to aid primary care physicians. Postgrad Med. 2010 Mar;122(2):157-61. Pubmed
• Terkeltaub R: Update on gout: new therapeutic strategies and options. Nat Rev Rheumatol. 2010 Jan;6(1):30-8. Pubmed
• Suzuki I, Yamauchi T, Onuma M, Nozaki S: Allopurinol, an inhibitor of uric acid synthesis--can it be used for the treatment of metabolic syndrome and related disorders? Drugs Today (Barc). 2009 May;45(5):363-78. Pubmed
• George J, Struthers AD: Role of urate, xanthine oxidase and the effects of allopurinol in vascular oxidative stress. Vasc Health Risk Manag. 2009;5(1):265-72. Epub 2009 Apr 8. Pubmed
• Pacher P, Nivorozhkin A, Szabo C: Therapeutic effects of xanthine oxidase inhibitors: renaissance half a century after the discovery of allopurinol. Pharmacol Rev. 2006 Mar;58(1):87-114. Pubmed