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Nabumetone

产品号 DB00461 公司名称 DrugBank
CAS号 42924-53-8 公司网站 http://www.ualberta.ca/
分子式 C15H16O2 电 话 (780) 492-3111
分子量 228.28634 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 344

产品价格信息

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产品别名

标题
Nabumetone
IUPAC标准名
4-(6-methoxynaphthalen-2-yl)butan-2-one
IUPAC传统名
nabumetone
商标名
Unimetone
Nabuser
Listran
Relifex
Relafen
Arthaxan
Balmox
Consolan
Dolsinal
Flambate
Mebutan
Prodac
Relif
Relifen
别名
Nabumetona
Nabumetonum [INN-Latin]

产品登记号

PubChem SID 46507729
PubChem CID 4409
CAS号 42924-53-8

产品性质

疏水性(logP) 3.1
溶解度 Practically insoluble

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved
Description Nabumetone is a nonsteroidal anti-inflammatory drug (NSAID) of the arylalkanoic acid family (which includes diclofenac). Marketed under the brand name Relafen, it has been shown to have a slightly lower risk of gastrointestinal side effects than most other non-selective NSAIDs.

Indication For acute and chronic treatment of signs and symptoms of osteoarthritis and rheumatoid arthritis.
Pharmacology Nabumetone is a naphthylalkanone. Is is a non-selective prostaglandin G/H synthase (a.k.a. cyclooxygenase or COX) inhibitor that acts on both prostaglandin G/H synthase 1 and 2 (COX-1 and -2). Prostaglandin G/H synthase catalyzes the conversion of arachidonic acid to prostaglandin G2 and prostaglandin G2 to prostaglandin H2. Prostaglandin H2 is the precursor to a number of prostaglandins involved in fever, pain, swelling, inflammation, and platelet aggregation. The parent compound is a prodrug that undergoes hepatic biotransformation to the active compound, 6-methoxy-2-naphthylacetic acid (6MNA). The analgesic, antipyretic and anti-inflammatory effects of NSAIDs occur as a result of decreased prostaglandin synthesis.
Toxicity The one overdose occurred in a 17-year-old female patient who had a history of abdominal pain and was hospitalized for increased abdominal pain following ingestion of 30 nabumetone tablets (15 grams total). Stools were negative for occult blood and there was no fall in serum hemoglobin concentration. The patient had no other symptoms.
Affected Organisms
Humans and other mammals
Biotransformation Undergoes rapid biotransformation to the principal active metabolite, 6-methoxy-2-naphthylacetic acid (6MNA). Approximately 35% of a 1000 mg oral dose of nabumetone is converted to 6MNA and 50% is converted into unidentified metabolites which are subsequently excreted in the urine.
Absorption Well absorbed from the gastrointestinal tract. Coadministration of food increases the rate of absorption and subsequent appearance of 6MNA (the active metabolite) in the plasma but does not affect the extent of conversion of nabumetone into 6MNA.
Half Life Approximately 23 hours for the active metabolite, 6MNA. Increased in patients with renal insufficiency.
Protein Binding The active metabolite, 6MNA, is more than 99% bound to plasma proteins.
Elimination Approximately 35% of a 1000 mg oral dose of nabumetone is converted to 6MNA and 50% is converted into unidentified metabolites which are subsequently excreted in the urine.
Clearance * 20 - 30 mL/min
External Links
Wikipedia
RxList
PDRhealth
Drugs.com

参考文献