トルメチン 化学特性,用途語,生産方法
効能
抗炎症薬, シクロオキシゲナーゼ阻害薬
説明
An antiinflammatory, analgesic, and antipyretic that is as efficacious as
moderate doses of aspirin and better tolerated. Tolmetin produces
a number of adverse effects including epigastric pain, dyspepsia,
nausea, and vomiting. Tolmetin is approximately 99% plasma
protein bound, yet does not interfere with concurrent treatment
with oral hypoglycemics. Tolmetin has been found to be effective in the treatment of osteoarthritis and rheumatoid arthritis.
使用
Tolmetine is an NSAID.
定義
ChEBI: A monocarboxylic acid that is (1-methylpyrrol-2-yl)acetic acid substituted at position 5 on the pyrrole ring by a 4-methylbenzoyl group. Used in the form of its sodium salt dihydrate as a nonselective nonsteroidal anti-inflammatory drug.
適応症
Tolmetin (Tolectin) is indicated for the relief of osteoarthritis,
rheumatoid arthritis, ankylosing spondylitis,
and moderate pain. It is ineffective in gouty arthritis for
unknown reasons.Tolmetin can inhibit both COX-1 and
COX-2 but has a moderate selectivity for COX-1. The
most frequently reported side effects are GI disturbance
and CNS reactions (e.g., headache, asthenia, and
dizziness). These effects are less frequently observed
than after aspirin or indomethacin use. Blood pressure
elevation, edema, and weight gain or loss have been
associated with tolmetin administration. Tolmetin metabolites
in urine have been found to produce pseudoproteinuria
in some laboratory tests.
生物学の機能
Tolmetin (Tolectin) is an antiinflammatory, analgesic,
and antipyretic agent that produces the usual gastric
distress and ulceration observed with NSAIDs.
However, tolmetin is better tolerated than aspirin and
produces less tinnitus and vertigo. Tolmetin is a substitute
for indomethacin in indomethacin-sensitive patients
and is unique among such drugs in that it can be
used to treat juvenile arthritis.
一般的な説明
Tolmetin sodium (Tolectin), is an arylacetic acid derivativewith a pyrrole as the aryl group. This drug is well absorbed and has a relatively short plasma half-life (1 hour). It is recommendedfor use in the management of acute and chronicRA. Its efficacy is similar to aspirin and indomethacin, butwith less frequency of the adverse effects and tinnitus associatedwith aspirin. It does not potentiate coumarin-likedrugs nor alter the blood levels of sulfonylureas or insulin.However, tolmetin, and especially its closely related drug,zomepirac (i.e., with a p-chlorobenzoyl group and an additionalmethyl group on the pyrrole ring), can produce a rarebut fatal anaphylactic reaction because of irreversible bindingof their unstable acyl glucuronides. Zomepirac waswithdrawn from market because it is eliminated only via theester-type, acyl glucuronide. It is possible that tolmetin isless toxic in this regard because it undergoes additional hepaticbenzylic hydroxylation via its p-methyl group and isexcreted as its stable ether glucuronide.
製品名
Artrocaptin (Estedi, Spain),
Tolectin (Cilag, Belgium; Janssen-Cilag, Austria; McNeil, USA).
トルメチン 上流と下流の製品情報
原材料
準備製品