디클로페낙

디클로페낙 속성

디클로페낙 C화학적 특성, 용도, 생산

용도

prostaglandin synthetic inhibitor

Indications

Diclofenac (Voltaren, Cataflam) is approved for use in rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, dysmenorrhea, and topically for the treatment treatment of ocular inflammation and actinic keratosis. Diclofenac exhibits approximately equal selectivity for COX-1 and COX-2. The most common adverse reactions are GI disturbances and headache.A reversible elevation of serum transaminases occurs in 15% of patients.

Biological Functions

Diclofenac (Voltaren) is a phenylacetic acid derivative that is a potent inhibitor of COX and that has analgesic, antiinflammatory, and antipyretic effects. Its use is accompanied by side effects similar to those of other NSAIDs. Indications for the drug include rheumatoid arthritis, osteoarthritis, and ophthalmic inflammation (use of an ophthalmic preparation).

Mechanism of action

Diclofenac is unique among the NSAIDs in that it possesses three possible mechanisms of action: 1) inhibition of the arachidonic acid cyclooxygenase system (3 to 1,000 times more potent than other NSAIDs on a molar basis), resulting in a decreased production of prostaglandins and thromboxanes; 2) inhibition of the lipoxygenase pathway, resulting in decreased production of leukotrienes, particularly the pro-inflammatory LKB4; and 3) inhibition of arachidonic acid release and stimulation of its reuptake, resulting in a reduction of arachidonic acid availability.

Pharmacokinetics

Diclofenac is rapidly and completely (～100%) absorbed on oral administration, with peak plasma levels being reached within 1.5 to 2.5 hours. The free acid (pKa = 4.0) is highly bound to serum proteins (99.5%), primarily albumin. Only 50 to 60% of an oral dose is bioavailable because of extensive hepatic metabolism.

Clinical Use

Diclofenac is synthesized from N-phenyl-2,6-dichloroaniline. It is available in 120 different countries and, perhaps, is the most widely used NSAID in the world. It was introduced in the United States in 1989 but was first marketed in Japan in 1974. It ranks among the top prescription drugs in the United States. Diclofenac possesses structural characteristics of both arylalkanoic acid and the anthranilic acid classes of anti-inflammatory drugs, and it displays anti-inflammatory, analgetic, and antipyretic properties.

신진 대사

Four major metabolites resulting from aromatic hydroxylation have been identified. The major metabolite via CYP3A4 is the 4′-hydroxy derivative and accounts for 20 to 30% of the dose excreted, whereas the 5-hydroxy, 3′-hydroxy, and 4′,5-dihydroxy metabolites via CYP2C9 account for 10 to 20% of the excreted dose. The remaining drug is excreted in the form of sulfate conjugates. Although the major metabolite is much less active than the parent compound, it may exhibit significant biological activity, because it accounts for 30 to 40% of all of the metabolic products.

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디클로페낙 공급 업체

공급자	전화	이메일	국가	제품 수	이점
SUZHOU AUSUN CHEMICAL CO., LTD.	0512-68244182 15850237342	ausunjoy@163.com	China	29	58
Shanghai Boyle Chemical Co., Ltd.	021-50182298 021-50180596	sales@boylechem.com	China	2202	55
J & K SCIENTIFIC LTD.	18210857532 18210857532	jkinfo@jkchemical.com	China	96815	76
Meryer (Shanghai) Chemical Technology Co., Ltd.	4006356688 18621169109	market03@meryer.com	China	40202	62
Chembest Research Laboratories Limited	021-20908456	sales@BioChemBest.com	China	5996	61
TCI (Shanghai) Development Co., Ltd.	021-67121386	Sales-CN@TCIchemicals.com	China	24512	81
Beijing HwrkChemical Technology Co., Ltd	89508211 18501085097	sales.bj@hwrkchemical.com	China	9409	55
Energy Chemical	400-0056266	sales8178@energy-chemical.com	China	44852	61
Beijing Ouhe Technology Co., Ltd	13552068683 13522913783	2355560935@qq.com	China	11777	60
LGM Pharma	1-(800)-881-8210	inquiries@lgmpharma.com	United States	2110	70

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