Diclofenac
From Proteopedia
(Difference between revisions)
| Line 3: | Line 3: | ||
Diclofenac is believed to work by decreasing the production of [[prostaglandins]], like other drugs in this class. | Diclofenac is believed to work by decreasing the production of [[prostaglandins]], like other drugs in this class. | ||
| + | |||
| + | As with most NSAIDs, the primary mechanism responsible for its anti-inflammatory, antipyretic, and analgesic action is thought to be inhibition of prostaglandin synthesis through [[cycloxygenase]] inhibition. Diclofenac inhibits COX-1 and COX-2 with relative equipotency.<ref name="a42">PMID:8265610</ref> | ||
| + | |||
| + | The main target in inhibition of prostaglandin synthesis appears to be the transiently expressed prostaglandin-endoperoxide synthase-2 (PGES-2) also known as cycloxygenase-2 (COX-2). | ||
| + | |||
| + | It also appears to exhibit bacteriostatic activity by inhibiting bacterial DNA synthesis.<ref name="a43">PMID:10773497</ref> | ||
| + | |||
| + | Diclofenac has a relatively high lipid solubility, making it one of the few NSAIDs that are able to enter the brain by crossing the blood-brain barrier. In the brain, too, it is thought to exert its effect through inhibition of COX-2.<ref name="a43">PMID:25078485</ref> In addition, it may have effects inside the spinal cord.<ref name="a43">PMID:27014880</ref>. | ||
</StructureSection> | </StructureSection> | ||
== References == | == References == | ||
<references/> | <references/> | ||
Revision as of 12:23, 3 July 2023
| |||||||||||
References
- ↑ Mitchell JA, Akarasereenont P, Thiemermann C, Flower RJ, Vane JR. Selectivity of nonsteroidal antiinflammatory drugs as inhibitors of constitutive and inducible cyclooxygenase. Proc Natl Acad Sci U S A. 1993 Dec 15;90(24):11693-7. PMID:8265610 doi:10.1073/pnas.90.24.11693
- ↑ 2.0 2.1 2.2 Dastidar SG, Ganguly K, Chaudhuri K, Chakrabarty AN. The anti-bacterial action of diclofenac shown by inhibition of DNA synthesis. Int J Antimicrob Agents. 2000 Apr;14(3):249-51. PMID:10773497 doi:10.1016/s0924-8579(99)00159-4
