Sodium tolmetin dihydrate

Chemical properties

Crystalline Solid

The Uses of Sodium tolmetin dihydrate

Anti-inflammatory

The Uses of Sodium tolmetin dihydrate

beta-adrenergic blocker

The Uses of Sodium tolmetin dihydrate

Anti-inflammatory.

What are the applications of Application

Tolmetin Sodium is an antiinflammatory antirheumatic agent

Definition

ChEBI: An organic sodium salt that is the dihydrate form of tolmetin sodium. Used as a nonselective nonsteroidal anti-inflammatory drug.

Biological Activity

tolmetin is a non-steroidal anti-inflammatory drug that non-selectively inhibits human cox-1 and -2 [1].the cyclooxygenase (cox) is a therapeutic target for preventing cancer. two isoforms of cox have been identified: cox 1 and cox 2. cox 1 has been constitutively expressed in most tissues and involved in mediating production of prostaglandins that control normal physiological functions, such as maintenance of the gastric mucosa and regulation of renal blood flow. cox 2 is undetectable in most normal tissues [2].

in vitro

tolmetin inhibited the activity of human cox-1 and -2 with ic50 values of 0.35 and 0.82 μm, respectively [1]. tolmetin was a competitive and reversible inhibitor of prostaglandin synthetase [3].

in vivo

in rats, pretreatment with tolmetin reduced prostaglandin synthesis by minces of renal medulla. incubation of medullary tissue with tolmetin decreased prostagland production. in anesthetized dogs, tolmetin reduced renal blood flow and shifted the distribution of renal cortical flow from the inner cortex toward the outer cortex [4].

References

[1] warner t d, giuliano f, vojnovic i, et al. nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: a full in vitro analysis[j]. proceedings of the national academy of sciences, 1999, 96(13): 7563-7568.
[2] dannenberg a j, altorki n k, boyle j o, et al. cyclo-oxygenase 2: a pharmacological target for the prevention of cancer[j]. the lancet oncology, 2001, 2(9): 544-551.
[3] taylor r j, salata j j. inhibition of prostaglandin synthetase by tolmetin (tolectin, mcn-2559), a new non-steroidal anti-inflammatory agent[j]. biochemical pharmacology, 1976, 25(22): 2479-2484.
[4] noordewier b, stygles v g, hook j b, et al. effect of tolmetin on renal function and prostaglandin metabolism[j]. journal of pharmacology and experimental therapeutics, 1978, 204(2): 461-468.