NSAID’s

Incorporation of the 2-aryl-2-methylacetic acid moiety characteristic of NSAID s as part of... 

Apart from their anti-inflammatory activity the NSAIDs also show, dependent on the condition and the type of pain, considerable analgesic efficacy. In some forms of postoperative pain the NSAID s can be as efficacious as opioids, especially when prostaglandins, bradykinin and histamine, which are released by inflammation, have caused sensitization of pain receptors to normally painless stimuli. In Table 4 some advantages and disadvantages of NSAID s and opioids are compared. Although analgesic effects at peripheral or central neurons cannot be excluded completely, most studies indicate that... 

They are useful in relieving all dull itching, throbbing pain of muscles and joints, dysmenorrhoea, toothache, headache etc. The NSAID s are the mainstay for the management of acute dental pain. 

The important use of prostaglandin analogues is in the arthritic patients who are on chronic use of NSAID s and are not responding to receptor antagonists. 

Pairs of spin labels were introduced in human prostaglandin endoperoxide H2 synthase-2 (PGHS-2) at locations where significant structural changes had been observed in X-ray crystal structures of holoenzyme and protein bound to NSAID s.75 Interspin distances were obtained by Fourier deconvolution of spectra recorded at 183 K for 10 doubly spin-labelled mutants. Interspin distances for complexes with arachidonic acid, flurbiprofen, and SC-58125 agree well with values predicted from X-ray crystal structures, but do not agree well for the holoenzyme. It is proposed that the predominant conformation of the holoenzyme in solution is different from the structure in the crystal. 

A major aim of enteric coating is protection of drugs that are sensitive or unstable at acidic pH. This is particularly important for drugs such as enzymes and proteins, because these macromolecules are rapidly hydrolyzed and inactivated in acidic medium. Antibiotics, especially macrolide antibiotics like erythromycin, are also rapidly degraded by gastric juices. Others, such as acidic drugs like NSAID s (e.g., diclofenac, valproic acid, or acetylsalicylic acid) need to be enteric coated to prevent local irritation of the stomach mucosa. 

The potential contamination from either stereochemical impurities or stereochemical inversion of NSAID S (such as etodolac) that might take place when using ethyl chloroformate as the derivatizing agent in the sample preparation described above [33] was investigated in a separate study [34]. The study concluded that the extent of stereochemical conversion induced by assay procedures was small (approximately 1%) for... 

Etodolac distributes well into synovial fluid, the proposed primary site of action of NSAID s. Following multiple doses of 200 mg twice daily for 7 days, the Cmax in synovial fluid was 2.6 pg /mL and the tmax was 3.2 hours [44]. The synovial fluid AUC of total etodolac was about 67% of the serum values [44]. The AUC of the unbound etodolac was 172% of the serum values. After a single 200 mg dose of etodolac, the ratio of (S)-etodolac to (i )-etodolac in six subjects with rheumatoid arthritis was 0.074 in plasma and 0.17 in synovial fluid [45]. 

Drug(s) affected by NSAIDs NSAID(s) implicated Effect(s) Management... 

Wilder-Smith CH, Hill L, Spargo K, Kalla A. Treatment of severe pain from osteoarthritis with slow-release tramadol or dihydrocodeine in combination with NSAID s. A randomised study comparing analgesia, antinociception and gastrointestinal effects. Pain 2001 91(l-2) 23-31. 

Gowik, P. Julicher, B. Behaviour of Some Selected NSAID s Under Electrospray LC-MS Conditions. In Residues of Veterinary Drugs in Food, Proceedings of the Euroresidue III Conference, Veldhoven, May 6-8, 1996 Haagsma, N., Ruiter, A., Eds. Fac. Vet. Med., Univ. Utrecht The Netherlands, 1996. 

Many athletes rely on NSAID s to help with pain and soreness. 

The method works best with primary halides because a competitive 1 elimination reaction can occur when a secondary or tertiary alkyl halide I used (Section 11.15). Nevertheless, some unhindered secondary halid react well. An example occurs in the commercial synthesis of fenoprofen, nonsteroidal anti-inflammatory drug, or NSAID, marketed under the tradi name Mylan. (See Aspirin and Other Aromatic NSAID s at the end of Chap- ] ter 15.)... 

Chronic nonsteroidal anti-inflammatory drags (NSAID s) decrease risk of AD by two to four times. 

Mayo Clinic. (2000, January 6). NSAID s Helpful, but serious side effects. Mayo Foundation for Medical Education and Research, p. 4. 

---