Piroxicam, a potent inhibitor of prostaglandin production in cell culture. Structure-activity study

Carty, Thomas J.; Eskra, James D.; Lombardino, Joseph G.; Hoffman, William W.

doi:10.1016/0090-6980(80)90153-7

Cited by 64 publications

(8 citation statements)

References 10 publications

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“…Little blocking activity is observed at the phospholi pase, thromboxane or prostacyclin synthetase and arachidonic acid lipoxygenase steps [12], In vitro, the half-maximal inhibition of prostaglandin E produc tion of MC5-5 cell monolayers in the presence of ara chidonic acid occurred at a piroxicam concentration of 0.5 p M [13]. In our studies, scrum piroxicam levels exceeded this value more than 50-or 100-fold, de pending on the administered dose.…”

Section: Discussionmentioning

confidence: 67%

Experimental Allergic Encephalomyelitis – Prophylactic and Therapeutic Treatment with the Cyclooxygenase Inhibitor Piroxicam (Feldene®)

Weber

Meyermann²,

Hempel³

1991

Int Arch Allergy Immunol

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Prophylactic administration of Piroxicam (Feldene®), a reversible inhibitor of prostaglandin biosynthesis, significantly reduced the occurrence of paralytic signs and the amount of antibodies against myelin basic protein in the model of mild acute experimental allergic encephalomyelitis in the Lewis rat. Mononuclear infiltration of the central nervous system remained unaffected. A therapeutic intervention with piroxicam, however, increased paresis and CNS pathology. Immunohistochemical studies revealed an increased proportion of ED1-positive macrophages and monocytes in the infiltrates of the spinal cord in animals treated with piroxicam. Possible reasons for the different effects of the prophylactic and therapeutic treatment are discussed in the study.

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Section: Discussionmentioning

confidence: 67%

Experimental Allergic Encephalomyelitis – Prophylactic and Therapeutic Treatment with the Cyclooxygenase Inhibitor Piroxicam (Feldene®)

Weber

Meyermann²,

Hempel³

1991

Int Arch Allergy Immunol

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“…Furthermore, not all COX inhibitors promoted adipocyte differentiation. Likewise, we have found that several COX inhibitors, including the potent NSAID piroxicam (38), fail to promote adipocyte differentiation. These data provide compelling evidence that the effects of indomethacin are not mediated through the inhibition of prostaglandin production.…”

Section: Discussionmentioning

confidence: 99%

Peroxisome Proliferator-activated Receptors α and γ Are Activated by Indomethacin and Other Non-steroidal Anti-inflammatory Drugs

Lehmann¹,

Lenhard

Oliver³

et al. 1997

Journal of Biological Chemistry

1,035

669

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Indomethacin is a non-steroidal anti-inflammatory drug (NSAID) and cyclooxygenase inhibitor that is frequently used as a research tool to study the process of adipocyte differentiation. Treatment of various preadipocyte cell lines with micromolar concentrations of indomethacin in the presence of insulin promotes their terminal differentiation. However, the molecular basis for the adipogenic actions of indomethacin had remained unclear. In this report, we show that indomethacin binds and activates peroxisome proliferatoractivated receptor ␥ (PPAR␥), a ligand-activated transcription factor known to play a pivotal role in adipogenesis. The concentration of indomethacin required to activate PPAR␥ is in good agreement with that required to induce the differentiation of C3H10T1/2 cells to adipocytes. We demonstrate that several other NSAIDs, including fenoprofen, ibuprofen, and flufenamic acid, are also PPAR␥ ligands and induce adipocyte differentiation of C3H10T1/2 cells. Finally, we show that the same NSAIDs that activate PPAR␥ are also efficacious activators of PPAR␣, a liver-enriched PPAR subtype that plays a key role in peroxisome proliferation. Interestingly, several NSAIDs have been reported to induce peroxisomal activity in hepatocytes both in vitro and in vivo. Our findings define a novel group of PPAR␥ ligands and provide a molecular basis for the biological effects of these drugs on adipogenesis and peroxisome activity.Indomethacin and other NSAIDs 1 are used clinically for their anti-inflammatory, anti-pyretic, and analgesic properties (1). The molecular basis for the therapeutic actions of NSAIDs is believed to be their ability to inhibit cyclooxygenase (COX)

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“…28 Comparison of PG biosynthesis inhibitory activity of piroxicam with other NSAIDs marks piroxicam as the most effective drug in pulpitis. 29 Naproxen is an NSAID that inhibits the cyclooxygenase pathway, thus preventing the release of inflammatory mediators, such as prostaglandins. 30 These drugs are beneficial in providing relief of pain and inflammation in irreversible pulpitis and helps in providing effectiveness of inferior alveolar nerve block.…”

Section: Jaypeementioning

confidence: 99%

Effectiveness of Premedication with Analgesics vs Placebo for Success of Inferior Alveolar Nerve Block in Irreversible Pulpitis

Wali¹,

Siddiqui²,

Qamar³

et al. 2012

International Journal of Prosthodontics and Restorative Dentistry

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Pain is considered to be the major cause for seeking emergency endodontic treatment. Pain management is of vital importance in endodontics with no exception. Local anesthesia is considered to be the primary method to control pain. An effective local anesthesia cannot be obtained if pulp is inflamed. Clinician prescribes nonsteroidal anti-inflammatory drugs (NSAIDs) as premedication on a routine basis for mild to moderate pain to reduce pulpal inflammation before injecting anesthesia. These drugs are beneficial in providing relief from pain and inflammation in irreversible pulpitis and helps in providing effectiveness of inferior alveolar nerve block. Moreover, they have a short half life, which would make them ideal for a single dosage prior to the management of severe pain. Aim To conduct a randomized-placebo controlled clinical trial to compare the effectiveness of premedication with analgesics vs placebo for success of inferior alveolar nerve block in irreversible pulpitis. Materials and methods The study consisted of 80 adult patients attending operative Outpatient Department in Baqai Dental College. Informed Consent was obtained from each participant. Subjects were randomly divided in four groups comprising of 20 subjects in each group. Group A received piroxicam (Feldene 20 mg, Pfizer), group B received diclofenac potassium (Fastaid Plus, 50 mg platinum pharmaceutic), group C received naproxen sodium (Synflex 550 mg, ICI), and group D received a placebo drug becefol (Abbott). Medication was given 1 hour before initiating endodontic treatment. After 1 hour of oral administration of tablets, inferior alveolar nerve block using 1.8 ml of 2% lidocaine containing 1: 200,000 epinephrine was given. After 15 minutes, access cavity preparation was initiated and patients were asked to inform if they experienced pain. Patients were excluded from the study if they experienced pain but if the patient did not feel pain endodontic treatment was continued. p-value was set at 0.05. Data was analyzed by using Chi-square test (SPSS 19). Results The result showed that out of 80 patients who participated in the study, success rate for piroxicam came out to 90% (10 male and 8 female patients), followed by diclofenac potassium with 75% success rate (9 male and 6 female patients), naproxen sodium with 35% success rate (3 male and 4 female patients) and placebo with 10% success (1 male and 1 female patient). Conclusion The current study concludes that premedication given 1 hour before injecting anesthesia is helpful in reducing pain intensity and thus causing inferior alveolar nerve block to be effective. How to cite this article Wali A, Siddiqui TM, Qamar N, Khan R, Jawaid N. Effectiveness of Premedication with Analgesics vs Placebo for Success of Inferior Alveolar Nerve Block in Irreversible Pulpitis. Int J Prosthodont Restor Dent 2012;2(1):5-9.

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Piroxicam, a potent inhibitor of prostaglandin production in cell culture. Structure-activity study

Cited by 64 publications

References 10 publications

Experimental Allergic Encephalomyelitis – Prophylactic and Therapeutic Treatment with the Cyclooxygenase Inhibitor Piroxicam (Feldene®)

Experimental Allergic Encephalomyelitis – Prophylactic and Therapeutic Treatment with the Cyclooxygenase Inhibitor Piroxicam (Feldene®)

Peroxisome Proliferator-activated Receptors α and γ Are Activated by Indomethacin and Other Non-steroidal Anti-inflammatory Drugs

Effectiveness of Premedication with Analgesics vs Placebo for Success of Inferior Alveolar Nerve Block in Irreversible Pulpitis

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