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Chemopreventive Agents
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Most NSAIDs inhibit the activity of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), thereby blocking synthesis of the prostaglandins and thromboxanes from arachidonic acid. For all NSAIDs except aspirin (which causes irreversible inhibition) this inhibition is competitively reversible to varying degrees. COX-1 is constitutively expressed and regulates many normal physiological processes including protection of the stomach lining by prostaglandins which prevent the stomach mucosa from being damaged by its own acid production. When nonselective COX-1/COX-2 inhibitors (such as aspirin, ibuprofen, or naproxen) reduce prostaglandin levels, ulcers of the stomach or duodenum and internal bleeding can result. On the other hand, COX-2 is facultatively expressed in the inflammation process which provides the desirable effects of NSAIDs, a mechanism elucidated by John Vane who received a Nobel Prize for his studies in 1982. Therefore, inhibiting COX-2 by NSAIDs leads to their anti-inflammatory, analgesic, and antipyretic effects, while those agents that also inhibit COX-1 (especially the case for aspirin) can sometimes cause gastrointestinal bleeding and ulcers.
Suprofen
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Suprofen is a nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic and antipyretic activities. It binds to the cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) isoenzymes, preventing the synthesis of prostaglandins and reducing the inflammatory response. Currently, it appears not to be used systemically, but suprofen is utilized in eye drops to inhibit the miosis (pupil constriction) that may occur during ocular surgery (1). It is also available since 1989 in Japan in an ointment containing 1% suprofen (1,3). All reports of (photo)contact allergy thus far have come from Japan, with the exception of one patient who was sensitized during a clinical trial (12).
Anticoagulation in Pregnancy
Published in Afshan B. Hameed, Diana S. Wolfe, Cardio-Obstetrics, 2020
Rachel A. Newman, Ather Mehboob, Judith H. Chung
Aspirin (acetylsalicylic acid) is not an anticoagulant but is often used in pregnancy as part of a thromboprophylaxis regimen. The mechanism of action is to prevent platelet aggregation through irreversible inhibition of cyclooxygenase-1 and 2 (COX-1 and 2) enzymes [67].
Inflammation resolution and specialized pro-resolving lipid mediators in chronic rhinosinusitis
Published in Expert Review of Clinical Immunology, 2023
Peyton Z. Robinson, Daniel N. Frank, Vijay R. Ramakrishnan
An imbalance in prostaglandins and leukotrienes produced via the inducible cyclooxygenase-2 (COX-2) and constitutively expressed cyclooxygenase-1 (COX-1) enzymes has long been thought to be a critical contributor to CRS. This has been postulated based on implications derived from aspirin-exacerbated respiratory disease (AERD) and studies in CRS tissues [35,36]. When taken in the larger context of other fatty acid-derived mediators, we can recognize that eicosanoid regulation of CRS inflammation is considerably more complex. Specialized pro-resolving mediators (SPMs) are a novel class of polyunsaturated fatty acid (PUFA)-derived mediators that aid in facilitating the resolution of inflammation. These mediators consist of 4 major categories defined by their PUFA source and chemical structures – lipoxins, resolvins, maresins, and protectins [37].
Multimodal analgesia in neurosurgery: a narrative review
Published in Postgraduate Medicine, 2022
Caterina Aurilio, Maria Caterina Pace, Pasquale Sansone, Luca Gregorio Giaccari, Francesco Coppolino, Vincenzo Pota, Manlio Barbarisi
It is now understood that there are two forms of cyclooxygenase, termed cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2). COX-1 is a constitutive isoform found in normal tissues, while COX-2 is induced in settings of inflammation and is constitutively expressed in certain areas of brain. NSAIDs are usually classified as mild analgesics, but it is important to consider the type of pain and its intensity in the assessment of analgesic efficacy. In postoperative pain, the NSAIDs may be superior to the opioids because they are particularly effective in different contests in which inflammation has caused sensitization of pain receptors [16]. The inhibition of COX-1 correlates with the inhibition of endogenous prostaglandins that impairs platelet function and promotes the ability of these drugs to increase the perioperative bleeding time. Probably for this reason, there are few clinical studies on the use of NSAIDs in brain surgery. In a Cochrane review, six studies were included in a meta-analysis on 742 patients to assess acute postoperative intensity of pain in brain surgery [10,17,18].
Comparative safety review of current treatment options for chronic low back pain and unmet needs: a narrative review
Published in Expert Opinion on Drug Safety, 2021
Filip Jovanovic, Iulia Pirvulescu, Emilija Knezevic, Kenneth D. Candido, Nebojsa Nick Knezevic
Per an updated review of clinical practice guidelines, alongside their favorable safety profile over other pharmaceuticals, oral nonsteroidal anti-inflammatory drugs (NSAIDs) are considered the first-line treatment option for the management of CLBP for any duration of symptoms [75]. NSAIDs exert their analgesic, anti-inflammatory, and antipyretic effects by inhibiting the cyclooxygenase 1 (COX-1) and 2 (COX-2) enzymes. However, the affinity of particular NSAIDs at therapeutic doses toward COX-1/COX-2 enzymes is imperative when considering their safety profile and risk-benefit ratio. Two systematicreviews with placebo-controlled studies provided evidence that the frequency of AEs was not significantly higher in patients taking NSAIDs vs. placebo [76,77]. However, the small sample size and short follow-up periods question the validity of these results.