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Published in Henry J. Woodford, Essential Geriatrics, 2022
Non-pharmacological interventions include physiotherapy, weight reduction and increased exercise.24 Non-steroidal anti-inflammatory drugs (NSAIDs) are often used in younger patients, but carry a high risk of toxicity in older adults (including gastric bleeding, renal impairment, hypertension and heart failure). Cyclooxygenase 2 (COX-2) inhibitors may be less prone to cause gastric bleeding, but have all the other risks of harm plus a possible increase in cardiac ischaemic events. For these reasons all NSAIDs should be avoided in older adults unless absolutely necessary. Paracetamol (acetaminophen) and weak opioids are safer options for analgesia. Joint replacement surgery may be considered in those who have significant disability despite other therapeutic measures. In a cohort of older adults (mean age 75) with severe OA who underwent hip or knee replacement, post-operative complications occurred in 17% (none fatal), median time to independent walking was 12 days, and surgery was associated with significant symptomatic benefits at 12 months.25
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).
Novel treatment modalities
Published in Seema Chopra, Endometriosis, 2020
In experimental studies, ulipristal acetate exhibited proapoptotic effects, thereby causing regression and atrophy of endometriotic lesions in rats. It helps in limiting the cell proliferation, as shown by a decrease in Ki-67 expression. Its anti-inflammatory effect was indicated by a decrease in cyclooxygenase-2 expression [42]. The clinical use of ulipristal acetate as a therapeutic agent for endometriosis is still under evaluation. It is approved as an emergency contraceptive in the United States. Europe and Canada allow ulipristal for the treatment of fibroids [43].
Transdermal delivery of celecoxib and α-linolenic acid from microemulsion-incorporated dissolving microneedles for enhanced osteoarthritis therapy
Published in Journal of Drug Targeting, 2023
Jian Li, Xin Tian, Kang Wang, Yong Jia, Fuguang Ma
Osteoarthritis (OA) is a common age-related chronic musculoskeletal disease characterised by progressive joint degeneration, such as cartilage destruction, synovial inflammation, subchondral remodelling and macrophage activation [1]. A survey reports that ∼350 million people worldwide are suffering from OA [2]. Among the population, the patients aged 40 or older account for 10%–17%; the population aged 60 or older rises to ∼50%, and the percentage over 75-year-old is higher than 80% [3,4]. Notably, the disability rate of elderly OA patients nearly reaches 50% as reported previously [4]. Joint replacement surgery is the preferred option for advanced or end-stage OA patients [5]. Intra-articular injection of glucocorticoids and hyaluronic acid has been proven effective for middle-stage OA patients [6], although it is inconvenient and poorly compliant. Conservative therapy with non-steroidal anti-inflammatory drugs (NSAIDs) is the first option for most OA patients. For example, celecoxib, a representative of cyclooxygenase-2 (COX-2) inhibitors, has been the most commonly-used drug for relieving joint pain and inflammatory symptoms [7]. However, as scientists warn, the long-term oral administration of NSAIDs has inevitable side effects, such as gastrointestinal bleeding and liver damage [8,9]. Therefore, it is highly desired to design an effective but simple topical delivery system based on commonly used therapeutical agents.
Experimental in vivo model to evaluate the impact of Cernitin™ on pain response on induced chronic bladder inflammation
Published in Scandinavian Journal of Urology, 2022
Céline Augé, Nishtman Dizeyi, Lena Ramnemark, Philippe Lluel, Magnus Grabe
Cyclophosphamide-induced BPS in rodents is a well-characterized model [11–13]. Systemic CYP is metabolized in the liver but eliminated primarily through the kidneys. CYP’s major uro-toxic metabolite is acrolein, which causes mucosal inflammation as indicated by microscopic changes in the bladder and the presence of inflammatory cell infiltrations as well as visceral pain [2,14]. This experimental model makes CYP-induced BPS the optimal choice to elucidate mechanisms, identify specific biomarkers related to this chronic condition and subsequently finding effective therapeutic options. A chronic condition, inducing inflammation and tissue damage, can change the properties of sensory pathways leading to a reduction in pain threshold (allodynia) and an amplification of painful sensations (hyperalgesia) [2]. Furthermore, chronic CYP-induced BPS may involve alterations in neurotrophic factors, chemokines [12,15] and cytokines [16]. The presence of pro-inflammatory cytokines can induce cyclooxygenase-2 (COX-2) enzyme, an inflammatory early response gene [17] and generate prostaglandins, a substance that plays a role in the inflammation process. In this study, we hypothesize that CYP-induced BPS upregulates COX-2 [18] and prostanoids [19] in the urinary bladder, which contributes to altered urodynamic function. Cyclooxygenase-2 has also been reported to have a nociceptive (analgesic) effect in both the central and peripheral nervous systems. They show the improvement in bladder function with administration of a specific COX-2 inhibitor [20] suggesting the pivotal role of COX-2 and prostanoids in BPS.
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].