- |||||||||| aspirin / Generic mfg., warfarin / Generic mfg.
Clinical, Review, Journal: A systematic review of the evidence supporting post-operative antithrombotic use following cardiopulmonary bypass in children with CHD. (Pubmed Central) - Jan 19, 2022 There are few paediatric prospective randomised clinical trials evaluating antithrombotic therapeutics post-cardiac surgery; most studies have been observational and seldom employed clinical endpoints. Standardised, validated endpoints and pragmatic trial designs may allow investigators to determine the optimal drug, timing of initiation, dosing and duration to improve outcomes by limiting post-operative morbidity and mortality related to bleeding or thrombotic events.
- |||||||||| aspirin / Generic mfg.
Journal: Non-selective COX inhibitors impair memory formation and short-term but not long-term synaptic plasticity. (Pubmed Central) - Jan 11, 2022 Therefore, long-term administration of acetylsalicylic acid (ASA) and its main metabolite, salicylate, as a COX inhibitor may impair synaptic plasticity and subsequently memory formation...These data suggested that long-term inhibition of COX disrupted memory acquisition and retrieval. Interestingly, cognitive impairments happened along with short-term but not long-term synaptic plasticity disturbance.
- |||||||||| aspirin / Generic mfg.
Review, Journal: From NSAIDs to Glucocorticoids and Beyond. (Pubmed Central) - Jan 7, 2022 Hippocrates used willow bark to treat inflammation, and many centuries later, salicylic acid and its derivative aspirin's ability to inhibit cyclooxygenase enzymes was discovered...The discovery of the GC-inducible endogenous anti-inflammatory protein annexin A1 (AnxA1) and other endogenous proresolving mediators has opened a new era of anti-inflammatory therapy. This review aims to recapitulate the last four decades of research on NSAIDs, GCs, and AnxA1 and their anti-inflammatory effects.
- |||||||||| celecoxib oral / Generic mfg.
Journal, Adverse events: Design, synthesis and mechanistic study of novel diarylpyrazole derivatives as anti-inflammatory agents with reduced cardiovascular side effects. (Pubmed Central) - Jan 5, 2022 Remarkably, the most active COX inhibitors 6d and 11f possessed improved cardiovascular safety profiles, if compared to celecoxib, as shown by the laboratory evaluation of both essential cardiac biochemical parameters (troponin-1, prostacyclin, tumor necrosis factor-α, lactate dehydrogenase, reduced glutathione and creatine kinase-M) and histopathological studies...Also, in silico ADME studies prediction and drug-like properties of the compounds revealed favorable oral bioavailability results. Collectively, the present work could be featured as a promising future approach towards novel selective COX-2 inhibitors with declined cardiovascular risks.
- |||||||||| glibenclamide / Generic mfg.
Preclinical, Journal: Vasorelaxation effect of oxysophoridine on isolated thoracicc aorta rings of rats. (Pubmed Central) - Jan 4, 2022 In addition, vasodilatory effects of OSR were not inhibited in the presence of potassium channel blockers barium chloride (BaCl, 1 mmol·L) and tetraethylamine (TEA, 10 mmol·L), nitric oxide synthase inhibitor (L-NAME, 0.1 mmol·L) and COX inhibitor (INDO, 10 μmol·L). In conclusion, the vasodilatory effects of OSR on thoracic aorta rings is associated with K and K.
- |||||||||| ampicillin / Generic mfg.
Journal: Spectral characterization, antioxidant, antimicrobial, cytotoxic, and cyclooxygenase inhibitory activities of Aloysia citriodora essential oils collected from two Palestinian regions. (Pubmed Central) - Dec 30, 2021 The Baqa al-Gharbiyye AC EO has more potent antioxidant and cytotoxic activities than the Umm al-Fahm EO, but both have potential antimicrobial activity against MRSA, P. vulgaris, and C. albicans. These results suggest the use of AC EOs as promising sources of active ingredients in the food, cosmetic, and pharmaceutical industries.
- |||||||||| ibuprofen / Generic mfg.
Journal: The Mediation of Central Cyclooxygenase and Lipoxygenase Pathways in Orexin-Induced Cardiovascular Effects. (Pubmed Central) - Dec 23, 2021 In summary, our findings show that the central treatment with OX causes pressor and tachycardic cardiovascular responses along with an increase in posterior hypothalamic extracellular total prostaglandin concentrations. Furthermore, our results also demonstrate that central COX and LOX pathways mediate, at least in part, centrally administered OX-evoked pressor and tachycardic responses, as well.
- |||||||||| naproxen / Generic mfg.
Lipoxygenase inhibitors for the treatment of traumatic brain injury (Virtual Only) - Dec 20, 2021 - Abstract #Neuroscience2021Neuroscience_3194; Because COX inhibitors (e.g., ibuprofen, naproxen) are associated with gastrointestinal and cardiovascular adverse reactions, we have developed lipoxygenase (LOX) inhibitors that simultaneously inhibit 5-, 12-, and 15-LOX at low nM levels...Collectively, our findings suggest that further evaluation of LOX inhibitors in general, and our LOX inhibitors in particular, may be warranted as potential treatments for TBI.; Grant Support: Supported by the Office of the Assistant Secretary of Defense for Health Affairs through The Defense Medical Research and Development Program under Award No. W81XWH-19-1-0329.
- |||||||||| celecoxib oral / Generic mfg.
Journal: Anti-inflammatory activity of novel thiosemicarbazone compounds indole-based as COX inhibitors. (Pubmed Central) - Dec 16, 2021 Dietary copper NPs in both doses modified vasodilation through the vasoconstrictor 20-HETE and the TP receptors. These results demonstrate the potency of thiosemicarbazone derivatives containing indole and confirm their importance as scaffolds of molecules with notorious anti-inflammatory activity.
- |||||||||| Preclinical, Journal: Arrabidaea chica Verlot fractions reduce MIA-induced osteoarthritis progression in rat knees. (Pubmed Central) - Dec 16, 2021
In silico analyses indicate the presence of favourable interactions between some of the identified compounds and the COX-2 enzyme, mainly concerning alpha-tocopherol (Vitamin E), squalene and beta-sitosterol. The findings indicate that A. chica fractions display analgesic, anti-inflammatory properties, are non-toxic and are able to slow OA progression, and may, therefore, be prioritized as natural products in OA human clinical trials.
- |||||||||| celecoxib oral / Generic mfg.
Preclinical, Journal: The effective interplay of (non-) selective NSAIDs with neostigmine in animal models of analgesia and inflammation. (Pubmed Central) - Dec 16, 2021 The findings indicate that A. chica fractions display analgesic, anti-inflammatory properties, are non-toxic and are able to slow OA progression, and may, therefore, be prioritized as natural products in OA human clinical trials. Selective and non-selective NSAIDs examined in this study could be good adjunct options to general anesthetic agents and neostigmine in perioperative stages, an outcome that needs further clinical investigations.
- |||||||||| celecoxib oral / Generic mfg.
Journal: Optimization of pyrazole-based compounds with 1,2,4-triazole-3-thiol moiety as selective COX-2 inhibitors cardioprotective drug candidates: Design, synthesis, cyclooxygenase inhibition, anti-inflammatory, ulcerogenicity, cardiovascular evaluation, and molecular modeling studies. (Pubmed Central) - Dec 16, 2021 The results confirmed that compound 7a has a more favorable cardio profile than celecoxib...Finally, an ADME study was applied and proved the promising activity of the new compounds as a new oral anti-inflammatory agent. In conclusion, the newly developed compound 7a represents a potential selective COX-2 NSAID candidate with minimum cardiovascular risks.
- |||||||||| 5-fluorouracil / Generic mfg., oxaliplatin / Generic mfg.
Clinical, Review, Journal: Curcuma as an adjuvant in colorectal cancer treatment. (Pubmed Central) - Dec 16, 2021 Despite the evidence obtained in vitro and in vivo, clinical studies have not yet confirmed the therapeutic potential of curcumin against CRC. Here we reviewed the last scientific information that supports the consumption of curcumin as an adjuvant for CRC therapy.
- |||||||||| aspirin / Generic mfg.
Journal: Mollusc-Derived Brominated Indoles for the Selective Inhibition of Cyclooxygenase: A Computational Expedition. (Pubmed Central) - Dec 16, 2021 These indoles are projected to be non-mutagenic and free from hepatotoxicity, with no inhibition of human ether-a-go-go gene (hERG) I inhibitors, and the oral acute toxicity LD in rats is predicted to be similar or lower than aspirin. Overall, this work has identified a plausible mechanism for selective COX inhibition by natural marine indoles as potential therapeutic candidates for the mitigation of inflammation.
- |||||||||| tramadol hydrochloride / Generic mfg.
Clinical, Journal: A harm reduction model to assess the impact of new treatments for pain over standard of care among patients with osteoarthritis. (Pubmed Central) - Dec 16, 2021 OBJECTIVE: To develop a harm reduction model (HRM) to assess potential reductions of negative clinical outcomes, HRU, and medical costs associated with the use of new treatments in place of oral NSAIDs, tramadol, and non-tramadol opioids among patients with OA of the hip and/or knee in the United States...Robinson is an employee and minor stockholder of Eli Lilly and Company. Rice, White, and Fernan are employees of the Analysis Group, who were paid consultants to Pfizer and Eli Lilly and Company for this study and development of the manuscript.
- |||||||||| paracetamol / Generic mfg.
Review, Journal: Paracetamol (acetaminophen): A familiar drug with an unexplained mechanism of action. (Pubmed Central) - Dec 14, 2021 The current review gives an update and in some cases challenges the different theories on the pharmacology of paracetamol and raises questions on some of the inadequately explored actions of paracetamol. List of Abbreviations: AM404, N-(4-hydroxyphenyl)-arachidonamide; CB1R, Cannabinoid receptor-1; Cmax, Maximum concentration; CNS, Central nervous system; COX, Cyclooxygenase; CSF, Cerebrospinal fluid; ED, 50% of maximal effective dose; FAAH, Fatty acid amidohydrolase; IC, 50% of the maximal inhibitor concentration; LPS, Lipopolysaccharide; NSAIDs, Non-steroidal anti-inflammatory drugs; PGE, Prostaglandin E; TRPV1, Transient receptor potential vanilloid-1.
- |||||||||| Biomarker, PK/PD data, Journal: Pharmacokinetics of transdermal flunixin meglumine and effects on biomarkers of inflammation in horses. (Pubmed Central) - Nov 29, 2021
The mean (range) for C , T and the terminal half-life were 515.6 (369.7-714.0) ng/ml, 8.67 (8.0 12.0) h, and 22.4 (18.3-42.5) h, respectively. Following transdermal administration, based on effects on eicosanoid synthesis, flunixin meglumine inhibited cyclooxygenase 1 and 2 and 15-lipooxygenase activity, with anti-inflammatory effects lasting for 24-72 h.
- |||||||||| paracetamol / Generic mfg.
Preclinical, Review, Journal: Systematic Review of Systemic and Neuraxial Effects of Acetaminophen in Preclinical Models of Nociceptive Processing. (Pubmed Central) - Nov 21, 2021 Review of current targets for this molecule excludes a role of cyclooxygenase inhibitor but includes effects that may be mediated through metabolites acting on the TRPV1 channel, or by effect upon cannabinoid and serotonin signaling. These findings suggest that the mode of action of acetaminophen, a drug with a long therapeutic history of utilization, has surprisingly robust effects on a variety of pain states in clinical patients and in preclinical models with a good therapeutic index, but in spite of its extensive use, its mechanisms of action are yet poorly understood.
- |||||||||| Opdivo (nivolumab) / Ono Pharma, BMS
Clinical, Journal: Effect of cyclooxygenase inhibitor use on immunotherapy efficacy in non-small cell lung cancer. (Pubmed Central) - Nov 21, 2021 These findings suggest that the mode of action of acetaminophen, a drug with a long therapeutic history of utilization, has surprisingly robust effects on a variety of pain states in clinical patients and in preclinical models with a good therapeutic index, but in spite of its extensive use, its mechanisms of action are yet poorly understood. There was no additional or negative impact of COX-I use on the efficacy of ICIs in NSCLC.
- |||||||||| aspirin / Generic mfg.
Journal: A novel anti-inflammatory treatment for bradykinin-induced sore throat or pharyngitis. (Pubmed Central) - Nov 21, 2021 An ASA-based formula (Biovanta) mitigated bradykinin-induced inflammation more strongly than ASA alone in organotypic human respiratory tissues. Surprisingly, we found that many of the most common over the counter sore throat therapies exacerbate inflammation and IL-8 in organotypic human respiratory tissues, suggesting these common treatments may increase the likelihood of further respiratory complications.
- |||||||||| ketorolac / Generic mfg.
Preclinical, Journal: Cyclooxygenase inhibition attenuates brain angiogenesis and independently decreases mouse survival under hypoxia. (Pubmed Central) - Nov 17, 2021 In the present study, we chronically infused mice with ketorolac, a non-specific COX inhibitor that does not cross the blood-brain barrier (BBB), under normoxia or 50% isobaric hypoxia (10% O by volume)...These data also indicate a potential risk for using COX inhibitors under hypoxia conditions in clinics. Further studies are required to elucidate a complete mechanism for brain long-term angiogenesis regulation through COX activity.
- |||||||||| Journal: In a model of SAH-induced neurogenic fever, BAT thermogenesis is mediated by erythrocytes and blocked by agonism of adenosine A1 receptors. (Pubmed Central) - Nov 17, 2021
We demonstrate that following SAH the acute activation of brown adipose tissue leading to NF, is not dependent on PGE, that subarachnoid space injection of whole blood or erythrocytes, but not plasma alone, is sufficient to trigger brown adipose tissue thermogenesis, and that activation of adenosine A1 receptors in the CNS can block the brown adipose tissue thermogenic component contributing to NF after SAH. These findings point to a distinct thermogenic mechanism for generating NF, compared to those due to infectious causes, and will hopefully lead to new therapies.
|