Pharmacotherapy of Osteoarthritis

Stitik, Todd P.; Altschuler, Eric Lewin; Foye, Patrick M.

doi:10.1097/01.phm.0000245512.85085.a0

Cited by 21 publications

(13 citation statements)

References 83 publications

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“…The phenyl moiety of phenol was found to lay in the hydrophobic part of the hCA II active site, where CO 2 , the physiologic substrate of the CAs, binds in the precatalytic complex, explaining thus the behaviour of phenol as a unique CO 2 competitive inhibitor. It appeared thus of interest to extend the previous studies [221,222], including in this investigation phenols with clinical and antioxidant applications as food additives [223,224]. Indeed, the inhibition profile of various isozymes with this class of agents is very variable, with inhibition constants ranging from the millimolar to the submicromolar range for many simple phenols.…”

Section: Inhibition Effects Of Some Phenols On Carbonic Anhydrase Isomentioning

confidence: 92%

Phenolic Compounds as Antioxidants: Carbonic Anhydrase Isoenzymes Inhibitors

Gülçın

Beydemır²

2013

Mini Reviews in Medicinal Chemistry

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Antioxidant compounds can scavenge free radicals and increase shelf life by retarding the process of lipid peroxidation, which is one of the major reasons for deterioration of food, medicine and pharmaceutical products during processing and storage. An antioxidant molecule has been defined as any substance when found in low concentrations compared to that of an oxidizable substrate significantly delays or inhibits the oxidation. The major antioxidant compounds are especially phenolics and flavonoids, which are responsible for their health benefits. Carbonic anhydrase (EC 4.2.1.1., CA) is a pH regulatory/metabolic enzyme in all life kingdoms, being found in organisms all over the phylogenetic tree. It catalyzes the hydration of carbon dioxide (CO(2)) to bicarbonate (HCO(3) -) and the corresponding dehydration of HCO(3) -in acidic medium with regeneration of CO(2). Also, CA isoforms are found in a variety of tissues where they participate in several important biological processes such as acid-base balance, respiration, carbon dioxide and ion transport, bone resorption, ureagenesis, gluconeogenesis, lipogenesis and electrolyte secretion. On the other hand, the phenyl moiety of phenol was found to lay in the hydrophobic part of the CA active site, where CO(2), the physiologic substrate of the CAs, binds in the precatalytic complex, explaining thus the behavior of phenol as a unique CO(2) competitive inhibitor. This review consists of two main sections. The first section is devoted to main phenolic antioxidant compounds in the foodstuffs and beverages. The second general section is about some definitions of CA inhibitory effects of the main phenolic compounds used for antioxidant activity. The phenolic compounds and acids had marked especially CA I and CA II inhibitory effects and might be used as leads for generating CA isoenzyme inhibitors. This class of compounds may lead to isoform-selective inhibitors targeting just one or few of the medicinally relevant CAs. In addition, there are given some chemical and kinetic basis and technical details related to phenolic antioxidant compounds and carbonic anhydrase isoenzymes.

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Section: Inhibition Effects Of Some Phenols On Carbonic Anhydrase Isomentioning

confidence: 92%

Phenolic Compounds as Antioxidants: Carbonic Anhydrase Isoenzymes Inhibitors

Gülçın

Beydemır²

2013

Mini Reviews in Medicinal Chemistry

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“…Additionally, Tramadol hydrochloride seems to have a specific Open Access role in the treatment of opiate withdrawal [6] and premature ejaculation [7]. The most frequent adverse effects of Tramadol hydrochloride include constipation, nausea, dizziness, headache, somnolence, and vomiting [8]. The most serious adverse reactions include confusion, hallucination, convulsions, serotonin syndrome and hypersensitivity reactions also, several reports of .Tramadol has a dosedependent analgesic efficacy that lies between that of codeine and morphine, with parental potency comparable to that of pethidine, i.e.…”

Section: Introductionmentioning

confidence: 99%

The effect of Tramadol on some blood and biochemical parameters of male rats (Rattus norvegicus)

Journal¹

2015

Baghdad Sci.J

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The present study aimed to explain the dose-dependent possible deleterious effects of 30 day administration of Tramadol on some hematological and biochemical parameters of laboratory male rats (Rattus norvegicus), the study consisted of eighteen adult male rats randomly divided into three equal groups (each of six). Group 1 (control) were treated by intraperitoneal injection of normal saline solution (0.2 ml), group two (low dose) was treated by intraperitonealy (i.p) injection of Tramadol at a dose of 50 mg/kg/day, group three (high dose) was treated by intraperitonealy injection of Tramadol at a dose of 100 mg/kg/day for 30 days. At the end of experimental period, rats were sacrificed. Blood were collected by cardiac puncture to investigate blood film and biochemical parameters which include Aspartate transaminase (AST), Alanine transaminase (ALT), urea, and glucose. Results explained a significant reduction in hemoglobin (Hb), packed cell volume (PCV), and red blood cells count (RBC), in both treated group and significant elevation in WBC count which is clearly appeared in lymphocyte count, while the biochemical results showed a significant increased in ALT, blood urea, and decreased in blood glucose level in high dose treated group mostly

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“…On the other hand, the main objective of drug use in OA is symptomatic management, reducing both pain and underlying inflammation [22]. Various management guidelines have categorized these drugs as Symptom Modifying Osteoarthritis Drugs (SMOADS) [23, 24] which are divided into 2 subgroups:

rapid-acting drugs including analgesics, nonsteroidal anti-inflammatory drugs (NSAIDs), and intraarticular glucocorticoids and opioids;

slow-acting drugs or SYSADOA (Symptomatic Slow Acting Drugs for Osteoarthritis).

…”

Section: Therapeutic Management Of Osteoarthritismentioning

confidence: 99%

Glucosamine for Osteoarthritis: Biological Effects, Clinical Efficacy, and Safety on Glucose Metabolism

et al. 2014

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Osteoarthritis is a chronic degenerative disorder that currently represents one of the main causes of disability within the elderly population and an important presenting complaint overall. The pathophysiologic basis of osteoarthritis entails a complex group of interactions among biochemical and mechanical factors that have been better characterized in light of a recent spike in research on the subject. This has led to an ongoing search for ideal therapeutic management schemes for these patients, where glucosamine is one of the most frequently used alternatives worldwide due to their chondroprotective properties and their long-term effects. Its use in the treatment of osteoarthritis is well established; yet despite being considered effective by many research groups, controversy surrounds their true effectiveness. This situation stems from several methodological aspects which hinder appropriate data analysis and comparison in this context, particularly regarding objectives and target variables. Similar difficulties surround the assessment of the potential ability of glucosamine formulations to alter glucose metabolism. Nevertheless, evidence supporting diabetogenesis by glucosamine remains scarce in humans, and to date, this association should be considered only a theoretical possibility.

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Pharmacotherapy of Osteoarthritis

Cited by 21 publications

References 83 publications

Phenolic Compounds as Antioxidants: Carbonic Anhydrase Isoenzymes Inhibitors

Phenolic Compounds as Antioxidants: Carbonic Anhydrase Isoenzymes Inhibitors

The effect of Tramadol on some blood and biochemical parameters of male rats (Rattus norvegicus)

Glucosamine for Osteoarthritis: Biological Effects, Clinical Efficacy, and Safety on Glucose Metabolism

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