Ketorolac is a non-selective COX inhibitor. It is considered a first- generation NSAID.
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Piroxicam is an NSAID and, as such, is a non-selective COX inhibitor possessing both analgesic and antipyretic properties.
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It is not considered an NSAID because it does not exhibit significant anti-inflammatory activity (it is a weak COX inhibitor). This is despite the evidence that paracetamol and NSAIDs have some similar pharmacological activity.
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Use is not recommended in the third trimester of pregnancy. Naproxen is a nonselective COX inhibitor. It is in the propionic acid class of medications. As an NSAID, naproxen appears to exert its anti- inflammatory action by reducing the production of inflammatory mediators called prostaglandins.
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Tolfenamic acid (Clotam, Tufnil) is a member of the anthranilic acid derivatives (or fenamate) class of NSAID drugs discovered by scientists at Medica Pharmaceutical Company in Finland. Like other members of the class, it is a COX inhibitor and prevents formation of prostaglandins. It is used in the UK as a treatment for migraine.NHS Tolfenamic Acid (Tolfenamic acid 200mg tablets) Page accessed July 3, 2015 It is generally not available in the US.NIH LiverTox Database Mefenamic Acid Last updated June 23, 2015.
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Flufenamic acid (FFA) is a member of the anthranilic acid derivatives (or fenamate) class of NSAID drugs Like other members of the class, it is a COX inhibitor and prevents formation of prostaglandins. FFA is known to bind to and reduce the activity of prostaglandin F synthase and activate TRPC6. It is not widely used in humans as it has a high rate (30-60%) of gastrointestinal side effects. It is generally not available in the US.NIH LiverTox Database Mefenamic Acid Last updated June 23, 2015.
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Meclofenamic acid (meclofenamate sodium, brand Meclomen) is a drug used for joint, muscular pain, arthritis and dysmenorrhea. It is a member of the anthranilic acid derivatives (or fenamate) class of NSAID drugs and was approved by the FDA in 1980.FDA Meclomen page at FDA Page accessed July 3, 2015 Like other members of the class, it is a COX inhibitor and prevents formation of prostaglandins. Scientists led by Claude Winder from Parke-Davis invented meclofenamate sodium in 1964, along with fellow members of the class, mefenamic acid in 1961 and flufenamic acid in 1963.
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N-Arachidonoyl dopamine, an endocannabinoid found in the human CNS, structurally similar to capsaicin, activates the TRPV1 channel with an EC50 of approximately of 50 nM. N-Oleyl-dopamine, another endogenous agonist, binds to human VR1 with an Ki of 36 Nm. Another endocannabinoid anandamide has also been shown to act on TRPV1 receptors. AM404—an active metabolite of paracetamol (also known as acetaminophen) —that serves as an anandamide reuptake inhibitor and COX inhibitor also serves as a potent TRPV1 agonist. The plant-biosynthesized cannabinoid cannabidiol also shows "either direct or indirect activation" of TRPV1 receptors.
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Acemetacin acts as an inhibitor of cyclooxygenase (COX), producing the anti-inflammatory and analgetic (pain relieving) effects. In the body, it is partly metabolized to indometacin, which also acts as a COX inhibitor. The same mechanism is responsible for the antipyretic and antiplatelet effects, which are however not clinically used, as well as for the typical NSAID adverse effects. An advantage of acemetacin is that it reduces gastric damage as compared to indometacin, possibly because acemetacin has less effect on the increase of leukotriene B4 synthesis and tumor necrosis factor (TNF) expression, leading to less induction of leukocyte-endothelial adherence.
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NSAIDs such as ibuprofen work by inhibiting the cyclooxygenase (COX) enzymes, which convert arachidonic acid to prostaglandin H2 (PGH2). PGH2, in turn, is converted by other enzymes to several other prostaglandins (which are mediators of pain, inflammation, and fever) and to thromboxane A2 (which stimulates platelet aggregation, leading to the formation of blood clots). Like aspirin and indomethacin, ibuprofen is a nonselective COX inhibitor, in that it inhibits two isoforms of cyclooxygenase, COX-1 and COX-2. The analgesic, antipyretic, and anti- inflammatory activity of NSAIDs appears to operate mainly through inhibition of COX-2, which decreases the synthesis of prostaglandins involved in mediating inflammation, pain, fever, and swelling.
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Pravadoline (WIN 48,098) is an antiinflammatory and analgesic drug with an IC50 of 4.9 μM and a Ki of 2511 nM at CB1, related in structure to nonsteroidal anti-inflammatory drugs (NSAIDs) such as indometacin. It was developed in the 1980s as a new antiinflammatory and prostaglandin synthesis inhibitor, acting through inhibition of the enzyme cyclooxygenase (COX). However, pravadoline was found to exhibit unexpectedly strong analgesic effects, which appeared at doses ten times smaller than the effective anti- inflammatory dose and so could not be explained by its action as a COX inhibitor. These effects were not blocked by opioid antagonists such as naloxone, and it was eventually discovered that pravadoline represented the first compound from a novel class of cannabinoid agonists, the aminoalkylindoles.
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