Fenamates
Mefenamic Acid
Flufenamic Acid
ortho-Aminobenzoates
Niflumic Acid
Encyclopedias as Topic
Platelet Aggregation Inhibitors
Aspirin
Placebo Effect
Duodenum
Platelet Aggregation
Characterization of the interaction between fenamates and hippocampal neuron GABA(A) receptors. (1/11)
Fenamate NSAIDs have several central effects, including anti-epileptic and neuroprotective actions. The underlying mechanism(s) of these actions are not presently understood. In this study, the effects of five members of the fenamate NSAID group were investigated on native ligand-gated ion channels expressed in cultured rat hippocampal neurons. All fenamates tested (1-100 microM) dose-dependently potentiated GABA-evoked currents; mefenamic acid (MFA) was the most potent and efficacious and was found to shift the GABA dose-response curve to the left without effect on the maximum amplitude or the GABA Hill Slope. The modulation of GABA receptors by MFA was not reduced in the presence of the benzodiazepine antagonist, flumazenil (10 microM) and was moderately voltage-dependent. MFA at concentrations >or=10 microM evoked dose-dependent currents in the absence of GABA. These currents were potentiated by diazepam (1 microM) and blocked by bicuculline (10 microM). The MFA (50 microM) current-voltage relationship and reversal potential were similar to that evoked by GABA. MFA (1-100 microM) had no effects on sub-maximal glycine, glutamate or NMDA evoked currents. These data show that fenamate NSAIDs are a highly effective class of GABA(A) receptor modulator and activators. (+info)Competitive inhibition of organic anion transporting polypeptide 1c1-mediated thyroxine transport by the fenamate class of nonsteroidal antiinflammatory drugs. (2/11)
(+info)Activation of TRPA1 channels by fenamate nonsteroidal anti-inflammatory drugs. (3/11)
(+info)Characterization of renal papillary antigen 1 (RPA-1), a biomarker of renal papillary necrosis. (4/11)
(+info)Selective inhibition of the tumor marker AKR1B10 by antiinflammatory N-phenylanthranilic acids and glycyrrhetic acid. (5/11)
A human aldose reductase-like protein, AKR1B10 in the aldo-keto reductase (AKR) superfamily, was recently identified as a tumor marker of several types of cancer. Tolrestat, an aldose reductase inhibitor (ARI), is known to be the most potent inhibitor of the enzyme. In this study, we compared the inhibitory effects of other ARIs including flavonoids on AKR1B10 and aldose reductase to evaluate their specificity. However, ARIs showed lower inhibitory potency for AKR1B10 than for aldose reductase. In the search for potent and selective inhibitors of AKR1B10 from other drugs used clinically, we found that non-steroidal antiinflammatory N-phenylanthranilic acids, diclofenac and glycyrrhetic acid competitively inhibited AKR1B10, showing K(i) values of 0.35-2.9 microM and high selectivity to this enzyme (43-57 fold versus aldose reductase). Molecular docking studies of mefenamic acid and glycyrrhetic acid in the AKR1B10-nicotinamide adenine dinucleotide phosphate (NADP(+)) complex and site-directed mutagenesis of the putative binding residues suggest that the side chain of Val301 and a hydrogen-bonding network among residues Val301, Gln114 and Ser304 are important for determining the inhibitory potency and selectivity of the non-steroidal antiinflammatory drugs. Thus, the potent and selective inhibition may be related to the cancer chemopreventive roles of the drugs, and their structural features may facilitate the design of new anti-cancer agents targeting AKR1B10. (+info)Trapping of palindromic ligands within native transthyretin prevents amyloid formation. (6/11)
(+info)Fenamates as TRP channel blockers: mefenamic acid selectively blocks TRPM3. (7/11)
(+info)The pharmacological profile of brain liver intestine Na+ channel: inhibition by diarylamidines and activation by fenamates. (8/11)
(+info)Fenamates is a term used to refer to a group of non-steroidal anti-inflammatory drugs (NSAIDs) that have a chemical structure related to fenamic acid. This group includes medications such as mefenamic acid, flufenamic acid, and tolfenamic acid, among others.
Fenamates are used to relieve pain, reduce inflammation, and lower fever. They work by inhibiting the activity of cyclooxygenase (COX) enzymes, which play a key role in the production of prostaglandins, hormone-like substances that mediate various physiological processes, including inflammation and pain perception.
Like other NSAIDs, fenamates can cause gastrointestinal side effects such as stomach ulcers, bleeding, and perforation, especially when taken in high doses or for prolonged periods. They may also increase the risk of cardiovascular events such as heart attack and stroke, particularly in people with pre-existing cardiovascular disease or other risk factors.
It is important to use fenamates only under the supervision of a healthcare provider and to follow their dosage instructions carefully to minimize the risk of adverse effects.
Mefenamic Acid is a non-steroidal anti-inflammatory drug (NSAID) commonly used for its analgesic, antipyretic, and anti-inflammatory properties. It works by inhibiting the enzyme cyclooxygenase (COX), which is responsible for prostaglandin synthesis, a key player in pain and inflammation processes.
Mefenamic Acid is primarily used to treat mild to moderate pain, including menstrual cramps, primary dysmenorrhea, post-operative pain, and various types of inflammatory conditions such as rheumatoid arthritis and osteoarthritis.
Common side effects may include gastrointestinal disturbances like nausea, vomiting, diarrhea, or abdominal pain. Long-term use of Mefenamic Acid has been associated with increased risks of cardiovascular events, gastrointestinal ulcers, and bleeding. Therefore, it is essential to follow the recommended dosage and consult a healthcare professional for appropriate usage and potential interactions with other medications.
Flufenamic Acid is a type of non-steroidal anti-inflammatory drug (NSAID) that is used to relieve pain, reduce inflammation, and lower fever. It works by blocking the action of certain enzymes in the body, such as cyclooxygenase (COX), which are involved in producing substances that cause pain and inflammation. Flufenamic Acid is available in various forms, including tablets, capsules, and suppositories, and is used to treat a variety of conditions, such as menstrual cramps, arthritis, and muscle or bone injuries. It is important to note that like all NSAIDs, Flufenamic Acid can have side effects, particularly if taken in large doses or for long periods of time, so it should be used only under the supervision of a healthcare provider.
Ortho-Aminobenzoates are chemical compounds that contain a benzene ring substituted with an amino group in the ortho position and an ester group in the form of a benzoate. They are often used as pharmaceutical intermediates, plastic additives, and UV stabilizers. In medical contexts, one specific ortho-aminobenzoate, para-aminosalicylic acid (PABA), is an antibiotic used in the treatment of tuberculosis. However, it's important to note that "ortho-aminobenzoates" in general do not have a specific medical definition and can refer to any compound with this particular substitution pattern on a benzene ring.
Niflumic acid is a non-steroidal anti-inflammatory drug (NSAID) that is primarily used as a topical agent for the treatment of pain and inflammation associated with various musculoskeletal conditions, such as strains, sprains, and arthritis. It works by inhibiting the activity of cyclooxygenase (COX) enzymes, which are involved in the production of prostaglandins, chemicals that mediate inflammation, pain, and fever.
Niflumic acid is available as a cream or gel for topical application, and it is not typically used for systemic treatment due to its potential gastrointestinal side effects. It may also be used off-label for the treatment of other conditions that involve pain and inflammation. As with any medication, niflumic acid should only be used under the guidance of a healthcare professional, and it is important to follow all dosage instructions carefully to minimize the risk of adverse effects.
An encyclopedia is a comprehensive reference work containing articles on various topics, usually arranged in alphabetical order. In the context of medicine, a medical encyclopedia is a collection of articles that provide information about a wide range of medical topics, including diseases and conditions, treatments, tests, procedures, and anatomy and physiology. Medical encyclopedias may be published in print or electronic formats and are often used as a starting point for researching medical topics. They can provide reliable and accurate information on medical subjects, making them useful resources for healthcare professionals, students, and patients alike. Some well-known examples of medical encyclopedias include the Merck Manual and the Stedman's Medical Dictionary.
Platelet aggregation inhibitors are a class of medications that prevent platelets (small blood cells involved in clotting) from sticking together and forming a clot. These drugs work by interfering with the ability of platelets to adhere to each other and to the damaged vessel wall, thereby reducing the risk of thrombosis (blood clot formation).
Platelet aggregation inhibitors are often prescribed for people who have an increased risk of developing blood clots due to various medical conditions such as atrial fibrillation, coronary artery disease, peripheral artery disease, stroke, or a history of heart attack. They may also be used in patients undergoing certain medical procedures, such as angioplasty and stenting, to prevent blood clot formation in the stents.
Examples of platelet aggregation inhibitors include:
1. Aspirin: A nonsteroidal anti-inflammatory drug (NSAID) that irreversibly inhibits the enzyme cyclooxygenase, which is involved in platelet activation and aggregation.
2. Clopidogrel (Plavix): A P2Y12 receptor antagonist that selectively blocks ADP-induced platelet activation and aggregation.
3. Prasugrel (Effient): A third-generation thienopyridine P2Y12 receptor antagonist, similar to clopidogrel but with faster onset and greater potency.
4. Ticagrelor (Brilinta): A direct-acting P2Y12 receptor antagonist that does not require metabolic activation and has a reversible binding profile.
5. Dipyridamole (Persantine): An antiplatelet agent that inhibits platelet aggregation by increasing cyclic adenosine monophosphate (cAMP) levels in platelets, which leads to decreased platelet reactivity.
6. Iloprost (Ventavis): A prostacyclin analogue that inhibits platelet aggregation and causes vasodilation, often used in the treatment of pulmonary arterial hypertension.
7. Cilostazol (Pletal): A phosphodiesterase III inhibitor that increases cAMP levels in platelets, leading to decreased platelet activation and aggregation, as well as vasodilation.
8. Ticlopidine (Ticlid): An older P2Y12 receptor antagonist with a slower onset of action and more frequent side effects compared to clopidogrel or prasugrel.
Aspirin is the common name for acetylsalicylic acid, which is a medication used to relieve pain, reduce inflammation, and lower fever. It works by inhibiting the activity of an enzyme called cyclooxygenase (COX), which is involved in the production of prostaglandins, hormone-like substances that cause inflammation and pain. Aspirin also has an antiplatelet effect, which means it can help prevent blood clots from forming. This makes it useful for preventing heart attacks and strokes.
Aspirin is available over-the-counter in various forms, including tablets, capsules, and chewable tablets. It is also available in prescription strengths for certain medical conditions. As with any medication, aspirin should be taken as directed by a healthcare provider, and its use should be avoided in children and teenagers with viral infections due to the risk of Reye's syndrome, a rare but serious condition that can affect the liver and brain.
The placebo effect is a psychological or psychophysiological phenomenon in which a person's symptoms improve following a treatment but this improvement is not attributable to the properties of the treatment itself. Instead, it is believed to be due to the mind's belief in the effectiveness of the treatment, often influenced by positive expectations and the ritualistic aspects of the therapy itself.
Placebos are often used in clinical trials as a control group to compare against the actual treatment. The placebo effect can make it challenging to determine whether an observed improvement is truly due to the treatment or other factors.
The duodenum is the first part of the small intestine, immediately following the stomach. It is a C-shaped structure that is about 10-12 inches long and is responsible for continuing the digestion process that begins in the stomach. The duodenum receives partially digested food from the stomach through the pyloric valve and mixes it with digestive enzymes and bile produced by the pancreas and liver, respectively. These enzymes help break down proteins, fats, and carbohydrates into smaller molecules, allowing for efficient absorption in the remaining sections of the small intestine.
Platelet aggregation is the clumping together of platelets (thrombocytes) in the blood, which is an essential step in the process of hemostasis (the stopping of bleeding) after injury to a blood vessel. When the inner lining of a blood vessel is damaged, exposure of subendothelial collagen and tissue factor triggers platelet activation. Activated platelets change shape, become sticky, and release the contents of their granules, which include ADP (adenosine diphosphate).
ADP then acts as a chemical mediator to attract and bind additional platelets to the site of injury, leading to platelet aggregation. This forms a plug that seals the damaged vessel and prevents further blood loss. Platelet aggregation is also a crucial component in the formation of blood clots (thrombosis) within blood vessels, which can have pathological consequences such as heart attacks and strokes if they obstruct blood flow to vital organs.
Coronary artery bypass surgery, also known as coronary artery bypass grafting (CABG), is a surgical procedure used to improve blood flow to the heart in patients with severe coronary artery disease. This condition occurs when the coronary arteries, which supply oxygen-rich blood to the heart muscle, become narrowed or blocked due to the buildup of fatty deposits, called plaques.
During CABG surgery, a healthy blood vessel from another part of the body is grafted, or attached, to the coronary artery, creating a new pathway for oxygen-rich blood to flow around the blocked or narrowed portion of the artery and reach the heart muscle. This bypass helps to restore normal blood flow and reduce the risk of angina (chest pain), shortness of breath, and other symptoms associated with coronary artery disease.
There are different types of CABG surgery, including traditional on-pump CABG, off-pump CABG, and minimally invasive CABG. The choice of procedure depends on various factors, such as the patient's overall health, the number and location of blocked arteries, and the presence of other medical conditions.
It is important to note that while CABG surgery can significantly improve symptoms and quality of life in patients with severe coronary artery disease, it does not cure the underlying condition. Lifestyle modifications, such as regular exercise, a healthy diet, smoking cessation, and medication therapy, are essential for long-term management and prevention of further progression of the disease.