Acetohexamide: A sulfonylurea hypoglycemic agent that is metabolized in the liver to 1-hydrohexamide.Carbutamide: A sulfonylurea antidiabetic agent with similar actions and uses to CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p277)Cortisone Reductase: An enzyme that catalyzes the interconversion of a ketone and hydroxy group at C-20 of cortisone and other 17,20,21-trihydroxy steroids. EC 1.1.1.53.Chlorpropamide: A sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. (From Martindale, The Extra Pharmacopoeia, 30th ed, p277)Isoxsuprine: A beta-adrenergic agonist that causes direct relaxation of uterine and vascular smooth muscle. Its vasodilating actions are greater on the arteries supplying skeletal muscle than on those supplying skin. It is used in the treatment of peripheral vascular disease and in premature labor.KetonesAlcohol Oxidoreductases: A subclass of enzymes which includes all dehydrogenases acting on primary and secondary alcohols as well as hemiacetals. They are further classified according to the acceptor which can be NAD+ or NADP+ (subclass 1.1.1), cytochrome (1.1.2), oxygen (1.1.3), quinone (1.1.5), or another acceptor (1.1.99).DNA Barcoding, Taxonomic: Techniques for standardizing and expediting taxonomic identification or classification of organisms that are based on deciphering the sequence of one or a few regions of DNA known as the "DNA barcode".Anemia, Hemolytic: A condition of inadequate circulating red blood cells (ANEMIA) or insufficient HEMOGLOBIN due to premature destruction of red blood cells (ERYTHROCYTES).Heartburn: Substernal pain or burning sensation, usually associated with regurgitation of gastric juice into the esophagus.Patient Acceptance of Health Care: The seeking and acceptance by patients of health service.Bone Marrow DiseasesHypoglycemia: A syndrome of abnormally low BLOOD GLUCOSE level. Clinical hypoglycemia has diverse etiologies. Severe hypoglycemia eventually lead to glucose deprivation of the CENTRAL NERVOUS SYSTEM resulting in HUNGER; SWEATING; PARESTHESIA; impaired mental function; SEIZURES; COMA; and even DEATH.Monomethylhydrazine: Hydrazine substituted by one methyl group.Candy: Sweet food products combining cane or beet sugars with other carbohydrates and chocolate, milk, eggs, and various flavorings. In the United States, candy refers to both sugar- and cocoa-based confections and is differentiated from sweetened baked goods; elsewhere the terms sugar confectionary, chocolate confectionary, and flour confectionary (meaning goods such as cakes and pastries) are used.Blood Glucose: Glucose in blood.Blood Glucose Self-Monitoring: Self evaluation of whole blood glucose levels outside the clinical laboratory. A digital or battery-operated reflectance meter may be used. It has wide application in controlling unstable insulin-dependent diabetes.Tablets: Solid dosage forms, of varying weight, size, and shape, which may be molded or compressed, and which contain a medicinal substance in pure or diluted form. (Dorland, 28th ed)Terfenadine: A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME.Metformin: A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289)Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Thiazolidinediones: THIAZOLES with two keto oxygens. Members are insulin-sensitizing agents which overcome INSULIN RESISTANCE by activation of the peroxisome proliferator activated receptor gamma (PPAR-gamma).Histamine H1 Antagonists, Non-Sedating: A class of non-sedating drugs that bind to but do not activate histamine receptors (DRUG INVERSE AGONISM), thereby blocking the actions of histamine or histamine agonists. These antihistamines represent a heterogenous group of compounds with differing chemical structures, adverse effects, distribution, and metabolism. Compared to the early (first generation) antihistamines, these non-sedating antihistamines have greater receptor specificity, lower penetration of BLOOD-BRAIN BARRIER, and are less likely to cause drowsiness or psychomotor impairment.Hypoglycemic Agents: Substances which lower blood glucose levels.Histamine H1 Antagonists: Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.Tolazamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE.Sulfonylurea CompoundsTolbutamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290)Sulfonylurea Receptors: ATP-BINDING CASSETTE PROTEINS that are highly conserved and widely expressed in nature. They form an integral part of the ATP-sensitive potassium channel complex which has two intracellular nucleotide folds that bind to sulfonylureas and their analogs.Netherlands Antilles: Former Netherlands overseas territory in the Lesser Antilles in the West Indies. It had included the islands of Aruba, Bonaire, Curacao, Saba, St. Eustatius, and the southern part of St. Martin. The Netherlands Antilles dissolved on October 10, 2010. Aruba, Curacao and Sint Maarten became autonomous territories of the Kingdom of the Netherlands. Bonaire, Saba, and Sint Eustatius are under the direct administration of the Netherlands. (From US Department of State, Background Note)Domperidone: A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.Galactogogues: Substances that induce LACTATION.Gastrointestinal Motility: The motor activity of the GASTROINTESTINAL TRACT.Encyclopedias as Topic: Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)Gastroesophageal Reflux: Retrograde flow of gastric juice (GASTRIC ACID) and/or duodenal contents (BILE ACIDS; PANCREATIC JUICE) into the distal ESOPHAGUS, commonly due to incompetence of the LOWER ESOPHAGEAL SPHINCTER.Suppositories: Medicated dosage forms that are designed to be inserted into the rectal, vaginal, or urethral orifice of the body for absorption. Generally, the active ingredients are packaged in dosage forms containing fatty bases such as cocoa butter, hydrogenated oil, or glycerogelatin that are solid at room temperature but melt or dissolve at body temperature.Gastrointestinal Diseases: Diseases in any segment of the GASTROINTESTINAL TRACT from ESOPHAGUS to RECTUM.MedlinePlus: NATIONAL LIBRARY OF MEDICINE service for health professionals and consumers. It links extensive information from the National Institutes of Health and other reviewed sources of information on specific diseases and conditions.Consumer Health Information: Information intended for potential users of medical and healthcare services. There is an emphasis on self-care and preventive approaches as well as information for community-wide dissemination and use.Social Media: Platforms that provide the ability and tools to create and publish information accessed via the INTERNET. Generally these platforms have three characteristics with content user generated, high degree of interaction between creator and viewer, and easily integrated with other sites.Dissent and Disputes: Differences of opinion or disagreements that may arise, for example, between health professionals and patients or their families, or against a political regime.Internet: A loose confederation of computer communication networks around the world. The networks that make up the Internet are connected through several backbone networks. The Internet grew out of the US Government ARPAnet project and was designed to facilitate information exchange.Peer Review: An organized procedure carried out by a select committee of professionals in evaluating the performance of other professionals in meeting the standards of their specialty. Review by peers is used by editors in the evaluation of articles and other papers submitted for publication. Peer review is used also in the evaluation of grant applications. It is applied also in evaluating the quality of health care provided to patients.Carbamazepine: An anticonvulsant used to control grand mal and psychomotor or focal seizures. Its mode of action is not fully understood, but some of its actions resemble those of PHENYTOIN; although there is little chemical resemblance between the two compounds, their three-dimensional structure is similar.Anticonvulsants: Drugs used to prevent SEIZURES or reduce their severity.Phenytoin: An anticonvulsant that is used to treat a wide variety of seizures. It is also an anti-arrhythmic and a muscle relaxant. The mechanism of therapeutic action is not clear, although several cellular actions have been described including effects on ion channels, active transport, and general membrane stabilization. The mechanism of its muscle relaxant effect appears to involve a reduction in the sensitivity of muscle spindles to stretch. Phenytoin has been proposed for several other therapeutic uses, but its use has been limited by its many adverse effects and interactions with other drugs.Epilepsy: A disorder characterized by recurrent episodes of paroxysmal brain dysfunction due to a sudden, disorderly, and excessive neuronal discharge. Epilepsy classification systems are generally based upon: (1) clinical features of the seizure episodes (e.g., motor seizure), (2) etiology (e.g., post-traumatic), (3) anatomic site of seizure origin (e.g., frontal lobe seizure), (4) tendency to spread to other structures in the brain, and (5) temporal patterns (e.g., nocturnal epilepsy). (From Adams et al., Principles of Neurology, 6th ed, p313)Bone Marrow: The soft tissue filling the cavities of bones. Bone marrow exists in two types, yellow and red. Yellow marrow is found in the large cavities of large bones and consists mostly of fat cells and a few primitive blood cells. Red marrow is a hematopoietic tissue and is the site of production of erythrocytes and granular leukocytes. Bone marrow is made up of a framework of connective tissue containing branching fibers with the frame being filled with marrow cells.Epilepsies, Myoclonic: A clinically diverse group of epilepsy syndromes characterized either by myoclonic seizures or by myoclonus in association with other seizure types. Myoclonic epilepsy syndromes are divided into three subtypes based on etiology: familial, cryptogenic, and symptomatic (i.e., occurring secondary to known disease processes such as infections, hypoxic-ischemic injuries, trauma, etc.).Potassium Channels, Inwardly Rectifying: Potassium channels where the flow of K+ ions into the cell is greater than the outward flow.Membrane Potentials: The voltage differences across a membrane. For cellular membranes they are computed by subtracting the voltage measured outside the membrane from the voltage measured inside the membrane. They result from differences of inside versus outside concentration of potassium, sodium, chloride, and other ions across cells' or ORGANELLES membranes. For excitable cells, the resting membrane potentials range between -30 and -100 millivolts. Physical, chemical, or electrical stimuli can make a membrane potential more negative (hyperpolarization), or less negative (depolarization).Potassium: An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.Ion Channels: Gated, ion-selective glycoproteins that traverse membranes. The stimulus for ION CHANNEL GATING can be due to a variety of stimuli such as LIGANDS, a TRANSMEMBRANE POTENTIAL DIFFERENCE, mechanical deformation or through INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS.G Protein-Coupled Inwardly-Rectifying Potassium Channels: A family of inwardly-rectifying potassium channels that are activated by PERTUSSIS TOXIN sensitive G-PROTEIN-COUPLED RECEPTORS. GIRK potassium channels are primarily activated by the complex of GTP-BINDING PROTEIN BETA SUBUNITS and GTP-BINDING PROTEIN GAMMA SUBUNITS.Potassium Channels: Cell membrane glycoproteins that are selectively permeable to potassium ions. At least eight major groups of K channels exist and they are made up of dozens of different subunits.

Differential pharmacokinetics of acetohexamide in male Wistar-Imamichi and Sprague-Dawley rats: role of microsomal carbonyl reductase. (1/10)

Acetohexamide (AH) is reduced to its alcohol metabolite by carbonyl reductase. We have previously shown that carbonyl reductase present in the liver microsomes of rats is a male-specific and androgen-dependent enzyme. In the present study, the role of microsomal carbonyl reductase in the pharmacokinetics of AH was examined in male Wistar-Imamichi (WI) and Sprague-Dawley (SD) rats after its intravenous administration. AH was eliminated more slowly from plasma in the WI strain, which lacks most of the microsomal carbonyl reductase, than in the SD strain. Furthermore, several pharmacokinetic parameters were derived from the data for the plasma concentrations of AH. The plasma clearance (CL(p)) of AH (72.8+/-11.2 ml/h/kg) in male WI rats was significantly smaller than that (105.5+/-11.1 ml/h/kg) in male SD rats. Testectomy caused a marked decrease, from 105.5+/-11.1 to 44.3+/-11.8 ml/h/kg, in the CL(p) of AH in male SD rats. These results indicate that microsomal carbonyl reductase plays a critical role in the differential pharmacokinetics of AH in male WI and SD rats.  (+info)

Characterization of the binding of sulfonylurea drugs to HSA by high-performance affinity chromatography. (2/10)

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Chromatographic analysis of acetohexamide binding to glycated human serum albumin. (3/10)

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Detection of heterogeneous drug-protein binding by frontal analysis and high-performance affinity chromatography. (4/10)

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In vitro inhibition of breast cancer spheroid-induced lymphendothelial defects resembling intravasation into the lymphatic vasculature by acetohexamide, isoxsuprine, nifedipin and proadifen. (5/10)

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Mechanism of interference with the Jaffe reaction for creatinine. (6/10)

We investigated the mechanism of the Jaffe reaction for determination of creatinine by studying the spectrophotometric, kinetic, and equilibrium properties of the reaction of picrate with creatinine and with cyclic and aliphatic ketones. Absorbance spectra for the reaction products of picrate with all the ketones were superimposable with that of creatinine (Amax, 490 nm). Cyclic ketones not containing nitrogen had a molar absorptivity less than half that of creatinine and equilibrium constants approximately 0.01 that of creatinine. Aliphatic ketones, except for benzylacetone, had molar absorptivities similar to that of creatinine, but all of these compounds had equilibrium constants approximately a tenth or less that of creatinine. The common structure for all of the compounds reacting with picrate is the carbonyl group. The variable magnitude of interference for aliphatic and cyclic ketones is ascribable to the different rate constants, molar absorptivities, and equilibrium constants as compared with creatinine. Structures adjacent to the carbonyl group significantly affect the absorptivity and equilibrium constant, but steric hindrance is the major factor affecting the rate of reaction. We postulate that the carbonyl group is required for the Jaffe reaction, and we suggest a mechanism for the reaction.  (+info)

The effect of sulfonylurea drugs on rabbit myocardial contractility, canine purkinje fiber automaticity, and adenyl cyclase activity from rabbit and human hearts. (7/10)

Long-term clinical studies have associated tolbutamide therapy with an increased incidence of cardiovascular deaths. The effects of this and other sulfonylurea drugs on contractility and rate of isolated rabbit atria, automaticity of isolated dog Purkinje fibers, and adenyl cyclase activity in particulate preparations of rabbit and human hearts were studied. At concentrations that are attained clinically, tolbutamide (10 mg/100 ml) increased contractility of driven rabbit atria to 124+/-5% of control, acetohexamide (3.9 mg/100 ml) to 140+/-5%, chlorpropamide (8.3 mg/100 ml) to 139+/-6%, and tolazamide (3.1 mg/100 ml) to 119+/-6%. These effects were accentuated in the presence of 2.5 x 10(-4) M theophylline and were not blocked by 1 x 10(-5) M propranolol. Adenyl cyclase was activated by each of these drugs at concentrations below those which increase contractility. The drugs also increased the rate and slope of phase 4 depolarization in spontaneously beating Purkinje fibers, but did not alter the spontaneous rate of isolated rabbit atria. Since inotropic and chronotropic stimulation can be deleterious in some clinical settings, these findings may be of significance in interpretation of cardiovascular mortality data.  (+info)

Purification and catalytic properties of a novel acetohexamide-reducing enzyme from rabbit heart. (8/10)

An enzyme catalyzing the metabolic reduction of acetohexamide [4-acetyl-N-(cyclohexyl-carbamoyl)benzenesulfonamide], an oral antidiabetic drug, was purified to homogeneity from the cytosolic fraction of rabbit heart. The molecular mass of the purified enzyme was estimated to be 110 kDa by gel filtration and nondenaturing PAGE and 28 kDa by SDS-PAGE, suggesting that the enzyme is composed of four identical-size subunits. 4-Benzoyl-pyridine and p-nitroacetophenone, typical substrates of carbonyl reductase [EC 1.1.1.184], were not reduced by the enzyme. Of drugs with a ketone group tested, only acetohexamide was a good substrate of the enzyme. the enzyme effectively reduced analogs substituted with various alkyl groups instead of the cyclohexyl group in acetohexamide, although it had little or no ability to reduce analogs substituted with various alkyl groups instead of the methyl group in acetohexamide. The enzyme was inhibited not only by quercetin, a well-known inhibitor of carbonyl reductase, but also by phenobarbital, a potent inhibitor of aldehyde reductase [EC 1.1.1.2]. These results indicate that the enzyme purified from rabbit heart is a novel enzyme responsible for the reduction of acetohexamide and its analogs.  (+info)

The IUPHAR/BPS Guide to Pharmacology. acetohexamide ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs.
If your blood sugar gets too low, you may feel weak, drowsy, confused, anxious, or very hungry. You may also sweat, shake, or have blurred vision, a fast heartbeat, or a headache that will not go away. If you have symptoms of low blood sugar (hypoglycemia), check your blood sugar. If your blood sugar is 70 mg/dL (milligrams per deciliter) or below, do one of the following: Drink 4 ounces (one-half cup) of fruit juice, or eat 5 to 6 pieces of hard candy, or take 2 to 3 glucose tablets. Recheck your blood sugar 15 minutes later. If your blood sugar goes above 70 mg/dL, eat a snack or a meal. If your blood sugar is still below 70 mg/dL, drink one-half cup juice, or eat 5 to 6 pieces of candy, or take 2 to 3 glucose tablets. Carry candy or some type of sugar with you at all times, especially if you are away from home. You can take this if you feel that your blood sugar is too low, even if you do not have a blood glucose meter. Always carefully follow your doctors instructions about how to treat ...
Hypoglycemia (blood sugar levels that are too low), resulting in shakiness, headache, cold sweats, anxiety, and changes in mental state. Stop taking the drug and seek medical help immediately. Severe diarrhea, bleeding, bruising, chills, fever, stomach pain, or heartburn may also occur; stop taking the drug and notify your doctor. Other serious but less-common side effects include bone marrow suppression, hemolytic anemia, and elevation of liver-associated enzymes; these problems can be detected by your doctor ...
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Antibiotic resistance The rise of antibiotic-resistant bacteria in recent times has been well documented but the development and launch of new antimicrobials has actually been slowing down rather than increasing to meet the challenge. Some scientists and clinicians have expressed concern at this imbalance and are worried that the range of...
A microreactor by immobilized trypsin on the activated glycidyl methacrylate-modified cellulose membrane packed column was constructed, Immobilized trypsin mirrored the properties of the free enzyme and showed high stability. A novel method to characterize the activity and reaction kinetics of the immobilized enzyme has been developed based on the frontal analysis of enzymatic reaction products, which was performed by the on-line monitoring of the absorption at 410 nm of p-nitroaniline from the hydrolysis of N-alpha -benzoyl-DL-arginine-p-nitroanilide (BAPNA). The hydrolytic activity of the immobilized enzyme was 55.6% of free trypsin. The apparent Michaelis-Menten kinetics constant (K-m) and V-max values measured by the frontal analysis method were, respectively, 0.12 mM and 0.079 mM min(-1) mg enzyme(-1). The former is very close to that observed by the static and off-line detection methods, but the latter is about 15% higher than that of the static method. Inhibition of the immobilized ...
Define ketone group. ketone group synonyms, ketone group pronunciation, ketone group translation, English dictionary definition of ketone group. n chem the functional group of ketones: a carbonyl group attached to the carbon atoms of two other organic groups Noun 1. ketone group - a group having the...
Analusis, a European journal on Analytical Chemistry, is published under the auspices of the Société Française de Chimie, the Société de Chimie Industrielle and the Gesellschaft Deutscher Chemiker
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Reactive continuous rods of macroporous poly(glycidyl methacrylate-co-ethylene dimethacrylate) were prepared within the confines of a stainless steel column. Then papain was immobilized on these monoliths either directly or linked by a spacer arm. In a further step, a protein A affinity column was used for the characterization of the digestion products of human immunoglobulin G (IgG) by papain. The results showed that papain immobilized on the monolithic rod through a spacer arm exhibits higher activity for the digestion of human IgG than that without a spacer arm. The apparent Michaelis-Menten kinetic constants of free and immobilized papain, K-m and V-max, were determined. The digestion conditions of human IgG with free and immobilized papain were optimized. Comparison of the thermal stability of free and immobilized papain showed that the immobilized papain exhibited higher thermal stability than the free enzyme. The half-time of immobilized papain reaches about a week under optimum pH and ...
Global oral antidiabetic drug market is expected to reach USD 35.91 billion by 2022, growing at a CAGR of 10.2% between 2017 and 2022.
On the basis on the end users/applications, this report focuses on the status and outlook for major applications/end users, consumption (sales), market share and growth rate of Oral Antidiabetic Drugs for each application
ORGANIC COMPOUNDS -- PART OF THE CLASS 532-570 SERIES : : Fatty compounds having an acid moiety which contains the carbonyl of a carboxylic acid, salt, ester, or amide group bonded directly to one end of an acyclic chain of at least seven (7) uninterrupted carbons, wherein any additional carbonyl in the acid moiety is (1) part of an aldehyde or ketone group, (2) bonded directly to a noncarbon atom which is between the additional carbonyl and the chain, or (3) attached indirectly to the chain via ionic bonding : Additional carbonyl in the acid moiety (e.g., oiticica oil, licanic acid, etc.) : The additional carbonyl is in a -C(=O)O- group : Plural additional carbonyls in the acid moiety : Additional oxygen bonded directly to the ring ...
This page includes the following topics and synonyms: First Generation Sulfonylurea, Tolbutamide, Tolazamide, Chlorpropamide, Acetohexamide.
Experimentally, sulfonylureas increase infarct size and accelerate the death of hypoxic cardiomyocytes through blockade of KATPchannels that mediate ischemic preconditioning in myocardium (8,27,28). Increased vulnerability of myocardium to ischemic insult in the presence of sulfonylurea drugs may have contributed to the increased mortality observed in this group of diabetic patients. Indeed, it has been demonstrated in isolated human myocardium (18)and in patients undergoing balloon angioplasty (26)that sulfonylurea drug treatment abolishes the cardioprotective efficacy of ischemic preconditioning. Although the extent of cell damage was not measured in the present study, increased ischemic myocardial injury should result in greater impairment of contractile function, which is an important known determinant of survival after acute MI (29,30). In this regard, our observations that the mean left ventricular ejection fraction was lower and requirement of intra-aortic balloon pump support was greater ...
Tight glycemic control is mandatory for the prevention and treatment of vascular complications in patients suffering from diabetes mellitus. After onset of Type 2 Diabetes, patients are usually treated with diet along with or without different combinations of oral drugs. One first-line drug class are sulfonylurea drugs that are preferably provided to patients who are not obese. The mode of action of sulfonylurea drugs is to increase beta-cell secretion, but it could be shown that they lead to deterioration of the beta-cell secretion product over time, resulting in increased proinsulin secretion. Since proinsulin is an independent cardiovascular risk factor, recent publications have demonstrated an increased risk for cardiovascular events in patients treated with sulfonylurea drugs as compared to other treatment methods.. Combination therapy of sulfonylurea drugs with glitazones has been shown to counterbalance the effect of deteriorated beta-cell secretion and to improve insulin sensitivity and ...
There is much interest in the interactions between the active constituents of traditional Chinese medicine and biomolecules. By use of frontal analysis on an affinity column we have examined the...
Japans largest platform for academic e-journals: J-STAGE is a full text database for reviewed academic papers published by Japanese societies
1. Sepharose 6B gel-filtration analysis of soluble adenylate cyclase from bovine corpus luteum is described. Both zonal and frontal techniques of analysis were used. 2. Under conditions of zonal analysis recoveries of activity were low. It was concluded that dissociation of two or more components of the adenylate cyclase complex was occurring on the column and that the maintenance of the complex was essential for the high-activity state of the catalytic unit. Two peaks of adenylate cyclase activity, of approximate mol. wts. 45,000 and 160,000 were detected. 3. The theory of frontal analysis (or steady-state gel filtration), applied to the study of the interacting components of the adenylate cyclase complex is discussed, and activity profiles are predicted. Activity profiles obtained experimentally be frontal analysis compared well with the theoretically predicted profile and provide evidence that dissociation of a high-activity complex, with concomitant loss of activity, does occur. Recoveries ...
TY - JOUR. T1 - Chromatographic studies of chlorpropamide interactions with normal and glycated human serum albumin based on affinity microcolumns. AU - Tao, Pingyang. AU - Li, Zhao. AU - Matsuda, Ryan. AU - Hage, David S.. PY - 2018/10/15. Y1 - 2018/10/15. N2 - Sulfonylurea drugs have significant binding to proteins in blood, with most of this binding believed to occur with human serum albumin (HSA). High performance affinity chromatography and affinity microcolumns containing immobilized HSA were used to investigate binding by the sulfonylurea drug chlorpropamide to normal HSA and glycated HSA, which is a modified form of HSA that has an increased serum concentration in diabetes. Experiments employing frontal analysis indicated that the binding by chlorpropamide gave a good fit to a two-site model for both normal HSA and glycated HSA samples that were representative of controlled or advanced diabetes. These interactions involved a set of moderate-to-high affinity sites and a set of lower ...
The Jaffe reaction is a colorimetric method used in clinical chemistry to determine creatinine levels in blood and urine. In 1886, Max Jaffe (1841-1911) wrote about its basic principles in the paper Über den Niederschlag, welchen Pikrinsäure in normalem Harn erzeugt und über eine neue Reaction des Kreatinins in which he described the properties of creatinine and picric acid in an alkaline solution. The color change that occurred was directly proportional to the concentration of creatinine, however he also noted that several other organic compounds induced similar reactions. In the early 20th century, Otto Folin adapted Jaffes research into a clinical procedure. The Jaffe reaction, despite its nonspecificity for creatinine, is still widely employed as the method of choice for creatinine testing due to its speed, adaptability in automated analysis, and cost-effectiveness, and is the oldest methodology continued to be used in the medical laboratory. It is this nonspecificity that has motivated ...
Patients with type 2 diabetes frequently have to be treated with more than one drug. Effects of oral antidiabetic drugs depend on the extent of drug absorption from the gut lumen, on metabolism of the drug in the liver, and on the extent of its excretion into bile and urine (21). In general, modification of all these processes by a second, concomitantly administered drug can alter the effects of oral antidiabetic drugs (21).. Recently, it was recognized that a broad variety of drugs, including many cardiovascular drugs such as statins and angiotensin II-receptor antagonists, is transported through biological membranes via specific transport proteins (15,22-24). For example, the efflux transporter P-glycoprotein, which translocates its substrates from the inside of the cell to the outside (e.g., from the hepatocyte into bile) is a major determinant of drug effects (1). If P-glycoprotein-mediated drug excretion is inhibited by a second, concomitantly administered compound, drug plasma ...
Portions of this document last updated: March 01, 2017. Copyright © 2017 Truven Health Analytics Inc. All rights reserved. Information is for End Users use only and may not be sold, redistributed or otherwise used for commercial purposes.. ...
05 Mar 2020 vTv Therapeutics has potential to be strong player in up-and-coming oral drug market for type 1 diabetics Posted in Pharma vTv Therapeutics recently announced positive Phase 2 results for its oral antidiabetic drug, TTP-399, when used as an adjunct therapy to insulin in type 1 diabetes (T1D) patients. If the drug can show potential in allowing certain subsets of T1D patients
HOUSTON -- Diabetic patients treated with three commonly prescribed sulfonylurea drugs had a 50% higher mortality risk compared with patients treated with metformin, data from a large retrospective co
Purpose - Little is known about the comparative effects of common oral antidiabetic drugs ([OADs] metformin, sulfonylureas, or thiazolidinediones [THZs]) on chronic kidney disease (CKD) outcomes in patients newly diagnosed with type 2 diabetes (T2DM) and followed in community primary care practices. Electronic health records (EHRs) were used to evaluate the relationships
Aims: Many clinicians have not employed the frontal perspective. Therefore, the purposes of this paper are to: (1) update the findings in morphology and growth in the transverse dimension; (2) simplify evaluation of facial asymmetry using the Ricketts and Grummons frontal analyses; and (3) describe practical clinical applications of anteroposterior images and analysis. Methods: Maxillary width variations, frontal (anteroposterior) anatomic landmark locations, and frontal tracing methods are specified. Asymmetry conditions are differentially treated. Results: Utilizing frontal facial information, therapeutic approaches are more specific and effective, while directed toward particular etiology. Occlusal plane, midline, chin location, and smile esthetics are primarily addressed. Beautiful facial proportions and smile harmony are demonstrated. Asymmetry of the facial parts is the rule, rather than the exception. Conclusion: Patients view themselves from the frontal perspective, so this carries ...
The invention relates to a flavonoid ester. This flavonoid ester results from the reaction product of at least one flavonoid selected from the group consisting of a flavonoid with a ketone group in the 4-position, a salt, ester or ether of such a flavonoid, and a C-heteroside and/or O-heteroside derivative of such a flavonoid, with the proviso that this flavonoid contains at least one free alcohol group, with an organic monoacid having from 3 to 30 carbon atoms. These flavonoid esters constitute useful active principles for the manufacture of cosmetic, dermopharmaceutical, pharmaceutical, dietetic or agri-foodstuff compositions.
The main ingredient in a standard lollipop is sugar. Sugars are fully hydrated carbon chains meaning that there is a water molecule attached to each carbon. Sugars come in two forms; straight-chain and ring form. When sugars are in straight-chain form, aldehyde and ketone groups are open which leaves them very susceptible to reaction. In this state, sugars are unstable. In ring form, sugars are stable and therefore exist in this form in most foods, including lollipops.. Sugar is a very versatile ingredient and is used in many of food and products we consume every single day. What makes sugar different is the way it interacts with the other ingredients and systems within the food as well as how it is treated. When it is heated enough to break the molecules apart, it generates a complex flavor, changes the color, and creates a pleasing aroma.[10] Sugar can form two types of solids in foods; crystalline and glassy amorphous. Crystalline solids can be found in food products like fondant, fudge, and ...
definition of micronase - an oral antidiabetic drug (trade names DiaBeta and Micronase) that stimulates the release of insulin from the pancreas
Diarrhoea occurs in many illnesses. The aspect of the stools, associated symptoms, the patients medical history, countries visited and medicines being taken all help to identify the causes.. These various causes include a number of drugs that expose patients to acute or chronic diarrhoea, appearing within varying time frames and of very diverse intensity or severity. This applies to some antibiotics, but also to oral antidiabetic drugs, rheumatological and anti-ulcer medication, neurological and psychiatric treatments, anti-cancer drugs etc. As a rule, the consequences are minimal. But sometimes they result in severe disorders, such as dehydration, especially in patients at risk (the elderly and infants). Anti-cancer drugs and some antibiotics expose patients to particularly severe diarrhoea, and patients should be informed and advised to consult a physician, especially if the diarrhoea is accompanied by mucus, blood or a fever.. For some drugs with a narrow therapeutic range (i.e. the ...
Wje diabetes cure. . Type 2 diabetes has traditionally been considered a chronic and incurable disease with treatment focussed on food, oral antidiabetic drugs and. Debido a que los síntomas de otros tipos de diabetes y prediabetes aparecen más de la Diabetes Juvenil al CURE ().. las revistas sobre el síndrome metabólico de la diabetes y la obesidad.
Vonach C, Viola K, Giessrigl B, Huttary N, Raab I, Kalt R, Krieger S, Vo TP, Madlener S, Bauer S, Marian B, Hämmerle M, Kretschy N, Teichmann M, Hantusch B, Stary S, Unger C, Seelinger M, Eger A, Mader R, Jäger W, Schmidt W, Grusch M, Dolznig H, Mikulits W, Krupitza G. NF-κB mediates the 12(S)-HETE-induced endothelial to mesenchymal transition of lymphendothelial cells during the intravasation of breast carcinoma cells. Br. J Cancer. 105:263-71 (2011).. ...
Abstract number 1: Comment on Detection of an Infectious Retrovirus, XMRV, in Blood Cells of Patients with Chronic Fatigue Syndrome Cathie Sudlow,...
Summary: To examine the effect of beta adrenergic drugs on fetal lung development, we administered isoxsuprine to pregnant rabbits for 24 hr and measured indices of pulmonary surfactant synthesis, storage, and release in rabbit fetuses at 26 days gestation. Incorporation of radiolabeled choline into total and disaturated phosphatidylcholine was measured in vitro in fetal lung slices. There was a significant increase in the rate of choline incorporation into disaturated phosphatidylcholine in the isoxsuprine-treated group and a tendency toward an increased incorporation into total phosphatidylcholine as well. We also observed an increase in the pulmonary phospholipid reservoir as evidenced by a significant increase in total lung disaturated phosphatidylcholine and a trend toward higher total lung phosphatidylcholine in the isoxsuprine group. In addition, there was a significant increase in lung lavage L/S ratio in the treated fetuses and in lung deflation stability determined by pressure volume curve. We
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Blood glucose profile characteristics before and at the conclusion of therapy were comparable for the two groups. Eighty-two percent of the glyburide- and 88% of the insulin-treated subjects were able to achieve targeted levels of glycemia. However, eight glyburide-treated women (4%) failed to achieve the desired level of control early in the third trimester and were transferred to insulin therapy. None of the patients developed severe symptoms of hypoglycemia. However, in the insulin-treated group, a significantly higher rate of subjects had 1-6% of their SMBG results in the hypoglycemic range (, 40 mg/dl).. The glyburide- and insulin-treated groups had similar rates of preeclampsia (6%) and cesarean section (23-24%). Neonatal outcomes did not differ significantly between the two groups. Furthermore, the groups had similar rates of LGA infants (12 and 13%, respectively), macrosomia (7 and 4%), lung complications (8 and 6%), hypoglycemia (9 and 6%), admission to a neonatal intensive care unit (6 ...
Alfentanil, alfuzosin, alprazolam, amlodipin, amprenavir, aprepitant, aripiprazol, atazanavir, atorvastatin, bosentan, budesonid, buprenorfin, buspiron, ciklesonid, ciklosporin, darifenacin, darunavir, dasatinib, deksametason, diltiazem, docetaxel, dronedaron, dutasterid, ebastin, eletriptan, eplerenon, erlotinib, ergotamin, erytromycin, etinyløstradiol, etravirin, everolimus, felodipin, fentanyl, fesoterodin, fosamprenavir, flutikason, gefinitib, haloperidol, imatinib, indinavir, isradipin, itrakonazol, ivabradin, kabergolin, karbamazepin, ketokonazol, klaritromycin, kvetiapin, labatinib, lerkandipin, loperamid, lopinavir, loratadin, lovastatin, maraviroc, metadon, metylprednisolon, midazolam, nelfinavir, nevirapin, nifedipin, nilotinib, nimodipin, oksykodon, paklitaxel, pazopanib, prednisolon, prednison2, posakonazol, ranolazin, reboksetin, rifampicin, risperidon, ritonavir, sakinavir, saksagliptin, sertindol, sertralin, sibutramin, sildenafil, simvastatin, sirolimus, solifenacin, sunitinib, ...
IFG = Impaired Fasting Glucose defined as a Postprandial Plasma Glucose (PPG) value ≥140 and ,200 mg/dL (ie, ≥7.8 and ,11.1 mmol/L), with a Fasting Plasma Glucose (FPG) ,126 mg/dL (7.0 mmol/L). IGT = Impaired Glucose Tolerance defined as an FPG ≥110 and ,126 mg/dL (≥6.1 and ,7 mmol/L), without diabetes mellitus (PPG must be ,200 mg/dL [11.1 mmol/L]). OAD = oral antidiabetic drug ...
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23 year old male working at the airport in hospitality. Done my degree in security so will end up perusing that in the near future. Have a bearded dragon as a pet as well who Iv had for about 5 years. Love my sport and socialise but also like to have my alone time. Would a nice clean home as I myself like to be tidy. And a pretty quite house especially when I am on earlys. Hopefully to look for a long term stay. ...
TY - JOUR. T1 - Hydroxyl radical-suppressing mechanism and efficiency of melanin-mimetic nanoparticles. AU - Hayashi, Koichiro. AU - Tokuda, Atsuto. AU - Sakamoto, Wataru. PY - 2018/8/7. Y1 - 2018/8/7. N2 - Harnessing melanins to scavenge free radicals in vivo may yield treatment methods for inflammatory disorders. Furthermore, elucidation of the mechanism underlying melanin-mediated suppression of free radicals, which is yet unclear, is warranted. Herein, we chemically synthesized melanin-mimetic nanoparticles (MeNPs) and investigated the mechanism underlying their use. MeNPs efficiently suppressed hydroxyl radicals by converting some MeNP hydroxyl groups to ketone groups. Furthermore, they suppressed hydroxyl radicals produced by lipopolysaccharide-treated Kupffer cells involved in hepatic cirrhosis pathogenesis, without causing significant cytotoxicity. The present results indicate the suitability of MeNPs to treat hepatic cirrhosis; however, further in vivo studies are warranted to determine ...
Close The Infona portal uses cookies, i.e. strings of text saved by a browser on the users device. The portal can access those files and use them to remember the users data, such as their chosen settings (screen view, interface language, etc.), or their login data. By using the Infona portal the user accepts automatic saving and using this information for portal operation purposes. More information on the subject can be found in the Privacy Policy and Terms of Service. By closing this window the user confirms that they have read the information on cookie usage, and they accept the privacy policy and the way cookies are used by the portal. You can change the cookie settings in your browser. ...
In the Jaffe reaction, creatinine reacts with picric acid to form a colored complex. This forms the basis for the commonest methods for measuring serum creatinine. However, this test has well known limitations. Under normal circumstances, the Jaffe reaction overestimates the serum creatinine concentration by 10-20% because of the presence of endogenous chromogens. These chromogens include acetone and acetoacetate which, in the case of diabetic ketoacidosis, can lead to a significant overestimation of the serum creatinine. Similarly, certain drugs, including cephalosporins, flucytosine and barbiturates, can interfere with the assay ...
definition of glyburide - an oral antidiabetic drug (trade names DiaBeta and Micronase) that stimulates the release of insulin from the pancreas
There is more evidence that sulfonylurea drugs, a mainstay for glucose control in type 2 diabetes for decades, increase the risk of mortality from cardiac events. In a retrospective study, mortality risk showed a dose-dependent rise, which further suggests a causal link to adverse cardiac events for sulfonylureas,
Article: OCarroll R, Chambers J, Dennis M, Sudlow C & Johnston M (2014) Improving medication adherence in stroke survivors: Mediators and moderators of treatment effects. |i|Health Psychology|/i|, 33 (10), pp. 1241-1250. https://doi.org/10.1037/hea0000082
The alkylation of bromobenzene and toluene on zeolite H-USY (Si/Al 15) was studied using a high-throughput frontal analysis experimental setup. Adsorption properties of the involved components were determined using the batch technique. Reactions were performed using allyl alcohol, allyl acetate, 1-octen-3-ol, and allyl chloride as alkylating agents at 200 degrees C in the liquid phase. The reaction products could be divided into 3 fractions: (1) light components formed in side reactions of the alkylating agent; (2) primary alkylation products resulting from the alkylation of bromobenzene or toluene and subsequent rearrangement reactions; and (3) a heavy fraction consisting of secondary alkylation products and polyaromatics. Whereas the use of allyl chloride and 1-octen-3-ol as alkylating agents resulted mainly in the formation of undesired side products, bromobenzene was efficiently alkylated with allyl alcohol and allyl acetate, resulting in the formation of allyl bromobenzene, cis-2-propenyl ...
Oral antidiabetic medication used for treatment of Diabetes Type II, Obesity and Polycystic Ovarian Syndrome (PCOS). Biguanide drugs act by decreasing Neoglycogenesis (new formation of sugar) in the liver. Low risk of Hypoglycemia. Metformin is excreted into breast milk in non-significant amount and without harmful effect on breastfed infants of treated mothers, Obesity is associated with breastfeeding difficulties. In spite of Metformin has beneficial effect on Obesity, this is not true with PCOS because lactation capacity is related to growth of breast tissue during pregnancy which is not improved by the use of Metformin, Oral antidiabetic drugs are not effective for Diabetes Type I. For Diabetes Type II diet, physical exercise and breastfeeding may ameliorate glycemia levels. See remarks on mothers Diabetes Mellitus by consulting specific item.
Monosaccharides (C-H2O)n, n , 3, are the simplest form of carbohydrates. They may be subcategorized as aldoses or ketoses, if the molecule contains an aldehyde or ketone functional groups respectively. Aldoses have a carbonyl group in the form of an aldehyde on the end of the carbon chain and ketoses have a ketone group somewhere along the sugar backbone. The simplest ketose is dihydroxyacetone (has no chiral centers) while the simplest aldose is glyceraldehyde, which can be found as either the L or D enantiomer. Monosaccharides may be further classified based on the number of carbon atoms as triose (n=3), tetrose (n=4), pentose (n=5), hexose (n=6), heptose (n=7), etc. For example, glucose is known as a aldohexose (a six carbon aldose) and ribose is considered an aldopentose (a five carbon aldose). Sugars have the ability to form cyclic compounds, typically five or six member heterocyclic rings. In addition, sugars can be reducing or non-reducing depending on whether a sugar has a carbonyl ...
Two new eunicellin-based diterpenes, seco-briarellinone (1) and briarellin S (2), and a known seco-asbestinin (3) have been isolated from the methanolic extract of the common octocoral Briareum asbestinum collected in Bocas del Toro, Caribbean of Panama. The structures and relative stereochemistry of the compounds were defined using extensive spectroscopic analysis including 1D, 2D-nuclear magnetic resonance (NMR) and high-resolution mass spectrometry (HRMS). Compounds 1 and 2 displayed anti-inflammatory properties inhibiting nitric oxide (NO) production induced by lipopolisacharide (LPS) in macrophages with an Inhibitory concentration 50% (IC50) of 4.7 μM and 20.3 μM, respectively. This is the first report of briarellin diterpenes containing a ketone group at C-12.
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Free, official coding info for 2018 ICD-10-CM T38.3X6A - includes detailed rules, notes, synonyms, ICD-9-CM conversion, index and annotation crosswalks, DRG grouping and more.
Gabriel B Jaffe MD is a Internal Medicine who practices in Lanham, MD. Get a full report about this doctors background by clicking here.
The next in the Kinsey Millhone Alphabet mystery series from bestselling author Sue Grafton.J is for Jaffe: Wendell Jaffe, dead these past five years. Or s...
Diabetic patients have a significantly worse prognosis after an acute myocardial infarction (AMI) than their counterparts. Previous studies have shown that the number of circulating endothelial progenitor cells (EPCs) significantly increase early after an AMI in normoglycemic patients. However, it is well known that type 2 diabetes mellitus (DM) is associated with impaired function and reduced circulating EPCs levels. Nonetheless, few studies have analyzed EPCs response of diabetics to an AMI and the EPC response of pre-diabetic patients has not been reported yet. Therefore, we hypothesized that in the acute phase of an AMI, diabetic and pre-diabetics have lower circulating EPCs levels than patients with normal glucose metabolism. We also evaluated the possible capacity of chronic antidiabetic treatment in the recovery of EPCs response to an AMI in diabetics. One-hundred AMI patients were prospectively enrolled in the study. Using the high-performance flow cytometer FACSCanto II, circulating EPCs
Oral antidiabetic drug may act by constricting mainly the rectum from kvinder viagra the third. [from old french rehercier to harrow again, from re- back + capere, ceptum to take] mecholyl n. A visual illusion produced by halothane, except that prednisolone 27 mg per day, the rating on the use of perioperative arrhythmia and may enhance their toxicity. Assume the patient has no significant differences in visible hair loss, arthralgia, intracranial hypertension, particularly after surgery (eras ) society recommendations part ii. The test assumes that the deciding on the dsm-iv or icd-6) excludes sounds perceived as four (or sometimes five, six, or seven) qualitatively different emotions tend to initiate micturition when the thickness of the construction which achieves the same cells that protrude into the drug can halt the degradation process. Dysfunction. Behavioural ecology n. A conception of number, english translation published in 1979, entitled notes upon a finding of normal testosterone and ...
Gibson, Lorna; Paul, Laura; Sudlow, Cathie LM. (2017). Potentially serious incidental findings on brain and body magnetic resonance imaging conducted among apparently healthy adults: a systematic review and meta-analysis, [dataset]. http://dx.doi.org/10.7488/ds/2100 ...
... is a member of the sodium channel blocking class of antiepileptic drugs.[60] This may suppress the release of glutamate and aspartate, two of the dominant excitatory neurotransmitters in the CNS.[61] It is generally accepted to be a member of the sodium channel blocking class of antiepileptic drugs,[62] but it could have additional actions since it has a broader spectrum of action than other sodium channel antiepileptic drugs such as phenytoin and is effective in the treatment of the depressed phase of bipolar disorder, whereas other sodium channel blocking antiepileptic drugs are not, possibly on account of its sigma receptor activity. In addition, lamotrigine shares few side-effects with other, unrelated anticonvulsants known to inhibit sodium channels, which further emphasises its unique properties.[63] It is a triazine derivate that inhibits voltage-sensitive sodium channels, leading to stabilization of neuronal membranes. It also blocks L-, N-, and P-type calcium channels and ...
The hormone prolactin stimulates lactation (production of breast milk). Dopamine, released by the hypothalamus stops the release of prolactin from the pituitary gland. Domperidone, by acting as an anti-dopaminergic agent, results in increased prolactin secretion, and thus promotes lactation (that is, it is a galactogogue). In some nations, including Australia, domperidone is used off-label, based on uncertain and anecdotal evidence of its usefulness, as a therapy for mothers who are having difficulty breastfeeding.[24][25] In the United States, domperidone is not approved for this or any other use.[26][27] A study called the EMPOWER trial was designed to assess the effectiveness and safety of domperidone in assisting mothers of preterm babies to supply breast milk for their infants.[28] The study randomized 90 mothers of preterm babies to receive either domperidone 10 mg orally three times daily for 28 days (Group A) or placebo 10 mg orally three times daily for 14 days followed by domperidone ...
... (DHP) is a molecule based upon pyridine, and the parent of a class of molecules that have been semi-saturated with two substituents replacing one double bond. They are particularly well known in pharmacology as L-type calcium channel blockers, used in the treatment of hypertension. Compared with certain other L-type calcium channel blockers (for example those of the phenylalkylamine class such as verapamil) that have significant action at the heart, they are relatively vascular selective in their mechanism of action in lowering blood pressure. ...
InChI=1S/C20H27N5O5S/c1-15-14-18(23-30-15)19(26)21-11-10-16-6-8-17(9-7-16)31(28,29)24-20(27)22-25-12-4-2-3-5-13-25/h6-9,14H,2-5,10-13H2,1H3,(H,21,26)(H2,22,24,27) ...
... (CBZ), sold under the trade name Tegretol among others, is an anticonvulsant medication used primarily in the treatment of epilepsy and neuropathic pain.[1] It is not effective for absence or myoclonic seizures.[1] It is used in schizophrenia along with other medications and as a second-line agent in bipolar disorder.[3][1] Carbamazepine appears to work as well as phenytoin and valproate for focal and generalised seizures.[4] Common side effects include nausea and drowsiness.[1] Serious side effects may include skin rashes, decreased bone marrow function, suicidal thoughts, or confusion.[1] It should not be used in those with a history of bone marrow problems.[1] Use during pregnancy may cause harm to the baby; however, stopping the medication in pregnant women with seizures is not recommended.[1] Its use during breastfeeding is not recommended.[1] Care should be taken in those with either kidney or liver problems.[1] Carbamazepine was discovered in 1953 by Swiss chemist Walter ...
A channel that is "inwardly-rectifying" is one that passes current (positive charge) more easily in the inward direction (into the cell) than in the outward direction (out of the cell). It is thought that this current may play an important role in regulating neuronal activity, by helping to stabilize the resting membrane potential of the cell. By convention, inward current (positive charge moving into the cell) is displayed in voltage clamp as a downward deflection, while an outward current (positive charge moving out of the cell) is shown as an upward deflection. At membrane potentials negative to potassium's reversal potential, inwardly rectifying K+ channels support the flow of positively charged K+ ions into the cell, pushing the membrane potential back to the resting potential. This can be seen in figure 1: when the membrane potential is clamped negative to the channel's resting potential (e.g. -60 mV), inward current flows (i.e. positive charge flows into the cell). However, when the ...
... also binds to and blocks α2δ subunit-containing VDCCs, similarly to gabapentin and pregabalin, and hence is a gabapentinoid.[9][16] Both (R)-phenibut and (S)-phenibut display this action with similar affinity (Ki = 23 and 39 μM, respectively).[9] Moreover, (R)-phenibut possesses 4-fold greater affinity for this site than for the GABAB receptor (Ki = 92 μM), while (S)-phenibut does not bind significantly to the GABAB receptor (Ki , 1 mM).[9] As such, based on the results of this study, phenibut would appear to have much greater potency in its interactions with α2δ subunit-containing VDCCs than with the GABAB receptor (between 5- to 10-fold).[9] For this reason, the actions of phenibut as a α2δ subunit-containing voltage-gated calcium channel blocker or gabapentinoid may be its true primary mechanism of action, and this may explain the differences between phenibut and its close relative baclofen (which, in contrast, has essentially insignificant activity as a gabapentinoid; Ki = 6 ...
InChI=1S/C24H34N2O/c1-21(2)19-27-20-24(25-15-9-10-16-25)18-26(23-13-7-4-8-14-23)17-22-11-5-3-6-12-22/h3-8,11-14,21,24H,9-10,15-20H2,1-2H3 ...
... (marketed as Depamide by Sanofi-Aventis) is a carboxamide derivative of valproic acid used in the treatment of epilepsy and some affective disorders. It is rapidly metabolised (80%) to valproic acid (another anticonvulsant) but has anticonvulsant properties itself. It may produce more stable plasma levels than valproic acid or sodium valproate and may be more effective at preventing febrile seizures. However, it is over one hundred times more potent as an inhibitor of liver microsomal epoxide hydrolase. This makes it incompatible with carbamazepine and can affect the ability of the body to remove other toxins. Valpromide is no safer during pregnancy than valproic acid. Valpromide is formed through the reaction of valproic acid and ammonia via an intermediate acid chloride. In pure form, valpromide is a white crystalline powder and has melting point 125-126 °C. It is practically insoluble in water but soluble in hot water. It is available on the market in some European countries. ...
Most frequent side effects are nausea, orthostatic hypotension, headaches, and vomiting through stimulation of the brainstem vomiting centre.[9] Vasospasms with serious consequences such as myocardial infarction and stroke that have been reported in connection with the puerperium, appear to be extremely rare events.[10] Peripheral vasospasm (of the fingers or toes) can cause Raynaud's Phenomenon. Bromocriptine use has been anecdotally associated with causing or worsening psychotic symptoms (its mechanism is in opposition of most antipsychotics, whose mechanisms generally block dopamine).[11] Pulmonary fibrosis has been reported when bromocriptine was used in high doses for the treatment of Parkinson's disease.[12] Use to suppress milk production after childbirth was reviewed in 2014 and it was concluded that in this context a causal association with serious cardiovascular, neurological or psychiatric events could not be excluded with an overall incidence rate estimated to range between 0.005% ...
Class Ib antiarrhythmic agents are sodium channel blockers. They have fast onset and offset kinetics, meaning that they have little or no effect at slower heart rates, and more effects at faster heart rates. Class Ib agents shorten the action potential duration and reduce refractoriness. These agents will decrease Vmax in partially depolarized cells with fast response action potentials. They either do not change the action potential duration, or they may decrease the action potential duration. Class Ib drugs tend to be more specific for voltage gated Na channels than Ia. Lidocaine in particular is highly frequency dependent, in that it has more activity with increasing heart rates. This is because lidocaine selectively blocks Na channels in their open and inactive states and has little binding capability in the resting state. Class Ib agents are indicated for the treatment of ventricular tachycardia and symptomatic premature ventricular beats, and prevention of ventricular fibrillation. Class Ib ...
... has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels.[1] How this effect is mediated and to what extent this mechanism is involved in the anxiolytic and analgesic effects of kavalactones on the central nervous system is unknown. Kavain's pharmacological activities have not been sufficiently investigated, and neither its effect as a serotonin reuptake inhibitor nor its monoamine (norepinephrine) uptake inhibitions and activation of NMDA receptors have been confirmed. The mechanism behind the psychotropic, sedative, and anxiolytic actions of kavain and related kavalactones is still debated. Direct binding to the benzodiazepine/flumazenil binding site of the GABA-A receptor does not occur with kavain enantiomers.[2] Many studies involved kava extracts from different plant parts and are, therefore, not applicable to kavain itself. In 2016, kavain was shown to bind at the α4β2δ GABAA receptor and ...
... has a potential for drug interactions; caution should be used in combining other medicines with it, including other antiepileptics and mood stabilizers.[12] Lower levels of carbamazepine are seen when administrated with phenobarbital, phenytoin, or primidone, which can result in breakthrough seizure activity. Carbamazepine, as a CYP450 inducer, may increase clearance of many drugs, decreasing their concentration in the blood to subtherapeutic levels and reducing their desired effects.[19] Drugs that are more rapidly metabolized with carbamazepine include warfarin, lamotrigine, phenytoin, theophylline, and valproic acid.[12] Drugs that decrease the metabolism of carbamazepine or otherwise increase its levels include erythromycin,[20] cimetidine, propoxyphene, and calcium channel blockers.[12] Carbamazepine also increases the metabolism of the hormones in birth control pills and can reduce their effectiveness, potentially leading to unexpected pregnancies.[12] As a drug that induces ...
... occludes the pore of calcium-activated voltage-gated shaker K+ channels by binding to one of four independent, overlapping binding sites.[6][7] It binds both to the open and the closed states. In addition, the block is enhanced as the ionic strength is lowered.[8] This block occurs as the Asn 30 on the CTX interacts with the Asp 381 on the K+ channel.[9] The blockade of K+ channels by the charybdotoxin peptide causes neuronal hyperexcitability. Mutations of the Lys31Gln and the Asn30Gln had the effect of lessening the CTX block of the pore on the shaker channel.[9] ...
... has several uses including the treatment of abnormal heart rhythms or arrhythmias, chronic pain, and myotonia. In general when treating arrhythmias, mexiletine is reserved for use in dangerous heart rhythm disturbances such as ventricular tachycardia.[2] It is of particular use when treating arrhythmias caused by long QT syndrome.[3] The LQT3 form of long QT syndrome is amenable to treatment with mexiletine as this form is caused by defective sodium channels that continue to release a sustained current rather than fully inactivating, however other forms of long QT syndrome can also be treated with this medication.[3] Mexiletine has been used to treat chronic pain and may also be used to treat muscle stiffness resulting from myotonic dystrophy (Steinert's disease) or nondystrophic myotonias such as myotonia congenita (Thomsen syndrome or Becker syndrome).[4][5] ...
... is available as a generic medication and usually not too expensive.[7] Wholesale it costs between US$0.003 and US$0.15 per dose.[8] A month of treatment is about US$30 in the United States.[2] Since September 2012, the marketing licence in the UK has been held by Flynn Pharma Ltd, of Dublin, Ireland, and the product, although identical, has been called Phenytoin Sodium xxmg Flynn Hard Capsules. (The xxmg in the name refers to the strength-for example "Phenytoin sodium 25 mg Flynn Hard Capsules").[49] The capsules are still made by Pfizer's Goedecke subsidiary's plant in Freiburg, Germany and they still have Epanutin printed on them.[50] After Pfizer's sale of the UK marketing licence to Flynn Pharma, the price of a 28-pack of 25 mg phenytoin sodium capsules marked Epanutin rose from 66p (about $0.88) to £15.74 (about $25.06). Capsules of other strengths also went up in price by the same factor-2384%,[51] costing the UK's National Health Service an extra £43 million (about $68.44 ...
A press release by GlaxoSmithKline in February 2007 noted that there is a greater incidence of fractures of the upper arms, hands and feet in female diabetics given rosiglitazone compared with those given metformin or glyburide. The information was based on data from the ADOPT trial. Following release of this statement, Takeda Pharmaceutical Company, the developer of pioglitazone (sold as Actos in many markets) admitted that it has similar implications for female patients.[7] The risk of hypoglycemia is low in the absence of other drugs that lower blood glucose. Pioglitazone can cause fluid retention and peripheral edema. As a result, it may precipitate congestive heart failure (which worsens with fluid overload in those at risk). It may cause anemia. Mild weight gain is common due to increase in subcutaneous adipose tissue. In studies, patients on pioglitazone had an increased proportion of upper respiratory tract infection, sinusitis, headache, myalgia and tooth problems. Chronic ...
... is effective for prevention of shivering during surgery or recovery from surgery.[5][6] Nefopam was significantly more effective than aspirin as an analgesic in one clinical trial,[7] although with a greater incidence of side effects such as sweating, dizziness and nausea, especially at higher doses.[8][9] The estimated relative potency of nefopam to morphine indicates that 20 mg of nefopam HCl is the approximate analgesic equal of 12 mg of morphine with comparable analgesic efficacy to morphine,[10][11][12] or oxycodone,[13] while Nefopam tends to produce fewer side effects, does not produce respiratory depression,[14] and has much less abuse potential, and so is useful either as an alternative to opioids, or as an adjunctive treatment for use alongside opioid(s) or other analgesics.[12][15] Nefopam is also used to treat severe hiccups.[16] ...
First generation drugs include acetohexamide, carbutamide, chlorpropamide, glycyclamide (tolhexamide), metahexamide, tolazamide ...
Acetohexamide A pill taken to lower the level of glucose (sugar) in the blood. People with Type 2 diabetes may take these pills ...
acetoHEXAMIDE buPROPion vs. busPIRone chlorproMAZINE vs. chlorproPAMIDE clomiPHENE vs. clomiPRAMINE cycloSERINE vs. ...
First-generation agents tolbutamide acetohexamide tolazamide chlorpropamide Second-generation agents glipizide glyburide or ...
... acetohexamide MeSH D02.886.590.795.204 --- carbutamide MeSH D02.886.590.795.283 --- chlorpropamide MeSH D02.886.590.795.475 ... acetohexamide MeSH D02.948.828.204 --- carbutamide MeSH D02.948.828.283 --- chlorpropamide MeSH D02.948.828.475 --- gliclazide ...
A10BB08 Gliquidone A10BB09 Gliclazide A10BB10 Metahexamide A10BB11 Glisoxepide A10BB12 Glimepiride A10BB31 Acetohexamide ...
3-alpha-hydroxyacyl-CoA dehydrogenase deficiency 3-Methylcrotonyl-CoA carboxylase deficiency ACAD9 deficiency Acetohexamide ...
For this reason, acetohexamide is not used to treat diabetes mellitus type 1. Oral hypoglycemic drugs, including acetohexamide ... Acetohexamide lowers blood sugar by stimulating the pancreas to secrete insulin and helping the body use insulin efficiently. ... Acetohexamide (trade name Dymelor) is a first-generation sulfonylurea medication used to treat diabetes mellitus type 2, ...
Read the side effects of Acetohexamide as described in the medical literature. In case of any doubt consult your doctor or ... Acetohexamide - Information. Acetohexamide is used to treat type 2 diabetes mellitus for controlling the high blood sugar level ... Side effect(s) of Acetohexamide Read the side effects of Acetohexamide as described in the medical literature. In case of any ...
Testing Status of Acetohexamide 10667-R. CASRN: 968-81-0. Formula: C15-H20-N2-O4-S. Synonyms/Common Names. *4-Acetyl-N-(( ...
Acetohexamide has been discontinued in the US market. ... Sulfonylureas such as acetohexamide bind to an ATP-dependent K+ ... Acetohexamide may increase the anticoagulant activities of (R)-warfarin.. (S)-Warfarin. Acetohexamide may increase the ... Acetohexamide (Watson) / Dimelin (Shionogi Seiyaku) / Dymelor (Lilly) / Gamadiabet (Salvat). Categories. *Alimentary Tract and ... Acetohexamide has one-third the potency of chlorpropamide, and twice the potency of tolbutamide; however, similar hypoglycemic ...
Do not stop taking acetohexamide without consulting your doctor. Prolonged Use. The dosage may need to be adjusted with ... Acetohexamide may pass into breast milk; caution is advised. Consult your doctor if you are considering breast feeding. ... Acetohexamide is not usually given during pregnancy. Insulin is generally the treatment of choice for pregnant diabetic ... The effects of acetohexamide can be altered by anti- coagulants, antidepressants, aspirin, over-the-counter cold preparations ...
... acetohexamide explanation free. What is acetohexamide? Meaning of acetohexamide medical term. What does acetohexamide mean? ... Looking for online definition of acetohexamide in the Medical Dictionary? ... acetohexamide. Also found in: Dictionary, Thesaurus, Wikipedia.. Related to acetohexamide: acetazolamide, glyburide, tolazamide ... acetohexamide,. n brand names: Dimelor, Dymelor; drug class: sulfonylurea; antidiabetic; action: causes functioning β cells in ...
acetohexamide ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs. ...
Acetohexamide Illinois EPA list. Keith list. Colborn list. Benbrook list. Danish Inert list. EU list. Not Listed. Not Listed. ... Acetohexamide WHO Acute Hazard. TRI Acute Hazard. Material Safety Data Sheets. Acute rating from U.S. EPA product label. U.S. ... Acetohexamide CA Prop 65 Developmental Toxin. U.S. TRI Developmental Toxin. CA Prop 65 Female Reproductive Toxin. CA Prop 65 ... Acetohexamide IARC Carcinogens. U.S. NTP Carcinogens. California Prop 65 Known Carcinogens. U.S. EPA Carcinogens. TRI ...
Acetohexamide (By mouth). Acetohexamide (a-seet-oh-HEX-a-mide). Lowers the level of sugar in your blood. Used together with ... You should not use this medicine if you have had an allergic reaction to acetohexamide or other diabetes drugs such as ... There are many other medicines that you should not use together with acetohexamide. This includes nonprescription (over-the- ...
... ,4-Acetyl-N-[(cyclohexylamino)carbonyl]benzenesulfonamide,1-[(p-acetylphenyl)sulfonyl]-3-cyclohexylurea,3- ...
Acetohexamide medical facts from Drugs.com Physician reviewed acetohexamide patient information - includes acetohexamide ... Acetohexamide - Drugs.com Acetohexamide is a medicine available in a number of countries worldwide. A list of US medications ... Acetohexamide lowers blood sugar by stimulating the pancreas to secrete insulin and helping the body use insulin efficiently.[1 ... Acetohexamide (trade name Dymelor) is a first-generation sulfonylurea medication used to treat diabetes mellitus type 2, ...
www.drugguide.com/ddo/view/Davis-Drug-Guide/51007/all/acetoHEXAMIDE. Quiring C, Sanoski CA, Vallerand AH. AcetoHEXAMIDE. ... acetoHEXAMIDE is a topic covered in the Daviss Drug Guide. To view the entire topic, please sign in or purchase a subscription ... TY - ELEC T1 - acetoHEXAMIDE ID - 51007 A1 - Quiring,Courtney, AU - Sanoski,Cynthia A, AU - Vallerand,April Hazard, BT - ... "AcetoHEXAMIDE." Daviss Drug Guide, 16th ed., F.A. Davis Company, 2019. ...
Acetohexamide Acetohexamide is used to treat type 2 diabetes mellitus for controlling the high blood sugar level together with ...
Acetohexamide Acetohexamide is a first-generation sulfonylurea agent, prescribed for type 2 (non-insulin dependent) diabetes. ...
Dymelor (acetohexamide) disease Interactions. There are 5 disease interactions with Dymelor (acetohexamide) which include:. * ... Dymelor (acetohexamide) alcohol/food Interactions. There is 1 alcohol/food interaction with Dymelor (acetohexamide) ... Check for interactions with Dymelor (acetohexamide). Type in a drug name and select a drug from the list. ... A total of 903 drugs (5914 brand and generic names) are known to interact with Dymelor (acetohexamide). ...
Acetohexamide, acetohexamide (medication), Acetohexamide [Chemical/Ingredient], acetoHEXAMIDE, acetohexamide, Acetylcholine ... Acetohexamide - chemical, Acetylcholine chloride - chemical, Acetohexamide (product), Acetohexamide (substance), ACETOHEXAMIDE ... Ontology: Acetohexamide. (C0000992) Definition (NCI) An intermediate-acting, first-generation sulfonylurea with hypoglycemic ... Acetohexamide is metabolized in the liver to its active metabolite hydroxyhexamide. Definition (MSH) A sulfonylurea ...
Lamotrigine is a member of the sodium channel blocking class of antiepileptic drugs.[60] This may suppress the release of glutamate and aspartate, two of the dominant excitatory neurotransmitters in the CNS.[61] It is generally accepted to be a member of the sodium channel blocking class of antiepileptic drugs,[62] but it could have additional actions since it has a broader spectrum of action than other sodium channel antiepileptic drugs such as phenytoin and is effective in the treatment of the depressed phase of bipolar disorder, whereas other sodium channel blocking antiepileptic drugs are not, possibly on account of its sigma receptor activity. In addition, lamotrigine shares few side-effects with other, unrelated anticonvulsants known to inhibit sodium channels, which further emphasises its unique properties.[63] It is a triazine derivate that inhibits voltage-sensitive sodium channels, leading to stabilization of neuronal membranes. It also blocks L-, N-, and P-type calcium channels and ...
The hormone prolactin stimulates lactation (production of breast milk). Dopamine, released by the hypothalamus stops the release of prolactin from the pituitary gland. Domperidone, by acting as an anti-dopaminergic agent, results in increased prolactin secretion, and thus promotes lactation (that is, it is a galactogogue). In some nations, including Australia, domperidone is used off-label, based on uncertain and anecdotal evidence of its usefulness, as a therapy for mothers who are having difficulty breastfeeding.[24][25] In the United States, domperidone is not approved for this or any other use.[26][27] A study called the EMPOWER trial was designed to assess the effectiveness and safety of domperidone in assisting mothers of preterm babies to supply breast milk for their infants.[28] The study randomized 90 mothers of preterm babies to receive either domperidone 10 mg orally three times daily for 28 days (Group A) or placebo 10 mg orally three times daily for 14 days followed by domperidone ...
Dihydropyridine (DHP) is a molecule based upon pyridine, and the parent of a class of molecules that have been semi-saturated with two substituents replacing one double bond. They are particularly well known in pharmacology as L-type calcium channel blockers, used in the treatment of hypertension. Compared with certain other L-type calcium channel blockers (for example those of the phenylalkylamine class such as verapamil) that have significant action at the heart, they are relatively vascular selective in their mechanism of action in lowering blood pressure. ...
InChI=1S/C20H27N5O5S/c1-15-14-18(23-30-15)19(26)21-11-10-16-6-8-17(9-7-16)31(28,29)24-20(27)22-25-12-4-2-3-5-13-25/h6-9,14H,2-5,10-13H2,1H3,(H,21,26)(H2,22,24,27) ...
Carbamazepine (CBZ), sold under the trade name Tegretol among others, is an anticonvulsant medication used primarily in the treatment of epilepsy and neuropathic pain.[1] It is not effective for absence or myoclonic seizures.[1] It is used in schizophrenia along with other medications and as a second-line agent in bipolar disorder.[3][1] Carbamazepine appears to work as well as phenytoin and valproate for focal and generalised seizures.[4] Common side effects include nausea and drowsiness.[1] Serious side effects may include skin rashes, decreased bone marrow function, suicidal thoughts, or confusion.[1] It should not be used in those with a history of bone marrow problems.[1] Use during pregnancy may cause harm to the baby; however, stopping the medication in pregnant women with seizures is not recommended.[1] Its use during breastfeeding is not recommended.[1] Care should be taken in those with either kidney or liver problems.[1] Carbamazepine was discovered in 1953 by Swiss chemist Walter ...
A channel that is "inwardly-rectifying" is one that passes current (positive charge) more easily in the inward direction (into the cell) than in the outward direction (out of the cell). It is thought that this current may play an important role in regulating neuronal activity, by helping to stabilize the resting membrane potential of the cell. By convention, inward current (positive charge moving into the cell) is displayed in voltage clamp as a downward deflection, while an outward current (positive charge moving out of the cell) is shown as an upward deflection. At membrane potentials negative to potassiums reversal potential, inwardly rectifying K+ channels support the flow of positively charged K+ ions into the cell, pushing the membrane potential back to the resting potential. This can be seen in figure 1: when the membrane potential is clamped negative to the channels resting potential (e.g. -60 mV), inward current flows (i.e. positive charge flows into the cell). However, when the ...
Phenibut also binds to and blocks α2δ subunit-containing VDCCs, similarly to gabapentin and pregabalin, and hence is a gabapentinoid.[9][16] Both (R)-phenibut and (S)-phenibut display this action with similar affinity (Ki = 23 and 39 μM, respectively).[9] Moreover, (R)-phenibut possesses 4-fold greater affinity for this site than for the GABAB receptor (Ki = 92 μM), while (S)-phenibut does not bind significantly to the GABAB receptor (Ki , 1 mM).[9] As such, based on the results of this study, phenibut would appear to have much greater potency in its interactions with α2δ subunit-containing VDCCs than with the GABAB receptor (between 5- to 10-fold).[9] For this reason, the actions of phenibut as a α2δ subunit-containing voltage-gated calcium channel blocker or gabapentinoid may be its true primary mechanism of action, and this may explain the differences between phenibut and its close relative baclofen (which, in contrast, has essentially insignificant activity as a gabapentinoid; Ki = 6 ...
InChI=1S/C24H34N2O/c1-21(2)19-27-20-24(25-15-9-10-16-25)18-26(23-13-7-4-8-14-23)17-22-11-5-3-6-12-22/h3-8,11-14,21,24H,9-10,15-20H2,1-2H3 ...
Valpromide (marketed as Depamide by Sanofi-Aventis) is a carboxamide derivative of valproic acid used in the treatment of epilepsy and some affective disorders. It is rapidly metabolised (80%) to valproic acid (another anticonvulsant) but has anticonvulsant properties itself. It may produce more stable plasma levels than valproic acid or sodium valproate and may be more effective at preventing febrile seizures. However, it is over one hundred times more potent as an inhibitor of liver microsomal epoxide hydrolase. This makes it incompatible with carbamazepine and can affect the ability of the body to remove other toxins. Valpromide is no safer during pregnancy than valproic acid. Valpromide is formed through the reaction of valproic acid and ammonia via an intermediate acid chloride. In pure form, valpromide is a white crystalline powder and has melting point 125-126 °C. It is practically insoluble in water but soluble in hot water. It is available on the market in some European countries. ...
  • The risk or severity of hypoglycemia can be increased when Acetohexamide is combined with 2,4-thiazolidinedione. (drugbank.ca)
  • acetoHEXAMIDE is a topic covered in the Davis's Drug Guide . (drugguide.com)
  • www.drugguide.com/ddo/view/Davis-Drug-Guide/51007/all/acetoHEXAMIDE. (drugguide.com)