A sulfonylurea hypoglycemic agent that is metabolized in the liver to 1-hydrohexamide.
A sulfonylurea antidiabetic agent with similar actions and uses to CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p277)
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.
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)
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.
'Ketones' are organic compounds with a specific structure, characterized by a carbonyl group (a carbon double-bonded to an oxygen atom) and two carbon atoms, formed as byproducts when the body breaks down fats for energy due to lack of glucose, often seen in diabetes and starvation states.
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).

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)

Acetohexamide is a first-generation sulfonylurea oral hypoglycemic medication that is used in the management of type 2 diabetes. It works by stimulating the release of insulin from the pancreas and increasing insulin sensitivity in peripheral tissues, thereby lowering blood glucose levels.

The chemical name for Acetohexamide is N-(2-Hydroxyethyl)-1-((p-tbutylphenyl)sulfonyl)urea, and it has a molecular formula of C13H19N2O4S. It is available in various forms, including tablets, for oral administration.

Acetohexamide is typically prescribed when diet and exercise have failed to control blood sugar levels effectively. Like other sulfonylureas, it carries a risk of hypoglycemia (low blood sugar) as a side effect, particularly in elderly patients or those with impaired kidney function. Therefore, it is essential to monitor blood glucose levels regularly while taking this medication and adjust the dosage accordingly.

It's important to note that Acetohexamide should be used under the supervision of a healthcare provider, and patients should follow their doctor's instructions carefully when taking this medication.

Carbutamide is a first-generation sulfonylurea oral antidiabetic drug. It is used in the treatment of type 2 diabetes mellitus to lower blood glucose levels by stimulating insulin secretion from the pancreas. Carbutamide acts by closing the K+ channels in the beta cells of the pancreas, which leads to depolarization of the cell membrane and opening of Ca2+ channels. The influx of Ca2+ ions triggers the exocytosis of insulin-containing vesicles, resulting in increased insulin secretion.

Carbutamide has been largely replaced by newer sulfonylureas due to its shorter duration of action and higher incidence of side effects such as hypoglycemia, allergic reactions, and gastrointestinal disturbances. It is not commonly used in clinical practice today.

Cortisone reductase is not a widely used medical term, but it generally refers to an enzyme that converts cortisone to its active form, cortisol. Cortisol is a steroid hormone produced by the adrenal gland that helps regulate metabolism and helps your body respond to stress. The enzyme responsible for this conversion is specifically called 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1).

There are two types of 11β-HSD enzymes: 11β-HSD1 and 11β-HSD2. While 11β-HSD1 acts as a reductase, converting cortisone to cortisol, 11β-HSD2 has an opposing function, working as a dehydrogenase that converts cortisol to cortisone. These enzymes play crucial roles in maintaining the balance of cortisol levels in the body and are involved in various physiological processes.

It is important to note that 'cortisone reductase' may not be a term commonly used by medical professionals, and it might be more appropriate to refer to the enzyme as 11β-HSD1 for clarity and precision.

Chlorpropamide is a type of oral anti-diabetic drug known as a sulfonylurea, which is used to lower blood glucose levels in people with type 2 diabetes. It works by stimulating the release of insulin from the pancreas and increasing the sensitivity of peripheral tissues to insulin.

Here's the medical definition:

Chlorpropamide: A first-generation sulfonylurea medication used in the management of type 2 diabetes mellitus. It acts by stimulating the release of insulin from the pancreatic beta cells and increasing peripheral tissue sensitivity to insulin. Chlorpropamide has a longer duration of action than other sulfonylureas, with a peak effect at around 6-12 hours after administration. Common side effects include hypoglycemia, weight gain, and gastrointestinal symptoms such as nausea and diarrhea. It is important to monitor blood glucose levels regularly while taking chlorpropamide to avoid hypoglycemia.

Isoxsuprine is a medication that belongs to a class of drugs known as vasodilators. It works by relaxing and widening the blood vessels, which improves the flow of blood and oxygen to the heart. Isoxsuprine is primarily used in the treatment of chronic foot pain (vasospastic disorders) associated with peripheral vascular disease, such as Raynaud's phenomenon or intermittent claudication.

The medical definition of Isoxsuprine can be stated as:

A synthetic imidazolidinone derivative and a selective beta-2 adrenergic receptor agonist, used in the form of its hydrochloride salt (Isoxsuprine HCl) for the treatment of chronic foot pain caused by peripheral vascular disorders. Isoxsuprine acts as a vasodilator, relaxing and widening blood vessels, thereby enhancing blood flow and oxygen supply to the heart. It is also used off-label in some cases to manage premature labor due to its ability to relax uterine smooth muscle.

Ketones are organic compounds that contain a carbon atom bound to two oxygen atoms and a central carbon atom bonded to two additional carbon groups through single bonds. In the context of human physiology, ketones are primarily produced as byproducts when the body breaks down fat for energy in a process called ketosis.

Specifically, under conditions of low carbohydrate availability or prolonged fasting, the liver converts fatty acids into ketone bodies, which can then be used as an alternative fuel source for the brain and other organs. The three main types of ketones produced in the human body are acetoacetate, beta-hydroxybutyrate, and acetone.

Elevated levels of ketones in the blood, known as ketonemia, can occur in various medical conditions such as diabetes, starvation, alcoholism, and high-fat/low-carbohydrate diets. While moderate levels of ketosis are generally considered safe, severe ketosis can lead to a life-threatening condition called diabetic ketoacidosis (DKA) in people with diabetes.

Alcohol oxidoreductases are a class of enzymes that catalyze the oxidation of alcohols to aldehydes or ketones, while reducing nicotinamide adenine dinucleotide (NAD+) to NADH. These enzymes play an important role in the metabolism of alcohols and other organic compounds in living organisms.

The most well-known example of an alcohol oxidoreductase is alcohol dehydrogenase (ADH), which is responsible for the oxidation of ethanol to acetaldehyde in the liver during the metabolism of alcoholic beverages. Other examples include aldehyde dehydrogenases (ALDH) and sorbitol dehydrogenase (SDH).

These enzymes are important targets for the development of drugs used to treat alcohol use disorder, as inhibiting their activity can help to reduce the rate of ethanol metabolism and the severity of its effects on the body.

... ". The Practitioner. 193: 555-60. PMID 14216839. "Acetohexamide". DrugBank. "Acetohexamide". Medline Plus. ... Acetohexamide bind to an ATP-sensitive K+ (KATP) channel on the cell membrane of pancreatic beta cells. This inhibits the out ... Acetohexamide (trade name Dymelor) is a first-generation sulfonylurea medication used to treat diabetes mellitus type 2, ... Oral hypoglycemic drugs, including acetohexamide, have been associated with increased cardiovascular mortality. Talk to your ...
Acetohexamide A pill taken to lower the level of glucose (sugar) in the blood. People with Type 2 diabetes may take these pills ...
They include acetohexamide, carbutamide, chlorpropamide, glycyclamide (tolcyclamide), metahexamide, tolazamide and tolbutamide ...
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... acetohexamide MeSH D02.948.828.204 - carbutamide MeSH D02.948.828.283 - chlorpropamide MeSH D02.948.828.475 - gliclazide MeSH ... acetohexamide MeSH D02.886.590.795.204 - carbutamide MeSH D02.886.590.795.283 - chlorpropamide MeSH D02.886.590.795.475 - ...
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 ...
Sulfamethoxypyridazine Sulfametoxydiazine Ultra long-acting Sulfadoxine Sulfametopyrazine Terephtyl Acetohexamide Carbutamide ...
... acetohexamide acetohexamide (INN) acetohydroxamic acid (INN) acetophenazine (INN) acetorphine (INN) Acetoxyl acetryptine (INN) ...
First-generation agents tolbutamide acetohexamide tolazamide chlorpropamide Second-generation agents glipizide glyburide or ...
Acetohexamide". The Practitioner. 193: 555-60. PMID 14216839. "Acetohexamide". DrugBank. "Acetohexamide". Medline Plus. ... Acetohexamide bind to an ATP-sensitive K+ (KATP) channel on the cell membrane of pancreatic beta cells. This inhibits the out ... Acetohexamide (trade name Dymelor) is a first-generation sulfonylurea medication used to treat diabetes mellitus type 2, ... Oral hypoglycemic drugs, including acetohexamide, have been associated with increased cardiovascular mortality. Talk to your ...
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Chlorpropamide (Diabinese), tolazamide (Tolinase), acetohexamide (Dymelor), or tolbutamide (Orinase) You are also at increased ...
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  • A child in whom ingestion of any first-generation sulfonylurea (eg, chlorpropamide, acetohexamide, tolbutamide, tolazamide) is suspected should be admitted to the pediatric ward for at least 24 hours of observation, regardless of initial symptoms. (medscape.com)
  • Acetohexamide (trade name Dymelor) is a first-generation sulfonylurea medication used to treat diabetes mellitus type 2, particularly in people whose diabetes cannot be controlled by diet alone. (wikipedia.org)
  • Also it can be used for the study of acetohexamide, Takla and Dakas demonstrated alerid that in each case. (naplesforumonservice.it)
  • Current approaches include the study of acetohexamide, Takla and penisole oil Dakas demonstrated that in contrast to other industries and services. (buyo-g.net)
  • Additional solid-state techniques The study metfornin of acetohexamide, Takla and Dakas demonstrated that in each case. (auxerretv.com)
  • Here is an example: Acetazolamide (diuretic) vs. Acetohexamide (treats diabetes and helps lower blood glucose) Also, during this step confirm that the medication is not expired or damaged along with the patient's allergies. (collepals.com)
  • Post hii inahusu zaidi dawa ya Acetohexamide kwa matibabu ya sukari, kama tulivyoona katika post iliyopita kwamba kuna kipindi ambacho kongosho linatoa insulini lakini seli haziko tayari kupokea hiyo insulini. (bongoclass.com)
  • Oral hypoglycemic drugs, including acetohexamide, have been associated with increased cardiovascular mortality. (wikipedia.org)
  • Acetohexamide (trade name Dymelor) is a first-generation sulfonylurea medication used to treat diabetes mellitus type 2, particularly in people whose diabetes cannot be controlled by diet alone. (wikipedia.org)
  • 2023. https://nursing.unboundmedicine.com/nursingcentral/view/Davis-Drug-Guide/51007/4/acetoHEXAMIDE. (unboundmedicine.com)
  • We report a case of cholestatic hepatitis accompanied by peripheral and hepatic eosinophilia in a patient taking acetohexamide for a period of 1.5 yr. (nih.gov)
  • Oral hypoglycemic drugs, including acetohexamide, have been associated with increased cardiovascular mortality. (wikipedia.org)
  • An overview of Genetic Toxicology Mammalian Cell Mutagenicity study conclusions related to Acetohexamide (968-81-0). (nih.gov)
  • The FDA stated in the study of acetohexamide, Takla and Dakas demonstrated that macrocyclic antibiotic CSP with MS wellbutrin detection. (losaltos.com)