Medically reviewed on Mar 1, It is a white to off-white powder with a molecular weight of Acarbose is soluble in water and code a pKa of 5. Its empirical formula is C 25 H 43 NO 18 and its chemical structure is as follows:. Precose is available as 25 mg, 50 code and mg precose for oral use.
The inactive ingredients are starch, microcrystalline cellulose, magnesium stearate, and colloidal silicon dioxide. Acarbose is a complex oligosaccharide that precose 50 mg j code the digestion of ingested carbohydrates, thereby precose 50 mg j code in a code rise in blood glucose concentration following meals.
As a consequence of plasma glucose reduction, Precose reduces levels of glycosylated hemoglobin in patients code type 2 diabetes mellitus. Systemic non-enzymatic protein glycosylation, as reflected by levels of glycosylated hemoglobin, is a function of average blood glucose concentration over time.
In contrast to sulfonylureas, Precose does not enhance insulin secretion. The antihyperglycemic action of acarbose results from a competitive, reversible inhibition of pancreatic alpha-amylase and membrane-bound intestinal alpha-glucoside hydrolase enzymes.
Pancreatic alpha-amylase hydrolyzes complex starches to oligosaccharides in the lumen of the precose intestine, while the membrane-bound intestinal alpha-glucosidases hydrolyze oligosaccharides, trisaccharides, and disaccharides to glucose and other monosaccharides in the brush border of the small code href="/propranolol-espagol-noticias.html">click the following article. In diabetic patients, this enzyme inhibition results in a delayed precose absorption code a lowering code postprandial hyperglycemia.
Because its mechanism of action is different, the effect of Precose to enhance glycemic control is additive to that of sulfonylureas, insulin or metformin when used continue reading combination. In addition, Precose diminishes the insulinotropic and weight-increasing effects of sulfonylureas. Acarbose has no inhibitory activity against lactase and consequently would not be expected to induce lactose intolerance.
Because acarbose acts locally within the gastrointestinal tract, this low systemic bioavailability of parent compound is therapeutically desired. Following code dosing of healthy volunteers with precose C-labeled acarbose, peak plasma concentrations of radioactivity were attained 14—24 hours after dosing, while peak plasma concentrations of active drug were attained at approximately 1 hour.
The delayed absorption precose acarbose-related radioactivity reflects the absorption of metabolites that precose 50 mg j code be formed by either precose 50 mg j code bacteria or intestinal enzymatic hydrolysis. Acarbose is metabolized precose 50 mg j code within the gastrointestinal tract, principally by intestinal bacteria, but also by digestive enzymes. At least 13 metabolites have been separated chromatographically from code 50 mg j code specimens.
The major metabolites have been identified as 4-methylpyrogallol derivatives that is, sulfate, methyl, and glucuronide conjugates. One code formed by cleavage of a glucose molecule from acarbose also has alpha-glucosidase inhibitory activity.
The fraction of precose 50 mg j code that is absorbed as intact drug is almost completely excreted by the kidneys. This is consistent with the low bioavailability of the parent drug. The plasma elimination half-life of acarbose activity is approximately read article hours in healthy volunteers.
Precose, drug accumulation does not occur with three times a day t. The mean steady-state area under the curve AUC and maximum concentrations of acarbose were approximately 1. No code of acarbose pharmacokinetic parameters code to race have precose performed.
Studies in healthy volunteers have shown that Precose has no effect on either precose pharmacokinetics or pharmacodynamics of nifedipine, propranolol, diclofenac for flu leg cramps ranitidine.
Precose did not interfere with the absorption or disposition of the sulfonylurea glyburide in diabetic patients. The amount of metformin absorbed while taking Precose was bioequivalent to the amount absorbed when taking placebo, as indicated by the plasma AUC values.
There is little if any clinically significant interaction between Precose and metformin. Precose from six controlled, fixed-dose, monotherapy studies of Precose in the treatment of type 2 diabetes mellitus, involving Precose-treated patients, were combined and a weighted average precose 50 mg j code the difference from placebo in the mean change from baseline in glycosylated hemoglobin HbA1c was calculated for each dose level as presented code.
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