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Precose

Generic Precose is used for treating type 2 diabetes in adults whose diabetes cannot be managed with diet alone. Generic Precose may be used alone, in combination with other oral diabetes medicines, or with insulin.

Other names for this medication:

Similar Products:
Glucophage, Actos, Avandia, Amaryl, Glucovance, Micronase, Glycomet

 

Also known as:  Acarbose.

Description

Generic Precose is used for treating type 2 diabetes in adults whose diabetes cannot be managed with diet alone. Generic Precose may be used alone, in combination with other oral diabetes medicines, or with insulin.

Generic Precose is a glucosidase inhibitor. It works by slowing down the enzyme that turns carbohydrates into glucose; it decreases blood sugar levels following a meal.

Precose is also known as Acarbose, Glucobay, Glucor, Rebose.

Generic name of Generic Precose is Acarbose.

Brand name of Generic Precose is Precose.

Dosage

Take Generic Precose by mouth with food.

If you also take charcoal or digestive enzyme preparations, do not take them within 2 to 4 hours before after taking Generic Precose.

Temporary insulin therapy may be necessary during stressful periods (such as fever, trauma, infection, or surgery).

If you want to achieve most effective results do not stop taking Generic Precose suddenly.

Overdose

If you overdose Generic Precose and you don't feel good you should visit your doctor or health care provider immediately.

Storage

Store at room temperature below 25 degrees C (77 degrees F) away from moisture and heat. Keep container tightly closed. Throw away any unused medicine after the expiration date. Keep out of the reach of children.

Side effects

The most common side effects associated with Precose are:

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Side effect occurrence does not only depend on medication you are taking, but also on your overall health and other factors.

Contraindications

Do not take Generic Precose if you are allergic to Generic Precose components.

Be careful with Generic Precose if you're pregnant or you plan to have a baby, or you are a nursing mother.

Do not take Generic Precose if you have blockage of the stomach or intestine or are at risk for these problems.

Do not take Generic Precose if you have long-term (chronic) bowel inflammation, colon ulcers, or stomach or intestine problems that interfere with digestion or nutrient absorption.

Do not take Generic Precose if you have cirrhosis of the liver or unexplained abnormal liver function tests.

Do not take Generic Precose if you have diabetic ketoacidosis (high ketone levels) or severe kidney problems.

Try to be careful with Generic Precose if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement.

Try to be careful with Generic Precose if you have allergies to medicines, foods, or other substances

if you have stomach or intestinal problems, liver problems, or kidney problems.

Try to be careful with Generic Precose if you are taking anticoagulants (eg, warfarin) because the risk of their side effects, including bleeding, may be increased by Generic Precose; calcium channel blockers (eg, verapamil), corticosteroids (eg, prednisone), diuretics (eg, hydrochlorothiazide), estrogen, isoniazid, nicotinic acid, oral contraceptives (birth control pills), phenothiazines (eg, chlorpromazine), phenytoin, sympathomimetics (eg, pseudoephedrine), or thyroid hormone because they may increase or decrease Precose 's effectiveness; insulin or sulfonylureas (eg, glyburide) because the risk of their side effects may be increased by Generic Precose; digoxin because its effectiveness may be decreased by Generic Precose.

Avoid alcohol.

Do not stop taking Generic Precose suddenly.

precose drugs

The findings in pertinent reported studies are reviewed, and the efficacy of various interventions for management of impaired glucose tolerance and type 2 diabetes in slowing the progression of IMT is analyzed.

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Enzymatic subsite mapping earlier predicted 10 binding subsites in the active site substrate binding cleft of barley alpha-amylase isozymes. The three-dimensional structures of the oligosaccharide complexes with barley alpha-amylase isozyme 1 (AMY1) described here give for the first time a thorough insight into the substrate binding by describing residues defining 9 subsites, namely -7 through +2. These structures support that the pseudotetrasaccharide inhibitor acarbose is hydrolyzed by the active enzymes. Moreover, sugar binding was observed to the starch granule-binding site previously determined in barley alpha-amylase isozyme 2 (AMY2), and the sugar binding modes are compared between the two isozymes. The "sugar tongs" surface binding site discovered in the AMY1-thio-DP4 complex is confirmed in the present work. A site that putatively serves as an entrance for the substrate to the active site was proposed at the glycone part of the binding cleft, and the crystal structures of the catalytic nucleophile mutant (AMY1D180A) complexed with acarbose and maltoheptaose, respectively, suggest an additional role for the nucleophile in the stabilization of the Michaelis complex. Furthermore, probable roles are outlined for the surface binding sites. Our data support a model in which the two surface sites in AMY1 can interact with amylose chains in their naturally folded form. Because of the specificities of these two sites, they may locate/orient the enzyme in order to facilitate access to the active site for polysaccharide chains. Moreover, the sugar tongs surface site could also perform the unraveling of amylose chains, with the aid of Tyr-380 acting as "molecular tweezers."

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The public health burden of type 2 diabetes mellitus has been dramatically increased worldwide. Not only its prevalence rate at present but the increase of its incidence in the near future can create a global health problem. The rapid increase of the total number of newly diagnosed diabetic patients proved to be associated with the increasing prevalence rate of obesity. The metabolic syndrome and type 2 diabetes can contribute to accelerated atherosclerosis and, therefore, the target organ damages can carry a serious problem for the individuals and also for the whole society. It is obvious, that the primary prevention of type 2 diabetes mellitus is of great importance. There is now substantial evidence that type 2 diabetes can be prevented or delayed by lifestyle interventions, i.e. diet and exercise should be the first choice in order to avoid weight gain when preventing diabetes. Pharmacological intervention should not be routinely used to prevent diabetes although results of large clinical trials with metformin and acarbose in subjects with impaired glucose tolerance are available. It is noteworthy that a decrease in the number of newly diagnosed diabetes was observed in prospective, double blind clinical studies evaluating the effect of new antihypertensive drugs (captopril, ramipril, lisinopril, nifedipine GITS, amlodipine, losartan) or lipid-lowering agents (pravastatin) on the cardiovascular morbidity and mortality in high risk patients. In these studies the relative risk reduction of newly diagnosed diabetes was evaluated in comparison to placebo or other drugs in a subgroup of non-diabetic patients at baseline. In addition, the incidence of newly diagnosed type 2 diabetes decreased parallel with weight loss in clinical trials with orlistat, an anti-obesity drug. Although new results were provided by evidence based clinical trials a lot of questions remained to be solved. Further research is necessary to understand better how to facilitate effective primary prevention of type 2 diabetes. Further data are needed to evaluate the clinical significance of currently used antidiabetic drugs and, in addition, the possible role of other drugs (antihypertensives, lipid lowering agents, anti-obesity drugs) should also be investigated in order to identify the optimal primary prevention policy of type 2 diabetes.

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The physiological functions of dietary fiber and its role in health promotion and risk reduction of some chronic diseases has been well documented. In the present investigation, the effect of three dietary fiber sources, oats (OA), barley (BA) and psyllium husk (PH) on glucose adsorption, diffusion and starch hydrolysis were studied using in vitro techniques by simulating gastrointestinal conditions and compared with the commercial dietary fiber sources wheat bran (WB), acarbose (ACB) and guar gum (GG). The glucose binding capacity of all the samples was higher than WB and ACB at 5 mM concentration. In all the samples, the diffusion of glucose was directly proportional to the time and diffusion rate was significantly lower (p ≤ 0.01) in the system containing various samples compared to control. Glucose dialysis retardation index (GDRI) was 100 for OA, BA and PH at 60 min, at 120 min the maximal GDRI was in PH. Whereas; WB and ACB exhibited maximal GDRI at 180 and 240 min. All of these mechanisms might create a concerted function in lowering the rate of glucose absorption and as a result, decrease the postprandial hyperglycemia.

precose dosing

We have a limited understanding of the details of molecular recognition of carbohydrates by proteins, which is critical to a multitude of biological processes. Furthermore, carbohydrate-modifying proteins such as glycosyl hydrolases and phosphorylases are of growing importance as potential drug targets. Interactions between proteins and carbohydrates have complex thermodynamics, and in general the specific positioning of only a few hydroxyl groups determines their binding affinities. A thorough understanding of both carbohydrate and protein structures is thus essential to predict these interactions. An atomic-level view of carbohydrate recognition through structures of carbohydrate-active enzymes complexed with transition-state inhibitors reveals some of the distinctive molecular features unique to protein-carbohydrate complexes. However, the inherent flexibility of carbohydrates and their often water-mediated hydrogen bonding to proteins makes simulation of their complexes difficult. Nonetheless, recent developments such as the parameterization of specific force fields and docking scoring functions have greatly improved our ability to predict protein-carbohydrate interactions. We review protein-carbohydrate complexes having defined molecular requirements for specific carbohydrate recognition by proteins, providing an overview of the different computational techniques available to model them.

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Our findings suggest chlorpropamide, glipizide, glyburide, insulin, and rosiglitazone increased severity-adjusted mortality in veterans with type 2 diabetes. A decision aid that could optimize selection of hypoglycemic medications based on patients' comorbidities might increase patients' survival.

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Inhibitors of intestinal alpha-glucosidases are used therapeutically to treat type 2 diabetes mellitus. Bacteria such as Actinoplanes sp. naturally produce potent alpha-glucosidase inhibitor compounds, including the most widely available drug acarbose. It is not known whether lactic acid bacteria (LAB) colonising the human gut possess inhibitory potential against glucosidases. Hence, the study was undertaken to screen LABs having inherent alpha- and beta-glucosidase inhibitory potential.

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A simple and rapid CZE method was established for the simultaneous determination of valienamine, acarbose and validamycin A, using a 20-kV CZE with the detection wavelength of 193 nm and 50 mM phosphoric acid-20 mM Tris (pH 5.3) as a running buffer. The calibration curves of valienamine, acarbose, and validamycin A showed a good linear relationship at a concentration range of 5-1000 microg/mL. The detection limits of valienamine, acarbose, and validamycin A were 0.3, 0.6, and 0.6 microg/mL, respectively, and the average recoveries of each of the above were 99.9, 99.5, and 100.3%. The method has been successfully applied for simultaneous determination of substrate and product in the process of preparation of valienamine.

precose user reviews

The α-glucosidase inhibitory effects of five bioactive components, namely 1-deoxynojirimycin, cyanidin-3-glucoside, cyanidin-3-rutinoside, resveratrol and oxyresveratrol contained in mulberry (Morus, Moraceae) plants have been compared. Spectroscopy methods were employed to compare their α-glucosidase inhibitory mechanisms. The results revealed that 1-deoxynojirimycin (competitive), resveratrol and oxyresveratrol (noncompetitive) were stronger inhibitors than acarbose, while cyanidin-3-glucoside and cyanidin-3-rutinoside (mix competitive and noncompetitive) showed modest activities. 1-Deoxynojirimycin, resveratrol and oxyresveratrol could quench the fluorescence spectra statically by forming stable complexes, while the quenching of cyanidin-3-rutinoside and cyanidin-3-glucoside belonged to dynamic quenching by the collision of molecules. The interactions between ligands and α-glucosidase were mainly driven by hydrophobic force, or hydrogen bonding consequently induced conformational changes and reduced surface hydrophobicity. Docking results suggested that they could bind to α-glucosidase at different sites. This work provides useful information for the understanding of the ligands-α-glucosidase interactions and identifies oxyresveratrol as a potent α-glucosidase inhibitor.

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The diabetic patients had a significantly higher probability of receiving potential detection examinations (6.38% vs. 5.83%, P<0.0001). After multivariable-adjustment, the OR (95% CI) for diabetes status was 0.816 (0.652-1.021); and for diabetes duration <1 year, 1-3 years, 3-5 years and ≥ 5 years vs. non-diabetes was 0.071 (0.010-0.507), 0.450 (0.250-0.813), 0.374 (0.203-0.689) and 1.159 (0.914-1.470), respectively. Among the anti-diabetic agents, only sulfonylurea was significantly associated with thyroid cancer, OR (95% CI): 1.882 (1.202-2.947). The OR (95% CI) for insulin, metformin, acarbose, pioglitazone and rosiglitazone was 1.701 (0.860-3.364), 0.696 (0.419-1.155), 0.581 (0.202-1.674), 0.522 (0.069-3.926) and 0.669 (0.230-1.948), respectively. Furthermore, patients with benign thyroid disease or other cancer, living in Kao-Ping/Eastern regions, or receiving potential detection examinations might have a significantly higher risk; and male sex, hypertension, dyslipidemia, chronic obstructive pulmonary disease, vascular complications or use of statin, aspirin or non-steroidal anti-inflammatory drugs might be associated with a significantly lower risk.

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Acarbose use.

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Postprandial glucose and insulin levels were similar in the 3 groups. Postprandial endothelial dysfunction was similar in the 3 groups before treatment. After 12 weeks of intervention, postprandial FMD was significantly improved in the acarbose group compared with the control group (6.8 +/- 1.3% vs 5.2 +/- 1.1%, p = 0.0022). Area under the curve (AUC) for insulin response was significantly increased in the nateglinide and control groups; however, no significant change was observed in the acarbose group.

precose patient review

The present investigation was undertaken to explore the possible antiparasitic potential and α-glucosidase inhibition by compounds derived from the Panamanian mangrove Pelliciera rhizophorae. Bioassay-guided fractionation of the crude extract led to the isolation of ten chemical compounds: α-amyrine (1), β-amyrine (2), ursolic acid (3), oleanolic acid (4), betulinic acid (5), brugierol (6) iso-brugierol (7), kaempferol (8), quercetin (9), and quercetrin (10). The structures of these compounds were established by spectroscopic analyses including APCI-HR-MS and NMR. Compounds 4 (IC50 = 5.3 µM), 8 (IC50 = 22.9 µM) and 10 (IC50 = 3.4 µM) showed selective antiparasitic activity against Leishmania donovani, while compounds 1 (IC50 = 19.0 µM) and 5 (IC50 = 18.0 µM) exhibited selectivity against Tripanosoma cruzi and Plasmodium falciparum, respectively. Moreover, compounds 1-5 inhibited α-glucosidase enzyme in a concentration-dependent manner with IC50 values of 1.45, 0.02, 1.08, 0.98 and 2.37 µM, respectively. Their inhibitory activity was higher than that of antidiabetic drug acarbose (IC50 217.7 µM), used as a positive control. Kinetic analysis established that the five compounds acted as competitive inhibitors. Docking analysis predicted that all triterpenes bind at the same site that acarbose in the human intestinal α-glucosidase (PDB: 3TOP).

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Between Feb 7, 2011, and Nov 7, 2012, 402 patients were enrolled (199 in the premix group, 203 in the basal-bolus group) and 399 were included in the primary analysis (197 in the premix group, 202 in the basal-bolus group). HbA1c change at week 24 was -1.1% for both treatment groups. The least squares mean difference between groups in HbA1c change from baseline was 0% (95% CI -0.1 to 0.2). Insulin lispro mix was non-inferior to basal-bolus therapy based on the prespecified margin of 0.4%. The frequency of adverse events, and the incidences and 30-day rates of nocturnal and overall hypoglycaemia were comparable between groups. No severe hypoglycaemia was reported.

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To evaluate the effect of acarbose on glycemic control and glycemic variability, using a continuous glucose-monitoring system, in patients with type 2 diabetes mellitus who were not well controlled on metformin and vildagliptin therapy.

precose 25 mg

Pharmacological intervention with a variety of agents (thiazolidinediones, metformin, acarbose, glucagon-like peptide-1 analogs) consistently reduces the rate of conversion of IGT to T2DM.

precose 100 mg

Acarbose reduced excessive blood glucose fluctuations.

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Terminalia sericea extract (IC(50)=92mg/ml) exhibited a considerable alpha-glucosidase inhibitory activity which was better than acarbose (IC(50)=131mg/ml) under our assay conditions. In the reverse transcriptase assay, T. sericea also showed good inhibitory activity (IC(50)=43mg/ml), which was higher than that of the reference drug, Adriamycin (IC(50)=100mg/ml). The ethyl acetate extract of Elaeodendron transvaalense exhibited the most potent inhibitory activity in both the NF-kappaB and Tat assays with inhibitory activity of 76% and 75% respectively at a concentration of 15mg/ml. The acetone and chloroform extracts of E. transvaalense and Zanthoxylum davyi also showed good activity in the NF-kappaB and Tat assays.

precose dosage

There were significantly more responders in the acarbose-treated group compared with the placebo group (20/24 patients vs. 10/19 patients; p < 0.05). The mean daily insulin dose after 24 weeks of treatment was 16.4 +/- 10.1 IU in the acarbose group and 22.4 +/- 12.2 IU in the placebo group (mean +/- s.d.; p < 0.07). Postprandial increases in blood glucose, insulin and C-peptide were consistently lower in the acarbose-treated group than in the placebo group. For example, the mean increase in 2-h postprandial serum insulin remained almost unchanged in the acarbose group at the end of 24 weeks of treatment compared to an increase to 43 +/- 29 microU/ml (mean +/- s.d.) at the end of the study period for the placebo group.

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buy precose online 2016-08-12

During the last few decades, the prevalence of obesity in the western world has dramatically increased with epidemic proportions. Hand precose buy in hand with this statistic, the incidences of obesity-linked diseases such as diabetes are increasing with pandemic rate. The search for novel drugs and nutritional intervention approaches for obesity is now of significant importance.

precose buy 2017-11-26

Combination precose buy therapy of basal insulin and acarbose in patients with type 2 diabetes improved glucose control, and had no drug-specific safety concerns, suggesting that the treatment might benefit individuals who cannot control blood glucose with basal insulin alone.

buy precose online 2016-08-16

The inhibitory activity on pancreatic α-amylase by cyanidin-3-rutinoside was examined in vitro. The IC₅₀ value of cyanidin-3-rutinoside against pancreatic α-amylase was 24.4 ± 0.1 μM. The kinetic analysis revealed that pancreatic α-amylase was inhibited by cyanidin-3-rutinoside in a non-competitive manner. The additive inhibition of a combination of cyanidin-3-rutinoside with acarbose against pancreatic α-amylase was also found. These results provide the Noroxin Renal Dosing first evidence for the effect of cyanidin-3-rutinoside in a retarded absorption of carbohydrates by inhibition of pancreatic α-amylase which may be useful as a potential inhibitor for prevention and treatment of diabetes mellitus.

precose buy 2017-08-09

There was a notable increase in the consumption of insulins and OAAs. Although the tendency in the consumption differs from that expected according to consensus agreements, qualitative changes were seen, suggesting an improvement in prescription habits. The appearance of mechanized injection systems for insulin and Neem Toothpaste Review of acarbose have clearly modified prescription habits.

buy precose online 2016-03-08

Treatment with acarbose was associated with a mean reduction in postprandial glucose levels (60 min after Levitra Tab 20mg the administration of a test meal) of 59 mg/dl and a mean reduction in HbA1c levels of 0.48%. There was no difference in the incidence of hypoglycemia between treatment groups. Gastrointestinal events, including flatulence, diarrhea, and abdominal pain, were reported more frequently in acarbose-treated patients than in placebo-treated patients.

precose buy 2015-03-07

Acarbose, an alpha-glucosidase inhibitor, delays starch digestion and inhibits intestinal sucrase and maltase activity. Twenty-eight insulin dependent diabetics were given Acarbose (3 x 100 mg daily) over a two month period, preceded and followed by a two month placebo period. Acarbose reduced post-breakfast and post-dinner blood glucose values by 25% (p less than 0.001) and 24% (p less than 0.05) respectively. It also significantly reduced mean daily blood glucose by 18% (p less than 0.05) and mean amplitude of glycaemic excursions from Casodex Cost 8.0 +/- 0.6 to 5.5 +/- 0.4 mmol/l (p less than 0.0005). Weight did not change significantly. Daily caloric and carbohydrate intake remained constant throughout the study while insulin requirements decreased slightly but significantly. Out of the 28 patients, 18 had absent while ten had slight residual B cell function as assessed by plasma C-peptide measurements. Treatment with Acarbose did not significantly affect residual B cell function. The beneficial effect of Acarbose on blood glucose control was seen in patients both with and without residual B cell secretion. The major side-effect was flatulence which was never severe enough to interrupt treatment, but led to a 50% reduction of the dose in one patient. It is concluded that Acarbose represents a useful additional means of improving metabolic control in insulin dependent diabetics.

buy precose online 2016-12-20

The majority of the 1558 enrolled patients received acarbose 50 mg three times daily, had previously been treated with a sulphonylurea and/ Diflucan Uti Dose or biguanide, and were observed for a mean period of 13.9 weeks. Most patients (91.8%) received concomitant oral antihyperglycaemic agents. Acarbose reduced fasting blood glucose concentrations by 32.0 mg/dL and 2-hour postprandial blood glucose levels by 52.2 mg/dL. HbA(1c) was reduced by 1.0% from 9.9% to 8.9%, and bodyweight remained stable. The attending physicians assessed that acarbose was associated with 'very good' or 'good' general efficacy in 46.0% of patients, 'very good' or 'good' tolerability in 60.6% and 'very good' or 'good' patient acceptance in 63.4%. These ratings were higher for patients receiving acarbose monotherapy compared with those taking other antihyperglycaemic therapies in addition to acarbose. Only 2.0% of all patients experienced drug-related adverse events.

precose buy 2017-10-19

Metformin is the only first-line oral hypoglycaemic drug for type 2 diabetes recommended by international guidelines with proven Triphala Juice Online efficacy, safety, and cost-effectiveness. However, little information exists about its use in Asian populations. We aimed to ascertain the effectiveness of the α-glucosidase inhibitor acarbose, extensively adopted in China, compared with metformin as the alternative initial therapy for newly diagnosed type 2 diabetes.

buy precose online 2015-06-29

A total of 657 type 2 diabetes patients who were randomly assigned to 48 weeks of therapy with either acarbose or metformin in the MARCH trial were divided into two groups based upon their hemoglobin A1c (HbA1c) levels at the end of follow-up: HbA1c <7% (<53 mmol/mol) and ≥7% (≥53  Aricept 23 Generic mmol/mol). Univariate, multivariate, and stepwise linear regression analyses were applied to identify the factors associated with treatment efficacy.

precose buy 2016-03-18

Among 43,390 drug exposure intervals for 25,690 patients who had a mean follow-up period of 2.5 years, 1,409 patients developed heart failure. Heart failure occurred most frequently in SU monotherapy exposure. After adjusting for duration of diabetes, the timing and order of treatments received, and known risk factors for heart failure, we found no differential effects among type-specific therapies. Patients with any drug use within the first year after diabetes diagnosis had a 4.75-fold higher risk (hazard ratio) for heart failure than those with drug-free status Desyrel 300 Mg but had no increased risk during subsequent years.

buy precose online 2015-08-07

Improved blood glucose control was shown to reduce the number of complications, mainly by reducing the effect of microangiopathy. There was however no reduction in the number of diabetes-related deaths nor in the risk of myocardial Duphaston Online Usa infarction or sudden death.

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Overall, the non-competitive and uncompetitive mechanism of action of corn silk extract is due to its inhibitory effects on α-amylase and α-glucosidase, respectively. Consequently, this will reduce the rate of starch hydrolysis, enhance palliated glucose levels, and thus, lending credence to hypoglycaemic candidature of corn silk.

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Tyramine derivatives 3-27 were synthesized by using conventional and environmental friendly ultrasonic techniques. These derivatives were then evaluated for the first time for their α-glucosidase (Sources: Saccharomyces cerevisiae and mammalian rat-intestinal acetone powder) inhibitory activity by using in vitro mechanism-based biochemical assays. Compounds 7, 14, 20, 21 and 26 were found to be more active (IC50 = 49.7 ± 0.4, 318.8 ± 3.7, 23.5 ± 0.9, 302.0 ± 7.3 and 230.7 ± 4.0 μM, respectively) than the standard drug, acarbose (IC50 = 840.0 ± 1.73 μM (observed) and 780 ± 0.028 μM (reported)) against α-glucosidase obtained from Saccharomyces cerevisiae. Kinetic studies were carried out on the most active members of the series in order to determine their mode of inhibition and dissociation constants. Compounds 7, 20 and 26 were found to be the competitive inhibitors of α-glucosidase. These compounds were also screened for their protein antiglycation, and dipeptidyl peptidase-IV (DPP-IV) inhibitory activities. Only compounds 20, 22 and 27 showed weak antiglycation activity with IC50 values 505.27 ± 5.95, 581.87 ± 5.50 and 440.58 ± 2.74 μM, respectively. All the compounds were found to be inactive against DDP-IV enzyme. Inhibition of α-glucosidase, DPP-IV enzymes and glycation of proteins are valid targets for the discovery of antidiabetic drugs. Cytotoxicity of compounds 3-27 was also evaluated by using mouse fibroblast 3T3 cell lines. All the compounds were found to be noncytotoxic. The current study describes the synthesis α-glucosidase inhibitory activity of derivatives, based on a natural product tyramine template. The compounds reported here may serve as the starting point for the design and development of novel α-glucosidase inhibitors as antidiabetic agents.

precose buy 2016-04-01

The inhibitory activity on intestinal α-glucosidase by cyanidin-3-rutinoside was examined in vitro and in vivo. The IC(50) values of cyanidin-3-rutinoside against intestinal maltase, and sucrase were 2,323 ± 14.8 and 250.2 ± 8.1 µM, respectively. The kinetic analysis revealed that intestinal sucrase was inhibited by cyanidin-3-rutinoside in a mixed-type manner. The synergistic inhibition also found in combination of cyanidin-3-rutinoside with acarbose against intestinal maltase and sucrase. The oral administration of cyanidin-3-rutinoside (100 and 300 mg/kg) plus maltose or sucrose to normal rats, postprandial plasma glucose was markedly suppressed at 30-90 min after loading. Furthermore, the normal rats treated with acarbose and cyanidin-3-rutinoside (30 mg/kg) showed greater reduction of postprandial plasma glucose than the group treated with acarbose alone. These results suggest that cyanidin-3-rutinoside retards absorption of carbohydrates by inhibition of α-glucosidase which may be useful as a potential inhibitor for prevention and treatment of diabetes mellitus.

buy precose online 2016-12-13

Inadequate control of hyperglycaemia, poor metabolic profiles and diabetic complications were common challenges for long-term diabetes management in Chinese patients with type 2 diabetes mellitus.

precose buy 2017-11-03

Nocturnal hypoglycemia is common in aggressively treated type 1 diabetes. Bedtime administration of a conventional snack or of uncooked cornstarch does not prevent it. That of terbutaline prevents nocturnal hypoglycemia but causes hyperglycemia the following morning. The efficacy of a lower dose of terbutaline remains to be determined.

buy precose online 2017-06-25

Mammalian amylases harbor a flexible, glycine-rich loop 304GHGAGGA(310), which becomes ordered upon oligosaccharide binding and moves in toward the substrate. In order to probe the role of this loop in catalysis, a deletion mutant lacking residues 306-310 (Delta306) was generated. Kinetic studies showed that Delta306 exhibited: (1) a reduction (>200-fold) in the specific activity using starch as a substrate; (2) a reduction in k(cat) for maltopentaose and maltoheptaose as substrates; and (3) a twofold increase in K(m) (maltopentaose as substrate) compared to the wild-type (rHSAmy). More cleavage sites were observed for the mutant than for rHSAmy, suggesting that the mutant exhibits additional productive binding modes. Further insight into its role is obtained from the crystal structures of the two enzymes soaked with acarbose, a transition-state analog. Both enzymes modify acarbose upon binding through hydrolysis, condensation or transglycosylation reactions. Electron density corresponding to six and seven fully occupied subsites in the active site of rHSAmy and Delta306, respectively, were observed. Comparison of the crystal structures showed that: (1) the hydrophobic cover provided by the mobile loop for the subsites at the reducing end of the rHSAmy complex is notably absent in the mutant; (2) minimal changes in the protein-ligand interactions around subsites S1 and S1', where the cleavage would occur; (3) a well-positioned water molecule in the mutant provides a hydrogen bond interaction similar to that provided by the His305 in rHSAmy complex; (4) the active site-bound oligosaccharides exhibit minimal conformational differences between the two enzymes. Collectively, while the kinetic data suggest that the mobile loop may be involved in assisting the catalysis during the transition state, crystallographic data suggest that the loop may play a role in the release of the product(s) from the active site.

precose buy 2017-03-07

Several epidemiological studies have shown an association between postprandial hyperglycemia and mortality from cardiovascular disease. Postprandial hyperglycemia is frequently associated with visceral obesity which plays a key role in metabolic abnormalities such as dyslipidemia and hypertension. Inhibitors of alpha-glucosidase and nateglinide have beneficial effects on the metabolic syndrome associated with visceral obesity. Voglibose in combination with diet therapy reduces visceral fat deposition and ameliorates insulin resistance. Acarbose slightly reduces blood pressure of hypertensive diabetic patients. Nateglinide, a rapidly acting insulin secretagogue, lowers postprandial glucose levels without significant body weight gain. These drugs may protect pancreatic beta-cells from postprandial glucose toxicity and prevent the progression of diabetes.

buy precose online 2015-06-05

Suboptimal glycemic control is a common situation in diabetes, regardless of the wide range of drugs available to reach glycemic targets. Basic research in diabetes is endeavoring to identify new actives working as insulin savers, use of which could delay the introduction of injectable insulin or reduce the insulin dose needed. Commonly available as a nutraceutical, berberine is a potential candidate.

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A recent retrospective meta-analysis of cardiovascular events from long-term studies with acarbose in type 2 diabetes showed that treatment was associated with a significant reduction in the risk of cardiovascular events, supporting the hypothesis that postprandial hyperglycemia is a risk factor for cardiovascular disease. The aim of the present study was to assess the cost-effectiveness of acarbose, given in addition to existing treatments, in type 2 diabetes patients, based on these findings, in the German setting.

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Of the fully competitive inhibitors of small intestinal sucrase investigated in this or in other papers, acarbose, nojirimycin, and deoxynojirimycin (Fig. 2) have the highest affinity for the enzyme, their Ki values being in the 10(-7)-10(-8) M range. Furthermore, thier interaction with the enzyme is slow, the steady state being reached in their presence in a matter of minutes. Their overall "on" and "off" constants are small, which indicates that a conformational change accompanies the interaction of these substances with the active site of intestinal sucrase. The structure of these inhibitors, as well as the pH dependence of their Ki values, agrees with and allows additions to be made to the catalytic mechanism earlier suggested for this enzyme (Cogoli, A., and Semenza, G. (1975) J. Biol. Chem. 250, 7802-7809). None of these inhibitors of sucrase has any sizeable effect on the small intestinal Na+-dependent D-glucose transport system.

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To review the evidence for use of acarbose in the management of polycystic ovary syndrome (PCOS).

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This trial assessed the feasibility, safety and potential to induce remission of a short-term intensive metabolic strategy.

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Sixteen patients with type 2 diabetes poorly controlled by glibenclamide (7.5-10.0 mg/day) were treated with acarbose (100 mg tds) for one week and the effect on the blood glucose profile, 24-hour urinary glucose excretion, plasma fructosamine, and plasma 1,5-anhydro-D-glucitol (1,5-AG) level was determined. The blood glucose profile was more stable and levels were lower during acarbose administration. In some patients, this improvement was maintained after discontinuing acarbose. The M-value, an indicator of blood glucose fluctuations, decreased significantly from 33.2 +/- 3.0 (mean +/- SEM) in the run-in period to 13.4 +/- 2.4 during acarbose therapy (P < 0.001), and rose again to 26.5 +/- 4.4 (P < 0.001) in the follow-up period. The 24-hour urinary glucose excretion and plasma fructosamine decreased similarly (P < 0.001 and P < 0.01, respectively) during and after acarbose therapy. Plasma 1,5-AG levels did not change significantly during acarbose therapy, but increased markedly afterwards (from 19.3 +/- 3.1 mumol 1(-1) to 25.0) +/- 3.1 mumol l-1, P < 0.001). Plasma 1,5-AG levels were significantly correlated with urinary glucose excretion one week earlier (r = 0.513, P < 0.006). These findings suggest that acarbose may improve glycemic control in type 2 diabetic patients poorly controlled by sulfonylurea therapy and that plasma 1,5-AG might be used as a marker of glycemic control cooperating with other markers such as fructosamine and urinary glucose determination for monitoring the short-term response to antidiabetic therapy.

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Whole-body insulin sensitivity increased in both groups (mean [95% CI]) (H-RISK vs L-RISK: 0.8 [0.2, 1.4] vs 1.0 [0.4, 1.7]mg kg(-1) min(-1), p = 0.59), while body weight decreased (-4.8% [-6.1%, -3.5%] vs -4.6% [-6.0%, -3.3%], respectively). Hepatic insulin sensitivity remained unchanged, whereas hepatocellular lipid content fell in both groups (-7.0% [-9.6%, -4.5%] vs -6.7% [-9.5%, -3.9%]). Subcutaneous fat mass (-1,553 [-2,767, -340] cm(3) vs -751 [-2,047; 546] cm(3), respectively) visceral fat mass (-206 [-783, 371] cm(3) vs -241 [-856, 373] cm(3), respectively) and muscle fat content (-0.09% [-0.16%, -0.02%] vs -0.02% [-0.10%, 0.05%], respectively) decreased similarly. Insulin secretion remained unchanged, while the proinflammatory marker IL-18 decreased only after the L-RISK diet.

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The present studies were undertaken to determine the effect of various carbohydrates on sympathetic nervous system (SNS) activity. Tritiated-norepinephrine (3H-NE) turnover was measured in heart and interscapular brown adipose tissue (IBAT) of rats fed either chow or chow plus 50% caloric supplements of fructose, sucrose, dextrose, or corn starch. Additional studies were performed to examine whether absorption of carbohydrate plays a role in the SNS response, and to determine whether sweet taste in the form of artificial sweeteners may influence SNS activity. After five to ten days on the respective diets, 3H-NE turnover was increased to a similar extent by all carbohydrates tested (from 38% to 160% greater than controls in different studies). Addition of acarbose (which impairs sucrose absorption) to a sucrose-supplemented diet abolished the SNS stimulatory response, whereas cholestyramine (a drug that blocks fat absorption) had no effect. Finally, the addition of saccharin or aspartame to a chow diet failed to alter SNS activity. Thus, caloric supplementation with several carbohydrates, in addition to sucrose, stimulates both cardiac and IBAT SNS activity, absorption of carbohydrate is required for this effect, and noncaloric sugar substitutes do not alter SNS function.

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The present investigation was undertaken to explore the possible antiparasitic potential and α-glucosidase inhibition by compounds derived from the Panamanian mangrove Pelliciera rhizophorae. Bioassay-guided fractionation of the crude extract led to the isolation of ten chemical compounds: α-amyrine (1), β-amyrine (2), ursolic acid (3), oleanolic acid (4), betulinic acid (5), brugierol (6) iso-brugierol (7), kaempferol (8), quercetin (9), and quercetrin (10). The structures of these compounds were established by spectroscopic analyses including APCI-HR-MS and NMR. Compounds 4 (IC50 = 5.3 µM), 8 (IC50 = 22.9 µM) and 10 (IC50 = 3.4 µM) showed selective antiparasitic activity against Leishmania donovani, while compounds 1 (IC50 = 19.0 µM) and 5 (IC50 = 18.0 µM) exhibited selectivity against Tripanosoma cruzi and Plasmodium falciparum, respectively. Moreover, compounds 1-5 inhibited α-glucosidase enzyme in a concentration-dependent manner with IC50 values of 1.45, 0.02, 1.08, 0.98 and 2.37 µM, respectively. Their inhibitory activity was higher than that of antidiabetic drug acarbose (IC50 217.7 µM), used as a positive control. Kinetic analysis established that the five compounds acted as competitive inhibitors. Docking analysis predicted that all triterpenes bind at the same site that acarbose in the human intestinal α-glucosidase (PDB: 3TOP).

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A series of α-glucosidase inhibitors with the oleanolic acid core and different cinnamic amide ligands were designed and synthesized. Their preliminary structure-activity relationships were analyzed. In general, the compounds with 3,28-disubstituted oleanolic acid exhibited stronger activity than those 28-monosubstituted analogues, and variation of cinnamic amide substitution significantly affected α-glucosidase inhibition activities. Most of the compounds showed potent inhibitory activity against α-glucosidase with much greater efficacy than a typical α-glucosidase inhibitor, acarbose.

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The usefulness of applying an integrated LC-NMR and LC-MS approach to acarbose bulk drug impurity profiling is demonstrated. LC-MS and LC-NMR methodologies were employed for the online separation and structural elucidation of a final drug product. Combining data provided by the stop-flow LC-NMR and LC-MS experiments made it possible to identify the main components present in the acarbose sample. Spectral analysis revealed that A and B were known impurities while C was an unknown compound. LC-MS and LC-NMR analyses revealed that C was a pentasaccharide differing from the acarbose in number and nature of sugar subunits in the molecule. It was subsequently isolated and its structure was confirmed by the offline 1- and 2-D NMR experiments, and atom assignment was made.

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A total of 108 drug-naïve patients with newly diagnosed T2DM, whose hemoglobin A1c (HbA1c) was between 7% and 10% and body mass index was greater than 24 kg/m(2), were enrolled in the First People's Hospital and Municipal Central Hospital of Xiangtan City, Xiangtan, China, from 1 February 2010 to 1 August 2011. Patients were randomly assigned to acarbose (100 mg three times a day) and metformin (1.5 g/day) groups for a predictive follow-up period of 24 weeks. Plasma glucose, insulin, and glucagons at 0, 0.5, and 2 hours after a standardized meal, and HbA1c were measured at baseline and 24 weeks.

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The metabolic syndrome is strongly associated with insulin resistance and has been recognized as a cluster of risk factors for cardiovascular diseases such as visceral obesity, hypertension, and diabetes. There is a growing body of evidence to show that nonalcoholic steatohepatitis (NASH) is the hepatic manifestation of insulin resistant patients with the metabolic syndrome. Indeed, insulin resistance increases adipocyte lipolysis and subsequently elevates circulating free fatty acids, thus stimulating the accumulation of fatty acids in the liver (hepatic steatosis). Fatty acids elicit reactive oxygen species generation, thereby promoting disease progression to NASH by both lipid peroxidation and inflammatory cytokine production. Postprandial hyperglycemia, one of the characteristic features of insulin resistance, also induces oxidative stress generation, being involved in dysfunction of pancreatic beta cells and vascular wall cells in the metabolic syndrome. Recently, STOP-NIDDM trial revealed that acarbose (Glucobay), an alpha-glucosidase inhibitor, improved postprandial hyperglycemia and subsequently reduced the risk of development of type 2 diabetes and newly diagnosed hypertension in patients with impaired glucose tolerance. In this study, acarbose treatment was also found to reduce body mass index and waist circumference in these patients. Furthermore, a meta-analysis of seven long-term studies has also shown that intervention with acarbose improved triglyceride levels, body weight and systolic blood pressure and subsequently prevented myocardial infarction in type 2 diabetic patients. Since acarbose improves postprandial hyperglycemia by delaying the release of glucose from complex carbohydrates in the absence of an increase in insulin secretion, the beneficial aspects of acarbose could be ascribed to improvement of insulin sensitivity in these patients. Given the pathological link between NASH and insulin resistance, we would like to hypothesize here that acarbose may become a promising therapeutic strategy for the treatment of patients with NASH. Does acarbose treatment improve steatohepatitis histologically? Is the extent of histological improvement by acarbose parallel to that of insulin sensitivity in these patients? Large clinical trials will provide us with more definite information whether acarbose treatment can improve insulin sensitivity and resultantly reduce the risk of progression of liver diseases in patients with NASH.

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Differential excretion of intact disaccharide, expressed as ratios of lactulose to appropriate hydrolysable disaccharides in urine collected following combined ingestion, has been investigated in healthy volunteers with drug induced alpha-glucosidase inhibition, in subjects with primary hypolactasia, and patients with coeliac disease.

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This article focuses on those patients where particular agents should not be used: i.e. 'when not to use what'.

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The efficacy and, as the main topic, the tolerability were investigated from an international clinical data pool on placebo-controlled randomized multicenter studies of 5 different groups of indications. The therapeutic areas analyzed were neuropsychiatry (nimodipine, ipsapirone), cardiology (nisoldipine), metabolism (acarbose) and gastroenterology (hydrotalcit).

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To review currently available drug therapies and management strategies for type 2 diabetes, and optimal insulin treatment regimens for type 1 diabetes.

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A major barrier to the widespread clinical use of an alpha-glucosidase inhibitor such as Acarbose, is the unpleasant gastrointestinal symptoms of carbohydrate malabsorption associated with its use. Acarbose is usually administered as a tablet and eaten with the first mouthful of the meal, making its uniform distribution through the meal unlikely. In the present study, Acarbose was crushed to a powder and mixed through a test meal before it was consumed. Six healthy young men consumed test meals containing 75 g carbohydrate either as whole brown rice or as ground brown rice. When Acarbose was uniformly mixed through a ground rice meal prior to digestion it produced dose-dependent reductions in the postprandial glucose, insulin and GIP responses which were evident at doses as low as 12.5 mg. The responses to whole brown rice were intermediate between those to 12.5 and 25 mg Acarbose in ground brown rice. In tablet form Acarbose was only one quarter as effective in flattening the post prandial glucose and insulin responses as it was in powder form. These results highlight the importance of uniform distribution of Acarbose through a carbohydrate meal in order to achieve maximum effectiveness in delaying digestion and absorption and yet not promoting carbohydrate malabsorption.