New horizons in diabetes therapy--alpha glucosidase inhibitors (original) (raw)
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Low-dose acarbose does not delay digestion of starch but reduces its bioavailability
Diabetic Medicine, 2007
Aims Slowly digestible starch is associated with beneficial health effects. The glucose-lowering drug acarbose has the potential to retard starch digestion since it inhibits α -amylase and α -glucosidases. We tested the hypothesis that a low dose of acarbose delays the rate of digestion of rapidly digestible starch without reducing its bioavailability and thereby increasing resistant starch flux into the colon.
Acarbose: its role in the treatment of diabetes mellitus
The Annals of …, 1996
To review the role of acarbose in the pharmacotherapy of diabetes mellitus. Searching MEDLINE was searched for articles and reviews (no search strategy or restrictions provided), and Bayer Pharmaceuticals (drug manufacturer) was contacted. Study selection Study designs of evaluations included in the review Clinical trials adhering to the following criteria: (1) randomised, double-blind, placebo-controlled, parallel group study design; (2) minimum of 25 patients enrolled per treatment arm; (3) treatment duration of 90 days or more; and (4) adherence to Food and Drug Administration Good Clinical Practice guidelines. Specific interventions included in the review Acarbose (alpha-glucosidase inhibitor), tolbutamide, combined acarbose and tolbutamide, metformin, sulfonylurea, insulin and placebo. Participants included in the review Patients with non insulin-dependent diabetes mellitus (NIDDM) were included. Outcomes assessed in the review The outcomes assessed were haemoglobin A1c levels, fasting blood glucose levels, postprandial blood glucose (PPG) levels, postprandial triglyceride, and adverse effects (weight gain). How were decisions on the relevance of primary studies made? The authors do not state how the papers were selected for the review, or how many of the authors performed the selection. How were differences between studies investigated? Descriptions of characteristics of the studies, such as drug treatment, dosage regimen, duration of the phases of the study and patient characteristics, were provided. No measure of heterogeneity was presented.
The Effect of Acarbose on Insulin Sensitivity in Subjects With Impaired Glucose Tolerance
Diabetes Care, 1996
OBJECTIVE To study the effect of acarbose, an α-glucosidase inhibitor, on postprandial plasma glucose and insulin and insulin sensitivity in subjects with impaired glucose tolerance (IGT). RESEARCH DESIGN AND METHODS Subjects with IGT were randomly treated in a double-blind fashion with placebo (n = 10) or acarbose (n = 8) at 100 mg t.i.d. for 4 months. All subjects were submitted before randomization and at the end of the study to a standardized breakfast and a 12-h daytime plasma glucose and plasma insulin profile, and insulin sensitivity was measured as steady-state plasma glucose (SSPG) using the insulin suppression test. RESULTS While placebo had no effect on postprandial plasma glucose and plasma insulin incremental area under the curve (AUC) (3.03 ± 0.5 vs. 3.76 ± 0.6 mmol·h−1 · l−1, P = NS; 1,488 ± 229 vs. 1,609 ± 253 pmol · h−1 · l−1, P = NS), acarbose resulted in a significant reduction for both glucose (1.44 ± 0.3 vs. 4.45 ± 0.9 mmol · h−1 · l−1, P = 0.002) and insulin (6...
REVIEW ON ROLE OF NATURAL ΑLPHA-GLUCOSIDASE INHIBITORS FOR MANAGEMENT OF DIABETES MELLITUS
International Journal of Biomedical Research, 2011
Diabetes, a state of improperly regulated homeostasis of carbohydrate and lipid metabolism is one of the major killers in recent times. Most prevalent form of diabetes is non insulin dependent diabetes mellitus (NIDDM/type II). Rapid hydrolysis of starch mediated by pancreatic α-amylase and α-glucosidases followed by glucose uptake at intestine results in sudden rise in blood glucose levels, causing hyperglycemia in type II diabetes patients. Alpha-glucosidase inhibitors act as competitive inhibitors of enzymes needed to digest carbohydrates: specifically alpha-glucosidase enzymes in the brush border of the small intestines. Inhibition of these enzyme systems reduces the rate of digestion of carbohydrates. Less glucose is absorbed because the carbohydrates are not broken down into glucose molecules. Natural alpha-glucosidase inhibitors such as Acarbose and Miglitol used for management of diabetes widely, but they are associated with side effects, in this review search for more natural alpha-glucosidase inhibitors are discussed which are safer as compared to insulin and other oral hypoglycaemic drugs.
Protocols, 1996
Analysis 1.1. Comparison 1 Acarbose versus placebo, Outcome 1 Incidence of type 2 diabetes mellitus.. .. .. Analysis 1.2. Comparison 1 Acarbose versus placebo, Outcome 2 Occurrence of death (total).. .. .. .. . Analysis 1.3. Comparison 1 Acarbose versus placebo, Outcome 3 Occurrence of cardiovascular death.. .. .. . Analysis 1.4. Comparison 1 Acarbose versus placebo, Outcome 4 Occurrence of cardiovascular disease (any).. .. Analysis 1.5. Comparison 1 Acarbose versus placebo, Outcome 5 Occurrence of myocardial infarctions.. .. .. Analysis 1.6. Comparison 1 Acarbose versus placebo, Outcome 6 Occurrence of angina pectoris.. .. .. .. Analysis 1.7. Comparison 1 Acarbose versus placebo, Outcome 7 Occurrence of revascularisation procedures.. .. Analysis 1.8. Comparison 1 Acarbose versus placebo, Outcome 8 Occurrence of congestive heart failure.. .. .. Analysis 1.9. Comparison 1 Acarbose versus placebo, Outcome 9 Occurrence of cerebrovascular events.. .. .. Analysis 1.10. Comparison 1 Acarbose versus placebo, Outcome 10 Occurrence of peripheral vascular events.. .. Analysis 1.11. Comparison 1 Acarbose versus placebo, Outcome 11 Change in glycated haemoglobin (%).. .. . Analysis 1.12. Comparison 1 Acarbose versus placebo, Outcome 12 Change in fasting blood glucose (mmol/l).. . Analysis 1.13. Comparison 1 Acarbose versus placebo, Outcome 13 Change in post-load blood glucose (mmol/l).. Analysis 1.14. Comparison 1 Acarbose versus placebo, Outcome 14 Change in total cholesterol (mmol/l).. .. . Analysis 1.15. Comparison 1 Acarbose versus placebo, Outcome 15 Change in HDL-cholesterol (mmol/l).. .. . Analysis 1.16. Comparison 1 Acarbose versus placebo, Outcome 16 Change in LDL-cholesterol (mmol/l).. .. . Analysis 1.17. Comparison 1 Acarbose versus placebo, Outcome 17 Change in triglycerides (mmol/l).. .. .. Analysis 1.18. Comparison 1 Acarbose versus placebo, Outcome 18 Change in fasting insulin levels (pmol/l).. .. Analysis 1.19. Comparison 1 Acarbose versus placebo, Outcome 19 Change in post-load insulin levels (pmol/l).. . Analysis 1.20. Comparison 1 Acarbose versus placebo, Outcome 20 Change in body weight (Kg).. .. .. .. Analysis 1.21. Comparison 1 Acarbose versus placebo, Outcome 21 Change in body mass index (Kg/m2).. .. . Analysis 1.22. Comparison 1 Acarbose versus placebo, Outcome 22 Change in diastolic blood pressure (mmHg).. Analysis 1.23. Comparison 1 Acarbose versus placebo, Outcome 23 Change in systolic blood pressure (mmHg).. . Analysis 1.24. Comparison 1 Acarbose versus placebo, Outcome 24 Occurrence of side effects (total).. .. .. . Analysis 1.25. Comparison 1 Acarbose versus placebo, Outcome 25 Occurrence of gastro-intestinal side-effects.. . Analysis 2.1. Comparison 2 Acarbose versus metformin, Outcome 1 Incidence of type 2 diabetes mellitus.. .. . Analysis 2.2. Comparison 2 Acarbose versus metformin, Outcome 2 Change in fasting blood glucose (mmol/l).. . Analysis 2.3. Comparison 2 Acarbose versus metformin, Outcome 3 Change in post-load blood glucose (mmol/l).. Analysis 2.4. Comparison 2 Acarbose versus metformin, Outcome 4 Change in total cholesterol (mmol/l).. .. . Analysis 2.5. Comparison 2 Acarbose versus metformin, Outcome 5 Change in triglycerides (mmol/l).. .. .. Analysis 2.6. Comparison 2 Acarbose versus metformin, Outcome 6 Change in body mass index (Kg/m2).. .. . Analysis 2.7. Comparison 2 Acarbose versus metformin, Outcome 7 Change in diastolic blood pressure (mmHg).. Analysis 2.8. Comparison 2 Acarbose versus metformin, Outcome 8 Change in systolic blood pressure (mmHg).. . Analysis 3.1. Comparison 3 Acarbose versus diet and exercise, Outcome 1 Incidence of type 2 diabetes mellitus.. . Analysis 3.2. Comparison 3 Acarbose versus diet and exercise, Outcome 2 Change in fasting blood glucose (mmol/l). Analysis 3.3. Comparison 3 Acarbose versus diet and exercise, Outcome 3 Change in post-load blood glucose (mmol/l). Analysis 3.4. Comparison 3 Acarbose versus diet and exercise, Outcome 4 Change in total cholesterol (mmol/l).. .
Acarbose in the treatment of elderly patients with type 2 diabetes
Diabetes Research and Clinical Practice, 2003
To study the effect of acarbose, an a-glucosidase inhibitor, on glycemic control in elderly patients with type 2 diabetes. Methods: Elderly patients with type 2 diabetes treated with diet alone were randomly treated in a double-blind fashion with placebo (n 0/99) or acarbose (n 0/93) for 12 months. Results: After 12 months of therapy, there was a statistically significant difference in the change in glycated haemoglobin (HbA 1c ) ((/0.6%) in the acarbose group versus placebo, as well as in the incremental post-prandial glucose values ((/2.1 mmol h/l) and mean fasting plasma glucose ((/ 0.7 mmol/l). Although there was no effect of acarbose on insulin release, there was a clear effect of acarbose to decrease relative insulin resistance ((/0.8) (HOMA method). In addition, acarbose was generally well tolerated and safe in the elderly; most discontinuations were due to gastrointestinal side effects such as flatulence and diarrhea. There were no
Alpha-glucosidase inhibitors in the early treatment of type 2 diabetes
Vascular health and risk management, 2008
Alpha-glucosidase inhibitors (AGIs) are drugs that inhibit the absorption of carbohydrates from the gut and may be used in the treatment of patients with type 2 diabetes or impaired glucose tolerance. There is currently no evidence that AGIs are beneficial to prevent or delay mortality or micro- or macrovascular complications in type 2 diabetes. Its beneficial effects on glycated hemoglobin are comparable to metformin or thiazolidinediones, and probably slightly inferior to sulphonylurea. In view of the total body of evidence metformin seems to be superior to AGIs. More long-term studies are needed to study the effects of AGIs compared to other drugs. For patient with impaired glucose tolerance AGIs may prevent, delay or mask the occurrence of type 2 diabetes. A possible beneficial effect on cardiovascular events should be confirmed in new studies.
Archives of Medical Science, 2012
Post-prandial hyperglycemia still remains a problem in the management of type 2 diabetes mellitus. Of all available anti-diabetic drugs, α-glucosidase inhibitors seem to be the most effective in reducing post-prandial hyperglycemia. We conducted a review analyzing the clinical efficacy and safety of α-glucosidase inhibitors, both alone and in combination with other anti-diabetic drugs, with respect to glycemic control, inflammation and atherosclerosis. α-Glucosidase inhibitors proved to be effective and safe both in monotherapy and as an addon to other anti-diabetic drugs. Compared to miglitol and voglibose, acarbose seems to have some additive effects such as stabling carotid plaques, and reducing inflammation. Acarbose also proved to reverse impaired glucose tolerance to normal glucose tolerance.
2015
The important therapeutic approach for treating type 2 diabetes mellitus is to decrease the post-prandial glucose levels which could be done by decreasing the absorption of glucose through the inhibition of the carbohydrates-hydrolyzing enzymes such as I±-amylase and I±-glucosidase present in the small intestinal brush border that are responsible for the breakdown of oligosaccharides and disaccharides into monosaccharide’s and suitable for absorption. Inhibition of I±-amylase generally considered as strategy for the treatment of disorders in carbohydrate uptake, such as diabetes and obesity. Among the marketed allopathic preparations carbohydrates-hydrolyzing enzymes Inhibitors like acarbose, voglibose etc delay carbohydrate digestion and prolong overall carbohydrate digestion time, causing a reduction in the rate of glucose absorption and consequently blunting the postprandial plasma glucose rise. Some of the plants are also considered as an important source of chemical constitue...