Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0011860 (type 2 diabetes)
 57,723 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Six months monotherapy with Acarbose vs. glibenclamide led to a marked improvement of BG and HbA1 in NIDDM, insufficiently controlled with diet. Beneficial effects of these distinct principles of action were statistically not different.
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PMID:Efficacy of 6 months monotherapy with glucosidase inhibitor Acarbose versus sulphonylurea glibenclamide on metabolic control of dietary treated type II diabetics (NIDDM). 149 Jun 92

Acarbose (Bay g 5421, Glucobay; CAS 56180-94-0) inhibits alpha-glucosidases of the small intestine and thus delays glucose release from complex carbohydrates. It is therefore efficient as a first-line drug in the treatment of noninsulin-dependent diabetics (NIDDM) insufficiently treated with diet alone. Information is scarce whether under acarbose treatment the lipid metabolism can also be improved. Therefore the changes of triglycerides, cholesterol and HDL-cholesterol were analyzed in a randomized double-blind placebo-controlled trial. In brief, 94 NIDDM aged 43 to 70, after a pretreatment period of at least 3 months, were treated with 100 mg acarbose t.i.d. or placebo for 24 weeks. The patients were recruited after a 4-week screening phase with reinforcement of diet. The most impressive results of acarbose treatment were lowering of blood glucose and insulin, especially in the postprandial state, and of HbA1 (glycosylated hemoglobin). Results on lipids: The initial serum cholesterol levels showed a broad spectrum. Low concentrations remained unchanged under acarbose, while high concentrations (the upper tercile) decreased from 273 to 251 mg/dl. This effect was statistically significant compared to placebo. HDL-cholesterol levels increased continuously under acarbose and placebo as well thus indicating some study effect. Similarly, fasting triglycerides leveled down under acarbose and placebo. However, drastic differences appeared in postprandial triglycerides which were checked 1 and 5 h after a test meal given at entry and at finish of the study. The lowering by acarbose compared to placebo was highly significant for the 1 h postprandial concentrations. It is concluded that acarbose treatment can reduce elevated cholesterol concentrations and postprandial triglyceride concentrations.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Beneficial effects on serum lipids in noninsulin dependent diabetics by acarbose treatment. 177 63

The sulphonylureas and the biguanides are widely used as adjuncts to dietary measures in the treatment of non-insulin-dependent (type 2) diabetes mellitus (NIDDM). Adverse effect profiles differ markedly between the sulphonylureas and biguanides, reflecting differences in chemical structure and mode of action. Sulphonylureas are generally well tolerated, although pharmacokinetic differences between these agents have important clinical implications. The main adverse effect associated with sulphonylureas is hypoglycaemia. This effect is a predictable consequence of the principal pharmacological effect of these drugs, i.e. sensitisation of the islet beta-cell to glucose, resulting in enhanced endogenous insulin secretion. Sulphonylurea-induced suppression of hepatic glucose production may cause profound and protracted hypoglycaemia, especially in elderly patients, in individuals with intercurrent illnesses and reduced caloric intake, or when taken in combination with other compounds with hypoglycaemic potential, e.g. alcohol (ethanol). Sulphonylureas with a longer duration of action, notably chlorpropamide and glibenclamide (glyburide), are more liable to induce serious hypoglycaemia, particularly when drug elimination is reduced by renal impairment. Other drugs such as salicylates may potentiate the actions of sulphonylureas, thereby increasing the risk of hypoglycaemia. Biguanide therapy is associated with alterations in lactate homeostasis which under certain clinical circumstances may result in fatal lactic acidosis. Phenformin is associated with a markedly greater risk of lactic acidosis than metformin. Phenformin has been withdrawn in many countries for this reason. All biguanides must be avoided in patients with renal impairment, hepatic dysfunction and cardiac failure--conditions where drug accumulation or disordered lactate metabolism may predispose to lactic acidosis. Phenformin should not be given to individuals who exhibit a severe, genetically conferred hepatic defect of hydroxylation which impedes metabolism of this drug. Less seriously, the biguanides are associated with a relatively high incidence of gastrointestinal adverse effects which limit compliance. Acarbose, a competitive inhibitor of intestinal alpha-glucosidases, has recently been introduced. In contrast to the sulphonylureas and biguanides, acarbose has not been associated with life-threatening adverse effects. This reflects the low systemic absorption of the drug and, predictably, its principal unwanted effects are gastrointestinal disturbances resulting from iatrogenic carbohydrate malabsorption.
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PMID:Comparative tolerability profiles of oral antidiabetic agents. 784 43

With alpha-glucosidase inhibitors generally improved metabolic control is achieved in NIDDM patients regardless of whether acarbose is administered in addition to other oral anti-diabetic agents or to diet alone. The most significant finding is the reduction of postprandial blood glucose concentrations. Long-term studies show a decrease in glycosylated haemoglobin and often also in fasting blood glucose levels. Placebo-controlled studies have proven that postprandial insulin concentrations are decreased under acarbose treatment while fasting plasma insulin is usually unchanged. The major side-effects of acarbose treatment involve the gastrointestinal system and include flatulence, abdominal discomfort and diarrhoea. Symptoms diminish with treatment time and are less severe when the treatment is started with low doses. Acarbose should usually be initiated as a 50 mg dose immediately before each major carbohydrate containing meal. Monotherapy with acarbose does not cause hypoglycaemia, however, hypoglycaemia may occur with combination of sulphonylurea or insulin treatment by the well-known reasons. In this case hypoglycaemia has to be treated by taking glucose.
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PMID:alpha-Glucosidase inhibitors in diabetes: efficacy in NIDDM subjects. 800 25

Oral antidiabetic agents continue to play an important role in the treatment of type 2 diabetes. Of decisive importance is the timing of their use, together with a knowledge of their specific properties. Acarbose, which needs to be initiated at a low, slowly increasing dose, is noted for the fact that it has virtually no systemic side effects. Metformin reduces plasma glucose levels without inducing hyperinsulinemia, and carries virtually no risk of lactic acidosis. Glibenclamide can be used either alone to treat type 2 diabetes or in combination with other oral antidiabetics or insulin. Today, intensified insulin therapy represents the optimal standard of insulin replacement. It permits meal-oriented injection of normal insulin and the use of longer-acting insulin overnight. This form of treatment is now facilitated by the possibilities of plasma glucose selfmonitoring and the use of injection aids (pen). Intensified treatment should be initiated at the time type I diabetes is diagnosed. In the case of a particularly instable metabolic situation or neuropathy, it may become necessary to use insulin pumps.
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PMID:[Management of diabetes in general practice--current requirements. 2: Oral antidiabetics and insulin therapy]. 820 Jun 2

Acarbose is an alpha-glucosidase inhibitor which delays the absorption of glucose from the intestine. Taken orally before a meal, acarbose delays absorption of carbohydrates and decreases the postprandial plasma glucose and plasma insulin rise. A pilot study has been carried out to investigate whether acarbose can improve insulin sensitivity in subjects with impaired glucose tolerance (IGT). 18 subjects were randomized to receive either acarbose, 100 mg t.d.s., or placebo for 16 weeks. Acarbose therapy was found to decrease 2-hour plasma glucose and plasma insulin levels and to increase insulin sensitivity. Insulin resistance is an important factor in the development of non-insulin dependent diabetes mellitus (NIDDM).these results suggest that acarbose therapy may be able to prevent or delay the progression of IGT to NIDDM. A multicentre phase III clinical trial is now planned to investigate this possibility.
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PMID:The effect of acarbose on insulin sensitivity in subjects with impaired glucose tolerance. 868 58

The efficacy and safety of acarbose (100 mg three times a day for 12 weeks) was investigated in an open study in patients with non-insulin dependent diabetes mellitus who could not achieve satisfactory glycaemic control by diet alone. Acarbose significantly decreased fasting plasma glucose from 165.9 +/- 16.0 mg/dl to 159.5 +/- 16.9 mg/dl (P value < 0.01). The reduction of postprandial plasma glucose was 11.2 per cent and 9.8 per cent for 1 hour and 2 hours respectively. HbAic also significantly decreased from the baseline. The most common side effects were mild to moderate flatulence and abdominal distension. There were no significant changes in body weight, lipid profile and other biochemical parameters. These results indicate that treatment with acarbose is safe and effective in adjunct to dietary therapy for the treatment of NIDDM.
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PMID:Efficacy of acarbose as monotherapy in NIDDM patients. 886 16

Acarbose represents a new pharmacological approach to achieving the metabolic benefits of a slower carbohydrate absorption in diabetes, by acting as a potent, competitive inhibitor of intestinal alpha-glucosidases. Acarbose molecules attach to the carbohydrate binding sites of alpha-glucosidases, with an affinity constant that is much higher than that of the normal substrate. Because of the reversible nature of the inhibitor-enzyme interaction, the conversion of oligosaccharides to monosaccharides is only delayed rather than completely blocked. Acarbose has the structural features of a tetrasaccharide and does not cross the enterocytes after ingestion. Thus, its pharmacokinetic properties are well suited to the pharmacological action directed exclusively towards the intestinal glucosidases. The most important clinical consequence of the delayed carbohydrate digestion caused by acarbose is the attenuation of postprandial increases in blood glucose levels. Other effects have also been described: a decreased beta-pancreatic response to meals, and influences on gut hormone secretion and plasma lipid levels. Gastrointestinal discomfort is frequently reported as an adverse effect of acarbose administration, but incidence usually decreases with time. The suitability of acarbose for improving glucose homeostasis as an adjunct to dietary control or to administration of sulphonylureas or insulin has been extensively studied in patients both with type 1 (insulin-dependent) and type 2 (non-insulin-dependent) diabetes mellitus. Acarbose can be used as first-line therapy in patients with type 2 diabetes which is poorly controlled by diet alone. Moreover, the lack of bodyweight gain or hypoglycaemic effects reported during acarbose treatment may be advantageous for obese or elderly patients. Finally, the reduction in fluctuations of glucose levels throughout the day may help to control type 1 diabetes in patients with 'brittle diabetes'. Long term prospective studies are still needed to confirm these indications and the usefulness of acarbose in conditions other than diabetes, notably reactive hypoglycaemia and dumping syndrome.
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PMID:Pharmacokinetic-pharmacodynamic relationships of Acarbose. 890 94

Non-insulin-dependent diabetes mellitus (NIDDM) is a metabolic disease that is common in the elderly, and is characterised by insulin insufficiency and resistance. Measures such as bodyweight reduction and exercise improve the metabolic defects, but pharmacological therapy is the most frequently used and successful therapy. The sulphonylureas stimulate insulin secretion. Metformin and troglitazone increase glucose disposal and decrease hepatic glucose output without causing hypoglycaemia. Acarbose is a dietary aid that spreads the dietary carbohydrate challenge to endogenous insulin over time. These pharmacological agents, either alone or in combination, should improve blood glucose regulation in patients with NIDDM.
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PMID:Oral antidiabetic drug use in the elderly. 897 42

Non-insulin-dependent diabetes mellitus is a metabolic disease that is common and is characterized by insulin insufficiency and resistance. Measures such as body weight reduction and exercise improve the metabolic defects, but pharmacological therapy is the most frequently used and successful therapy. The sulphonylureas stimulate insulin secretion. Metformin and troglitazone increase disposal and decrease hepatic glucose output without causing hypoglycemia. Acarbose is a dietary aid that spreads the dietary carbohydrate challenge to endogenous insulin over time. These pharmacological agents, either alone or in combination, can improve blood glucose regulation in patients with non-insulin-dependent diabetes mellitus.
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PMID:Pharmacological regulation of blood glucose levels in non-insulin-dependent diabetes mellitus. 912 43


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