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At least 397 records · Page 22Linked to original sources
PubMed1986

Hypoglycemic action of karanjin.

The hypoglycemic activity of karanjin, 3-methoxy flavono 7,8-furan, was investigated in normal and alloxan-induced diabetic albino rats. Oral administration of karanjin at a dose of 2 mg/kg/day for 7 days caused a significant reduction in blood sugar level both in normal and in alloxan-induced diabetic rats. Acute treatment with a single dose of karanjin, 0.5 mg/kg i.p., produced a significant fall in blood sugar level in normal rats while in alloxan-induced diabetic rats it was ineffective. Impaired glucose tolerance was also improved by karanjin treatment. It is concluded that karanjin has a significant hypoglycemic effect in albino rats.

Animals↗
PubMed1985

Effect of a new hypoglycemic agent (MDL-310) on glucose metabolism.

N-[3-(dimethylamino)-2-propoxy-2-propenylidene]- N-methylmethanaminium as the iodide or camsylate salt (MDL-310) is a newly reported chemical which has been shown to produce hypoglycemia in vivo. The studies reported here describe in vivo and in vitro effects of MDL-310 on carbohydrate metabolism. In nonfasted mice, MDL-310 decreased liver glycogen and then produced hypoglycemia, concomitant with a near total depletion of liver glycogen stores. In fasted rats, nonhypoglycemic doses of MDL-310 increased glucose production and utilization as determined by tracer studies with [6-3H]glucose. Hypoglycemic doses decreased glucose production and increased blood lactate, which suggests an inhibition of gluconeogenesis. In isolated rat hepatocytes MDL-310, at concentrations of greater than or equal to 5 X 10(-6) M, inhibited gluconeogenesis from lactate (10 mM) plus pyruvate (2 mM). We conclude that the primary action of MDL-310 is to increase glucose utilization and that decreased production due to the inhibition of gluconeogenesis is involved in the hypoglycemic action. A single metabolic action of MDL-310 to increase glycolytic metabolism of glucose is proposed which could explain both the increase in glucose utilization and decrease in glucose production.

Animals↗
PubMedDate not supplied

[Hypoglycemic activity of aromatic sulfohydrazides and their derivatives].

Tests on rabbits revealed the aromatic sulfohydrazides and their derivatives to display hypoglycemic action. A number of compounds superior to butamide by their sugar-lowering action and of low toxicity were discovered. The relationship between the chemical structure of the study substances and their hypoglycemic action is discussed.

Animals↗
PubMed1983

Fenfluramine in the treatment of non-insulin-dependent diabetics: hypoglycemic versus anorectic effect.

A few studies have suggested that the anorectic drug fenfluramine has a hypoglycemic effect. The major problem in interpreting those studies, however, is the difficulty in dissociating the effect of weight loss on blood glucose from the direct effect of fenfluramine. In a double-blind study of 28 diabetic females treated with oral hypoglycemic agents, a significant decrease in fasting blood glucose (from 195 +/- 17 mg/dl to 152 +/- 15 mg/dl after four weeks, and to 155 +/- 14 mg/dl after eight weeks) was observed in fenfluramine-treated patients (n = 14). Corresponding values in the placebo group were 185 +/- 12 mg/dl and 201 +/- 16 mg/dl respectively. Glucose tolerance after a standard meal was also improved after fenfluramine treatment. Weight loss was minimal and not significantly different for the two groups. From these observations, it can be concluded that fenfluramine has a lowering effect on blood glucose which is independent of its effect on weight.

Aged↗
PubMed1983

Stoichiometry of calcium binding by hypoglycemic sulfonylureas.

In a two-phase bulk system for the study of Ca ionophoresis, certain hypoglycemic sulfonylureas, when added to the organic phase, were translocated into the aqueous medium. Nevertheless, the stoichiometry of Ca binding by these agents could be assessed by repeated mixing of the aqueous medium with organic phases. At saturation, the binding of Ca ranged from 0.5 to 1.0 mole/mole of sulfonylurea. A 1:1 molar ratio was observed with glibenclamide, and this was found to be compatible with the conformational analysis of the Ca-glibenclamide complex. There was a tight correlation between the stoichiometry of the Ca-sulfonylurea complex and the biological potency of each drug. This suggests that such a stoichiometry may be responsible, in part at least, for differences in the insulinotropic capacity of distinct hypoglycemic sulfonylureas.

Calcium↗
PubMed1981

A study of the possible interaction of indoprofen with hypoglycemic sulfonylureas in diabetic patients.

Phenylbutazone was shown to impair tolbutamide metabolism with resulting potentiation of its hypoglycemic effect and increased danger of hypoglycemia. As indoprofen is widely used for treating rheumatic conditions, and in particular osteoarthritis, the possibility that it may increase the effect of sulfonylureas on blood glucose levels has been investigated. Clinical studies have been carried out in 24 patients with osteoarthritis. All of them had maturity-onset diabetes mellitus and were on sulfonylurea drugs (tolbutamide or glipizide). The trials were double-blind and were carried out according to two different experimental designs. Twelve patients were treated with 600 mg/daily of indoprofen for five days and placebo for an equivalent period of time according to a cross-over scheme. Another group of patients was treated with indoprofen for eight days preceded and followed by a four-day placebo treatment. In both studies concomitant treatment with the hypoglycemic drug was maintained with a fixed dosage. No important differences were found between blood glucose levels when the periods of treatment with indoprofen and placebo were compared. Consequently, it is unlikely that indoprofen treatment at the doses employed may interfere at the clinical level with the effect of tolbutamide or glipizide on glucose metabolism.

Aged↗
PubMed1978

Effects of glucose and some oral hypoglycemic agents upon the plasma glucose and immuno-reactive insulin (IRI) in normal and streptozotocin induced diabetic rat.

An investigation has been made to see the effect of oral hypoglycemic agants on the blood sugar (BS) and plasma Immuno-Reactive Insulin (IRI) in normal and streptozotocin diabetic rats. Plasma IRI was significantly reduced in a streptozotocin treated diabetic rat 8 weeks after streptozotocin injection. In normal rats oral administration of Sodium tolbutamide (TOL) and Glybenclamide (GLI) produced a significant fall in BS and a concurrent increase in plasma IRI, but phenformin (PHE) was without any effect on both these parameters. Unlike normal rats streptozotocin treated diabetic rats did not show lowering of BS and increase in plasma IRI following TOL and GLI. PHE, however, did produce a significant fall in BS. Oral glucose load did show a typical glucose tolerance curve and insulin release in normal rats. However, in the diabetic rats there was no significant increase in plasma IRI following glucose load. It is therefore concluded that streptozotocin treated diabetic rats differ from the maturity onset diabetic as regards the responses of TOL and GLI are concerned and this animal model can therefore be useful in differentiating the two types of oral hypoglycemic agents.

Animals↗
PubMedDate not supplied

Interaction of diphenylhydantoin and some oral hypoglycemic drugs related to carbohydrate metabolism in rats.

Daily treatment of rats with 50 or 100 mg/kg ip of diphenylhydantoin (DPH) for 3 weeks caused a significant elevation of blood glucose level and reduction of hepatic glycogen content. In rats receiving daily oral doses of tolbutamide (100 mg/kg) or phenformin (50 mg/kg) for the last 7 days of DPH treatment, the blood glucose level did not differ from those in the control group; in rats receiving the low doses of DHP, the reduction in hepatic glycogen content was prevented by either hypoglycemic drug; in rats receiving the high dose of DPH in combination with the hypoglycemics the glycogen reduction was smaller than in rats receiving DPH alone. A week's treatment with tolbutamide (100 mg/kg) alone resulted in a significant depression of the blood glucose level and elevation of hepatic glycogen content; phenformin (50 mg/kg) given alone for one week elevated the level of hepatic glycogen, but to a lesser degree than tolbutamide did, and did not affect the blood glucose level.

Administration, Oral↗
PubMed1976

Clinical use of oral hypoglycemic agents.

The pharmacology, mechanism of action, indications, interactions and clinical effectiveness of oral hypoglycemic agents, specifically the sulfonylureas and biguanides, are reviewed. The use of these agents is discussed in view of the findings of the University Group Diabetes Program study. It is concluded that oral hypoglycemic agents, in conjunction with diet and weight reduction, may be useful in selected patients but that insulin is preferable in most instances.

Biguanides↗
PubMed1994

Synthesis and pharmacological evaluation of novel series of sulfonate ester-containing 1,3,4-oxadiazole derivatives with anticipated hypoglycemic activity.

Four series of 2,5-disubstituted 1,3,4-oxadiozole derivatives (IV, VII, IX and X) have been synthesized from 4-(4- (Z)-[p- (benzenesulfonyloxy) phenylmethylene]- 5-oxo-1-phenyl-2-imidazolin-1-yl) benzoyl hydrazine derivative (II) with a view to investigate the effect of different structural changes in the oxadiazole moiety on the pharmacological activity of these compounds as possible hypoglycemic agents. The structure of the synthesized compounds was inferred from elemental and spectral data and their hypoglycemic effect, antimicrobial activity and toxicity were evaluated. Twelve of these compounds were effective, when administered at an oral dose of 100 mg/kg, to induce marked reduction in blood glucose level.

Animals↗
PubMed1993

[Plants with hypoglycemic effects].

Diabetes mellitus is a metabolic disorder which has affected several millions of population all over the world. It is characterized by an excess of sugar in the blood and urine, hunger, thirst and gradual loss of weight. Insulin is a hormone which regulates the carbohydrate and triacylglyceride metabolism through its action at several sites and facilitates the entry of glucose accumulation in the blood. Insulin also stimulates the synthesis of glucokinase and moderates the degree of gluconeogenesis. In the diabetic patient, there is an aberration in the functioning of insulin. Prior to the 1950s, control of diabetes was based entirely on insulin therapy. Unfortunately, some patients developed complications and thus need for some other therapy was realized. Presently control of NIDDM relies on compounds from two classes--sulphonylureas and biguanides. Although these drugs are widely accepted as being efficacious in treating some diabetics, they are ineffective in many others. Consequently, testing of many chemicals and plant extracts has continued. The object of the present paper is to bring up-to-date information on the hypoglycemic activity of plants, above all the plants occurring in our country, and those who se hypoglycemic activity has been scientifically documented in a more detailed way. Recent theories on the mechanism of action of these plants are also discussed.

Diabetes Mellitus↗
PubMed1993

[Cardiovascular risk factors and treatment with insulin in type II diabetic patients in whom oral hypoglycemic drugs have failed].

BACKGROUND: To find whether insulin treatment in type II diabetic patients in whom treatment with oral hypoglycemic treatment has failed changes body fat distribution or modifies cardiovascular risk factors. METHODS: Twenty-six patients (16 women and 10 men with a mean age of 62.3 +/- 9.8 years and 12.8 +/- 8.5 years of evolution) were studied before and 3 months after starting insulin treatment at a daily dose of 0.3 IU/kg of body weight. RESULTS: HbA1c decreased from 9.9 +/- 2.1 to 8.2 +/- 1.6% (p < 0.001) similar to fructosamine (from 407 +/- 86 to 350 +/- 71 mumol/l; p < 0.001) following treatment with insulin, but a increase in body weight, body mass index, blood pressure and a decrease in the concentration of HDL-cholesterol (p < 0.05) were observed. Weight was gained in 21 patients (80%) (3.7 +/- 1.9 kg), increasing body fat of central distribution in 13 (50%) and of peripheral distribution in 8 (30%). The patients in whom body fat of central distribution was increased fundamentally differentiated from the remaining patients by having a greater body mass index (p < 0.01), in all cases greater than 25 kg/m2 upon initiation of the insulin treatment, and by a significantly greater increase in body weight, blood pressure and total cholesterol after the insulin treatment. Patients who increased body fat of peripheral distribution or who did not gain weight did not present these changes in cardiovascular risk factors and were characterized by an increase of at least 500 kcal/week consumed by physical exercise. CONCLUSIONS: Treatment with insulin in type 2 diabetic patients in whom oral hypoglycemic drugs have failed improves glycemic control, but induces an increase in weight and worsens cardiovascular risk factors in patients with a CMI greater than 25 kg/m2. This change may be prevented by an increase in physical activity.

Adipose Tissue↗
PubMed1995

[Immunologic and insulin secretion markers in non insulin dependent diabetic patients with secondary failure to oral hypoglycemic drugs].

BACKGROUND: The pathogenesis of secondary failure to hypoglycemic agents is heterogeneous. Some patients are true insulin dependent diabetics with a slow autoimmune disease suggested by their positive islet cell antibodies. Others, have an increased insulin resistance. AIM: To assess the frequency of positive islet cell antibodies in diabetic patients with secondary failure to oral hypoglycemic agents. PATIENTS AND METHODS: Thirty one diabetics, 16 with recent (less than six months) secondary failure and 15 with metabolically stable non insulin dependent diabetes were studied. All patients were older than 25 years old and had a body mass index of less than 30 kg/m2. C peptide levels before and at 5, 15 and 30 min after IV glucagon, islet cell antibodies using the Poly Human IgG peroxidase method and insulin sensitivity and secretion (estimated by the Homeostasis Model Assessment) were measured. RESULTS: Patients with secondary failure had lower C peptide levels, compared to subjects with stable diabetes (basal: 1.5 +/- 0.2 and 2.8 +/- 0.2 ng/ml; 5 min: 2.4 +/- 0.3 and 5.5 +/- 0.5 ng/ml; 15 min: 1.9 +/- 0.3 and 4.0 +/- 0.6 ng/ml; 30 min: 1.6 +/- 0.3 and 3.4 +/- 0.5 ng/ml). Beta cell activity was 20.6 +/- 4.3% in patients with secondary failure and 92.2 +/- 9% in stable diabetics (p < 0.01). Insulin sensitivity was similar in both groups (48.6 +/- 6 and 42.8 +/- 3.5% respectively). Three patients with secondary failure and none with stable diabetes had positive islet cell antibodies. When comparing patients with secondary failure and positive antibodies and subjects with secondary failure and negative antibodies, the former had non significantly lower age, BMI and C peptide levels. CONCLUSIONS: Some diabetic patients with secondary failure have positive islet cell antibodies. They should be measured in these patients to start insulin treatment precociously.

Administration, Oral↗
PubMed1977

Comparative hypoglycemic and hypoketonemic effects of tolbutamide and glypentide in rat.

Fed and 24 h fasted rats were treated by stomach tube with different doses of either tolbutamide or gluypentide and they were compared with controls treated with placebo. At low doses glypentide was ten times more effective as hypoglycemic agent than tolbultamide whereas it was only twice as effective in the fasted rats. Supramaximal doses of either drug produced the same effect decreasing blood glucose levels. Both drugs were able to decrease the rise of blood ketones in fasted rats, but the comparative effect was not parallel to the one observed on glycemia and not proportional to the doses used. The different responses are interpreted as function of the hypoglycemic effect, which would be mainly mediated through the insulinotropic action of these drugs, while the hypoketonemic would be the result of both their insulinotropic effect and their direct action on lipolysis and ketogenesis.

Animals↗
PubMed1977

Encephalopathy induced by oral hypoglycemic drugs.

Three patients experienced severe hypoglycemic encephalopathy during oral therapy of adult-onset diabetes mellitus. Disabling residual neurological deficits were observed in two of these patients. The insidious time course of drug-induced hypoglycemia appeared to prevent patient recognition of sustained hypoglycemia. These cases indicate the need for further caution in the administration of oral hypoglycemic agents.

Brain Diseases, Metabolic↗
PubMedDate not supplied

Evaluation of some acylamide derivatives as potential hypoglycemic agents.

A series of new acylamide derivatives with piperidine, pyrrolidinyl and alanyl have been tested for their hypoglycemic activities. 2-(Pyrrolidynyl)-N-(3-chlorophenyl) acetamide and 2-(Piperazinyl)-N-(4-methoxy phenyl) acetamide were found most active hypoglycemic compounds. Probably the amides have mode of action similar to sulphonylureas.

Acetanilides↗
PubMedDate not supplied

[Effect of a new hypoglycemic drug on the blood sugar in rats].

A sesquiterpenic lactone has been isolated from an extract of Artemisia cannariensis Lee by Clark's method and column chromatography. The hypoglycemic effects of the drug have been assayed in rats, as compared to different doses of insulin and a known sulphonylures drug. The subatance, which has been identified as vulgarine by professor Gonzalez, has highly significant hypoglycemic effects when administered orally or intravenously in relation to glycemia curves of rats previously injected with saline.

Administration, Oral↗
PubMedDate not supplied

[Hypoglycemic activity of Bouvardia terniflora, Brickellia veronicaefolia, and Parmentiera edulis].

OBJECTIVE: To evaluate the hypoglycemic activity of the hexane, chloroform and methanol extracts of Bouvardia terniflora, Brickelia veronicaefolia and Parmentiera edulis. MATERIAL AND METHODS: Normal and alloxan-induced diabetic mice were administered these plant extracts (intraperitoneal 100, 200 and 300 mg/kg). RESULTS: The administration of 300 mg/kg of chloroform extracts from P. edulis and B. terniflora and hexane from B. veronicaefolia to diabetic mice decreased the blood glucose levels in 43.75, 58.56 and 72.13%, respectively. These extracts administered to normal mice reduced blood glucose levels in 29.61, 33.42 and 39.84%, respectively. CONCLUSIONS: The hypoglycemic effect of these plant extracts used in traditional medicine for diabetes treatment is confirmed.

Alloxan↗