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At least 1,063 records · Page 59Linked to original sources
PubMed1997

[Trial for transdermal administration of sulfonylureas].

Sulfonylureas are widely used as oral hypoglycemic drugs in the treatment of non insulin dependent diabetes mellitus (NIDDM). Since sulfonylureas are usually taken for a long period, the compliance of the patients is very important. Therefore, for the improvement of the compliance of the patients, the development of a transdermal dosage form of sulfonylureas was attempted in this study. Glibenclamide (GLI) or chlorpropamide (CHL) was chosen as a principal agent and ointments were prepared by mixing 5% of GLI or CHL with a FAPG ointment base. Penetration and shearing stresses of the ointments were determined as physical characteristics of the ointments. There was no obvious difference of characteristics between the GLI ointment, or the CHL ointment and the FAPG ointment base. In drug release tests, the CHL ointment showed better release of the drug than the GLI ointment. In both ointments, comparatively rapid release of drug was observed in the initial 1 h, and continuous slow release was observed thereafter. When the ointments were applied on the back of male Wistar rats and the plasma glucose level was measured, both CHL and GLI ointments gave lower blood glucose levels than the control (FAPG base). At the all measuring points, the GLI ointment brought about significantly lower blood glucose levels than the control (p < 0.01). Thus, it was demonstrated that sulfonylureas were absorbed through the skin and lowered the blood glucose levels. The results suggest the possibility of transdermal administration of sulfonylureas for the treatment of NIDDM.

Animals↗
PubMed1984

Glibenclamide is exceptional among hypoglycaemic sulphonylureas in accumulating progressively in beta-cell-rich pancreatic islets.

Six hypoglycaemic sulphonylurea compounds were compared with regard to their ability to bind to beta-cell-rich pancreatic islets microdissected from ob/ob-mice. Glibenclamide differed from carbutamide, tolbutamide, chlorpropamide, glibornuride and glipizide in not being rapidly bound to an equilibrium, but accumulating progressively in amounts far exceeding the water space. An inhibitor of the anion channels in the beta-cell membrane, 4-acetamido-4'-isothiocyanate-stilbene-2,2'-disulphonic acid (SITS), suppressed the islet uptake of glibenclamide and to some extent also that of carbutamide and glibornuride. The unusual uptake characteristics of glibenclamide had their counterpart in a retardation of its maximal action in promoting the entry of Ca2+ into the beta-cells.

Animals↗
PubMed1975

A new method for the production of experimental diabetes in rabbits.

Oral administration of 250 mg hydrochlorothiazide/kg, with previous i.v. injection of 4 i.u. soluble insulin or s.c. injection of protamine-zinc insulin, has been found to produce stable hyperglycaemia in rabbits irrespective of sex. It is thought that insulin helps the selective action of hydrochlorothiazide on the beta cells by removing the protective glucose barrier. Although stimulation of glucagon or some extra-pancreatic mechanism at the initial stage could not be altogether ruled out, the central action of the drug is supported by the finding that the hydrochlorothiazide-induced hyperglycaemia was lowered by the sulphonylurea derivative, chlorpropamide.

Administration, Oral↗
PubMed1976

Relationship of serum glucose concentration to changes in refraction.

The effect of chronic changes in serum glucose concentration on refraction was studied by increasing the dose of insulin or chlorpropamide in 10 diabetic patients who initially had relatively high glucose concentrations. In every case when serum glucose concentration was reduced the vision became less myopic or more hyperopic. To assess acute changes. 10 diabetics (including four with aphakic eyes) were given an intravenous injection of glucose. In patients with intact lenses the vision became more myopic or less hyperopic following the administration of glucose, but in the aphakic eyes hyperopia increased. It is concluded from both the acute and chronic studies that higher levels of serum glucose concentration produce myopia and lower levels produce hyperopia. Furthermore, these changes are related to changes in the optical properties of the crystallin lens.

Blood Glucose↗
PubMed1986

Aldehyde dehydrogenase activity and large vessel disease in diabetes mellitus. A preliminary study.

Type II diabetic subjects, 26 with symptoms and/or signs of large vessel disease (LVD group) and 26 free from clinical vascular disease (FVD group), matched for sex, age, body weight, and duration of diabetes after diagnosis, together with 28 healthy controls participated in a preliminary study on new potential risk factors of large vessel disease. The activity of erythrocyte aldehyde dehydrogenase (ALDH) was significantly higher (P less than 0.005) in the LVD than in the FVD group and in the controls, as indicated by a shorter half-life of acetaldehyde in homogenates of erythrocytes and plasma (100 +/- 11, 203 +/- 28, and 180 +/- 21 min, respectively). The results were unaffected by antidiabetes therapy, blood glucose control, alcohol consumption, or by recognized risk factors of angiopathy, such as blood pressure, hyperlipidemia, or smoking. Whether ALDH activity is a primary factor in large vessel disease or is merely a secondary phenomenon is unknown. However, ALDH activity is a critical factor determining chlorpropamide alcohol flush (CPAF), which has been suggested to be an inherited trait in some type II diabetic subjects. In conclusion, high ALDH activity was shown to be associated with an increased risk of large vessel disease in diabetes.

Acetaldehyde↗
PubMedDate not supplied

Efficacy of glyburide in diabetics poorly controlled on first-generation oral hypoglycemics.

Twenty-four type II (non-insulin-dependent) diabetic patients poorly controlled on maximum doses of first-generation oral hypoglycemic agents were switched to glyburide. There was a significant decrease in glycosylated hemoglobin, but the level was normalized in only four patients; there was no correlation with age, weight, or duration of diabetes. The best predictor for improvement was initial failure on tolbutamide, as opposed to the other first-generation drugs. Patients not controlled with 500 mg/day of chlorpropamide were less likely to benefit from glyburide therapy.

Administration, Oral↗
PubMed1993

Administration of sulfonylureas can increase glucose-induced insulin secretion for decades in patients with maturity-onset diabetes of the young.

OBJECTIVE: To ascertain whether the effect of sulfonylureas on glucose-mediated insulin release persists for years to decades in patients with maturity-onset diabetes of the young. RESEARCH DESIGN AND METHODS: The effect of sulfonylurea treatment on glucose-induced insulin secretion was ascertained prospectively for up to 33 yr in 12 diabetic patients of the maturity-onset diabetes of the young RW pedigree, who are genetically homogeneous because they share DNA markers on chromosome 20q. In 7 of these patients, paired glucose tolerance tests, given while the patients were on and off sulfonylureas, were performed after 7-31 yr. RESULTS: Glucose-induced insulin secretion showed an average increase of 68% in diabetic patients who remained responsive to chlorpropamide after having been on and off the drug for decades. In most patients, however, glucose-induced insulin secretion declines over time (1-4%/yr). Some patients become unresponsive to sulfonylureas after 3-25 yr and then have very small or no increases in glucose-induced insulin secretion and require treatment with insulin to normalize fasting hyperglycemia. CONCLUSIONS: Increase in glucose-induced insulin secretion remains the most important mechanism of the action of sulfonylureas during long-term administration.

Adolescent↗
PubMedDate not supplied

Correlation of serum lipids with diabetes control in sulfonylurea-treated diabetic patients.

The relationships between fasting blood glucose, glycosylated hemoglobin A1, and several lipid parameters were studied in 67 non-insulin-dependent diabetic patients (19 men, 48 women) being treated with tolbutamide, chlorpropamide, or glibenclamide. All patients were over 60 yr of age with a mean age of 76.4 +/- 6.7 yr (+/- SD). There were positive associations between fasting blood glucose and serum cholesterol, LDL cholesterol, and serum triglycerides. A strong association between total cholesterol and triglycerides was also evident. Diabetes control and HDL cholesterol did not correlate with each other. A weak inverse correlation existed between fasting blood glucose and the HDL cholesterol/total cholesterol ratio. HDL cholesterol concentrations were low in the diet- and drug-treated diabetic patients. No deleterious sulfonylurea effects on cholesterol, LDL cholesterol, and triglyceride concentrations or HDL cholesterol/total cholesterol ratio were noted.

Aged↗
PubMedDate not supplied

The effect of oral hypoglycaemic agents on dyslipidaemia in Nigerian patients with newly diagnosed non-insulin dependent diabetes mellitus--a prospective study.

Thirty-five patients with non-insulin dependent diabetes (NIDDM) were treated and followed up for 24 weeks. Six of whom were managed with diet and/or metformin, nine received glibenclamide, twelve had a combination of metformin and glibenclamide, while the remaining eight patients received metformin and/or some other type of sulphonylurea (chlorpropamide or glipizide). By an analysis of variance, the different drug regimes showed equivalent glycaemic controlling effects, but the influence on dyslipidaemia was variable within the treatment groups, while these changes were insignificant between the groups. It is thus concluded that commonly used oral hypoglycaemic agents do not adversely affect plasma lipid levels in Nigerian patients with NIDDM.

Administration, Oral↗
PubMedDate not supplied

The antihyperglycamic effect of Telfaria occidentalis in mice.

The hypoglycemic effect of Telfaria occidentalis was studied in mice. The effect of the aqueous extract of the leaves on blood glucose level were assessed in normoglycaemic, glucose induced hyperglycaemic and streptozotocin (STZ) induced diabetic mice. The aqueous extract given orally in 1 g/kg did not alter the blood glucose level in normoglycaemic mice. In glucose-induced hyperglycemia, antidiabetic activity was seen when the extract and glucose were administered simultaneously and when the extract was giving to the mice 60 minutes before glucose. In STZ-induced diabetic mice, a reduction in the blood glucose level was seen from day two of the administration of the extract. The hypoglycemic effect of the aqueous extract was compared with that of an oral dose of chlorpropamide (200 mg/kg) under the same conditions. The results of this study indicate that the aqueous extract of the leaves of Telfaria occidentalis possess hypoglycaemic activity.

Administration, Oral↗
PubMed1975

Sulphonylureas and insulin resistance.

This is a case report of a diabetic who required 750-1000 units of insulin per day when gangrene of the leg developed, whereas previously he had needed no insulin. After amputation of the leg, the patient remained asymptomatic for 9 weeks without insulin. This was clearly related to an increased concentration of circulating antibody-bound insulin. Despite healing at the site of amputation, diabetic symptoms and insulin resistance reappeared. Chlorpropamide treatment reduced the insulin requirement to zero, which was unrelated to a change in insulin antibody concentration.

Chlorpropamide↗
PubMed1976

Influence of diabetes mellitus on drug metabolism in man.

Drug metabolizing capacity was assessed in 29 normal subjects and in 28 diabetics on various treatment regimes using the rate of antipyrine elimination as reflux. Plasma half-life of antipyrine was markedly shorter (38%), and the plasma clearance of this drug greater (40%) in diabetics receiving insulin than in controls. There was also an indication of a small increase in rate of test drug elimination in diabetics taking chlorpropamide. Patients being controlled solely on diet or those on tolbutamide did not exhibit an altered rate of drug elimination. The rate of metabolism and inactivation of other drugs may be altered in diabetics taking insulin so that optimal doses of some comcomitantly administered drugs may be different in this group of patients.

Antipyrine↗
PubMed1976

[Experience with the tegretol treatment of diabetes insipidus].

The use of tegretol in a 24-hour dose of 200-600 mg in 12 patients with diabetes incipidus led to the improvement of their general condition, lesser thirst, reduction of the 24-hour diuresis and increase of specific gravity of the urine. A positive effect of prescribing tegretol together with chlorpropamide was noted in a patient with diabetes mellitus and incipidus.

Adult↗
PubMedDate not supplied

[The efficacy of quercetin in alloxan diabetes].

It has been established that quercetin in doses of 10 and 50 mg/kg promotes normalization of the level of glycemia and blood coagulation, increases liver glycogen content, reduces high blood serum concentrations of cholesterol and low density lipoproteins, seen in diabetes. In some cases, the efficacy of quercetin exceeds that of chlorpropamide and dry Eleutherococcus extract in white rats with alloxan diabetes.

Animals↗
PubMedDate not supplied

Hypoglycaemic and hypotensive effects of Harpephyllum caffrum Bernh ex CF Krauss (Anacardiaceae) stem-bark aqueous extract in rats.

The stem bark of Harpephyllum caffrum Bernh ex CF Krauss (family: Anacardiaceae) is used traditionally in African folk medicine to manage, control and/or treat an array of human ailments, including diabetes mellitus and hypertension. In order to scientifically appraise some of the anecdotal, folkloric and ethnomedical uses of Harpephyllum caffrum, this study was undertaken to examine the hypoglycaemic and hypotensive effects of Harpephyllum caffrum stem bark aqueous extract (HCE) in rat experimental paradigms. The hypoglycaemic effect of the plant extract (HCE) was examined in normal and diabetic rats, using a streptozotocin (STZ)-induced diabetes mellitus model. Hypertensive, Dahl salt-sensitive rats were used to investigate the hypotensive (antihypertensive) effect of the plant extract. Chlorpropamide (250 mg/kg po) was used as the reference hypoglycaemic agent for comparison. Acute oral administrations of the plant extract (HCE, 50-800 mg/kg po) caused dose-related, significant (p < 0.05- 0.001) hypoglycaemia in normal (normoglycaemic) and STZ-treated diabetic rats. Furthermore, acute intravenous administrations of the plant extract (HCE, 25-400 mg/kg iv) produced dose-dependent, significant reductions (p < 0.05-0.001) in systemic arterial blood pressures and heart rates of the hypertensive, Dahl salt-sensitive rats used. Although the exact mechanisms of action of the plant extract still remain obscure at the moment, it is unlikely that the plant causes hypotension in the mammalian experimental animal model used, via the cholinergic mechanism, since its hypotensive effect was resistant to atropine pretreatment. The numerous polyphenolic compounds and flavonoids present in the plant are speculated to account for the observed hypoglycaemic and hypotensive effects of the extract. However, the findings of this experimental animal study indicate that the stem-bark aqueous extract of H caffrum possesses hypoglycaemic and hypotensive properties, and thus lend pharmacological support to the suggested folkloric, anecdotal and ethnomedical uses of the plant in the management and/or control of adult-onset type 2 diabetes mellitus and hypertension in some rural communities of southern African.

Animals↗
PubMedDate not supplied

Hypoglycaemic and hypotensive effects of Momordica charantia Linn (Cucurbitaceae) whole-plant aqueous extract in rats.

Various morphological parts (roots, stems, leaves and fruits) of Momordica charantia Linn (family: Cucurbitaceae) are used traditionally in African folk medicine to manage, control and/or treat a plethora of human ailments, including diabetes mellitus and hypertension. In order to scientifically appraise some of the folkloric, anecdotal and ethnomedical uses of M charantia, the present study was undertaken to investigate the hypoglycaemic and hypotensive effects of M charantia whole-plant aqueous extract (MCE) in rat experimental paradigms. The hypoglycaemic effect of the plant extract was examined in normal and diabetic rats, using streptozotocin (STZ)- induced diabetes mellitus models. Normotensive (normal), and hypertensive Dahl salt-sensitive rats were used to probe the hypotensive (antihypertensive) effect of the plant extract. Chlorpropamide was used as reference hypoglycaemic agent for comparison. Acute oral administrations of the plant extract caused dose-related, significant hypoglycaemia in normal (normoglycaemic) and STZ-treated, diabetic rats. Furthermore, acute intravenous administrations of MCE produced dose-dependent, significant reductions in systemic arterial blood pressure and heart rates of normal, and hypertensive Dahl salt-sensitive rats. Although the exact hypoglycaemic and hypotensive mechanisms of action of the plant extract remain speculative at the moment, it is unlikely that the herb causes hypotension in the mammalian experimental animal model used via cholinergic mechanisms, since its cardiovascular effects are resistant to atropine pretreatment. However, the findings of this experimental animal study indicate that the plant extract possesses hypoglycaemic and hypotensive properties, and therefore, lend pharmacological credence to folkloric, ethnomedical uses of the plant in the management and/or control of diabetes mellitus and hypertension in some rural African communities.

Animals↗
PubMed1991

Compliance in black patients with non-insulin-dependent diabetes mellitus receiving oral hypoglycaemic therapy.

Poor compliance with drug therapy is an important cause of therapeutic failure. Sixty-eight black patients with non-insulin-dependent diabetes mellitus receiving oral hypoglycaemic agents were interviewed and various factors, such as age, sex, degree of control and type of therapy, were recorded by means of a questionnaire. Compliance was determined by qualitatively assessing urine for the presence of the drugs. An alarmingly high incidence of non-compliance of 65% was found, which could still be an under-estimation because of the long half-life of one of the drugs involved--chlorpropamide. Although interesting trends were noted, no statistically significant differences between compliant and non-compliant patients were found. In the light of the high incidence of non-compliance, a larger and more detailed study seems to be warranted to identify problem areas and to plan appropriate interventions.

Black or African American↗