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At least 451 records · Page 25Linked to original sources
PubMed2005

Pioglitazone, rosiglitazone, and rosiglitazone + metformin: new drugs. Glitazone + oral antidiabetic combination: inadequately evaluated.

(1) When single-agent therapy provides inadequate glycaemic control for patients with type 2 diabetes, most guidelines recommend metformin in combination with a glucose-lowering sulphonylurea as standard treatment, despite the lack of any proven impact on morbidity or mortality. Other options include switching to insulin or abandoning the target of strict glycaemic control. (2) Pioglitazone and rosiglitazone are approved for use in combination with a glucose-lowering sulphonylurea when metformin is poorly tolerated or contraindicated, and in combination with metformin in overweight patients. (3) A fixed-dose combination containing 1 or 2 mg of rosiglitazone plus 500 mg of metformin (hydrochloride) was launched onto the French market in October 2004. (4) The indication for rosiglitazone was extended to include its use as triple-agent therapy in combination with metformin and a glucose-lowering sulphonylurea. (5) No clinical trials assessing effects on mortality or morbidity have evaluated rosiglitazone or pioglitazone in combination with other oral antidiabetic drugs. (6) Several trials have compared the glucose-lowering effects of dual-agent therapy using rosiglitazone or pioglitazone plus a glucose-lowering sulphonylurea or metformin versus dual-agent therapy with metformin and a glucose-lowering sulphonylurea. (7) These clinical trials indicate that in terms of HbA1c level, dual-agent therapy based on rosiglitazone or pioglitazone is about as effective as combination therapy with metformin plus a glucose-lowering sulphonylurea. (8) The main known adverse effect of pioglitazone and rosiglitazone is water-sodium retention, which can provoke oedema and haemodilution anaemia, and can aggravate or reveal heart failure. (9) Pioglitazone has a positive effect on the lipid profile, whereas rosiglitazone increases the LDL-cholesterol level. (10) Dual-agent therapy with pioglitazone and a sulphonylurea causes more weight gain than metformin plus a sulphonylurea. (11) Several trials have assessed triple-agent regimens containing a glitazone. Three placebo-controlled double-blind trials have tested pioglitazone (one trial, nearly 300 patients) or rosiglitazone (two trials, about 1200 patients) for 12 to 26 weeks in patients whose glycaemia was poorly controlled by dual-agent therapy with a sulphonylurea plus metformin. The glycated haemoglobin level fell by 0.3% to 1.1% (in absolute values), depending on the trial and the dosage, but at a cost of the usual adverse effects such as weight gain, anaemia and oedema. Three unblinded trials have compared oral triple-agent regimens containing glitazone versus insulin plus metformin, alone or in combination with a glucose-lowering sulphonylurea; the treatment including glitazone was no more effective in terms of the glycated haemoglobin level, but was associated with an increase in adverse effects and dropouts. (12) Given the limited clinical data available in early 2005, pioglitazone and rosiglitazone have no place in the management of type 2 diabetes.

Clinical Trials as Topic↗
PubMed2005

[Prevalence of diabetes, antidiabetic treatment and chronic diabetic complications reported by general practitioners].

INTRODUCTION: Prevalence of type 2 diabetes has increased greatly over the past decade and focus of care for people with diabetes has shifted from specialists to general practitioners (GPs). Because of lack of the central registry, a real number of diagnosed diabetes in Poland is unknown, as unknown is the prevalence of diabetes in patients attending primary health care, provided treatment and a prevalence of chronic diabetic complications registered by GPs. AIM OF STUDY: Assessment of the prevalence of diabetes registered in primary health care, recommended antidiabetic treatment and prevalence of microangiopathic diabetic complications diagnosed by GPs. MATERIAL AND METHODS: Study was performed in Szczecin, a city of 450 000 inhabitants, located in North-West part of Poland. Data were obtained in year 2002 from one of the primary health care centers, in which health care was provided by 12 GPs for 27 932 inhabitants (15655 females and 12277 males), aged 0-98 years (average 38.3 +/- 23.2 years). Data were extracted from medical records and provided by GP doctors. RESULTS: Number of diagnosed and registered diabetics was 993 (prevalence--3.56%), age 3-95 years (mean 65.4 +/- 13.6 years). The diabetic group consisted of 611 females (mean age 67.5 +/- 12.4)--prevalence--3.90% and 382 males (mean age 62.0 +/- 14.7)--prevalence--3.11% (p = 0.003). Mean duration of diabetes was 7.4 +/- 6.9 years and it was similar for males and females. Type 2 diabetes was diagnosed in 94.4%, type 1 diabetes in 4.5%, other types of diabetes in 1.1% of all patients. Prevalence of registered diabetes in the group of 0-10 years old was 0.08%, in the group 11-20 years--0.33%, 21-30 years--0.25%, 31-40 years--0.44%, 41-50 years--1.93%, 51-60 years--5.03%, 61-70 years--9.88% and in the group over 70 years old--14.37%. Prevalence of diabetes in the group over 14 years old was 4.38%, in the group over 20 years--4.86%, and in subjects older than 35 years--6.84%. Elderly patients, over 60 years account for 74% of all diabetic subjects and subjects over 70 years--for 45% of them. Reported treatment of type 2 diabetes: diet alone--9%, oral agents--68%, oral agents combined with insulin--10.5%, insulin alone--12.5%. Mean HbA1c value measured in 307 type 2 diabetic subjects was 7.25 +/- 1.28%. According to GPs' opinion chronic microangiopathic diabetes complications were present in 36.6% of type 2 diabetic subjects. Retinopathy was reported in 24.8% of patients, polyneuropathy in 2.4%, nephropathy in 1.5%, diabetic foot in 0.5%, and combination of different complications in 7.4% of them. In type 1 diabetes chronic diabetic complications were stated in 42.2% of subjects--retinopathy--in 15.6%, polyneuropathy--in 2.2%, nephropathy--in 2.2%, diabetic foot--in 2.2%, and combination of them--in 20.0%. Average number of registered diabetics was 83 per physician, however 6 doctors took care of 107-158 diabetic subjects. In the past year diabetologist consultation or hospitalisation in internal medicine unit was provided for 47% of type 2 diabetics and for 98% of type 1 diabetics. CONCLUSIONS: 1. The prevalence of diabetes registered in primary health care in Szczecin is higher than expected on the basis of European data. 2. Low number of type 2 diabetics is treated with diet alone and quite high number is treated with insulin. 3. Low number of chronic diabetic complications reported by GPs, despite long duration of disease, indicates the necessity of special training in delivering care for diabetic people, diagnosis of diabetic complications, increased access to secondary care and better cooperation between primary and secondary care.

Adolescent↗
PubMed2005

[PPARgamma agonists--antidiabetics with positive effects on cardiovascular risk?].

INTRODUCTION: Peroxisome proliferator-activated receptor agonists are used as an antidiabetic drug with particular effect on insulin sensitivity. MATERIAL AND METHODS: This paper is based upon own literature and a Medline search. RESULTS AND INTERPRETATION: The drug improves insulin sensitivity, but has several cardiovascular effects as well. Blood pressure, serum lipids, endothelial function, inflammation and growth of smooth muscle are all modulated by these agonists. This group of drugs shows constant antiatherosclerotic properties. Larger clinical studies will give the answer whether this treatment can reduce micro- and macro-vascular complications in diabetes.

Albuminuria↗
PubMed2006

[Synthesis of phenyloxyisobutyric acid derivatives and their antidiabetic activity in vitro].

AIM: To design and synthesize new phenyloxyisobutyric acid analogues as antidiabetic compounds. METHODS: Eight new target compounds were synthesized by combination of lipophilic moieties and acidic moiety with nucleophilic replacement or Mitsunobu condensation. The eight compounds were confirmed by 1H NMR, 13C NMR, IR and MS. RESULTS: In vitro insulin-sensitizing activity (3T3-L1 adipocyte) demonstrated, that the cultured glucose concentration of up-clear solution detected with GOD-POD assay were 5.942, 6.339, 6.226 and 6.512 mmol x L(-1), respectively, when rosiglitazone, pioglitazone, compounds A and B were added to the insulin-resistant system. CONCLUSION: In vitro insulin-sensitizing activity of target compound A is in between that of rosiglitazone and pioglitazone, and activity of target compound B is slightly less than that of pioglitazone.

3T3-L1 Cells↗
PubMed2005

Antihyperlipidemic and antidiabetic effects of umbelliferone in streptozotocin diabetic rats.

The aim of the study was to evaluate blood glucose and lipid lowering effects of Umbelliferone (UMB) in streptozotocin (STZ) diabetic rats. Male albino Wistar rats (180 to 200 g) were induced diabetes by administration of STZ (40 mg/kg) intraperitonially. Normal and diabetic rats were treated with UMB in 10 percent dimethyl sulfoxide (DMSO) for 45 days. Diabetic rats had increased plasma glucose and decreased insulin, total proteins (TP), and albumin in addition to decreased food intake and body weight. Elevation in total cholesterol (TC), low density lipoprotein cholesterol (LDL-C), very low density lipoprotein cholesterol (VLDL-C), triglycerides (TG), free fatty acids (FFA), and phospholipids (PL), and reduction in high density lipoprotein cholesterol (HDL-C) in the plasma were observed. Liver and kidney tissues of diabetic rats had elevation in the levels of TC, TG, FFA, and PL. Treatment with UMB decreased plasma glucose and increased insulin, TP, and albumin apart from food intake and body weight. In UMB-treated diabetic rats, plasma and tissue TC, TG, PL and FFA, and plasma LDL-C, VLDL-C, and HDL-C reversed to near normal. Thus, reduction of blood glucose and lipid profiles indicates that UMB has antidiabetic and antihyperlipidemic effects in diabetic rats.

Albumins↗
PubMed2006

[Oral antidiabetic agents: which role in 2006?].

This article offers a review of the five classes of oral antidiabetics which are currently available, and focuses on practical considerations about the daily use of these drugs. Based on data from recent studies, it addresses several frequently asked questions. Which treatment to choose for which patient? How to adapt the treatment facing the progression of type 2 diabetes, which most often necessitates an intensification of the therapeutic means over time? Usually there are several initial therapeutic options for a given patient. The glycemic control over the following months allows to verify the efficiency of the treatment chosen. In case of a persistant glycemic imbalance, early intensification of the treatment is recommended.

Administration, Oral↗
PubMed2006

Antidiabetic activity of an ethanol extract obtained from the stem bark of Psidium guajava (Myrtaceae).

This study analyzed the antidiabetic properties of an ethanol extract of the stem bark of Psidium guajava, an indigenous medicinal plant used to control diabetes in Indian System of Medicine. The anti-hyperglycaemic activity of this plant on blood glucose levels of normal, normal glucose loaded (OGTT) and alloxan-induced hyperglycaemic rats was evaluated. The results showed that ethanol stem bark extract exhibited statistically significant hypoglycaemic activity in alloxan-induced hyperglycaemic rats but was devoid of significant hypoglycaemic effect in normal and normal glucose loaded rats (OGTT).

Animals↗
PubMed1990

[Antidiabetic treatment and monitoring during pregnancy in diabetes].

In pregnant diabetic women one of the goals of antidiabetic treatment and monitoring is to maintain blood glucose near normal values between 4.4 and 6.1 mmol/l. If possible such values should be obtained before conception. To reach these goals four components of health care delivery are of major importance. Education dealing with contraception and planification of the pregnancy, diet modified according to the state of pregnancy, self blood glucose monitoring to allow anticipatory optimized insulin therapy. During pregnancy the systematic use of continuous subcutaneous insulin infusion does not seem to be associated with any significant benefit dealing with metabolic control or the perinatal and neonatal morbidity and mortality. In pregnant diabetic patients the usefulness of the dosage of glycated haemoglobin is limited due to the spontaneous fluctuations of this value during pregnancy, as well as the delay of the variation of this index during a period of poor glycemic control. In this condition glycated proteins as fructosamine may be more useful but many technical problems for this determination are still to be solved.

Biomarkers↗
PubMed1990

[Prognosis for requirements for oral antidiabetic agents in Bohemia].

The authors elaborated the prognosis of requirements of oral antidiabetics (PAD) in the CSR, based on the estimate of the number of diabetics, using the method of demographic projection and the estimate of the number of diabetics treated by this therapy. The respective numbers of diabetics are circulated for five-year age-groups, separately for men and women. The need of PAD is derived from the mean daily dose per diabetic patient treated with PAD, separately for biguanides and derivatives of sulphonyl urea. The prognosis respects the basic factors which influence the need of PAD, i.e. the development of the diabetic population, incl. the evolution of its structure, and the development of the attitude to PAD therapy. The application of various assumptions on the future development leads various to variants of the prognosis. Comparison with the actual development is important for evaluation of applied therapeutic methods and for planning purposes. The results of the prognosis indicate that in 1995 the need of PAD in the CSR will vary between 140 and 190% of the consumption in 1980, however, as a result of an uneven development the annual increment could be as high as 19% or there could be a slight drop.

Administration, Oral↗
PubMedDate not supplied

[The forensic chemical determination of antidiabetic agents].

Method of detection, purification and determination of some antidiabetic agents (ADA)--bucarban, butamid, glybenclamid, glybutide, methformine, prediane, chlorpropamide, chlocyclamide, cyclamide in biological material was developed. Microcrystalline reaction with 10% alcoholic potassium iodide, colour reactions and investigation by TLC method both native substances and nitration products were developed to identify ADA. The assay is performed by spectrophotometry. Detection limit is 2-5 mg of each substance in 50 g of the material.

Chromatography, Thin Layer↗
PubMed1988

Antidiabetic sulfonylureas control action potential properties in heart cells via high affinity receptors that are linked to ATP-dependent K+ channels.

Both avian and mammalian heart cells have high affinity receptors for antidiabetic sulfonylureas. The biochemical identification of these receptors has been carried out with [3H]glibenclamide. The Kd values for the most potent sulfonylureas, such as glibenclamide itself, are in the nanomolar range. Comparative studies of structure-function relationships indicate high similarities of binding properties between the sulfonylurea receptors in cardiac cells and insulinoma cells, respectively. The duration of the action potential of guinea pig cardiac cells was drastically reduced by decreasing intracellular ATP concentrations by perfusion or by blockade of oxidative phosphorylation. Glibenclamide was found to restore normal or nearly normal action potential properties in [ATP]in-depleted cardiac cells. Single channel recording using the patch-clamp technique has shown that this effect is associated with high affinity blockade of ATP-sensitive K+ channels by sulfonylureas.

ATP-Binding Cassette Transporters↗
PubMed1989

Antidiabetic effect of a leucocyanidin derivative isolated from the bark of Ficus bengalensis Linn.

A dimethoxy derivative of leucocyandin 3-O-beta-D-galactosyl cellobioside isolated from the bark of F. bengalensis Linn demonstrated antidiabetic action. On oral administration, it decreased blood sugar very significantly both in normal and moderately diabetic rats and increased serum insulin significantly in the latter at a dosage of 250 mg/kg for a 2 hr period. During one month treatment of the diabetic rats orally with the active principle, at a dosage of 100 mg/kg, there was a significant decrease in blood and urine sugar, certain lipid components in serum and tissues and glucose-6-phosphatase activity in liver, but significant increase in body weight and the activities of hexokinase and HMGCOA reductase in tissues as compared to diabetic control. The mechanism of action of the principle may be related to its protective/inhibitory action against the insulin degradative processes.

Animals↗
PubMed1989

[The 2d generation of sulfonylurea antidiabetic agents].

The author gives an account of oral sulphonyl urea antidiabetics of the second generation which are registered in Czechoslovakia. Their pharmacokinetic characteristics are given as the main differentiating sign for their different dosage in otherwise similar indications, contraindications and undesirable effects.

Humans↗
PubMed1986

Regional and international comparison in utilization of antidiabetic drugs.

Data are expressed in the comparable manner through the method of defined daily doses (DDD), which has been adopted for drugs in our country according to the internationally agreed method of drug utilization [Stanulović et al. 1981]. Together with Iceland, Novi Sad had the lowest insulin utilization in 1976, the rate being 1.7 DDD/1000 inhabitants per day. Insulin was used 7.2 times less than in Sweden. However, the utilization of biguanide of 6 DDD/1000 inhabitants per day was 10 times greater than in other European countries. Prescribing rate of preparations of sulfonylurea in Novi Sad was high (8.2 DDD/1000 inhabitants per day); only Sweden came closer to these values. Causes contributing to these differences could be found in the relation between juvenile diabetes and adult onset diabetes as well as in physicians' attitudes towards therapy, in nutritional status and degree of obesity in the population, age structure of population, number of dietitians in the diabetological service, etc. Diabetologists and clinical pharmacologists should explain causes leading to these differences and determine side effects of available antidiabetic drugs, either positive or negative, in order to enable their optimum utilization.

Diabetes Mellitus↗
PubMed1985

Inhibition of 3H-glibenclamide binding to sulfonylurea receptors by oral antidiabetics.

Specific binding of 3H-glibenclamide (HB 419) is observed with membranes from rat cerebral cortex and rat beta-cell tumor. 3H-Glibenclamide binding is of high affinity, reversible, saturable, and can be displaced by oral antidiabetics of different structural types. Half maximal inhibition of binding correlates with the hypoglycemic action of the compounds.

Animals↗
PubMed1983

[Oral antidiabetic agents: recent aspects].

Sulfonylureas are the most potent and widely used oral antidiabetic agents. Despite the finding of possible side effects in a large multicenter trial (UGDP Study) demonstrating increased cardiovascular mortality during tolbutamide therapy, prescription of sulfonylureas has not declined in view of the inconclusive results of the study. In addition, new aspects of their mode of action have been discovered. Sulfonylureas may enhance insulin sensitivity of peripheral tissues, particularly by raising the decreased number of insulin receptors in type II diabetics. While this extrapancreatic effect appears to be quantitatively important, it is only present when insulin secretion is simultaneously stimulated. Insulin release is enhanced due to an increase in the sensitivity of the B-cell to glucose challenge. There is evidence to suggest that the extrapancreatic effect of sulfonylureas is secondary to their pancreatic effect. Pointers in the same direction emerged from our own results in a study on the influence of sulfonylureas added to insulin therapy on insulin sensitivity in type I diabetics. Sulfonylureas failed to increase insulin sensitivity and insulin requirements in these patients. The first generation compounds of sulfonylureas are associated with more side effects and drug interactions than the second generation preparations. However, the latter are more frequently associated with hypoglycemia since they are more potent and have a prolonged duration of action. Biguanides have almost fallen into disuse as therapeutic agents due to the potentially lethal complication of lactic acidosis. Only metformin may still be indicated in certain cases. Inhibitors of intestinal amylase and glucosidase represent a new therapeutic principle in diabetes therapy whose aim is to reduce postprandial hyperglycemia. Their value as therapeutic agents is not yet clearly established.

Administration, Oral↗
PubMed1982

Antidiabetic effects of lithium.

Lithium carbonate was administered to a female manic depressive patient who also had maturity onset diabetes mellitus. She was found to have lowered blood glucose levels with administration of lithium without change in the other variables which could effect blood glucose levels. In could be concluded that lithium carbonate had antidiabetic effects in this case.

Bipolar Disorder↗
PubMedDate not supplied

Effect of the antidiabetic treatment of hyperlipoproteinemia in newly detected diabetes mellitus.

A parallel study concerning the influence of antidiabetic treatment of the carbohydrate and lipid disturbances were carried out in 209 patients with newly discovered diabetes mellitus: 120 females and 89 males, ranging in age from 28 to 73 years. The treatment applied in terms of the clinical from of the disease was: insulin in 12 cases, tolbutamide in 25 cases, glurenorm (a sulphenyl urea derivative in 114 cases, biguanide in 45 cases, tolbutamide associated with biguanide in 13 cases. After 60 days of treatment, the incidence of HLP fell from 55.02% to 43.06% (in 90 of 209 cases), with a change in the distribution of the five HLP types. Parallel analysis of blood glucose, triglycerides (Tg) and cholesterol (Ch) revealed appraisable differences in the post-therapeutic evolution of the three biochemical parameters in terms of the treatment applied. A statistically significant, parallel and comparable decrease in glycemia, Tg and Ch was recorded after insulin and glurenorm; biguanides lowered only glycemia and Tg, and tolbutamide only glycemia. The fact that correction of carbohydrate disturbances is accompanied by a significant decrease only of Tg and not of Ch suggests that the pathophysiologic mechanisms by which these lipid fractions are modified in diabetes mellitus, differ and are probably independent on one another. The close relationship between the weight excess and plasma Tg (but not also plasma Ch) levels, likewise lends support to this assumption.

Adult↗