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PubMed1988

Clinically significant diuretic-induced glucose intolerance.

Diuretic-induced glucose intolerance is cited frequently as a problem of only limited clinical significance. In certain populations, such as Mexican-Americans, this effect may be much more dramatic. A 50-year-old obese Mexican-American woman presented with a three-month history of increased thirst and frequent urination. A fasting blood glucose concentration of 365 mg/dL prompted initiation of chlorpropamide therapy. A review of her medical history revealed that a thiazide diuretic was started six months previously. A reduction in thiazide dose and potassium supplementation together with chlorpropamide therapy controlled the patient's blood glucose. Subsequently, all three medications were discontinued, and the patient remained normoglycemic during a full year of follow-up. The temporal relationship between symptomatic diabetes and hydrochlorothiazide therapy incriminates the diuretic as the most probable cause.

Benzothiadiazines↗
PubMed1987

Bezafibrate and fenofibrate in type II diabetics with hyperlipoproteinaemia.

A double-blind study was carried out in 64 Type II diabetic patients, controlled with diet therapy and sulphonylureas (glibenclamide or chlorpropamide), who had associated hyperlipoproteinaemia which could not be normalized during a run-in period of 2 months by hygiene and dietary measures alone. The patients were allocated at random into 4 groups and each group was treated over 4 months with bezafibrate (600 mg/day) or fenofibrate (300 mg/day) in addition to their glibenclamide (5 to 15 mg/day) or chlorpropamide (250 to 500 mg/day) therapy plus diet. The results of monthly laboratory investigations showed that both hypolipaemic agents produced significant reductions in serum triglycerides, total cholesterol and LDL cholesterol and an increase in HDL cholesterol. There was a significantly greater increase in HDL cholesterol in patients treated with bezafibrate and glibenclamide, particularly in women, and greater control of blood glucose in those on bezafibrate. Both hypolipaemic drugs were well tolerated. Slight increases were recorded in serum transaminases in fenofibrate patients and in bleeding time in bezafibrate patients. It is concluded that, because of its greater effect on blood glucose and HDL cholesterol, the combination of bezafibrate with glibenclamide would appear to be the best of the regimens studied for the treatment of non-insulin-dependent diabetics with associated hyperlipoproteinaemia.

Adult↗
PubMedDate not supplied

Hypoglycemic effect of methanolic extract of Musa paradisiaca (Musaceae) green fruits in normal and diabetic mice.

Diabetes mellitus is a debilitating hormonal disorder in which strict glycemic control and prevention of associated complications are of crucial importance. This study was designed to evaluate the hypoglycemic effect of methanolic extract of mature, green fruits of Musa paradisiaca (MEMP) in normal (normoglycemic) and streptozotocin (STZ)-treated, diabetic (hyperglycemic) mice, using chlorpropamide as the reference antidiabetic agent. MEMP (100-800 mg/kg p.o.) induced significant, dose-related (p < 0.05-0.001) reductions in the blood glucose concentrations of both normal and diabetic mice. Chlorpropamide (250 mg/kg p.o.) also produced significant (p < 0.01-0.001) reductions in the blood glucose concentrations of normal and diabetic mice. The results of this experimental study indicate that, in the mammalian model used, MEMP possesses hypoglycemic activity. Although the precise mechanism of the hypoglycemic action of MEMP is still unclear and will have to await further studies, it could be due, at least in part, to stimulation of insulin production and subsequent glucose utilization. Nevertheless, the findings of this experimental animal study indicate that MEMP possesses hypoglycemic activity, and thus lends credence to the suggested folkloric use of the plant in the management and/or control of adult-onset, type-2 diabetic mellitus among the Yoruba-speaking people of South-Western Nigeria.

Animals↗
PubMed2005

Identification and quantification of 8 sulfonylureas with clinical toxicology interest by liquid chromatography-ion-trap tandem mass spectrometry and library searching.

BACKGROUND: Identification of sulfonylureas in blood may be useful in the evaluation of hypoglycemic crises of unknown origin. The aim of the present study was to develop a highly selective liquid chromatography-electrospray tandem mass spectrometry (MS-MS) method using an ion-trap detector for rapid screening, identification, and quantification of sulfonylureas in human plasma. METHODS: After standard liquid-liquid extraction with glisoxepide as an internal standard, 8 sulfonylureas (glibenclamide, glipizide, gliclazide, glibornuride, glimepiride, carbutamide, chlorpropamide, and tolbutamide) were eluted from a C18 column within 10 min with an isocratic mobile phase. Drugs were identified and quantified in full-scan MS-MS mode by use of a homemade MS-MS library. We used the assay in 134 cases of hypoglycemic crises of unknown origin. RESULTS: No ion suppression effect was noted for the analytes at their specific retention-time windows. For all drugs, assay validation showed good linearity (r2>0.990) and acceptable imprecision and recovery based on commonly used criteria of acceptance. The mean extraction recoveries were 63%-87% for 5 sulfonylureas but <45% for 3 (carbutamide, chlorpropamide, and tolbutamide). Nevertheless, the high sensitivity of the MS instrument made possible detection and quantification of all 8 drugs at subtherapeutic to toxic concentrations with good precision. Sulfonylureas were found in 9 hypoglycemic patients. CONCLUSION: The described assay method allows accurate, rapid identification and quantification of 8 sulfonylureas in human plasma and can be used for specific diagnosis of factitious hypoglycemia caused by ingestion of these drugs.

Chromatography, Liquid↗
PubMed1996

Five year retrospective evaluation of sulfonylurea ingestion in children.

BACKGROUND: Oral hypoglycemic medications are frequently used for Type II diabetes and accidental ingestions by children may occur. There are no comprehensive pediatric studies documenting poison center experiences. STUDY OBJECTIVE: To evaluate the toxicity of oral sulfonylurea ingestion in children and the efficacy of treatments instituted in these cases. METHOD: Retrospective review of all ingestions of oral sulfonylureas reported to a single regional poison control center 1987-1991. RESULTS: Ninety-three cases were identified, one to 16 years old (mean of 3.5 years). Eighty cases (86%) were less than six years of age. Of the six medications used, three, chlorpropamide, glipizide and glyburide made up 88 (95%) cases. Twenty-five patients (27%) became hypoglycemic (glucose < 60 mg/dL). The mean minimum blood glucose in these patients was 46.5 mg/dL (minimum 20 mg/dL). Time of onset of hypoglycemia ranged from 0.5 to 16 h (mean 4.3 h; median 2 h). Only four patients had the onset of chemical hypoglycemia more than four hours postexposure. Persistent hypoglycemia occurred in nine children (10%) despite intravenous glucose therapy. There were no seizures. Mean time to decontamination of patients with and without hypoglycemia was 1.4 and 1.2 h respectively. Intravenous glucose of the following concentrations was administered: 5% (40), 10% (15), 20% (1), and 50% (3). Accidental ingestion of a single tablet of chlorpropamide (250 mg), glipizide (5 mg). and glyburide (2.5 mg) each produced hypoglycemia in children ages one to four years. Accidental ingestion of 5-10 mg glyburide produced a blood glucose of 57 mg/dL in an 11-year-old child. All patients recovered fully. There were no neurological sequelae noted. CONCLUSION: Children ingesting oral hypoglycemics should be admitted to a health care facility for 24 h observation. In this series a single tablet produced hypoglycemia.

Adolescent↗
PubMed1976

Effect on carbohydrate metabolism of hypotensive adrenergic neurone blocking agents.

In subjects with normal metabolism sugar tolerance was not appreciable influenced by 4 or 5-day courses of guanethidine and guanazodine. Upon perfusion in isolated rat liver, glycogen metabolism and hepatic sugar release were increased by guanazodine, guanethidine and debrisoquine alike. However, when these drugs were used simultaneously with chlorpropamide debrisoquine proved to be the weakest in counteracting the inhibitory effect of chlorpropamide on glycogen metabolism and sugar release. The observation may have clinical significance.

Adolescent↗
PubMed1990

Antidiabetic agents.

Although either insulin or oral hypoglycemics may be used in conjunction with diet and exercise in the management of type II diabetes, drug therapy for type I diabetes involves only insulin. C-peptide levels can be tested to assess whether the patient has remaining pancreatic endocrine function. Patients being started on insulin for the first time should receive a single injection of an intermediate-acting insulin of "human" origin at a dose of approximately 0.5 U/kg. Thereafter, fasting, mid-morning, mid-afternoon, bedtime, and possibly early morning blood sugars should be examined periodically to determine if the insulin dose needs to be increased, decreased, split, or if the patient needs to be on a two-insulin regimen. Intensive insulin therapy has become commonplace to control plasma glucose levels in the majority of patients receiving insulin therapy. Proper patient education regarding the insulin regimen, injection techniques, blood glucose monitoring, as well as diet, exercise, and foot care are essential if the patient's diabetes is to be controlled adequately. Guidelines for "adequate" glycemic control are outlined in Table 6. Recent evidence suggests that tight control of plasma glucose levels may decrease the macrovascular complications of diabetes. Although there is also evidence to suggest that the onset of microvascular complications might be delayed with strict glycemic control, the data are conflicting. The benefits of strict control must be weighted against the problems of hypoglycemia experienced by many patients who attempt tight control of their blood glucose levels. Biguanide compounds are available in Europe, but the sulfonylureas comprise the only class of oral agents in the United States commercially available for the treatment of type II diabetes. The two generations of these drugs reflect their potency and possible side-effect profiles. Of the first-generation agents, tolbutamide and chlorpropamide are the most widely prescribed. Tolbutamide is the weakest of the sulfonylureas, possibly making it a good drug for initiating oral therapy in the elderly. Chlorpropamide is becoming a less popular agent because of its long duration of action and its increased incidence of side effects. Of the second-generation agents, glyburide offers a better dosing schedule (once daily compared with twice daily for glipizide); however, glyburide may produce a greater incidence of hypoglycemia, particularly in the elderly or in patients with significant renal impairment. There are few good studies comparing these two drugs so that recommending one over the other is difficult. Drug interactions are numerous with the first-generation drugs, but less so with the newer second-generation agents.(ABSTRACT TRUNCATED AT 400 WORDS)

Diabetes Mellitus↗
PubMedDate not supplied

Non-insulin-dependent diabetes: 10-year outcome in relation to initial response to diet and subsequent sulfonylurea therapy.

Thirty-eight non-insulin-dependent diabetic patients within 130% of desirable body weight were given a 100-g oral glucose tolerance test (OGTT) at diagnosis and after at least 1 mo of dietary treatment with energy and carbohydrate restriction. Thirteen "responders" showed an improvement in fasting blood glucose, glucose tolerance, and insulin secretion, with near-normalization of plasma, lactate, pyruvate, free fatty acids, glycerol, and ketone bodies. There were no significant changes in the 25 "non-responders." The responders were, at diagnosis, heavier than the non-responders (75.5 versus 64.3 kg, P less than 0.01). Twenty non-responders subsequently completed a prospective controlled study of glibenclamide, chlorpropamide, and placebo lasting for 16 mo with OGTTs at the end of each 4-mo treatment phase. The results showed that there were no significant differences between the metabolic effects of glibenclamide and chlorpropamide. On active treatment, insulin levels rose coincident with a fall in fasting blood glucose and an improvement in glucose tolerance and near-normalization of plasma lactate, pyruvate, free fatty acids, glycerol, and ketone bodies, all of which relapsed to initial values after placebo. Ten years after the initial study, 29 of the original patients were traced and reviewed and the outcome related to their earlier tests. Twenty-two percent of the responders and 70% of the non-responders were now on insulin (P less than 0.02); the initial insulin response to OGTT at the end of the diet treatment was significantly lower in those subsequently treated with insulin (P less than 0.01).(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗
PubMed1982

Facial and sublingual temperature changes following intravenous glucose injection in diabetics.

Facial and sublingual temperatures were measured in 61 diabetics undergoing intravenous glucose tolerance tests. Within 2 minutes of starting glucose injection, 58 patients felt warm in the face and trunk, 56 showed a rise in cheek temperature and 23 had visible facial reddening. The most important determinant of cheek temperature rise was initial cheek temperature. Cheek temperature rise was a unimodally distributed variable and was significantly larger in patients with fasting plasma glucose greater than or equal to 6.1 mmol/l than in those with lower glucose (despite similar initial cheek temperatures). Initial cheek temperature correlated with ambient temperature in men with fasting glucose greater than or equal to 6.1 mmol/l but not in those with fasting glucose less than or equal to 6.0 mmol/l nor in women. Initial tongue temperature was also related to ambient temperature in men but not in women and fell following the glucose injection. Although the glucose flush differs from the the chlorpropamide-alcohol flush in its unimodal distribution and relatively small temperature rise, some of the factors which influence reaction could well be considered with benefit in analysis of the chlorpropamide-alcohol flush, in particular the initial cheek (and ambient) temperatures, sex and fasting plasma glucose concentration.

Blood Glucose↗
PubMed1997

Studies on the phototoxic effects of oral antidiabetics and diuretics.

A number of sulphonamide derived oral antidiabetics (chlorpropamide, glibenclamide, glipizide, gliquidone, glymidine, tolazamide and tolbutamide) and diuretics (bemetizide, bendroflumethiazide, benzylhydrochlorothaizide, bumetanide, butizide, chlortalidone, furosemide, hydrochlorothiazide, hydroflumethiazide, indapamide, piretanide, polythiazide, trichlormethiazide and xipamide) were investigated for phototoxicity in a cell culture model. Cell death dependent on UVA fluence and test substance concentration was observed in the presence of the oral antidiabetics glibenclamide and gliquidone, as well as the diuretics bemetizide, bendroflumethiazide, benzylhydroxhlorothiazide, bumetanide, butizide, hydrochlorothiazide, hydroflumethiazide, piretanide, polythiazide and trichlormethiazide. Bendroflumethiazide was phototoxic at 5 x 10(-5) mol/l and higher concentrations, bemetizide, benzylhydrochlorothiazide, bumetanide and hydroflumethiazide were phototoxic at 2.5 x 10(-4) mol/l and higher concentrations, and the oral antidiabetics glibenclamide and gliquidone as well as the diuretics butizide, hydrochlorothiazide, piretanide, polythiazide and trichlormethiazide were phototoxic at 5 x 10(-4) mol/l and higher concentrations. The oral antidiabetics chlorpropamide, glipizide, glymidine, tolazamide and tolbutamide as well as the diuretics chlortalidone, furosemide, indapamide and xipamide did not induce phototoxicity in this assay.

Carcinoma in Situ↗
PubMed1986

The mechanisms of sulfonylurea-induced immune hemolysis: case report and review of the literature.

Chlorpropamide, a sulfonylurea antidiabetic drug, was found to be the etiologic agent in a patient with immune hemolytic anemia. Hemolysis was severe, and ceased promptly when the drug was discontinued. The direct antiglobulin test was positive for complement, and the indirect antiglobulin test was also positive when the drug, patient serum, and fresh serum complement were all present. In this patient, and in four other patients described in the literature, hemolysis was mediated by the immune complex mechanism. In reports of two other patients taking a sulfonylurea drug, a milder form of hemolysis was mediated by the hapten mechanism. Sulfonylurea drugs are widely used. Since immune complex-mediated hemolysis in these patients is dramatic, it is not likely to be missed. However, the slower, milder hemolysis mediated by the hapten mechanism may be more common than is realized. Such patients may have only mild anemia and a near-normal reticulocyte count, making the diagnosis difficult. It is thus important to consider drug-immune hemolysis in patients who become anemic while taking sulfonylurea drugs.

Anemia, Hemolytic, Autoimmune↗
PubMed1976

Gas chromatographic and mass spectrometric analysis of the products of methylation of sulfonylurea drugs.

Gas chromatographic analysis of the products of reaction of diazomethane with tolbutamide and chlorpropamide indicates the formation of three compounds in both cases. As expected, N-methylation (at sulfonamide nitrogen) is the predominant reaction; minor amounts of O-methylated product are also observed. The third product in both cases is the N-methylsulfonamide formed by decomposition of the N-methylated sulfonylurea during gas chromatography. Electron impact and chemulfonylurea during gas chromatography. Electron impact and chemical ionization mass spectrometric analysis, as well as 1H nuclear magnetic resonance examination of samples collected from gas chromatography, confirm the structural assignments. Additionally, proton magnetic resonance analysis of the crude reaction products established that N-methylsulfonamides are not formed in the course of the diazomethane reaction and that the O-methylated derivatives are true products of the reaction. The use of a paramagnetic shift reagent allowed direct estimation of the ratios of N- to O-methylation, and the demonstration that these ratios are not vitiated during gas chromatographic analysis.

Chemical Phenomena↗
PubMedDate not supplied

Glyburide: a second-generation sulfonylurea hypoglycemic agent. History, chemistry, metabolism, pharmacokinetics, clinical use and adverse effects.

Glyburide, a second-generation hypoglycemic sulfonylurea, is 200 times as potent as tolbutamide. This increase is due to greater intrinsic hypoglycemic potency of the molecule rather than to a prolonged biologic half-life. Glyburide is inactivated by the liver to 4-trans-hydroxyglyburide and 3-cis-hydroxyglyburide; 50% of these compounds is excreted in the urine and 50% in the bile. Although the serum concentration of glyburide can be measured by radioimmunoassay and high-performance liquid chromatography, the importance of its serum concentration in the reduction of hyperglycemia is not yet established. Glyburide has a therapeutic effectiveness comparable to that of the first-generation sulfonylurea chlorpropamide; however, it has a lower frequency of adverse effects. To date it has a low frequency of clinically significant interactions with other drugs. Glyburide should not be prescribed for patients with liver disease or significant renal disease. Because glyburide is a potent hypoglycemic agent, it should be prescribed in small initial doses, particularly for elderly patients with diabetes. At the present time there is no definite evidence that it modifies the increased risk of cardiovascular disease of diabetic patients. Although glyburide is a potent stimulator of pancreatic insulin secretion after short-term administration, an additional mechanism of action during long-term administration is to decrease the resistance of muscle and liver to the action of insulin. It is a useful medication for patients with type II diabetes whose hyperglycemia is not adequately reduced by dietary management and exercise. It can be used as the initial drug in these patients or as the replacement drug for those with primary or secondary failure during therapy with first-generation sulfonylureas.

Animals↗
PubMed1981

High-performance liquid chromatographic assay of tolbutamide and carboxytolbutamide in human plasma.

A high-performance liquid chromatographic method was developed for the simultaneous measurement of tolbutamide and its major metabolite, carboxytolbutamide, in plasma. The assay involves the ether extraction of 1 ml of plasma, using chlorpropamide and an internal standard. The extract is dried, the residue is taken up in acetonitrile, and 5 micro l is injected into a reversed-phase column. The mobile phase consisted of 35% acetonitrile and 65% 0.05 M phosphoric acid buffer (pH 3.9). A fixed-wavelength detector was set at 254 nm. The sensitivity limits for the tolbutamide and carboxytolbutamide assay were 2 and 0.1 microgram/ml, respectively. The ratio of carboxytolbutamide to tolbutamide in plasma obtained from a subject given a 500-mg tolbutamide tablet was 1:20.

Chlorpropamide↗
PubMed2000

Identification of sulfonylureas in serum by electrospray mass spectrometry.

Identification of sulfonylureas in serum is important in the diagnosis of hypoglycemic crisis of unknown origin. Methods based on HPLC with UV or fluorescence detection may give false positive results. Mass spectrometry may successfully avoid this problem. The described method allows the simultaneous identification and quantification of tolbutamide, chlorpropamide, glibenclamide, and glipizide in human serum using one of the tested sulfonylureas as the internal standard. Serum purification is carried out by solid-phase extraction with ENVI-C18 cartridges and samples are analyzed by liquid chromatography-electrospray mass spectrometry. For all drugs, the limit of detection and the limit of quantification are about 2 and 10 ng/ml, respectively.

Calibration↗
PubMed1984

Monitoring patients on long-term drug therapy for genotoxic effects.

The problems associated with the design and conduct of experiments involving surveys of human population sister chromatid exchange (SCE) frequencies are discussed. It is suggested that the problems of variation between culture occasions may be overcome by the rigid control of experimental conditions and the inclusion of the same negative controls (herein called "base controls") on all culture occasions. In addition, all experimental subjects are cultured, as far as possible, at the same time as controls drawn from the same population and matched for age (+/- 5 yr) and sex. Many factors in such surveys remain uncontrolled but the collection of data on potential environmental mutagen exposure in all subjects is suggested as a mechanism to measure and evaluate such factors. Data are reported on SCE frequencies in lymphocytes from patients receiving 4 separate drugs for chronic conditions. Using a square root transformation of SCE frequencies and the analysis of variance, there is clear evidence for a rise in SCE frequency in patients receiving sulphasalazine (SASP) and azathioprine (Aza). On the other hand, patients receiving atenolol or chlorpropamide show no evidence of a rise in SCE frequency.

Atenolol↗
PubMed1976

Effect of inhibitors of sterol biosynthesis on growth and sexuality of Pythium and Zygorhynchus.

Seven commercial inhibitors of sterol biosynthesis were tested for their effect upon vegatative growth and sexuality in Pythium acanthicum and Zygorhynchus moelleri. Five compounds (SKF 525, Chlorpropamide, Tolbutamide, Benzmalacene, AY 9944) inhibited both growth and sexuality of both fungi and two (SKF 7732 and SKF 7997) were ineffective. Pythium was more sensitive to the activity of the inhibitors than was Zygorhynchus. None of the compounds tested inhibited sexuality without similarly reducing vegetative growth.

Chlorpropamide↗
PubMed1980

Irregular drug intake and serum chlorpropaminde concentrations.

In patients with maturity onset diabetes serum chlorpropamide concentrations (s-CPA) and fasting blood glucose (FBG) were measured before and after self recording of drug intake in order to evaluate the role of compliance with the therapeutic regimen in variation in s-CPA and clinical outcome. Nine out of 57 patients (16%) had to be excluded because they did not comply with the clinical routines and the test procedure. Of the remaining 48 patients, only two recorded small deviations from the prescribed dosage, and nine (19%) noted variations in medication time of more than +/- 2h. By contrast, irregular drug intake was indicated in 29 of the 48 patients (60%) based on statistical evaluation of changes in s-CPA. Clinical control (FBG) was influenced significantly in only half of these 29 patients. Improved adherence to the dietary regimen was observed in 12 of the 48 patients (25%). Patient medication behaviour seems to be an important determination of variation in s-CPA, and is as important as adherence to the dietary regimen in clinical control of "drug requiring" patients with maturity onset diabetes.

Aged↗