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At least 721 records · Page 40Linked to original sources
PubMed1986

Prevalence of diabetes mellitus treated with insulin and oral hypoglycemic agents in Denmark.

During a period of 12 months all diabetics treated with insulin or oral hypoglycemic agents (OHA) were registered by collection of prescriptions on the island of Falster, Denmark, with 44,498 inhabitants. The overall prevalence of diabetes mellitus was 12.4 per 1,000 (553 diabetics). Insulin-treated diabetics comprised 231 persons (prevalence rate 5.2 per 1,000) and OHA-treated diabetics comprised 322 persons (prevalence rate 7.2 per 1,000). The prevalence of insulin-treated diabetes especially with an age less than 30 yr was significantly higher than the prevalence in 2 other areas in Denmark. 50% of the insulin-treated diabetics with an onset age greater than or equal to 30 yr were overweight in contrast to 6% of insulin-treated diabetics with an onset age less than 30 yr (p less than 0.01). Among OHA-treated diabetics, 65% were overweight.

Age Factors↗
PubMedDate not supplied

[Comparative evaluation of the hypoglycemic activity of the vegetal complex of Phaseolus vulgaris and chlorpropamide in experimental diabetes].

Experiments on rabbits with alloxan diabetes showed that the plant complex (PC) reduced the level of glycemia after single administration for 6-8 h by 27-32%. A similar effect was demonstrated with chlorpropamide. However the PC produced a longer hypoglycemic effect. In course treatment the PC returned the blood level of glucose (5.14 +/- 0.62 mmol/l) to normal on the 11th day whereas with chlorpropamide this indicator was almost normal (6.6 +/- 1.1 mmol/l) on the 15th day only. A rapid decrease in the blood glucose concentration caused by the PC was observed in AIS induced hyperglycemia. The PC demonstrated its sugar reducing action by extrapancreatic means.

Alloxan↗
PubMed1979

Hypoglycemic effect of Opuntia cactus.

Nopal (Opuntia sp.) has been traditionally used by the Mexican population for the treatment of diabetes mellitus. The purpose of this work is to describe effects produced by directly liquified nopal and extracts from this plant in healthy and pancreatectomized rabbits. Preliminary results allow us to conclude that Opuntia streptacantha, Lemaire, has hypoglycemic properties when orally administered, in animals with experimentally induced diabetes as well as in healthy ones with physiologic hyperglycemia.

Administration, Oral↗
PubMed1978

Hypoglycemic activity of amine derivatives. A possible mode of action.

Experiments were carried out to explain the hypoglycemic effect of dicyclohexylamine (DCH) and related compounds. The agents antagonized blood glucose increase in intact and hepatectomized rats infused with glucose, but not in intact rats receiving epinephrine, and induced liver glycogen rise in normal fasted but not in adrenalectomized rats. No effect on blood glucose of pancreatectomized dogs was found. DCH lowered blood triglycerides without influencing the concentration of plasma fatty acids. Intestinal absorption of glucose was not influenced by low concentrations of the amines. Hypoglycemia may result, at least in part, from stimulated glucose transformation in the muscle tissue without an enhancement of anaerobic glycolysis.

Adipose Tissue↗
PubMed1983

Effect of the oral hypoglycemic agent pirogliride (McN-3495) on glycogen levels of normal and diabetic rats.

Pirogliride, a new oral hypoglycemic agent unrelated structurally or mechanistically to either the sulfonylureas or biguanides, produced a dose-dependent increase in liver but not muscle glycogen levels of fasted non-diabetic rats and produced at 100 mg/kg, p.o. a modest increase in liver but not gastrocnemius muscle glycogen of fasted streptozotocin diabetic rats. This liver glycogenic effect of pirogliride was similar to that obtained using insulin but differed from the decrease of liver glycogen levels which occurred following acute phenformin treatment.

Animals↗
PubMed1984

Sulfonyliminoimidazolidines, a new class of oral hypoglycemic agents. 4. Toxicity and general pharmacology of 1-[p-[2-(crotonylamino)-ethyl]-phenylsulfonyl]-3-cyclohexy l-2-imino- imidazolidine (CGP 11 112).

Results of a first segment of toxicity tests and general pharmacological investigations with 1-[p-[2-(crotonylamino)-ethyl]-phenylsulfonyl]-3-cyclohexyl- 2- iminoimidazolidine (CGP 11 112), a potent new oral hypoglycemic agent, are reported. The acute LD50 in rats was 600 mg/kg p.o. and 25 mg/kg i.v. In a range finding study doses of 60 mg/kg p.o. and 10 mg/kg i.p., administered daily for 10 days, were tolerated without symptoms in rats, and 30 mg/kg p.o. produced no unequivocal toxic effects in dogs. Slight and transient increases of blood pressure were observed in anaesthetized cats at doses of 0.3 mg/kg i.v. and above. 3 mg/kg i.v. (1/10 LD) caused a transient blood pressure decrease. Heart rate, tidal volume and blood pressure effects of epinephrine (adrenaline), norepinephrine (noradrenaline) and acetylcholine were not significantly influenced in a dose range from 0.01 to 1.0 mg/kg i.v. In isolated organ segments, CGP 11 112 produced only unspecific effects at high concentrations. No intrinsic activity, but antagonism against BaCl2-induced contractions were observed in isolated guinea-pig ileum (one third papaverine hydrochloride). Rate and force of contraction of isolated guinea-pig atria were not affected up to 2.4 mumol/l; higher concentrations were cardiodepressant. In rats, CGP 11 112 increased the excretion of urine, sodium and chloride, but not potassium, dose-dependently (range 10-100 mg/kg). Similar effects observed in dogs suggest that the compound may affect fluid and electrolyte balance at high doses. Moderate antiphlogistic activity (ED40 10-40 mg/kg) was observed in the carrageenin-induced rat paw oedema.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Oral↗
PubMed1983

Derivatives of 4,5,6,7-tetrahydro-7,8,8-trimethyl-3-phenylamino-4,7-methano-2H-indazole with hypoglycemic and hypotensive activities.

By reaction of camphor enamine (I) with phenyl isothiocyanate, the N-phenyl thiocarboxamide (II) was obtained in excellent yield, and in turn gave 4,5,6,7-tetrahydro-7,8,8-trimethyl-3-phenylamino-4,7-methano-2H-indazole (III) in very good yield by reaction with hydrazine hydrate. A series of N-substituted ureas (IV) were synthesized in satisfactory yield by reaction of (III) with alkyl and aryl isocyanates. Ureas (IV) showed in general hypoglycemic and in some cases hypotensive activity in rats, whereas only hypotensive activity was present in the thiocarboxamide (II). Effects on heart rate, antiinflammatory and antipyretic activities in rats, infiltration anesthesia and antiarrhythmic activity in mice, as well as antiacetylcholine activity in vitro, are also reported.

Anesthesia, Intravenous↗
PubMed1984

Derivatives of 4,5,6,7-tetrahydro-7,8,8-trimethyl-3-phenylamino-4,7-methano-2H-ind azo le with hypotensive and hypoglycemic activities. II.

A series of N-substituted thioureas (II) and some ureas (III) were synthesized in excellent yields by reaction of 4,5,6,7-tetrahydro-7,8,8-trimethyl-3-phenylamino-4,7-methano-2H-indazole with alkyl, aryl isothiocyanates and isocyanates, respectively. On the whole compounds (II) and (III) showed hypotensive and in some cases hypoglycemic activity in rats. Effects on heart rate in rats, infiltration anesthesia in mice and antiacetylcholine activity in vitro are also reported.

Acetylcholine↗
PubMedDate not supplied

[Comparative evaluation of the hypoglycemic effect of the 2d-generation sulfonylurea preparations maninil and diamicron in diabetes mellitus].

Glycemia level and diurnal glucosuria were studied in the morning, afternoon and evening in a group of 27 patients with insulin-dependent diabetes mellitus before and after diamicron therapy for 1.5 to 3 months. A similar investigation was performed in a group of 20 patients, suffering from diabetes mellitus of the second type before and following maninil treatment during 1.5 to 2 months. It was shown that diamicron exerts a more pronounced sugar-lowering effect in comparison with that of maninil. It promotes stable glycemia development and should take an appropriate place among hypoglycemics used now in diabetology.

Adult↗
PubMedDate not supplied

[Resistance to hypoglycemic sulfanilamides and biguanidines and its immune genesis].

In blood of patients with diabetes mellitus receiving bucarban or adebit antibodies to these drugs were discovered. Patients medicated with bucarban demonstrated an elevated content of antibodies to insulin. The appearance of specific antibodies occurred in rabbits and rats following introduction of bucarban, glucophage or adebit per se or when mixed with adjuvants. An increased production of antibodies to endogenous insulin was observed in all animals reveiving bucarban. Introduction to rats of inactivated (at 56 degrees C for 30 minutes) serum of patients with diabetes mellitus that contained antibodies to bucarban or adebit as well as immune rabbit sera greatly mitigated the hypoglycemic effect of the latter. Introduction to rats of the blood serum taken in patients reveiving bucarban allso attenuated the effect of exogenous insulin. These findings suggest that, possessing neutralizing properties, these antibodies to bucarban, adebit and glucophage cause habituation to these substances. Accumulation in the blood of autoantibodies to insulin following introduction of bacarban reduces the sensitivity to the exogenous hormone and manifests the existence of an immune mechanism securing the preservation of chemical homeostasis in the organism.

Administration, Oral↗
PubMed1982

Effect of oral hypoglycemic drugs on heart norepinephrine (NE) in rats and mice.

We studied the effect of oral hypoglycemic drugs on heart NE in normal and diabetic animals as a possible model for obtaining some insight into the mechanism for the alleged cardiotoxicity of these drugs in diabetic humans. The biguanides, but not the sulfonylureas, lowered NE in the hearts of rats and mice. Our results indicate this effect is not due to changes in blood glucose or a metabolite of the biguanides, but do not completely rule out an effect on biosynthesis or interference with the NE uptake pump in the adrenergic nerve endings. However, the data identify the biguanide portion of the molecule to be the active moiety and suggest that an indirect toxic effect of the drug probably is involved.

Animals↗
PubMed1982

Lack of Ca2+ ionophoretic activity of hypoglycemic sulfonylureas in excitable cells and isolated secretory granules.

Beta-Cell-rich pancreatic islets, neurohypophyses, and adrenal medullae were used for exploring whether hypoglycemic sulfonylureas exhibit Ca2+ ionophoretic properties. Exposure of these excitable organs to depolarizing concentrations of K+ resulted in stimulation both of 45Ca uptake and efflux. Although tolbutamide does not bind preferentially to pancreatic islets, this sulfonylurea was specific in stimulating the fluxes of 45Ca in these endocrine specimens. A chromaffin granule preparation was used for studies of both the net transport of Ca2+ with the metallochromic indicator arsenazo III and the proton concentration gradient (delta pH) with the fluorescent probe 9-aminoacridine. Even at high concentrations, tolbutamide and glibenclamide did not mediate Ca2+ -H+ exchange diffusion whether or not the granules were made permeable to protons by the addition of the protonophore carbonyl cyanide rho-trifluoromethoxyphenylhydrazone, nor did the sulfonylureas affect Ca2+ -H+ exchange diffusion induced by the addition of A-23187. The data indicate that the Ca2+ fluxes associated with sulfonylurea-stimulated insulin secretion do not result from the Ca2+ -ionophoretic properties of the drugs but rather reflect depolarization of the beta-cells.

Animals↗
PubMedDate not supplied

Pharmacokinetics of a new hypoglycemic agent SPC-703.

Pharmacokinetic of a new hypoglycemic agent, SPC-703 was studied in rats after iv, ip and po administration of two doses of the drug. It was found that biological half-time (t 1/2) did not depend upon the route of administration, t 1/2 value was 12.5-13.8 hr. There was no statistically significant difference in the pharmacokinetic parameters of SPC-703 after administration of two doses, 25 and 50 mg/kg of the drug. The volume of distribution of the unbound to serum protein SPC-703 was 93 ml, the volume of distribution assayed for the total amount of SPC-703 was 42.4 ml. SPC-703 in humans was absorbed rapidly from the gastrointestinal tract to the general circulation, ka = 1.21 hr-1, half-time of absorption was 0.65 hg (39 min). The volume of distribution of absorbed SPC-703 Vd/F was 10.1 l.

Animals↗
PubMed1995

Hypoglycemic action of Murraya koenigii (curry leaf) and Brassica juncea (mustard): mechanism of action.

Effect of Murraya koenigii and Brassica juncea on carbohydrate metabolism has been studied using rats as experimental animals. Both showed significant hypoglycemic action. There was increase in the concentration of hepatic glycogen and glycogenesis, as evident from the increased activity of glycogen synthetase, and decrease in glycogenolysis and gluconeogenesis as evident from the decreased activity of glycogen phosphorylase and gluconeogenic enzymes.

Animals↗
PubMedDate not supplied

[A comparative evaluation of the hypoglycemic activity of acetyl-alpha-carnitine and chlorpropamide in experimental diabetes].

The comparison of the action shown by acetyl-alpha-carnitine and chloropropamide in rabbits with experimental diabetes has demonstrated that the former has a more pronounced hypoglycemic action. In combined administration, acetyl-alpha-carnitine substantially enhanced the effects of chloropropamide in the animals with experimental diabetes, which should be taken into account by clinicians in its use.

Acetylcarnitine↗
PubMed1994

[An animal model for testing hypoglycemic and hypolipidemic drugs].

A new animal model of hyperglycemia and hyperlipidemia was established by treating normal Kunming mice with alloxan (iv). After different time intervals, the levels of blood glucose (BG) and serum triglyceride (TG) were determined. Forty-eight h after alloxan administration, the BG increased significantly, and the level of serum triglyceride reached maximum. The levels of blood glucose, serum triglyceride, cholesterol (CHOL) and free fatty acid (FFA) for vehicle treated mice were about 3.1, 4.0, 1.1, and 1.7 times those of normal Kunming mice, respectively. To evaluate the new animal model, four drugs were used. Two of them were antihyperglycemic drugs, metformin and a Recipe of Chinese Herbs (RCH). The other two were antihyperlipidemic agents, clofibrate and fenofibrate. All drugs showed positive effects on this kind of alloxan-diabetic Kunming mice. It can be concluded that this kind of alloxan-treated Kunming mice is useful for testing hypoglycemic and hypolipidemic drugs.

Animals↗
PubMed1994

Synthesis and characterization of some novel substituted benzenesulphonamides of potential hypoglycemic activity.

Two series of substituted benzenesulphonamides (Va-e and VIa-e) have been synthesized from 4-methoxycarbonyl-1-[p-(acetylamino)benzenesulphonylimino]pyridini um ylide (II) with a view to investigate their pharmacological activity. The structure of the synthesized products was inferred from elemental and spectral data. The hypoglycemic effect, antimicrobial activity and toxicity of the possible chemotherapeutic agents were evaluated. Six of these products were effective, when administered at an oral dose of 100 mg/kg b. wt., inducing marked reduction in blood glucose level.

Animals↗