Drugs online research references
MMW Fortschr Med. 2000 Sep 21;142(38):31-3.
[Insulin sensitizer. A new therapy option for type 2 diabetic patients]
[Article in German]
Filz HP.
Chefarzt Innere Medizin/Diabeteszentrum am Luisenkrankenhaus, Lindenfels.
The glitazones, also known as insulin sensitizers, represent a new concept in the treatment of type 2 diabetes. While previously available antidiabetics have no influence on an existing insulin resistance, the glitazones act directly on the receptors in the muscles, fatty tissue and liver, and in this way reduce insulin resistance. To date, three members of this group of substances are known: troglitazone, rosiglitazone and pioglitazone. In a study done to investigate pioglitazone, fasting blood sugar and HbA1c achieved virtually normal values, and lipid metabolism also improved. On the basis of the results of studies done to date, the tolerability of both pioglitazone and rosiglitazone is good. In contrast to troglitazone, no evidence has been found for a hepatotoxic effect. Insulin sensitizers do not cause hypoglycemia, since they do not stimulate the pancreas. They are suitable both for monotherapy and combination treatment with metformin, sulfonylureas and insulin.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11050888&dopt=Abstract
dundee.ac.uk
AIMS: To determine the changes in oral hypoglycaemic therapy and the time to incidence of insulin therapy in people with Type 2 diabetes. METHODS: A retrospective incidence cohort was constructed of 1305 subjects with Type 2 diabetes, who obtained a first prescription for oral hypoglycaemic medication between 1 July 1993 and 31 December 1994 in Tayside, Scotland. The primary endpoint of changes in oral hypoglycaemic therapy and time to insulin was determined up to the end of the follow-up, on 31 December 1995. RESULTS: Overall, 9.4% of subjects switched to insulin, while 11% of those initially on sulphonylurea, and 6% of those initially on metformin switched to insulin therapy. Approximately three-quarters (72%) remained on the same class of drug throughout the study period (median follow-up 588 days). Only 9% died during the follow-up and this did not differ appreciably by drug group. Males were more likely to switch to insulin compared with females (10.3% vs. 8.5%), and those who switched were slightly younger with a mean age of 58 years compared with a mean age of 60 years of those who did not switch. The median time of switching to insulin was 186 days or approximately 6 months for this cohort, giving a rate of switching to insulin of 5.84% per year. Poorer glycaemic control (HBA1c) and low body mass index (BMI) were associated with switching to insulin. CONCLUSIONS: Following initial therapy with oral hypoglycaemic medication in the population, switching to insulin occurred at a rate of 5.84% per year. Switching to insulin was associated with being younger, male, having low BMI and higher HbA1c.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12099966&dopt=Abstract
Br J Pharmacol. 1996 Mar;117(6):1318-24.
Regulation by metformin of the hexose transport system in vascular endothelial and smooth muscle cells.
Sasson S, Gorowits N, Joost HG, King GL, Cerasi E, Kaiser N.
Department of Pharmacology, Hebrew University School of Medicine, Jerusalem, Israel.
1. The effect of the biguanide metformin on hexose transport activity was studied in bovine cultured aortic endothelial (BEC) and smooth muscle cells (BSMC). 2. Metformin elevated the rate of hexose transport determined with 2-deoxyglucose (2DG) in a dose- and time-dependent manner in both cell types. Similar ED50 values (0.8-1.0 mM) were determined for the effect of metformin on 2DG uptake in both BEC and BSMC following 24 h exposure to increasing concentrations of metformin, with maximal stimulation at 2 mM. 3. In BEC, metformin increased the hexose transport rate 2-3 fold at all glucose concentrations tested (3.3-22.2 mM). In BSMC incubated with 22.2 mM glucose, metformin elevated the hexose transport approximately 2 fold. The drug was also effective at lower glucose levels, but did not exceed the maximal transport rate observed in glucose-deprived cells. 4. Similar results were obtained when the effect of metformin on hexose transport activity was assessed with the non-metabolizable hexose analogue, 3-O-methylglucose, suggesting that the drug affects primarily the rate of hexose transport rather than its subsequent phosphorylation. 5. The metformin-induced increase in hexose transport in BSMC treated for 24 h with the drug correlated with increased abundance of GLUT1 protein in the plasma membrane, as determined by Western blot analysis. 6. These data indicate that in addition to its known effects on hexose metabolism in insulin responsive tissues, metformin also affects the hexose transport system in vascular cells. This may contribute to its blood glucose lowering capacity in patients with Type 2, non-insulin-dependent diabetes mellitus.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8882631&dopt=Abstract
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