Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P01275 (glucagon)
 26,492 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The incretin hormones are intestinal peptides that enhance insulin secretion following ingestion of nutrients. Liraglutide is a glucagon-like peptide-1 receptor analogue, which is obtained by derivatising glucagon-like peptide-1 with a fatty acid, providing a compound with pharmacokinetic properties that are suitable for once-daily dosing. Liraglutide has demonstrated lasting improvement of HbA(1c )levels, weight reduction and improved beta-cell function in patients with Type 2 diabetes mellitus. Liraglutide is well tolerated; the adverse events that are most frequently reported being transient nausea and diarrhoea. This article reviews the mechanisms of action and efficacy of liraglutide for the treatment of Type 2 diabetes mellitus. This agent is presently in Phase III clinical development.
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PMID:Liraglutide: a once-daily GLP-1 analogue for the treatment of type 2 diabetes mellitus. 1724 43

Exenatide is the first drug in the incretin mimetic class and is indicated for treatment of type 2 diabetes mellitus. Although structurally similar to the native glucagon-like peptide, this synthetic form has a much longer duration of action. Randomized trials have shown exenatide to be efficacious in improving glycemic control when combined with either metformin or a sulfonylurea. The dose is initially 5 mcg subcutaneously twice daily and may be titrated to 10 mcg subcutaneously twice daily to achieve better diabetes management. Nausea, vomiting, and diarrhea were the most common adverse events reported with exenatide therapy. Exenatide is not associated with hypoglycemia, which may provide advantages over adding insulin to a sulfonylurea or metformin.
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PMID:Exenatide (Byetta) as a novel treatment option for type 2 diabetes mellitus. 1725 50

GLP-1 receptor agonists such as exenatide are a group of new therapeutic agents that mimic the gut-derived incretin hormone GLP-1. These drugs stimulate insulin secretion while suppressing glucagon secretion, inhibit gastric motility, reduce appetite and hence, food intake. This group of drugs also induce reduction in fasting and postprandial glucose concentrations, HbA1c and ultimately lead to weight loss. The drugs are administered subcutaneously (exenatide twice daily). The most common side effect is mild nausea. Although short-term studies are promising, long-term clinical studies are needed to determine the benefits of this approach for the treatment of type 2 diabetes.
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PMID:[Glucagon-like peptide 1 (GLP-1)]. 1771 50

Exenatide is the first in a new class of compounds, which possess similar activity to the naturally-occurring hormone glucagon-like peptide-1 (GLP-1). It mirrors many of the effects of GLP-1, improving glycaemic control through a combination of mechanisms, which include glucose-dependent stimulation of insulin secretion, suppression of glucagon secretion, slowing of gastric emptying and reduced appetite. Phase III clinical trials showed exenatide therapy for 30 weeks significantly reduced glycated haemoglobin, and fasting and postprandial plasma glucose compared with baseline when added to metformin and sulfonylureas or a combination of the two, with an average weight loss of approximately 2 kg. Exenatide can also be used in combination with thiazolidinediones and may be an alternative to insulin in patients requiring additional therapy. In patients with established Type 2 diabetes, control of both glycaemia and body weight are important to minimise the risk of future diabetes complications. Open-label extensions from these pivotal trials demonstrate that patients treated with exenatide for < or = 3 years sustained the reductions in glycaemic control achieved at 30 weeks and had a progressive reduction in body weight. Exenatide is generally well tolerated; nausea is the most commonly reported side effect, but can be significantly reduced when a target dose of exenatide is achieved in patients with gradual dose titration. Hypoglycaemia has been encountered in clinical trials of exenatide, especially on initiation of therapy with sulfonylureas (not with metformin). Exenatide may enable patients with Type 2 diabetes to improve glycaemic control and reduce or eliminate the risk of hypoglycaemia and weight gain.
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PMID:Exenatide. 1793 Oct 93

Type 1 diabetes mellitus is classified as either autoimmune or idiopathic. Fulminant type 1 diabetes was originally reported as a subtype of idiopathic type 1 diabetes. Though involvement of viral infections has been suggested as a triggering mechanism, its pathogenesis remains unknown. Here, we present a case of fulminant type 1 diabetes associated with significant elevation of mumps titers. A 56-year-old Japanese man had suffered from nausea and generalized fatigue for two days before being transferred to our hospital in a confused state. Findings on admission revealed a high blood glucose level, near-normal HbA1c level, metabolic acidosis, and increased urinary ketone levels. Serum tests for islet-associated autoantibodies were negative. The serum, urinary C-peptide levels and the result of glucagon test indicated severe impairment of insulin secretion. These results were compatible with the diagnosis of fulminant type 1 diabetes. Also, he was suspected as having mumps infection on the basis of serological testing. These findings suggest that fulminant type 1 diabetes developed after mumps virus infection in our case. To the best of our knowledge, no other report has indicated an association between a recent mumps infection and the onset of fulminant type 1 diabetes. This case suggests an association between fulminant type 1 diabetes and mumps virus infection.
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PMID:A case of fulminant type 1 diabetes associated with significant elevation of mumps titers. 1852 Jan 3

Type 2 diabetic patients who have not achieved adequate glucose control at the maximum tolerated doses of their oral therapies currently have no alternative other than insulin. A new approach has been developed, using the glucoregulatory properties of the intestinal incretin hormone glucagon-like peptide-1 (GLP-1). This has resulted in the development of a new therapeutic class, the incretin mimetics, of which exenatide is the first to have been approved. Exenatide can bind to the endogenous receptors of GLP-1 and mimic its glucoregulatory actions. It improves glycemic control by acting on the key organs involved in glucose homeostasis: it stimulates insulin secretion and suppresses glucagon secretion in a glucose-dependent way, slows gastric emptying and reduces food intake. It consequently produces significant reductions in fasting and postprandial hyperglycemia. Various clinical studies, both versus placebo and versus insulin, have shown a significant decrease in HbA1c levels (of about 1%), accompanied by weight loss, in patients treated with exenatide. Exenatide efficacy is sustained and all the studies have shown a comparable tolerance profile. The most frequently reported adverse effects were nausea and hypoglycemia when the patient received concomitant sulfonylurea therapy. The aim of this article is to summarize main clinical data on exenatide and to discuss its position in current therapeutic strategy.
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PMID:Exenatide: its position in the treatment of type 2 diabetes. 1853 26

Pramlintide is a synthetic version of the naturally occurring pancreatic peptide called amylin. Amylin and pramlintide have similar effects on lowering postprandial glucose, lowering postprandial glucagon and delaying gastric emptying. Pramlintide use in type 1 and insulin requiring type 2 diabetes mellitus (DM) is associated with modest reductions in HbAlc often accompanied by weight loss. Limited data show a neutral effect on blood pressure. Small studies suggest small reductions in LDL-cholesterol in type 2 DM and modest reductions in triglycerides in type 1 DM. Markers of oxidation are also reduced in conjunction with reductions in postprandial glucose. Nausea is the most common side effect. These data indicate that pramlintide has a role in glycemic control of both type 1 and type 2 DM. Pramlintide use is associated with favorable effects on weight, lipids and other biomarkers for atherosclerotic disease.
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PMID:Pramlintide, the synthetic analogue of amylin: physiology, pathophysiology, and effects on glycemic control, body weight, and selected biomarkers of vascular risk. 1856 11

Exenatide (Byetta) is a synthetic derivative of exendin-4 and an agonist of receptors of glucagon-like peptide-1 (GLP-1). It is resistant to the rapid inactivation by dipeptidylpeptidase-4 and acts as an incretin mimetic. It stimulates insulin secretion by the B cell in a glucose-dependent manner whereas it inhibits glucagon secretion. Exenatide improves mainly postprandial glucose concentrations and lowers glycated haemoglobin (HbA(1c)) levels, without being directly responsible for hypoglycaemia or requiring mandatory home blood glucose monitoring. Furthermore, it slows down gastric emptying and promotes sustained body weight reduction, even in absence of frequently reported nausea following treatment initiation. Exenatide is recommended and reimbursed in Belgium for the treatment of type 2 diabetes, in combination with metformin and a sulfonylurea, in patients not adequately controlled with maximal tolerated doses of these oral glucose-lowering agents. Exenatide is presented as pre-filled pens for subcutaneous injection. The recommended initial dose is 5 microg before morning and evening meals, to be up titrated to 10 microg twice daily. Exenatide may represent a valuable alternative to insulin therapy, especially in overweight or obese patients with type 2 diabetes and not ready to perform home blood glucose monitoring.
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PMID:[Medication of the month... Exenatide (Byetta) incretinomimetic in the treatment of type 2 diabetes after failure and as add-on therapy to oral agents]. 1856 73

'Incretin effect' refers to increased insulin response to oral glucose as compared to i.v. glucose response. Incretin mimetics are a new class of antidiabetic drugs lowering hyperglycaemia. Incretin mimetics mimic the natural human hormones called 'incretins' with blood glucose regulating action. Exenatide is a synthetic analogue GLP-1 which is resistant to enzymatic degradation by DPP IV. Subcutaneously administered exenatide stimulates insulin secretion, suppresses glucagon secretion, slows down stomach evacuation and reduces the weight. Its administration is safe and the most frequent side effect is mild nausea.
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PMID:[Exenatid and its position as antidiabetic drug in the treatment of type 2 diabetes mellitus]. 1863 Jun 17

The incretin effect denominates the phenomenon that oral glucose elicits a higher insulin response than intravenous glucose. Glucagon like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide are the principal hormones responsible for incretin effect. In patients with type 2 diabetes the incretin effect of these hormones is impaired. Therapeutic approaches for enhancing the incretin action include degradation resistant GLP-1 receptor agonists (incretin mimetics) and inhibitors of dipeptidyl peptidase-IV (DLP-IV) activity (incretin enhancers- gliptins). These groups of medications have similar efficacy with regards to glycaemic improvement (reduction of HbA1c between 0.5 to 1.1%) and have side-effects like nausea. The incretin mimetics are injectable agents and are more likely to reduce weight or be weight neutral when compared to the oral gliptins. Long-term studies are essential to determine the real potential and role of these newer agents in the management of type 2 diabetes.
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PMID:Incretin based therapies for type 2 diabetes mellitus. 1883 49


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