Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0011849 (diabetes)
 277,896 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Insulin glulisine is a new rapid-acting insulin analog. The aim of this study was to assess the glucodynamic efficacy of insulin glulisine compared with regular human insulin (RHI) using a manual euglycemic clamp technique. Steady-state pharmacokinetics of insulin glulisine, and its cardiac safety (ECG) and tolerability after intravenous administration, were also determined. This was a single center, randomized, open-label, two-way crossover study in healthy male subjects (n = 16). At the treatment visits subjects received an intravenous infusion of the study drug at a rate of 0.8 mU kg (-1) . min (-1) for 2 hours. Individual baseline glucose concentrations were targeted for euglycaemia and maintained with a manual adjusted 20 % glucose solution over the clamp period of a maximum 6 hours. A glulisine-specific antibody was used to quantify glulisine concentrations by radioimmunoassay, while a non-specific insulin antibody and C-peptide based correction for endogenous insulin was used to estimate exogenous human insulin (RHI). At steady state (90 - 120 min), insulin glulisine and RHI had equivalent glucose utilization (GIR-AUC (SS), 209 [corrected] mg . kg (-1) for glulisine, 214 [corrected] mg . kg (-1) for RHI) and infusion rates (GIR (SS), 7.0 and 7.2 [corrected] mg . kg (-1) . [corrected] min (-1) . kg (-1)). Both insulins also presented equal total glucose disposal (GIR-AUC (0 - clamp end), 995 and 1050 [corrected] mg . kg (-1)) and onset of activity within 20 min. Insulin glulisine and RHI showed parallel time concentration profiles with similar distribution and elimination, but the different antibodies employed for radioimmunoassay impeded a quantitative comparison. There were no noteworthy individual or within-group changes in cardiac repolarisation parameters measured by 12-lead ECG during insulin glulisine infusion. In conclusion, insulin glulisine and RHI show similar distribution and elimination profiles and equivalent glucodynamic efficacy on a molar, unit-per-unit basis.
Exp Clin Endocrinol Diabetes 2005 May
PMID:A comparison of the steady-state pharmacokinetics and pharmacodynamics of a novel rapid-acting insulin analog, insulin glulisine, and regular human insulin in healthy volunteers using the euglycemic clamp technique. 1592 16

Insulin glulisine (Apidra, Sanofi-Aventis), a new and recently approved rapid-acting insulin analogue, mimics the pharmacokinetic and pharmacodynamic profiles of physiological human insulin, but has a rapid onset, peak effect at 1h, and a shorter duration of action (approximately 4 h). Its rapid-action properties are maintained across subject types. Formal clinical evaluations show that insulin glulisine can be administered safely and effectively pre- and postmeal. When injected immediately premeal, insulin glulisine provides superior postprandial blood glucose control compared with regular human insulin (RHI) injected 30 min premeal. These data highlight the flexibility in the dosing schedule with insulin glulisine. Clinical trials have demonstrated that insulin glulisine elicits a greater reduction in glycosylated haemoglobin at end point than RHI, in both type 1 and 2 diabetes mellitus. In addition, the safe administration of insulin glulisine by continuous subcutaneous insulin infusion has been demonstrated in patients with type 1 diabetes. In conclusion, insulin glulisine is an effective, safe and well-tolerated rapid-acting insulin analogue.
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PMID:Insulin glulisine: a new rapid-acting insulin analogue for the treatment of diabetes. 1593 90

In patients with diabetes, the benefit of conventional insulin therapy can be limited due to difficulty in achieving tight glycemic control, which is critical to reducing the risk of long-term diabetes-related complications. The recent development of recombinant analogs of regular human insulin is changing the clinical management of diabetes. One of the newest members of this class of hypoglycemic agents is insulin glulisine, a rapid-acting insulin analog with a pharmacokinetic profile that more closely mimics the natural pattern of insulin secretion than regular human insulin. Subcutaneous administration of insulin glulisine has a faster subcutaneous absorption, a more rapid onset of activity, and a shorter duration of action than regular human insulin. These properties of insulin glulisine allow it to be administered shortly before or soon after meals by subcutaneous injection or by continuous subcutaneous pump infusion. Insulin glulisine effectively controls postprandial glucose excursions in both type 1 and type 2 diabetic patients without increasing the risk of hypoglycemia. One unit of insulin glulisine has the same glucose-lowering effect as one unit of regular human insulin. Insulin glulisine has a favorable safety profile, which is not significantly different from that of regular human insulin. This review summarizes the current data on the clinical efficacy and safety of insulin glulisine in type 1 and type 2 diabetic patients.
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PMID:Insulin glulisine. 1619 96

Insulin glulisine (glulisine), a human insulin analogue with a rapid-acting time-action profile, has been developed to fulfil the mealtime (bolus) insulin requirement in patients with diabetes. The aim of this multinational, multi-centre, controlled, open-label, randomized, parallel-group study was to compare the efficacy and safety of insulin glulisine (glulisine) to that of insulin lispro (lispro) in adults diagnosed with Type 1 diabetes. Of the 683 patients randomized, 672 received treatment (339 patients received glulisine, 333 patients received lispro). Over the 26-week study, a similar reduction in mean HbA1c occurred in both groups (adjusted mean change from baseline -0.14% in both groups). The basal insulin dose was relatively unchanged from baseline in the glulisine group but increased in the lispro group (glulisine: 0.12 IU vs. lispro: 1.82 IU; p = 0.0001). As a consequence, total daily insulin dose decreased in the glulisine group but increased in the lispro group (glulisine: -0.86 IU vs. lispro: 1.01 IU; p = 0.0123). There was no relevant difference between the two groups in the reporting of symptomatic hypoglycaemia (overall, nocturnal and severe). This study demonstrates that glulisine provides equivalent glycaemic control to lispro. The clinical relevance of any difference in total daily insulin dose remains to be established.
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PMID:Efficacy and safety of insulin glulisine in patients with type 1 diabetes. 1630 40

Insulin and related synthetic therapeutics have been prohibited by the World Anti-Doping Agency for athletes demonstrably not suffering from diabetes mellitus. The primary specimen for doping controls has been urine, but the renal excretion of intact human insulin as well as synthetic analogues such as the rapid-acting products Humalog LisPro, Novolog Aspart, and Apidra Glulisine has been reported negligible owing to metabolic degradation. Nevertheless, employing solid-phase extraction in combination with immunoaffinity purification followed by a top-down sequencing-based mass spectrometric approach, an assay was established allowing the identification of three intact rapid-acting synthetic insulins in doping control urine samples. A volume of 25 mL of urine was concentrated, insulin analogues were isolated from the concentrate by immunoaffinity chromatography, and the eluate was analyzed using microbore liquid chromatography/tandem mass spectrometry. Characteristic product ion spectra obtained from 5-fold protonated intact analytes as well as isolated insulin B-chains allowed the unambiguous identification of target analytes with detection limits of 0.05 ng/mL (9 fmol/mL). Moreover, assay validation demonstrated recoveries between 72 and 80% for Humalog LisPro, Novolog Aspart, and Apidra Glulisine, and assay precisions ranged from 9 to 16%. A reliable tool is provided that allows the qualitative determination of rapid-acting insulins in urine specimens collected for sports drug testing.
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PMID:Doping control analysis of intact rapid-acting insulin analogues in human urine by liquid chromatography-tandem mass spectrometry. 1653 26

Diabetes is a metabolic disease with high prevalence worldwide. Exogenous insulin is used in the management of this condition. The development of human insulin has provided tighter control of glycaemia in diabetic patients. Insulin analogues like insulin lispro and aspart were developed to closely match its profile with physiological secretion. The newer additions to this armamentarium are insulin glulisine, insulin detemir and albulin. Insulin glulisine is a short acting analogue with a rapid onset of action. The antiapoptotic property, mediated through insulin substrate receptor-2 has a favourable protective action on beta cells. Insulin detemir is a long acting analogue, soluble at neutral pH, which reversibly binds to albumin in plasma, prolonging its action. Its lower affinity for insulin receptors necessitates higher doses compared to human insulin. The reduction in body weight is an additional advantage of detemir. A major concern about all newer insulin analogues is their altered mitogenic properties and resultant risk of carcinogenicity on long term use. Albulin is a latest addition of insulin analogue which is under various in vitro and in vivo studies. Inhaled insulin in powder form (Exubera) is recently approved by FDA and appears promising.
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PMID:Newer insulin analogues and inhaled insulin. 1656 28

Insulin glulisine is a rapid-acting human insulin analogue that has a faster onset of action and shorter duration of action than regular human insulin (RHI) in patients with type 1 or 2 diabetes mellitus and is efficacious in controlling prandial blood glucose levels in these patients. In large, well designed trials in patients with type 1 diabetes, insulin glulisine demonstrated a similar degree of glycaemic control, as measured by glycosylated haemoglobin (HbA(1c)) levels, to RHI after 12 weeks and insulin lispro after 26 weeks. Pre-meal insulin glulisine was also more effective than RHI at controlling 2-hour post-prandial glucose excursions in patients with type 1 or 2 diabetes over a period of 12 weeks. In patients with type 2 diabetes, insulin glulisine induced significantly greater reductions in HbA(1c) levels and 2-hour post-breakfast and post-dinner blood glucose levels than RHI over a period of 26 weeks. Insulin glulisine was generally well tolerated by patients with type 1 or 2 diabetes and had a similar safety profile to insulin lispro or RHI. Severe hypoglycaemia was experienced by similar proportions of insulin glulisine or comparator insulin (insulin lispro or RHI) recipients with type 1 or type 2 diabetes.
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PMID:Insulin glulisine. 1670 59

Achieving and maintaining glycemic control (glycated hemoglobin--HbA(1c)< or =7.0% according to American Diabetes Association and < or =6.5% according to International Diabetes Federation) is the primary goal in treating diabetes, which lowers the risk for diabetes-related complications. Insulin therapy is essential for type 1 diabetes treatment. Insulin therapy in type 2 diabetes is initiated when glycemic control is inadequate despite the combination of antihyperglycemic drugs. The type of insulin therapy is selected according to the patient's lifestyle and needs. Multiple insulin injection therapy and premixed insulin therapy are usually administered. In multiple insulin injection therapy, basal insulin is administered one or two times a day, and regular human insulin or rapid-acting insulin analog is administered with each meal. The duration of action of regular insulin is 6-8 hours; therefore, the risk for postprandial hypoglycemia is increased. The action of novel insulin analogs (rapid- and long-acting) closely mimics physiological insulin secretion. Three rapid-acting insulin analogs are currently available: insulin lispro, insulin aspart, and insulin glulisine. Insulin glulisine is the most recently approved rapid-acting insulin analog. It is safe, flexible, and effective in achieving target postprandial glycemic control. Moreover, the pharmacokinetics of insulin glulisine does not depend on the amount of subcutaneous fat. Basal insulins include intermediate-acting human insulins (neutral protamine Hagedorn) and long-acting insulin analogs (insulin glargine, insulin detemir). The latter are the optimal choice covering basal insulin requirement. Compared to neutral protamine Hagedorn insulin, long-acting insulin analogs have no pronounced concentration peak and reduce nocturnal hypoglycemia risk and weight gain.
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PMID:[An update on multiple insulin injection therapy in type 1 and 2 diabetes]. 1702 76

The advancement in protein engineering offers targeted development of insulin analogs that display either faster absorption kinetics or longer time-action profiles compared with human insulin and, therefore, more closely mimic endogenous insulin secretion. Insulin glulisine (3(B)Lys29(B) Glu-human insulin) is a new fast-acting analog that provides absorption and onset of action more rapidly with a shorter duration of action compared with regular human insulin, and thus better resembles physiologic mealtime insulin requirements. Insulin glulisine has been designed to exhibit intrinsic stability while maintaining rapid deployment of insulin monomers. Pharmacokinetic and pharmacodynamic profiling of insulin glulisine in healthy subjects and patients with type 1 and type 2 diabetes not only confirms the rapid absorption and fast action of insulin glulisine compared with human insulin, but also provides evidence that the unique drug formulation may offer additional benefits. Insulin glulisine complements insulin glargine (21(A)-Gly30(Ba)-L-Arg-30(Bb)-L-Arg-human insulin), the first long-acting basal insulin analog that displays a smoothed time-action profile with a 24-h duration of action. Together these analogs offer patients a more physiologic approach to insulin replacement.
Diabetes Technol Ther 2007 Feb
PMID:Insulin glulisine complementing basal insulins: a review of structure and activity. 1827 64

SoloStar (sanofi-aventis) is a new, disposable insulin pen for the administration of insulin glargine (Lantus, sanofi-aventis) or insulin glulisine (Apidra, sanofi-aventis). SoloStar was developed to address a wide range of patient needs and demonstrates advancement over previous devices, owing to its appropriate combination of ergonomically-tested and mechanically improved features. The authors report the results of key investigations carried out by sanofi-aventis as part of the SoloStar development plan, including dose accuracy and injection force testing. Comparisons between SoloStar and two commonly used pens, FlexPen (Novo Nordisk) and the Humulin/Humalog pen (Eli Lilly) establish SoloStar as a state of the art pen that is suitable for most patients with diabetes.
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PMID:Dose accuracy and injection force dynamics of a novel disposable insulin pen. 1733 13


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