Insulin degludec (INN/USAN) is a basal ultralong insulin analog developed by Novo Nordisk under the brand name Tresiba . This is given by subcutaneous injection once a day to help control blood sugar levels of diabetics. It has a duration of action lasting up to 42 hours (compared with 18 to 26 hours provided by other long-acting insulin marketed such as insulin glargine and insulin detemir), making it once-daily basal insulin, it is one that provides basic insulin levels, which contrary to fast and short acting bolus insulin.
Insulin degludec is a modified insulin that has a single amino acid removed from human insulin, and is conjugated to hexadecanedioic acid via gamma-L-glutamyl spacer in lysine amino acid at position B29.
Video Insulin degludec
Efek samping
A significant side effect of insulin therapy is hypoglycemia. A meta-analysis of clinical trials published in July 2012 found 39 to 47.9 hypoglycemia events (defined as blood glucose & lt; 56 mg/dL) per year of patients, with higher levels in the more concentrated degludec formulations. Rates of nocturnal hypoglycemia range from 3.7 to 5.1 events per patient year.
Maps Insulin degludec
Pharmacology
Action mechanism
Insulin degludec is an ultra long working insulin which, unlike insulin glargine, is active at physiological pH. The addition of hexadecanedioic acid to lysine at position B29 allows the formation of multi-hexamers in subcutaneous tissue. This allows the formation of a subcutaneous depot that results in the release of slow insulin into the systemic circulation.
Pharmacokinetics
Insulin degludec has an action onset of 30-90 minutes (similar to insulin glargine and insulin detemir). There is no peak in activity, due to slow release to the systemic circulation. Duration of degludec insulin work is reported to be longer than 24 hours.
Profile effectiveness
Studies have shown that patients taking insulin degludec are required to take significantly smaller basal insulin doses than those taking insulin glargine U100, while achieving the same level of blood glucose. Insulin degludec also has the ability to be mixed with other insulin, thereby increasing glycemic control. This can not be done using long-acting insulin at this time. A doctor who was involved in the trial was quoted as saying,
This allows the creation of new formulations that retain subtle control of long-acting basalt with fast feeding control of insulin aspart. This 2-component insulin maintains the risk characteristics of ultralow degludec with simultaneous feeding times.
History
Insulin degludec has been submitted for registration in the United States. Novo Nordisk hopes to start marketing insulin analogs by 2015 or 2016 after the completion of additional cardiac safety studies requested by the US Food and Drug Administration (FDA) in February 2013. Insulin degludec receives FDA approval September 25, 2015 and marketing begins on January 26, 2016.
Clinical test data
Diabetes mellitus type 1
Insulin degludec was studied as an alternative to insulin glargine as part of a basal-bolus regimen in BEGIN Basal-Bolus Type 1 trials. 629 patients with type 1 diabetes were randomized in a 3: 1 ratio to insulin degludec (n = 472) or insulin glargine (n = 157) in addition to feeding insulin aspart time. Patients in the degludec treatment group were transferred from basal insulin to insulin degludec in a 1: 1 ratio, with a 20-30% dose reduction in patients receiving some basal doses per day. After 52 weeks, patients treated with insulin degludec resulted similar reductions in HbA1c (0.40% vs 0.39%) met the criteria for noninferiority. Unwanted events were similar in both treatment groups; However, rates of nocturnal hypoglycemia (between midnight and 6 am) were 27% lower in patients treated with insulin degludec (3.91 vs. 5.22%, p = 0.024). Reduced incidence of hypoglycemia is seen as a therapeutic benefit, since hypoglycemia is often a dose that limits toxicity in insulin therapy.
Diabetes mellitus type 2
In BEGIN Basal-Bolus Type 2 trials, insulin degludec was studied as an alternative to insulin glargine in patients with type 2 diabetes mellitus. 995 patients were randomized to receive insulin degludec (n = 755) or insulin glargine (n = 251), in addition to both feeding time of aspart insulin, metformin, and/or pioglitazone. Patients in this trial had mean HbA1c 8.3-8.4%, and 49-50% on a regimen consisting of bolus-basal insulin plus oral antidiabetic drugs. After 52 weeks, degludec insulin was found to be noninferior to insulin glargine, giving the same HbA1c-lowering effect (-1.10 vs -1.18%). The overall rate of hypoglycemia was significantly lower with insulin degludec (11.09 vs 13.63%/year, p = 0.0359), including cases of nocturnal hypoglycemia (1.39 vs 1.84%/year, p = 0.0399 ).
References
External links
- Novo Nordisk
- US. National Drug Library: Drug Information Portal - Insulin degludec
Source of the article : Wikipedia
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