Insulin degludek specifically binds to human endogenous insulin receptor and interacts with it realizes its pharmacological effect similar to the effect of human insulin. Degludek hypoglycemic effect of insulin due to an increase glucose utilization by tissues after binding to insulin receptors of muscle and fat cells and simultaneous decrease liver glucose production rate.
The drug what does proviron do is a basal insulin analogue of human action extremely long; after subcutaneous injection it forms soluble multigeksamery in the subcutaneous depot, where there is a continuous and prolonged absorption degludek insulin into the bloodstream, providing extremely long, flat profile of action and stable hypoglycemic effect . During the 24-hour monitoring period, the hypoglycemic effect of the drug in patients who are insulin degludek dose was administered once a day, in contrast to insulin glargine, showed an even volume distribution between the action of the first and second 12-hour period .
Proved that a linear relationship between increasing doses and its overall hypoglycemic action.
The studies revealed no clinically significant differences in the pharmacodynamics between elderly patients and adult patients younger.
Clinical efficacy and safety
A 11 international randomized, open-label clinical studies Treat-to-Target (strategy “treat to target”) lasting 26 and 52 weeks, conducted in parallel groups, which included, a total of 4275 patients (1102 patients with type 1 diabetes and 3173 a patient with type 2 diabetes), receiving .
The effectiveness has been studied in patients with type 1 diabetes who had not received prior to this insulin, and type 2 diabetes treated with insulin, a fixed or flexible dosing regimen . It proved no superiority comparator drugs (insulin detemir and insulin glargine) in reducing HbA figure 1C from power on until the end of the study. The exception was the preparation of sitagliptin, in comparison demonstrated a statistically significant superiority of his in reducing masteron before and after.
The results of the clinical study (strategy “treat to target”) to initiate insulin therapy in patients with type 2 diabetes have shown a decrease of 36% in the incidence of episodes of the confirmed nocturnal hypoglycemia (defined as a hypoglycemic episodes occurred during the time of day between zero o’clock and six o’clock in the morning , confirmed the result of the measurement of plasma glucose <3.1 mmol / l, or evidence that the patient to restore the state needed help of third parties) on a background of daily administration once daily in combination with oral hypoglycemic agents (oral agents) on compared to that with insulin glargine and combined with oral agents. The results of the clinical study (strategy “treat to target”) to assess the basal-bolus regimen of insulin therapy in patients with type 2 diabetes have demonstrated a lower overall risk of hypoglycemic episodes and nocturnal hypoglycemia during treatment with what does proviron do compared with those with insulin glargine .
Results of a prospective meta-analysis received during the seven-designed according to the principle “treat to target” of clinical trials involving patients with diabetes mellitus type 1 and 2, demonstrated the benefits of therapy in relation to lower, compared to insulin glargine, the incidence of patient-confirmed episodes of hypoglycemia and nocturnal hypoglycemia episodes the confirmed. Reducing the frequency of hypoglycemia during treatment has been achieved at a lower average of glucose in blood plasma on an empty stomach than with insulin glargine treatment.
Absorption of extremely long due to the action of insulin degludek specially created structure of its molecules. After the formation of subcutaneous injection of soluble stable multigeksamerov that create a depot of insulin in adipose tissue. Multigeksamery gradually dissociate releasing insulin monomers degludek, resulting in a slow and sustained delivery of the drug into the bloodstream. The equilibrium concentration plasma levels achieved in 2-3 days after drug administration. The action of insulin degludek for 24 hours at his daily administered once a day, distributed evenly between the first and second .
Distribution of insulin Communication degludek plasma proteins (albumin) is> 99%.
Metabolism The collapse of insulin degludek similar to that of human insulin; all metabolites formed are inactive.
Elimination half-life after subcutaneous injection is determined by the rate of its absorption from the subcutaneous tissue. The half-life what does proviron do is approximately 25 hours and is independent of dose.
Linearity Subcutaneous administration total plasma concentrations were administered dose proportional in the range of therapeutic doses.
Special patient groups There were no differences in the pharmacokinetic properties , depending on the sex of the patient.
Elderly patients, patients of different ethnic groups, patients with impaired renal or hepatic function There were no clinically relevant differences in the pharmacokinetics of insulin degludek between the elderly and younger patients, between patients of different ethnic groups, between patients with impaired renal and hepatic function, and healthy patients.
Children and adolescents The pharmacokinetic properties of insulin degludek in the study in children (6-11 years) and adolescents (12-18 years) with type 1 diabetes compared to those of adult patients. On the background of single administration in patients with type 1 diabetes mellitus it has been demonstrated that the total exposure dose in children and adolescents higher compared with that in adults.
These preclinical safety studies
Preclinical data based on studies of pharmacological safety, what does proviron do toxicity of repeated doses, a carcinogenic potential toxic effects on the reproductive function, have not revealed any risk for insulin degludek cheloveka.Sootnoshenie metabolic and mitogenic activity of insulin degludek is similar to that of human insulin.