Victose

Victoza is an antidiabetic medication. Liraglutide is an analogue of the natural element GLP-1, which is produced using recombinant DNA biotechnology, which uses a strain of brewer's yeast that is 97% homologous to human GLP-1. This component is synthesized and activates the endings of natural GLP-1. These endings act as targets for natural GLP-1 (the internal hormone incretin, which stimulates glucose-dependent insulin secretion within the β-cells of the pancreas).

Indications Victose

It is used in the case of type 2 diabetes mellitus in combination with physical procedures and diet in order to gain glycemic control. Can be administered as monotherapy; in addition, in combination with one or more oral antidiabetic drugs (sulfonylurea derivatives, as well as metformin or thiazolidinedilones) in people who have not been helped by previous treatment. In addition, it is used in combination with insulin in people who have not been able to get the result when using liraglutides with metformin.

It is used to reduce the likelihood of CVD disorders (such as death due to CVD disease, stroke and myocardial infarction, which did not lead to death) in diabetics (type 2) with diagnosed CVS pathology - as an addition to standard therapy for CVD diseases (based on on the analysis of the period of development of the first significant dysfunction of the CVS).

Release form

The drug is released in the form of a liquid for n / a injections, inside 3 ml cartridges; also inside the pack contains special syringe pens.

Pharmacodynamics

The long term plasma half-life is associated with 3 mechanisms: self-association, which slows drug absorption, synthesis with albumin, and an increased index of enzyme stability in relation to DPP-4 and the NEP enzyme.

Liraglutide interacts with the GLP-1 endings, which increases the cAMP values. As a result, glucose-dependent stimulation of insulin secretion develops and the activity of β-cells of the pancreas improves. Along with this, under the influence of Victoza, glucose-dependent inhibition of excess glucagon excretion develops. As a result, with an increase in blood sugar levels, inhibition of glucagon secretion develops and insulin secretion is stimulated. At the same time, at low blood glucose values, liraglutide reduces insulin secretion, but does not inhibit glucagon secretion. [1]

With a weakening of glycemia, there is some delay in gastric emptying. The medication reduces weight and fat levels, reducing energy costs and the feeling of hunger.

GLP-1 helps physiologically regulate calorie intake and appetite, and its endings are found in several areas of the brain that help regulate appetite.

Pharmacokinetics

Absorption of liraglutide with subcutaneous injection occurs at a low speed, the plasma Tmax is 8-12 hours. Plasma values of Cmax with s / c administration of a single portion of 600 μg are equal to 9.4 nmol / l.

After applying a portion of 1.8 mg of liraglutide, the average values of its plasma Css are about 34 nmol / l. The exposure level of the substance increases in proportion to the dosage used. After using a 1-fold dose of drugs, the intrapopulation rate of variation in AUC is 11%. The values of the absolute bioavailability of the component with a s / c injection are approximately 55%.

The apparent indices of the tissue Vd of the drug with subcutaneous injection are 11-17 liters. The average Vd values for intravenous administration are 0.07 l / kg. Most of liraglutide is synthesized with blood protein (> 98%).

After the application of 1-fold portion of [3H] -liraglutide (pre-labeled with an isotope of the radioactive type) to volunteers, liraglutide remained the main element of plasma in an unchanged state for a period of 24 hours. Inside the plasma, 2 metabolic elements were registered (≤9% and ≤5% of the total intraplasmic radioactivity). Metabolic processes of liraglutide occur endogenously (similar to large proteins).

After injection of a portion of [3H] -liraglutide, the unchanged element was not observed inside feces or urine. Only a small part of the radioactive components in the form of metabolic elements synthesized with liraglutide (6% and 5%, respectively) were excreted through the kidneys or intestines. By these routes, excretion occurs mainly during the first 6-8 days after the use of drugs. The average level of clearance for subcutaneous injection of a single dose of the drug is approximately 1.2 l / h; half-life is approximately 13 hours.

The exposure index of liraglutide in persons with mild and moderate liver failure decreases by 13-23%. In people with severe impairment, these values are significantly lower (by 44%).

In case of insufficient renal function, the exposure is reduced by 33% (CC value within 50-80 ml per minute), 14% (CC is 30-50 ml / minute), 27% (CC - <30 ml / minute) and 28% (terminal phase of illness; dialysis patients).

Dosing and administration

The medicine should be injected subcutaneously, once a day, into the thigh, abdomen or shoulder area. It is forbidden to use intramuscular or intravenous administration.

The starting serving size is 0.6 mg per day. After use for at least 1 week, the dosage is increased to 1.2 mg. To obtain maximum glycemic control, taking into account the clinical effect of the drug, it is allowed to increase the portion to 1.8 mg (also after a minimum of 1 week of using a portion of 1.2 mg). It is forbidden to enter a daily portion of more than 1.8 mg.

When used in addition to the administration of metformin or the combination therapy of thiazolidinedione with metformin, these drugs are used in the same dosages.

The use of Victoza together with sulfonylurea derivatives requires a reduction in the portion of the latter - in order to reduce the likelihood of developing side signs of hypoglycemia.

• Application for children

It is forbidden to use the medication in pediatrics (for persons under the age of 18).

Use Victose during pregnancy

You can not prescribe Victoza with hepatitis B and pregnancy.

Contraindications

The main contraindications:

• type 1 diabetes mellitus;
• severe renal dysfunction;
• ketoacidosis of the diabetic type;
• hepatic dysfunction;
• failure of the heart of the 3-4th grade;
• inflammation in the intestinal area;
• gastric paresis;
• severe intolerance to liraglutide.

Side effects Victose

Among the side symptoms:

• problems with metabolic processes: hypoglycemia is often noted (especially when combined with sulfonylurea derivatives), decreased appetite and anorexia;
• violations of the activity of the National Assembly: cephalalgia often appears;
• disorders of the digestive function: mainly diarrhea and nausea occur. Dyspepsia, constipation, vomiting, gastritis, bloating, belching, upper abdominal pain and GERD are common;
• infectious lesions: infections of the upper respiratory tract are mainly observed;
• signs of allergies: Quincke's edema occurs singly;
• others: occasionally there are manifestations in the thyroid region. Sometimes the formation of antibodies against liraglutide occurs (does not lead to a weakening of the drug efficacy).

Interactions with other drugs

Some delay in gastric emptying associated with the use of liraglutide may also affect the absorption of oral medications used with it. Diarrhea that develops with the administration of Victoza can alter the absorption of oral medications used in combination with it.

At the beginning of the use of liraglutide, persons using warfarin should regularly monitor the MHO indicator.

Storage conditions

Victoza should be kept out of the reach of small children. Temperature indicators - within 2-8˚С. You cannot freeze the solution.

Shelf life

Victoza can be used for a period of 30 months from the date of manufacture of the therapeutic substance. The shelf life after the 1st use is 1 month.

Analogs

Analogs of the medication are the drugs Guarem, Bayeta with Novonorm and Invokana.