Baeta solution for subcutaneous injection 250 µg/ml 1.2ml syringe-pen cartridges, 1pc

Composition

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1 ml contains exenatide 250 mcg.

Auxiliary substances:

sodium acetate trihydrate,

glacial acetic acid,

mannitol,

metacresol,

d/i water.

Pharmacological action

Baeta is a hypoglycemic drug. Exenatide (exendin-4) is a mimetic of incretin and is a 39-amino acid amidopeptide.

Incretins, such as glucagon-like peptide-1 (GLP-1), enhance glucose-dependent insulin secretion, improve beta-cell function, suppress inadequately increased glucagon secretion, and slow gastric emptying after they enter the general bloodstream from the intestine. Exenatide is a potent incretin mimetic that increases glucose-dependent insulin secretion and has other hypoglycemic effects inherent in incretins, which can improve glycemic control in patients with type 2 diabetes mellitus.

The amino acid sequence of exenatide partially corresponds to the sequence of human GLP-1, as a result of which it binds and activates GLP-1 receptors in humans, which leads to increased glucose-dependent synthesis and secretion of insulin from pancreatic beta-cells involving cyclic AMP and/or other intracellular signaling pathways. Exenatide stimulates the release of insulin from beta cells in the presence of elevated glucose concentrations.

By chemical structure and pharmacological action, exenatide differs from insulin, sulfonylurea derivatives, D-phenylalanine derivatives and meglitinides, biguanides, thiazolidinediones, and alpha-glucosidase inhibitors.

Exenatide improves glycemic control in patients with type 2 diabetes mellitus through the following mechanisms.

In hyperglycemic conditions, exenatide increases glucose-dependent insulin secretion from pancreatic beta cells. This insulin secretion stops as blood glucose levels decrease and the blood glucose level approaches normal levels, thereby reducing the potential risk of hypoglycemia.

Insulin secretion during the first 10 minutes (in response to increased glycemia), known as the “first phase of the insulin response”, is specifically absent in patients with type 2 diabetes. In addition, loss of the first phase of the insulin response is an early violation of beta-cell function in type 2 diabetes mellitus. The use of exenatide restores or significantly enhances both the first and second phase of the insulin response in patients with type 2 diabetes mellitus.

In patients with type 2 diabetes mellitus with hyperglycemia, exenatide use suppresses excessive glucagon secretion. However, exenatide does not interfere with the normal glucagon response to hypoglycemia.

It has been shown that the use of exenatide leads to a decrease in appetite and a decrease in food intake; it suppresses gastric motility, which leads to a slowdown in its emptying.

In patients with type 2 diabetes mellitus, exenatide therapy in combination with metformin, thiazolidinedione and / or sulfonylureas leads to a decrease in fasting blood glucose, postprandial blood glucose, and HbA1c, thereby improving glycemic control in these patients.

Indications

Monotherapy: type 2 diabetes mellitus as monotherapy in addition to diet and exercise to achieve adequate glycemic control.

Combination therapy: type 2 diabetes mellitus as adjunctive therapy to metformin, a sulfonylurea derivative, thiazolidinedione, a combination of metformin and a sulfonylurea derivative, or metformin and thiazoldinedione if adequate glycemic control is not achieved.

Use during pregnancy and lactation

The drug is contraindicated during pregnancy and lactation.

Contraindications

• Hypersensitivity to exenatide or excipients included in the preparation;
• Type 1 diabetes mellitus or diabetic ketoacidosis.
• Severe renal insufficiency (creatinine clearance
• The presence of severe diseases of the gastrointestinal tract with concomitant gastroparesis.

Side effects

Adverse reactions that occurred more frequently than in isolated cases are listed according to the following gradation: very common – ≥10%, often – ≥1%, but

From the digestive system:  very often — nausea, vomiting, diarrhea; often-decreased appetite, dyspepsia, gastroesophageal reflux; sometimes-abdominal pain, bloating, belching, constipation, impaired taste sensations, flatulence.

From the central nervous system:  often — dizziness, headache; rarely-drowsiness.

From the endocrine system:  very often — hypoglycemia (in combination with sulfonylurea derivatives); often — a feeling of trembling, weakness, hyperhidrosis.

Allergic reactions:  rarely-rash, pruritus, angioedema; extremely rarely — anaphylactic reaction.

Other services:  often-skin reaction at the injection site; rarely-dehydration (associated with nausea, vomiting and / or diarrhea). Several cases of increased clotting time (INR) have been reported with concomitant use of warfarin and exenatide, sometimes accompanied by bleeding.

Due to the fact that the frequency of hypoglycemia increases with the co-use of Baeta with sulfonylurea derivatives, it is necessary to consider reducing the dose of sulfonylurea derivatives with an increased risk of hypoglycemia. Most episodes of hypoglycemia were mild or moderate in intensity and were stopped by oral carbohydrate intake.

Overall, the intensity of side effects was mild or moderate and did not lead to discontinuation of treatment. Most often, mild or moderate-intensity nausea was reported as dose-dependent and decreased over time without interfering with daily activity.

Interaction

Baeta® should be used with caution in patients taking oral medications that require rapid absorption from the gastrointestinal tract, as Baeta® may cause delayed gastric emptying. Patients should be advised to take oral medications that depend on their threshold concentration (for example, antibiotics) at least 1 hour before exenatide use. If these medications need to be taken with food, then they should be taken during those meals when exenatide is not administered.

When digoxin is administered concomitantly (at a dose of 0.25 mg 1 time / day) with Baeta®, the Cmax of digoxin decreases by 17%, and Tmax increases by 2.5 h. However, the overall pharmacokinetic effect does not change at steady state.

During the use of Baeta®, the AUC and Cmax of lovastatin decreased by approximately 40 and 28%, respectively, and Tmax increased by approximately 4 hours. Co-use of Baeta® with HMG-CoA reductase inhibitors was not accompanied by changes in the blood lipid composition (HDL-cholesterol, LDL-cholesterol, total cholesterol and triglycerides).

In patients with mild or moderate arterial hypertension stabilized by lisinopril (5-20 mg/day), Baeta® did not change the AUC and Cmax of lisinopril at steady state. Tmax of lisinopril at steady state increased by 2 h. There were no changes in the indicators of average daily sBP and dBP.

It was noted that when warfarin was administered 30 minutes after Baeta®, Tmax increased by approximately 2 hours. No clinically significant changes in Cmax and AUC were observed.

The use of Baeta in combination with insulin, D-phenylalanine derivatives, meglitinides, or alpha-glucosidase inhibitors has not been studied.

How to take, course of use and dosage

N / a, in the area of the hip, abdomen, or forearm.

The initial dose is 5 mcg, which is administered 2 times / day at any time during the 60-minute period before the morning and evening meal. Do not administer the drug after a meal. If the drug injection is missed, treatment continues without changing the dose.

1 month after the start of treatment, the dose of the drug can be increased to 10 mcg 2 times / day.

When co-administered with metformin, thiazolidinedione or a combination of these drugs, the initial dose of metformin and / or thiazolidinedione can not be changed. In the case of a combination of Baeta with sulfonylurea derivatives, it may be necessary to reduce the dose of the sulfonylurea derivative in order to reduce the risk of hypoglycemia.

Overdose

Symptoms:  severe nausea and vomiting, as well as rapid development of hypoglycemia (when taking a dose 10 times higher than the maximum recommended dose).

Treatment:  symptomatic therapy is performed, including parenteral use of glucose in the case of severe hypoglycemia.

Special instructions

Intravenous or intramuscular use of the drug is not recommended.

Baeta should not be used if particles are found in the solution or if the solution is cloudy or has a staining.

Against the background of therapy with Baeta, antibodies to exenatide may appear. However, this does not affect the frequency and types of reported side effects.

Patients should be informed that treatment with Baeta may lead to a decrease in appetite and / or body weight and that due to these effects, there is no need to change the dosage regimen.

Before starting treatment with Baeta, patients should read the “Manual for using the pen”provided with the drug.

Form of production

Solution for subcutaneous use

Storage conditions

Store in a dark place, at a temperature of 2-8 °C (do not freeze)

Shelf life

2 years

Active ingredient

Exenacid

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection

Purpose

For adults as directed by your doctor

Indications

Type 2 Diabetes