Byetta
Byeta: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Byetta
ATX code: A10BX04
Active ingredient: Exenatide (Exenatide)
Manufacturer: Baxter Pharmaceutical Solutions (USA)
Description and photo updated: 30.11.2018
Prices in pharmacies: from 4979 rubles.
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Byetta is a glucagon-like polypeptide receptor agonist, a hypoglycemic agent.
Release form and composition
Dosage form - a solution for subcutaneous (s / c) administration: transparent, colorless (1.2 or 2.4 ml in a cartridge installed in a syringe pen, in a cardboard box 1 syringe pen and instructions for using Byeta).
Composition of 1 ml solution:
- active substance: exenatide - 250 mcg;
- auxiliary components: metacresol, mannitol, acetic acid, sodium acetate trihydrate, water for injection.
Pharmacological properties
Pharmacodynamics
The active substance of Byeta is exenatide, a 39-amino acid aminopeptide, a mimetic of the glucagon-like polypeptide receptors.
It is a potent agonist of incretins, such as glucagon-like peptide-1 (GLP-1), which improve β-cell function, increase glucose-dependent insulin secretion, suppress inadequately increased glucagon secretion, slow down gastric emptying (after entering the general bloodstream from the intestine), and have other hypoglycemic effects. Thus, Exenatide improves glycemic control in type 2 diabetes.
The amino acid sequence of Exenatide closely matches the sequence of human GLP-1, due to which the drug binds to the GLP-1 receptors in humans and activates them. As a result, glucose-dependent synthesis and secretion of insulin from β-cells of the pancreas are enhanced with the participation of cyclic adenosine monophosphate (AMP) and / or other intracellular signaling pathways. Exenatide promotes the release of insulin from β-cells in case of increased glucose concentration.
In terms of chemical structure and pharmacological action, Exenatide differs from alpha-glucosidase inhibitors, sulfonylurea derivatives, insulin, biguanides, meglitinides, thiazolidinediones and D-phenylalanine derivatives.
Glycemic control in type 2 diabetes is improved through the following mechanisms:
- glucose-dependent insulin secretion: Exenatide enhances glucose-dependent insulin secretion from pancreatic β-cells in patients with hyperglycemic conditions. As the level of glucose in the blood decreases, insulin secretion decreases, after approaching the norm, it stops, thereby reducing the potential risk of hypoglycemia;
- the first phase of the insulin response: in type 2 diabetes mellitus, insulin secretion is specifically absent during the first 10 minutes. Moreover, the loss of this phase is an early dysfunction of β-cells. The use of Exenatide restores or significantly enhances the first and second phases of the insulin response;
- Glucagon secretion: in the case of hyperglycemia, Exenatide suppresses excess glucagon secretion, while not interfering with the normal glucagon response to hypoglycemia;
- food intake: Exenatide reduces appetite and, as a result, the amount of food consumed;
- gastric emptying: By suppressing gastric motility, exenatide slows down gastric emptying.
Application of type 2 diabetes exenatide in combination with a thiazolidinedione, metformin and / or sulfonylurea contributes to lower blood glucose level of fasting and postprandial blood glucose, and hemoglobin A1c (Hb A1 c), than improves glycemic control.
Pharmacokinetics
After subcutaneous administration, Exenatide is rapidly absorbed. The average maximum concentration (C max) is reached within 2.1 hours and is 211 pg / ml.
The area under the concentration-time curve (AUC) after s / c administration of Exenatide at a dose of 10 μg - 1036 pg × h / ml, this figure increases in proportion to the dose increase, but does not affect C max. The same effect was noted with subcutaneous administration of Byeta in the shoulder, abdomen or thigh.
The volume of distribution (V d) is approximately 28.3 liters. It is excreted mainly by glomerular filtration with subsequent proteolytic degradation. The ground clearance is about 9.1 l / h. The final half-life (T ½) is 2.4 hours. The indicated pharmacokinetic parameters of the drug do not depend on the dose.
The measured concentrations are determined approximately 10 hours after the administration of a dose of Exenatide.
Pharmacokinetics in special cases:
- impaired renal function: with mild and moderate functional impairments [creatinine clearance (CC) 30–80 ml / min], significant differences in the pharmacokinetics of Exenatide are not detected, therefore dose adjustment is not required. In patients with end-stage renal failure on dialysis, the clearance of the drug decreases to about 0.9 l / h (in healthy patients - 9.1 l / h);
- impaired liver function: significant differences in the plasma concentration of Exenatide were not found, since the drug is excreted mainly by the kidneys;
- age: in children, the pharmacokinetics of Exenatide has not been studied; in adolescents 12–16 years old with type 2 diabetes mellitus, when using Exenatide at a dose of 5 μg, pharmacokinetic parameters similar to those in adult patients were revealed; in the elderly, there are no changes in pharmacokinetic characteristics, therefore, dose adjustment is not required;
- gender and race: significant differences in the pharmacokinetics of exenatide between women and men are not observed, race also does not significantly affect this parameter;
- body weight: no significant correlation was found between body mass index and exenatide pharmacokinetics.
Indications for use
As a monotherapy for type 2 diabetes, Byetu is used in addition to diet therapy and exercise to achieve adequate glycemic control.
As part of combination therapy for type 2 diabetes mellitus, Byetu is used to improve glycemic control in the following cases:
- in addition to metformin / sulfonylurea derivative / thiazolidinedione / metformin + sulfonylurea derivative combination / metformin + thiazolidinedione combination;
- in addition to the combination of basal insulin + metformin.
Contraindications
Absolute:
- type 1 diabetes mellitus;
- diabetic ketoacidosis;
- severe diseases of the gastrointestinal tract with concomitant gastric paresis;
- acute pancreatitis;
- severe renal failure (CC <30 ml / min);
- age up to 18 years;
- period of pregnancy and lactation;
- hypersensitivity to any component of the drug.
The drug Byeta should be used with caution in patients with a history of pancreatitis.
Byetta, instructions for use: method and dosage
Byetta's solution is injected subcutaneously into the abdomen, thigh, or shoulder area.
At the beginning of treatment, the drug is prescribed 5 mcg 2 times a day before meals (at any time within a 60-minute period before breakfast and dinner; do not administer after meals). If the next dose is missed, you should not double it, you must adhere to the usual schedule.
If glycemic control is insufficient, a month later, the dose of Byeta may be increased to 10 μg 2 times a day.
When carrying out combination therapy, the dose of metformin, thiazolidinedione, or their combination may not be changed. When prescribing sulfonylurea or insulin derivatives, their dose may need to be reduced.
Side effects
Side effects of Byetta, which were reported more often than in isolated cases, were classified as follows: very often - ≥ 10%, often - from ≥ 1% to 0.1% to 0.01% to <0.1%, very rarely - <0.01%.
Monotherapy
- very often: itching at the injection site;
- often: decreased appetite, dyspepsia, diarrhea, nausea, vomiting, dizziness, hypoglycemia;
- rarely: skin reactions at the injection site (rash, redness).
Combination therapy
- very often: hypoglycemia (with the simultaneous use of sulfonylurea derivatives), diarrhea, nausea, vomiting, itching at the injection site;
- often: decreased appetite, dyspepsia, gastroesophageal reflux, headache, trembling, weakness, dizziness;
- infrequently: violation of taste, bloating, abdominal pain, flatulence, belching, constipation;
- rarely: rash and redness at the injection site, dehydration (often associated with nausea, vomiting and / or diarrhea), drowsiness, acute pancreatitis, impaired renal function (including an increase in serum creatinine concentration, acute renal failure or worsening of the course chronic renal failure), angioedema;
- very rare: anaphylactic reaction, increased blood clotting time, sometimes accompanied by bleeding (with the simultaneous use of warfarin).
In general, adverse reactions were mild or moderate and did not require discontinuation of therapy. The reported nausea was most often dose-dependent, decreased with continued treatment, and did not interfere with daily activities.
With the joint appointment of sulfonylurea derivatives, the frequency of hypoglycemia increases, which may require a decrease in their dose. Most episodes of hypoglycemia are mild to moderate in intensity and are controlled by ingestion of carbohydrates.
Post-marketing messages
- from the digestive system: flatulence, constipation, belching; rarely - acute pancreatitis; very rarely - hemorrhagic or necrotizing pancreatitis;
- from the nervous system: drowsiness, dysgeusia;
- on the part of the urinary system: changes in renal function (including an increase in serum creatinine concentration, acute renal failure or worsening of the course of chronic renal failure);
- on the part of nutrition and metabolism: dehydration (usually due to nausea, vomiting and / or diarrhea), weight loss;
- from the immune system: very rarely - anaphylactic reaction;
- on the part of the skin and subcutaneous tissue: itching, urticaria, papular or macular skin rashes, alopecia, angioedema;
- laboratory data: when combined with warfarin - an increase in the INR (International Normalized Ratio), in some cases associated with the development of bleeding.
Overdose
In the case of taking a dose that is 10 times higher than the maximum recommended, such disturbances as severe nausea, vomiting, severe hypoglycemia are possible.
Overdose treatment is symptomatic. With severe hypoglycemia, dextrose solution is administered intravenously.
special instructions
Byet's solution cannot be administered intravenously or intramuscularly. It is forbidden to enter after meals.
The drug should not be used in case of a change in the appearance of the solution: turbidity, staining, precipitation.
Before starting treatment, you should carefully study the attached "Guidelines for using a syringe pen".
Given the potential immunogenicity of drugs containing peptides and proteins, antibodies to Exenatide can be produced during therapy with Byetta. In most of these patients, the antibody titer decreased with continued use of the drug and remained low for 82 weeks. The presence of antibodies does not affect the types of reported side effects and their frequency.
Patients should be warned that Byetta may reduce appetite and / or promote weight loss, but this phenomenon is not a reason to change the dosage regimen.
There are rare cases of functional renal impairment (increased serum creatinine levels, development of renal failure, including acute, or worsening of chronic renal failure), some patients required hemodialysis. Some disorders have occurred in patients who simultaneously received one or more drugs that affect renal function and / or water metabolism, as well as in the case of concomitant hydration disorders such as diarrhea, nausea and / or vomiting. Concurrently used drugs included non-steroidal anti-inflammatory drugs, angiotensin-converting enzyme inhibitors, and diuretics. After discontinuation of the drug, presumably causing the pathological changes, and symptomatic therapy, the impaired renal function was restored. In preclinical and clinical studies, no direct nephrotoxicity of Exenatide has been identified.
There have been rare reports of cases of acute pancreatitis during the period of Byeta's use. Patients should be warned about the need for immediate medical attention if severe persistent abdominal pain occurs. Symptomatic therapy is required.
In preclinical studies in rodents, the carcinogenic effect of Exenatide has not been established. When a dose was used in rats, which was 128 times higher than that in humans, a quantitative increase in C-cell adenomas of the thyroid gland without any signs of malignancy was noted, which was associated with an increase in the life expectancy of animals receiving Exenatide.
Application during pregnancy and lactation
Byetta is contraindicated in pregnant and breastfeeding women.
Pediatric use
Byeta is not used in children and adolescents (under 18 years old).
With impaired renal function
With mild and moderate functional renal impairment (CC 30–80 ml / min), dose adjustment is not required.
In severe renal failure (CC <30 ml / min), Byetta is contraindicated.
For violations of liver function
With functional disorders of the liver, the therapy regimen is not adjusted.
Use in the elderly
For elderly patients, Byetu is prescribed in the same doses as for younger patients.
Drug interactions
With caution, Byetu should be used in combination with other oral drugs that require rapid absorption from the gastrointestinal tract, since Exenatide can delay gastric emptying. Medicines, the action of which depends on their threshold concentration (for example, antibiotics), should be taken at least 1 hour before the administration of Byeta. If these drugs must be taken with meals, then this should be done during meals before which Exenatide is not administered.
Exenatide increases the C max of digoxin (applied at 0.25 mg once a day) by 17%, and the time to reach C max by 2.5 hours. AUC does not change in equilibrium.
With the combined use of warfarin 35 minutes after Byeta, the time to reach C max by 2 hours is increased. Clinically significant changes in the maximum concentration and the area under the concentration-time curve were not observed.
In lisinopril (in daily doses from 5 to 20 mg), used in patients with mild and moderate arterial hypertension, with the simultaneous use of Byeta, C max and AUC do not change, however, in an equilibrium state, the time to reach C max increases by 2 hours. time indices of average daily diastolic and systolic blood pressure do not change.
Byetta reduces the C max and AUC of lovastatin by 28 and 40%, respectively, increases the time to reach its C max by about 4 hours. The simultaneous use of HMG-CoA reductase inhibitors is not accompanied by changes in the lipid composition of the blood (total cholesterol, low and high density lipoproteins, thyroglobulin).
The use of Byetta in combination with alpha-glucosidase inhibitors, meglitinides and D-phenylalanine derivatives has not been studied.
Analogs
Byeta's analogs are: Byeta Long, Victoza, Lixumia, Saxenda, Trulicity, etc.
Terms and conditions of storage
Store at a temperature of 2-8 ° C out of the reach of children, protected from light. Avoid freezing.
The shelf life is 3 years.
The used syringe pen should be stored for no more than 30 days at temperatures up to 25 ° C.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Baet
Reviews about Bayt are mostly positive: the drug allows you to effectively control blood sugar levels. Additional benefits include decreased appetite and weight loss. Many consider the disadvantage of the need for daily injections, therefore, they prefer tabletted hypoglycemic agents.
Byeta's cost is generally high.
The price of Byetu in pharmacies
Approximate prices for Byetu: 1 syringe pen with a 1.2 ml cartridge - 4660–5479 rubles, 1 syringe pen with a 2.4 ml cartridge - 7200–8790 rubles.
Byeta: prices in online pharmacies
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Drug name Price Pharmacy |
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Byetta 250 mcg / ml 5 mcg solution for subcutaneous administration 1.2 ml 1 pc. 4979 RUB Buy |
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Byetta 250 mcg / ml 10 mcg solution for subcutaneous administration 2.4 ml 1 pc. RUB 7615 Buy |
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Byetta Long 2 mg powder for suspension for subcutaneous administration of prolonged action 4 pcs. 10959 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
