Yuglin - instructions for use, dose, side effects, contraindications

Active substanceGlikvidonGlikvidon

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Glyurenorm®

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Boehringer Ingelheim International GmbH Germany

Yuglin

pills inwards

Pharmasintez-Tyumen, Open Company Russia

Dosage form: & nbsppills

Composition:

Active substance: glikvidon - 30 mg.

Excipients: lactose monohydrate - 134.0 mg, potato starch - 70.0 mg, sodium carboxymethyl starch - 5.0 mg, silicon dioxide colloid - 0.6 mg, magnesium stearate - 0.4 mg.

Description:Round biconvex tablets white or almost white with a risk.

Pharmacotherapeutic group:Hypoglycemic agent for oral use of the second-generation sulfonylurea group

ATX: & nbsp

A.10.B.B.08 Glikvidon

Pharmacodynamics:

Glikvidon - a hypoglycemic agent for oral use refers to the derivatives of sulfonylureas of the second generation, has pancreatic and extra-pancreatic effects. Stimulates the secretion of insulin, potentiating the glucose-mediated way of insulin formation. In animal experiments it was shown that glycidone reduces insulin resistance in the liver and adipose tissue by increasing the receptors for insulin, as well as stimulation of the insulin mediated post-receptor mechanism.

Hypoglycemic effect develops after 60-90 minutes after ingestion, the maximum of action occurs in 2-3 hours and lasts about 8-10 hours.

Pharmacokinetics:

Suction

After ingestion of a single dose of glycidone (15 or 30 mg), the drug is absorbed quickly and almost completely (80-95%) from the gastrointestinal tract, reaching a plasma concentration of 0.65 μg / ml (range 0.12-2.14 μg / ml). The mean time to reach the maximum concentration (Cmah) of the drug in plasma is 2 hours 15 minutes (range: 1.25-4.75 hours). The value of the area under the curve "concentration-time" (AUC_0-∞) is 5.1 μg / hr / ml (range: 1.5-10.1 μg * h / ml).

There are no differences in pharmacokinetic parameters in patients with diabetes mellitus and in healthy individuals.

Distribution

Glikvidon has a high affinity for plasma proteins (> 99%). There is no data on the possible passage of glycidone or its metabolites through the blood-brain barrier or placenta. There is no data on the possibility of glycidone penetrating into breast milk.

Metabolism

Glikvidon is completely metabolized by the liver, mainly by hydroxylation and demethylation. Metabolites of glycidone do not have or have poorly expressed pharmacological activity in comparison with the initial substance.

Excretion

The major part of metabolites is excreted through the intestine. Only a small part of the metabolites is excreted by the kidneys.In studies, it was shown that after ingestion about 86% of the isotope-labeled drug (¹⁴C) is excreted through the intestine. Regardless of the dose and mode of administration, about 5% (in the form of metabolites) of the administered amount of the drug is excreted by the kidneys. The level of excretion of glycidone by the kidneys remains minimal even with regular administration.

The half-life is 1.2 hours (in the range of 0.4-3.0 hours), the final half-life is approximately 8 hours (in the range of 5.7-9.4 hours).

Elderly patients

Pharmacokinetic parameters are similar in elderly patients and middle-aged patients.

Patients with impaired renal and hepatic function

Since the bulk of the drug is excreted through the intestine, the drug does not accumulate in patients with impaired renal function. There is evidence that the metabolism of the drug does not change in patients with hepatic insufficiency.

Indications:

Diabetes mellitus type 2 in patients of middle and advanced age (with ineffectiveness of diet therapy).

Contraindications:

- Hypersensitivity to sulfonamides, glycidone or any of the excipients of the drug;

- type 1 diabetes mellitus;

- Diabetic acidosis, ketoacidosis, precoma and coma;

- condition after resection of the pancreas;

- acute intermittent porphyria;

- hepatic failure of severe degree;

- Some acute conditions (for example, infectious diseases or large surgical operations);

- rare hereditary diseases, such as galactosemia, lactase deficiency, glucose-galactose malabsorption;

- age to 18 years (due to insufficient data on the efficacy and safety of the drug in this age group).

Carefully:

Feverish syndrome, thyroid disease (with impaired function), deficiency of glucose-6-phosphate dehydrogenase, alcoholism.

Pregnancy and lactation:

There is no data on the use of glycidone in women during pregnancy and breastfeeding. It is not known whether the glycidone or its metabolites into breast milk. Pregnant women with diabetes require careful monitoring of blood glucose concentrations. The intake of oral hypoglycemic drugs in pregnant women does not provide adequate glaucoma and control.Therefore, the use of the drug Yuglin during pregnancy and breastfeeding is contraindicated. In case of pregnancy or when planning pregnancy during treatment with glycvidone, the drug should be canceled and switched to insulin therapy.

Dosing and Administration:

The drug is used inside. It is necessary to follow the doctor's recommendations regarding the dose of the drug and compliance with the diet. Do not stop taking the medication without consulting your doctor.

The initial dose of glycidone is usually 1/2 tablet (15 mg) at breakfast time. The drug must be taken at the beginning of the meal. After taking glycidone, you should not skip meals.

If taking 1/2 tablet (15 mg) does not lead to adequate glycemic control, after consultation with your doctor, the dose of glycidone should be gradually increased. If the daily dose of the drug does not exceed 2 tablets (60 mg), it can be prescribed in 1 reception, during breakfast.

When a higher dose is prescribed, a better effect can be achieved by taking a daily dose divided into 2-3 doses. In this case, the highest dose should be taken at breakfast.An increase in the dose of more than 4 tablets (120 mg / day) usually does not result in a further increase in efficacy.

The maximum daily dose of the drug is 4 tablets (120 mg).

Admission of the drug in patients with impaired renal function

Around 5 % metabolites of the drug is excreted by the kidneys. In patients with impaired renal function, dose adjustment is not required.

Admission of the drug in patients with impaired liver function

Taking a dose exceeding 75 mg in patients with impaired liver function requires careful monitoring of the patient's condition. The drug should not be prescribed to patients with severe hepatic insufficiency, since 95% of the dose is metabolized in the liver and is excreted through the intestine.

Combination Therapy

If there is a lack of clinical effect of monotherapy with Juglin, only the additional appointment of metformin can be recommended.

Side effects:

Violations from the blood and lymphatic system: thrombocytopenia, leukopenia, agranulocytosis.

Metabolic and litany disorders: hypoglycemia, decreased appetite.

Impaired nervous system: headache, dizziness, drowsiness, paresthesia.

Disorders from the side of the organ of vision: violation of accommodation.

Heart Disease: angina, extrasystole.

Vascular disorders: cardiovascular insufficiency, decrease blood pressure.

Disorders from the gastrointestinal tract: nausea, vomiting, constipation, diarrhea, a feeling of discomfort in the abdomen, dryness in the oral cavity.

Disorders from the liver and bile ducts: cholestasis.

Disturbances from the skin and subcutaneous tissues: rash, itching, hives, Stevens-Johnson syndrome, photosensitivity reaction.

General disorders and disorders at the site of administration: pain in the chest, fatigue.

Overdose:

Overdose of sulfonylurea derivatives can lead to hypoglycemia.

Symptoms: tachycardia, increased sweating, hunger, palpitation, tremor, headache, insomnia, irritability, speech and vision impairment, motor anxiety and loss of consciousness.

Treatment: In case of symptoms of hypoglycemia, glucose (dextrose) or foods rich in carbohydrates should be ingested. In severe hypoglycemia (loss of consciousness, coma) intravenously injected with dextrose.After the restoration of consciousness - the reception of digestible carbohydrates (to avoid the re-development of hypoglycemia).

Interaction:

It is possible to intensify hypoglycemic action with simultaneous administration of glycidone and angiotensin-converting enzyme inhibitors, allopurinol, analgesics and nonsteroidal anti-inflammatory drugs, antifungal agents, chloramphenicol, clarithromycin, clofibrate, coumarin derivatives, fluoroquinolones, heparin, monoamine oxidase inhibitors, sulfinpyrazone, sulfonylamides, tetracyclines and tricyclic antidepressants , cyclophosphamide and its derivatives, insulin and oral hypoglycemic agents. Beta-blockers, sympatholytics (including clonidine), reserpine and guanethidine can enhance the hypoglycemic effect and simultaneously mask the symptoms of hypoglycemia.

It is possible to reduce hypoglycemic action with the simultaneous administration of glycidone and aminoglutethimide, sympathomimetics, glucocorticosteroids, thyroid hormones, glucagon, thiazide and loop diuretics, oral contraceptives, diazoxide, phenothiazine, and preparations containing nicotinic acid.

Barbiturates, rifampicin and phenytoin can also reduce the hypoglycemic effect of glycidone.

The increase or decrease in the hypoglycemic effect of glycidone has been described with the use of histamine H2 receptor blockerscimetidine, ranitidine) and ethanol.

Special instructions:

Patients with diabetes should strictly follow the doctor's recommendations. Especially careful control is needed when choosing a dose or when switching from another hypoglycemic drug. Oral hypoglycemic agents should not replace a therapeutic diet, which allows you to control the body weight of the patient. Skipping meals or not following a doctor's recommendation can significantly reduce the concentration of glucose in the blood and lead to unconsciousness. When taking the pill before meals, and not as recommended, at the beginning of the meal, the effect of the drug on the concentration of glucose in the blood is more pronounced, which increases the risk of developing hypoglycemia.

When symptoms of hypoglycemia appear, you should immediately take food containing easily digestible carbohydrates. In the case of persisting hypoglycemia, you should immediately consult a doctor.

Physical activity can exacerbate hypoglycemic effects.

Alcohol or stress may increase or decrease the hypoglycemic effect of sulfonylurea derivatives.

The use of sulfonylurea derivatives in patients with glucose-6-phosphate dehydrogenase deficiency can lead to the development of hemolytic anemia. As glycidone refers to the derivatives of sulfonylureas, caution should be exercised when using the drug in patients with glucose-6-phosphate dehydrogenase deficiency and, if possible, it is necessary to decide on the drug change.

One tablet of the drug Yuglin contains 134.0 mg of lactose (536.0 mg of lactose in the maximum daily dose). Patients with rare hereditary diseases, such as galactosemia, lactase deficiency, glucose-galactose malabsorption, should not take the drug.

Glikvidon refers to short-acting sulfonylureas and is therefore used in patients with type 2 diabetes with an increased risk of hypoglycemia, for example in elderly patients and patients with impaired renal function.Since the excretion of glycidone by the kidneys is insignificant, the drug Yuglin can be used in patients with renal insufficiency and diabetic nephropathy. However, treatment of patients with severe renal insufficiency should be carried out under close medical supervision.

There is evidence that the use of glycidone in patients with type 2 diabetes mellitus having concomitant liver disease is effective and safe. Only the excretion of inactive metabolites in these patients is somewhat delayed. In clinical studies in patients with diabetes mellitus and violations of liver function of varying severity (including acute cirrhosis of the liver with portal hypertension), glycidone did not cause further impairment of liver function, the incidence of side effects did not increase, hypoglycemic reactions were not detected. However, patients with diabetes mellitus and concomitant hepatic insufficiency of severe degree are not recommended.

During clinical trials, it was found that the use of glycidone for 18 and 30 months did not lead to an increase in body weight, even there were cases of weight loss of 1-2 kg.In comparative studies with other derivatives sulfonylureas, it was shown that in patients taking glycidone more than a year, there are no significant changes in body weight.

Effect on the ability to drive transp. cf. and fur:

There is no data on the effect of the drug on the ability to drive vehicles, mechanisms. However, patients should be warned about such manifestations of hypoglycemia as drowsiness, dizziness, disruption of accommodation, which may occur when taking the drug. Care must be taken when driving vehicles and mechanisms. When hypoglycemic conditions should be avoided the management of vehicles, mechanisms.

Form release / dosage:Tablets, 30 mg.

Packaging:

Primary packaging

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

At 30.60 and 120 tablets in a jar of low-pressure polyethylene with a cover pulled with the control of the first opening. Free space is filled with cotton wool. On cans are labeled from paper label or from polymer materials, self-adhesive.

Secondary packaging

For 3 or 6 contour squares, together with the instructions for use, they are placed in a pack of cardboard for consumer containers.

On 1 bank together with instructions on application place in a pack from a cardboard for consumer tare.

Storage conditions:

In the original packaging of the manufacturer at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-004519

Date of registration:31.10.2017

Expiration Date:31.10.2022

The owner of the registration certificate:Pharmasintez-Tyumen, Open CompanyPharmasintez-Tyumen, Open Company Russia

Manufacturer: & nbsp

FARMASINTEZ, JSC (Irkutsk) Russia

Pharmasintez-Tyumen, Open Company Russia

Information update date: & nbsp23.11.2017

Illustrated instructions

Instructions

Yuglin (Uglin)