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

Excipients, calcium stearate - 4.0 mg, hypromellose (metocel K 100 LV CR Premium, metolose 90SH-100SH) - 148.0 mg, silicon dioxide colloid (aerosil) 2.0 mg, talc 12.0 mg, lactose monohydrate (tablettose 80) - 174.0 mg.

Description:

Round tablets of white or almost white color, flat-cylindrical with a facet and a risk. Presence of marble is admissible.

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

ATX: & nbsp

A.10.B.B.09 Gliclazide

Pharmacodynamics:

Gliclazide is a derivative of sulfonylurea, a hypoglycemic preparation for oral administration, which differs from similar drugs by the presence N- containing heterocyclic ring with an endocyclic linkage.

Gliklazid reduces the concentration of blood glucose, stimulating the secretion of insulin beta cells of the islets of Langerhans. The increase in the concentration of postprandial insulin and C-peptide persists after 2 years of therapy.

Addition effects on carbohydrate metabolism glycazide has hemovascular effects.

Influence on secretion of insulin

In type 2 diabetes, the drug restores the early peak of insulin secretion in the glucose intake report and enhances the second phase of insulin secretion. A significant increase in insulin secretion is observed in response to stimulation caused by food intake or the introduction of glucose.

Hemovascular effects

Gliklazid reduces the risk of thrombosis of small vessels, affecting the mechanisms that can cause the development of complications in diabetes mellitus: partial inhibition of platelet aggregation and adhesion and a decrease in the concentration of platelet activating factors (beta-thromboglobulin, thromboxane B2), as well as to restore the fibrinolytic activity of the vascular endothelium and increase the activity of the tissue activator of plasminogen.

Intensive glycemic control based on the use of modified-release glycazide (target glycosylated hemoglobin (HbAlc) < 6,5 %) significantly reduces the risk of micro- and macrovascular complications of type 2 diabetes mellitus, in comparison with standard glycemic control.

Pharmacokinetics:

Suction

After oral administration glycazide completely absorbed.The concentration of glycazide in the blood plasma increases gradually, leaving the plateau after 6 hours and maintained for 6-12 hours. Individual variability is low.

Eating does not affect the rate or degree of absorption of the glycazide.

Distribution

About 95% of the glycazide binds to plasma proteins. The volume of distribution is about 30 liters. Taking the drug at a dose of 60 mg once a day ensures the maintenance of an effective concentration of gliclazide in the blood plasma for more than 24 hours.

Metabolism

Gliklazid is metabolized primarily in the liver. There are no active metabolites in the blood plasma.

Excretion

Gliklazid is excreted mainly by the kidneys: excretion is carried out in the form of metabolites, less than 1% is excreted by the kidneys unchanged. The half-life of gliclazide averages from 12 to 20 hours.

Linearity

The relationship between the dose taken (up to 120 mg) and the area under the pharmacokinetic curve "concentration-time" is linear.

Aged people

In elderly people, there are no significant changes in pharmacokinetic parameters.

Indications:

Diabetes mellitus type 2 with insufficient effectiveness of diet therapy, exercise and weight loss.
Prevention of complications of diabetes mellitus: reducing the risk of microvascular (nephropathy, retinopathy) and macrovascular complications (myocardial infarction, stroke) in patients with type 2 diabetes by intensive glycemic control.

Contraindications:

hypersensitivity to glycazide, other derivatives of sulfonylurea, sulfonamides or to the auxiliary substances included in the preparation;
type 1 diabetes mellitus;
Diabetic ketoacidosis, diabetic precoma, diabetic coma;
severe renal or hepatic insufficiency (in these cases it is recommended to use insulin);
lactose intolerance, lactase deficiency, glucose-galactose malabsorption (due to the presence of lactose monohydrate);
taking miconazole (see section "Interaction with other drugs");
pregnancy and the period of breastfeeding (see the section "Pregnancy and the period of breastfeeding");
age to 18 years due to lack of data on efficacy and safety of use.

It is not recommended to use in combination with phenylbutazone or danazol (see Fig.section "Interaction with other drugs")

Carefully:

Elderly age, irregular and / or unbalanced diet, insufficiency of glycocose-6-phosphate dehydrogenase, severe cardiovascular diseases (including number, ischemic heart disease, atherosclerosis), hypoituitarism, hypothyroidism, adrenal or pituitary insufficiency, renal and / or hepatic insufficiency, long-term glucocorticosteroid therapy, alcoholism.

Pregnancy and lactation:

Experience with the drug during pregnancy is absent. Data on the application

other derivatives of sulfonylureas during pregnancy are limited.

In studies on laboratory animals, teratogenic affects of glycazide were not identified.

To reduce the risk of developing congenital malformations, optimal control (appropriate therapy) of diabetes before optimal conception is necessary. Oral hypoglycemic drugs during pregnancy are not applied. Insulin is the drug of choice for the therapy of diabetes mellitus in pregnant women. It is recommended to replace the intake of oral hypoglycemic drugs with insulin therapy in the case of a planned pregnancy,if the pregnancy occurred against the background of taking oral hypoglycemic drugs. Given the lack of data on the flow of gliclazide into breast milk and the risk of neonatal hypoglycemia, during therapy with breastfeeding is contraindicated.

Dosing and Administration:

PrePArat is intended only for the treatment of adults.

The recommended dose of the drug should be taken orally, once a day, preferably during breakfast.

The daily dose can be 30-120 mg (1 / 2-2 tablets) in one session.

It is recommended to swallow a pill or half of the whole tablet without chewing or grinding.

If you skip one or more doses of the drug, you can not take a higher dose to the next dose, the missed dose should be taken the next day.

As with other hypoglycemic drugs, the drug dose in each case should be selected individually depending on the concentration of blood glucose and glycosylated hemoglobin (NAls).

Initial dose

The initial recommended dosage (including elderly patients> 65 years old) - 30 mg per day (half a tablet).

In case of adequate control, the drug in this dose can be used for maintenance therapy. With inadequate glycemic control, the daily dose of the drug can be sequentially increased to 60, 90 or 120 mg.

Increase in the dose is possible not earlier than after 1 month of therapy with the drug in the previously prescribed dose. Exception is made by patients, in whom the blood glucose concentration did not decrease after 2 weeks of therapy. In such cases, the dose of the drug may be increased 2 weeks after the start of the treatment.

The maximum recommended daily dose of the drug is 120 mg.

1 tablet of the drug Diabeticonium tablets with a sustained release of 60 mg is equivalent to 2 tablets of the drug Diabetolong tablets with a modified release of 30 mg. Presence of risks on 60 mg tablets allows you to divide the pill and take the daily dose as 30 mg (1/2 tablet 60 mg) and if necessary 90 mg (1 and 1/2 tablets 60 mg).

Transition from taking another hypoglycemic drug to Diabetolong® sustained release tablets 60 mg

Diabetolong Diabetes Tablets with prolonged release of 60 mg can be used in place of another hypoglycemic drug for oral administration.In this case, their dose and half-life should be taken into account. As a rule, a transition period is not required. The initial dose should be 30 mg and then should be titrated depending on the concentration of blood glucose.

When you replace the drug Diabetalong sulfonylureas with a long half-life in order to avoid hypoglycemia caused by the additive effect of two hypoglycemic agents, you can stop taking them for several days. The initial dose of the drug Diabetolong is also 30 mg (1/2 tablet 60 mg) and, if necessary, can be further increased as described above.

Combination with another hypoglycemic drug

The drug can be used in combination with biguanides, alpha-glucosidase inhibitors or insulin.

With inadequate glycemic control, additional insulin therapy should be prescribed with careful medical supervision.

Elderly patients

Correction of the dose of the drug for patients over 65 years is not required.

Patients with renal insufficiency

The results of clinical studies showed that correction of the dose of the drug in patients with mild and moderate renal insufficiency is not required.It is recommended that a thorough medical control

Patients at risk of developing hypoglycemia

In patients who are at risk for developing hypoglycemia (insufficient or unbalanced diet, severe or poorly compensated endocrine disorders - pituitary and adrenal insufficiency, hypothyroidism, elimination of glucocorticosteroids after long-term administration and / or intake in high doses, severe cardiovascular disease, cardiovascular system - severe ischemic heart disease, severe atherosclerosis of the carotid arteries, widespread atherosclerosis), it is recommended to use the minimum dose (30 mg) of the drug a.

Prevention of complications of diabetes mellitus

To achieve intensive glycemic control, you can gradually increase the dose of the drug to 120 mg / day in addition to diet and exercise until the target level of HbAlc. It should be remembered about the risk of developing hypoglycemia. In addition, other hypoglycemic drugs may be added to therapy, for example, metformin, an alpha-glucosidase inhibitor, a thiazolidinedione derivative or insulin.

Side effects:

Considering the experience of using glycazide, one should remember about the possibility of developing the following side effects.

Hypoglycaemia

Like other sulfonylureas preparations Diabetalong drug may cause hypoglycemia in the case of irregular ingestion, and particularly if meal skipped. Possible symptoms of hypoglycemia include headache, severe hunger, nausea, vomiting, fatigue, sleep disturbance, irritability, agitation, decreased concentration, slowed reactions, depression, confusion, impaired vision and speech, aphasia, tremor, paresis, self-loss , helplessness, impaired perception, dizziness, weakness, convulsions, bradycardia, lightheadedness, shortness of breath, drowsiness, loss of consciousness with the possible development of coma, or death.

Also can be marked adrenergic reactions: sweating, "sticky" skin, anxiety, tachycardia, hypertension, palpitations, arrhythmia, and angina pectoris.

As a rule, the symptoms of hypoglycemia are stopped by the intake of carbohydrates (sugar). The intake of sugar substitutes is ineffective.Against the background of other derivatives of sulfonylureas, there were relapses of hypoglycemia after its successful cupping.

With severe or prolonged hypoglycemia, emergency medical care is indicated, possibly with hospitalization, even if there is an effect of taking carbohydrates.

Other side effects

From the gastrointestinal tract: abdominal pain, nausea, vomiting, diarrhea, constipation. Taking the drug during breakfast allows you to avoid these symptoms or minimize them.

From the skin and subcutaneous tissue: rash, itching, hives, Quincke's edema, erythema, maculopapular rash, bullous reactions (Stevens-Jones syndrome, toxic epidermal necrolysis).

On the part of the organs of hematopoiesis and lymphatic system: hematological disorders (anemia, leukopenia, thrombocytopenia, granulocytopenia). As a rule, these phenomena are reversible in the event of discontinuation of therapy.

From the liver and bile ducts: increased activity of "hepatic" enzymes (aspartate aminotransferase (ACT), alanine aminotransferase (ALT), brush phosphatase), hepatitis (isolated cases). When cholestatic jaundice occurs, therapy should be discontinued.

These phenomena are usually reversible in the event of discontinuation of therapy.

From the sense organs: may occur transient visual disorders caused by changes in blood glucose concentration, especially at the beginning of therapy.

Side effects inherent in sulfonylurea derivatives: erythrocytopenia, agranulocytosis, hemolytic anemia, pancytopenia, allergic vasculitis, hyponatremia. There was an increase in the activity of "hepatic" enzymes, a violation of liver function (for example, with the development of cholestasis and jaundice) and hepatitis; manifestations decreased with time after the withdrawal of sulfonylureas, but in some cases led to life-threatening liver failure.

Overdose:

In case of an overdose of sulfonylureas, hypoglycemia may develop. If mild symptoms of hypoglycemia occur without a loss of consciousness or neurological symptoms, you should increase the intake of carbohydrates with food, reduce the dose of the drug and / or change the diet. Close medical observation of the patient's condition should continue until the norm, until there is no certainty that his health is not threatened.

Possible development of severe hypoglycemic conditions, accompanied by coma, seizures or other neurological disorders.If such symptoms appear, emergency medical care and immediate hospitalization are necessary.

In the case of hypoglycemic coma or if it is suspected, 50 ml of a 20-40% solution of dextrose (glucose) is injected intravenously. Then 10% dextrose solution is administered intravenously dropwise to maintain a glucose concentration in the blood above 1 g / l. Careful monitoring of blood glucose and monitoring of the patient should be carried out for at least 48 consecutive hours. After this period of time, depending on the patient's condition, the attending physician decides on the need for further observation.

Dialysis is ineffective due to the expressed binding of gliclazide to blood plasma proteins

Interaction:1) Drugs and substances that increase the risk of hypoglycemia:

(enhancing the action of gliclazide)

Contraindications

- Miconazole (with systemic administration and with the use of gel on the mucous membrane of the mouth): enhances the hypoglycemic effect of glycazide (hypoglycemia may develop up to the state of coma).

Unrecommended combinations

- Phenylbutazone (systemic administration): enhances the hypoglycemic effect of sulfonylurea derivatives (displaces them from binding to plasma proteins and / or slows their elimination from the body). It is more preferable to use another anti-inflammatory drug. If the reception of phenylbutazone is necessary, the patient should be warned about the need for glycemic control if necessary. The dose of Diabeticon should be adjusted during the administration of phenylbutazone and after its completion.
- Ethanol: increases hypoglycemia, inhibiting compensatory reactions, can contribute to the development of hypoglycemic coma. It is necessary to refuse from taking medicines, which include ethanol, and the use of alcohol.

Combinations that require precautions

Admission gliclazide in combination with some drugs: other hypoglycemic agents (insulin, acarbose, metformin, thiazolidinidiones, inhibitors of dipeptidyl peptidase-4, glucagon-like peptide-1 receptor agonists (GLP-1)); beta-adrenoblockers, fluconazole; inhibitors of angiogenesis-converting enzyme - captopril, enalapril; blockers H₂-gistaminovyh receptors; monoamine oxidase inhibitors; sulfonamides; clarithromycin and non-steroidal anti-inflammatory drugs, is accompanied by increased hypoglycemic effect and risk of hypoglycemia.

2) Preparations, contributing to increased blood glucose: (weakening action of Glyclazide)

Unrecommended combinations

- Danazol: has a diabetic effect. AT If the drug is needed, the patient should be carefully monitored for blood glucose. If it is necessary to simultaneously use drugs, it is recommended to select a dose of hypoglycemic agent both during danazol administration and after its cancellation.

Combinations that require precautions
- Chlorpromazine (antipsychotic): in high doses (more than 100 mg per day) increases the concentration of blood glucose, reducing the secretion of insulin. Careful glycemic control is recommended. If it is necessary to simultaneously use drugs, it is recommended to select a dose of hypoglycemic agent both during the administration of the antipsychotic and after its withdrawal.
- GCS (systemic and topical application: intraarticular, external, rectal administration) and tetracosactide: increases the concentration of blood glucose with the possible development of ketoacidosis (reduced tolerance to carbohydrates). Careful glycemic control is recommended, especially at the beginning of treatment. If it is necessary to use drugs simultaneously, it may be necessary to correct the dose of hypoglycemic agent both during the reception of GCS, and after their cancellation.
- Ritodrin, salbutamol, terbutaline (intravenous administration): beta-2-adrenomimetics help increase blood glucose concentration.

It is necessary to pay special attention to the importance of independent glycemic control. If necessary, it is recommended to transfer the patient to insulin therapy.

3) Combinations that must be taken into account:

- Anticoagulants (eg, warfarin): sulfonylureas derivatives can enhance the effect of anticoagulants with simultaneous application. You may need to adjust the dose of anticoagulant.

Special instructions:

Hypoglycaemia

When taking sulfonylurea derivatives, including Diabeticone, hypoglycaemia may develop,in some cases - in a severe and prolonged form, requiring hospitalization and intravenous administration of a dextrose solution for several days (see the "Side effect" section).

The drug can be prescribed only to those patients, whose meals are regular and includes breakfast. It is very important to maintain sufficient intake of carbohydrates with pizza, as the risk of developing gynoglycemia increases with irregular or inadequate nutrition, as well as when consuming food poor in carbohydrates. Hypoglycemia often develops with a low-calorie diet, after prolonged or vigorous exercise, after drinking alcohol or taking several hypoglycemic drugs at the same time.

Typically, the symptoms of hypoglycemia go away after eating a meal rich in carbohydrates (such as sugar). It should be borne in mind that the use of sugar substitutes does not help to eliminate hypoglycemic symptoms. The experience of using other sulfonylurea derivatives suggests that hypoglycemia can recur despite effective initial arrest of this condition.In the event that hypoglycemic symptoms have a pronounced character or are prolonged, even in the case of temporary improvement after a meal rich in carbohydrates, it is necessary to provide emergency medical care, up to hospitalization.

In order to avoid the development of hypoglycemia, careful individual selection of drugs and dosing regimens is necessary, as well as providing the patient with complete information about the treatment.

An increased risk of hypoglycemia may occur in the following cases:

Failure or inability of the patient (especially the elderly) to follow the doctor's appointments and monitor his condition;
Insufficient and irregular meals, skipping meals, fasting and changing rations;
an imbalance between exercise and the amount of carbohydrates taken;
Point insufficiency;
severe hepatic impairment;
an overdose of Diabetolong;
Some endocrine disorders: thyroid disease, pituitary and adrenal insufficiency;
concomitant use of certain medicines.section "Interaction with other drugs").

Renal and hepatic impairment

In patients with hepatic and / or severe renal insufficiency, the pharmacokinetic and / or pharmacodynamic properties of the glycazide can vary. The condition of hypoglycemia, developing in such patients, can be quite long, in such cases, immediate appropriate therapy is needed.

Information for patients

It is necessary to inform the patient, as well as members of his family about the risk of developing hypoglycemia, its symptoms and conditions conducive to its development. The patient should be informed of the potential risks and benefits of the proposed treatment.

The patient needs to explain the importance of dieting, the need for regular exercise and control of blood glucose.

Insufficient glycemic control

Glikemic control in patients receiving therapy with hypoglycemic agents may be weakened in the following cases: fever, trauma,

Infectious diseases or large surgical interventions.With these conditions, it may be necessary to stop Diabeticon and prescribe insulin therapy.

In many patients, the effectiveness of oral hypoglycemic agents, including Diabetolong®, tends to decline after a long treatment period. This effect can be due to both the progression of the disease and the decrease in the therapeutic response to the drug. This phenomenon is known as secondary drug resistance, which must be distinguished from the primary, in which the drug already at the first appointment does not give the expected clinical effect. Before diagnosing the patient's secondary drug resistance, it is necessary to evaluate the adequacy of dose selection and patient compliance with the prescribed diet.

Laboratory Tests

For evaluation of glycemic control, regular determination of fasting blood glucose and glycosylated hemoglobin HbAlc. In addition, it is advisable to regularly conduct self-monitoring of blood glucose concentration. Sulfonylurea derivatives can cause hemolytic anemia in patients with deficiency of glucose-6-phosphate dehydrogenase.Because the glycazide is a derivative of sulfonylureas, caution should be exercised when it is administered to patients with deficiency of glucose-6-phosphate dehydrogenase. One should evaluate the possibility of prescribing a hypoglycemic drug of another group.

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

In connection with the possible development of hypoglycemia in the use of Diabetolong, patients should be aware of the symptoms of hypoglycemia and should be careful when driving vehicles or performing work that requires a high rate of physical and mental reactions, especially at the beginning of therapy.

Form release / dosage:

Tablets with prolonged release of 60 mg.

Packaging:

For 10 or 20 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

According to 1, 2, 3, 6 contour cell packs of 10 tablets or 1, 3, 5, 6 contour cell packs of 20 tablets with instructions for use are placed in a pack of cardboard.

Storage conditions:

In the dark place 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-003155

Date of registration:25.08.2015

The owner of the registration certificate:MS-VITA, LLC MS-VITA, LLC Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Representation: & nbspSYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products SYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products Russia

Information update date: & nbsp11.01.2016

Illustrated instructions

Instructions

Diabetolong (Diabetalong)