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

Excipients: hypromellose (methocel K 100 LV CR Premium) - 74 mg, silicon dioxide colloid (aerosil) - 1 mg, calcium stearate - 2 mg, talc - 6 mg, lactose monohydrate (tabletose 80) - 87 mg.

Description:

Tablets white or almost white, flat-cylindrical, with a bevel. 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:

Oral hypoglycemic agent, derivative of sulfonylureas of the second generation.

It stimulates the secretion of insulin by the pancreas, lowers blood glucose levels, enhances the insulin secretory effect of glucose and increases the sensitivity of peripheral tissues to insulin. After 2 years of treatment, most patients do not develop addiction to the drug (the level of postprandial insulin and the secretion of C-peptides remain).

Reduces the time interval from the time of food intake to, the beginning of secretion of insulin. Restores the early peak of insulin secretion in response to the intake of glucose (unlike other sulfonylurea derivatives that have an effect, mainly,during the second stage of secretion). It also enhances the second phase of insulin secretion. Reduces the peak of hyperglycemia after eating (reduces postprandial hyperglycemia).

Gliclazide increases the sensitivity of peripheral tissues to insulin (ie, has a pronounced extrapancreatic effect). In muscle tissue, the effect of insulin on glucose uptake, due to the improvement in tissue sensitivity to insulin, is significantly increased (to + 35%), since glycazide stimulates the activity of muscle glycogen synthetase.

Reduces the formation of glucose in the liver, normalizing fasting glucose levels.

In addition to influencing carbohydrate metabolism, glycazide improves microcirculation. The drug reduces the risk of thrombosis of small vessels, affecting two mechanisms that can be involved in 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 restoration of fibrinolytic activity of the vascular endothelium and an increase in the activity of the tissue activator of plasminogen.

Gliclazide has antioxidant properties: reduces the level of lipid peroxides in plasma, increases the activity of erythrocyte superoxide precursor.

Due to the peculiarities of the dosage form, the daily intake of a single dose of tablets Gliklazid MB 30 mg provides an effective therapeutic concentration of glycazide in blood plasma for 24 hours.

Pharmacokinetics:

After oral administration glycazide completely absorbed from the gastrointestinal tract. Eating does not affect absorption. The concentration of the active substance in the blood plasma gradually gradually increases, reaches a maximum and leaves on the plateau 6-12 hours after taking the drug. Individual variability is relatively low. The relationship between the dose taken and the concentration of the drug in the blood plasma is a linear time dependence.

The connection with plasma proteins is approximately 95%.

Metabolised in the liver and excreted mainly by the kidneys. Kidney excretion is carried out mainly in the form of metabolites, less than 1% of the drug is excreted unchanged.

There are no active metabolites in the plasma.The half-life is approximately 16 hours (12 to 20 hours).

In elderly people, clinically significant changes in pharmacokinetic parameters are not observed.

Indications:

Diabetes mellitus type 2 in combination with diet therapy with insufficient effectiveness of diet and exercise.

Contraindications:

increased sensitivity to gliclazide or any of the excipients of the drug, to other derivatives of sulfonylurea, to sulfonamides;
diabetes mellitus type 1;
Diabetic ketoacidosis, diabetic precoma, diabetic coma;
severe renal and / or hepatic insufficiency;

pregnancy and the period of breastfeeding;
age to 18 years;
miconazole;
congenital lactose intolerance, lactase deficiency or glucose-galactose malabsorption.

It is not recommended to use the drug simultaneously in combination with phenylbutazone or danazol.

Carefully:

old age, irregular and / or unbalanced diet, severe cardiovascular diseases (including IHD, atherosclerosis), hypothyroidism, adrenal or pituitary insufficiency, hypopituitarism,renal and / or hepatic insufficiency, long-term glucocorticosteroid therapy (GCS), alcoholism, insufficiency of glucose-6-phosphate dehydrogenase.

Pregnancy and lactation:

Experience with glycazide during pregnancy is absent.

Data on the use of other derivatives of sulfonylurea during pregnancy are limited.

In studies on laboratory animals teratogenic effects of glycazide were not revealed.

To reduce the risk of developing congenital malformations, optimal control (appropriate therapy) of diabetes mellitus is necessary.

Oral hypoglycemic drugs during pregnancy are not applied.

The drug of choice for the treatment of diabetes in pregnant women is insulin.

It is recommended to replace the intake of oral hypoglycemic drugs with insulinotherapy in the case of a planned pregnancy, and if the pregnancy occurred against the background of taking the drug.

Lactation

Taking into account the lack of data on the intake of glycazide in breast milk and the risk of developing neonatal hypoglycemia, it is contraindicated during therapy with the drug.

Dosing and Administration:

PREPARATION IS INTENDED FOR ADULT TREATMENT!

Tablets Gliklazid MB with a modified release of 30 mg taken orally 1 time per day during breakfast.

For patients who have not previously received treatment, the initial dose is 30 mg (including those over 65 years of age). Then the dose is selected individually to achieve the desired therapeutic effect.

Selection of the dose should be carried out in accordance with the level of glucose in the blood after the start of treatment. Each subsequent dose change can be taken after at least a two-week period.

The daily dose of the drug can vary from 30 mg (1 tablet) to 90-120 mg (3-4 tablets). The daily dose should not exceed 120 mg (4 tablets).

Gliklazid MB can replace gliclazide tablets with normal release (80 mg) in doses from 1 to 4 tablets per day.

If you skip one or more doses of the drug, you can not take a higher dose to the next dose (the next day).

When replacing another hypoglycemic drug with tablets, Gliklazid MB 30 mg does not require any transitional period of time. It is necessary to first complete the intake of a daily dose of another drug and only the next day to begin taking this medication.

If the patient has previously received sulfonylureas with a longer half-life, careful monitoring (blood glucose control) for 1-2 weeks is necessary to avoid hypoglycemia as a consequence of the residual effects of previous therapy.

Tablets Gliklazid MB can be used in combination with biguanides, alpha-glucosidase inhibitors or insulin.

Patients with renal insufficiency light and moderate severity of the drug is prescribed in the same doses as patients with normal renal function. With renal insufficiency, severe Gliclazide MB tablets are contraindicated.

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, cancellation of GCS after prolonged use and / or reception in high doses, severe cardiovascular disease 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 Gliklazid MB.

Side effects:

Hypoglycemia (with dysregulation and inadequate diet): headache, fatigue, hunger, increased sweating, severe weakness, palpitations, arrhythmia, increased blood pressure, drowsiness, insomnia, agitation, aggressiveness, anxiety, irritability, impaired concentration, inability to concentrate and delayed reaction, depression, visual impairment, aphasia, tremor, paresis, sensory disorders, dizziness, feelings of helplessness, loss of self-control, delirium, with cramps, shallow breathing, bradycardia, loss of consciousness, coma.

On the part of the digestive system: nausea, vomiting, diarrhea, abdominal pain, constipation (the severity of these symptoms decreases with admission during meals); rarely - violations of the liver (hepatitis, cholestatic jaundice - requires the drug to cancel, increase the activity of "liver" transaminases, alkaline phosphatase).

From the hematopoiesis: oppression of bone marrow hematopoiesis (anemia, thrombocytopenia, leukopenia, granulocytopenia).

Allergic reactions: skin itching, urticaria, skin rash, incl. maculopapular and bullous), erythema.

Other: impaired vision.

Common side effects of sulfonylurea derivatives: erythropenia, agranulocytosis, hemolytic anemia, pancytopenia, allergic vasculitis; life-threatening liver failure.

Overdose:

Symptoms: hypoglycemia, impaired consciousness, hypoglycemic coma.

Treatment: if the patient is conscious, take sugar inside.

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.

If suspected or diagnosed hypoglycemic coma, the patient quickly intravenously administered 50 ml of a 40% solution of dextrose (glucose). Then, 5% dextrose (glucose) solution is administered intravenously dropwise to maintain the required blood glucose level.

After the restoration of consciousness it is necessary to give the patient food that is rich in easily assimilated carbohydrates (in order to avoid the re-development of hypoglycemia). 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 monitoring.

Dialysis is ineffective due to the expressed binding of glycazide to plasma proteins.

Interaction:

Gliclazide enhances the effect of anticoagulants (warfarin), an anticoagulant dose adjustment may be required.

Miconazole (with systemic administration and with the use of gel on the oral mucosa) enhances the hypoglycemic effect of the drug (hypoglycemia may develop up to the state of coma).

Phenylbutazone (systemic administration) enhances the hypoglycemic effect of the drug (displaces plasma from plasma binding and / or slows the elimination from the body), blood glucose control and correction of the dose of gliclazide are necessary, both during the administration of phenylbutazone and after its withdrawal.

Ethanol and ethanol-containing drugs increases hypoglycemia, inhibiting compensatory reactions, can promote the development of hypoglycemic coma.

With simultaneous administration with other hypoglycemic drugs (insulin, acarbose, biguanides), beta-adrenoblockers, fluconazole, angiotensin-converting enzyme inhibitors (captopril, enalapril), blockers of H2-histamine receptors (cimetidine), monoamine oxidase inhibitors, sulfonamides and non-steroidal anti-inflammatory drugs (NSAIDs) - increased hypoglycemic effect and risk of hypoglycemia.

Danazol - Diabetogenic effect. It is necessary to control the blood glucose level and correct the dose of gliclazide, both during the reception of danazol, and after its cancellation.

Chlorpromazine in high doses (more than 100 mg / day) increases the glucose level in the blood, reducing the secretion of insulin. It is necessary to monitor blood glucose and dose correction of gliclazide, both during the intake of chlorpromazine, and after its withdrawal

SCS (systemic, intraarticular, external, rectal administration) increases blood glucose levels with the possible development of ketoacidosis (reduced tolerance to carbohydrates). It is necessary to monitor blood glucose and dose correction of gliclazide, both during the admission of GCS, and after their withdrawal.

Ritodrin, salbutamol, terbutaline (intravenous) - increase blood glucose.It is recommended to monitor blood glucose and, if necessary, transfer the patient to insulin therapy.

Special instructions:

Treatment with tablets Gliklazid MB is carried out only in combination with a low-calorie diet with a low carbohydrate content. It is necessary to regularly monitor the glucose level in the blood on an empty stomach and after meals, especially in the first days of treatment with the drug.

Gliklazid MB tablets can be prescribed only to patients receiving regular meals, necessarily including breakfast and ensuring sufficient intake of carbohydrates.

When prescribing the drug, it should be borne in mind that hypoglycemia may develop, due to the administration of sulfonylurea derivatives, and in some cases, in severe and prolonged form, requiring hospitalization and administration of glucose for several days. Hypoglycemia often develops with a low-calorie diet, after prolonged or vigorous exercise, after drinking alcohol or while taking several hypoglycemic drugs at the same time.

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

With physical and emotional overstrain, when changing the diet regime, a dose adjustment of Gliklazid MB tablets is necessary.

Particularly sensitive to the effects of hypoglycemic drugs: the elderly; patients who do not receive a balanced diet, with a general weakened state; patients suffering from pituitary-adrenal insufficiency.

Beta-blockers, clonidine, reserpine, guanethidine may mask the clinical manifestations of hypoglycemia.

Patients should be warned about the increased risk of hypoglycemia in cases of taking ethanol, NSAIDs, with fasting.

In the case of taking ethanol (alcohol), it is also possible to develop a disulfiram-like syndrome (abdominal pain, nausea, vomiting, headache).

Large surgical interventions and trauma, extensive burns, infectious diseases with febrile syndrome may require the abolition of oral hypoglycemic drugs and the appointment of insulin therapy.

It is possible to develop secondary drug resistance (it is necessary to distinguish from the primary drug, in which the drug already at the first appointment does not give the expected clinical effect).

Against the background of tablets Gliclazide CF, the patient should refrain from drinking alcohol and / or containing ethanol preparations and food products.

During the treatment with Gliclazide MB tablets, the patient should regularly determine glucose and glycosylated hemoglobin levels in the blood, the glucose content in the urine.

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets with modified release of 30 mg.

Packaging:

10, 20 tablets in contiguous cell packages.

1, 2, 3, 6 contour cell packs on 10 tablets or 1, 3, 5, 6 contour cell packs of 20 tablets with instructions for use are packs 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.

The drug should not be used after the expiry date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-008619/09

Date of registration:28.10.2009 / 05.03.2013

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: & nbsp15.01.2016

Illustrated instructions

Instructions

Diabetolong (Diabetalong)