Composition, form of production and packaging
Tablets with modified release of white or almost white color, flat-cylindrical, with a facet, the presence of marble is supposed.
1 tab.
gliclazide 30 mg
Excipients: hypromellose (Metocel K-100 LV CR Premium), silicon dioxide colloid (aerosil), calcium stearate, talc, lactose monohydrate (tabletose 80).
10 pieces. - packings cellular planimetric (3) - packs cardboard.
10 pieces. - packings cellular planimetric (6) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2013.
PHARMACHOLOGIC EFFECT
Oral hypoglycemic drug, 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 onset of insulin secretion. It restores the early peak of insulin secretion in response to the intake of glucose (unlike other sulfonylurea derivatives, which 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 (that is, it has a pronounced extrapancreatic action). 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 muscle glycogen synthetase activity.
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 the 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 B 2 ), as well as recovery fibrinolytic activity of the vascular endothelium and an increase in the activity of the tissue plasminogen activator.
Gliklazid has antioxidant properties: reduces the level of lipid peroxides in plasma, increases the activity of erythrocyte superoxide dismutase.
Due to the peculiarities of the dosage form, daily intake of a single dose of Diabeticon В® 30 mg tablets provides an effective therapeutic concentration of Gliclazide in the blood plasma for 24 hours.
PHARMACOKINETICS
Suction
After ingestion, the glyclazid is completely absorbed from the digestive 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.
Distribution and Metabolism
Binding to plasma proteins is approximately 95%.
Metabolised in the liver and excreted mainly by the kidneys. There are no active metabolites in the plasma.
Excretion
Kidney excretion is carried out mainly in the form of metabolites, less than 1% of the drug is excreted unchanged.
T 1/2 is about 16 hours (12 to 20 hours).
Pharmacokinetics in special clinical cases
In elderly people, clinically significant changes in pharmacokinetic parameters are not observed.
INDICATIONS
- Type 2 diabetes in combination with diet therapy with insufficient diet and exercise.
DOSING MODE
The drug is intended only for the treatment of adults .
Diabetanolong В® tablets with a modified release of 30 mg are taken orally 1 time / day during breakfast.
For patients who have not previously received treatment, (including those over 65 years of age ), the initial dose is 30 mg. 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 tab.) To 90-120 mg (3-4 tablets). The daily dose should not exceed 120 mg (4 tablets).
Diabeticon В® can replace gliclazide tablets with normal release (80 mg) in doses from 1 to 4 tablets / 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 Diabeticon В® 30 mg tablets, no transitional period of time is required. It is necessary to first complete the reception of a daily dose of another drug and only the next day to start taking this drug.
If the patient has previously received therapy with 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.
Diabeticon В® can be used in combination with biguanides, alpha-glucosidase inhibitors or insulin.
Patients with renal insufficiency of mild to moderate severity are prescribed in the same doses as patients with normal renal function. In case of severe renal insufficiency, Diabeticon В® is contraindicated.
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 minimal dose (30 mg 1 time / day) of Diabetolong В® .
SIDE EFFECT
Hypoglycemia (with dysregulation and inadequate diet): headache, fatigue, hunger, increased sweating, severe weakness, palpitation, arrhythmia, increased blood pressure, drowsiness, insomnia, agitation, aggressiveness, anxiety, irritability, impaired concentration, inability concentrate and delayed reaction, depression, visual impairment, aphasia, tremor, paresis, sensory disorders, dizziness, feelings of helplessness, loss of self-control, delirium, convulsions, superficial e respiration, bradycardia, unconsciousness, 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, increased activity of hepatic transaminases, alkaline phosphatase, cholestatic jaundice - requires withdrawal of the drug).
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 sulfonylureas: erythropenia, agranulocytosis, hemolytic anemia, pancytopenia, allergic vasculitis, life-threatening liver failure.
CONTRAINDICATIONS
- Type 1 diabetes mellitus;
- diabetic ketoacidosis, diabetic precoma, diabetic coma;
- severe renal and / or liver failure;
- age up to 18 years;
- taking miconazole;
- Pregnancy;
- the period of breastfeeding (lactation);
- Congenital lactose intolerance, lactase deficiency or glucose-galactose malabsorption;
- Hypersensitivity to gliclazide or any of the excipients of the drug, to other derivatives of sulfonylurea, to sulfonamides.
It is not recommended to use the drug simultaneously in combination with phenylbutazone or danazol.
Precautions: elderly age, irregular and / or unbalanced diet, severe cardiovascular diseases (including CHD, atherosclerosis), hypothyroidism, adrenal or hypophysial insufficiency, hypopituitarism, renal and / or hepatic insufficiency, long-term GCS therapy, 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 insulin therapy, both in the case of a planned pregnancy, and if the pregnancy has occurred while taking the drug.
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.
APPLICATION FOR FUNCTIONS OF THE LIVER
Patients with renal insufficiency of mild to moderate severity are prescribed in the same doses as patients with normal renal function. In case of severe renal insufficiency, Diabeticon В® is contraindicated.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution in liver failure.
Contraindicated:
- severe renal and / or hepatic insufficiency.
APPLICATION FOR CHILDREN
Contraindicated in children under 18 years.
APPLICATION IN ELDERLY PATIENTS
For patients who have not previously received treatment, (including those over 65 years of age ), the initial dose is 30 mg. Then the dose is selected individually to achieve the desired therapeutic effect.
SPECIAL INSTRUCTIONS
Treatment 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.
Diabeticon В® 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 Diabetolong В® is necessary.
Particularly sensitive to the effects of hypoglycemic drugs are the elderly, patients who do not receive a balanced diet, with a general weakened state, patients with pituitary-adrenal insufficiency.
Beta-adrenoblockers, clonidine, reserpine, guanethidine may mask 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 therapy with Diabetolong В®, the patient should stop using alcohol and / or ethanol-containing drugs and food products.
During treatment with Diabeticon В® , the patient should regularly determine the levels of glucose and glycosylated hemoglobin in the blood, the content of glucose in the urine.
Impact on the ability to drive vehicles and manage mechanisms
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.
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, convulsions or other neurological disorders. If such symptoms appear, emergency medical care and immediate hospitalization are necessary.
If suspected or diagnosed with hypoglycemic coma, the patient is rapidly injected with 50 ml of a 40% solution of dextrose (glucose) rapidly. Then 5% dextrose solution (glucose) is injected intravenously into / in order to maintain the required level of glucose in the blood.
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.
DRUG INTERACTION
Gliklazid increases the effect of anticoagulants (warfarin), it may be necessary to correct the dose of anticoagulant.
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), requires blood glucose control and correction of the dose of gliclazide, both during the administration of phenylbutazone and after its withdrawal.
Ethanol and ethanol-containing drugs increase hypoglycemia, inhibiting compensatory reactions, can promote the development of hypoglycemic coma.
With simultaneous administration with other hypoglycemic drugs (insulin, acarbose, biguanides), beta-adrenoblockers, fluconazole, ACE inhibitors (captopril, enalapril), histamine H2-receptor blockers (cimetidine), MAO inhibitors, sulfonamides and NSAIDs, hypoglycemic effect and the risk of hypoglycemia.
With simultaneous administration with danazol, a diabetic effect is noted. It is necessary to monitor the blood glucose level and dose correction of gliclazide, both during the intake 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 administration of GCS, and after their withdrawal.
Ritodrin, salbutamol, terbutaline (iv administration) increase the blood glucose level. It is recommended to monitor blood glucose and, if necessary, transfer the patient to insulin therapy.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored in a dry, protected from light, out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 3 years.
