Diabetalong, 30 mg 60 pcs

The oral hypoglycemic drug, sulfonylurea derivative of the II generation.

Stimulates insulin secretion by the pancreas, lowers blood glucose levels, increases the insulin-secretory action 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 (increased postprandial insulin levels and C-peptide secretion are maintained).

It shortens the time from the moment of food intake to the beginning of insulin secretion. Restores the early peak of insulin secretion in response to glucose intake (unlike other sulfonylurea derivatives, which act primarily during the second stage of secretion). Also increases the second phase of insulin secretion. Reduces the peak of hyperglycemia after a meal (reduces postprandial hyperglycemia).

Glicliquid increases the sensitivity of peripheral tissues to insulin (i.e. it has a pronounced extrapancreatic effect). In muscle tissue, the effect of insulin on glucose uptake due to improved tissue insulin sensitivity is significantly increased (up to +35%) because gliclazide stimulates muscle glycogen synthetase activity.

Limits glucose formation in the liver, normalizing fasting glucose levels.

In addition to affecting carbohydrate metabolism, gliclazide improves microcirculation. Preparation decreases risk of small vessel thrombosis by influence on two mechanisms which may be involved in complications of diabetes mellitus: partial inhibition of platelet aggregation and adhesion and decrease of concentration of platelet-activating factors (beta-thromboglobulin, thromboxane B2) and restoration of fibrinolytic activity of vascular endothelium and increase of tissue plasminogen activator activity.

Glyclazide has antioxidant properties: decreases plasma levels of lipid peroxides and increases erythrocyte superoxide dismutase activity.

Drug formulation gives effective therapeutic plasma concentrations of gliclazide for 24 hours with a single daily dose of Diabetalong® 30 mg tablets.

Pharmacokinetics

Intake

After oral administration, gliclazide is completely absorbed from the GI tract. Food intake has no effect on absorption. The plasma concentration of the active ingredient increases gradually, reaches a maximum and reaches a plateau 6-12 hours after drug administration. Individual variability is relatively low. The relationship between the dose taken and the plasma concentration of the drug is a linear relationship with time.

Distribution and metabolism

The binding to plasma proteins is approximately 95%.

Metabolized in the liver and excreted primarily by the kidneys. There are no active metabolites in plasma.

Elevation by the kidneys occurs mainly as metabolites; less than 1% of the drug is excreted unchanged.

The T1/2 is approximately 16 h (12 to 20 h).

Pharmacokinetics in special clinical cases

There are no clinically significant changes in pharmacokinetic parameters in elderly persons.

Indications

Type 2 diabetes mellitus in combination with diet therapy when diet and exercise are not effective.

Active ingredient

Composition

1 tablet gligliclazide30 mg

Auxiliary substances:

hypromellose (Metocel K-100 LV CR Premium),

colloidal silicon dioxide (aerosil),

How to take, the dosage

The drug is for the treatment of adults only.

Diabetalong® Tablets with modified-release 30 mg are taken orally once daily with breakfast.

For untreated patients (including those over 65 years of age), the starting dose is 30 mg. Then the dose is adjusted individually until the desired therapeutic effect is achieved.

The dose should be adjusted according to the blood glucose level after the start of treatment. Each subsequent dose change can be undertaken after at least a two-week period.

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

Diabetalong® may substitute for gliclazide tablets with normal release (80 mg) in doses of 1 to 4 tablets/day.

If one or more doses are missed, the higher dose should not be taken at the next dose (next day).

There is no transition time required when replacing another hypoglycemic drug with Diabetalong® 30 mg tablets. You must first complete the daily dose of the other medication and only start this medication the next day.

If a patient has previously received therapy with sulfonylureas with a longer half-life, close monitoring (blood glucose monitoring) is required for 1-2 weeks to avoid hypoglycemia as a residual effect of prior therapy.

Diabetalong® may be used in combination with biguanides, alpha-glucosidase inhibitors or insulin.

Patients with mild to moderate renal impairment are prescribed the drug in the same doses as patients with normal renal function. Diabetalong® is contraindicated in severe renal failure.

In patients belonging to risk group of hypoglycemia development (insufficient or unbalanced nutrition; severe or poorly compensated endocrine disorders – pituitary and adrenal insufficiency, hypothyroidism; discontinuation of GCS after long-term and/or high-dose use; severe cardiovascular disease /severe CHD, severe carotid atherosclerosis, widespread atherosclerosis/) a minimum dose (30 mg once daily) of Diabetalong® is recommended.

Interaction

Gliclazide increases the effect of anticoagulants (warfarin), correction of the anticoagulant dose may be required.

Miconazole (when administered systemically and when using gel on the oral mucosa) increases the hypoglycemic effect of the drug (possible development of hypoglycemia up to the state of coma).

Phenylbutazone (systemic administration) increases the hypoglycemic effect of the drug (displaces it from binding to plasma proteins and/or slows excretion from the body), blood glucose control and correction of the dose of gliclazide is necessary, both during phenylbutazone administration and after its withdrawal.

Ethanol and ethanol-containing drugs exacerbate hypoglycemia, inhibiting compensatory responses, may contribute to the development of hypoglycemic coma.

. When concomitant use with other hypoglycemic drugs (insulin, acarbose, biguanides), beta-adrenoblockers, fluconazole, ACE inhibitors (captopril, enalapril), histamine H2-receptor blockers (cimetidine), MAO inhibitors, sulfonamides and NSAIDs an increase of hypoglycemic effect and risk of hypoglycemia is noted.

Diabetogenic effect is noted when concomitantly taken with danazol. Blood glucose levels should be monitored and the dose of gliclazide corrected, both during danazol administration and after withdrawal.

Chlorpromazine in high doses (over 100 mg/day) increases blood glucose levels, reducing insulin secretion. Blood glucose control and gliclazide dose adjustment are necessary, both during chlorpromazine administration and after its withdrawal.

The GCS (systemic, intraarticular, external, rectal use) increase blood glucose with possible development of ketoacidosis (reduced carbohydrate tolerance). Blood glucose control and gliclazide dose adjustment are necessary both during GCS use and after their withdrawal.

Ritodrine, salbutamol, terbutaline (IV administration) increase blood glucose. It is recommended to control blood glucose and, if necessary, transfer the patient to insulin therapy.

Special Instructions

Treatment is carried out only in combination with a low-calorie, low-carbohydrate diet.

Blood glucose levels should be monitored regularly on an empty stomach and after meals, especially in the first days of treatment with the drug.

Diabetalong® can only be prescribed to patients on a regular diet that includes breakfast and provides adequate carbohydrate intake.

When prescribing the drug, it should be noted that hypoglycemia may occur with sulfonylurea derivatives, and in some cases it may be severe and prolonged, requiring hospitalization and glucose administration for several days. Hypoglycemia occurs more often with a low-calorie diet, after prolonged or vigorous exercise, after drinking alcohol or while taking several hypoglycemic drugs simultaneously.

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

The dose of Diabetalong® must be adjusted in case of physical and emotional strain, and in case of dietary changes.

Particularly sensitive to the action of hypoglycemic drugs are elderly people, patients who do not receive a balanced diet, patients with general debility, patients with pituitary-adrenal insufficiency.

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

Patients should be cautioned about the increased risk of hypoglycemia when taking ethanol, NSAIDs, or when fasting.

In case of ethanol (alcohol) intake, disulfiram-like syndrome (abdominal pain, nausea, vomiting, headache) may also occur.

Major surgical interventions and trauma, extensive burns, infectious diseases with febrile syndrome may require withdrawal of oral hypoglycemic drugs and prescription of insulin therapy.

Secondary drug resistance may develop (this must be distinguished from primary resistance, where the drug does not have the expected clinical effect the first time it is prescribed).

During therapy with Diabetalong® the patient should refrain from drinking alcohol and/or drugs containing ethanol and food products.

During treatment with Diabetalong® the patient’s blood glucose and glycosylated hemoglobin levels, glucose content in urine should be determined regularly.

Impact on driving and operating machinery

When taking this medication, caution must be exercised while driving motor vehicle and engaging in other potentially hazardous activities requiring increased concentration and quick psychomotor reactions.

Contraindications

The drug is not recommended when used in combination with phenylbutazone or danazol.

With caution: advanced age, irregular and/or unbalanced diet, severe cardiovascular disease (including IHD, atherosclerosis), hypothyroidism, adrenal or pituitary insufficiency, hypopituitarism, renal and/or hepatic insufficiency, long-term GCS therapy, alcoholism, glucose-6-phosphate dehydrogenase insufficiency.

Side effects

Gastrointestinal organs: very rare – dyspeptic complaints (nausea, vomiting, abdominal pain), very rare – jaundice.

Cardiovascular system and blood: reversible cytopenia, eosinophilia, anemia.

Skin disorders: rare – skin allergic reactions, photosensitization.

Metabolism disorders: hypoglycemia.

Nervous system and sensory system disorders: weakness, headache, dizziness, change in sense of taste.

Overdose

Symptoms: hypoglycemia, impaired consciousness, hypoglycemic coma.

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

The development of severe hypoglycemic states accompanied by coma, seizures or other neurological disorders is possible. If these symptoms occur, emergency medical assistance and immediate hospitalization is necessary.

If hypoglycemic coma is suspected or diagnosed, the patient is quickly injected 50 ml of 40% dextrose (glucose) solution by IV. Then a 5% dextrose (glucose) solution is given by IV drip to maintain the desired blood glucose level.

After recovery of consciousness, the patient should be given food rich in easily digestible carbohydrates (to avoid recurrence of hypoglycemia). Close monitoring of blood glucose levels and observation of the patient should be done for at least 48 subsequent hours. After this period of time, depending on the patient’s condition, the attending physician will decide whether further monitoring is necessary.

Dialysis is ineffective due to significant binding of gliclazide to plasma proteins.

Similarities