Glurenorm, pills 30mg, 60pcs

Composition

Active ingredient:

gliquidone 30 mg.

Auxiliary substances:

lactose monohydrate – 134.6 mg,

dried corn starch-70 mg,

soluble corn starch-5 mg,

magnesium stearate-0.4 mg

Pharmacological action

Glurenorm is a hypoglycemic drug for oral use, a second-generation sulfonylurea derivative.

It has pancreatic and extra-pancreatic effects.

It stimulates insulin secretion by potentiating the glucose-mediated pathway of insulin production.

Animal studies have shown that Glurenorm reduces insulin resistance in the liver and adipose tissue by increasing insulin receptors, as well as stimulating the post-receptor mechanism mediated by insulin.

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

Pharmacokinetics

 Suction

After ingestion of a single dose of gliquidone (15 mg or 30 mg), the drug is rapidly and almost completely (80-95%) absorbed from the gastrointestinal tract, reaching a plasma concentration of 0.65 mcg/ml (range 0.12-2.14 mcg/ml). The average time to reach Cmax of the drug in plasma is 2 h 15 min (range: 1.25-4.75 h). The AUC0 – ∞ value is 5.1 µg×h / 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

Gliquidone has a high affinity for plasma proteins (>99%). There are no data on the possible passage of gliquidone or its metabolites through the BBB or placenta. There are no data on the possibility of penetration of gliquidone into breast milk.

Metabolism

Gliquidone is completely metabolized by the liver, mainly by hydroxylation and demethylation. Gliquidone metabolites do not have or have weakly expressed pharmacological activity in comparison with the starting substance.

Deduction

Most of the metabolites are excreted through the intestines. Only a small fraction of the metabolites are excreted by the kidneys. Studies have shown that after oral use, about 86% of the isotope-labeled drug (14C) is excreted through the intestine. Regardless of the dose and method of use, about 5% (in the form of metabolites)is excreted by the kidneys depending on the amount of the drug administered. The level of excretion of Glyrenorm by the kidneys remains minimal even with regular use.

T1 / 2 is 1.2 h (in the range of 0.4-3.0 h), the final T1 / 2 is approximately 8 h (in the range of 5.7-9.4 h).

Pharmacokinetics in special clinical cases

In elderly and middle-aged patients, the pharmacokinetic parameters are similar.

The main part of the drug is excreted through the intestines. There is evidence that the metabolism of the drug does not change in patients with hepatic insufficiency. Elimination of gliquidone by the kidneys is insignificant, in patients with impaired renal function, the drug does not accumulate.

Indications

Type II diabetes mellitus in adults.

Contraindications

• diabetes mellitus type 1;
• diabetic acidosis, ketoacidosis, coma and precoma;
• condition after resection of the pancreas;
• acute intermittent porphyria;
• severe hepatic impairment;
• some acute conditions (e. g., infectious diseases or large surgery);
• a rare genetic diseases such as galactosemia, lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
• pregnancy;
• lactation (breastfeeding);
• the age of 18 (due to the lack of data on efficacy and safety of the drug in this age group);
• hypersensitivity to sulfonamides.

With caution

• , febrile syndrome;
• thyroid diseases (with impaired function);
• glucose-6-phosphate dehydrogenase deficiency;
• alcoholism.

Side effects

From the hematopoietic system: thrombocytopenia, leukopenia, agranulocytosis.

From the side of metabolism: hypoglycemia.

Nervous system disorders: headache, dizziness, drowsiness, paresthesia, fatigue.

From the side of the visual organ: accommodation disorders.

From the cardiovascular system: angina pectoris, extrasystole, cardiovascular insufficiency, hypotension.

From the digestive system: decreased appetite, nausea, vomiting, constipation, diarrhea, abdominal discomfort, dry mouth, cholestasis.

Skin and subcutaneous tissue disorders: rash, pruritus, urticaria, Stevens-Johnson syndrome, photosensitization reaction.

Other: chest pain.

Interaction

It is possible to increase the hypoglycemic effect with simultaneous use of gliquidone and ACE inhibitors, allopurinol, analgesics and NSAIDs, antifungal drugs, chloramphenicol, clarithromycin, clofibrate, coumarin derivatives, fluoroquinolones, heparin, MAO inhibitors, sulfinpyrazone, sulfonamides, tetracyclines and tricyclic antidepressants, cyclophosphamide and its derivatives insulin and oral hypoglycemic agents.

Beta-blockers, sympatholytics (including clonidine), reserpine, and guanethidine may enhance the hypoglycemic effect while masking the symptoms of hypoglycemia.

It is possible to reduce the hypoglycemic effect with simultaneous use of gliquidone and aminoglutetimide, sympathomimetics, corticosteroids, thyroid hormones, glucagon, thiazide and loop diuretics, oral contraceptives, diazoxide, phenothiazine and drugs containing nicotinic acid.

Barbiturates, rifampicin, and phenytoin may also reduce the hypoglycemic effect of gliquidone.

An increase or decrease in the hypoglycemic effect of gliquidone has been reported with histamine H2-receptor blockers (cimetidine, ranitidine) and ethanol.

How to take, course of use and dosage

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

The initial dose of Glyrenorm is usually 1/2 tab. (15 mg) during breakfast. The drug should be taken at the beginning of a meal. After taking Glyrenorm, meals should not be skipped.

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

If a higher dose is prescribed, the best 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 lead to a further increase in effectiveness.

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

Patients with impaired renal function

About 5% of the drug’s metabolites are excreted by the kidneys. No dose adjustment is required in patients with impaired renal function.

Patients with impaired liver function

Taking a dose of more than 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 impairment, since 95% of the dose is metabolized in the liver and excreted through the intestine.

Combination therapy

In case of insufficient clinical effect of monotherapy with Glyrenorm®, only additional use of metformin may be recommended.

Overdose

Overdose of sulfonylureas can lead to hypoglycemia.

Symptoms: tachycardia, increased sweating, hunger, palpitations, tremors, headache, insomnia, irritability, impaired speech and vision, motor restlessness, and loss of consciousness.

Treatment: in case of symptoms of hypoglycemia, glucose (dextrose) or carbohydrate-rich foods should be ingested. In severe hypoglycemia (loss of consciousness, coma), dextrose is administered intravenously. After regaining consciousness-intake of easily digestible carbohydrates (to avoid the re-development of hypoglycemia).

Special instructions

Glyrenorm should not replace a therapeutic diet that allows you to control the patient’s body weight and reduce the risk of developing cardiovascular disorders.

Form of production

Tablets

Storage conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C.

Shelf

life is 5 years.

Active ingredient

Gliquidone

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as prescribed by a doctor, For the elderly

Indications

Type 2 Diabetes