Glurenorm, tablets 30 mg 60 pcs

Glurenorm is a hypoglycemic drug for oral use, a sulfonylurea derivative of the II generation.

It has pancreatic and extrapancreatic effects.

Stimulates insulin secretion by potentiating the glucose-mediated pathway of insulin formation.

In animal experiments, Glurenorm has been shown to reduce insulin resistance in the liver and adipose tissue by increasing insulin receptors and stimulating the insulin-mediated post-receptor mechanism.

Hypoglycemic effect develops 60-90 minutes after oral administration, maximum action occurs after 2-3 h and lasts about 8-10 h.

Pharmacokinetics

Intake

. After a single oral dose of glyquidone (15 mg or 30 mg), the drug is rapidly and almost completely (80-95%) absorbed from the GI tract, reaching plasma concentrations of 0.65 µg/ml (range 0.12-2.14 µg/ml). 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 between diabetic patients and healthy subjects.

Distribution

Glyquidone has high affinity to plasma proteins (>99%). There are no data on the possible passage of glyquidone or its metabolites through the GEB or the placenta. There are no data on the possibility of glyquidone penetration into breast milk.

Metabolism

Glyquidone is completely metabolized by the liver, mainly by hydroxylation and demethylation. Glyquidone metabolites have no or little pharmacological activity compared to the parent substance.

The bulk of the metabolites are excreted through the intestine. Only a small portion of the metabolites is excreted by the kidneys. In studies it has been shown that after oral administration about 86% of the isotope-labeled drug (14C) is excreted through the intestine. Regardless of the dose and route of administration, the kidneys excrete about 5% (as metabolites) of the administered amount. The level of excretion of Glurenorm by the kidneys remains minimal even with regular administration.

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

Pharmacokinetics in special clinical cases

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

The bulk of the drug is excreted through the intestine. There is evidence that the metabolism of the drug is not altered in patients with hepatic impairment. Excretion of glyquidone by the kidneys is insignificant, in patients with impaired renal function the drug does not accumulate.

Indications

Type 2 diabetes

Type II diabetes mellitus in adults.

Active ingredient

Gliquidone

Composition

Active substance:

Glyquidone 30 mg.

Auxiliary substances:

Lactose monohydrate – 134.6 mg,

dried corn starch – 70 mg,

soluble corn starch – 5 mg,

magnesium stearate – 0.4 mg.

How to take, the dosage

The drug is administered orally. It is necessary to follow the doctor’s recommendations regarding the dose of the drug and compliance with the diet. The drug should not be discontinued without consulting a doctor.

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

If taking 1/2 tablet (15 mg) does not result in adequate improvement, the dose should be gradually increased after consulting a physician. If the daily dose of Glurenorm does not exceed 2 tablets (60 mg), it may be prescribed at 1 meal, with breakfast.

If a higher dose is prescribed, the best effect may be achieved when the daily dose is divided into 2-3 doses. In this case, the highest dose should be taken at breakfast. Increasing the dose over 4 tablets (120 mg)/day usually does not further increase efficacy.

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

Patients with impaired renal function

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

Patients with hepatic impairment

The dose higher than 75 mg in patients with hepatic impairment requires close monitoring of the patient. The drug should not be administered to patients with severe hepatic impairment because 95% of the dose is metabolized in the liver and excreted through the intestine.

Combination therapy

In case of insufficient clinical effect of Glurenorm® monotherapy only additional administration of metformin may be recommended.

Interaction

Hypoglycemic effect may be enhanced with concomitant administration of glyquidone 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-adrenoblockers, sympatholytics (including clonidine), reserpine and guanethidine may increase the hypoglycemic effect and simultaneously mask the symptoms of hypoglycemia.

The hypoglycemic effect may be decreased when glyquidone and aminoglutethimide, sympathomimetics, GCS, thyroid hormones, glucagon, thiazide and “loop” diuretics, oral contraceptives, diazoxide, phenothiazine and drugs containing nicotinic acid are prescribed simultaneously.

Barbiturates, rifampicin and phenytoin may also decrease the hypoglycemic effect of glyquidone.

Augmentation or attenuation of the hypoglycemic effect of glyquidone has been described when taking histamine H2-receptor blockers (cimetidine, ranitidine) and ethanol.

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Special Instructions

Glurenorm should not replace a therapeutic diet to control a patient’s body weight and reduce the risk of cardiovascular events.

Contraindications

• High sensitivity to estriol, Lactobacilli or other Gynoflora E substances;
• Estrogen-dependent tumors in the breasts, uterus or vagina;
• endometriosis;
• vaginal bleeding of unknown origin;
• not recommended before first menstruation.

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Side effects

Blood system disorders: thrombocytopenia, leukopenia, agranulocytosis.

Metabolism disorders: hypoglycemia.

Nervous system disorders: headache, dizziness, somnolence, paresthesia, feeling of fatigue.

Visually: accommodation disorders.

Cardiovascular system: angina, extrasystole, cardiovascular failure, hypotension.

Digestive system disorders: decreased appetite, nausea, vomiting, constipation, diarrhea, abdominal discomfort, dry mouth, cholestasis.

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

Others: pain in the chest.

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Overdose

Overdose with sulfonylurea derivatives may lead to hypoglycemia.

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

Treatment: in case of symptoms of hypoglycemia, glucose (dextrose) or products rich in carbohydrates should be taken orally. In severe hypoglycemia (loss of consciousness, coma) dextrose is administered intravenously. After recovery of consciousness, intake of easily digestible carbohydrates (to avoid the recurrence of hypoglycemia).