Glumedex (Tablets) Instructions for Use

Marketing Authorization Holder

Shin Poong Pharmaceutical, Co. Ltd. (Republic Of Korea)

ATC Code

A10BB12 (Glimepiride)

Active Substance

Glimepiride (Rec.INN registered by WHO)

Dosage Form

Glumedex

Tablets 2 mg: 30 pcs.

Dosage Form, Packaging, and Composition

10 pcs. – blisters (3) – cardboard packs.

Clinical-Pharmacological Group

Oral hypoglycemic drug

Pharmacotherapeutic Group

Hypoglycemic agent for oral administration of the third-generation sulfonylurea group

Pharmacological Action

An oral hypoglycemic agent, a sulfonylurea derivative. It stimulates insulin secretion by pancreatic beta-cells and increases insulin release. It increases the sensitivity of peripheral tissues to insulin.

Pharmacokinetics

After repeated oral administration at a dose of 4 mg/day, the C_max in blood serum is reached in approximately 2.5 hours and is 309 ng/ml; there is a linear relationship between the dose and C_max, as well as between the dose and AUC. Food intake does not have a significant effect on absorption.

The V_d is about 8.8 L. Plasma protein binding is more than 99%.

Clearance is about 48 ml/min.

It undergoes metabolism. Hydroxylated and carboxylated metabolites of glimepiride are formed, apparently as a result of metabolism in the liver, and are found in urine and feces.

The T_1/2 is 5-8 hours. After administration of glimepiride in high doses, the T_1/2 increases. After a single oral dose of radioactively labeled glimepiride, 58% of the radioactivity was found in urine and 35% in feces. No unchanged active substance was found in urine.

The T_1/2 of the hydroxylated and carboxylated metabolites of glimepiride were about 3-6 hours and 5-6 hours, respectively.

In patients with impaired renal function (with low creatinine clearance), a tendency towards an increase in the clearance of glimepiride and a decrease in its mean serum concentrations was observed. Thus, there is no additional risk of glimepiride accumulation in this category of patients.

Indications

Type 2 diabetes mellitus (non-insulin-dependent) in case of ineffectiveness of diet therapy and physical exercise.

ICD codes

Dosage Regimen

Determine the initial and maintenance dose individually based on regular monitoring of blood glucose and glycated hemoglobin levels.

Start therapy with 1 mg once daily. Administer the dose with the first main meal or immediately before it.

Increase the dose gradually. Titrate the daily dose upwards by 1 mg increments at 1-2 week intervals based on the patient’s glycemic response.

The usual maintenance dose is 1 mg to 4 mg once daily. After a dose of 2 mg, consider a twice-daily regimen.

Do not exceed the maximum recommended daily dose of 8 mg.

Monitor patients closely, especially during the first weeks of therapy, for signs of hypoglycemia.

Adjust the dosage when changing from other oral hypoglycemic agents, considering the potency and duration of action of the previous drug.

Reduce the dose or discontinue therapy if hypoglycemia occurs or if glycemic control is achieved through diet, exercise, or weight loss.

Re-evaluate the dosage regimen during stress, such as trauma, surgery, or infection, as temporary insulin therapy may be required.

Use caution during dose titration in elderly patients, debilitated patients, and those with adrenal or pituitary insufficiency due to an increased risk of hypoglycemia.

Adverse Reactions

Metabolism disorders: hypoglycemia, hyponatremia.

Digestive system: nausea, vomiting, epigastric discomfort, abdominal pain, diarrhea, increased activity of liver transaminases, cholestasis, jaundice, hepatitis (up to the development of liver failure).

Hematopoietic system: thrombocytopenia, leukopenia, erythropenia, granulocytopenia, agranulocytosis, pancytopenia, hemolytic anemia.

Organ of vision: transient visual disturbances.

Allergic reactions: itching, urticaria, skin rash; rarely – dyspnea, drop in blood pressure, anaphylactic shock, allergic vasculitis, photosensitivity.

Contraindications

Type 1 diabetes mellitus (insulin-dependent), ketoacidosis, precoma, coma, hepatic failure, renal failure (including patients on hemodialysis), pregnancy, breastfeeding period, children and adolescents under 18 years of age, hypersensitivity to glimepiride, other sulfonylurea derivatives and sulfonamides.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy. In case of planned pregnancy or if pregnancy occurs, the woman should be switched to insulin.

During lactation, the woman should be switched to insulin.

In experimental studies, it was found that Glimepiride is excreted in breast milk.

Use in Hepatic Impairment

Contraindicated in hepatic failure.

Use in Renal Impairment

Contraindicated in renal failure (including patients on hemodialysis).

Pediatric Use

Contraindicated for use in children and adolescents under 18 years of age.

Geriatric Use

Use with caution in elderly patients.

Special Precautions

Use with caution in patients with concomitant endocrine diseases affecting carbohydrate metabolism (including thyroid dysfunction, adenohypophyseal or adrenocortical insufficiency).

In stressful situations (trauma, surgery, infectious diseases accompanied by fever), it may be necessary to temporarily transfer the patient to insulin.

It should be taken into account that symptoms of hypoglycemia may be smoothed out or completely absent in elderly patients, patients with neurocirculatory dystonia, or those receiving concurrent treatment with beta-blockers, clonidine, reserpine, guanethidine, or other sympatholytics.

When compensation for diabetes mellitus is achieved, sensitivity to insulin increases; in this regard, the need for glimepiride may decrease during treatment. To avoid the development of hypoglycemia, it is necessary to reduce the dose or discontinue Glimepiride in a timely manner. Dose adjustment should also be carried out when the patient’s body weight changes or when their lifestyle changes, or when other factors contributing to the development of hypo- or hyperglycemia appear.

When switching to Glimepiride from another drug, it is necessary to take into account the degree and duration of the effect of the previous hypoglycemic agent. It may be necessary to temporarily discontinue treatment to avoid an additive effect.

In the first weeks of treatment, the risk of developing hypoglycemia may increase, which requires particularly strict monitoring of the patient. Factors contributing to the development of hypoglycemia include: irregular, inadequate nutrition; changes in the usual diet; alcohol consumption, especially in combination with skipping a meal; changes in the usual regimen of physical activity; simultaneous use of other medications. Hypoglycemia can be quickly relieved by immediate intake of carbohydrates.

During treatment, regular monitoring of blood and urine glucose levels, as well as the concentration of glycated hemoglobin, is necessary.

Effect on ability to drive vehicles and machinery

During treatment, one should refrain from engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Drug Interactions

Enhancement of the hypoglycemic effect of glimepiride is possible with simultaneous use with insulin or other hypoglycemic drugs, ACE inhibitors, allopurinol, anabolic steroids and androgens, chloramphenicol, coumarin derivatives, cyclophosphamide, disopyramide, fenfluramine, phenyramidol, fibrates, fluoxetine, guanethidine, ifosfamide, MAO inhibitors, miconazole, PAS, pentoxifylline (with injectable administration in high doses), phenylbutazone, azapropazone, oxyphenbutazone, probenecid, quinolones, salicylates, sulfinpyrazone, sulfonamides, tetracyclines.

Weakening of the hypoglycemic effect of glimepiride is possible with simultaneous use with acetazolamide, barbiturates, corticosteroids, diazoxide, diuretics, epinephrine (adrenaline) and other sympathomimetics, glucagon, laxatives (after long-term use), nicotinic acid (in high doses), estrogens and progestogens, phenothiazine, phenytoin, rifampicin, thyroid hormones.

With simultaneous use, histamine H₂-receptor blockers, clonidine, and reserpine can both potentiate and reduce the hypoglycemic effect of glimepiride.

Against the background of glimepiride use, the effect of coumarin derivatives may be enhanced or weakened.

Ethanol may enhance or weaken the hypoglycemic effect of glimepiride.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.