EUGLUCON ® - Glibenclamide

EUGLUCON ® is a drug based on Glibenclamide

THERAPEUTIC GROUP: Oral hypoglycemic agents - Sulfonylureas

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

Indications EUGLUCON ® - Glibenclamide

EUGLUCON ® is a drug indicated for the treatment of type II diabetes mellitus in the absence of satisfactory results obtained by non-pharmacological therapies.

EUGLUCON ® can be used both as monotherapy and in combination with insulin or other oral hypoglycemic agents.

Mechanism of action EUGLUCON ® - Glibenclamide

Glibenclamide, the active ingredient of EUGLUCON ® is an oral hypoglycemic agent belonging to the pharmaceutical category of sulfonylureas and one of the oral hypoglycemic drugs.

Its therapeutic action is associated with two main mechanisms able to guarantee better control of both post-prandial and basal glycaemia.

The first mechanism is performed at the pancreatic level, where this active ingredient can act on the beta cell, inhibiting the potassium channels of the SUR family, thus facilitating the depolarization of the cell membrane and the consequent release of insulin, while the second, decidedly more complex and coordinated, it seems to correlate with the ability of glibenclamide to increase the sensitivity of insulin receptors to insulin, enhancing the metabolic effects of this hormone at the peripheral level.

The hypoglycemic action is carried out for about 24 hours after taking it, thus allowing a simple 24-hour glycemic control with the simple administration of one tablet a day.

The drug, metabolized at the hepatic level, is subsequently excreted in the form of inactive metabolites in almost equal quantities between faeces and urine.

Studies carried out and clinical efficacy

1. EFFECTIVENESS OF GLIBENCLAMIDE

Glibenclamide has proved particularly effective not only in ensuring better insulin secretion, useful for the control of blood glucose, but also in reducing hepatic secretion of glucose. This statistically significant study conducted on patients with type II diabetes supports the hypothesis of an extrapancreatic mechanism of action of glibenclamide.

2. GLIBENCLAMIDE AND RENAL PATHOLOGY

One of the most important consequences of diabetic disease is the onset of kidney disease and kidney failure. In this study we evaluate the contribution that drug therapy offers to the establishment of this condition. Specifically, glibenclamide, like rosiglitazone, has been shown to be safer for renal pathology, compared with, for example, metformin, which has recorded a greater number of cases of renal failure in 5 years.

3. THE DANGER OF HYPOGLYCAEMIA

One of the most important risks associated with glibenclamide therapy is hypoglycemia, due to its important systemic effects. In this case report, we report the death of a patient due to hypoglycemia following the ingestion of excessive doses of glibenclamide. The intent of this work is to reaffirm the importance of the correct dosage formulation and periodic control of glycemic levels, in order to avoid unpleasant consequences.

Method of use and dosage

EUGLUCON ® Glibenclamide 5 mg tablets: after monitoring blood glucose levels and adjusting the diet, the first administration of EUGLUCON ® should not exceed ½ tablet daily.

In the event that the initial portion of the drug is not capable of producing the expected therapeutic results, the doctor could increase the dosage up to a maximum of 2-3 tablets daily.

Given the long efficacy of action of glibenclamide, EUGLUCON ® should be taken once a day at the main meal.

Warnings EUGLUCON ® - Glibenclamide

The correct therapeutic approach to diabetic pathology should primarily include the adoption of non-pharmacological measures such as diet and lifestyle, accompanied in the event of poor therapeutic results by drug therapy.

Before starting the treatment and during the therapy it is of fundamental importance, to periodically monitor the glycemic levels, both to evaluate the efficacy of the therapy and to correctly adjust the dose of the drug, thus avoiding glycemic disorders.

In fact, it is important to remember that hypoglycemic crises are accompanied by severe symptoms, such as to seriously compromise the patient's state of health.

Administration of glibenclamide in patients with impaired hepatic and renal function, or with G6PD enzyme deficiency should be avoided in order to prevent the development of adverse reactions such as pronounced hemolysis.

EUGLUCON ® contains lactose, therefore its intake could be followed by annoying side effects concentrated in the gastro intestinal tract in patients with lactase enzyme deficiency or glucose / galactose malabsorption.

It is also essential to remember that among the manifestations of hypoglycemia there is the reduction of the patient's perceptive abilities which could make the use of machinery or driving vehicles dangerous.

PREGNANCY AND BREASTFEEDING

The high risk to the health of the fetus, documented by several studies in the literature that tested the efficacy and safety of glibenclamide in pregnant women, and the possibility of using more effective and characterized therapeutic protocols, severely contraindicating the use of EUGLUCON ® during the period of pregnancy.

The contraindication to use also extends to the period of breastfeeding, given the secretion of the active ingredient in breast milk, which could cause hypoglycemia in the infant.

Interactions

As described for the other sulfonylureas also glibenclamide can interact with numerous other active principles, also varying significantly its pharmacokinetic and therapeutic properties.

Indeed the concomitant administration of insulin and other oral antidiabetic agents, ACE inhibitors, anabolic steroids and male sex hormones, chloramphenicol, coumarin derivatives, cyclophosphamide, disopyramide, fenfluramine, pheniramidol, fibrates, fluoxetine, ifosfamide, MAO inhibitors, miconazole, para- acid aminosalicylic acid, pentoxifylline (parenteral with high doses), phenylbutazone, azapropazone, oxyphenbutazone, probenecid, quinolonics, salicylates, sulfinpyrazone, sulfonamides, sympatholytic drugs such as beta-blockers and guanethidine, clarithromycin, tetracycline, tritoqualine, trophosphamide, may increase the effect hypoglycemic agent of EUGLUCON ® increasing the risk of hypoglycemia.

On the contrary the concomitant intake of acetazolamide, barbiturates, corticosteroids, diazoxide, diuretics, adrenaline and other sympathomimetic drugs, glucagon, laxatives (after prolonged use), nicotinic acid (at high doses), estrogens and progestins, phenothiazines, phenytoin, thyroid hormones and rifampicin could reduce the therapeutic efficacy of the drug thus leading to an altered and ineffective glycemic control.

Glibenclamide could also increase the plasma concentrations of ciclosporin, significantly increasing its toxicity.

Contraindications EUGLUCON ® - Glibenclamide

EUGLUCON ® is contraindicated in patients suffering from diabetes mellitus of the first type, severe hepatic and renal dysfunction, precoma and diabetic coma, keto diabetic acidosis, in case of hypersensitivity to the active ingredient or to one of its excipients and during pregnancy and 'feeding time

This medicine is also contraindicated during pregnancy and lactation.

Undesirable effects - Side effects

Various clinical trials and careful post-marketing monitoring seem to agree on the good tolerability of glibenclamide if taken in the doses and with the appropriate modalities.

The main side effects in fact, have been observed following the formulation of excessive dosages, and materialized in the appearance of episodes of hypoglycemia, easily reversible with oral intake of simple sugars.

On the other hand, adverse reactions to the gastro-intestinal and hematologic apparatus were more rare, promptly regressed once the therapy was suspended.

Dermatological conditions such as rash and urticaria have been observed in patients who are hypersensitive to the drug or to one of its components.