METFORAL ® Metformin

METFORAL ® is a drug based on Metformin Hydrochloride

THERAPEUTIC GROUP: Oral anti-diabetics

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

Indications METFORAL ® Metformin

METFORAL ® is indicated both in monotherapy and in combination therapy, in the treatment of type II diabetes, not corrected by a balanced diet and a normal lifestyle.

Mechanism of action METFORAL ® Metformin

The therapeutic efficacy of metformin contained in METFORAL ® and of biguanides in general, is due to its ability to modulate glucose metabolism, without acting on the pancreatic beta cells responsible for insulin secretion, guaranteeing in any case a good control of both basal glycemia and post-prandial, minimizing the risk of hypoglycemia.

From the pharmacodynamic point of view this active ingredient acts at the hepatic level, reducing gluconeogenesis and glycogenolysis, processes through which it increases hepatic secretion of glucose, and at the muscular level by increasing glucose uptake through the expression of specific receptors such as GLUT4.

However, the therapeutic action of metformin also appears to affect lipid metabolism, promoting the oxidation of fatty acids and reducing the synthesis of lipoproteins and NEFA (non-esterified fatty acids), partly responsible for the insulin resistance observed in diabetic patients of type II.

METFORAL ® therapy is facilitated by the easy intake of the drug, which, introduced orally, can reach the intestinal environment where it is absorbed at the intestinal level, reaching the maximum plasma concentration in two and a half hours, and being subsequently eliminated through the urine in unchanged form.

Studies carried out and clinical efficacy

1. METFORMIN THE FIRST CHOICE DRUG

Metformin is the drug of first choice in the treatment of prediabetic condition and type II diabetes. Its success is not to be attributed exclusively to the metabolic role, but also to the positive role in the prevention of cardiovascular and tumor diseases, in the improvement of bone, liver and gonadal health.

2. METFORMIN AND GASTRO-INTESTINAL ADVERSE REACTIONS

Nausea, vomiting and diarrhea are the most common adverse reactions described following metformin intake. Despite the high incidence of these conditions, the pathogenic mechanism is not yet fully understood, although it seems in part associated with the increased production of intestinal serotonin and a malabsorption of bile salts. Understanding the pathogenic mechanism could be important in the development of analogues with fewer side effects.

3. METFORMIN AND POLYCHISTIC OVEN SYNDROME

Polycystic ovary syndrome is one of those pathological conditions associated with hyperglycemia for which metformin therapy guarantees a significant improvement in symptoms. This study characterizes the mechanism of action of this drug, which is able to increase the expression of GLUT4 on the surface of granulosa cells in the presence of insulin, thus improving glucose uptake and facilitating follicle growth.

Method of use and dosage

METFORAL ® meformin coated tablets 500 - 850 mg: hypoglycemic therapy should start for the first two weeks with the intake of 2 or 3 tablets a day, during meals, and then adjust the dosage to the patient's blood sugar levels.

The maximum dose should never exceed 3 grams daily of metformin.

A further adaptation of the therapy should be provided for pediatric patients, the elderly and patients with reduced kidney function.

Warnings METFORAL ® Metformin

The potential risk of metabolic acidosis following the excessive intake or accumulation of metformin due to reduced renal excretion, should push the physician towards constant monitoring of blood glucose values and the creatininemia of the patient undergoing treatment.

Moreover, especially in individuals with reduced kidney function, it would be of fundamental importance, with quarterly frequency, to also check the functioning status of this organ, possibly adjusting the dosage or suspending therapy.

The therapy should also be suspended in case of surgical interventions at least 48 hours before, in order to avoid metabolic risks.

The dosage of METFORAL ® should be established by the doctor and possibly adapted to the improvement of blood chemistry parameters.

In order for the therapeutic protocol to be complete, it is necessary that the pharmacological therapy is combined with a generalized improvement in eating habits and lifestyle.

Although metformin is not capable of inducing hypoglycemia, combined therapy with insulin and sulfonylureas could lead to a significant drop in blood sugar making it dangerous to use machinery and drive vehicles.

PREGNANCY AND BREASTFEEDING

Several studies have shown the good safety profile of metformin for fetal health when taken during pregnancy; however the need for a fine glycemic control and the need to avoid potentially dangerous hyperglycaemias for the health of the unborn child, pushes doctors to prefer insulin as a drug of choice in the treatment of hyperglycemia during pregnancy.

On the contrary, it is strongly contraindicated to take METFORAL ® during breastfeeding, given the presence of the active ingredient in breast milk and the potential side effects for the health of the infant.

Interactions

The risk of lactic acidosis could increase in case of concomitant intake of alcohol or intravascular iodinated contrast agents, capable of reducing the excretory capacity.

Furthermore, the concomitant intake of glucocorticoids, beta-agonists and diuretics could reduce the therapeutic efficacy of metformin, in contrast to ACE inhibitors able to increase the risk of hypoglycemia, especially for combination therapies.

Contraindications METFORAL ® Metformin

METFORAL ® is contraindicated in case of hypersensitivity to the active ingredient or to one of its excipients, diabetic ketoacidosis, diabetic pre-coma, renal failure or renal dysfunction, dehydration, infections and shock, heart and respiratory failure, liver failure and during lactation .

Undesirable effects - Side effects

Although metformin intake was free of particularly significant side effects, METFORAL ® therapy was associated with the appearance of gastro-intestinal disorders such as

nausea, vomiting, diarrhea, abdominal pain and loss of appetite.

There were also more serious adverse reactions such as alterations in the absorption of vitamin B12, dermatological reactions on an allergic basis and alterations in the perception of taste, which however were observed only in rare cases.

One of the most clinically important adverse reactions from the sometimes fatal outcome associated with metformin therapy is lactic acidosis, which fortunately is very rarely observed in patients with reduced kidney function and in the event of an overdose of the active ingredient.