METFORAL ® Metformin
METFORAL ® is a drug based on Metformin Hydrochloride
THERAPEUTIC GROUP: Oral antidiabetics
Indications METFORAL ® Metformin
METFORAL ® is indicated both in monotherapy and in combined therapy, in the treatment of type II diabetes, not corrected by a balanced diet and a strange lifestyle.
METFORAL ® Mechanism of Action Metformin
The therapeutic efficacy of the metformin contained in METFORAL ® and of the biguanides in general is due to the ability to modulate the glucose metabolism, without acting on the pancreatic beta cells responsible for the secretion of insulin, guaranteeing in any case a good control of both basal and than post-prandial, minimizing the risk of hypoglycemia.
From a pharmacodynamic point of view, this active ingredient acts at the hepatic level, reducing gluconeogenesis and glycogenolysis, processes through which hepatic secretion of glucose increases, and at the muscle level by increasing glucose uptake through the expression of specific receptors such as GLUT4.
However, the therapeutic action of metformin also seems to affect lipid metabolism, promoting the oxidation of fatty acids and reducing the synthesis of lipoproteins and NEFA (non-esterified fatty acids), which are partly responsible for the insulin resistance observed in diabetic patients. 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 in the intestine, reaching maximum plasma concentration in two and a half hours, and being subsequently eliminated in the urine. in unchanged form.
Studies carried out and clinical efficacy
1. METFORMIN THE FIRST CHOICE DRUG
Vnitr Lek. 2010 Dec; 56: 1225-7.
Metformin as the first line antidiabetic agent
Metformin is the drug of choice for the treatment of prediabetic condition and type II diabetes. Its success is not to be attributed exclusively to the metabolic role, but also to its positive role in the prevention of cardiovascular and tumor pathologies, in improving bone, liver and gonadal health.
2. METFORMIN AND ADVERSE GASTRO-INTESTINAL REACTIONS
Diabetes Metab. 2011 Jan 12.
Metformin and digestive disorders.
Bouchoucha M, Uzzan B, Cohen R.
Nausea, vomiting and diarrhea are the most common adverse reactions described following the intake of metformin. 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 serotonin. intestinal and bile salts malabsorption Understanding the pathogenic mechanism could be important in the development of analogues with fewer side effects.
3. METFORMIN AND POLYCISTIC OVARIAN SYNDROME
J Clin Endocrinol Metab. 2011 Mar; 96: E427-35.
Action of metformin on the insulin-signaling pathway and on glucose transport in human granulosa cells.
Rice S, Pellatt LJ, Bryan SJ, Whitehead SA, Mason HD.
Polycystic ovary syndrome is one of those pathological conditions associated with hyperglycemia for which therapy with metformin guarantees a significant improvement in symptoms. This study characterizes the mechanism of action of this drug, capable of increasing the expression of GLUT4 on the granulosa cell surface in the presence of insulin, thus improving glucose uptake and facilitating follicle growth.
Method of use and dosage
METFORAL ® coated tablets of 500 - 850 mg meformin: hypoglycemic therapy should begin for the first two weeks with the intake of 2 or 3 tablets per day, during meals, and then the dosage should be adjusted to the patient's blood glucose values.
The maximum dose should never exceed 3 grams of metformin per day.
Further adaptation of the therapy should be envisaged for pediatric patients, the elderly and patients with impaired renal function.
METFORAL ® Metformin warnings
The potential risk of metabolic acidosis following excessive intake or accumulation of metformin due to reduced renal excretion should prompt the physician to constantly monitor the patient's blood glucose and creatinine levels.
Furthermore, especially in individuals with reduced renal function, it would be of fundamental importance to also check the functioning status of this organ on a quarterly basis, possibly adjusting the dosage or suspending therapy.
Therapy should also be suspended in case of surgery at least 48 hours before, in order to avoid metabolic risks.
The dosage of METFORAL ® should be established by the physician and possibly adapted to the improvement of blood chemistry parameters.
For the therapeutic protocol to be complete, it is necessary that the drug therapy is also combined with a generalized improvement in eating habits and lifestyle.
Although metformin itself is not capable of inducing hypoglycaemia, combined therapy with insulin and sulfonylureas could result in a significant drop in blood glucose, making it dangerous to use machinery and drive vehicles.
PREGNANCY AND BREASTFEEDING
Several studies have demonstrated the good safety profile of metformin for fetal health when taken during pregnancy; however, the need for fine glycemic control and the need to avoid hyperglycemia potentially dangerous for the health of the unborn child, pushes doctors to prefer insulin as the drug of choice in the treatment of hyperglycemia in pregnancy.
On the contrary, it is strongly contraindicated to take METFORAL ® during the breastfeeding period, given the presence of the active ingredient in breast milk and the potential side effects for the health of the infant.
The risk of lactic acidosis could increase in case of concomitant intake of alcohol or intravascular iodinated contrast media, which can reduce the emunctory capacities.
Furthermore, the concomitant intake of glucorticoids, beta-agonists, diuretics could reduce the therapeutic efficacy of metformin, unlike ACE inhibitors capable of increasing the risk of hypoglycaemia, especially for combined therapies.
Contraindications METFORAL ® Metformin
METFORAL ® is contraindicated in case of hypersensitivity to the active substance or to one of its excipients, diabetic ketoacidosis, diabetic pre-coma, renal insufficiency or renal dysfunction, dehydration, infections and shock, cardiac and respiratory insufficiency, hepatic insufficiency and during lactation. .
Undesirable Effects - Side Effects
Although the intake of metformin was free of particularly significant side effects, therapy with METFORAL ® has been associated with the onset of gastro-intestinal disorders such as
nausea, vomiting, diarrhea, abdominal pain and loss of appetite.
There was no lack of more serious adverse reactions such as alterations in the absorption of vitamin B12, allergic-based dermatological reactions and alterations in the perception of taste, which however were observed only in rare cases.
One of the most clinically important adverse reactions with a sometimes fatal outcome associated with metformin therapy is lactic acidosis, which fortunately is very rarely observed in patients with impaired renal function and in the case of overdose of the active substance.
METFORAL ® can only be sold under medical prescription.
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