GLUCOPHAGE ® Metformin

GLUCOPHAGE ® 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 GLUCOPHAGE ® Metformin

GLUCOPHAGE ® is indicated in improving glycemic control in patients with type II diabetes mellitus, especially in the presence of overweight / obesity and lack of response to dietary therapy and exercise.

The drug can be effective both as monotherapy and in combination with insulin or sulfonylureas.

Mechanism of action GLUCOPHAGE ® Metformin

GLUCOPHAGE ® is a drug based on metformin, an active ingredient belonging to the biguanide category, useful in reducing both post-prandial and basal glycaemia.

Once taken orally it is absorbed at the gastrointestinal level, reaching its maximum plasma concentration in about two and a half hours, with an absolute bioavailability of 50/60%.

Through the circulatory stream, it reaches the sensitive tissues, above all the muscles and the liver, where, by activating the AMP-dependent protein kinase, it regulates the expression of different genes involved in the regulation of glucose metabolism (not promoting pancreatic insulin secretion).

More precisely, metformin acts at the hepatic level by inhibiting gluconeogenesis (glucose synthesis starting from non-glucide precursors) and glycogenolysis, increasing the oxidation of fatty acids and reducing the synthesis of non-esterified fatty acids and lipoproteins probably involved in insulin receptor desensitization .

At the muscular level instead, thanks also to the increase in the expression of glucose receptors, this active ingredient is able to increase glucose uptake, thereby reducing blood sugar levels.

After its activity the metforima, after a half-life of about six hours, is excreted unchanged in the urine.

Studies carried out and clinical efficacy

1. METFORMIN AND CARDIOVASCULAR RISK

Work that evaluated as many as 35 clinical trials, for over 11, 000 participants, relative to the ability of metformin, to reduce the risk of cardiovascular events and associated mortality. From the statistical re-elaboration of the data, it was observed how the metotherapy assumption of monotherapy can be associated with a reduction in mortality and an increase in survival.

2. EFFECTS OF METFORMIN ON THE WEIGHT AND RISK FACTORS IN OBESE CHILDREN

Metmorphine is known to generally contribute to weight loss by improving glucose homeostasis and promoting fatty acid oxidation. This study carried out on children with age between 6 and 12 years with BMI around 34, treatment with metformin showed a modest but favorable effect in 6 months in the improvement of body composition, glucose homeostasis and insulin sensitivity .

3. METFORMIN AND SEED QUALITY

All-Italian study, which evaluated the ability of metformin to improve semen quality in patients suffering from metabolic syndrome and astenozoospermia oligo-terate. More precisely, the treatment with this oral hypoglycemic agent has guaranteed a significant improvement in the quality of the seed, reducing insulin resistance, the presence of globulin binding steroid hormones and increasing blood concentrations of androgens.

Method of use and dosage

GLUCOPHAGE ® meformin coated tablets 500 - 850 - 1000 mg: the dosage formulation should be established by the doctor following the evaluation of the patient's glycemic profile.

In any case, the initial dosage should start with a 500 mg tablet 2 or 3 times a day during or after meals, to reach a maximum of 3 g per day based on the patient's blood sugar levels.

Additional dose adjustments should be made for elderly, pediatric or concomitant insulin therapy.

It is important to reiterate the need to adapt the metformin dose to the patient's glycemic profile and to his general health conditions.

Warnings GLUCOPHAGE ® Metformin

Excessive intake of metformin or the concomitant presence of factors or pathologies capable of reducing renal secretion of this active ingredient, could determine the onset of a severe and lethal metabolic pathology such as lactic acidosis.

In this regard it is therefore of fundamental importance, especially for patients with reduced kidney function, to constantly monitor the levels of creatinine, and the functionality of the organ itself, in order to avoid unpleasant side effects, thus adjusting the dosage.

Treatment with metformin should be suspended at least 48 before surgery, to avoid serious metabolic problems, while it is essential, to improve the patient's general health conditions, to combine a healthy lifestyle with pharmacological therapy.

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

The treatment of hyperglycemia in pregnancy is of fundamental importance to safeguard the health of the fetus, reducing the risk of complications and abortions.

For this reason, although metformin has a good safety profile, it is preferred to use insulin in glycemic control.

On the contrary, metformin intake during breastfeeding is contraindicated, given the secretion of the active ingredient in breast milk.

Interactions

One of the most important risks associated with potential interactions between metformin and other active ingredients is lactic acidosis, which could occur following the concomitant use of alcohol or iodinated intravascular contrast agents, which can reduce renal excretion, increasing its blood concentrations.

From the glycemic point of view, on the other hand, the concomitant use of glucocorticoids, beta-agonists, diuretics could reduce the therapeutic efficacy of metformin, while the simultaneous intake of ACE inhibitors could, by reducing glycaemia, lead to an ineffective control of glucose metabolism .

Contraindications GLUCOPHAGE ® Metformin

GLUCOPHAGE ® 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

Metformin intake is very frequently associated with the appearance of side effects on the gastro-intestinal level such as nausea, vomiting, diarrhea, abdominal pain and loss of appetite.

Rarer, but clinically more relevant, were reactions such as decreased vitamin B12 absorption, lactic acidosis, increased transaminase and allergic skin reactions.

The concomitant administration of insulin, however, could be associated with the appearance of hypoglycemia, with potentially dangerous side effects.