Metformin Long - start of therapy for type 2 diabetes mellitus

One of the most common diseases in modern society is diabetes mellitus (DM). The medical and social significance of diabetes is determined by the steady increase in the number of patients, the high risk of macro- and microvascular complications, as well as the impact of the disease on the quality and life expectancy of patients. A similar global trend of steady growth in the number of people with diabetes mellitus also occurs in the Republic of Belarus. Over the past 10 years, the number of such patients in Belarus has increased from 150 thousand to 336 thousand people, 94% of whom suffer from type 2 diabetes (data as of 01/01/2019). And every year there are more patients with type 2 diabetes in the country. Currently, the drug metformin occupies a central place in all current recommendations for the management of type 2 diabetes.

Thus, the 2021 consensus algorithm of the American and European Diabetes Associations (ADA/EASD) strongly recommends the use of metformin as a first-line agent (in the absence of contraindications or intolerance), immediately upon diagnosis of type 2 diabetes, in addition to image correction life (dietary recommendations and exercise). The preference given to this drug is not accidental: the effectiveness and safety of metformin have a huge evidence base, its cost is low, the drug reduces the risk of developing cardiovascular complications, helps reduce body weight, and the risk of hypoglycemia when taking it is minimal. In 2021, the American Diabetes Association released new recommendations that metformin remains the preferred drug for initiating glucose-lowering therapy in patients with type 2 diabetes (Evidence Level A). However, unfortunately, the tolerability of metformin is limited by side effects from the gastrointestinal tract, which, according to some data, develop in almost 25% of patients, which leads to discontinuation of the drug in 5-10% of patients. In addition, splitting up metformin intake throughout the day and a large number of tablets, if necessary, to take other drugs to treat concomitant diseases, creates additional inconvenience for patients. Insufficiently good tolerability from the gastrointestinal tract and the need to take it more than once a day leads to decreased adherence to metformin therapy in some patients. The new extended-release dosage form of metformin has been designed to provide sustained release of the drug to improve tolerability and ensure prolonged action of the drug. This dosage form helps slow down the transit of the tablet from the stomach through the pylorus, thereby significantly increasing the time the drug remains in the stomach. In vitro studies have shown that 90% of metformin in the conventional dosage form is released within 30 minutes. In contrast, extended-release metformin releases 90% of the drug within 10 hours, relatively independent of gastrointestinal pH and motility. Thus, the dosage form of Metformin Long provides a slower, smoother and longer delivery of the drug without an initial rapid increase in the concentration of the drug in the plasma. When prescribed in the evening with food, due to its dosage form, Metformin Long acts synchronously with natural physiological processes, when gastrointestinal emptying slows down at night. This leads to prolonged absorption of metformin and justifies the administration once a day.

However, patients should be aware and warned that the inactive portion of the metformin extended-release tablet is excreted unchanged. Otherwise, this may lead to erroneous conclusions and unmotivated refusal to use this dosage form. The hypoglycemic effect of modified-release metformin is comparable to that of immediate-release metformin. Thus, modified-release metformin, having all the advantages of the conventional form of the drug, is devoid of a significant part of its disadvantages: taking extended-release metformin once a day significantly simplifies the treatment regimen and, together with a decrease in the frequency of side effects, increases patient adherence to treatment. Metformin Long, the first long-acting generic metformin in the Republic of Belarus, is produced by the Borisov Medical Preparations Plant Open Joint Stock Company in dosages of 500 mg, 750 mg and 1000 mg. The indication for the use of drugs Metformin Long 500, 750, 1000 is type 2 diabetes mellitus in adults (especially in overweight patients) with ineffective diet therapy and exercise, as monotherapy or in combination with other oral hypoglycemic agents or together with insulin . When used as monotherapy or combination therapy in combination with other oral hypoglycemic agents, Metformin Long is used as follows:

The recommended initial dose is 1 tablet of Metformin Long 500 per day.
After 10-15 days of treatment, the dose must be adjusted in accordance with the results of measurements of glucose levels in the blood serum. Slowly increasing the dose helps reduce gastrointestinal side effects. The maximum recommended dose is 4 Metformin Long 500 tablets per day (2000 mg).
It is recommended to take the dose of the drug once a day with meals in the evening, increasing by 500 mg every 10-15 days to a maximum dose of 2000 mg. If, when using Metformin Long at a maximum dose of 2000 mg 1 time per day, the required level of glycemia cannot be achieved, the dose taken can be divided into 2 doses (morning and evening during meals). If the required glycemic level is not achieved after this, metformin immediate-release tablets can be used at the maximum recommended dose of 3000 mg per day.
For patients already taking metformin, the starting dose of Metformin Long should be equivalent to the immediate-release tablet dose. For patients taking metformin at a dose above 2000 mg, switching to Metformin Long is not recommended.
If you switch to Metformin Long, you must stop taking the other antidiabetic drug.
Metformin Long 750 and Metformin Long 1000 are intended for patients already receiving metformin immediate-release tablets.
Doses of Metformin Long 750 or Metformin Long 1000 should be equivalent to the daily dose of metformin immediate-release tablets with a maximum dose of 1500 mg or 2000 mg, respectively, taken in the evening with meals.

In combination therapy in combination with insulin, Metformin Long is used as follows:

To achieve better control of blood glucose levels, metformin and insulin can be used in combination therapy. Typically, the initial dose of Metformin Long 500 is 1 tablet per day with meals in the evening; the dose of insulin must be adjusted in accordance with the results of measuring blood glucose levels.
For patients already receiving metformin and insulin in combination therapy, the dose of Metformin Long 750 or Metformin Long 1000 should be equivalent to the daily dose of metformin with a maximum dose of 1500 mg or 2000 mg, respectively, in the evening with meals, while the insulin dose is adjusted to based on blood glucose measurements.
For elderly patients and patients with reduced renal function, the dose is adjusted based on assessment of renal function, which should be carried out regularly.
Due to the lack of data on use, Metformin Long should not be used in children under 18 years of age.
Medicines Metformin Long 500, Metformin Long 750, Metformin Long 1000 are available with a doctor's prescription.

How can metformin be useful in bodybuilding?

It’s no secret (and for some it’s a secret) that bodybuilders’ main weapon for fat loss is a low-carb diet. During a low-carbohydrate diet, the body receives few carbohydrates (which are the main and preferred “fuel” for the body), and therefore the body is forced to switch to fat nutrition (burns accumulated fat reserves).

Thus, we can say that a low-carbohydrate diet and taking metformin create essentially similar conditions in the body. Both lead to fat burning by limiting the amount of carbohydrates entering the body and lowering blood sugar levels.

Therefore, metformin can be used in bodybuilding in two ways: to “replace” a low-carbohydrate diet (that is, in cases where the athlete wants to burn fat without dietary restrictions, or without resorting to too strict restrictions), or to complement a low-carbohydrate diet, in order to obtain more pronounced results.

How else can metformin be useful?

Although there are rumors (more precisely, not even rumors, but the results of scientific research) according to which metformin can increase life expectancy. The studies have so far been conducted on animals, which does not allow us to say 100% that this will have the same effect on humans. However, this possibility cannot be ruled out.

This information is difficult to verify in practice (in relation to humans), since the human life expectancy is already quite long, and conducting such an experiment on humans seems problematic (to wait too long for the results to make sure whether this is really the case).

What to watch out for when taking metformin

From all of the above, we can conclude that metformin is an excellent drug for enhancing fat burning in bodybuilding. This is partly true, however, this drug has some side effects that can spoil the first positive impression of it. It must be said that for the most part these effects are not so terrible, but you need to be aware of them.

The most famous side effect of metformin is diarrhea. It does not always occur and not for everyone, so here you need to look, first of all, at your personal feelings.

If taking metformin does not cause you to experience this unpleasant effect, then you can safely continue taking it. If this trouble does not pass you by, try reducing the dosage (about dosages - below), and/or reducing the amount of carbohydrates in the diet, since it is often the excess of carbohydrates that leads to this.

It may take some time for the body to adapt to taking metformin, so if diarrhea occurs, you can first reduce the dosage and then gradually increase it. As a last resort, if these measures do not help, it is better to stop taking the drug.

Nausea may also occur. It should be dealt with in the same ways as with diarrhea (first of all, reducing the dosage, with a possible, but not mandatory, subsequent increase).

The most important thing you need to watch out for when taking metformin is drinking alcohol! Alcohol is strictly incompatible with metformin . It significantly enhances the above side effects and can lead to lactic acidosis (and advanced lactic acidosis can even lead to death (!)).

Extreme caution should be used when combining metformin with other drugs that lower blood sugar levels. Their combined effects can cause your blood sugar to drop too low, which in turn can lead to a hypoglycemic coma.

These warnings are the most basic. There may also be some other minor side effects (such as skin rash or loss of appetite), but these are the ones you should be aware of first.

There is also an opinion that metformin reduces testosterone levels. For example, Anton Petryakov (Basilio) speaks about this:

If this is true, then this is a big disadvantage for bodybuilders. However, by and large there is no unambiguous information about the degree of testosterone reduction (if you have it, write in the comments).

If this decrease is insignificant, then we can say that the positive effects outweigh the negative ones (you can put up with this for the sake of fat burning). If metformin leads to a significant decrease in testosterone, then this is a reason to think about it.

Do not use metformin if you have metabolic diseases. If you continue to feel unwell as a result of taking metformin, be sure to consult your doctor.