Metformin is a tablet drug intended for the treatment of diabetes and belongs to the biguanide group. It promotes rapid weight loss, which is why it is used for weight loss. Metformin is quite often used in bodybuilding for the so-called drying, which improves muscle definition. Today, metformin can be purchased under various trade names - Siofor, Glucophage, Diaformin, Gliformin, etc. Before taking the drug, you should familiarize yourself with its mechanism of action , a list of contraindications and possible adverse reactions.
What is metformin
Initially, metformin was (and still is) a drug prescribed to diabetics to lower blood sugar levels. This drug has shown to be highly effective and is widely used in medical practice.
Bodybuilders, realizing the possible positive effects of taking it, took metformin into their arsenal and began to use it to enhance fat burning.
The fat-burning properties of metformin are of interest not only to bodybuilders, but also to ordinary people concerned about the problem of excess weight.
How does metformin work?
Metformin slows down the absorption of carbohydrates (glucose) in the digestive tract. This leads to a noticeable decrease in blood sugar levels. First of all, it is for this purpose that this drug is prescribed to diabetics.
However, metformin does not completely block the entry of carbohydrates into the blood, so during meals the body begins to produce insulin. This is the body's natural reaction to the supply of nutrients.
Insulin is responsible for “pulling” nutrients received during food intake throughout the body’s cells. Under normal conditions, these substances are absorbed and accumulated by both muscle tissue (this is good) and fat tissue (this is bad).
Taking metformin, in addition to lowering sugar levels, helps reduce insulin production, as well as lowering the level of sensitivity of insulin receptors in cells. Thus, metformin prevents the deposition of nutrients (fats and carbohydrates) in the tissues of the body, and leads to the fact that these substances do not accumulate “in reserve”, but circulate in the blood and are used by the body to cover current energy costs.
As a result of all this (there is little sugar in the blood, plus it is not stored in fat), the person does not get fat (or gets fat less than usual).
Metabolic syndrome: possibilities of using metformin
RGMU named after N.I.
Pirogov M
metabolic syndrome X is a complex of interrelated disorders of carbohydrate and fat metabolism, as well as mechanisms of regulation of blood pressure (BP) and endothelial function, the development of which is based on a decrease in tissue sensitivity to insulin - insulin resistance (IR). Patients with metabolic syndrome, as a rule, seek medical help for arterial hypertension, type 2 diabetes mellitus or coronary heart disease, and therefore find themselves in the field of view of doctors of various specialties: therapists, cardiologists, endocrinologists.
Modern ideas about the pathogenesis of metabolic syndrome
In the development of IR, both the factor of genetic predisposition (impairment of receptor and post-receptor mechanisms of insulin signal transmission) and certain lifestyle features are important: excess nutrition, decreased physical activity.
As a result of a decrease in the sensitivity of target cells to the action of insulin, the absorption of glucose by insulin-dependent tissues (liver, muscles and adipose tissue) is disrupted and the preconditions are created for the development of hyperglycemia. However, due to a compensatory increase in insulin secretion by pancreatic b-cells, the concentration of glucose in the blood serum can remain normal for a long time. Thus, hyperinsulinemia
(GI) is the earliest and most constant marker of IR.
Having a powerful lipotropic effect, GI promotes an increase in body weight due to the accumulation of adipose tissue mainly in the upper half of the body and in the abdominal cavity (in the omentum and mesentery). Abdominal obesity
is one of the key points in the development of metabolic syndrome.
Free fatty acids (FFA), released in large quantities from abdominal adipose tissue, enter the portal vein into the liver, and then into the systemic circulation. In the liver, FFAs activate the processes of gluconeogenesis, which leads to an increase in glucose production by the liver
and the development of fasting hyperglycemia.
FFAs entering the systemic circulation disrupt the function of insulin receptors and aggravate IR (lipotoxicity effect)
.
Under these conditions, the amount of insulin secreted by b-cells may be insufficient to overcome the IR barrier and a relative insulin deficiency
.
The inability of b-cells to provide the required level of insulin hypersecretion leads to the development of carbohydrate metabolism disorders:
from a moderate increase in plasma glucose concentration, first on an empty stomach, then after a food load, and finally to type 2 diabetes mellitus.
In turn, hyperglycemia causes a deterioration in pancreatic b-cell function ( glucotoxicity effect
), completing a vicious circle.
Excessive intake of FFAs into the liver, which are substrates for the synthesis of triglycerides, leads to an increase in the production of very low density lipoproteins (VLDL). At the same time, the elimination of VLDL and low-density lipoproteins (LDL) in IR is reduced due to a decrease in lipoprotein lipase activity. The level of high-density lipoproteins (HDL), on the contrary, decreases, since their formation requires apoproteins and phospholipids released from VLDL and LDL during their lipolysis. In addition, with IR, changes occur in the composition of LDL, in which the protein content increases and the amount of cholesterol esters decreases. As a result, smaller and denser LDL are formed, characterized by a high degree of atherogenicity.
Thus, the main characteristics of dyslipidemia in metabolic syndrome are:
hypertriglyceridemia, increased levels of VLDL and LDL, changes in the structure of LDL and decreased levels of HDL.
It has been established that IR and compensatory HI affect a number of mechanisms of blood pressure regulation. GI has a prohypertensive effect by increasing the reabsorption of sodium and water by the kidneys, stimulating the centers of the sympathetic nervous system and activating Na+/H+ metabolism in vascular smooth muscle cells, which promotes the accumulation of Na+ and Ca2+ ions in them and increases sensitivity to the pressor effects of catecholamines and angiotensin II . Through the local renin-angiotensin vascular system, insulin stimulates the growth and proliferation of smooth muscle cells and promotes the development of remodeling processes (hypertrophy of the muscular lining of blood vessels, reduction in internal diameter), which is a factor in stabilizing elevated blood pressure levels.
In addition, with IR, the synthesis and secretion of nitric oxide (NO) by the vascular wall is disrupted. Considering that NO, in addition to its vasodilating effect, also has antiatherogenic properties, disruption of this mechanism can contribute to the development of not only hypertension, but also atherosclerosis.
Diagnostics
To diagnose metabolic syndrome, the presence of two of its three main manifestations is sufficient: abdominal obesity (the earliest clinical marker of IR), dyslipidemia, and impaired carbohydrate metabolism (Table 1).
Arterial hypertension is not an obligatory component of the metabolic syndrome, but is often detected in patients with IR. Thus, in type 2 diabetes mellitus, hypertension is registered in 50% of cases.
On the other hand, in patients with hypertension (HTN), manifestations of metabolic syndrome are present in more than 80% of cases. Elevated insulin concentrations have also been found to predispose to the development of hypertension. The results of long-term observation of people with hyperthyroidism showed that they are more likely than people with normal levels of insulin in the blood plasma to subsequently develop hypertension. At the same time, other manifestations of IR (dyslipidemia, impaired glucose tolerance or type 2 diabetes mellitus) also developed in parallel. Whether IR is an independent cause of the development of hypertension or contributes to the implementation of a genetic predisposition has not yet been definitively established.
In the future, the importance of IR in the pathogenesis of hypertension may recede into the background. Activation of the renin-angiotensin system, development of vascular remodeling processes, restructuring of kidney function and baroreceptor apparatus contribute to the “fixation” of elevated blood pressure levels. However, IR may contribute during headache and at later stages of its development. Activation of the sympatho-adrenal system under the influence of GI and increased levels of FFA leads to a disruption of the circadian rhythm of blood pressure with its insufficient decrease at night, i.e. to the development of nocturnal hypertension. In addition, IR contributes to the formation of a complex of additional risk factors (hyperglycemia, dyslipidemia, disorders of the fibrinolysis system), which significantly increase the total risk of developing cardiovascular complications.
Even when the only manifestation of IR is compensatory GI, the risk of developing cardiovascular complications is already significantly increased. The appearance of IGT is accompanied by a sharp jump in the frequency of macrovascular complications, and by the time chronic hyperglycemia develops, which meets the diagnostic criteria for diabetes, many patients already have clinical manifestations of coronary artery disease, including a previous myocardial infarction. This circumstance emphasizes the need for timely diagnosis of metabolic syndrome X and correction of associated metabolic disorders.
Treatment
A prerequisite for successful treatment of patients with MS is lifestyle changes aimed at reducing body weight (Table 2). Considering that non-drug approaches are not feasible for most patients, the use of drugs that promote weight loss and drugs that restore tissue sensitivity to insulin in the treatment of these patients is of particular interest.
Thiazolidinediones are a relatively new class of antidiabetic drugs, the main mechanism of action of which is to reduce tissue IR, mainly myocytes and adipocytes. However, the widespread use of drugs in this group is currently limited by the presence of a hepatotoxic effect.
Another group of drugs that can increase tissue sensitivity to insulin are biguanides (phenformin, buformin and metformin). Due to the high risk of developing lactic acidosis with the use of phenformin and buformin, the only biguanide currently used is metformin (Siofor®, Berlin-Chemie).
Metformin
The effect of metformin on glucose metabolism is mediated by three main mechanisms: improving the utilization of glucose by tissues, reducing glucose production by the liver and inhibiting glucose absorption in the small intestine. As a result, metformin effectively reduces blood glucose levels both on an empty stomach and after a meal.
Unlike sulfonylurea derivatives, metformin does not have a stimulating effect on insulin secretion, therefore treatment with metformin is not accompanied by the risk of developing hypoglycemic conditions and weight gain. On the contrary, metformin promotes stabilization and even some weight loss in obese patients (Table 3).
Information about the effect of metformin on blood pressure levels is quite contradictory. Giugliano D. et al. (1993) noted a significant hypotensive effect of metformin in hypertensive patients with obesity and type 2 diabetes mellitus. However, Snorgaard O. et al. (1997) found no effect of metformin on blood pressure in patients with both normal and overweight.
We studied the effect of metformin on the 24-hour blood pressure profile in overweight hypertensive patients. 11 patients had abdominal obesity combined with impaired glucose tolerance, 15 patients had abdominal obesity and normal glucose tolerance, and 12 patients had peripheral obesity without signs of impaired carbohydrate metabolism. After 6 weeks of treatment with metformin at a daily dose of 1500–1700 mg, a decrease in blood pressure levels according to the results of daily monitoring was noted only in patients with impaired glucose tolerance. In this group of patients, a decrease in systolic blood pressure (SBP) by 8.4 (1.1–13.6) mmHg was noted. Art. during the day and by 10.7 (2.2–15.5) mm Hg. Art. at night, as well as a decrease in load indicators of both blood pressure and diastolic blood pressure (BPd) at night. The ADS time index decreased by 16.7 (4.0–54.6)%, the ADD time index – by 68.2 (42.3–92.3)%, the ADS area index – by 66.2 (49.1 –71.1)%, area index ADD – by 88.6 (1.3–100.0)%. Changes in the daily blood pressure profile during treatment with metformin occurred in parallel with the dynamics of other manifestations of IR (body weight, glycemic levels, concentrations of insulin and uric acid in the blood plasma).
Metformin is contraindicated in patients with chronic renal failure, hypoxic conditions of various etiologies (anemia, cardiac or respiratory failure, infectious conditions), as well as alcohol abuse and liver dysfunction (increased ALT and AST by more than 2 times). The incidence of lactic acidosis in patients taking metformin is 5–9 cases per 100 thousand people per year, which is almost 20 times less than when treating with buformin and phenformin.
The results of a multicenter prospective study on the primary prevention of diabetes complications (United Kingdom Prospective Diabetes Study, UKPDS) completed in 1998 demonstrated the effectiveness and safety of long-term treatment with metformin.
In patients with type 2 diabetes with obesity, there was a 36% reduction in all-cause mortality, a 32% reduction in the incidence of all diabetes complications, and a 30% reduction in the incidence of macrovascular complications of diabetes, including a 39% reduction in the risk of myocardial infarction. Moreover, among 342 patients who took metformin at a daily dose of 1700–2550 mg/day for an average of 10.7 years, not a single case of lactic acidosis was recorded. The results of this study proved the feasibility of using metformin for the treatment of patients with type 2 diabetes with obesity. According to our data and the results of a number of other studies, it seems promising to prescribe metformin (Siofor) at earlier stages of the development of metabolic syndrome: in patients with impaired glucose tolerance and in patients with mild hypertension with manifestations of IR (in combination with measures to change lifestyle ). References:
1. Reaven GM Role of Insulin Resistance in Human Disease. Diabetes 1988; 37(12): 1595–1600.
2. Almazov V.A., Blagosklonnaya Ya.B., Shlyakhto E.V., Krasilnikova E.I. The role of abdominal obesity in the pathogenesis of insulin resistance syndrome. Therapeutic Archive 1999; 10: 18–22.
3. Moiseev V.S., Ivleva A.Ya., Kobalava Zh.D. Hypertension, diabetes mellitus, atherosclerosis are clinical manifestations of metabolic syndrome X. Bulletin of the Russian Academy of Medical Sciences 1995; 5:15–8.
4. Kobalava Zh.D., Kotovskaya Yu.V. Features of the daily blood pressure profile in hypertensive patients with metabolic disorders. Clinical Pharmacology and Therapy 1995; 4(3): 50–1.
5. Crofford OB Metformin. N Engl J Med 1995; 333(9): 588–9.
Metformin –
Siofor (trade name)
(Berlin-Chemie AG)
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 to lose weight quickly with Metformin
As you already understand, Metformin only blocks carbohydrate metabolism. This means that sweets, baked goods or pasta eaten will not spoil your figure, although you will still have to suffer: at least a day of rumbling in the stomach, gas and loose stools are guaranteed. But even if you don’t eat carbohydrates at all and at the same time lean on fatty foods, you won’t be able to lose weight. Therefore, the first rule is to eat dietary foods.
With the help of Metformin, carbohydrates formed in the body are captured by muscle cells, where they are burned. This is why athletes love this drug before competitions: a lot of energy is accumulated for the muscles, they become stronger and more resilient. But if you dream about losing weight, swallow pills and sit in front of the TV, glucose will not be able to burn. If you don’t want a loose cellulite mass to sway in the mirror instead of a slender bodybuilder’s body, even small, but daily physical activity should become the norm.
The third rule concerns health. There is no need to take risks and take other weight loss supplements or medications that contain diuretic or laxative components along with Metformin. In such cases, there is always a risk of damaging the kidneys, and then you will have to forget about your figure and fight for your own life.
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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.
Metformin for weight loss and cutting in bodybuilding
1. Evgeniy Shvachko I have a rather serious question.
I understand that it is not very easy to answer this, but I am looking for an intelligible explanation for this. I turned to you because you are a pragmatic, well-read and thoughtful person. Now the situation itself: I have been suffering from a very strong neurological disorder for quite some time. I won’t describe the symptoms, because... for a long time, and no one cares. Previously, like most people, when stressed, I would go into overdrive, drink a couple of glasses, and light a cigarette. I started eating smaller meals, eliminating high-calorie foods and all sorts of crap from my diet. This is already the third week, I feel a hundred times better, almost like I did in childhood. The convulsions have gone away, I have stopped most medications, but sometimes involuntary twitching of the muscles of the face and neck occurs. Today is one of those days.
I endured it for a long time, then I felt that I really wanted either sunflower seeds or nuts. At this time I don’t feel hungry. Has gained. I ate a handful of seeds, 10 grams, no more. After 2 minutes everything passed as if nothing had happened. Previously, I also noticed that when I eat a small amount of hazelnuts, it’s bad. nuts, peanuts or seeds, my health improved. So what's the secret? Sorry for being so detailed.
All the best.
2. I’m Julia. In my case, metwormin helped me a lot to lose weight. But I’m a woman and I don’t need testosterone for muscles.
But proper nutrition, swimming, classes with a trainer did not give me the desired result, or rather it was, but in a month and a half minus 1600! When others were losing 6 per month. I went to the endocrinologist and a miracle happened! But I also took it with vitamin D drops.
Diarrhea, of course, happens, but only on condition that you overeat on jam or chocolate.)) Otherwise, after three or five days everything will return to normal. The doctor helped me normalize my weight in three months, but everything was under supervision and with tests.
The doctor immediately said that with my tests I could die on the treadmill, but I would lose weight 10 grams at a time. Everything is individual. Now with training I manage to maintain weight without medication. I’m not campaigning, but I received more benefit than harm..
3. moroz78ps5 Dear Basilio. I watch your videos with interest, I learned a lot of useful things! I also learned a lot about sports supplements. I’ve been working out for three years now, I started buying sports nutrition probably a year ago. If it’s not too difficult, maybe you can tell me the correct dosage regimen, what’s what.
I exercise exclusively in the morning, but I can’t find anywhere how to take it correctly. Everywhere there are instructions for evening workouts... I consume protein, BCA, citrulline, AKG, glutamine, I recently took betaalanine after watching your video about sports nutrition). I’m not sure what you’ll answer, of course... I’ll probably download it from such letters). But an attempt is not torture).
Thank you if you at least read it)
4. monster0385 Basilio, hello. I enjoy watching your videos and learned a lot. Let me go a little off topic. I asked it in a video about the keto diet, I’ll duplicate it here. Please tell me, maybe it was somewhere, but I didn’t see it.
What does the smell of ammonia indicate during cardio exercise? After strength training I do cardio for 40 minutes, after 20 minutes the smell of ammonia appears. I hardly eat carbohydrates, about 50 grams. My weight is now about 103 kg. I started with 122 kg, lost it in three months.
I feel good. Thank you
5. Igor Kislyakov Thanks for the video, Basilio.
And I’ve been using bronholitin 25 grams, caffeine 200 mg, aspirin forte 200 mg, yohimbine 10 mg for 3 weeks now, and all this once a day in the morning, every day, I’ve lost 5 kg of folds, cardio with weights on the stairs is going great and then follows split strength into 2 muscle groups. I previously lost weight on water on a workout, lost 22 kg in 6 months, then everything stopped. I had to try eca with yohimbine, it worked so far, we’ll see.
6. Heinrich the Mad I remember accidentally watching a video on YouTube about metformin and was so glad that such a miracle drug exists) But that video did not talk about the disadvantages) Basilio, thank you for being there
