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Active Ingredient: Metformin

Metformin is a tableted hypoglycemic drug of the biguanide class for ingestion. This drug is used in the treatment of type 2 diabetes mellitus, especially in people who are overweight and obese, while maintaining normal kidney function. Studies are being conducted on the use of metformin in gestational diabetes and polycystic ovary syndrome. The drug has been studied for other diseases in which insulin resistance may be an important factor.

When administered correctly, metformin causes few side effects (among which gastrointestinal disorders are more frequent) and is associated with a low risk of hypoglycemia. Lactic acidosis (accumulation of lactic acid in the blood) can be a serious problem when overdosing and when prescribed to people with contraindications, but otherwise there is no significant risk. Metformin helps reduce LDL cholesterol and triglycerides and is not associated with weight gain. One of the most significant effects of Metformin is a significant reduction in mortality from cardiovascular complications in diabetes mellitus. Included in the list of the most important drugs of the World Health Organization, along with another oral antidiabetic drug glibenclamide.


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There has been a rise in the rate of lifestyle diseases. Some of these diseases include metabolic diseases such diabetes. This is a condition which has such risk factors as genetics and also a poor lifestyle. This includes diets with a lot of calories coupled with lack of exercise and this leads to obesity. There are many types of diabetes and metformin is mainly used for type two diabetes but it has been used in other types of conditions. Metformin is a prescription drug that has various uses but usually used for the treatment of diabetes mellitus type 2.This drug can be used on its own or in combination with other drugs.

Brief history

This drug is in the class of oral anti-diabetic drugs called biguanides. Interest in metformin began a long time ago in the year 1920.It later resumed in 1940 where first, its ingredients were used in the treatment of influenza. During this time, it was found that it had the ability to lower blood sugars. This led to the development of the drug as an antidiabetic drug.

Chemistry of the drug

This drug is composed of 2-cyanoguanidine and dimethylamine hydrochloride. These two compounds are usually added to toluene and then later hydrogen chloride is added. Heating of the compound leads to the formation of a metformin precipitate.


Pharmacokinetics of a drug usually means simply what the body does to a drug. Any drug has to undergo various processes when it enters the body through any route to the body. Usually, metformin is available in an oral form and when taken without food, it has an oral bioavailability of about 50%.Usually, the drug reaches its peak plasma concentrations within around two hours after taking the drug and it has a low plasma protein binding ability. After taking the drug a steady state is likely to be reached after about one day. When metformin is in the non-ionized state, it usually has low solubility in lipids and this means that this drug is not able to penetrate various membranes of the body at a fast rate. Usually, many drugs are usually metabolized in the liver. However, metformin is usually not metabolized and is excreted unchanged in the renal tubules. This drug has been shown to have a life of about 6 hrs.


This term refers to how the drug influences the body or various mechanisms of action. One of the major effects of metformin is to reduce the rate by which the liver produces sugars. In this way, there is the reduction in the glucose levels in the blood. Usually, there is a process which usually takes place in the liver called gluconeogenesis. This process leads to the production of glucose and therefore, its suppression allows for the control of blood sugars. Some of the molecular mechanisms of actions, though not fully understood, have been suggested to be inhibition of the respiratory process of the mitochondria and inhibition of increase of cyclic adenosine monophosphate. Other mechanisms of action suggested include increasing the peripheral sensitivity of insulin. The role of insulin is to increase glucose uptake into the cells and therefore, increasing sensitivity enables for the decrease of glucose in the bloodstream. Metformin also increases the uptake of glucose peripherally by the use of GLUT 4. Another mechanism of action is that there is a reduction in the absorption of glucose from the gastrointestinal tract. Usually, after digestion, glucose is absorbed from the ileum and therefore, inhibition of this process leads to a reduction of sugars in the bloodstream

Therapeutic uses of metformin

There are many uses of metformin and one of the main uses is in the management of diabetes mellitus type 2.This is the condition that this drug was originally prescribed for.

Type 2 diabetes

Metformin is the drug of choice for diabetes mellitus type 2.It has been shown to be effective in controlling the sugar levels. This drug has been shown to be effective in that it has reduced the rate of cardiovascular complications in diabetes mellitus. This is because over a long time diabetes mellitus has been shown to be a very big risk factor for cardiovascular diseases. However, this has reduced with the management of diabetes mellitus with metformin. Metformin has been shown to have low risks of hypoglycemia and also reduces the levels of triglycerides and low-density lipoproteins.

Prediabetic state

Metformin has been shown to be effective in the management of people at high risk of developing diabetes. This one with the combination of exercises and other methods of preventing diabetes like dieting has been shown to reduce the progression to diabetes. According to a research done, there was a lower incidence of diabetes in metformin-treated patients than those who used lifestyle modification alone.

Polycystic ovary syndrome

Polycystic ovary syndrome is a condition which affects women. It is a pathological benign disorder that is characterized by the presence of bilateral ovarian cysts coupled with obesity, hirsutism and abdominal enlargement. This condition has been associated with insulin resistance. Normally, we know that insulin increases glucose uptake into cells. Therefore, as we already know that metformin mechanism of action is to increase insulin sensitivity, it will be able to correct this pathology of insulin resistance in polycystic ovarian syndrome.

Female infertility

Metformin has been shown to be effective in the management of infertility. According to a study that was done it has been shown that combination of clomiphene with metformin was found to be effective in the treatment of infertility in women. The research showed that metformin could be used as second-line medication when clomiphene fails. There is another research which showed that metformin could be used in the treatment because it has very positive effects on the management of anovulation and at the same time it is very effective in the treatment of peripheral insulin resistance, obesity, and also presence of hirsutism in a situation whereby someone is suffering from polycystic ovarian syndrome.

Gestational diabetes

Gestational diabetes is a form of diabetes that affects women during pregnancy and it has to be termed so if the woman was previously having normal sugar levels and usually recovers after some weeks post-delivery. Metformin has been shown to be effective in the management of gestational diabetes and it has been shown to be effective in that the complications of diabetes in pregnancy are reduced or are never there. This includes the complications related to the fetus and also the mother.

Other uses

Metformin has been shown to be effective in that it can be used for the prevention of weight gain. Use of antipsychotic drugs has been shown to be associated with side effects of weight gain. Metformin has been shown to work well in the prevention of weight gain. Such drugs include olanzapine, clozapine and many others. Metformin has also been shown to reduce the requirement of insulin in diabetes mellitus type 1.

Contraindications for Metformin

Metformin has been contraindicated in certain situations. It has been shown to worsen lactic acidosis in people with such conditions as liver disease, lung disease and also kidney disease. Metformin has been shown to have effects when used at the time of doing contrast imaging studies because the contrast may impair kidney function and this might cause lactic acidosis. Therefore, metformin is usually discontinued for some days while doing these studies.

Gastrointestinal effects

Metformin has been shown to have effects on the gastrointestinal system such as developing nausea, vomiting and some diarrhoea. It has been shown to cause some discomfort. Some of the effects have been shown to be worse such as causing malabsorption of vitamin B12.This is bad because it has been shown to affect cell metabolism and also this could lead to the development of megaloblastic anaemia.

Lactic acidosis

This is the most serious side effect because metabolic imbalances could cause serious effects such as convulsions, confusion and poor body function. Therefore, it is very important to monitor for these side effects. Lactic acidosis is usually treated with the use of sodium bicarbonate.


Use of metformin in large doses could lead to some toxic effects. One of the effects includes hypoglycemia. Others include drowsiness which could be as a result of lactic acidosis. The person could also diarrhoea and has abdominal discomfort. Usually, the treatment of metformin toxicity requires just supportive management.

Drug interactions

Cimetidine and cephalexin have been shown to cause increased levels of metformin in blood.

Type 2 Diabetes


Diabetes mellitus is a condition that is characterized by elevated blood sugar levels in the bloodstream due to inadequate insulin secretion or peripheral resistance. There are many types of Diabetes mellitus and in this case, diabetes mellitus type 2 will be discussed in detail. Type 2 diabetes mellitus is mainly due to insulin resistance coupled with a relative dysfunction of beta cells. Diabetes mellitus may lead to complications and therefore, it is important to ensure you prevent and manage diabetes adequately to reduce the rate of complications. Therefore, once the condition is diagnosed, it is important to follow up and also maintain long-term therapy.


The pathogenesis of diabetes type 2 diabetes mellitus is mainly because of peripheral insulin resistance and an inability of the beta cells of the pancreas to produce an adequate amount of insulin. This leads to elevation of glucose in the bloodstream. It has been shown that elevated levels of free fatty acids and inflammatory mediators such as cytokines usually contribute to the insulin resistance. This leads to decreased uptake of glucose into various muscle cells. They also lead to increased rate of production of glucose by the liver cells and also increased catabolism of body fat. There is also a very big role of glucagon when it comes to the pathogenesis of diabetes mellitus type 2.It has been shown that there is also hyperactivity of the alpha cells of the pancreas. These cells usually play a big role in the production of glucagon. This leads to more glucagon and hence more blood sugar levels.

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Usually for a person to develop type 2 diabetes mellitus there has to be peripheral insulin resistance and low levels of insulin in the body. Therefore, for a person to develop diabetes mellitus there is usually inability of a person to sectrete more insulin to cater for the insulin resistance. Therefore, insulin levels can be high in people with diabetes mellitus type 2 but be functionally low due to the level of resistance. When a person has diabetes for a long time, he or she might develop pancreas atrophy.

Beta dysfunction

The pancreas has many types of cells with different roles. It has beta cells which play the role of producing insulin in the body. Development of diabetes has been largely attributed to the inability of these cells to produce enough insulin which plays a very big role in the uptake of glucose into the cells. Therefore, it is important to also focus on this issue when developing therapies or managing type 2 diabetes mellitus.

Peripheral insulin resistance

Insulin resistance has also been shown to play a very big role when it comes to the development and progression of diabetes mellitus. Insulin resistance eventually leads to a higher level of blood glucose levels immediately after feeding. Later on, even fasting sugar levels also increase and this is usually accompanied by failure of gluconeogenesis process in the liver to be suppressed. This is usually accompanied by high level of glucagon. Glucagon leads to further increase in the levels of glucose in the blood. This is how diabetes mellitus develops.

Role of genetics

There has been shown that genetics play a big role in genetics in the pathogenesis of diabetes mellitus. It has been shown that there is usually a familial history of diabetes in people diagnosed with diabetes mellitus.HMGA1 is one of the genes that have been attributed to the development of diabetes mellitus.

Role of amino acids

Amino acids have also been shown to have a role in the pathogenesis of diabetes mellitus. This has been tested by measuring the levels of certain amino acids in the blood and it was shown that people who have diabetes have higher levels of these amines.

Signs and symptoms

It is important to understand the clinical presentation of diabetes mellitus. Some of these include the classic symptoms such as polyuria. Polyuria is mainly due to increase in osmolarity of urine. Therefore, as urine flows through the renal tubules, there is usually reduced reabsorption of water and therefore the urine contains more water and hence it is increased in amount. There is also polydipsia which occurs because there is increased loss of water through urine. Polyphagia which is increased food intake and also weight loss. Patients may also present with blurred vision and also paraesthesia. People with diabetes also are at a risk of developing infections such as urinary tract infections and yeast infections.


Diabetes type 2 is usually diagnosed by checking fasting glucose levels. Random blood sugar levels are also used for screening.


This includes lifestyle management such as exercise and dieting. It is also important to ensure that you control glucose by use of metformin.


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