The substance of the biguanide like metformin

The substance of the biguanide (metformin)
Metformin belongs to the biguanide derivatives and is the only representative of this class of substance use in the current diabetes therapy. Metformin is a synthetic compound with hypoglycemic effect.

Mode of action of metformin
Metformin has several targets that are important for effective blood sugar. Metformin delayed glucose uptake in the intestinal cell and reduces the release of glucose from the liver. The latter leads to an inhibition of the increase in fasting blood glucose. The effect of insulin is enhanced, leading to an increase in glucose uptake and consumption by muscle and fat cells.
Thus, the fasting blood glucose level is reduced on average by 25 percent without hypoglycemia are generated. The HbA1c value indicating the level of blood sugar over the past two to three months can be reduced with metformin on average by 1.5 percent.

Application and dosage
Metformin has been approved for the treatment of diabetes 2 type. The prerequisite for the use of metformin, the pancreas (pancreatic) still produces insulin. This drug has become the first choice for drug therapy in overweight and lean diabetics.
Metformin may be used as a monotherapy or in combination with other oral antidiabetic agents or insulin.

The metformin therapy should be started in a creeping dose. It is recommended to start treatment with 500 mg after dinner and 1 tablet twice and after another four to five days to increase the dose to 1 tablet three times after four to five days. Depending on the metabolism, the dose may be increased within four weeks to the therapeutically meaningful level. The maximum dose is 850 mg of metformin three times each with main meals. Higher doses do not lead to an increase in action and will not be tolerated by the patient because of side effects in the gastrointestinal tract.
Metformin is generally taken after a meal whole with liquid.

Side effects of metformin
At the start of metformin may occasionally side effects such as nausea, stomach pressure, bloating, diarrhea or metallic taste in the mouth may occur. In most cases, these side effects are formed in continuation of metformin spontaneously. In very rare cases, disorders of vitamin B12 metabolism occur, but can be solved by a pharmacological vitamin B12 therapy. In this case, an annual check of blood counts is recommended. In hypersensitive patients, skin redness (erythema) may occur.

The most serious side effect that can occur during treatment with metformin is called lactic acidosis. Under lactic acidosis refers to the acidity in the blood by lactic acid (Laketat). This carries the risk of coma even be fatal, especially if severe comorbidities exist. The symptoms are uncharacteristic early and not very strong. They are similar to side effects that occur early in treatment with metformin in appearance, but can be distinguished from these, since they occur only after a longer symptom-free period of ingestion. Initially appear symptoms such as fatigue and weakness. Occur gastrointestinal discomfort or fever a few days or weeks before the onset of lactic acidosis. Within a few hours there may be a state of unconsciousness accompanied by a rapid and deep breathing, called the respiratory Kussmaul'schen come.

The lactic acidosis is extremely rare and only occurs when the exclusion criteria (contraindications) for treatment with metformin are disregarded. A particular danger involves the presence of renal failure (kidney failure). Among other things, metformin also in chronic alcoholism, in severe infections or systemic diseases, with severe heart failure (congestive heart failure) is contraindicated. Metformin under a semi-annual monitoring of creatinine levels is recommended. The before and after metformin should not be used even with contrast examinations.

Boundaries of the treatment tablets

Type 2 diabetics who are set with hypoglycemic tablets, often make excessive demands on their "sugar pills". They hope by taking optimal blood sugar levels, are but little part motivated to change their lifestyle in terms of their diet and lack of exercise often. The ability of the resulting cardiovascular complications and often severe change in insulin therapy will be ignored by a part of the treated diabetics. It is certainly not easy to drastically change a lifestyle that has become part of for decades. However, these changes contribute to a greatly improved treatment option with reduction of late complications may occur.

Evaluation of drug

Due to the favorable metabolic effects of metformin for type 2 diabetes is the drug of first choice. Metformin no weight gain is observed. It affects the metabolism of fat positive. The risk of hypoglycemia is practically non-existent, since metformin beta cells of the pancreas elicits no insulin. Thus, metformin is considered to be an extremely valuable and safe drug for the treatment of diabetes type second
Since elevated lactate levels represent a potential risk for a severe metabolic derangement, the exclusion criteria (contraindications) must be strictly observed.

Contraindication
Metformin should not be used in patients who suffer from renal impairment or severe liver disease. Also acute conditions that may lead to impairment of renal function (eg, dehydration (dehydration, water loss), severe infection, shock) are among the contraindications. In the event of severe febrile infection or any surgery is imminent, therapy with metformin must be stopped to minimize the risk of severe metabolic decompensation (lactic acidosis) as low as possible. Metformin should be discontinued at least two days before an examination with iodinated contrast media. Treatment may only be resumed if normal renal function was noted. The administration of iodinated X-ray contrast agents may lead to renal function and metformin, which is normally excreted exclusively by the kidney, accumulates in the body. This in turn can lead to lactic acidosis. Dieting, alcoholism or diseases associated with poor oxygenation of the body (heart failure or severe respiratory failure), and a recent myocardial infarction or breast-feeding also provide exclusion criteria dar. If pregnancy known as a strict indication applies. This means that so far have provided no evidence of harm only animal tests, "epidemiological data" are not yet available. For this reason, should be switched to insulin therapy.

Interactions

Concomitant administration of various drugs interactions may occur. There are several possible mechanisms that may lead to drug interactions. Drugs may have a shortened or prolonged duration of action, be faster or slower in their onset, have a stronger or weaker or an unexpected show "new" effect. The number usually increases with the number of drugs taken.

Metformin in combination with other drugs
With the simultaneous intake of glucocorticoids (systemic (eg tablets) or locally (eg creams or ointments), Beta-2-Agonisten/-Symphatomimetika (eg medicines to treat asthma, such as salbutamol) or diuretics may result in a reduction of the blood glucose lowering effect of metformin.
If the same ACE inhibitors, however, can be taken the hypoglycemic effect be enhanced. In these cases, a dose adjustment of metformin is possible and in consultation with the attending physician is required.