Metformin

What is Metformin HCL?

Metformin is commonly prescribed for; Treatment of Type 2 Diabetes

 

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General information:

Metformin 500 mg belongs to the group of medicines called biguanides (a class of oral antidiabetics).It is used for the treatment of type 2 diabetes when diet and physical exercise alone are not sufficient to achieve adequate levels of normal blood sugar in adults, in children from 10 Years of age and adolescents. Insulin is a hormone that allows tissues to pick up glucose (sugar) from the blood for use as energy or to store it for future use.

Patients with type 2 diabetes do not synthesize enough insulin in the pancreas or their body does not respond adequately to the insulin they produce. This causes an increase in blood glucose. Metformin improves the body’s sensitivity to insulin, which helps restore the way the body uses glucose. In overweight adult diabetic patients, long-term use of metformin also helps reduce the risk of complications associated with diabetes.

In adults, 500 mg may be given as a single drug, along with other oral antidiabetics, or with insulin. In children over 10 years of age and adolescents, 500 mg may be given as a single drug or together with insulin.

Mechanism of action:

Metformin is a biguanide with anti hyperglycaemic effect, which decreases postprandial and basal plasma glucose. It does not stimulate insulin secretion and, therefore, does not produce hypoglycemia. It acts by three main mechanisms:

1) In the intestine decreases the absorption of the glucose;

2) In the liver, reducing gluconeogenesis and glycogenolysis;

3) in the muscle increases insulin sensitivity by improving the uptake and utilization of peripheral glucose through the increasing of activity of the enzyme IP3 kinase in the cellular insulin receptor. Regardless of its action on glycaemia, Metformin has favorable effects on lipid metabolism, reducing levels of total cholesterol, LDL and triglycerides. One of the mechanisms of action at the cellular level that have been proposed for it has to do with a unique property.

The drug achieves inhibition of the mitochondrial respiratory chain specifically at the level of complex I without affecting the other stages of the mitochondrial machinery. This unique property of the drug induces a decrease in the oxidation of NADH, pumping protons through the internal mitochondrial membrane and the rate of oxygen uptake. This ultimately leads to the reduction of the proton gradient and ultimately to A reduction in the synthesis of ATP from ADP and phosphate groups.

Pharmacokinetics:

The absolute bioavailability of a 500 mg dose of Metformin under fasting conditions is approximately 50 to 60%. Studies using single oral doses of the drug between 500 and 1,500 mg and between 850 and 2,550 mg indicate that there is a lack of proportionality of bioavailability with increasing doses, which is due to a decrease in absorption rather than an alteration In the elimination. Ingestion of food delay the absorption of Metformin and decrease the maximum concentration (maxC) by approximately 40%, the area under the curve (AUC) decreases by 25% and the time to maxC is prolonged by 35 minutes.

Side effects:

Like all medicines, Metformin 500 mg can have side effects, although not everybody gets them.

The following adverse events were observed in clinical studies or in the routine follow-up of patients. They are presented by frequency groups (very common: at least 1 in 10 patients, at least 1 in 100 patients, rare: at least 1 in 1,000 patients, rare: at least 1 in 10,000, very rare: Less than 1 per 10,000 patients, including isolated cases).

-Very common:

Gastrointestinal disorders: nausea, vomiting, diarrhea, abdominal pain and loss of appetite. These side effects occur more frequently at the start of treatment. They improve if the tablets are taken during or after meals. If symptoms persist, discontinue treatment and consult your doctor.

-Frequent:

Alterations in the sense of taste

-Very rare:

Lactic acidosis: is a very rare but serious complication, especially if your kidneys do not function properly. The symptoms of lactic acidosis are nonspecific such as vomiting, stomach pain (abdominal pain) with cramps, a general feeling of discomfort with intense tiredness and shortness of breath. Additional symptoms may be a decrease in body temperature and heart rate. If you experience any of these symptoms, you should seek immediate medical attention, as a lactic acidosis can lead to coma. Stop taking Metformin immediately and contact your doctor or nearest hospital right away. Skin reactions such as erythema (redness of the skin) and itching or hives (rash with itching) decrease B12 vitamin levels.

-Isolated cases:

Impaired liver function or hepatitis (inflammation of the liver), that can be resolved with discontinuation of treatment.

Storage Mode:

Keep this medicine out of the sight and reach of children. No special storage conditions required