In the sixties of the twentieth century, biochemists have determined the basic concept of type 2 diabetes mechanism development – obesity accompanied with insulin resistance, which in turn causes hyperinsulinemia, and as a result which leads to absolute insulin deficiency and hyperglycemia.
Insulin resistance in muscle, fat tissues, and liver cells is a genetically determined main component of type 2 diabetes origin, which is closely associated with pathological conditions such as displidemie, obesity, and hypertension.
In clinical practice for more than half a century for type 2 diabetes treatment, it is used biguanide class – Glucophage (HCL Metformin). Preparation pharmacological effect is produced in the form of round, biconvex film-coated white tablets.
Each tablet contains the active ingredient – hydrochloride metformin (500, 850, 1000 mg) and auxiliary elements are:
- magnesium stearate;
- hypromellose;
- povidone.
Metformin is an active substance which has a strong hypoglycemic property developing only under hypoglycemic conditions, that is, in people with normal blood glucose level. The substance does not have a hypoglycemic action.
The action mechanism of Glucophage is based on the ability to inhibit glycogenolysis and gluconeogenesis, reduce gastrointestinal tract glucose absorption and increase sensitivity to insulin. The preparation contributes to the effective decrease of glucose production in the liver, reduces its concentration in blood plasma and stimulates glucose utilization in muscles.
Metformin except expressed antihyperglycemic action has the effect of improving lipid metabolism, reducing cholesterol, triglycerides and lipoproteins level. It is also able properly to reduce and stabilize weight, so experts sometimes prescribe Glucophage for weight loss. The drug is absorbed into the gastrointestinal tract, peak plasma concentration is achieved 2-2.5 hours after dosing.
Metformin maximum concentration in plasma in case of Glucophage Long lasts 7 hours. This drug property is used to reduce the potential side effects. If ingestion is applied absolute bioavailability counts for 50-60%. The substance is not practically metabolized and excreted by the kidneys predominantly, only a small percentage -by intestines. There are reviews of Glucophage, confirming its ability to reduce appetite.
Indications and Contraindications for Use
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Instructions for use recommend this drug for patients suffering from type 2 diabetes, on expressed accompanying obesity background. Glucophage and Glucophage Long can be used as monotherapy, or in combination with insulin or other hypoglycemic agents.
Canadian Pharmacy reported that this drug can be administered to adults and children over 10 years old. Numerous reviews of Glucophage demonstrate its tolerability, however, but this drug has a list of specific contraindications.
The remedy should not be prescribed for people with hypersensitivity to drug components as treatment of diabetic ketoacidosis or diabetic coma. Instructions for use prohibit this drug in case of a renal function, and in the case of severe conditions, which may be accompanied by such violations, including:
- shock;
- infectious diseases;
- dehydration.
The drug should not be used in the following cases :
- an abnormal liver function;
- a respiratory or heart failures;
- diseases which are accompanied by hypoxia;
- myocardial infarction;
- reduced-calorie diet;
- chronic alcoholism or acute alcohol poisoning.