Pharmacological properties Pharmacodynamics Primobolan ® – a combination oral hypoglycemic means derivative II generation sulfonylureas and bituanida. It has pancreatic and vnepankreaticheskim effects. Glibenclamide belongs to the group of sulfonylureas II generation. It stimulates the secretion of insulin by lowering the threshold for glucose stimulation of beta cells in the pancreas to increase insulin sensitivity and degree of its binding to the target cells that increases insulin release, enhances insulin effect on glucose uptake by muscles and the liver, inhibits lipolysis in adipose tissue. Effective second stage insulin secretion.Metformin relates to biguanide group. It stimulates peripheral tissue sensitivity to insulin action (increases insulin binding to the receptors, enhances the effects. Insulin postreceptor level) reduce the absorption of glucose in the intestine, inhibit gluconeogenesis and has a beneficial effect on lipid metabolism, reduces overweight patients with diabetes mellitus and provides fibrinolytic action by inhibiting plasminogen activator inhibitor of the tissue type. The hypoglycemic effect of the drug develops within 2 hours and lasts 12 hours. The synergistic combination of the two active components of the preparation – the stimulating effect of the sulfonylurea derivative against endogenous insulin (pancreatic effect) and a direct influence biguanide on muscle and adipose tissue (a significant increase in glucose uptake – vnepankreaticheskim impact) and liver tissue (reduced gluconeogenesis), it allows for a certain dose ratio to reduce the content of each component. This helps to avoid over-stimulation of pancreatic beta cells, and therefore reduce the risk of violating its functions, and also provides improvement of safety of drugs and reduction of hypoglycemic incidence of side effects. Pharmacokinetics Glibenclamide quickly and adequately (84%) is absorbed from the gastrointestinal tract (GIT), time to maximum concentration of 2.1 h. The connection to plasma proteins is 97%. Almost completely metabolized in the liver to inactive metabolites. Excreted by the kidneys – 50% in the bile and – 50%. The half-life is from 5 to 10 hours. Metformin adequately absorbed in the gastrointestinal tract, rapidly distributed in the fabric substantially does not bind to plasma proteins. Is not metabolized in the organism, is output unchanged mainly kidneys and partly intestine. The half-life of approximately 7 hours.
Type 2 diabetes (the poor diet, and prior therapy biguanides or sulfonylureas and other oral hypoglycemic agents).
– Hypersensitivity to metformin, glyburide, or other derivatives of sulfonylurea, as well as other components of the preparation;
– type 1 diabetes;
– gestational diabetes;
– diabetic ketoacidosis, diabetic precoma, diabetic coma;
– lactic acidosis (including history );
– state, accompanied by malabsorption of food and the development of hypoglycemia;
– abnormal liver function;
– acute conditions that can lead to changes in kidney function: dehydration, severe infection, shock, intravascular administration of iodinated contrast media;
– renal failure or renal dysfunction (creatinine level above 135 mg / dL for men and greater than 110 mg / dL for women);
– infections, gangrene, major surgery, trauma, acute massive blood loss, extensive burns and other conditions requiring insulin therapy;
– hypoxic conditions ( cardiac or respiratory failure, recent myocardial infarction, shock, severe airway disease);
– a period of 48 hours before and 48 hours after the radioisotope or radiological examinations introduction iodinated contrast agent,
– the period within 48 hours before and 48 hours after surgical intervention;
– degenerative diseases (myotonic dystrophy, lipodystrophy)
– chronic alcoholism, acute alcohol intoxication;
– compliance with a strict low-calorie diet (less than 1000 kcal / day.);
– lack of glucose-6-fosfodegidrogenazy;
– pregnancy, breast-feeding;
-. the age of 18 years
is not recommended to use the drug in patients older than 60 years, performing heavy physical work, which is associated with an increased risk of developing lactic acidosis.
– feverish syndrome;
– thyroid disease (with impaired function);
– hypofunction of the anterior pituitary and / or adrenal cortex;
– hard physical work (risk of lactic acidosis).
Pregnancy and lactation
Use of the drug Primobolan ® during pregnancy and lactation is contraindicated.
Dosing and dose
The dose and dosing regimen and treatment duration set by the attending physician, especially in accordance with the state of carbohydrate metabolism of the patient, depending on the glucose concentration in the blood plasma. Typically, the initial dose is 1-3 tablets per day with the main meals, with gradual dose selection to achieve sustained normalization of plasma glucose concentration. The maximum daily dose – 6 tablets of the drug Primobolan ® .
Possible side effects when using the drug Primobolan ® are listed below in descending frequency of occurrence: often (≥ 1/100, <1/10), uncommon (≥ 1/1000, <1/100), rarely (≥ 1/10000, <1/1000), very rare (<1/10000), including isolated reports. From the digestive system: rare: nausea, vomiting, loss of appetite, abdominal pain, diarrhea, feeling of “metallic” taste; in some cases: increased activity of “liver” enzymes. From the hematopoietic system: Rare: leukopenia, thrombocytopenia, erythropenia; very rarely, agranulocytosis, haemolytic or megaloblastic anemia, pancytopenia. On the part of the central nervous system: Uncommon: headache. For the skin: Rare: urticaria, erythema, pruritus, photosensitivity. On the part of metabolism: rarely: . hypoglycaemia Very rare : lactic acidosis. when lactic acidosis symptoms (vomiting, abdominal pain, weakness, muscle cramps), you must immediately stop taking the drug and seek emergency medical attention. Other: disulfiramopodobnyh reaction while receiving alcohol (the most common symptoms: redness of the skin of the face and the upper half body, headache, nausea and vomiting, palpitations, increased blood pressure).