Glukonorm, 2.5mg+400 mg 40 pcs

Gluconorm is a fixed combination of two oral hypoglycemic agents of different pharmacological groups: metformin and glibenclamide.

Metformin belongs to the biguanide group and reduces serum glucose levels by increasing the sensitivity of peripheral tissues to the action of insulin and increasing glucose uptake.

It reduces absorption of carbohydrates in the gastrointestinal tract and inhibits gluconeogenesis in the liver. The drug also has a favorable effect on the lipid profile of the blood, reducing the level of total cholesterol. LDL and triglycerides. It does not cause hypoglycemic reactions.

Glibenclamide belongs to the group of sulfonylurea derivatives of the II generation. It stimulates insulin secretion by reducing the threshold of glucose irritation of pancreatic β-cells, increases insulin sensitivity and the degree of its binding with target cells, increases insulin release, increases the effect of insulin on glucose absorption by muscles and liver, inhibits lipolysis in adipose tissue. Acts in the second stage of insulin secretion.

Pharmacokinetics

Glibenclamide

In oral administration, absorption from the GI tract is 48-84%. Time to reach Cmax is 1-2 hours. Vd – 9-10 liters. The binding to plasma proteins is 95%.

It is almost completely metabolized in the liver with the formation of two inactive metabolites, one of which is excreted by the kidneys and the other by the intestine. T1/2- from 3 to 10-16 h.

Metformin

After oral administration is completely absorbed from the gastrointestinal tract, 20-30% of the dose is found in the feces. Absolute bioavailability is 50 to 60%. When concomitant food intake, absorption of metformin is reduced and delayed. It is rapidly distributed in the tissues, practically does not bind with plasma proteins.

It is very poorly metabolized and excreted by the kidneys. T1/2 is approximately 9-12 hours.

Indications

Type 2 diabetes mellitus in adults:

Active ingredient

Composition

Active substances:

Glibenclamide 2.5 mg;

metformin hydrochloride 400 mg;

Auxiliary substances:

microcrystalline cellulose – 100 mg,

corn starch – 20 mg,

How to take, the dosage

The drug is administered orally, with meals. The dose of the drug is determined by the doctor individually for each patient depending on the blood glucose level.

The usual starting dose is 1 tablet (400 mg/2.5 mg)/day. Every 1-2 weeks after the start of treatment, the dose of the drug is adjusted depending on the blood glucose level. When replacing the previous combined therapy with metformin and glibeclamide, 1-2 tablets are prescribed. Gluconorm depending on the previous dose of each component.

The maximum daily dose is 5 tablets.

Interaction

The hypoglycemic effect of the drug is enhanced by ACE inhibitors (captopril, enalapril), histamine H2-receptor blockers (cimetidine), antifungal agents (miconazole, fluconazole), NSAIDs (phenylbutazone, azapropazone, oxyphenbutazone), fibrates (clofibrate, besafibrate), anti-tuberculosis drugs (etionamide), salicylates, coumarin-type anticoagulants, anabolic steroids, beta-adrenoblockers, MAO inhibitors, long-acting sulfonamides, cyclophosphamide, chloramphenicol, phenfluramine, fluoxetine, guanethidine, pentoxifylline, tetracycline, theophylline, tubule secretion blockers, reserpine, bromocriptine, disopyramide, pyridoxine, other hypoglycemic drugs (acarbose, biguanides, insulin), allopurinol.

. Weaken the effect of barbiturates, GCS, adrenostimulants (epinephrine, clonidine), antiepileptic drugs (phenytoin), “slow” calcium channel blockers, carboanhydrase inhibitors (acetazolamide), thiazide diuretics, chlorthalidone, furosemide, triamterene, asparaginase, baclofen, danazol, diazoxide, isoniazid, morphine, ritodrine, salbutamol, terbutaline, glucagon, rifampicin, iodine-containing thyroid hormones, lithium salts, in high doses – nicotinic acid, chlorpromazine, oral contraceptives and estrogens.

The urine acidifying drugs (ammonium chloride, calcium chloride, ascorbic acid in high doses) increase the effect by reducing the degree of dissociation and increasing reabsorption of glibenclamide.

Ethanol increases the likelihood of lactacidosis.

Metformin decreases Cmax and T1/2 of furosemide by 31% and 42.3%, respectively.

Furosemide increases the Cmax of metformin by 22%.

Nifedipine increases absorption, Cmax slows metformin excretion.

Cationic drugs (amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterene, and vancomycin) that are secreted in tubules compete for tubular transport systems and can increase Cmax of metformin by 60% with long-term therapy.

Contraindications

The drug is not recommended for persons older than 60 years of age who perform heavy physical work, due to the increased risk of lactacidosis in them.

With caution: febrile syndrome, adrenal insufficiency, hypothyroidism, and thyroid dysfunction.

Side effects

Carbohydrate metabolism: hypoglycemia is possible.

Gastrointestinal and liver disorders: rarely – nausea, vomiting, abdominal pain, loss of appetite, “metallic” taste in the mouth; in some cases – cholestatic jaundice, increased activity of liver enzymes, hepatitis.

Hematopoietic system: rarely – leukopenia, thrombocytopenia, erythrocytopenia; very rarely – agranulocytosis, hemolytic or megaloblastic anemia, pancytopenia.

CNS disorders: headache, dizziness, weakness, fatigue; rarely – paresis, sensitivity disorders.

Allergic and immunopathological reactions: rarely – urticaria, erythema, skin itching, increased body temperature, arthralgia, proteinuria.

Dermatological reactions: rarely – photosensitization.

Metabolic reactions: lactacidosis.

Others: acute reaction of intolerance to alcohol after its use, manifested by complications of the circulatory and respiratory organs (disulfiram-like reaction: vomiting, fever in the face and upper trunk, tachycardia, dizziness, headache).

Similarities