Active substanceGlimepirideGlimepiride
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  • Meglimide
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  • Dosage form: & nbsppills
    Composition:


    1 mg

    2 mg

    3 mg

    4 mg

    6 mg

    Active substance:

    MG

    MG

    MG

    MG

    MG

    glimepiride

    1,00

    2,00

    3,00

    4,00

    6 mg

    Auxiliary

    substances:

    Lactose Monohydrate

    138,95

    137,20

    136,95

    135,85

    133,95

    Sodium carboxymethyl starch

    8,00

    8,00

    8,00

    8,00

    8,00

    Cellulose micro-

    crystalline


    20,00


    20,00


    20,00


    20,00


    20,00

    Povidone KZO

    1,00

    1,00

    1,00

    1,00

    1,00

    Magnesium stearate

    1,00

    1,00

    1,00

    1,00

    1,00

    iron dye red oxide (E172);

    0,05





    iron dye oxide yellow (E172);


    0,4

    0,05



    dye indigo carmine (E132)



    0,40


    0,15


    dye sunset sunset yellow (E110);






    0,05

    Description:

    Tablets 1 mg: oblong tablets of light pink color, with a risk on both sides. There is a slight marbling.

    Tablets 2 mg: oblong tablets of light green color, with a risk on both sides. There is a slight marbling.

    Tablets 3 mg: oblong pills of light yellow color, with a risk on both sides. There is a slight marbling.

    Pharmacotherapeutic group:hypoglycemic agent for oral use of the sulfonylurea group of the third generation
    ATX: & nbsp

    A.10.B.B.12   Glimepiride

    Pharmacodynamics:

    Glimepiride is a hypoglycemic preparation for oral use - a derivative of sulfonylureas of a new (third) generation.

    Glimepiride acts mainly by stimulating the secretion and release of insulin from the beta cells of the pancreas (pancreatic action). As with other sulfonylureas, this effect is based on an increase in the response of beta cells of the pancreas to physiological stimulation with glucose, while the amount of secreted insulin is significantly less than that of traditional sulfonylureas. The least stimulating effect of glimepiride on insulin secretion provides a lower risk of hypoglycemia. In addition, glimepiride has an extra-pancreatic action - the ability to improve the sensitivity of peripheral tissues (muscle, fat) to the action of their own insulin, reduce the absorption of insulin by the liver; inhibits the production of glucose in the liver. Glimepiride selectively inhibits cyclooxygenase and reduces the conversion of arachidonic acid to thromboxane A2, which promotes platelet aggregation, thus providing an antithrombotic effect.

    Glimepiride promotes the normalization of lipid content, reduces the level of small aldehyde in the blood,which leads to a significant decrease in lipid peroxidation, this contributes to the anti-atherogenic effect of the drug. Glimepiride increases the level of endogenous alpha-tocopherol, the activity of catalase, glutathione peroxidase and superoxide dismutase, which contributes to the reduction of the oxidative stress in the patient's body, which is constantly present in type 2 diabetes mellitus.

    Pharmacokinetics:With repeated administration of glimepiride in a daily dose of 4 mg, the maximum concentration in the blood serum (Сmах) is reached after about 2.5 hours and is 309 ng / ml; there is a linear relationship between dose and Сmах, as well as between the dose and AUC (area under the curve "concentration - time"). When administered glimepiride, its bioavailability is 100%. Eating does not have a significant effect on absorption, except for a slight slowing of the absorption rate. For glimepiride characterized by a very low volume of distribution (about 8.8 liters) approximately equal to the albumin distribution volume, a high degree of binding to plasma proteins (99%) and low clearance (about 48 ml / min).

    After a single intake of glimepiride dose, 58% are excreted by the kidneys and 35% through the intestine, Unchanged substance in the urine was not detected. The half-life at plasma concentrations of the drug in the serum, corresponding to a multiple dosing regimen, is 5-8 hours. After taking high doses, the elimination half-life increases slightly.

    In urine and feces, two inactive metabolites are identified, most likely formed as a result of metabolism in the liver, one of them is a hydroxy derivative, and the other is a carboxy derivative. After ingestion of glimepiride, the terminal half-life of these metabolites is 3-5 hours and 5-6 hours, respectively.

    Glimepiride is excreted in breast milk and penetrates the placental barrier. The drug does not penetrate the hemato-encephalic barrier poorly.

    In patients with impaired renal function (with low creatinine clearance), there was a tendency to increase the clearance of glimepiride and to reduce its average serum concentrations, which is likely due to a faster elimination of the drug due to its lower binding to the protein.Thus, in this category of patients there is no additional risk of cumulation of the drug.

    Indications:

    The drug is indicated for the treatment of type 2 diabetes with ineffectiveness of a previously prescribed diet and exercise.

    If glomepiride monotherapy is ineffective, its use in combination therapy with metformin or with insulin is possible.

    Contraindications:

    • type 1 diabetes mellitus;
    • diabetic ketoacidosis, diabetic precoma and coma; hypersensitivity to glimepiride or to any inactive component of the drug, to other derivatives of sulfonylureas or to sulfonamide preparations (risk of developing hypersensitivity reactions);
    • severe violations of liver function;
    • severe violations of kidney function (including patients on hemodialysis);
    • pregnancy and lactation
    • hereditary intolerance to galactose, lactase Lalpa deficiency, or glucose-galactose malabsorption.


    Carefully:conditions requiring the transfer to insulin therapy: extensive burns, severe multiple injuries, extensive surgical interventions, impaired absorption of food and drugs in the gastrointestinal tract (incl.intestinal obstruction, paresis of the stomach), febrile syndrome, alcoholism, adrenal insufficiency, thyroid disease (hypothyroidism or thyrotoxicosis).
    Pregnancy and lactation:

    Glimepiride is contraindicated for use in pregnant women. In the case of a planned pregnancy or at the onset of pregnancy, a woman should be transferred to insulin therapy.

    As glimepiride, apparently, penetrates into breast milk, it should not be prescribed to women during lactation. In this case, you need to switch to insulin therapy or stop breastfeeding.

    Dosing and Administration:

    The drug is administered orally. The initial and maintenance doses of Meglimate are determined individually based on the results of regular monitoring of the glucose concentration in the blood.

    Initial dose and dose selection

    At the beginning of treatment, 1 mg of Meglimate is prescribed once a day. When the optimal therapeutic effect is achieved, it is recommended to take this dose as a supporting dose. In the absence of glycemic control, the daily dose should be gradually increased by regular monitoring of blood glucose concentrations (at intervals of 1-2 weeks) to 2 mg, 3 mg or 4 mg per day. Doses over 4 mg per day are effective only in exceptional cases.The maximum recommended daily dose is 6 mg.

    Use in combination with metformin

    In the absence of glycemic control, concomitant therapy with Meglimide may be initiated in patients taking metromorphine. While maintaining the dose of metformin at the same level, treatment with Meglimate begins with a minimal dose, and then the dose gradually increases depending on the desired level glycemic control, up to the maximum daily dose. Combination therapy should be conducted under close medical supervision.

    Use in combination with insulin

    In cases where it is not possible to achieve glycemic control by taking the maximum dose of Meglimide in monotherapy or in combination with the maximum dose of metformin, a combination of Meglimate with insulin is possible. In this case, the last dose of Meglimate prescribed to the patient remains unchanged. In this case, treatment with insulin begins with a minimal dose, with the possible subsequent gradual increase in its dose under the control of the concentration of glucose in the blood. Combined treatment requires compulsory medical supervision.

    Time and frequency of admission The daily dose is determined by the doctor taking into account the lifestyle of the patient. It is usually sufficient assignment daily dose in one step directly before or during breakfast or dense first main meal. Meglymide tablets are taken whole, not liquid, with a sufficient amount of liquid (about 0.5 cup). It is very important not to skip meals after taking Meglimate.

    As a rule, Meglimate treatment can be long.

    Transfer of a patient from another oral hypoglycemic preparation to Meglimate

    When transferring a patient from another oral hypoglycemic drug to a glimepiride the initial daily dose of the latter should be 1 mg (even if the patient is transferred to Meglimate from a maximum dose of another oral hypoglycemic drug). Any increase in the dose of Meglimide should be carried out in stages in accordance with the recommendations given above. It is necessary to take into account the effectiveness, dose and duration of action of the hypoglycemic agent used. In some cases, especially when taking hypoglycemic drugs with a long half-life (for example,chlorpropamide), there may be a need for a temporary (within a few days) cessation of treatment to avoid an additive effect that increases the risk of developing hypoglycemia.

    Transfer of a patient from insulin to Meglimate.

    In exceptional cases, when insulin therapy is performed in patients with type 2 diabetes mellitus, when the disease is compensated and the secretory function of the beta cells of the pancreas is preserved, it is possible to replace insulin with Meglimide. The translation should be carried out under the close supervision of a physician. In this case, the patient's transfer to Meglimate begins with a minimum dose of 1 mg.

    Side effects:

    From the side of metabolism; In rare cases, the development of hypoglycemic reactions (dizziness, headaches, asthenia) is possible. These reactions mainly occur shortly after taking the drug, and they can not always be easily stopped.

    From the side of the organs of sight: during treatment (especially at the beginning), transient visual impairments due to changes in the concentration of glucose in the blood can be observed.

    On the part of the digestive system: sometimes there may be nausea, vomiting,a feeling of heaviness or discomfort in the epigastrium, abdominal pain, diarrhea; very rarely leading to discontinuation of treatment, in rare cases - increased activity of liver enzymes, cholestasis, jaundice, hepatitis (until the development of liver failure).

    On the part of the hematopoiesis system: rarely possible thrombocytopenia (och moderate to severe), leukopenia, hemolytic or aplastic anemia, erythrocytopenia, granulocytopenia, agranulocytosis and pancytopenia.

    Allergic reactions: Sometimes it is possible to develop symptoms of urticaria (pruritus, skin rash.) Such reactions are usually mild, but they can progress, accompanied by a drop in blood pressure, dyspnea, until anaphylactic shock develops. an allergy with other sulfonylurea derivatives, sulfonamides, or the like, it is also possible to develop an allergic vasculitis.

    Other side effects: In exceptional cases, it is possible to develop photosensitization, late cutaneous porphyria, hyponatremia.

    Since some side effects, such as severe hypoglycemia, severe changes in the blood picture, severe allergic reactions, liver failure, can under certain circumstances pose a life threat, if the unwanted or severe reactions develop, the patient should immediately be notified of the treating doctor and do not continue taking the drug without his recommendation.

    Overdose:

    Symptoms: after ingestion of a large dose of glimepiride, the development of hypoglycemia, lasting from 12 to 72 hours, may occur, which may recur after the initial restoration of the glucose concentration in the blood. In most cases, monitoring in a hospital is recommended. Nausea, vomiting and pain in the epigastric region may occur. Hypoglycemia is accompanied by the appearance of neurologic symptoms, such as anxiety, tremor, visual disorders, increased blood pressure (BP), tachycardia, impaired coordination, drowsiness, coma, and seizures.

    Treatment: includes induction of vomiting, a plentiful drink with activated charcoal (adsorbent) and sodium sulfate (laxative).When receiving a large amount of the drug shows gastric lavage, followed by the introduction of activated carbon and sodium sulfate. In case of severe overdose, hospitalization is indicated. As soon as possible, start the injection of dextrose, if necessary in the form of IV infusion of 50 ml of 40% solution, followed by infusion of 10% solution with careful monitoring of blood glucose, 1-2 mg glucagon. In the future, treatment should be symptomatic.

    Interaction:

    The increase in hypoglycemic action and the associated possible development of hypoglycemia can be observed with the simultaneous use of glimepiride with insulin or other oral hypoglycemic drugs, metformin, angiotensin-converting enzyme (ACE) inhibitors, allopurinol, anabolic steroids and male sex hormones, chloramphenicol, coumarin derivatives, cyclo-, tro- and isophosphamide, fenfetramine, fibrates, fluoxetine, sympatholytics (guanethidine), monoamine oxidase (MAO) inhibitors, miconazole, pentoxifylline (with parenteral administration at high doses), phenylbutazone, azapropion,oxyphenbutazone, probenicide, quinolones, salicides and aminosalicylic acid, sulfin-pyrazone, certain long-acting sulfanilamides, tetracyclines, tritqualin.

    The weakening of hypoglycemic action and the associated increase in blood glucose concentration can be observed with the simultaneous use of glimepiride with acetaminophen, barbiturates, glucocorticosteroids, diazoxide, saluretics, thiazide diuretics, epinephrine and other sympathomimetic agents, glucagon, laxatives (with prolonged use), nicotinic acid (in high doses) and nicotinic acid derivatives, estrogens and progestogens, phenothiazines, chlorpromazine, phenytoin , rifampicin, thyroid hormones, lithium salts.

    Blockers of H2 receptors. clonidine and reserpine how can potentiate or weaken the hypoglycaemic action of glimepiride.

    Under the influence of such sympatholytic agents as beta-adrenoceptor blockers, clonidine, guanethidine and reserpine, possibly weakening or lack of clinical signs of hypoglycemia.

    Against the background of taking glimepiride, there may be an increase or decrease in action derivatives of coumarin.

    When used simultaneously with drugs, oppressing bone marrow hematopoiesis, the risk of myelosuppression increases.

    Single or chronic use alcohol can both enhance and weaken the hypoglycemic effect of glimepiride.

    Special instructions:

    Meglimate should be taken at recommended doses and at the appointed time. Errors in the use of the drug, for example, admission, can never be eliminated by the subsequent administration of a higher dose. The doctor and the patient should discuss in advance the measures that should be taken in case of such mistakes (for example, skipping a drug or eating a meal) or in situations when it is not possible to take a regular dose of the drug at the set time. The patient should immediately inform the doctor if too high a dose is taken.

    If the patient develops a hypoglycemic reaction with taking 1 mg of glimepiride per day, this indicates that in this patient the normalization of the blood glucose level can be achieved with a single diet.

    At achievement of indemnification of a diabetes of type 2 sensitivity to an insulin raises. In this regard, the treatment process may reduce the need for glimepiride. To avoid the development of hypoglycemia, it is necessary to temporarily reduce the dose or cancel glimepiride, Dose correction should also be carried out when the patient's body weight changes, if his lifestyle changes, or if other factors contribute to an increased risk of developing hypo- or hyperglycemia.

    Adequate diet, regular and sufficient physical exercise and, if necessary, weight loss are just as important for achieving optimal control of blood glucose levels, as is the regular intake of glimepiride. Clinical symptoms hyperglycemia (insufficient reduction in blood glucose) are: increased frequency of urination, severe thirst, dry mouth and dry skin.

    In the first weeks of treatment, the risk of developing hypoglycemia may increase, which requires particularly careful monitoring of the patient. On the background of treatment with glimepiride with irregular intake of food or skipping meals can develop hypoglycemia. Its possible symptoms are: headache, hunger, nausea, vomiting, tiredness, sleepiness, sleep disturbances, restlessness, aggressiveness, impaired concentration, attention and reaction, depression, confusion, speech and visual disorders, aphasia, tremor, paresis, sensory disturbances,

    dizziness, helpless state, the loss of self-control, delirium, cerebral convulsions, confusion or loss of consciousness including coma, shallow breathing, bradycardia. In addition, as a result of the adrenergic feedback mechanism, symptoms such as cold, sticky sweat, anxiety, tachycardia, increased blood pressure, angina and heart rhythm disturbances can occur.

    Factors contributing to the development of hypoglycemia include:

    • reluctance or (especially in old age) the patient's inadequate ability to cooperate with a doctor;

    • inadequate, irregular meals, skipping meals, starvation, changes in the habitual diet;

    • an imbalance between exercise and consumption, carbohydrates;

    • alcohol consumption, especially when combined with a skipping meal;

    • impaired renal function;

    • severe liver dysfunction;

    • an overdose of glimepiride;

    • Some uncompensated diseases of the endocrine system affecting the carbohydrate metabolism (for example, thyroid dysfunction, pituitary insufficiency or adrenocortical insufficiency);

    • simultaneous use of some other medicines (see section "Interaction with other drugs").

    The doctor should be informed of the above factors and episodes of hypoglycemia, because they require very strict monitoring of the patient. In the presence of such factors that increase the risk of hypoglycemia, the dose of glimepiride or the entire treatment regimen should be adjusted. This must also be done in the case of an intercurrent disease or a change in the patient's lifestyle. Symptoms of hypoglycemia can be smoothened or completely absent in elderly patients, in patients suffering from autonomic neuropathy or receiving simultaneous treatment padrenoblockers, clonidine, reserpine, guanethidine, or other immunopathy.Hypoglycemia can almost always be quickly stopped by the immediate intake of carbohydrates (glucose or sugar, for example, in the form of a piece of sugar, sweet fruit juice or tea). In this regard, the patient should always have at least 20 grams of glucose (4 pieces of sugar). Sugary substitutes are ineffective in the treatment of hypoglycemia.

    From experience with other sulfonylureas, it is known that, despite the initial success of stopping hypoglycemia, it is possible to relapse. In this regard, continuous and careful monitoring of the patient is necessary. Severe hypoglycemia requires immediate treatment under the supervision of a doctor, and under certain circumstances and hospitalization of the patient.

    If a patient suffering from diabetes mellitus is treated by different doctors (for example, during a hospital stay after an accident, during a weekend illness), he must necessarily inform them about his illness and about the previous treatment.

    During treatment with glimepiride, regular monitoring of liver function and peripheral blood pattern (especially the number of leukocytes and platelets) is required.

    In stressful situations (for example, with trauma, surgical intervention, infectious diseases accompanied by fever), it may be necessary to transfer the patient to insulin therapy in a timely manner.

    There is no experience with glimepiride in patients with severe impairment of liver and kidney function or patients on hemodialysis. Patients with severe "impaired renal and hepatic function are indicated by a transfer to insulin therapy." During treatment with glimepiride, regular monitoring of blood glucose concentration as well as the concentration of glycosylated hemoglobin is necessary.

    At the beginning of treatment, when switching from one drug to another, or with an irregular intake of glimepiride, there may be a hypoglycemic or hyperglycemia-induced decrease in the concentration of attention and speed of the patient's psychomotor reactions. This can adversely affect the ability to drive vehicles or to manage various machines and mechanisms.

    Meglimate 6 mg tablets contain a sunny yellow sunset dye (E110), which can cause allergic reactions.

    Meglimate contains lactose, therefore the drug is not recommended for patients with hereditary intolerance to galactose and with lactase deficiency of Lappa or glucose-galactose malabsorption.

    Form release / dosage:Tablets 1 mg, 2 mg, 3 mg, 4 mg and 6 mg.
    Packaging:

    10 tablets in a blister pack. For 1, 3, 6, 9 or 12 blisters in a cardboard pack together with instructions for use.

    Storage conditions:

    Store at a temperature not exceeding 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    Tablets 1 mg - 2 years.

    Tablets 2 mg, 3 mg, 4 mg, 6 mg - 3 years

    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-007097/08
    Date of registration:05.09.2008 / 25.06.2013
    Date of cancellation:2018-02-06
    The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO
    Manufacturer: & nbsp
    Representation: & nbspKRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO
    Information update date: & nbsp06.02.2018
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