Glirid

General characteristics. Structure:

Tablets of 2 mg, No. 30

Active agent: Glimepirid of 2 mg

Other ingredients: lactoses monohydrate, sodium krakhmalglikolit (type A), K30 povidone, cellulose microcrystallic, magnesium stearate, ferrous oxide yellow (E172), indigo carmine (E132).

With notches on both sides of a tablet.

Tablets of 4 mg, No. 30

Active agent: Glimepirid of 4 mg

Other ingredients: lactoses monohydrate, sodium krakhmalglikolit (type A), K30 povidone, cellulose microcrystallic, magnesium stearate, indigo carmine (E132).

With notches on both sides of a tablet.

Pharmacological properties:

Pharmacodynamics. Active ingredient of drug Glirid — глимепирид — represents peroral gipoglikemiziruyushchy drug — derivative sulphonylurea. Glirid stimulates insulin secretion with pancreas β-cells, increases insulin release, increases sensitivity of peripheral fabrics to insulin. The maximum effect is reached in 2–3 h and more than 24 p last.

Pharmacokinetics. At intake глимепирид it is completely soaked up irrespective of meal. Cmax in a blood plasma is reached in 2,5 h after reception. Distribution volume low (about 8,8 l), clearance — about 48 ml/min., linkng with proteins of plasma — more than 99%, T½ — about 5-8 h. After administration of drug in high doses of T½ increases.
Glimepirid is metabolized in a liver to hydroxylated derivatives which reveal as in urine (about 58% of a single dose of drug), and in Calais (35–40%). At a single dose of drug and at use within several days of 1 times in days of a significant difference in pharmacokinetics it is not revealed. Drug does not collect. Pharmacokinetic parameters at patients of different age and a floor are similar.
The tendency to increase in clearance of a glimepirid and decrease in its average concentration in a blood plasma at patients with renal failures is observed.

Indications to use:

Non-insulin-dependent diabetes mellitus of the II type if sugar level in blood cannot be supported adequately only by a diet, physical exercises and decrease in body weight.

Route of administration and doses:

Successful treatment of a diabetes mellitus depends on observance by the patient of the corresponding food allowance, regular physical activity, and also constant control of level of glucose in blood and urine. Non-compliance with a diet by the patient is not compensated by reception of tablets or insulin. Drug is used at adults. It is necessary to swallow of tablets without chewing, washing down with liquid.
The dosage depends on the content of glucose in a blood plasma and urine. Usually Glirid apply 1 time a day. Drug is recommended to be accepted shortly before or during a nourishing breakfast or if there is no breakfast, shortly before or during the first main meal. If the next administration of drug was missed, it is not necessary to increase a dose at the following reception.
Monotherapy
The initial dose makes 1 mg of a glimepirid a day. If such dose allows to control adequately sugar level, it is applied as supporting.
If glycemic control is not optimum, the dose should be increased gradually (at an interval of 1–2 weeks) to 2; 3 or 4 mg of a glimepirid a day. If at the patient hypoglycemic reaction at reception of 1 mg of Glirid a day develops, it means that the disease can be controlled only by means of observance of a diet. The dose more than 4 mg/days yields the best results only in some cases. The maximum recommended dose — 6 mg of Glirid a day.
Combination with Metforminum
If the maximum daily dose of Metforminum does not provide sufficient glycemic control, it is possible to begin the accompanying therapy glimepiridy. Adhering to the previous dosing of Metforminum, Glirid's reception should be begun with a low dose (1 mg) which then can be raised gradually to the maximum daily dose, being guided by the desirable level of metabolic control. The combination therapy should be carried out under observation of the doctor.
Combination with insulin
If the maximum daily dose of Glirid does not provide appropriate glycemic control, if necessary it is possible to begin the accompanying therapy with insulin. Adhering to the previous dosing of a glimepirid, treatment by insulin should be begun with the low recommended dose which can be raised gradually, being guided by the desirable level of metabolic control. The combination therapy should be carried out under observation of the doctor.
Improvement of control of diabetes is followed by increase in sensitivity to insulin therefore during therapy the need for a glimepirida can decrease. In order to avoid a hypoglycemia it is necessary to reduce gradually a dose or in general to interrupt therapy. Need for dosing review can also arise if at the patient the body weight or a way of life changes or other factors increasing risk hypo - or a hyperglycemia work.
Transition from peroral hypoglycemic means on Glirid
Glirid it is usually possible to pass with drug to therapy from other peroral hypoglycemic agents. During such transition it is necessary to consider force of action and T½ of the previous means. In certain cases, especially if anti-diabetic drug has long T½ (for example Chlorproramidum), before Glirid's reception it is recommended to wait several days. It will allow to reduce risk of hypoglycemic reactions owing to the additive action of two agents.
The recommended initial dose — 1 mg of a glimepirid a day. The dose can be step by step raised taking into account reaction to drug.
Transition from insulin on Glirid
In exceptional cases by the sick diabetes mellitus of the II type receiving insulin its replacement on Glirid can be shown. Such transition should be carried out only on condition of careful medical control.

Features of use:

The corresponding diet, regular and sufficient physical exercises and if necessary degrowth of a body have the same importance for achievement of optimum level of glucose in blood, as well as regular reception of a glimepirid. Clinical symptoms of insufficient decrease in level of glucose in blood (hyperglycemia) are increase in frequency of urination, strong thirst, dryness in a mouth and a xeroderma.
Glirid it is necessary to accept shortly before or during food. If meal occurs every time at different times or is missed in general, administration of drug can cause a hypoglycemia.
Symptoms can almost always be eliminated quickly if immediately to accept carbohydrates (sugar). Artificial sweeteners will not give any effect.
From experience of use of other derivatives of sulphonylurea it is known that medical actions at first can be successful, but, despite it, symptoms of a hypoglycemia can appear again.
The heavy or long hypoglycemia which can be only temporarily reduced by the use of usual amount of sugar demands immediate drug treatment, and sometimes — hospitalization.
The factors promoting emergence of a hypoglycemia are: unwillingness or (is more often at elderly patients) impossibility to cooperate with the doctor; malnutrition, irregular food or the missed meal, the starvation periods; change of a diet; an imbalance between an exercise stress and consumption of carbohydrates; alcohol intake, especially in combination with passed meal; moderate renal failures and liver; Glirid's overdose; the certain noncompensated frustration of endocrine system influencing metabolism of carbohydrates or reversible regulation of a hypoglycemia (for example dysfunction of a thyroid gland, insufficiency of function of a front share of a hypophysis or bark of adrenal glands), a concomitant use of some medicines.
At treatment by Glirid it is necessary to control constantly glucose level in blood and urine. Besides, it is recommended to control amount of glikozilirovanny hemoglobin.
During use of drug regular control of function of a liver and a blood count is necessary (especially quantities of leukocytes and thrombocytes).
In stressful situations (the accidents, urgentny operations, infections which are followed by fever) temporary transfer of the patient on insulin can be shown.
There are no data on Glirid's use for patients with a heavy abnormal liver function or that to whom dialysis is shown. Patients with a heavy renal or liver failure should be transferred to insulin reception.
It is necessary to consider that symptoms of a hypoglycemia can be hidden or are absent at patients of advanced age with vegetative neuropathy or at those who receive simultaneous treatment by blockers of β-adrenoceptors, Reserpinum, a clonidine, guanetidiny or other sympatholytics. If the effect is insufficient or action is reduced, the combination with metformin or insulin in case of long therapy is recommended.
In case of compensation of a diabetes mellitus sensitivity to insulin in this connection in the course of treatment the need for drug can decrease increases. In order to avoid development of a hypoglycemia it is necessary to lower timely a dose or to cancel drug. Dose adjustment should be carried out also at change of body weight of the patient or his way of life or in case of other factors promoting hypo - or a hyperglycemia.
Patients should not appoint drug with rare hereditary intolerance of a galactose, a lactose intolerance or disturbance of absorption of glucose galactose.
Use during pregnancy or feeding by a breast. Drug is used during pregnancy. If the patient who accepts глимепирид, plans pregnancy or became pregnant, it as soon as possible needs to be transferred to therapy by insulin.
As other derivatives of sulphonylurea reveal in breast milk, it is recommended to stop treatment glimepiridy because of risk of emergence of a hypoglycemia at the newborn.
Children. Drug is used for treatment of children.
Ability to influence speed of response at control of vehicles or other mechanisms. Under the influence of drug at patients such functions as concentration of attention, speed of response can worsen that is result hypo - or a hyperglycemia, and also sight dysfunction. It should be considered to the patients who are engaged in potentially dangerous types of activity requiring special attention and speed of psychomotor reactions.

Side effects:

From blood and lymphatic system: seldom — thrombocytopenia from average to heavy degree, a leukopenia, a granulocytopenia, an agranulocytosis, an erythrocytopenia, hemolitic anemia and a pancytopenia which usually disappear after the treatment termination.
Immune disturbances: very seldom — an allergic vasculitis, hypersensitivity reactions from insignificant to serious with development диспноэ, decrease in the ABP; sometimes — shock. The cross allergy with sulphonylurea, streptocides or related connections is possible.
Metabolism disturbances: seldom — the hypoglycemic reactions arising preferential in an initiation of treatment can get severe forms and not always corrections easily give in (symptoms of a hypoglycemia are given in the section OVERDOSE). Emergence of these reactions depends on subjective factors, such as feeding habits and dosing.
Vision disorders: because of change of level of glucose in blood there can be temporary vision disorders, especially in an initiation of treatment.
From a GIT: very seldom — nausea, vomiting, diarrhea, feeling of pressure or overflow of a stomach, an abdominal pain which can sometimes demand the therapy termination.
From a liver and gall bladder: increase in level of enzymes of a liver can be observed; very seldom — an abnormal liver function (for example a cholestasia and jaundice), hepatitis which can progress to a liver failure.
From skin and hypodermic fabric: hypersensitivity reactions — an itch, rash and urticaria; very seldom — hypersensitivity of skin to light.
Laboratory indicators: seldom — decrease in level of sodium in a blood plasma.

Interaction with other medicines:

The concomitant use of Glirid with certain medicines can cause both easing, and strengthening of hypoglycemic action of a glimepirid. Therefore other drugs should be accepted only from consent (or to destination) the doctor. Glimepirid is metabolized by means of P450 cytochrome (CYP 2C9). It is known that as a result of a concomitant use of inductors (for example rifampicin) or inhibitors (for example a flukonazola) CYP 2C9 this metabolism can change. Flukonazol, one of the strongest CYP 2C9 inhibitors, doubles AUC of a glimepirid approximately.
Strengthen action of a glimepirid at simultaneous use: phenylbutazone, азапропазон, оксифенбутазон, Sulfinpyrazonum, insulin and peroral antidiabetic drugs, some streptocides of long action, metformin, tetracyclines, salicylates and p-aminosalicylic acid, MAO inhibitors, anabolic steroids and male sex hormones, hinolonovy antibiotics, chloramphenicol, пробенецид, indirect anticoagulants, Miconazolum, фенфлюрамин, пентоксифиллин (at parenteral administration of high doses), fibrata, тритоквалин, APF inhibitors, флуконазол, fluoxetine, Allopyrinolum, sympatholytics, cyclophosphamide, isophosphamide, трофосфамид, Disopyramidum, фенирамидол, гуанетидин.
Reduce hypoglycemic effect of a glimepirid at simultaneous use: estrogen and progestogens, saluretics, thiazide diuretics, hormones of a thyroid gland and drugs which stimulate function of a thyroid gland, the corticosteroids derivative a fenotiazina, Chlorpromazinum, Epinephrinum and other sympathomimetics, niacin (high doses) and its derivatives, a glucagon, purgatives (prolonged use), Phenytoinum, diazoxide, barbiturates, rifampicin, acetazoleamide.
Antagonists of H2 receptors, blockers of β-adrenoceptors, can both strengthen a clonidine and Reserpinum, and to weaken hypoglycemic effect. Under the influence of sympatholytics, such as blockers of β-adrenoceptors, a clonidine, гуанетидин and Reserpinum, manifestations of adrenergic return regulation of a hypoglycemia can decrease or disappear. Alcohol intake can strengthen or weaken hypoglycemic action of a glimepirid in an unexpected way.
Glimepirid is capable both to increase, and to reduce influence of derivatives of coumarin.

Contraindications:

Hypersensitivity to a glimepirid or any components of drug, to derivatives of sulphonylurea or other streptocides. Insulin-dependent diabetes mellitus of the I type. Diabetic ketoacidosis, diabetic coma. Heavy renal failures and liver.
In case of a heavy renal failure or a liver it is necessary to transfer the patient to therapy by insulin.

Overdose:

The overdose can lead to a hypoglycemia which lasts from 12 to 72 h and after the first simplification can repeatedly appear. Symptoms can be shown in 24 h after drug absorption. As a rule, such patients have to be in a hospital.
Hypoglycemia symptoms: nausea, vomiting and pain in a stomach, a headache, a tremor, a vision disorder, a lack of coordination, drowsiness, a sleep disorder, concern, aggression, disturbance of concentration of attention and time of reaction, a depression, a disorientation, alalias, aphasia, paresis, sensitivity disturbance, dizziness, helplessness, self-checking loss, a delirium, cerebral spasms, a loss of consciousness up to development of a coma, shallow breathing and bradycardia. Besides, such signs of the return adrenergic regulation as excessive sweating, uneasiness, tachycardia, AG, a heart consciousness, stenocardia and arrhythmia can be observed. The clinical picture of a heavy hypoglycemic attack can remind a stroke.
Treatment. Treatment consists, first of all, in drug absorption preventing. For this purpose it is necessary to cause vomiting, and then to drink water or lemonade with absorbent carbon (adsorbent), use of a purgative is shown. In case of heavy overdose hospitalization in intensive care unit is necessary. As soon as possible it is necessary to begin administration of glucose: if necessary — at first one-time in/in an injection of 50 ml of 50% of solution, and then in/in kapelno 10% solution, constantly controlling glucose level in blood. Symptomatic further treatment.

Storage conditions:

At a temperature up to 25 °C.

Issue conditions:

According to the recipe

Packaging:

Tablets of 1 mg blister, No. 30

Tablets of 2 mg blister, No. 30

Tablets of 3 mg blister, No. 30

Tablets of 4 mg blister, No. 30