medicalmeds.eu Medicines Peroral antidiabetic drugs. Глимакс

Глимакс

Producer: LLC Kusum Pharm Ukraine

Code of automatic telephone exchange: A10BB12

Release form: Firm dosage forms. Tablets.

General characteristics. Structure:

Active ingredient: glimepiride;
1 tablet contains a glimepirid of 2 mg, 3 mg or 4 mg.

Excipients (tablets on 2 mg): lactoses monohydrate, sodium krokhmalglikolit (type A), K-30 povidone, cellulose microcrystallic, magnesium stearate, ferrous oxide yellow (Е 172), ferrous oxide red (Е 172).

Excipients (tablets on 3 mg): lactoses monohydrate, sodium krokhmalglikolit (type A), K-30 povidone, cellulose microcrystallic, magnesium stearate.

Excipients (tablets on 4 mg): lactoses monohydrate, sodium krokhmalglikolit (type A), K-30 povidone, cellulose microcrystallic, magnesium stearate; ferrous oxide yellow (Е 172), ferrous oxide red (Е 172).

Pharmacological properties:

Pharmacodynamics. Glimepirid – the peroral gipoglikemiziruyushchy means derivative of sulphonylurea. Stimulates insulin secretion with pancreas β-cells, strengthens insulin release, increases sensitivity of peripheral fabrics to insulin. The maximum effect is reached in 2 – 3 hours and more than 24 hours last.

Pharmacokinetics. At intake глимепирид it is completely soaked up irrespective of meal. The maximum concentration in blood serum is reached in 2,5 hours after reception. Distribution volume low (about 8,8 l), clearance – about 48 ml/min., linkng with proteins of plasma – about 99%. An elimination half-life – about 5-8 hours. After administration of drug in high doses the elimination half-life increases.
Glimepirid is metabolized in a liver to hydroxylic derivatives which are shown as in urine (about 58% of a single dose of drug), and in excrements (35 – 40%). At one-time administration of drug and when using within several days of 1 times in days of a considerable 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 blood serum at patients with disturbances of functions of kidneys is observed.

Indications to use:

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 by adults. It is necessary to swallow of a tablet, without chewing, washing down with liquid.
The dosage depends on the content of glucose in blood serum and urine. Usually Глимакс apply once a day. Drug is recommended to be used shortly before or during a nourishing breakfast or if there is no breakfast, then shortly before or during the first main meal. If the next administration of drug was missed, you should not increase a dose at the following reception.

Monotherapy.
The initial dose makes 1 mg of a glimepirid a day. If such dose gives the chance to adequately control sugar level, it is applied as supporting.
If glycemic control is not optimum, it is necessary to increase a dosage 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 to reception of 1 mg of Glimaks in days is observed, it means that the disease can be controlled only by means of observance of a diet. The dose, is more than 4 mg in days, yields the best results only in some cases. The maximum recommended dose – 6 mg of Glimaks 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 dosage of Metforminum, Glimaks's reception should be begun with a low dose (1 mg) which can be raised then gradually to the maximum daily dose, being guided by the desirable level of metabolic control. The combination therapy should be carried out under fixed observation of the doctor.

Combination with insulin.
If the maximum daily dose of Glimaks does not provide appropriate glycemic control, in case of need it is possible to begin the accompanying therapy with insulin. Adhering to the previous dosage of a glimepirid, treatment by insulin should be begun with the lowest recommended dose which can be raised gradually, being guided by the desirable level of metabolic control. The combination therapy should be carried out under fixed observation of the doctor.
Improvement of controllability of diabetes is followed by increase in sensitivity to insulin therefore, during therapy the need for a glimepirida can decrease. To avoid a hypoglycemia it is necessary to reduce gradually a dose or in general to interrupt therapy. Need for review of a dosage can also arise if at the patient the body weight or a way of life changed, or other factors which increase risk hypo - or a hyperglycemia work.

Transition from peroral hypoglycemic funds for Glimaks®.
It is usually possible to pass to therapy by Glimaks from other peroral hypoglycemic agents. During such transition it is necessary to consider force of action and an elimination half-life of the previous means. In certain cases, especially if anti-diabetic drug has a long elimination half-life (for example, Chlorproramidum), before Glimaks's reception it is recommended to wait several days. It will give the chance 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 increased taking into account reaction to drug.

Transition from insulin to Glimaks®.
In exceptional cases its replacement by Glimaks® can be shown by a sick diabetes mellitus of the II type which accept insulin. Such transition should be carried out only on condition of fixed medical control.

Features of use:

The correct diet, regular physical exercises and, in case of need, degrowth of a body are so significant for achievement of optimum control of level of sugar in blood, as well as regular reception of a glimepirid. Clinical symptoms of insufficient lowering of the level of sugar in blood (hyperglycemia) are increase in frequency of an urination, strong thirst, dryness in a mouth and dry skin.
Глимакс® it is necessary to accept shortly before or during food. If meal occurs every time at different times or in general is missed, administration of drug can cause a hypoglycemia.
Symptoms practically can always be softened quickly if urgently to accept carbohydrates (sugar). Artificial sweeteners will not give any effect.
As a matter of experience uses of other derivatives of sulphonylurea it is known that counter-measures at first can be successful, but, despite it, symptoms of a hypoglycemia can appear again.
The heavy and long hypoglycemia which can be only temporarily weakened by use of usual amount of sugar demands immediate drug treatment, and sometimes – hospitalization.
Factors which promote emergence of a hypoglycemia are: unwillingness or (is more often at patients aged) lack of an opportunity to cooperate with the doctor; malnutrition, irregular food or the missed meal, the starvation periods; change of a diet; an imbalance between physical loadings and reception of carbohydrates; alcohol intake, especially together with passed meal; moderate renal failures and liver; Glimaks's overdose; certain noncompensated frustration of endocrine system which influence metabolism of carbohydrates, or the return regulation of a hypoglycemia (for example, dysfunctions of a thyroid gland, insufficiency of function of a front share of a hypophysis or bark of epinephral glands), a concomitant use of some medicines.
During treatment by Glimaks 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 (for example, in case of accidents, urgentny operations, infections which are followed by fever) temporary convertion of the patient on insulin can be shown.
There are no data concerning Glimaks's use to patients with a heavy abnormal liver function or those to whom dialysis is shown. Patients with a serious renal or liver failure should be transferred to insulin reception.
It is necessary to consider that symptoms of a hypoglycemia can be hidden or be absent at patients of advanced age with vegetative neuropathy or at those who at the same time receive 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 Metforminum or with 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. 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 which promote hypo - or a hyperglycemia.
Patients who have rare hereditary intolerance of a galactose, a lactose intolerance or disturbances of absorption of glucose galactose should not appoint drug.

Ability to influence speed of response at control of motor transport or work with 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 a consequence of dysfunction of sight. It should be considered to the patients who are engaged in potentially dangerous types of activity which require special attention and speed of psychomotor reactions.

Side effects:

- From system of blood: 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.
- From immune system: very seldom – an allergic vasculitis, hypersensitivity reactions from insignificant to serious with development диспноэ, a lowering of arterial pressure, sometimes – shock. The cross allergy with sulphonylurea, sulfonamides or related connections is possible.
- Metabolic disturbances: seldom – hypoglycemic reactions which arise generally 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 a dosage.
- From organs of sight: because of change of level of glucose in blood there can be temporary vision disorders, treatments especially in the beginning.
- From a digestive tract: very seldom – nausea, vomiting, diarrhea, feeling of pressure or overpopulation of a stomach, an abdominal pain which can sometimes lead to the therapy termination.
- From gepatobiliarny system: 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, rashes and urticaria; very seldom – hypersensitivity of skin to light.
- Laboratory indicators: very seldom – decrease in level of sodium in blood serum.

Interaction with other medicines:

The concomitant use of Glimaks with certain medicines can cause both easing, and strengthening of hypoglycemic action of a glimepirid. Therefore other drugs should be accepted only at consent (or to destination) the doctor. Glimepirid is metabolized by means of P450 (CYP2C9) cytochrome. It is known that owing to a concomitant use of inductors (for example, rifampicin) or inhibitors (for example, a flukonazola) CYP2C9 this metabolism can change. Flukonazol, one of the strongest CYP2C9 inhibitors, doubles AUC of a glimepirid approximately.
Strengthen action of a glimepirid at the simultaneous use: phenylbutazone, азапропазон, оксифенбутазон, Sulfinpyrazonum, insulin and peroral anti-diabetic drugs, some sulfonamides of long action, metformin, tetracyclines, salicylates and r-aminosalicylic acid, MAO inhibitors, anabolic steroids and male sex hormones, hinolonovy antibiotics, chloramphenicol, пробенецид, coumarinic anticoagulants, Miconazolum, фенфлурамин, пентоксифиллин (at parenteral administration of high doses), fibrata, тритоквалин, APF inhibitors, флуконазол, fluoxetine, Allopyrinolum, sympatholytics, cyclophosphamide, ифосфамид, 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 and glucocorticoids 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, ß blockers, a clonidine and Reserpinum can both potentiate, and to weaken hypoglycemic effect. Under the influence of sympatholytics, such as ß blockers, 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 component of drug, to derivatives of sulphonylurea or to other sulfonamides. 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.

Drug is not used during pregnancy. If the patient who accepts глимепирид, plans pregnancy or became pregnant, it as soon as possible should be transferred to therapy by insulin.
As other derivatives of sulphonylurea are shown in breast milk, it is recommended to stop treatment glimepiridy because of risk of emergence of a hypoglycemia at the newborn.

Children.
Drug is not used.

Overdose:

The overdose can lead to a hypoglycemia which lasts from 12 to 72 hours and after the first simplification can repeatedly appear. Symptoms can be shown in 24 hours 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, frustration of a dream, concern, aggression, disturbances of concentration of attention and time of reaction, a depression, a disorientation, alalias, aphasia, paresis, sensitivity disturbances, 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 back adrenergic reaction as excessive sweating, uneasiness, tachycardia, arterial hypertension, a heart consciousness, stenocardia and cardiac arrhythmia can be observed. The clinical picture of a heavy hypoglycemic attack can remind a stroke.

Treatment. Treatment consists, first of all, in a drug absorption obstacle. 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: in case of need – at first a one-time internal injection of 50 ml of 50% of solution, and then – intravenously kapelno 10% solution, constantly controlling glucose level in blood. Symptomatic further treatment.