Oltar

Oltar is an effective antidiabetic drug, which is prescribed for diabetes mellitus.

Indications of the oltar

It is used for type 2 diabetes mellitus, in situations when the presence of physical exertion, weight reduction and strict adherence to the prescribed diet does not give the desired result.

[1]

Release form

The release is carried out in tablets, 30 pieces each inside a blister pack. In the box - 1 blister with tablets.

There are dosage forms with a volume of 1, 2 and 3 mg tablets.

Pharmacodynamics

The substance glimepiride effectively reduces the level of sugar. The drug is used for therapy in the insulin-dependent form of diabetes mellitus. The active component acts mainly to stimulate the insulin release from the pancreatic β-cells. This action arises from the increased response of β-cells to physiological stimulation with sugar.

Glimepiride helps in the release of insulin, affecting potassium channels, depending on the elements of ATP (located inside the membrane of β-cells). In addition, the substance has an extrapancreatic effect, increasing the sensitivity of peripheral tissues to insulin, and also reducing the liver's digestibility of insulin.

Pharmacokinetics

After ingestion glimepiride demonstrates full bioavailability. The use of food has little effect on the absorption of the drug - its degree in this case is reduced insignificantly. Peak serum values are noted after 2.5 hours after ingestion of the tablet. Peak indices inside the blood serum linearly correlate with the dosage size of the drug.

Glimepiride has a low index of distribution volume (about 8.8 liters), which is similar to that of albumins. Also, the substance has a high level of protein synthesis (more than 99%) and low clearance (48 ml / minute).

The half-life of blood serum averages about 5-8 hours. After a single dose of drugs, radioactive marks recorded the following radioactivity indices: 58% in urine and 35% in feces. In this case, the unchanged active component was not marked in the urine.

[2]

Dosing and administration

The size of the daily initial portion is 1 mg. If there is no result after taking this dosage, gradually increase the daily dose to 2-4 mg by observing a 1-2 weeks interval. Increase the dose does not follow - this does not increase the drug effect of drugs (although there are isolated cases of increasing the maximum daily dose to 6 mg). All daily dosage should be consumed for 1 reception - along with the main (first) consumption of food. Next, the tablets should be washed with water.

With the development of hypoglycemia after taking 1 mg of the drug, you should cancel its use, leaving as treatment only the appropriate diet

In the course of therapy, a reduction in the amount of glimepiride may be required, due to improved metabolic processes, as well as an increase in tissue sensitivity relative to insulin.

Oltar can be prescribed for monotherapy, and in addition it can be used in combination with metformin or insulin.

[6], [7]

Use of the oltar during pregnancy

There are only limited information on the use of drugs by pregnant women. In connection with this, when planning pregnancy, it is required to transfer the patient as quickly as possible to insulin medicines.

Contraindications

Among the contraindications:

• presence of ketoacidosis;
• ketoacidotic coma;
• diabetes mellitus type 1;
• hepatic or renal diseases in severe degree;
• hypersensitivity to glimepiride and other sulfonylureas;
• intolerance with regard to the auxiliary elements of Oltar.

Side effects of the oltar

Taking the drug may lead to the development of certain side effects:

• reactions from the systemic blood flow: occasionally there is thrombocyto-, leuko-, pancito- or granulocytopenia, and in addition agranulocytosis and hemolytic form of anemia. All these conditions can often be cured;
• immune disorders: there are rare symptoms of hypersensitivity, which manifest in the form of choking, anaphylaxis and a strong lowering of blood pressure. Very rarely, patients develop an allergic form of vasculitis, but also cross-intolerance with respect to sulfonamides and derivatives of sulfonylureas or related drugs;
• disturbance of metabolic processes: occasionally there is hypoglycemia;
• lesions of visual organs: at the initial stage of therapy, the development of curable visual disorders (in connection with fluctuations in glucose indices) is possible;
• symptoms from the gastrointestinal tract: the appearance of nausea, a feeling of overflow in the stomach, vomiting, diarrhea and abdominal pain. With the development of these signs, you should cancel the medicine;
• damage to the organs of the hepatobiliary system: an increase in the activity of liver enzymes. Hepatitis, jaundice, liver failure and cholestasis are noted singly;
• skin reactions: the appearance of urticaria, itching or exanthema. Photosensitivity develops;
• disturbance of electrolyte balance: hyponatremia is observed alone.

[3], [4], [5]

Overdose

The main symptom of glimepiride intoxication is hypoglycemia, which manifests itself in the form of vomiting with nausea, anxiety, weakness or severe hunger, and in addition headaches, hyperhidrosis and tachycardia. In addition, there is a disturbance in sleep with mydriasis, hypertension with tremor, and psychosyndrome of endocrine nature (there are behavioral disorders such as feelings of irritability, aggression and confusion, and also a state of depression and worsening of concentration). There is motor insecurity and a feeling of drowsiness, convulsions arise, and in addition, a coma develops or a nervous effect on the vascular and respiratory system develops. There are also focal signs (diplopia with hemiplegia and aphasia) and primitive automatism (such symptoms as grinding and champing, and at the same time grasping movements).

To eliminate the disorder, you must first remove the medicine from the body: rinse the stomach, induce vomiting, take sodium sulfate with activated charcoal. When hypoglycemia (if there is no loss of consciousness) should take 20 grams of sugar / glucose or fruit juice.

If there was a severe hypoglycemia, at which a loss of consciousness occurred, the catheter should be placed in a vein in an emergency and 20% glucose solution (approximately 40-100 ml) should be injected into the vein. You can also use the method in / m or s / to the introduction - for this glucagon (1-2 ml) is used. After the consciousness is fully restored, it is required to consume carbohydrates orally (in the amount of 20-30 grams) at intervals of 2-3 hours during the next 24-48 hours (this is required to prevent the recurrence). After removal from the hypoglycemic state, follow the patient's glucose values for another 48 hours.

If the state of the absent consciousness remains, it is necessary to continue injecting the patient with glucose (5-10% solution). In the absence of changes in the clinical picture, it is required to look for a different cause of loss of consciousness that is not related to hypoglycemia. At the same time, it is necessary to perform cerebral puffiness therapy (taking dexamethasone with sorbitol) and monitor the patient's condition.

Interactions with other drugs

When the drug is combined with certain other drugs, it is possible to reduce or undesirably increase its hypoglycemic effect. Glimepiride acts on the body with the help of hemoprotein P450 2C9. It has been found that the metabolism of this substance is affected by activators used in combination (such as rifampicin) or inhibitors (such as fluconazole) of the hemoprotein P450 2C9.

Strengthening hypoglycemic effects of Oltar occurs in the case of combination with sulfinpyrazone, and in addition with oxyphenbutazone, azapropase and phenylbutazone. The same effect occurs when combining drugs with oral hypoglycemic drugs, tetracyclines, MAOI, sulfonamides (with prolonged exposure), insulin, PASK and salicylates. In addition, with sex hormones (male) and anabolic agents, antibacterial drugs from the category of quinolone derivatives, as well as probenicides, chloramphenicol, fenfluramine, anticoagulants from a number of coumarins and miconazole with pentoxifylline (high dosages). This list includes ACE inhibitors, fibrates, fluoxetine with tritokvaline, sympatholytics, allopurinol, trophosfamide and cyclophosphamide, as well as fluconazole and ifosfamide.

The weakening of the hypoglycemic effect of drugs occurs in the case of combination with progestogens and estrogens, and in addition thiazide diuretics, saluretic drugs, stimulants of thyroid function, epinephrine and GCS, as well as sympathomimetics and phenothiazine derivatives with chlorpromazine. Also when combined with niacin and its derivatives, phenytoin, laxative drugs (if taken for a long time), glucagon and diazoxide, and in addition to rifampicin, barbiturates and acetazolamide.

Drugs that block β-adrenoreceptors and H2-endings, and clonidine with reserpine are both capable of potentiating and weakening the hypoglycemic effect of the drug. Under the influence of sympatholytic agents (among them clonidine with reserpine, drugs that block β-adrenoreceptors, as well as guanethidine), the effect of compensatory adrenergic effect, which helps to decrease glucose values, may decrease or disappear altogether.

Glimepiride worsens or potentiates the effects of coumarin derivatives.

[8], [9]

Storage conditions

Oltar is required to keep out of reach of young children, under normal conditions for medicines. The temperature is not more than 30 ° C.

Shelf life

Oltar can be used for 2 years from the date of manufacture of the drug.