Name: Amara (Amaryl)
Pharmacological Effects:
Amari – preparation sulfonylureas, oral hypoglycemic agent. Has primary prolonged effect. The mechanism of action is to stimulate the secretion and release of insulin from beta cells of the pancreas (pancreatic effect). Also increases the sensitivity of fat and muscle tissue to insulin (ekstrapankreatichesky effect). It acts by blocking the cytoplasmic ATP-dependent potassium channel beta-cells of the pancreas. This is accompanied by the opening of calcium channel beta-cell membranes and increase the infiltration of calcium (depolarization).
Active ingredient amara – glimepiride – quick disconnects and connects with the beta-cell proteins, which has a molecular mass of 65 kDa / SURX and is associated with adenosine triphosphoric-dependent potassium channels. From other sulfonylurea derivatives differs in that there is no interaction with the protein beta-cells with a molecular mass of 140 kD/SUR1. This leads to the exocytosis of insulin, and the content of released insulin is much less than the influence of other traditional medicines. Slight amara stimulating effect on the secretion of beta-cells, insulin leads to a lower risk of hypoglycemia.
Amara Ekstrapankreatichesky effect leads to a decrease in insulin resistance, a negligible impact on the cardiovascular system. Has antiagregantnym, antiatherogenic and antioxidant effects.
Increased glucose utilization of fat and muscle tissue is carried out due to the presence in cell membranes of specific transport proteins. With the penetration of glucose-insulin-dependent diabetes in these tissues is restricted at the stage of disposal. Amari rapidly increases the activity of transport proteins, through which glucose is absorbed better. There is also an increase in the number of transport proteins on the background of Amarah. Virtually no blocking effects on ATP-dependent potassium channels of cardiac myocytes. Saved on the possibility of metabolic adaptation of cardiomyocytes to ischemic conditions. Increases the activity of specific glikozil-phosphatidylinositol-phospholipase C, which accounts for observed correlated with the admission amara glikogenez and lipogenesis.
Amari blocking hepatic production of glucose by increasing the content in hepatocytes of fructose-2 ,6-bisfosfata (the latter also inhibits gluconeogenesis).
Against the background of the drug observed blocking secretion of COX and a decrease in the transformation of arachidonic acid to thromboxane A2, thereby decreasing platelet aggregation (antithrombotic effect). Influenced amara observed increase in the concentration of alpha-tocopherol, which is produced endogenously. Also there is increased activity of superoxide dismutase, catalase and glyutationperoksidazy that manifested reduced severity of oxidative reactions in diabetes mellitus.
Indications:
Insulin-dependent diabetes mellitus (type 2) – as monotherapy or in combination with insulin (or metformin).
Dosing:
Amari are inside. Tablets do not chew,? High water about 150 ml. It is important not to forget to eat after dosing.
Starting and maintenance dosage is established physician individually depending on the level of glucose in the blood serum and its excretion in the urine.
First, apply the medication to 1 mg / day, if necessary, you can gradually increase the daily dose of 6 mg. Dose escalation is carried out at intervals of 1-2 weeks according to the scheme: 1 mg/sutki-2 mg/sutki-3 mg/sutki-4 mg/sutki-6 mg / day Amarah. Not exceed the recommended dose amara more than 6 mg / day. Multiplicity and time consumption of the drug is determined by the individual physician, depending on the lifestyle of the patient. Typically, the daily dose prescribed amara 1 time per day during or before the first plentiful meal (breakfast). If the morning dose was not adopted – that during or before the second meal. Prolonged therapy.
Using a combination of Amar metformin. Those patients who are taking metformin, and they have observed the lack of decrease of glucose in the blood serum, you can start receiving additional Amarah. If the daily dosage of metformin does not change, then the therapy Amarillo begin with a dose of 1 mg / day. Subsequently amara dose can be increased to achieve the desired reduction of glucose in the blood serum up to 6 mg / day.
Using a combination of Amar insulin. To stabilize the glucose in the blood serum in cases where the use of monotherapy or combination Amar metformin inefficiently used a combination of insulin with Amarillo. This dose amara left unchanged, but insulin therapy starting with small doses. In the future, may increase insulin. Therapy should be accompanied by monitoring the concentration of glucose in the blood serum. The treatment is performed under the supervision of the treating physician. Scheme insulin-Amari can reduce the need for insulin by about 40%.
Replacing another antidiabetes therapies Amara. Launch treated with 1 mg / day Amarah, in not depending on the dose of previous medication (even if it was maximal). Depending on the therapeutic effect amara can increase the dose of the above rules. In some instances, removal of Amari because of the risk of hypoglycemia (especially if the Amari to use the drug with a high value of the half-life – hlorpropramid). Therapy is stopped for a few days (because of the probable additive effect).
Replacement of insulin in Amarah. In cases where patients with type 2 diabetes insulin is prescribed, but they remained intact insulinsekretiruyuschaya function of beta cells of the pancreas, can be translated to the patient an appointment with amara except insulin. In this case, therapy Amarillo begin with a dose of 1 mg / day.
Side effects:
Metabolism: The Rise of hypoglycemic reactions shortly after receiving Amari (such reactions are very difficult to correct).
Nervous system: headache, sleep disturbances, drowsiness, fatigue, aggressiveness, anxiety, changes in concentration and velocity of the psycho-motor responses, visual and speech disturbances, dizziness, confusion, depression, sensory disturbances, aphasia, disturbances of coordination, paresis, helpless condition, cerebral convulsions, loss of self-control, tremor, loss or confusion, delirium, coma, restlessness, cold, clammy sweat.
Gastrointestinal tract: vomiting, epigastric discomfort, hunger, abdominal pain, diarrhea, jaundice, cholestasis, elevation of liver transaminases, hepatitis, liver failure, nausea.
Cardiovascular system: tachycardia, cardiac arrhythmia, hypertension, bradycardia, angina pectoris.
Organ of: transient visual disturbances due to changes in blood glucose (especially in the beginning of therapy).
The respiratory system: shallow breathing.
Hematopoietic system: leucopenia, thrombocytopenia (moderate or severe), erythropenia, aplastic or hemolytic anemia, granulocytopenia, pancytopenia, agranulocytosis.
Hypersensitivity reactions: urticaria, itching, skin rashes, allergic vasculitis. Allergic reactions are usually slightly expressed, but it is sometimes possible progression up to anaphylactic shock. Perhaps cross-reaction to sulfonylureas, as well as sulfanilamidami.
Other: hyponatremia, photosensitivity.
Contraindications:
• genesis of diabetic ketoacidosis, diabetic coma and prekoma,
• insulin-dependent diabetes mellitus (type 1),
• Expression of renal dysfunction (including patients on hemodialysis),
• severe hepatic impairment,
• Individual hypersensitivity to Amarillo (Glimepiride) or other components of the drug, other means sulfonylureas, sulfonamides.
Pregnancy:
Amari should not be administered to pregnant women and women breast-feeding. If the patient is planning a pregnancy, it must be translated into the introduction of insulin with the exception of Amarah. If the patient is breastfeeding, she continued to insulin or breast-feeding stopped (because Amari passes into breast milk).
Interaction with other drugs:
In combination with insulin, other medication for the treatment of hypoglycemia, allopurinol, inhibitors of angiotensin-converting factor, male sex hormones, anabolic steroids, coumarin derivatives, chloramphenicol, fenfluramine, fluoxetine, fibrates, feniramidolom, MAO inhibitors, guanetidinom, pentoxifylline (with the introduction parenterally in large doses ), miconazole, azapropazonom, phenylbutazone, quinolones, probenecid, oksifenbutazonom, salicylates, sulfinpirazonom, tetracyclines, sulfonamides of prolonged action, tritokvalinom, Tropics, cyclo-, and ifosfamide may increase hypoglycemic effect of Amarah.
In combination with adrenaline (epinephrine) and sympathomimetics, acetazolamide, glucocorticosteroid, glucagon, diazoksidom, barbiturates, saluretics laxatives (prolonged use), thiazide diuretics, nicotinic acid in large doses, phenytoin, phenothiazines, rifampin, progestogens and estrogens, chlorpromazine , thyroid hormone, lithium salts may decrease hypoglycemic effect of Amarah.
In combination with amara reserpine, clonidine and blocking histamine H2-receptors may decrease as well as increased hypoglycemic effect.
May decrease or weakening of the effects of coumarin and its derivatives in conjunction with Amarillo. Prolonged or single use entanolsoderzhaschih drugs and drinks can both weaken and strengthen the hypoglycemic effect of Amarah.
Overdose:
In case of overdose amara possible hypoglycemia within 12-72 hours of admission amara in the high dose. Perhaps the re-development of hypoglycemia after the restoration of glucose in the blood. Hypoglycemia manifested by the following symptoms: high blood pressure, increased sweating, nausea, vomiting, arrhythmia, pain in the heart, anxiety, rapid increase of appetite, lethargy, dizziness, drowsiness, headache, anxiety, palpitations, aggression, violation of concentration, tremor , confusion, paresis, depression, breach of sensitivity, tachycardia, seizures of central origin. In some cases, hypoglycemia is manifested symptoms of stroke. There is a risk of coma. Treatment of hypoglycemia should begin with taking a piece of sugar, sweet tea or juice. The patient was warned that he always had with him approximately 20 g of glucose (in the form of 4 pieces of sugar, for example). In the treatment ineffective are the various sweeteners. In severe cases require hospitalization. By induction of vomiting, the patient spend dehydration (water with activated charcoal inside a laxative). Parenteral dextrose injected (intravenous bolus 40% solution 50 ml). In the future, use diluted dextrose (10% solution). Treatment was escorted to the constant control of glucose in the blood serum. Other indications cropped symptomatic treatment.
In case of accidental admission amara people without diabetes (children) need to avoid the development of hyperglycemia. A dose of dextrose carefully selected on the background monitoring of glucose in the blood serum.
Product:
Amari – tablets are dividing strip, elongated shape. Glimepiride Tablets 1 ml have a pink color. Amari, 2 ml – tablets green. Amari and 3 mg – Tablets light yellow color. Amari to 4 mg – green. In package 2 blisters, each with 15 tablets.
Storage:
Amari is stored at a temperature not exceeding 25 ° C. Shelf life – 3 years.
Ingredients:
Active ingredient: Glimepiride.
Inactive components: lactose monohydrate, polyvidone 25 000, sodium starch glycolate, microcrystalline cellulose, magnesium stearate, dyes (for amara 1 mg – iron oxide red (E172), for amara 2 mg – iron oxide yellow (E172) and indigo (E132) for amara 3 mg – iron oxide yellow (E172), for amara 4 mg – indigo (E132).
Extras:
In the treatment of Amarillo need to remember the states that require the transfer of the patient on parenteral administration of insulin (polytrauma, surgery, illness with fever, extensive burns, modified food absorption from the gastrointestinal tract in diseases – intestinal obstruction, intestinal paresis, etc.) .
In combination Amar metformin should be borne in mind that taking high doses of metformin and glimepiride sovrovozhdaetsya marked improvement in metabolism in patients with uncontrolled diabetes type. In the case of high doses of metformin and Amara, if the control still inadequate, it is possible to transfer the patient to a combination of Amar insulin.
Factors that encourage the development of hypoglycemia: low komplaentnost patient, inadequate, irregular meals, habitual diet changes, omissions, eating, drinking, fasting, changing the balance between carbohydrate intake and physical activity, severe dysfunction of the liver and kidneys; related uncompensated endocrine diseases , an overdose of Amara, thyroid gland, adrenal insufficiency, pituitary insufficiency, the combination with other drugs.
Signs of hypoglycemia are offset in the elderly, patients with neurocirculatory dystonia, patients who take beta-blockers, reserpine, clonidine, guanetidin, simpatolitiki.
Dose is adjusted individually depending on the content of glucose in the blood. If another dose is missed, absolutely not supposed to accept the next higher dose. Patient should inform your doctor about receiving too high doses of Amarah. In the case of compensation of diabetes may begin to improve sensitivity to insulin, thus possibly reducing the dose Amari (or even cancellation of the drug). Need to adjust the dose amara the appearance of various factors that may provoke hypoglycemia or hyperglycemia, as well as in the case of change of lifestyle. It must be remembered that the right diet, correction of physical activity, weight loss are of great importance for the treatment of diabetes while taking Amarah.
Should inform the patient that he immediately informed the doctor all the side effects that develop on a background therapy of Amarillo. It is also necessary to inform him about the factors that cause both hyper-and hypoglycemia and the symptoms of these conditions.
Therapy of Amarillo should be accompanied by regular monitoring of glucose in the blood serum, urine, determination of glycated hemoglobin concentration. Regular monitoring of these laboratory parameters in time helps to identify possible resistance to the drug of primary or secondary nature.
In the laboratory control includes the determination of liver function, complete blood count. Against the background of drug therapy may decrease the rate of psycho-motor reactions, and therefore work with the precise mechanisms and driving contraindicated. Especially concerns the initial stages of treatment Amarillo.
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Warning
Before using the product Amari, you should consult your doctor. This instruction is given a free transfer and is intended solely for review. For more information, please contact the manufacturer annotations.
