Glimepiride 3mg tabs 30 pcs vertex

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Glimepiride 3mg tabs 30 pcs vertex

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Description

Composition
Active substance:
Glimepiride – 3.0 mg ;.
Excipients:
Lactose monohydrate – 117.6 mg Microcrystalline cellulose – 18.0 mg Sodium carboxymethyl starch (sodium starch glycolate) – 7.5 mg Povidone K-30 – 1.5 mg polysorbate 80 – 0.9 mg magnesium stearate – 1.5 mg.
Description:
Round Valium tablets white or nearly white, with beveled.
Product form:
Tablets 1 mg, 2 mg, 3 mg, 4 mg and 6 mg. 10, 15, 20 or 30 tablets in blisters of PVC film and aluminum foil. 30 or 60 tablets in a bank of high-density polyethylene. 3 or 6 contour cell packs of 10 tablets, 2 or 4 blisters 15 tablets, 3 blisters with 20 tablets, 1 or 2 blisters of 30 tablets or one bank together with instructions for use in a stack of cardboard.
Contraindications
Diabetes mellitus type 1; diabetic ketoacidosis, diabetic coma and precoma; Hypersensitivity to glimepiride or to any inactive components of the drug to other sulfonylureas or sulfanilamides (risk of hypersensitivity reactions); severe liver function; severe renal impairment, including patients on hemodialysis; pregnancy and lactation; childhood; lactose intolerance; Lactase deficiency; glucose-galactose malabsorption.
The caution in the first week of treatment (increased risk of hypoglycaemia); in the presence of risk factors for hypoglycemia; during intercurrent diseases during treatment or lifestyle changes patients (diets change mealtime, increase or reduction of physical activity); at insufficiency of glucose-6-phosphate dehydrogenase; in disorders of food intake and drugs in the gastrointestinal tract (bowel obstruction, intestinal paresis).
Dosage
3 mg
Indications
Type 2 diabetes mellitus (in monotherapy or in combination therapy with metformin, or insulin).
Interaction with other drugs
Glimepiride is metabolized by cytochrome P450 2C9 (CYP2C9), which should be considered when an application with inducers (e.g. rifampicin), or isozyme inhibitors of CYP2C9 (e.g., fluconazole).
Potentiation of hypoglycemic action and in some cases associated with this possible development of hypoglycemia may occur in combination with one of the following medications: insulin and other oral hypoglycemic agents, inhibitors of angiotensin converting enzyme (ACE) inhibitors, anabolic steroids and male sex hormones, chloramphenicol, coumarin derivatives, cyclophosphamide, disopyramide, fenfluramine, feniramidolom, fibrates, fluoxetine, guanethidine, ifosfamide, mon inhibitors amino-oxidase (MAO), fluconazole, p-aminosalicylic acid, pentoxifylline (high dose parenteral), phenylbutazone, azapropazone, oxyphenbutazone, probenecid, quinolones, salicylates, sulfinpyrazone, clarithromycin, sulfonamides, tetracyclines, tritokvalinom, trofosfamide. Attenuation hypoglycemic action and the resulting increase in the concentration of glucose in blood may be observed in combination with one of the following medications: acetazolamide, barbiturates, corticosteroids, diazoxide, diuretics, epinephrine and other sympathomimetic agents, glucagon, laxatives (with prolonged use) nicotinic acid (high dose), estrogens and progestogens, phenothiazines, phenytoin, rifampin, iodine-containing thyroid hormones.
Blockers H2-histamine receptors, beta-blockers, clonidine and reserpine can both enhance and reduce the hypoglycemic effect of glimepiride.
Under the influence of sympatholytic drugs, beta-blockers, clonidine, guanethidine and reserpine, the signs of adrenergic kontrregulyatsii in response to hypoglycemia may be reduced or absent.
In patients receiving glimepiride may be a strengthening or weakening of the action of coumarin derivatives.
Single or chronic alcohol consumption can both strengthen and weaken the hypoglycemic action of glimepiride.
Colesevelam binds to glimepiride and reduces the absorption of glimepiride from the gastrointestinal tract. In the case of 4 hours glimepiride application at least until the reception colesevelam no interaction was observed. Therefore glimepiride necessary to take at least 4 hours prior to receiving colesevelam.
Overdose
symptoms of overdose
Acute overdose, as well as long-term treatment is too high dose of glimepiride can cause severe threatening hypoglycemia life, accompanied by symptoms such as headache, hunger, nausea, vomiting, tiredness, sleepiness, sleep disturbances, restlessness, aggressiveness, impaired concentration , vigilance and speed of reactions, depression, confusion, speech disorders, aphasia, visual disorders, tremor, paresis, sensory disturbances, dizziness, loss of self-control, eliry, cerebral convulsions, somnolence and loss of consciousness up to coma, shallow breathing, bradycardia. Additionally, in response to hypoglycemia may occur such phenomena adrenergic kontrregulyatsii like appearance cold “sticky” sweat, anxiety, tachycardia, increased blood pressure, angina, heart and sense cardiac arrhythmias.
treatment of overdose
As soon as you found glimepiride overdose, you should immediately inform your doctor. Hypoglycaemia can almost always be quickly cupped immediate intake of carbohydrates (glucose or sugars, sweet fruit juice or tea). In this regard, the patient should always be in possession of at least 20 grams of glucose (sugar 4 slices). Sweeteners are not effective in the treatment of hypoglycemia.
Until such time as the physician determines that the patient is out of danger, the patient requires careful medical supervision. It should be remembered that hypoglycemia can be renewed after the initial recovery of blood glucose concentration.
If a patient with diabetes mellitus treated by different doctors (for example, during a stay in the hospital after the accident, with the disease at the weekend), it should be sure to inform them about the disease and previous treatment.
Sometimes the patient may require hospitalization even if only as a precaution. A considerable overdose and severe reaction with symptoms such as loss of consciousness, or other severe neurological disorder is a medical condition and requires immediate treatment and hospitalization.
In the case of the unconscious state of the patient must be intravenous concentrated dextrose (glucose) (adults, starting from 40 ml of 20% solution). Alternatively adults may intravenous, subcutaneous or intramuscular injection of glucagon in a dose of 0,5-1 mg.
When treating hypoglycaemia due to accidental receiving glimepiride infants or young children the dose administered dextrose should be carefully adjusted in terms of the possibility of dangerous hyperglycemia and administration of dextrose should be under the permanent control of blood glucose concentration.
In overdose glimepiride may require gastric lavage and activated charcoal method.
After rapid recovery of blood glucose concentration must be carefully holding intravenous infusion of dextrose (glucose) at a lower concentration to prevent a recurrence of hypoglycemia. The concentration of glucose in the blood of such patients should be monitored continuously for 24 hours. In severe cases with protracted hypoglycemia hazard to the glucose concentration in the blood to hypoglycemic levels may persist for several days.
pharmachologic effect
Pharmacological group:
Hypoglycemic agent for ingestion group III generation sulfonylureas.
Pharmacodynamics:
Glimepiride lowers blood glucose concentration mainly by stimulating release of insulin from pancreatic beta cells. Its effect is mainly linked to the improvement of the ability of pancreatic beta cells respond to physiological glucose stimulation. Compared with glibenclamide, glimepiride reception in low doses causes the release of a smaller amount of insulin in achieving approximately the same reduction in blood glucose concentration. This fact testifies in favor of a extrapancreatic glimepiride hypoglycemic effects (increased sensitivity to insulin and insulinomimetichesky effect).
insulin secretion
Like all other sulfonylurea, glimepiride regulates insulin secretion by interaction with the ATP-sensitive potassium channels in the membranes of the beta cells. Unlike other sulfonylureas, glimepiride selectively binds to a protein having a molecular weight of 65 kilodaltons (kDa), located in the membranes of the pancreatic beta cells. This interaction with glimepiride binding protein with it regulates the opening or closure of ATP-sensitive potassium channels.
Glimepiride closes potassium channels. This causes a depolarization of the beta cells leads to the opening of voltage-sensitive calcium channels and calcium entry into the cell. As a result, an increase in intracellular calcium concentration activates secretion of insulin by exocytosis.
Glimepiride is much faster and therefore more likely to enter into bond and is released from the connection with the binding protein with him than glibenclamide. It is expected that this high rate of glimepiride exchange property with the binding to the protein it makes him a marked effect sensitization of beta cells to glucose, and their protection from desensitization and premature exhaustion.
The effect of increasing insulin sensitivity
Glimepiride increases the effects of insulin on glucose uptake by peripheral tissues.
Insulinomimetichesky effect
Glimepiride has effects similar to the effects of insulin on glucose uptake by peripheral tissues and glucose output from the liver. Glucose uptake by peripheral tissues is carried out by its transport into the muscle cells and adipocytes. Glimepiride directly increases the amount of glucose transporter molecules in the plasma membranes of adipocytes and muscle cells. Increased glucose Incoming inside cells leads to activation of glycosylphosphatidylinositol-specific phospholipase C. The resulting intracellular calcium concentration is reduced, causing a decrease in the activity of protein kinase A, which in turn leads to stimulation of glucose metabolism.
Glimepiride inhibits glucose output from the liver by increasing the concentration of fructose-2,6-bisphosphate, which inhibits gluconeogenesis.
Effect on platelet aggregation
Glimepiride reduces platelet aggregation in vitro and in vivo. This effect is apparently due to selective inhibition of cyclooxygenase responsible for the formation of thromboxane, an important factor endogenous platelet adhesion.
Anti-atherogenic effects of the drug
Glimepiride helps normalize lipid content, reduces the concentration of malondialdehyde in the blood, which leads to a significant reduction in lipid peroxidation.
In animals, glimepiride leads to a significant reduction in the formation of atherosclerotic plaques.
Reducing the severity of oxidative stress, which is always present in patients with type 2 diabetes. Glimepiride increases the concentration of alpha-tocopherol, catalase, glutathione peroxidase and superoxide dismutase.
Cardiovascular Effects
Through ATP-sensitive potassium channels (see. Above) sulfonylurea derivatives also have an effect on the cardiovascular system. Compared with conventional sulfonylureas, glimepiride has significantly less effect on the cardiovascular system that may be due to the specific nature of its interaction with the protein binding with him the ATP-sensitive potassium channels.
The effect of glimepiride is dose-dependent and reproducible. The physiological response to physical stress (reduced insulin secretion) is stored when receiving glimepiride.
There are no significant differences in effect depending on whether the drug was passed for 30 minutes before a meal or immediately before a meal. Patients with diabetes can be achieved adequate metabolic control over 24 hours after a single dose. In patients with renal failure (creatinine clearance 4-79 ml / min) may also be achieved adequate metabolic control.
Combination therapy with metformin
In patients with inadequate metabolic control in the application of the maximum dose of glimepiride can be started combination therapy with glimepiride and metformin. In two studies during combination therapy has been proven improvement of metabolic control as compared with that in the treatment of each of these drugs alone.
Combination therapy with insulin
In patients with inadequate metabolic control while taking the maximum dose of glimepiride can be started simultaneously with insulin therapy. In combination therapy requires a lower dose of insulin.
Use in children
There is insufficient data on the long-term efficacy and safety in children.
Pharmacokinetics:
Absorption and distribution
Repeated reception of glimepiride in a daily dose of 4 mg maximum concentration (Cmax) of glimepiride plasma levels achieved after about 2.5 hours and is 309 ng / ml. There is a linear relationship between dose and Cmax of glimepiride in blood plasma, as well as between the dose and the area under the curve “concentration – time» (AUC). When receiving glimepiride inside its absolute bioavailability is complete. Food intake has no significant effect on the absorption, with the exception of a slight slowing its speed.
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).
The average half-life is approximately 5-8 hours. Upon receiving high doses shows a modest increase in half-life. No significant accumulation of the drug.
Metabolism and excretion
After a single dose of glimepiride inwardly 58% of the dose excreted by the kidneys and 35% of the dose through the intestine. Glimepiride unchanged in the urine is detected. Urine and feces were detected two metabolites formed as a result of metabolism in the liver (mainly via CYP2C9 isozyme), one of them is hydroxy compound and another carboxy derivative. Upon receiving glimepiride inside the half-life of these metabolites was 3-5 hours and 5-6 hours, respectively.
Glimepiride passes into breast milk and through the placenta.
Pharmacokinetics in special patient groups
The pharmacokinetic parameters are similar in patients of different genders and different age groups. Patients with impaired renal function (low creatinine clearance) there is a tendency to increase clearance glimepiride and to reduce its average concentration in blood plasma, which is likely due to a more rapid clearance of the drug due to its lower binding protein. Thus, in these patients there is no additional risk of accumulation of the drug.
Pregnancy and breast-feeding
Pregnancy
Glimepiride is contraindicated during pregnancy. In the case of planned pregnancy or if pregnancy occurs the woman should be transferred to insulin.
Breastfeeding
It was found that glimepiride passes into breast milk. During the breastfeeding woman should be transferred to insulin or to stop breastfeeding.
Conditions of supply of pharmacies
Prescription.
side effects
Violations by the metabolism and nutrition
As a result, glimepiride hypoglycemic action may develop hypoglycemia, which, like the application of other sulphonylurea derivatives can be prolonged. Symptoms of hypoglycaemia include: headache, hunger, nausea, vomiting, tiredness, sleepiness, sleep disturbances, restlessness, aggressiveness, impaired concentration, alertness and reaction rate, depression, confusion, speech disorders, aphasia, visual disorders, tremor, paresis, sensory disturbances, dizziness, loss of self-control, delirium, cerebral convulsions, somnolence and loss of consciousness up to coma, shallow breathing, bradycardia. Additionally, in response to hypoglycemia may occur such phenomena adrenergic kontrregulyatsii like appearance cold “sticky” sweat, anxiety, tachycardia, increased blood pressure, angina, heart and sense cardiac arrhythmias.
The clinical picture of severe hypoglycemia may be similar to a stroke. The symptoms of hypoglycaemia nearly always disappear after its elimination.
Violations by the organ of vision
During treatment (especially at the beginning) may experience transient visual disturbances caused by changes in blood glucose concentration. Their cause is a temporary change in the swelling of the lens depending on the concentration of glucose in the blood, and thus the change in the refractive index of the lens.
Disorders of the gastrointestinal tract
In rare cases: nausea, vomiting, a feeling of heaviness or fullness in the epigastric pain, abdominal pain, diarrhea. In some cases: Hepatitis, elevated liver enzymes and / or cholestasis and jaundice, which can progress to life-threatening liver failure, but may be subject to regress to remove the drug.
Blood disorders and lymphatic system
Rare: thrombocytopenia. In some cases: leukopenia, hemolytic anemia, erythropenia, granulocytopenia, agranulocytosis and pancytopenia.
Violations by the immune system
In rare cases, and pseudo-allergic reactions such as itching, hives, skin rash. Such reactions are almost always mild, but can go into serious reactions with shortness of breath, a sharp decrease in blood pressure, sometimes progressing up to anaphylactic shock. If you have symptoms of urticaria should immediately consult a doctor. In some cases, you may experience an allergic vasculitis, photosensitivity.
Laboratory and instrumental data
In some cases, may reduce the sodium concentration in the blood plasma.
special instructions
In special clinical stress conditions such as trauma, surgery, infection occurring with febrile temperature, possibly worsening of metabolic control in patients with diabetes, which may require temporary transfer patients on insulin therapy to maintain adequate metabolic control.
In the first weeks of treatment may increase the risk of hypoglycemia, and therefore at this time require particularly careful monitoring of blood glucose concentration. In addition, we recommend regular monitoring of glycosylated hemoglobin.
Factors contributing to the risk of hypoglycemia include:
unwillingness or inability of the patient (most often observed in elderly patients) to cooperate with the doctor; malnutrition, irregular food intake or omissions meal; imbalance between physical activity and carbohydrate intake; changes in diet; the use of alcohol, especially in combination with skipping meals; severe renal impairment; severe liver function abnormalities (in patients with severe hepatic impairment shows transfer to insulin, at least until the metabolic control); overdose of glimepiride; Some decompensated endocrine disorders breaking carbohydrate metabolism or adrenergic kontrregulyatsii in response to hypoglycemia (e.g., some disorders of the thyroid gland and anterior pituitary, adrenal insufficiency); concomitant use of certain drugs (see “Interaction with other drugs.”); receiving glimepiride in the absence of evidence for its reception.
Treatment of sulfonylureas, which include glimepiride may lead to the development of hemolytic anemia, so in patients with deficiency of glucose-6-phosphate dehydrogenase to be particularly careful in the appointment of glimepiride, and better use hypoglycemic agents, non-sulfonylurea.
В случае наличия вышеперечисленных факторов риска развития гипогликемии может потребоваться коррекция дозы глимепирида или всей терапии. Это также относится к возникновению интеркуррентных заболеваний во время лечения или изменению образа жизни пациентов.
Те симптомы гипогликемии, которые отражают адренергическую контррегуляцию организма в ответ на гипогликемию, могут быть слабо выраженными или отсутствовать при постепенном развитии гипогликемии у пациентов пожилого возраста, у пациентов с вегетативной нейропатией или у пациентов, получающих бета-адреноблокаторы, клонидин, резерпин, гуанетидин и другие симпатолитические средства.
Гипогликемия может быть быстро устранена при немедленном приеме быстроусваиваемых углеводов (глюкозы или сахарозы).
Как и при приеме других производных сульфонилмочевины, несмотря на первоначальное успешное купирование гипогликемии, гипогликемия может возобновиться. Поэтому пациенты должны оставаться под постоянным наблюдением.
При тяжелой гипогликемии дополнительно требуется немедленное лечение и наблюдение врача, а в некоторых случаях госпитализация пациента.
During treatment glimepiride requires regular monitoring of liver function and peripheral blood picture (especially the number of leukocytes and platelets).
Поскольку отдельные побочные действия, такие как тяжелая гипогликемия, серьезные изменения картины крови, тяжелые аллергические реакции, печеночная недостаточность, могут при определенных обстоятельствах представлять собой угрозу для жизни, в случае развития нежелательных или тяжелых реакций пациенту необходимо сразу же информировать о них лечащего врача и ни в коем случае не продолжать прием препарата без его рекомендации.
Неправильный прием препарата (например, пропуск приема очередной дозы) никогда не должен восполняться путем последующего приема более высокой дозы. Действия пациента при ошибках при приеме препарата (в частности при пропуске приема очередной дозы или при пропуске приема пищи) или в ситуациях, когда нет возможности принять препарат, должны обговариваться пациентом и врачом заблаговременно.
Effects on ability to drive vehicles and mechanisms
В случае развития гипогликемии или гипергликемии, особенно в начале лечения или после изменения лечения, или когда препарат не принимается регулярно, возможно снижение внимания и скорости психомоторных реакций. Это может нарушить способность пациента управлять транспортными средствами или другими механизмами.
Storage conditions
Хранить в защищенном от света месте при температуре не выше 25 °С.
Keep out of the reach of children.
Dosing and Administration
Inside.
Таблетки глимепирида принимают не разжевывая, запивая достаточным количеством воды (около 0,5 стакана). При необходимости таблетки препарата Глимепирид могут быть разделены вдоль риски на равные части.
Начальная доза и подбор дозы
Как правило, доза глимепирида определяется целевой концентрацией глюкозы в крови. It should apply the lowest amount sufficient to achieve the necessary metabolic control.
Начальная доза глимепирида составляет 1 мг 1 раз в день.
При необходимости суточная доза может быть постепенно увеличена (с интервалами в 1-2 недели). Увеличение дозы рекомендуется проводить под регулярным контролем концентрации глюкозы в крови и в соответствии со следующим шагом повышения дозы: 1 мг – 2 мг – 3 мг – 4 мг – 6 мг ( 8 мг).
Диапазон доз у пациентов с хорошо контролируемым сахарным диабетом
Обычно суточная доза у пациентов с хорошо контролируемым сахарным диабетом составляет 1-4 мг глимепирида. Суточная доза более 6 мг (8 мг) является более эффективной только у небольшого количества пациентов.
Режим дозирования
Время приема препарата Глимепирид и распределение доз в течение дня устанавливается врачом в зависимости от образа жизни пациента в данное время (времени приема пищи, количества физических нагрузок).
Обычно достаточно однократного приема препарата Глимепирид в течение суток. Рекомендуется, чтобы в этом случае вся доза препарата Глимепирид принималась непосредственно перед полноценным завтраком или, в случае если она не была принята в это время, непосредственно перед первым основным приемом пищи.
Очень важно после приема препарата Глимепирид не пропускать прием пищи.
Since the improvement in metabolic control is associated with increased insulin sensitivity, in the course of treatment may decrease the need for glimepiride. Для того чтобы избежать развития гипогликемии, необходимо своевременно снижать дозы или прекращать прием глимепирида.
Состояния, при которых также может потребоваться коррекция дозы глимепирида: снижение массы тела у пациента; изменение образа жизни пациента (изменение диеты, времени приема пищи, количества физических нагрузок); возникновение других факторов, которые приводят к предрасположенности к развитию гипогликемии или гипергликемии (см. раздел «Особые указания»).
duration of treatment
Лечение глимепиридом обычно проводится длительно.
Перевод пациента с приема другого перорального гипогликемического средства на прием препарата Глимепирид
Не существует точного соотношения между дозами глимепирида и других пероральных гипогликемических средств. Когда другое пероральное гипогликемическое средство заменяется на глимепирид, рекомендуется, чтобы процедура его назначения была такой же, как при первоначальном назначении глимепирида, то есть лечение должно начинаться с начальной дозы 1 мг (даже в том случае, если пациента переводят на препарат Глимепирид с максимальной дозы другого перорального гипогликемического средства). Любое повышение дозы следует проводить поэтапно, с учетом реакции на глимепирид, в соответствии с приведенными выше рекомендациями.
Необходимо учитывать силу и продолжительность эффекта предшествующего перорального гипогликемического средства. Может потребоваться прерывание лечения для того, чтобы избежать какой-либо суммации эффектов, которая может увеличить риск развития гипогликемии.
Use in combination with metformin
У пациентов с недостаточно контролируемым сахарным диабетом при приеме максимальных суточных доз или глимепирида, или метформина может быть начато лечение комбинацией этих двух препаратов. При этом проводившееся ранее лечение или глимепиридом, или метформином продолжается в тех же дозах, а дополнительный прием метформина или глимепирида начинают с низкой дозы, которая затем титруется в зависимости от целевого уровня метаболического контроля вплоть до максимальной суточной дозы. Комбинированная терапия должна начинаться под строгим медицинским наблюдением.
Use in combination with insulin
Пациентам с недостаточно контролируемым сахарным диабетом при приеме максимальных суточных доз глимепирида может быть одновременно назначено введение инсулина. В этом случае последняя назначенная пациенту доза глимепирида остается неизменной. При этом лечение инсулином начинается с низких доз, которые постепенно повышаются под контролем концентрации глюкозы в крови. Комбинированное лечение требует тщательного медицинского наблюдения.
Use in patients with renal insufficiency
Имеется ограниченное количество информации по применению препарата Глимепирид у пациентов с почечной недостаточностью. Пациенты с нарушенной функцией почек могут быть более чувствительны к гипогликемическому эффекту глимепирида.
Use in patients with hepatic insufficiency
Имеется ограниченное количество информации по применению препарата Глимепирид при печеночной недостаточности.
Use in children
Данных по применению препарата Глимепирид у детей недостаточно.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist

Additional information

Weight0.100 kg
Manufacturer

VERTEX

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