AZULIX Glimepiride 2mg Tablet 100's
RXDRUG-DRP-2324
Discreet Packaging
FDA-registered Products
FDA-licensed Pharmacies
Indications/Uses
Indicated as an adjunct to diet and exercise to lower the blood glucose in patients with non-insulin dependent (Type II) Diabetes Mellitus whose hyperglycemia cannot be controlled by diet and exercise alone.
Dosage/Direction for Use
The starting dose is 1 mg glimepiride per day. If good control is achieved this dosage should be used for maintenance therapy. For the different dosage regimens appropriate strengths are available.
If control is unsatisfactory the dosage should be increased, based on the glycaemic control, in a stepwise manner with an interval of about 1 to 2 weeks between each step, to 2, 3 or 4 mg glimepiride per day.
A dosage of more than 4 mg glimepiride per day gives better results only in exceptional cases. The maximum recommended dose is 6 mg glimepiride per day.
In patients not adequately controlled with the maximum daily dose of metformin, concomitant glimepiride therapy can be initiated.
While maintaining the metformin dose, the glimepiride therapy is started with a low dose, and is then titrated up depending on the desired level of metabolic control up to the maximum daily dose. The combination therapy should be initiated under close medical supervision.
In patients not adequately controlled with the maximum daily dose of Glimepiride, concomitant insulin therapy can be initiated if necessary. While maintaining the glimepiride dose, insulin treatment is started at low dose and titrated up depending on the desired level of metabolic control. The combination therapy should be initiated under close medical supervision.
Normally a single daily dose of glimepiride is sufficient. It is recommended that this dose be taken shortly before or during a substantial breakfast or if none is taken-shortly before or during the first main meal.
If a dose is forgotten, this should not be corrected by increasing the next dose.
Tablets should be swallowed whole with some liquid.
If a patient has a hypoglycaemic reaction on 1 mg glimepiride daily, this indicates that they can be controlled by diet alone.
In the course of treatment, as an improvement in control of diabetes is associated with higher insulin sensitivity, glimepiride requirements may fall.
To avoid hypoglycaemia timely dose reduction or cessation of therapy must therefore be considered. Change in dosage may also be necessary, if there are changes in weight or life style of the patient, or other factors that increase the risk of hypo-or hyperglycaemia.
If control is unsatisfactory the dosage should be increased, based on the glycaemic control, in a stepwise manner with an interval of about 1 to 2 weeks between each step, to 2, 3 or 4 mg glimepiride per day.
A dosage of more than 4 mg glimepiride per day gives better results only in exceptional cases. The maximum recommended dose is 6 mg glimepiride per day.
In patients not adequately controlled with the maximum daily dose of metformin, concomitant glimepiride therapy can be initiated.
While maintaining the metformin dose, the glimepiride therapy is started with a low dose, and is then titrated up depending on the desired level of metabolic control up to the maximum daily dose. The combination therapy should be initiated under close medical supervision.
In patients not adequately controlled with the maximum daily dose of Glimepiride, concomitant insulin therapy can be initiated if necessary. While maintaining the glimepiride dose, insulin treatment is started at low dose and titrated up depending on the desired level of metabolic control. The combination therapy should be initiated under close medical supervision.
Normally a single daily dose of glimepiride is sufficient. It is recommended that this dose be taken shortly before or during a substantial breakfast or if none is taken-shortly before or during the first main meal.
If a dose is forgotten, this should not be corrected by increasing the next dose.
Tablets should be swallowed whole with some liquid.
If a patient has a hypoglycaemic reaction on 1 mg glimepiride daily, this indicates that they can be controlled by diet alone.
In the course of treatment, as an improvement in control of diabetes is associated with higher insulin sensitivity, glimepiride requirements may fall.
To avoid hypoglycaemia timely dose reduction or cessation of therapy must therefore be considered. Change in dosage may also be necessary, if there are changes in weight or life style of the patient, or other factors that increase the risk of hypo-or hyperglycaemia.
Overdosage
After ingestion of an overdosage hypoglycaemia may occur, lasting from 12 to 72 hours, and may recur after an initial recovery. Symptoms may not be present for up to 24 hours after ingestion. In general observation in hospital is recommended. Nausea, vomiting and epigastric pain may occur. The hypoglycaemia may in general be accompanied by neurological symptoms like restlessness, tremor, visual disturbances, co-ordination problems, sleepiness, coma and convulsions.
Treatment primarily consists of preventing absorption by inducing vomiting and then drinking water or lemonade with activated charcoal (adsorbent) and sodium-sulphate (laxative). If large quantities have been ingested, gastric lavage is indicated, followed by activated charcoal and sodium-sulphate.
In case of (severe) overdosage hospitalization in an intensive care department is indicated. Start the administration of glucose as soon as possible, if necessary by a bolus intravenous injection of 50 ml of a 50% solution, followed by an infusion of a 10% solution with strict monitoring of blood glucose. Further treatment should be symptomatic.
In particular when treating hypoglycemia due to accidental intake of Glimepiride in infants and young children, the dose of glucose given must be carefully controlled to avoid the possibility of producing dangerous hyperglycaemia. Blood glucose should be closely monitored.
Treatment primarily consists of preventing absorption by inducing vomiting and then drinking water or lemonade with activated charcoal (adsorbent) and sodium-sulphate (laxative). If large quantities have been ingested, gastric lavage is indicated, followed by activated charcoal and sodium-sulphate.
In case of (severe) overdosage hospitalization in an intensive care department is indicated. Start the administration of glucose as soon as possible, if necessary by a bolus intravenous injection of 50 ml of a 50% solution, followed by an infusion of a 10% solution with strict monitoring of blood glucose. Further treatment should be symptomatic.
In particular when treating hypoglycemia due to accidental intake of Glimepiride in infants and young children, the dose of glucose given must be carefully controlled to avoid the possibility of producing dangerous hyperglycaemia. Blood glucose should be closely monitored.
Administration
Should be taken with food: Take shortly before or during breakfast/main meal. Swallow whole w/ some liqd.
Contraindications
Glimepiride is contraindicated in patients with the following conditions: hypersensitivity to glimepiride, other sulfonylureas or sulfonamides or to any of the excipients; insulin dependent diabetes; diabetic coma; ketoacidosis; severe renal or hepatic function disorders. In case of severe renal or hepatic function disorders, a change over to insulin is required.
Special Precautions
Glimepiride must be taken shortly before or during a meal.
When meals are taken at irregular hours or skipped altogether, treatment with Glimepiride may lead to hypoglycemia. Possible symptoms of hypoglycemia include: headache, ravenous hunger, nausea, vomiting, lassitude, sleepiness, disordered sleep, restlessness, aggressiveness, impaired concentration, alertness and reaction time, depression, confusion, speech and visual disorders, aphasia, tremor, paresis, sensory disturbances, dizziness, helplessness, loss of self-control, delirium, cerebral convulsions, somnolence and loss of consciousness up to and including coma, shallow respiration and bradycardia. In addition, signs of adrenergic counter-regulation may be present such as sweating, clammy skin, anxiety, tachycardia, hypertension, palpitations, angina pectoris and cardiac arrhythmias.
The clinical picture of a severe hypoglycemic attack may resemble that of a stroke.
Symptoms can almost always be promptly controlled by immediate intake carbohydrates (sugar). Artificial sweeteners have no effect. It is known from other sulfonylureas that, despite initially successful countermeasures, hypoglycaemia may recur.
Severe hypoglycemia or prolonged hypoglycaemia, only temporarily controlled by the usual amounts of sugar, require immediate medical treatment and occasionally hospitalization.
Factors favoring hypoglycemia include: unwillingness or (more commonly in older patients) incapacity of the patient to cooperate, undernutrition, irregular mealtimes or missed meals or periods of fasting, alterations in diet, imbalance between physical exertion and carbohydrate intake, consumption of alcohol, especially in combination with skipped meals, impaired renal function, serious liver dysfunction, overdosage with Glimepiride, certain uncompensated disorders of the endocrine system affecting carbohydrate metabolism or counter-regulation of hypoglycaemia (as for example in certain disorders of thyroid function and in anterior pituitary or adrenocortical insufficiency), concurrent administration of certain other medicinal products.
Treatment with Glimepiride requires regular monitoring of glucose levels in blood and urine. In addition determination of the proportion of glycosylated haemoglobin is recommended.
Regular hepatic and haematological monitoring (especially leucocytes and thrombocytes) are required during treatment with Glimepiride. In stress-situations (e.g. accidents, acute operations, infections with fever, etc.) a temporary switch to insulin may be indicated.
No experience has been gained concerning the use of Glimepiride in patients with severe impairment of liver function or dialysis patients. In patients with severe impairment of renal or liver function change over to insulin is indicated.
Treatment of patients with G6PD-deficiency with sulfonylurea agents can lead to hemolytic anemia. Since glimepiride belongs to the class of sulfonylurea agents, caution should be used in patients with G6PD-deficiency and a non-sulfonylurea alternative should be considered.
Glimepiride contains lactose monohydrate. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Effects on ability to drive and use machines: No studies on the effects on the ability to drive and use machines have been performed.
The patient's ability to concentrate and react may be impaired as a result of hypoglycaemia or hyperglycaemia or, for example, as a result of visual impairment. This may constitute a risk in situations where these abilities are of special importance (e.g. driving a car or operating machinery).
Patients should be advised to take precautions to avoid hypoglycaemia while driving. This is particularly important in those who have reduced or absent awareness of the warning symptoms of hypoglycemia or have frequent episodes of hypoglycemia. It should be considered whether it is advisable to drive or operate machinery in these circumstances.
When meals are taken at irregular hours or skipped altogether, treatment with Glimepiride may lead to hypoglycemia. Possible symptoms of hypoglycemia include: headache, ravenous hunger, nausea, vomiting, lassitude, sleepiness, disordered sleep, restlessness, aggressiveness, impaired concentration, alertness and reaction time, depression, confusion, speech and visual disorders, aphasia, tremor, paresis, sensory disturbances, dizziness, helplessness, loss of self-control, delirium, cerebral convulsions, somnolence and loss of consciousness up to and including coma, shallow respiration and bradycardia. In addition, signs of adrenergic counter-regulation may be present such as sweating, clammy skin, anxiety, tachycardia, hypertension, palpitations, angina pectoris and cardiac arrhythmias.
The clinical picture of a severe hypoglycemic attack may resemble that of a stroke.
Symptoms can almost always be promptly controlled by immediate intake carbohydrates (sugar). Artificial sweeteners have no effect. It is known from other sulfonylureas that, despite initially successful countermeasures, hypoglycaemia may recur.
Severe hypoglycemia or prolonged hypoglycaemia, only temporarily controlled by the usual amounts of sugar, require immediate medical treatment and occasionally hospitalization.
Factors favoring hypoglycemia include: unwillingness or (more commonly in older patients) incapacity of the patient to cooperate, undernutrition, irregular mealtimes or missed meals or periods of fasting, alterations in diet, imbalance between physical exertion and carbohydrate intake, consumption of alcohol, especially in combination with skipped meals, impaired renal function, serious liver dysfunction, overdosage with Glimepiride, certain uncompensated disorders of the endocrine system affecting carbohydrate metabolism or counter-regulation of hypoglycaemia (as for example in certain disorders of thyroid function and in anterior pituitary or adrenocortical insufficiency), concurrent administration of certain other medicinal products.
Treatment with Glimepiride requires regular monitoring of glucose levels in blood and urine. In addition determination of the proportion of glycosylated haemoglobin is recommended.
Regular hepatic and haematological monitoring (especially leucocytes and thrombocytes) are required during treatment with Glimepiride. In stress-situations (e.g. accidents, acute operations, infections with fever, etc.) a temporary switch to insulin may be indicated.
No experience has been gained concerning the use of Glimepiride in patients with severe impairment of liver function or dialysis patients. In patients with severe impairment of renal or liver function change over to insulin is indicated.
Treatment of patients with G6PD-deficiency with sulfonylurea agents can lead to hemolytic anemia. Since glimepiride belongs to the class of sulfonylurea agents, caution should be used in patients with G6PD-deficiency and a non-sulfonylurea alternative should be considered.
Glimepiride contains lactose monohydrate. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Effects on ability to drive and use machines: No studies on the effects on the ability to drive and use machines have been performed.
The patient's ability to concentrate and react may be impaired as a result of hypoglycaemia or hyperglycaemia or, for example, as a result of visual impairment. This may constitute a risk in situations where these abilities are of special importance (e.g. driving a car or operating machinery).
Patients should be advised to take precautions to avoid hypoglycaemia while driving. This is particularly important in those who have reduced or absent awareness of the warning symptoms of hypoglycemia or have frequent episodes of hypoglycemia. It should be considered whether it is advisable to drive or operate machinery in these circumstances.
Use In Pregnancy & Lactation
Pregnancy: Risk related to the diabetes: Abnormal blood glucose levels during pregnancy are associated with a higher incidence of congenital abnormalities and perinatal mortality. So the blood glucose level must be closely monitored during pregnancy in order to avoid the teratogenic risk. The use of insulin is required under such circumstances. Patients who consider pregnancy should inform their physician.
Risk related to glimepiride: There are no adequate data from the use of glimepiride in pregnant women. Animal studies have shown reproductive toxicity which likely was related to the pharmacologic action (hypoglycemia) of glimepiride.
Consequently, glimepiride should not be used during the whole pregnancy.
In case of treatment by glimepiride, if the patient plans to become pregnant or if a pregnancy is discovered, the treatment should be switched as soon as possible to insulin therapy.
Breastfeeding: The excretion in human milk is unknown. Glimepiride is excreted in rat milk. As other sulfonylureas are excreted in human milk and because there is a risk of hypoglycaemia in nursing infants, breast-feeding is advised against during treatment with glimepiride.
Risk related to glimepiride: There are no adequate data from the use of glimepiride in pregnant women. Animal studies have shown reproductive toxicity which likely was related to the pharmacologic action (hypoglycemia) of glimepiride.
Consequently, glimepiride should not be used during the whole pregnancy.
In case of treatment by glimepiride, if the patient plans to become pregnant or if a pregnancy is discovered, the treatment should be switched as soon as possible to insulin therapy.
Breastfeeding: The excretion in human milk is unknown. Glimepiride is excreted in rat milk. As other sulfonylureas are excreted in human milk and because there is a risk of hypoglycaemia in nursing infants, breast-feeding is advised against during treatment with glimepiride.
Adverse ReactionsThrombocytopenia, leukopenia, granulocytopenia, agranulocytosis, erythropenia, hemolytic anemia & pancytopenia; hypoglycemia.
Click to view Azulix detailed prescribing informationThe following adverse reactions from clinical investigations were based on experience with Glimepiride and other sulfonylureas, were listed below by system organ class and in order of decreasing incidence (very common: 1/10; common: 1/100 to <1/10; uncommon: 1/1,000 to <1/100; rare: 1/10,000 to <1/1,000; very rare: <1/10,000), not known (cannot be estimated from the available data).
Blood and lymphatic system disorders: Rare: thrombocytopenia, leukopenia, granulocytopenia, agranulocytosis, erythropenia, hemolytic anaemia and pancytopenia, which are in general reversible upon discontinuation of medication.
Immune system disorders: Very rare: leukocytoclastic vasculitis, mild hypersensitivity reactions that may develop into serious reactions with dyspnea, fall in blood pressure and sometimes shock.
Not-known: cross-allergenicity with sulfonylureas, sulfonamides or related substances is possible.
Metabolism and nutrition disorders: Rare: hypoglycemia.
These hypoglycemic reactions mostly occur immediately, may be severe and are not always easy to correct. The occurrence of such reactions depends, as with other hypoglycemic therapies, on individual factors such as dietary habits and dosage.
Eye disorders: Not known: visual disturbances, transient, may occur especially on initiation of treatment, due to changes in blood glucose levels.
Gastrointestinal disorders: Very rare: nausea, vomiting, diarrhea, abdominal distension, abdominal discomfort and abdominal pain, which seldom lead to discontinuation of therapy.
Hepato-biliary disorders: Not known: hepatic enzymes increased. Very rare: hepatic function abnormal (e.g. with cholestasis and jaundice), hepatitis and hepatic failure.
Skin and subcutaneous tissue disorders: Not known: hypersensitivity reactions of the skin may occur as pruritus, rash, urticaria and photosensitivity.
Investigations: Very rare: blood sodium decrease.
Blood and lymphatic system disorders: Rare: thrombocytopenia, leukopenia, granulocytopenia, agranulocytosis, erythropenia, hemolytic anaemia and pancytopenia, which are in general reversible upon discontinuation of medication.
Immune system disorders: Very rare: leukocytoclastic vasculitis, mild hypersensitivity reactions that may develop into serious reactions with dyspnea, fall in blood pressure and sometimes shock.
Not-known: cross-allergenicity with sulfonylureas, sulfonamides or related substances is possible.
Metabolism and nutrition disorders: Rare: hypoglycemia.
These hypoglycemic reactions mostly occur immediately, may be severe and are not always easy to correct. The occurrence of such reactions depends, as with other hypoglycemic therapies, on individual factors such as dietary habits and dosage.
Eye disorders: Not known: visual disturbances, transient, may occur especially on initiation of treatment, due to changes in blood glucose levels.
Gastrointestinal disorders: Very rare: nausea, vomiting, diarrhea, abdominal distension, abdominal discomfort and abdominal pain, which seldom lead to discontinuation of therapy.
Hepato-biliary disorders: Not known: hepatic enzymes increased. Very rare: hepatic function abnormal (e.g. with cholestasis and jaundice), hepatitis and hepatic failure.
Skin and subcutaneous tissue disorders: Not known: hypersensitivity reactions of the skin may occur as pruritus, rash, urticaria and photosensitivity.
Investigations: Very rare: blood sodium decrease.
Drug Interactions
May influence metabolism w/ CYP2C9 inducers (eg, rifampicin) or inhibitors (eg, fluconazole). Increased AUC w/ fluconazole. Potentiation of blood-glucose-lowering effect & hypoglycemia w/ phenylbutazone, azapropazone & oxyfenbutazone; insulin or oral antidiabetics eg, metformin; salicylates & p-aminosalicylic acid; anabolic steroids & male sex hormones; chloramphenicol, certain long-acting sulfonamides, tetracyclines, quinolones & clarithromycin; coumarin anticoagulants; fenfluramine; disopyramide; fibrates; ACE inhibitors; fluoxetine, MAOIs; allopurinol, probenecid, sulfinpyrazone; sympatholytics; cyclophosphamide, trophosphamide & iphosphamides; miconazole, fluconazole; pentoxifylline (high-dose parenteral); tritoqualine. Weakened blood glucose-lowering effect & raised blood glucose levels w/ estrogens & progestogens; saluretics, thiazide diuretics; thyroid stimulating agents, glucocorticoids; phenothiazine derivatives, chlorpromazine; adrenaline & sympathicomimetics; nicotinic acid (high dosages) & nicotinic acid derivatives; laxatives (long-term use); phenytoin, diazoxide; glucagon, barbiturates & rifampicin; acetazolamide. May either potentiate or weaken blood glucose-lowering effect w/ H2-antagonist, β-blockers, clonidine & reserpine; alcohol. Reduced or absent signs of adrenergic counter regulation to hypoglycemia w/ sympatholytic drugs eg, β-blockers, clonidine, guanethidine & reserpine. May either potentiate or weaken effects of coumarin derivatives.
Storage
Store at temperatures not exceeding 30°C.
Action
Pharmacology: Pharmacodynamics: Glimepiride is an orally active hypoglycaemic substance belonging to the sulfonylurea group. It may be used in non-insulin dependent diabetes mellitus.
Glimepiride acts mainly by stimulating insulin release from pancreatic beta cells.
As with other sulfonylureas this effect is based on an increase of responsiveness of the pancreatic beta cells to the physiological glucose stimulus. In addition, glimepiride seems to have pronounced extrapancreatic effects also postulated for other sulfonylureas.
Insulin release: Sulfonylureas regulate insulin secretion by closing the ATP-sensitive potassium channel in the beta cell membrane. Closing the potassium channel induces depolarisation of the beta cell and results by opening of calcium channels-in an increased influx of calcium into the cell. This leads to insulin release through exocytosis.
Glimepiride binds with a high exchange rate to a beta cell membrane protein which is associated with the ATP-sensitive potassium channel but which is different from the usual sulfonylurea binding site.
Extrapancreatic Activity: The extrapancreatic effects are for example an improvement of the sensitivity of the peripheral tissue for insulin and a decrease of the insulin uptake by the liver. The uptake of glucose from blood into peripheral muscle and fat tissues occurs via special transport proteins, located in the cells membrane. The transport of glucose in these tissues is the rate limiting step in the use of glucose. Glimepiride increases very rapidly the number of active glucose transport molecules in the plasma membranes of muscle and fat cells, resulting in stimulated glucose uptake. Glimepiride increases the activity of the glycosyl-phosphatidylinositol-specific phospholipase C which may be correlated with the drug-induced lipogenesis and glycogenesis in isolated fat and muscle cells.
Glimepiride inhibits the glucose production in the liver by increasing the intracellular concentration of fructose-2, 6bisphosphate, which in its turn inhibits the gluconeogenesis.
Glimepiride acts mainly by stimulating insulin release from pancreatic beta cells.
As with other sulfonylureas this effect is based on an increase of responsiveness of the pancreatic beta cells to the physiological glucose stimulus. In addition, glimepiride seems to have pronounced extrapancreatic effects also postulated for other sulfonylureas.
Insulin release: Sulfonylureas regulate insulin secretion by closing the ATP-sensitive potassium channel in the beta cell membrane. Closing the potassium channel induces depolarisation of the beta cell and results by opening of calcium channels-in an increased influx of calcium into the cell. This leads to insulin release through exocytosis.
Glimepiride binds with a high exchange rate to a beta cell membrane protein which is associated with the ATP-sensitive potassium channel but which is different from the usual sulfonylurea binding site.
Extrapancreatic Activity: The extrapancreatic effects are for example an improvement of the sensitivity of the peripheral tissue for insulin and a decrease of the insulin uptake by the liver. The uptake of glucose from blood into peripheral muscle and fat tissues occurs via special transport proteins, located in the cells membrane. The transport of glucose in these tissues is the rate limiting step in the use of glucose. Glimepiride increases very rapidly the number of active glucose transport molecules in the plasma membranes of muscle and fat cells, resulting in stimulated glucose uptake. Glimepiride increases the activity of the glycosyl-phosphatidylinositol-specific phospholipase C which may be correlated with the drug-induced lipogenesis and glycogenesis in isolated fat and muscle cells.
Glimepiride inhibits the glucose production in the liver by increasing the intracellular concentration of fructose-2, 6bisphosphate, which in its turn inhibits the gluconeogenesis.
MedsGo Class
Antidiabetic Agents
Features
Brand
Azulix
Full Details
Dosage Strength
2 mg
Drug Ingredients
- Glimepiride
Drug Packaging
Tablet 100's
Generic Name
Glimepiride
Dosage Form
Tablet
Registration Number
DRP-2324
Drug Classification
Prescription Drug (RX)
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