Glimepiride STELLA

Glimepiride STELLA


Nhà sản xuất:

Stellapharm J.V.

Nhà phân phối:

Khuong Duy
Thông tin kê toa chi tiết tiếng Anh
Active ingredient: Glimepiride 2 mg or 4 mg.
The tablet can be divided into equal doses.
Excipients/Inactive Ingredients: Lactose monohydrate, microcrystalline cellulose, povidone K30, sodium lauryl sulfate, croscarmellose sodium, magnesium stearate, indigo carmine lake.
Pharmacotherapeutic Group: Blood glucose lowering drugs, excl. insulins: sulfonamides, urea derivatives. ATC Code: A10BB12.
Pharmacology: Pharmacodynamics: 2 mg: Glimepiride is an anti-diabetic type 2 (noninsulin-dependent) agent belonging to the sulfonylurea group. Glimepiride acts mainly by stimulating insulin release from pancreatic beta cells, so the drug is effective only when the pancreas still works (also capable of releasing insulin). The mechanism of action of glimepiride is to bind to the receptors on beta cell membrane, leading to closure of the ATP-sensitive potassium channels. Closing the potassium channel induces depolarization of the beta cell and results - by opening of calcium channels - in an increase influx of calcium into the cell. The increase in intracellular calcium concentration stimulates insulin release from the cells. Like other sulfonylureas, glimepiride produces hypoglycemia in patients with diabetes or healthy people without diabetes. Using glimepiride and sulfonylureas for long term also causes some extrapancreatic effects which significantly contribute to hypoglycemia effects. The main extrapancreatic effects are an improvement of the sensitivity of the peripheral tissues for insulin and a decrease of the glucose production in the liver. Glimepiride also has synergistic effects with metformin or insulin.
4 mg: Glimepiride is a drug for the treatment of type 2 diabetes mellitus of the sulfonylurea class. The primary mechanism of action of glimepiride in lowering blood glucose appears to be dependent on stimulating the release of insulin from functioning pancreatic beta cells. In addition, extrapancreatic effects may also play an important role in the activity of sulfonylureas such as glimepiride, which increased sensitivity of peripheral tissues to insulin.
Pharmacokinetics: 2 mg: The bioavailability of glimepiride after oral administration is complete. Food intake has no relevant influence on absorption, only the absorption rate is slightly diminished. Maximum plasma concentrations are reached 2.5 hours after oral intake. Glimepiride has a very low distribution volume (approx. 8.8 litres), which is roughly equal to albumin distribution space, high protein binding (99%) and a low clearance (approx. 48 ml/min). Mean dominant plasma half-life is about 5 - 8 hours. After high doses, slightly longer half-lives were noted. After a single dose of radiolabelled glimepiride, 58% of the radioactivity was recovered in the urine, and 35% in the faeces. No unchanged substance was detected in the urine. Two metabolites most probably resulting from hepatic metabolism (major enzyme is CYP2C9) were identified both in urine and faeces: The hydroxy derivative and the caboxy derivative.
4 mg: Glimepiride is completely absorbed from the gastrointestinal tract. Peak plasma concentrations occur in 2 to 3 hours, and it is highly protein bound. The drug is extensively metabolised to two main metabolites, a hydroxy derivative and a carboxy derivative. The half-life after multiple doses is about 9 hours. Approximately 60% of a dose is eliminated in the urine and 40% in the faeces.
Glimepiride is indicated as an adjunct to diet and exercise to lower the blood glucose in patients with noninsulin-dependent (type 2) diabetes mellitus (NIDDM) whose hyperglycemia cannot be controlled by diet and exercise alone.
Dosage/Direction for Use
Glimepiride STELLA 2 mg/Glimepiride STELLA 4 mg is orally taken. The drug usually is administered as a single daily dose given each morning with breakfast or with the first main meal.
Initial dosage in previously untreated patients: The usual initial adult dosage of glimepiride is 1-2 mg once daily. In debilitated, malnourished, or geriatric patients and in patients with hepatic or renal impairment and other patients at increased risk of hypoglycemia, the initial dosage of glimepiride should be 1 mg once daily.
Initial dosage in patients transferred from other antidiabetic agents: 2 mg: For the switch over to glimepiride, the strength and the half-life of the previous medicinal product has to be taken into account. In some cases, especially in antidiabetics with a long half-life (e.g. chlorpropamide), a wash out period of a few days is advisable in order to minimize the risk of hypoglycaemic reactions due to the additive effect. The initial dosage of glimepiride should be 1-2 mg once daily. The maximum dosage should not exceed 2 mg daily.
4 mg: The initial dosage of glimepiride in adults should be 1-2 mg once daily. The maximum dosage should not exceed 2 mg daily.
Maintenance dosage: The usual maintenance dosage of glimepiride from 1 - 4 mg once daily. In patients receiving 1 mg of glimepiride daily, the dosage may be increased to 2 mg daily if adequate glycemic control has not been achieved after 1 - 2 weeks. After reaching the 2 mg dosage, subsequent dosage should be adjusted according to the patient's tolerance and therapeutic response, increasing the dosage in increments of no more than 2 mg daily at 1- to 2-week intervals. The maximum recommended dosage of glimepiride is 8 mg daily.
Symptoms: Overdosage of sulfonylurea can produce hypoglycemia.
Treatment: Mild hypoglycemic symptoms without loss of consciousness or neurologic findings should be treated aggressively with oral glucose and adjustments in drug dosage and/or meal patterns.
Severe hypoglycemic reactions with coma, seizure, or other neurological impairment occur infrequently, but constitute medical emergencies requiring immediate hospitalization. If hypoglycemic coma is diagnosed or suspected, the patient should be given a rapid intravenous injection of concentrated (50%) glucose solution. This should be followed by a continuous infusion of a more dilute (10%) glucose solution at a rate that will maintain the blood glucose at a level above 100 mg/dl. Patients should be closely monitored for a minimum of 24 to 48 hours.
Hypersensitivity to glimepiride, other sulfonylurea or sulfonamides or excipients in the tablet.
Insulin dependent diabetes, diabetic coma, ketoacidosis.
Severe renal or hepatic function disorders: A changeover to insulin is required.
Pregnancy and lactation.
Special Precautions
The patient should be informed of the potential risks and advantages of glimepiride and of alternative modes of therapy.
Hypoglycemia: All sulfonylurea drugs are capable of producing severe hypoglycemia.
Patients with impaired renal function may be more sensitive to the glucose-lowering effect of glimepiride.
Debilitated or malnourished patients and those with hepatic, adrenal, or pituitary insufficiency are particularly susceptible to the hypoglycemic action. Hypoglycemia may be difficult to recognize in the elderly and in people who are taking beta-adrenergic blocking drugs or other sympatholytic agents.
Hypoglycemia is more likely to occur when caloric intake is deficient, after severe or prolonged exercise, when alcohol is ingested, or when more than one glucose-lowering drug is used.
Combined use of glimepiride with insulin or metformin may increase the potential for hypoglycemia.
Loss of control of blood glucose: When a patient stabilized on any diabetic regimen is exposed to stress such as fever, trauma, infection, or surgery, a loss of control may occur. At such times, it may be necessary to add insulin in combination with glimepiride or even use insulin monotherapy.
Fasting blood glucose should be monitored periodically to determine therapeutic response. Glycosylated hemoglobin should also be monitored, usually every 3 to 6 months, to more precisely assess long-term glycemic control.
Hypersensitivity reactions: 2 mg: There have been reports of hypersensitivity reactions in patients treated with glimepiride, including serious reactions such as anaphylaxis, angioedema, and Stevens-Johnson syndrome. If a hypersensitivity reaction is suspected, promptly discontinue glimepiride, assess for other potential causes for the reaction, and institute alternative treatment for diabetes.
Hemolytic anemia: 2 mg: Sulfonylureas can cause hemolytic anemia in patients with glucose 6-phosphate dehydrogenase (G6PD) deficiency. Because glimepiride is a sulfonylurea, use caution in patient with G6PD deficiency and consider the use of a non-sulfonylurea alternative. There are also reports of hemolytic anemia in patients receiving glimepiride who did not have known G6PD deficiency.
Increased risk of cardiovascular mortality with sulfonylureas: 2 mg: The administration of oral hypoglycemic drugs has been reported to be associated with increased cardiovascular mortality as compared to treatment with diet alone or diet plus insulin. The patients should be informed of the potential risks and advantages of glimepiride and of alternative modes of therapy.
Glimepiride STELLA 2 mg/Glimepiride STELLA 4 mg contains lactose. Patients with rare hereditary problems of galactose intolerance, total lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Effects on ability to drive and use machines: The patient's ability to concentrate and react may be impaired as a result of hypoglycaemia or hyperglycaemia or visual impairment. Patients should be advised to take precautions to drive or operate machinery.
Use In Pregnancy & Lactation
Pregnancy: 2 mg: Studies in animals show that drug has toxicity on embryo causing fetotoxicity and can cause congenital abnormalities. Therefore, glimepiride is contraindicated for pregnant women. People taking glimepiride were pregnant, immediately notify the physician to switch over to insulin therapy and insulin dose should be adjusted to keep blood glucose levels as normal.
Lactation: 2 mg: Glimepiride is excreted in breast milk. Therefore, glimepiride is contraindicated for breast-feeding women; insulin therapy should be used as an alternative mode. If glimepiride is required to use, they have to stop breastfeeding.
4 mg: Glimepiride should not be used during pregnancy and lactation.
Adverse Reactions
2 mg: The most significant adverse reaction is hypoglycemia.
Common (1/100 ≤ ADR < 1/10): Nervous system: Dizziness, fainting, headache.
Gastrointestinal: Nausea, vomiting, epigastric distension, abdominal pain, diarrhea.
Eye: Visual disturbance, transient, may occur especially on initiation of treatment, due to changes in blood glucose levels.
Uncommon (1/1,000 ≤ ADR < 1/100): Skin: Allergic or false allergic reactions, rash, urticaria, pruritus.
Rarely (1/10,000 ≤ ADR < 1/1,000): Hepatic: Hepatic enzymes increased, jaundice, hepatic failure.
Blood: Thrombocytopenia (mild or severe), hemolytic anemia, erythropenia, leukopenia, granulocytopenia.
Vascular system: Leukocytoclastic vasculitis.
Skin: Photosensitivity.
4 mg: Hypoglycemia, dizziness, asthenia, headache, nausea.
Gastrointestinal reactions: Vomiting, gastrointestinal pain, and diarrhea. In rare cases, there may be an elevation of liver enzyme levels. In isolated instances, impairment of liver function (e.g. with cholestasis and jaundice), as well as hepatitis.
Dermatologic reactions: Porphyria cutanea tarda, photosensitivity reactions, and allergic vasculitis.
Hematologic reactions: Leukopenia, agranulocytosis, thrombocytopenia, hemolytic anemia, aplastic anemia and pancytopenia.
Metabolic reactions: Hepatic porphyria reactions and disulfiram-like reactions, hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH).
Other reactions: Changes in accommodation and/or blurred vision.
Drug Interactions
Drug interactions: Coadministrations tend to produce hypoglycemia: Sulfonylurea and nonsteroidal anti-inflammatory drugs and other drugs that are highly protein bound, such as salicylates, sulfonamides, chloramphenicol, coumarin, probenecid, monoamine oxidase inhibitors, and beta adrenergic blocking agents.
Coadministrations tend to produce hyperglycemia and may lead to loss of control: Sulfonylurea and the thiazides and other diuretics, corticosteroids, phenothiazines, thyroid products, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics and isoniazid.
A potential interaction between oral miconazole and oral hypoglycemic agents leading to severe hypoglycemia has been reported.
There is potential interaction of glimepiride with inhibitors (e.g. fluconazole) and inducers (e.g. rifampicin) of cytochrome P450 2C9.
Drug incompatibilities: In the absence of incompatibility studies, this medicinal product must not be mixed with other medicinal products.
Storage condition: Store in a well-closed container, in a dry place. Do not store above 30°C.
Shelf-life: 24 months from the date of manufacturing.
MIMS Class
ATC Classification
A10BB12 - glimepiride ; Belongs to the class of sulfonylureas. Used in the treatment of diabetes.
Tab 2 mg (blue, biconvex, caplet-shaped with breakline on both edges, embossed "2" on one side and plain on the other side) x 3 x 10's, 6 x 10's. 4 mg (blue, flat, caplet-shaped with breakline on both two edges and two sides, embossed "4" on one side) x 3 x 10's, 6 x 10's.
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