Each tablet contains the following colourants: Perglim 1 mg: Ferric oxide (red); Perglim 2 mg: Ferric oxide (yellow) and lake of indigo carmine.
It also contains the following excipients: Lactose, microcrystalline cellulose, sodium starch glycollate, povidone, crospovidone, purified talc, magnesium stearate and anhydrous colloidal silica.
Pharmacology: The primary mechanism of action of glimepiride in lowering blood glucose appears to be dependent on stimulating the release of insulin from functioning pancreatic β-cells. In addition, extrapancreatic effects may also play a role in the activity of glimepiride. Glimepiride administration may lead to increased sensitivity of peripheral tissues to insulin. However, as with other sulphonylureas, the mechanism by which glimepiride lowers the blood glucose during long-term administration has not been clearly established.
A mild glucose lowering effect first appeared following oral doses as low as 0.5-0.6 mg in healthy subjects. The time required to reach maximum effect was about 2-3 hrs. The glucose lowering effect in all treatment groups was maintained for 24 hrs.
Pharmacokinetics: After oral administration, glimepiride is 100% absorbed from the GIT. There is significant absorption after 1 hr of administration and Cmax is achieved within 2-3 hrs. When glimepiride was given with meals, the Tmax was slightly increased and AUC was slightly decreased.
After IV dosing in normal subjects, the volume of distribution was 8.8 L. Total body clearance was 47.8 mL/min. Protein binding was >99.5%.
Glimepiride is completely metabolized by oxidative biotransformation after either an oral or IV dose. When radiolabelled glimepiride was given orally, about 60% of the total radioactivity was recovered in the urine in 7 days. About 40% of the radioactivity was recovered in the feces. No parent drug was recovered from the urine or feces.
Special Populations: Geriatrics: There was no much difference in glimepiride pharmacokinetics (AUC and weight adjusted clearance) between NIDDM patients >65 years and NIDDM patients <65 years.
Pediatrics: No pharmacokinetic study is done in pediatric patients.
Gender: There were no differences between males and females in the pharmacokinetics of glimepiride when adjustment in weight was done for differences in body weight.
Race: No pharmacokinetic studies to assess the effects of race have been performed.
Renal Insufficiency: Results of a clinical study showed that glimepiride serum levels decreased as renal function decreased.
A starting dose of glimepiride 1 mg may be given to NIDDM patients with kidney disease and the dose may be titrated based on fasting blood glucose levels.
Hepatic Insufficiency: No studies were performed in patients with hepatic insufficiency.
Non-insulin dependent (type II) diabetes, whenever blood sugar levels cannot be controlled adequately by diet, physical exercise and weight reduction. Use of glimepiride is a treatment in addition to diet and exercise and not as a substitute to it. Loss of blood glucose control on diet and exercise alone may be transient, thus requiring only short-term administration of glimepiride.
Initially 1 mg once daily.
Titration in dose is carried out stepwise as follows: 1 mg-2 mg-3 mg-4 mg-6 mg at the intervals of 1-2 weeks.
Normally, a single dose is sufficient and it should be taken immediately before a substantial breakfast of before the 1st main meal.
Usual Maintenance Dose: 1-4 mg once daily.
Maximum Recommended Dose: 8 mg once daily.
Overdosage can produce hypoglycemia. Mild symptoms without loss of consciousness can be treated with oral glucose. Severe hypoglycemic reactions eg, coma, seizures require medical emergencies. Hypoglycemic coma should be treated with rapid IV infusion of concentrated glucose (50%) solution. This should be followed by continuous infusion of dilute glucose (10%) to maintain glucose levels >100 mg/dL. Patients should be closely monitored for 24-48 hrs as hypoglycemia may recur.
Hypersensitivity to glimepiride or other sulphonylureas, insulin dependent (type 1) diabetes mellitus, diabetic precoma or coma.
There may be increased cardiovascular mortality as compared to treatment with diet alone or diet plus insulin.
In the initial weeks of treatment, the risk of hypoglycemia may be increased and necessitates careful monitoring. Glucose levels in blood and urine must be checked regularly, as should, additionally the proportion of glycated haemoglobin.
Information for Patients: Patients should be informed of the potential risks and advantages of Perglim and about other modes of therapy. They should be also informed about the importance of adherence to dietary instructions, of a regular exercise program and of regular testing of blood glucose.
The risks of hypoglycemia, its symptoms and treatment, and conditions that predispose to its development should be explained to patients and responsible family members. The potential for primary and secondary failure should also be explained.
Effects on the Ability to Drive or Operate Machinery: Alertness and reactions may be impaired due to hypo- or hyperglycemia. This may affect the ability to operate a vehicle or heavy machinery.
Use in pregnancy & lactation: As there are no adequate and well-controlled studies in pregnant women and lactating mothers with glimepiride, Perglim should not be used during pregnancy unless clearly needed. Recent studies indicate that abnormal blood glucose levels during pregnancy may lead to congenital abnormalities.
Similarly, caution should be exercised while administering Perglim to lactating mothers. A decision whether to discontinue nursing or the drug should be taken depending on the importance of the drug to the mother.
Use in children: Not recommended.
As there are no adequate and well-controlled studies in pregnant women and lactating mothers with glimepiride, Perglim should not be used during pregnancy unless clearly needed. Recent studies indicate that abnormal blood glucose levels during pregnancy may lead to congenital abnormalities.
Similarly, caution should be exercised while administering Perglim to lactating mothers. A decision whether to discontinue nursing or the drug should be taken depending on the importance of the drug to the mother.
Hypoglycemia, temporary visual impairment, GI disturbances. Rarely thrombopenia, leucopenia, haemolytic anaemia. Occasionally allergic or pseudoallergic reactions eg, itching, urticaria or rashes. In isolated cases, allergic vasculitis, photosensitivity or a decrease in serum sodium may occur. Inform the doctor in case of any adverse reactions related to drug use.
Hypoglycemic effect of glimepiride is enhanced by anticoagulants, androgens, chloramphenicol, clofibrate, fenfluramine, fluconazole, histamine H2 antagonists, magnesium salts, methyldopa, phenylbutazone, probenecid, sulphonamides and urinary acidifiers.
Hypoglycemic effect is inhibited by the following drugs: Blockers, rifampicin, diazoxide, thiazide diuretics and urinary alkalisers.
Store at 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F). Keep container tightly closed and protect from moisture and light.
Shelf-Life: 30 months.
A10BB12 - glimepiride ; Belongs to the class of sulfonylureas. Used in the treatment of diabetes.
Tab (uncoated) 1 mg x 3 x 10's. 2 mg x 3 x 10's.
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