Perglim Glimepiride Tablets

PERGLIM
(Glimepiride Tablets 1mg/2mg/3mg/4mg)

For the use of a Registered Medical Practitioner or a Hospital or a Laboratory only.

 

DESCRIPTION

Perglim brand of Gimepiride Tablets is chemically 1{(p-[2-(3-ethyl-4-methyl-2-oxo-3-pyrroline-1-carboxamido)ethyl]phenyl] sulphonyl)-3-(trans-4-methylcyclohexyl)urea

 

COMPOSITION

PERGLIM 1

Each uncoated tablet contains:

Glimepiride USP 1 mg

Colour: Ferric oxide (Red)

PERGLIM 2

Each uncoated tablet contains:

Gilmepiride USP 2 mg

Colours: Ferric oxide (Yellow), Lake of Indigo Carmine

PERGLIM 3

Each uncoated tablet contains:

Glimepiride USP 3 mg

Colour: Ferric oxide (Yellow)

PERGLIM 4

Each uncoated tablet contains:

Glimepiride USP 4 mg

Colour: Lake of lndigo Carmine

 

INACTIVE INGREDIENTS

Lactose, Microcrystalline cellulose, Sodium starch glycollate, Povidone, Crospovidone, Purified Talc, Magnesium stearate, Colloidal anhydrous 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 beta cell. 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 hours. The glucose lowering effect in all treatment groups was maintained for 24 hours.

 

PHARMACOKINETICS

After oral administration, Glimepiride is 100 % absorbed from the GI tract. There is significant absorption after 1 hour of administration and Cmax is achieved within 2 to 3 hours. When Glimepiride  was given with meals, the tmax was slightly increased and AUC was slightly decreased.

After intravenous dosing in normal subjects, the volume of distribution was 47.8 ml/min. Protein binding was greater than 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 above 65 years of age and NIDDM patients below 65 years of age.

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 1 mg Glimepiride 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.

 

INDICATIONS AND USAGE

Non-Insulin dependant (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.

 

CONTRAINDICATIONS

Hypersensitivity to Glimepiride or other sulphonylureas, insulin dependent (Type 1) diabetes mellitus, diabetic precoma or coma.

 

PRECAUTIONS AND WARNINGS

Keep out of reach of children.

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.

Use in pregnancy and lactation

As there are no adequate and well-controlled studies in pregnant women and lactating mothers with Glimepiride, the drug 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 administrating the drug 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.

Alertness and reactions may be impaired due to hypo or hyper glycemia. This may affect the ability to operate a vehicle or heavy machinery.

 

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.

 

ADVERSE REACTIONS

Hypoglycemia, temporary visual impairment, gastrointestinal disturbances. Rarely thrombopenia, leucopenia, haemolytic anaemia. Occasionally allergic or pseudoallergic reactions like itching, urticaria or rashes. In isolated cases, allergic vasculitis, photosensitivity or a decrease in serum sodium may occur. Inform your doctor in case of any adverse reactions related to drug use.

 

DRUG INTERACTION

Hypoglycemic effect of Glimepiride is enhanced by Anticoagulants, Androgens, Chloramphenicol, ClofIbrate, Fenfluramine, Fluconazole, Histamine H2 antagonists, Magnesium salts, Methyldopa; Phenylbutazone, Probenecid, Suphonamides and UrInary acidifiers. Hypoglycemic effect is Inhibited by the following drugs: blockers, Rifampicin, Diazoxide, Thiazide diuretics and urinary alkalisers.

 

OVERDOSAGE

Overdosage can produce hypoglycemia. Mild symptoms without loss of consciousness can be treated with oral glucose. Severe hypoglycemic reactions like coma, seizures require medical emergencies. Hypoglycemic coma should be treated with rapid i.v. infusion of conc. Glucose (50%) solution. This should be followed by continuous infusion of dilute glucose (10%) to maintain glucose levels above 100 mg / dl. Patient should be closely monitored for 24-48 hours as hypoglycemia may recur.

 

DOSAGE AND ADMINISTRATION

Initially 1 mg once daily.

Titration in dose is carried out step wise 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 or before the first main meal. Usual maintenance dose is 1 to 4 mg once daily. Maximum recommended dose is 8mg once daily.

Children: Not recommended.

The route of administration is peroral.

 

STORAGE

• Keep out of reach of children.

• Protect from light and moisture.

• Store below 30°C in a dry place.

 

SHELF LIFE

30 months.

 

PRODUCT SPECIFICATION

Manufacturer

 

PRESENTATION

PERGLIM Tablets are available in the strengths of 1 mg, 2 mg, 3 mg, 4 mg. 10 tablets in each blister.

• 100 tablets (10 x 10’s) in a box.

• 30 tablets (3 x 10’s) in a box.

 

NOTE

• Read the instructions thoroughly before use.

• Use upon doctor’s prescription only.

• Please do not use the drug after the expiry date.

• Please do not use the drug if there are any significant changes in appearance of the tablets.

• Keep out of reach of children.

 

NAFDAC Reg. No.:

PERGLIM 1: 04-8788

PERGLIM 2: 04-8872

PERGLIM 3: a4-6374

 

Manufactured for

MEGA LIFESCIENCES (AUSTRALIA) PTY LTD

Victoria 3810, Australia.

 

Manufactured by

INVENTIA HEALTHCARE PVT LTD.

F1-F1/1, Additional Ambernath, M.I.D.C.,

Ambernath (East)- 421 506, Dist. Thane, India.

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