Overview

This medication consists of Glimepiride and Metformin. Glimepiride is used to reduce high blood sugar levels in people with type 2 diabetes. It’s used in combination with a healthy diet and exercise.

Indications & Usage

• Glimepiride is indicated for the treatment of type 2 diabetes mellitus, when diet, physical exercise and weight reduction alone are not adequate.
• Non-insulin-dependent diabetes (NIDDM, type II)
• Metformin 500 mg Tablets can be given alone as initial therapy, or can be administered in combination with sulphonyl ureas after careful assessment of the contra-indications.

Pharmacology

Pharmacodynamic Properties of Glimepiride:

Glimepiride is an active hypoglycaemic substance belonging to the sulphonylurea group. It may be used in non-insulin dependent (type 2) 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.

Pharmacodynamics Properties of Metformin:

Metformin is an antihyperglycemic agent that improves glucose tolerance in patients with NIDDM, lowering both basal and postprandial plasma glucose. Metformin is not chemically or pharmacologically related to any other class of oral antihyperglycemic agents. Unlike sulfonylureas, metformin does not produce hypoglycemia in either patients with NIDDM or healthy subjects and does not cause hyperinsulinemia. Metformin does not affect insulin secretion.

Pharmacokinetics Properties of Glimepiride:

ABSORPTION: Completely (100%) absorbed
PROTEIN BINDING: Over 99.5% bound to plasma protein.
METABOLISM: Hepatic

Pharmacokinetics Properties of Metformin:

ABSORPTION: Absorbed over 6 hours, bioavailability is 50 to 60% under fasting conditions. The level of absorption is not dose-related, suggesting that absorption occurs through a saturable process.
DISTRIBUTION: Plasma protein binding is negligible. Metformin partitions into erythrocytes. The blood peak is lower than the plasma peak and appears at approximately the same time. The red blood cells most likely represent a secondary compartment of distribution. The mean volume of distribution (Vd) ranged between 63-276 l.
METABOLISM: Metformin is excreted unchanged in the urine.

Side Effects:

• Headache
• Nausea
• Dizziness
• Weakness
• Anxiety
• Irritability
• Sweating

Contraindications

This medication is contraindicated in patients with the following conditions:

• Insulin dependent diabetes
• Diabetic coma
• Renal or hepatic function disorders