Dianorm 1

Generic

Repaglinide

 

Indications

In patients with type 2 diabetes mellitus (NIDDM) whose hyperglycemia cannot be controlled adequately by diet and exercise alone, repaglinide is used as an addition to diet and exercise to lower blood glucose. It's also approved for use with Metformin to help individuals with hyperglycemia who can't control their blood sugar with exercise, diet, or either Repaglinide or Metformin alone.

 

Pharmacology

Repaglinide binds to specific receptors in the cell membrane, causing ATP-dependent K+ channels to close and the cell membrane to depolarize. This results in Ca++ inflow, increased intracellular Ca++, and insulin secretion stimulation.

 

Dosage & Administration

• For patients not previously treated or whose HbA1c is <8%, the starting dose should be 0.5 mg before each meal.
• For patients previously treated with blood glucose-lowering drugs and whose HbA1c is >8%, the initial dose is 1 or 2 mg before each meal.
• Repaglinide should be taken immediately or up to 30 minutes before each meal.
• Dosage should be adjusted according to response at intervals of 1-2 weeks; up to 4 mg may be given as a single-dose, maximum 16 mg daily.

 

Interaction

• Inhibitors of the cytochrome P450 enzyme system (azole antifungals and macrolides) can cause reduced clearance of repaglinide and a prolonged half-life.
• Inducers of the cytochrome P450 enzyme system (rifampin, phenobarbital, carbamazepine, troglitazone, etc.) can accelerate the metabolism of repaglinide and shorten its effect.
• Cimetidine has no significant effect on repaglinide absorption or clearance.
• Repaglinide has no significant effect on digoxin, theophylline, or warfarin.
• Drugs with high protein binding (eg, non-steroidal anti-inflammatory drugs) can increase plasma levels of unconjugated repaglinide and enhance its hypoglycemic effect. Therefore, the combination of these drugs with repaglinide may increase the risk of hypoglycaemia.
• When hypoglycemic medications are co-administered with certain medications (such as salicylate, sulfonamides, chloramphenicol, coumarin, probenecid, monoamine oxidase (MAO) inhibitors, and adrenergic blockers), the risk of hypoglycemia may also increase.

 

Contraindications

• Diabetic ketoacidosis, with or without coma, is contraindicated in individuals using repaglinide.
• Diabetes mellitus type 1 and a history of hypersensitivity to the medication or its inactive components.

 

Side Effects

Hypoglycemia and associated symptoms are the most common Repaglinide adverse effects. Upper respiratory infections, diarrhea, constipation, nausea, and vomiting are among the other symptoms. Rashes and urticaria are examples of hypersensitivity reactions.

 

Pregnancy & Lactation

There is no evidence of safety in pregnant women. Repaglinide should only be taken during pregnancy if it is absolutely necessary. Repaglinide is not known to be excreted in human milk. Because many medications are excreted in human milk and because Repaglinide can cause major adverse reactions in nursing infants, a choice should be made whether to stop breastfeeding or stop taking the drug, taking into account the drug's importance to the mother.

 

Precautions & Warnings

During concomitant illness (such as myocardial infarction, unconsciousness, infection, and trauma) and surgery, insulin should be substituted. Hypoglycemia can be caused by any oral blood glucose-lowering medication. To reduce the risk of hypoglycemia, repaglinide should be taken with meals.

 

Therapeutic Class

Meglitinide Analogues

 

Storage Conditions

Do not store above 30°C. Keep away from light and out of the reach of children.

 

Pharmaceutical Name

Rephco Pharmaceuticals Ltd.