Drug Interaction:
Antifungal agents like like ketoconazole and miconazole may inhibit repaglinide metabolism, and antibacterial agents like erythromycin.
Drugs that induce the cytochrome P450 enzyme system 3A4 may increase repaglinide metabolism.
Actions potentiated by certain drugs including NSAIDs and other drugs that are protein bound, salicylates, sulfonamides, chloramphenicol, coumarins, probenecid,
MAOs and beta blockers. Thiazides and diuretics, corticosteroids, phenothiazines, thyroid products, estrogens, oral cointraceptives, calcium channel blockers and iosoniazid tend to produce hyperglycemia and may lead to loss of glycemic control.
Indication:
Non-insulin dependent diabetes
New Drugs Approved by (DCI) Drug Controller GENERAL - India For Marketing
(Ref- IDMA Publication)
Name of Drug Indication Date of Approval
Repaglinide Anti Diabetic 23-03-2000
Adverse Reaction:
Hyperglycemia, hyoglycemia, nausea, diarrhea, constipation, vomiting, dyspepsia, arthralgia.
Contra-Indications:
Diabetic ketacidosis, with or without coma(treat with insulin); type 1 diabetes.
Hypersensity to the drug
Special precautions:
Drug administration associated with increased cardiovasculr mortality as compared with treatment with diet alone or diet plus insulin. Patients with impaired renal function.
Pregnancy and lactation. Potential for hypoglycemia in nursing mothers may exist.
Fasting blood sugars and glycosylated haemoglobulin HbA,C) levels should be continously monitored. Oral hypoglycemic agents are capable of producing hypoglycaemia. Patient selection and monitoring esstential.
Dosages/ Overdosage Etc:
Indications:
Non-insulin dependent diabetes
Dosage:
Start with 1 or 2mg to be taken 30 minutes before meals. Maximmum recommended dose is 4mg before meals to a maximum of 16mg.
May be dosed 2, 3 or 4 times a day in response to changes in patients meal pattern.
Patient Information:
1.Patients withg impaired renal function.
2.Pregnancy: Safety not establishe. To be used only if needed.
3.Lactation: Potential for hypoglycemia in nursing mothers may exist. Fasting blood sugars and glycosylated haemoglobulin HbA,C) levels should be continously monitored.
4.Oral hypoglycemic agents are capable of producing hypoglycaemia. Patient selection and monitoring esstential.
Pharmacology/ Pharmacokinetics:
Ref- Drug Facts And comparisons(2010)
Pharmacology:
Repaglinide stimulates release of insulin from pancreatic Beta cells by inhibiting potassium
refflux via closure of ATP- regulated K channels. This results in depolarisaton of the cell and opening of voltage dependent Ca channels, which increases influx of calcium into beta cells and causes release of insulin.
Pharmacokinetics:
Repaglinide is rapidly absorbed with time to peak plasma concentration of approximately
1 hour. Mean absolute bioavailability is 56%. Concurrent administration with food produced
clinically insignificant reductions in peak plasma concentrations. Terminal disposition half-life of repaglinide is approx 1 hour. Excretion occurs principally by the biliary route, with 6% being renally eliminated.
Repaglinide pharmacokinetic parameters in
Diabetic and healthy subjects
Parameter Patients withType 2 Diabetes
Dose AUC 0-24h (mean +/-SD)
(ng/mL*h)
0.5mg 68.9 +/- 154.4
1mg 125.8 +/-129.8
2mg 152.4 +/- 89.6
4mg 447.4 +/- 211.3
Dose Cmax 0.5 h( mean +/-SD)
(ng/mL)
0.5mg 9.8 +/- 10.2
1mg 18.3 +/- 9.1
2mg 26 +/- 13
4mg 65.8 +/- 30.1
Dose Tmax 0.5h
mean (SD)
0.5 to 4mg 1 to 1.4
(0.3 to 0.5) h
Dose t 1/2
(Ind Range)
0.5 to 4mg 1 to 1.4
(0.4 to 8)h
Parameter Healthy Subjects
CL based on IV 38+/- 18 L/h
Vss based on IV 31+/- 12L
Aabs bio 56+/- 9%
Interaction with Food:
Not significantly affected by predence of food.
Pregnancy and lactation:
Pregnancy:
Safety not established. To be used only if needed.
Lactation:
Potential for hypoglycemia in nursing mothers may exist.
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