Prandin (repaglinide) is an oral diabetes medicine that helps control blood sugar levels by stimulating the body to produce more insulin.

Prandin is used together with diet and exercise to treat type 2 diabetes.

If you are considering taking Prandin for a purpose other than diabetes control, be sure to speak with your doctor about the potential risks and benefits. Prandin has been shown to help lower blood sugar levels in people with type 2 diabetes, but it is not known if it can help with other conditions.

Prandin is available as a generic drug. Generic drugs are usually less expensive than brand-name drugs.

If you have any questions about Prandin, please talk with your doctor, pharmacist, or other health care provider.

Benefit of Prandin

Prandin can help you keep your blood sugar levels under control. It does this by stimulating your body to produce more insulin.

Insulin is a hormone that helps your body use glucose (sugar) for energy. It also helps your body store glucose for future use. When your blood sugar levels are too high, insulin helps to bring them down.

Side effects of Prandin may include:

• low blood sugar (hypoglycemia)

• feeling jittery or anxious

• sweating

• dizziness

• headache

• heartburn or indigestion

• nausea

• diarrhoea

If you experience any of these side effects, stop taking Prandin and talk to your doctor.

If you have any questions about Prandin, please talk with your doctor, pharmacist, or other health care provider.

Prandin may help you keep your blood sugar levels under control, but it is not a cure for diabetes. It is important to continue to follow a healthy diet and exercise program while taking this medication.

How does Prandin work?

Prandin works by stimulating the body to produce more insulin. Insulin is a hormone that helps your body use glucose (sugar) for energy. It also helps your body store glucose for future use. When your blood sugar levels are too high, insulin helps to bring them down.

Prandin can be used alone or with other diabetes medicines, such as metformin, sulfonylureas, or thiazolidinediones.

If you have any questions about Prandin, please talk with your doctor, pharmacist, or other health care provider.

Prandin is an oral diabetes medicine that helps control blood sugar levels by stimulating.

Pharmacokinetics

The pharmacokinetics of repaglinide has been evaluated in healthy adult volunteers and patients with NIDDM. Following oral administration, repaglinide is rapidly absorbed from the gastrointestinal tract and undergoes extensive first-pass metabolism in the liver. Peak plasma concentrations (Cmax) of repaglinide are reached approximately 1 hour (max) after a single oral dose. The mean apparent volume of distribution (V/F) is 11 L. Plasma protein binding is about 98%.

Elimination of repaglinide from plasma is biphasic with an initial rapid phase and a subsequent slower phase. The mean apparent clearance (CL/F) during the rapid phase is 131 mL/min while that during the slow phase is 4.7 mL/min. The mean residence time (MRT) is 3.3 hours.

After oral administration of 14C-labeled repaglinide in healthy volunteers, about 61% of the dose was recovered in the urine and 39% in the faeces over 120 hours. Urinary excretion was primarily as metabolites while faecal excretion represented both unchanged drugs and metabolites. Less than 0.1% of the dose was excreted unchanged in the urine.

Special Populations

Geriatric Patients: In a study of 11 geriatric patients with NIDDM (≥ 65 years old), the elimination half-life of repaglinide was prolonged compared to that in younger patients, with a mean value of 7.2 hours compared to 3.3 hours in patients 18 to 54 years old. In this study, the CL/F was reduced and the V/F was increased in the geriatric patients. No dosage adjustment is necessary for elderly patients with NIDDM.

Hepatic Impairment: The pharmacokinetics of repaglinide has been evaluated in 8 subjects with mild (n=4) and moderate (n=4) hepatic impairment following a single 0.5 mg oral dose. Subjects with mild hepatic impairment showed no significant change in Cmax but had an approximately 2-fold increase in Cmax and AUC compared to healthy subjects. In subjects with moderate hepatic impairment, Cmax was increased 3-fold, Tmax was prolonged, and AUC was 5-fold greater than in healthy subjects. The mean apparent clearance (CL/F) was decreased by approximately 50% in both mild and moderate hepatic impairment.

No dosage adjustment is necessary for patients with mild hepatic impairment. For patients with moderate hepatic impairment, the starting dose should be 0.5 mg once daily. The patient’s response to repaglinide should be closely monitored and the dose adjusted accordingly

Renal Impairment: In a study of 8 subjects with NIDDM and varying degrees of renal function (creatinine clearance ranging from 22 to 78 mL/min), there was a reduction in apparent clearance (CL/F) of repaglinide with a corresponding increase in AUC as renal function decreased.

No dosage adjustment is necessary for patients with mild to moderate renal impairment (creatinine clearance ≥ 30 mL/min). For patients with severe renal impairment (creatinine clearance < 30 mL/min), the starting dose should be 0.5 mg once daily. The patient’s response to repaglinide should be closely monitored and the dose adjusted accordingly

Drug-Drug Interactions: In vitro data suggest that repaglinide is a substrate of cytochrome P450 3A4 (CYP3A4). Concomitant administration of ketoconazole, an inhibitor of CYP3A4, resulted in a 2-fold increase in AUC and Cmax of repaglinide. When repaglinide was co-administered with gemfibrozil, another CYP3A4 inhibitor, there was no significant change in the pharmacokinetics of repaglinide.

Coadministration of repaglinide (0.5 mg single dose) and cimetidine (800 mg single dose), an inhibitor of gastric acid secretion, did not affect the pharmacokinetics of repaglinide.

In vitro data indicate that repaglinide is not an inhibitor of cytochrome P450 isozymes 1A2, 2C9, 2C19, 2D6 and 3A4.

In vitro data also suggest that repaglinide does not induce cytochrome P450 isozymes 1A2, 2B1, 2C9 and 3A4.

Repaglinide did not affect the pharmacokinetics of metformin following single-dose administration of metformin hydrochloride (500 mg) and repaglinide (0.5 mg) to healthy volunteers.

Repaglinide did not affect the pharmacokinetics of glipizide following single-dose administration of glipizide (10 mg) and repaglinide (0.5 mg) to healthy volunteers.