repaglinide (Rx)

Brand and Other Names:Prandin
  • Print

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 0.5mg
  • 1mg
  • 2mg
more...

Type 2 Diabetes Mellitus

Indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus

May be dosed 2, 3, or 4 times a day in response to changes in meal pattern

Starting dose

  • HbA1c <8%: 0.5 mg PO before each meal
  • HbA1c ≥8%: 1-2 mg PO before each meal

Dosage range

  • Dose range: 0.5-4 mg before meals
  • Maximum daily dose: Not to exceed 16 mg/day

Dosage adjustment

  • Double dose up to 4 mg with each meal until satisfactory glycemic control achieved
  • Wait at least 1 week to assess response after each dose adjustment
  • Skipped meals: Instruct patients to skip the scheduled repaglinide dose to reduce the risk of hypoglycemia
  • If hypoglycemia occurs, reduce repaglinide dose

Dosage Modifications

Renal impairment

  • CrCl 40-80 mL/min: No adjustments necessary
  • CrCl 20-40 mL/min: 0.5 mg with meals; titrate slowly and monitor
  • CrCl <20 mL/min: Data not available

Hepatic impairment

  • Use conservative initial and maintenance dosing; wait for longer intervals to make dosage adjustments

Drug interactions

  • Dosage adjustments are recommended in patients taking concomitant strong CYP3A4 or CYP2C8 inhibitors or strong CYP3A4 or CYP2C8 inducers
  • Gemfibrozil: Coadministration is contraindicated
  • Clopidogrel: Avoid coadministration; if unable to avoid, initiate repaglinide at 0.5 mg before each meal; do not exceed total daily dose of 4 mg
  • Cyclosporine: Do not exceed a total daily dose of 6 mg

Dosing Considerations

Combination therapy

  • If monotherapy does not result in adequate glycemic control, may add metformin or thiazolidinedione
  • If thiazolidinedione and metformin do not result in adequate glycemic control, repaglinide may be added
  • Starting dose and dose adjustments for combination therapy are the same as those for repaglinide monotherapy

Safety and efficacy not established

Next:

Interactions

Interaction Checker

and repaglinide

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 
            Previous
            Next:

            Adverse Effects

            >10%

            Hypoglycemia (16-31%)

            Upper respiratory infection (10-16%)

            Headache (9-11%)

            1-10%

            Back pain (5-6%)

            Sinusitis (3-6%)

            Arthralgia (3-6%)

            Bronchitis (2-6%)

            Diarrhea (4-5%)

            Serious CV events (4%; versus 3% incidence with glyburide and glipizide)

            Chest pain (2-3%)

            Constipation (2-3%)

            <1%

            Increased LFTs

            Thrombocytopenia

            Leukopenia

            Hemolytic anemia

            Pancreatitis

            Visual disturbances

            Anaphylactoid reactions

            Previous
            Next:

            Warnings

            Contraindications

            Hypersensitivity to repaglinide

            Diabetic ketoacidosis

            Type I diabetes mellitus

            Coadministration of gemfibrozil results in increased repaglinide plasma concentration (8-fold increase); may lead to severe hypoglycemia

            Cautions

            Stress due to infection, fever, trauma, or surgery; may need to discontinue if exposed to stress

            Hepatic/renal insufficiency

            Patients at risk of severe hypoglycemia: Elderly, debilitated, or malnourished; adrenal or pituitary insufficiency

            Myocardial ischemia reported in patients treated concomitantly with NPH-insulin; not indicated for use in combination with NPH-insulin

            Use caution in elderly and malnourished patients

            Pregnancy or lactation

            The use of sulfonylureas may be associated with increased cardiovascular events

            Drugs that inhibit organic anion transporting protein OATP1B1 (eg, cyclosporine) may increase plasma concentrations of repaglinide, which is a substrate for active hepatic uptake transporter OATP1B1

            Previous
            Next:

            Pregnancy & Lactation

            Pregnancy

            Limited available data from case reports and case series have not identified a drug-associated risk of major birth defects, miscarriage or adverse maternal, or fetal outcomes in women taking repaglinide while pregnant

            Clinical considerations

            • Poorly controlled diabetes in pregnancy increases the maternal risk for diabetic ketoacidosis, preeclampsia, spontaneous abortions, preterm delivery, and delivery complications
            • Poorly controlled diabetes increases the fetal risk for major birth defects, stillbirth, and macrosomia related morbidity

            Animal studies

            • Teratogenicity was not observed in rats and rabbits administered repaglinide during organogenesis at approximately 60 and 1 times the maximum daily clinical dose
            • Offspring of rat dams exposed to repaglinide at ≥22 times clinical exposure on a mg/m² basis during days 17 to 22 of gestation and during lactation were less viable and developed skeletal deformations consisting of shortening, thickening, and bending of the humerus during the postnatal period; this was not seen at doses up to 4 times clinical exposure

            Lactation

            • No data on the presence of repaglinide in human milk, the effects on the breastfeeding infant, or the effects on milk production
            • Because of the potential for hypoglycemia in breastfed infants, repaglinide is not recommended for use when breastfeeding

            Animal data

            Detected in breast milk of rat dams and lowered blood glucose levels were observed in the pups

            Cross fostering studies indicated that skeletal changes could be induced in control pups nursed by treated dams, although this occurred to a lesser degree than those pups treated in utero

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

            more...
            Previous
            Next:

            Pharmacology

            Mechanism of Action

            Increases insulin secretion by blocking ATP potassium channels on beta islet cells, which facilitates calcium entry through calcium channels; increased intracellular calcium stimulates insulin release from pancreatic beta cells

            Absorption

            Bioavailability: 56%

            Onset: 15-60 min (increased insulin levels)

            Duration: 4-6 hr

            Peak plasma time: 1 hr

            Distribution

            Protein bound: >98%

            Vd: 31 L

            Metabolism

            Metabolized extensively in liver, by CYP3A4 and CYP2C8

            Metabolites: Oxidized dicarboxylic acid, aromatic amine, acyl glucuronide (inactive)

            Elimination

            Half-life: 1 hr

            Total body clearance: 38 L/hr

            Excretion: Feces (90%); urine (8%)

            Previous
            Next:

            Administration

            Oral Administration

            Take dose 15 minutes before meal

            May be dosed 2, 3, or 4 times a day in response to changes in meal pattern

            Skipped meals: Instruct patients to skip the scheduled repaglinide dose to reduce the risk of hypoglycemia

            Previous
            Next:

            Images

            Previous
            Next:

            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
            Additional Offers
            Email to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Email Forms to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Previous
            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.