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repaglinide (Rx)Brand and Other Names:Prandin

 
 
 

Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet

  • 0.5 mg
  • 1 mg
  • 2 mg
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Type 2 Diabetes Mellitus

Initial dose 0.5 mg PO with no prior treatment, or 1-2 mg with prior treatment

Titrate by up to 4 mg; double preprandial dose until satisfactory blood glucose response attained; not to exceed 16 mg qDay

Take dose 15 minutes before meal; no more than 4 meals/day

Combination Therapy

If monotherapy does not result in adequate glycemic control may add metformin or thiazolidinedione

If thiazolidinedione and metformin does not result in adequate glycemic control, repaglinide may be added

Starting dose and dose adjustments for combination therapy are the same as repaglinide monotherapy

Renal Impairment

CrCl 40-80 mL/minute: No adjustments necessary

CrCl 20-40 mL/minute: 0.5 mg with meals; titrate slowly and monitor

CrCl < 20 mL/minute: Data not available

Hepatic Impairment

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

Other Indications & Uses

Management of type 2 diabetes mellitus adjunct to diet and exercise

Safety and efficacy not established

Initial dose 0.5 mg PO with no prior treatment, or 1-2 mg with prior treatment

Titrate by up to 4 mg; double preprandial dose until satisfactory blood glucose response attained; not to exceed 16 mg qDay

Take dose 15 minutes before meal; no more than 4 meals/day

Combo therapy: Administer as in adults

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Interactions

Interaction Checker

repaglinide and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Headache

            Hypoglycemia (16-31%)

            Upper respiratory infection (10-16%)

            1-10%

            Arthralgia (3-6%)

            Chest pain

            Constipation

            Back pain

            Sinusitis

            Bronchitis

            Diarrhea (4-5%)

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

            <1%

            Increased LFTs

            Thrombocytopenia

            Leukopenia

            Hemolytic anemia

            Pancreatitis

            Visual disturbances

            Anaphylactoid reactions

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            Warnings

            Contraindications

            Hypersensitivity to repaglinide

            Diabetic ketoacidosis

            Type I DM

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

            Cautions

            Stress due to infection, fever, trauma, or surgery, hepatic/renal insufficiency

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

            Pregnancy or lactation

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

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            Pregnancy & Lactation

            Pregnancy Category: C

            Lactation: Not known if crosses into breast milk, avoid

            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.

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            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.

            Pharmacokinetics

            Half-Life: 1 hr

            Onset: 30 min (initial effect); 60-90 min (maximum effect)

            Duration: <4 hr

            Bioavailability: 56%

            Vd: 24-30 L

            Protein Bound: >98%

            Total Body Clearance: 38 L/hr

            Metabolism: Extensively, in liver by CYP3A4 and CYP2C8

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

            Excretion: 90% feces; 8 % urine

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            Formulary

            FormularyPatient Discounts

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            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.
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