linagliptin (Rx)

Brand and Other Names:Tradjenta
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 5mg
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Type 2 Diabetes Mellitus

Indicated for adults with type 2 diabetes mellitus along with diet and exercise to lower blood sugar; may be used as monotherapy or in combination with other common antidiabetic medications including metformin, sulfonylurea, pioglitazone, or insulin

5 mg PO qDay

Dosage Modifications

Hepatic or renal impairment: No dosage adjustment required

Dosing Considerations

Not be used in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis, as it would not be effective in these settings

Has not been studied in patients with a history of pancreatitis; unknown whether patients with a history of pancreatitis are at an increased risk of developing pancreatitis when taking linagliptin

Administration

May administer with or without food

When used in combination with other antidiabetic agents, a lower dose of the insulin secretagogue (eg, sulfanylurea) or insulin may be required to reduce the risk of hypoglycemia

Safety and efficacy not established

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Interactions

Interaction Checker

and linagliptin

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    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            1-10%

            Nasopharyngitis (4.3%)

            Hyperlipidemia (2.8%; with pioglitazone)

            Cough (2.4%; with metformin and sulfonylurea)

            Hypertriglyceridemia (2.4%; with sulfonylurea)

            Weight gain (2.3%; with pioglitazone)

            Hypoglycemia

            • 7.6% overall incidence
            • 22.9% incidence compared with placebo plus metformin and a sulfonylurea
            • Incidence similar to placebo with monotherapy or combined with metformin or pioglitazone

            Postmarketing Reports

            Acute pancreatitis, including fatal pancreatitis

            Rash

            Mouth ulceration, stomatitis

            Hypersensitivity reactions including anaphylaxis, angioedema, and exfoliative skin conditions

            Severe disabling arthralgia

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            Warnings

            Contraindications

            Hypersensitivity (eg, anaphylaxis, angioedema, exfoliative skin conditions, urticaria, or bronchial hyperreactivity)

            Type 1 diabetes mellitus

            Diabetic ketoacidosis

            Cautions

            Use in combination with an insulin secretagogue (eg, sulfonylurea) was associated with a higher rate of hypoglycemia compared with placebo in a clinical trial

            Rifampin decreased linagliptin exposure suggesting that the levels may be reduced when administered in combination with a strong P-gp or CYP 3A4 inducer; alternative treatment is strongly recommended when linagliptin is to be administered with P-gp or CYP 3A4 inducers

            Serious hypersensitivity reactions reported including anaphylaxis, angioedema, and exfoliative skin conditions

            Severe and disabling arthralgia reported in patients taking DPP-4 inhibitors; consider as a possible cause for severe joint pain and discontinue drug if appropriate

            Heart failure has been observed with two other members of the DPP-4 inhibitor class; consider risks and benefits of empagliflozin in patients with risk factors for heart failure; monitor for signs and symptoms; if heart failure develops, manage accordingly to standard of care and consider interrupting treatment

            Bullous pemphigoid reported with DPP-4 inhibitor use, which required hospitalization; in reported cases, patients recovered with topical or systemic immunosuppressive treatment and discontinuation of DPP-4 inhibitor; patients should report development blisters/erosions; discontinue DPP-4 therapy and consult a dermatologist if bullous pemphigoid suspected

            Pancreatitis

            • Postmarketing reports of acute pancreatitis, including fatal pancreatitis; monitor for signs and symptoms of pancreatitis, and discontinue if suspected
            • Unknown if patients with history of pancreatitis are at increased risk for the development of pancreatitis while using linagliptin
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            Pregnancy & Lactation

            Pregnancy

            The limited data in pregnant women are not sufficient to inform of drug-associated risk for major birth defects and miscarriage; there are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy

            In animal reproduction studies, no adverse developmental effects were observed when linagliptin was administered to pregnant rats during period of organogenesis at doses similar to maximum recommended clinical dose, based on exposure

            Poorly controlled diabetes in pregnancy increases maternal risk for diabetic ketoacidosis, pre-eclampsia, and delivery complications; poorly controlled diabetes increases fetal risk for major birth defects, still birth, and macrosomia related morbidity

            Lactation

            There is no information regarding presence of linagliptin in human milk, the effects on breastfed infant, or effects on milk production; however, linagliptin is present in rat milk; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from therapy or from underlying maternal condition

            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

            Dipeptidyl peptidase 4 (DPP-4) inhibitor; increases and prolongs incretin hormone activity which is inactivated by DPP-4 enzyme

            Incretins regulate glucose homeostasis by increasing insulin synthesis and release from pancreatic beta cells and reducing glucagon secretion from pancreatic alpha cells

            Absorption

            Bioavailability: 30%

            Peak Plasma Time: 1.5 hr

            Peak Plasma Concentration: 8.9 nmol/L

            AUC: 139 nmol•h/L

            Distribution

            Protein Bound: 75-99%; concentration dependent

            Vd: 1,110 L

            Metabolism

            Small fraction metabolized to inactive metabolite

            Excretion

            Half-Life: 12 hr

            Terminal Half-Life: >100 hr

            Enterohepatic system (80%), urine (5%)

            Renal clearance: 70 mL/min

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            Administration

            Instructions

            May administer with or without food

            When used in combination with other antidiabetic agents, a lower dose of the insulin secretagogue (eg, sulfanylurea) or insulin may be required to reduce the risk of hypoglycemia

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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.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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