sitagliptin (Rx)

Brand and Other Names:Januvia
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 25mg
  • 50mg
  • 100mg

Type 2 Diabetes Mellitus

Indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus (T2DM)

100 mg PO qDay

Dosage Modifications

Renal impairment

  • eGFR ≥45 to <90 mL/min/1.73 m2: No dosage adjustment necessary
  • eGFR 30 to <45 mL/min/1.73 m2: 50 mg PO qDay
  • eGFR <30 mL/min/1.73 m2: 25 mg PO qDay
  • End-stage renal disease requiring hemodialysis or peritoneal dialysis: 25 mg PO qDay regardless of timing of dialysis

Hepatic impairment

  • Mild to moderate impairment: Dose adjustment not necessary
  • Severe impairment: Not studied

Dosing Considerations

Limitations of use

  • Should not be used in patients with type 1 diabetes
  • Not studied in patients with a history of pancreatitis; unknown whether these patients are at increased risk for development of pancreatitis while using sitagliptin

Safety and efficacy not established

Three double-blind, placebo-controlled studies evaluated the efficacy and safety of sitagliptin in patients (n=410) aged 10-17 years with uncontrolled T2DM, with or without insulin therapy; results showed effects of patients treated with sitagliptin were not significantly different from placebo

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Interactions

Interaction Checker

and sitagliptin

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Combination with insulin with or without metformin

            • Hypoglycemia (15.5%)

            Combination with glimepiride with or without metformin

            • Hypoglycemia (12.2%)

            1-10%

            Monotherapy

            • Nasopharyngitis (5.2%)
            • Upper respiratory tract infection (4.5%)
            • Headache (1.1%)

            Combination with pioglitazone

            • Upper respiratory tract infection (6.3%)
            • Headache (5.1%)

            Combination with metformin

            • Nasopharyngitis (6.2%)
            • Upper respiratory tract infection (5.9%)

            Combination with metformin and rosiglitazone

            • Nasopharyngitis (6.1%)
            • Upper respiratory tract infection (5.5%)

            Combination with glimepiride with or without metformin

            • Nasopharyngitis (6.3%)
            • Upper respiratory tract infection (5.9%)

            Postmarketing Reports

            Hypersensitivity reactions including anaphylaxis, angioedema, rash, urticaria, cutaneous vasculitis, and exfoliative skin conditions including Stevens-Johnson syndrome

            Hepatic enzyme elevations; acute pancreatitis, including fatal and nonfatal hemorrhagic and necrotizing pancreatitis

            Worsening renal function, including acute renal failure (sometimes requiring dialysis)

            Severe and disabling arthralgia

            Constipation, vomiting

            Headache, myalgia, pain in extremity, back pain

            Rhabdomyolysis

            Pruritus

            Bullous pemphigoid

            Mouth ulceration; stomatitis

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            Warnings

            Contraindications

            Serious hypersensitivity to sitagliptin (eg, anaphylaxis, angioedema)

            Cautions

            Acute pancreatitis reported, including fatal and nonfatal hemorrhagic or necrotizing pancreatitis; if pancreatitis suspected, discontinue promptly

            Acute renal failure reported, sometimes requiring dialysis; assess renal function before initiation and periodically thereafter

            Serious allergic and hypersensitivity reactions (eg, anaphylaxis, angioedema, exfoliative skin conditions including Stevens-Johnson syndrome) reported; promptly stop treatment and assess for other potential causes; appropriately monitor and treat

            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 observed with other DPP-4 inhibitors; consider risks and benefits 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; advise to report any developing blisters/erosions; discontinue DPP-4 therapy and consult a dermatologist if bullous pemphigoid suspected

            Drug interaction overview

            • Sitagliptin is a P-gp and organic anion transporter-3 substrate; weak CYP3A4 and CYP2C8 substrates
            • Insulin or insulin secretagogues
              • Increased risk of hypoglycemia when concomitantly used with insulin and/or an insulin secretagogue; consider lowering dose of insulin or insulin secretagogue
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            Pregnancy & Lactation

            Pregnancy

            Limited available data in pregnant females are not sufficient to inform a drug-associated risk for major birth defects and miscarriage

            Pregnancy registry

            • Monitors pregnancy outcomes in females exposed to drug during pregnancy
            • Encourage patients to report any prenatal exposure to drug by calling 1-800-986-8999

            Animal data

            • No adverse developmental effects were observed when administered to pregnant rats and rabbits during organogenesis at oral doses up to 30x and 20x, respectively, the 100-mg clinical dose, based on AUC

            Clinical considerations

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

            Lactation

            There is no information regarding presence of drug in human milk, effects on breastfed infants, or on milk production

            Present in rat milk and therefore possibly present in human

            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

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

            Incretins increase insulin release and synthesis from pancreatic beta cells and reduce glucagon secretion from pancreatic alpha cells

            Absorption

            Bioavailability: 87%

            Peak plasma time: 1-4 hr

            Peak plasma concentration: 950 nM (single oral 100-mg dose)

            AUC: 8.52 microM·hr (single oral 100-mg dose)

            Distribution

            Protein bound: 38%

            Vd: 198 L

            Metabolism

            Limited; primarily via CYP3A4 and CYP2C8

            Elimination

            Renal clearance: 350 mL/min

            Half-life, terminal: 12.4 hr

            Excretion: Urine (87% [79% unchanged]), feces (13%)

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            Administration

            Oral Administration

            Take with or without food

            Swallow tablet whole; do not chew, crush, or split

            Storage

            Store at 20-25ºC (68-77ºF), excursions permitted to 15-30ºC (59-86ºF)

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            Formulary

            FormularyPatient Discounts

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