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sitagliptin (Rx)Brand and Other Names:Januvia

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 25mg
  • 50mg
  • 100mg
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Diabetes Mellitus, Type 2

100 mg PO qDay

Dosing Modifications

Renal impairment

  • CrCl >50 mL/min: Dose adjustment not necessary
  • CrCl 30-50 mL/min: 50 mg PO qDay
  • CrCl <30 mL/min: 25 mg PO qDay
  • ESRD: 25 mg PO qDay regardless of hemodialysis

Hepatic impairment

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

Safety and efficacy not established

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Interactions

Interaction Checker

sitagliptin and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            1-10%

            Nasopharyngitis (5%)

            Diarrhea (4%)

            Headache (3.6%)

            Constipation (3%)

            Peripheral edema (2%)

            Nausea (2%)

            Pharyngitis (1%)

            Osteoarthritis (1%)

            URI (1%)

            <1%

            Hypersensitivity reactions such as 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

            Constipation

            Vomiting

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

            Severe and disabling arthralgia

            Myalgia

            Pain in extremity

            Back pain

            Postmarketing Reports

            Pruritus

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            Warnings

            Contraindications

            Documented hypersensitivity

            Cautions

            Use with caution in hepatic impairment, or heart failure

            Use with caution in renal failure; worsening of renal failure, including acute renal failure reported

            Not for use in diabetic ketoacidosis patients; not effective

            Not for use in type 1 diabetes mellitus; not effective

            Combo treatment studied only with metformin and thiazolidinediones, not with insulin or sulfonylureas

            Caution when coadministering with strong CYP3A4/5 inhibitors (may require dose adjustment)

            May cause acute pancreatitis, including hemorrhagic and necrotizing pancreatitis; unknown if patients with history of pancreatitis are at increased risk

            Concomitant use of insulin with secretagogues may increase risk of hypoglycemia

            Angioedema reported with other dipeptidyl peptidase-4 (DPP-4) inhibitors; caution with history of angioedema

            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

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            Pregnancy & Lactation

            Pregnancy category: B

            Lactation: Not known whether excreted in breast milk: use caution

            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

            DPP-4 inhibitor; therefore, 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

            Distribution

            Protein bound: 38%

            Vd: 198 L

            Metabolism

            Limited; primarily via CYP3A4 and CYP2C8

            Elimination

            Half-life, terminal: 12.4 hr

            Excretion: Urine (87%), feces (13%)

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            Administration

            Instructions

            Take with or without food

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

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            Images

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            Formulary

            FormularyPatient Discounts

            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.
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