alogliptin (Rx)Brand and Other Names:Nesina

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 6.25mg
  • 12.5mg
  • 25mg
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Diabetes Mellitus Type 2

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

25 mg PO qDay

Dosage Modifications

Renal impairment

  • Mild (CrCl ≥60mL/min): No dosage adjustment required
  • Moderate (CrCl ≥30 to <60 mL/min): Decrease dose to 12.5 mg PO qDay
  • Severe (CrCl ≥15 to <30 mL/min) or ESRD (CrCl <15 mL/min) or requiring hemodialysis: 6.25 mg PO qDay
  • May administer without regard to the timing of dialysis
  • Peritoneal dialysis: Not studied

Hepatic impairment

  • Mild-to-moderate (Child-Pugh A and B): No dosage adjustment required
  • Severe (Child-Pugh C): Not studied

Dosing Considerations

Limitations of use: Not indicated for the treatment of type 1 diabetes mellitus or diabetic ketoacidosis, as it would not be effective in these settings

Assess renal function before initiating alogliptin and periodically thereafter

Safety and efficacy not established

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Interactions

Interaction Checker

alogliptin 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%

            Hypoglycemia (1.5-35%); higher when added to insulin

            1-10%

            Nasopharyngitis (4.4%)

            Headache (4.2%)

            Upper respiratory tract infection (4.2%)

            <1%

            Hypersensitivity (0.6%)

            Pancreatitis (0.2%)

            Postmarketing reports

            Severe and disabling arthralgia

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            Warnings

            Contraindications

            Hypersensitivity to alogliptin, including anaphylaxis, angioedema, or severe cutaneous adverse reactions including Stevens-Johnson syndrome

            Cautions

            Pancreatitis reported; if pancreatitis suspected, discontinue therapy and initiate appropriate management

            Caution with sensitivity to another DPP-4 inhibitor; discontinue if serious hypersensitivity reaction suspected (see Contraindications)

            Fatal and nonfatal hepatic failure reported; type 2 DM is also known to cause fatty liver disease and liver enzyme elevation; monitor carefully and interrupt alogliptin treatment if LFTs elevated, do not restart alogliptin without another explanation for the liver test abnormalities; do not restart therapy if liver injury is confirmed and no alternative etiology can be found

            Insulin and insulin secretagogues (eg, sulfonylureas) are known to cause hypoglycemia; therefore, a lower dose of insulin of insulin secretagogue may be needed to minimize hypoglycemia risk

            There have been no clinical studies establishing conclusive evidence of macrovascular risk reduction with alogliptin or any other antidiabetic drug

            DPP-4 inhibitors may cause disabling joint arthralgia; resolves within a month upon discontinuing the drug

            Congestive heart failure (CHF) risk

            • The EXAMINE (Examination of Cardiovascular Outcomes with Alogliptin versus Standard of Care) trial enrolled 5,380 patients with type 2 diabetes and recent acute coronary syndrome
            • Hospitalization for CHF was observed in 106 (3.9%) patients treated with alogliptin and 89 (3.3%) patients treated with placebo; although the difference was not statistically significant (hazard ratio, 1.19), heart failure was not an end point of the study
            • Health care professionals should consider discontinuing medications containing alogliptin in patients who develop heart failure and monitor their diabetes control
            • If heart failure develops, evaluate and manage according to current standards of care and consider discontinuation
            • Lancet. 2015 May 23;385(9982):2067-76
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            Pregnancy & Lactation

            Pregnancy Category: B

            Lactation: Unknown whether distributed in breast milk

            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

            Selective dipeptidyl peptidase-4 (DPP-4) inhibitor; slows inactivation of incretin hormones (eg, GLP-1, GIP), thereby reducing fasting and postprandial glucose concentrations in a glucose-dependent manner

            Absorption

            Bioavailability: ~100%

            Peak plasma time: 1-2 hr

            Distribution

            Protein bound: 20%

            Vd: 417 L

            Metabolism

            Does not undergo extensive metabolism and 60-71% of the dose is excreted unchanged in the urine

            Active metabolite: N-demethylated (<1% of parent compound)

            Inactive metabolite: N-acetylated alogliptin (<6% of parent compound)

            Minor substrate of CYP3A4 and CYP2D6

            Elimination

            Half-life: 21 hr

            Renal clearance: 9.6 L/hr

            Total body clearance: 14 L/hr

            Excretion: 76% urine; 13% feces

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            Administration

            Instructions

            May take with or without food

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            Images

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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
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