Linagliptin

Aka: Linagliptin, Tradjenta, Trijardy XR

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II. Indications

  1. Type II Diabetes Mellitus
  2. Insulin deficiency and Insulin Resistance
    1. Adjunct to Glucophage, Sulfonylureas, Glitazones

III. Contraindications

  1. Type I Diabetes Mellitus
  2. Congestive Heart Failure
  3. Prior history of malignancy
    1. Due to increased risk of cancer invasion and metastases

IV. Mechanism

  1. See DPP-4 Inhibitor
  2. Dipeptidyl Peptidase-4 (DPP-4) is an enzyme that degrades the Incretins GLP-1 and GLP-2
    1. Incretins (GIP and GLP1) are normally released from GI Tract (enteroendocrine cells) following meals
    2. Incretins increase Glucose dependent Insulin secretion, and inhibit Glucagon secretion
  3. DPP4 Inhibitor Activity
    1. DPP-4 Inhibitors block Incretin degradation
      1. Allows accumulation of GLP-1 by 2-3 fold
    2. Activate Glucose-Dependent Insulinotropic Polypeptides
      1. Stimulates beta cells to secrete Insulin
      2. Lowers Blood Sugar, but low risk of Hypoglycemia
  4. Differs from GLP1 Agonists
    1. Weight neutral
    2. No Nausea

V. Precautions

  1. DPP-4 Inhibitors are less than half as effective as lower cost medications (e.g. Metformin, Sulfonylureas)
  2. No longterm evidence of improved outcomes
  3. Decrease dose in renal Impairment
  4. May consider for those close to goal AND
    1. Already either on other Oral Hypoglycemics or in whom they are contraindicated (e.g. Chronic Kidney Disease)

VI. Medications

  1. Linagliptin (Tradjenta) Tablets: 5 mg
  2. Combinations
    1. Trijardy XR (Linagliptin, Empagliflozin and Metformin XR)

VII. Dosing

  1. Linagliptin 5 mg orally daily
  2. No Renal Dosing required

VIII. Adverse Effects

  1. Unless otherwise noted, adverse effects are for DPP-4 Inhibitor in general
  2. Acute Pancreatitis
    1. Incidence may be as high as 1 in 50 for two years
    2. Singh (2013) JAMA Intern Med 173(7):534-9 [PubMed]
  3. Serious Allergic Reaction (Sitagliptin)
    1. Anaphylaxis
    2. Angioedema
  4. Hepatotoxicity (Alogliptin, Vlidagliptin)
  5. Headache
  6. Bullous Pemphigoid
  7. Congestive Heart Failure exacerbation
    1. Risk of hospitalized CHF exacerbation: 1 in 150 patients/2 years using Saxigliptin or Alogliptin
    2. Sitagliptin (Januvia) is less associated with CHF exacerbation
    3. Scirica (2013) N Engl J Med 369(14):1317-26 [PubMed]
  8. Severe, persistent Joint Pain (rare)
    1. Stop agent if suspect Gliptin-induced pain (and avoid other Gliptins)
    2. Consider other possible causes (e.g. Statin induced Myopathy)
    3. FDA Alert
      1. http://www.fda.gov/drugs/drugsafety/ucm459579.htm

IX. Safety

  1. Unknown safety in pregnancy (but generally avoided)
  2. Unknown safety in Lactation

X. Drug Interactions

  1. Significant CYP3A4 inducer and P-Glycoprotein Inducer

XI. Efficacy

  1. No longterm cardiovascular benefit (DPP-4 Inhibitor in general)
    1. Green (2015) N Engl J Med 373(3): 232-42 [PubMed]
    2. Scirica (2013) N Engl J Med 369(14): 1317-26 [PubMed]
    3. White (2013) N Engl J Med 369(14): 1327-35 [PubMed]
  2. Lowers HBA1C 0.5 to 0.9% with a mean 0.6% (DPP-4 Inhibitor in general)
    1. Contrast with Metformin, Sulfonylureas, GLP-1 Agonists, Pioglitazone lower A1C 1.0 to 1.5% at generic costs
    2. When combined with other hypoglycemics, its Glucose lowering effects are not additive

XII. Resources

  1. Linagliptin (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=c797ea5c-cab7-494b-9044-27eba0cfe40f

XIII. References

  1. (2013) Presc Lett 20(8):46
  2. Jones (2007) Am Fam Physician 75:1831-5 [PubMed]
  3. Steinberg (2019) Am Fam Physician 99(4): 237-43 [PubMed]
  4. Vaughan (2024) Am Fam Physician 109(4): 333-42 [PubMed]

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Related Studies

Cost: Medications

tradjenta (on 1/1/2023 at Medicaid.Gov Survey of pharmacy drug pricing)
TRADJENTA 5 MG TABLET $16.80 each
trijardy xr (on 1/1/2023 at Medicaid.Gov Survey of pharmacy drug pricing)
TRIJARDY XR 10-5-1,000 MG TAB $18.95 each
TRIJARDY XR 12.5-2.5-1,000 MG $9.53 each
TRIJARDY XR 25-5-1,000 MG TAB $18.87 each
TRIJARDY XR 5-2.5-1,000 MG TAB $9.51 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information. GoodRx is another tool for finding lower drug prices.

Related Topics in Pharmacology

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