TRADJENTA (linagliptin)

There are 1 contraindications. These drug combinations generally should not be dispensed or administered to the same patient. A manufacturer label warning that indicates the contraindication warrants inclusion of a drug combination in this category, regardless of clinical evidence or lack of clinical evidence to support the contraindication.

Drug Interaction

Drug Names

Lemborexant (Greater Than 5 mg)/Weak CYP3A4 Inhibitors SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient. MECHANISM OF ACTION: Inhibitors of CYP3A4 may inhibit the metabolism of lemborexant.(1) CLINICAL EFFECTS: Concurrent use of an inhibitor of CYP3A4 may result in increased levels of and effects from lemborexant, including somnolence, fatigue, CNS depressant effects, daytime impairment, headache, and nightmare or abnormal dreams.(1) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The maximum recommended dose of lemborexant with concurrent use of a weak CYP3A4 inhibitors should not exceed 5 mg per dose.(1) DISCUSSION: Lemborexant is a CYP3A4 substrate. In a PKPB model, concurrent use of lemborexant with itraconazole increased area-under-curve (AUC) and concentration maximum (Cmax) by 3.75-fold and 1.5-fold, respectively. Concurrent use of lemborexant with fluconazole increased AUC and Cmax by 4.25-fold and 1.75-fold, respectively.(1) Weak inhibitors of CYP3A4 include: alprazolam, amiodarone, amlodipine, asciminib, azithromycin, Baikal skullcap, belumosudil, berberine, bicalutamide, blueberry, brodalumab, cannabidiol, capivasertib, chlorzoxazone, cilostazol, cimetidine, ciprofloxacin, clotrimazole, cranberry, cyclosporine, daclatasvir, daridorexant, delavirdine, dihydroberberine, diosmin, everolimus, flibanserin, fosaprepitant, fostamatinib, gepotidacin, ginkgo, givinostat, glecaprevir/pibrentasvir, goldenseal, grazoprevir, isoniazid, istradefylline, ivacaftor, lacidipine, lapatinib, larotrectinib, lazertinib, leflunomide, levamlodipine, linagliptin, lomitapide, lurasidone, mavorixafor, olaparib, osilodrostat, palbociclib, pazopanib, peppermint oil, piperine, propiverine, propofol, ranitidine, ranolazine, remdesivir, resveratrol, roxithromycin, rucaparib, selpercatinib, simeprevir, sitaxsentan, skullcap, suvorexant, teriflunomide, ticagrelor, tolvaptan, trofinetide, viloxazine, and vonoprazan.(1,2)

DAYVIGO

Drug contraindication overview.

Linagliptin is contraindicated in patients with a history of hypersensitivity reaction (e.g., anaphylaxis, urticaria, angioedema, bronchial hyperreactivity) to linagliptin.

Adverse reaction overview.

Adverse effects reported in at least 5% of patients receiving linagliptin monotherapy include nasopharyngitis. Adverse effects reported in at least 2% of patients receiving linagliptin concomitantly with pioglitazone, a sulfonylurea, metformin, or basal insulin include nasopharyngitis, hyperlipidemia, cough, hypertriglyceridemia, weight gain, urinary tract infection, constipation, back pain, arthralgia, upper respiratory tract infection, headache, and pain in extremity. Adverse effects reported in at least 5% of patients receiving linagliptin and empagliflozin in clinical trials include urinary tract infection, nasopharyngitis, and upper respiratory tract infection. Adverse effects reported in at least 5% of patients receiving linagliptin and metformin hydrochloride in clinical trials include nasopharyngitis and diarrhea.

Safety and efficacy of linagliptin alone or in fixed combination with empagliflozin or fixed combination with immediate- or extended-release metformin hydrochloride have not been established in patients younger than 18 years of age.

Contraindicated

None

Severe Precaution

None

Management or Monitoring Precaution

None