Names and pronunciation
(lin′a-glip′tin) Tradjenta, Trajenta
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Drug reference
(lin′a-glip′tin) Tradjenta, Trajenta
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Func. class.: Antidiabetic
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Chem. class.: Didipeptidyl pepti- dase-4 inhibitor
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Do not confuse: Tradjenta/Tanzeum/Tresiba/Trulicity
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ACTION: Slows the inactivation of incretin hormones; concentrations of the active, intact hormones are increased, thereby increasing and pro- longing the action of these hormones; incretin hormones are released by the intestine throughout the day, and levels are increased in response to a meal
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USES: Type 2 diabetes mellitus
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CONTRAINDICATIONS: Hyper- sensitivity to linagliptin, type 1 diabetes mellitus, diabetic ketoacidosis (DKA) Precautions: Pregnancy, breastfeed- ing, adolescents or children <18 yr, debilitated physical condition, malnu- trition, uncontrolled adrenal insuffi- ciency, pituitary insufficiency, hypo/ hyperthyroidism, diarrhea, gastropare- sis, GI obstruction, ileus, female hor- monal changes, high fever, severe psy- chologic stress, uncontrolled hypercortisolism, HF
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SIDE EFFECTS CNS: Headache EENT: Nasopharyngitis ENDO: Hypoglycemia, hyperuricemia, hypertriglyceridemia GI: Body weight loss, pancreatitis INTEG: Serious hypersensitivity reac tions, urticaria, angioedema, exfoliative dermatitis MISC: Arthralgia, back pain RESP: Bronchial hyperreactivity (with bronchospasm), nasopharyngitis, cough
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INTERACTIONS • Long-term treatment in combination with strong CYP3A4 inducers, may reduce glyce- mic lowering effect of linagliptin Increase: hypoglycemia—sulfonylureas, β-blockers, ACE inhibitors, angiotensin II receptor antagonists, disopyramide, guanethidine, cloNIDine, octreotide, fen- fluramine, dexfenfluramine, fibric acid derivatives, monoamine oxidase inhibi- tors (MAOIs), FLUoxetine, salicylates L Increase: masking of the signs and symp- toms of hypoglycemia—reserpine, β-blockers Increase: need for dosing change—cis- apride, metoclopramide, tegaserod, androgens, alcohol, lithium, quinolones Decrease: hypoglycemic effect—dextro- thyroxine, bumetanide, furosemide, ethacrynic acid, torsemide, estrogens, progestins, oral contraceptives, thyroid hormones, glucocorticoids, glucagon, carbonic anhydrase inhibitors, phenytoin, fosphenytoin, or ethotoin; atypical antipsy- chotics (ARIPiprazole, cloZAPine, OLAN- Zapine, QUEtiapine, risperiDONE, and ziprasidone), phenothiazine, niacin (nico- tinic acid), triamterene, thiazide diuretics Decrease: effect of linagliptin—CYP3A4 inducers (topiramate, rifabutin, pioglit azone, OXcarbazepine, carBAMazepine, nevirapine, modafinil, metyrapone, etra- virine, efavirenz, bosentan, barbiturates, aprepitant, fosaprepitant) Drug/Herb Decrease: linagliptin effect—St. John’s wort Drug/Lab Test Increase: uric acid Decrease: HbA1c level, fasting blood glucose
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DOSAGE AND ROUTES • Adult: PO 5 mg daily; when used with a sulfonylurea or insulin, a lower dose of the sulfonylurea may be necessary to minimize the risk of hypoglycemia
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Available forms: Tab 5 mg
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Administer: • Once daily; may give without regard to food • May require an increased dose in stress, fever, surgery, trauma • Store at room temperature
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Evaluate: • Therapeutic response: improving blood glucose level, A1c; decreasing polydipsia, polyphagia, polyuria, clear sensorium, ab- sence of dizziness
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CLINICAL CONSIDERATIONS Assess • Diabetes: monitor blood glucose, A1c during treatment to determine diabetes control; monitor for hypoglycemia: confu- sion, sweating, tachycardia, anxiety; hyper- glycemia: polydipsia, polyuria, polyphagia • CBC baseline and periodically during treatment; report decreased blood counts • Pancreatitis (rare): severe abdominal pain, nausea, vomiting; may be fatal; dis continue product immediately, use sup portive therapy; monitor amylase, lipase, electrolytes • Arthralgia: may be severe, but temporary • Pregnancy/breastfeeding: use only if clearly needed; use caution in breast- feeding, excretion is unknown
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Patient and caregiver information: • About the symptoms of hypo/hypergly- cemia and what to do about each; to have glucagon emergency kit available, to carry sugar packets • That product must be continued on a daily basis, about the consequences of discontinuing product abruptly; to take only as directed • To avoid OTC products unless ap- proved by prescriber • That diabetes is a lifelong illness, that product will not cure diabetes • To carry emergency ID with prescriber, condition and medications taken • To immediately report skin disorders, swelling, difficulty breathing, or severe abdominal pain • Pregnancy/breastfeeding: to notify provider if pregnancy is planned or sus- pected, or if breastfeeding
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PHARMACOKINETICS Extensively distributed to tissues, pro- tein binding is concentration-depen- dent, weak to moderate inhibitor of CYP3A4, half life of >100 hr; effective half-life 12 hr, 90% excreted unchanged, 85% excreted enterohepatic system urine (5%), rapidly absorbed, peak in 1.5 hr; bioavailability 30%
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• Adult: PO 5 mg daily; when used with a sulfonylurea or insulin, a lower dose of the sulfonylurea may be necessary to minimize the risk of hypoglycemia
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