linagliptin

Inhibits the enzyme dipeptidyl peptidase-4 (DPP-4), which slows the inactivation of incretin hormones, resulting in increased levels of active incretin hormones. These hormones are released by the intestine throughout the day, and are involved in regulation of glucose. Increased/prolonged incretin levels increase insulin release and decrease glucagon levels.

Therapeutic effects:

Improved control of blood glucose.

Pharmacokinetics ⬆ ⬇

Absorption: 30% absorbed following oral administration.

Distribution: Extensively distributed to tissues.

Metabolism/Excretion: Minimally metabolized; primarily excreted in feces (80%) and urine (5%) as unchanged drug.

Half-Life: >100 hr (due to saturable binding to DPP-4).

Time/Action Profile ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
PO	unknown	1.5 hr‡	24 hr

‡Blood level.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity. Cross-sensitivity may exist with sitagliptin, alogliptin, or saxagliptin;
Type 1 diabetes mellitus;
Diabetic ketoacidosis.

Use Cautiously in:

History of pancreatitis;
History of HF or renal impairment (↑ risk of HF);
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Safety and effectiveness not established in children;
Geri: Older adults may have risk of hypoglycemia.

Adv. Reactions/Side Effects ⬆ ⬇

CV: HF

Derm: bullous pemphigoid, localized exfoliation, urticaria

Endo: hypoglycemia

GI: ↑lipase, PANCREATITIS

Metab: hypertriglyceridemia

MS: arthralgia, RHABDOMYOLYSIS

Resp: bronchial hyperreactivity

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS, ANGIOEDEMA, AND EXFOLIATIVE SKIN CONDITIONS)

Interactions ⬆ ⬇

Drug-drug:

↑risk of hypoglycemia with sulfonylureas or insulin; dose ↓ of sulfonylurea or insulin may be necessary.
Concurrent use of P-glycoprotein or CYP3A4 inducers, including rifampin, may ↓ levels and effectiveness and should be avoided.

Route/Dosage ⬆ ⬇

PO (Adults ): 5 mg once daily.

Availability ⬆ ⬇

(Generic available)

Tablets: 5 mg
In combination with: empagliflozin (Glyxambi); empagliflozin and metformin XR (Trijardy XR); metformin (Jentadueto); metformin XR (Jentadueto XR). See Appendix [not included in this PDA edition].

Assessment ⬆ ⬇

Assess for signs and symptoms of hypoglycemic reactions (abdominal pain, sweating, hunger, weakness, dizziness, headache, tremor, tachycardia, anxiety).
Monitor for signs of pancreatitis (nausea, vomiting, anorexia, persistent severe abdominal pain, sometimes radiating to the back) during therapy. If pancreatitis occurs, discontinue linagliptin and monitor serum and urine amylase, amylase/CCr ratio, electrolytes, serum calcium, glucose, and lipase.
Monitor for arthralgia. Severe joint pain usually disappears with discontinuation of linagliptin.

Lab Test Considerations:

Monitor hemoglobin A1C prior to and periodically during therapy.
- May cause ↑ uric acid levels.

Implementation ⬆ ⬇

Do not confuse linagliptin with linaclotide. Do not confuse Tradjenta with Toujeo, Tresiba, or Trulicity.
Patients stabilized on a diabetic regimen who are exposed to stress, fever, trauma, infection, or surgery may require administration of insulin.
PO: May be administered without regard to food.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take linagliptin as directed. Take missed doses as soon as remembered, unless it is almost time for next dose; do not double doses. Advise patient to read the Medication Guide before starting and with each Rx refill in case of changes.
Explain to patient that linagliptin helps control hyperglycemia but does not cure diabetes. Therapy is usually long term.
Instruct patient not to share this medication with others, even if they have the same symptoms; it may harm them.
Encourage patient to follow prescribed diet, medication, and exercise regimen to prevent hyperglycemic or hypoglycemic episodes.
Review signs of hypoglycemia and hyperglycemia with patient. If hypoglycemia occurs, advise patient to take a glass of orange juice or 2–3 tsp of sugar, honey, or corn syrup dissolved in water, and notify health care professional.
Instruct patient in proper testing of blood glucose and urine ketones. These tests should be monitored closely during periods of stress or illness and health care professional notified if significant changes occur.
Advise patient to notify health care professional promptly if signs and symptoms of pancreatitis or if rash; hives; blisters; or swelling of face, lips, or throat occur.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications, especially other oral hypoglycemic medications.
Rep: Insulin is the recommended method of controlling blood sugar during pregnancy. Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected, or if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇