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 and A1c.

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 inducers or CYP3A4 inducers, including rifampin, may ↓ levels and effectiveness; avoid concurrent use.

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), especially with use of insulin or an insulin secretagogue; dose adjustment may be required.
Assess for signs of HF (dyspnea, peripheral edema, rales/crackles, jugular venous distension) during therapy. Notify provider; may need to discontinue therapy.
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; however, may reoccur with another DPP-4 inhibitor.

Lab Test Considerations:

Monitor A1c twice yearly, every 3 mo when not meeting glycemic goals, or with change in 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 ⬆ ⬇

Explain the purpose and side effects of linagliptin. Instruct patient to take 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. Emphasize the importance of routine follow-up exams.
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 teaspoons of sugar, honey, or corn syrup dissolved in water, and notify health care provider.
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 provider notified if significant changes occur.
Warn patient to report symptoms and seek treatment for HF (trouble breathing, leg swelling, lung congestion, rapid weight gain).
Advise patient to notify health care provider promptly if signs and symptoms of pancreatitis or if rash; hives; blisters; or swelling of face, lips, or throat occur.
Advise patient to report severe and persistent joint pain; onset can occur 1 day to years after initiation and may require discontinuation of therapy.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care provider before taking other medications, especially other oral hypoglycemic medications.
Rep: Insulin is the recommended method of controlling blood sugar during pregnancy. Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected or if breastfeeding.

section name header

Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇