sitagliptin

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 homeostasis. Increased/prolonged incretin levels result in an increase in insulin release and decrease in glucagon levels.

Therapeutic effects:

Improved control of blood glucose.

Pharmacokinetics ⬆ ⬇

Absorption: 87% absorbed following oral administration.

Distribution: Extensively distributed to tissues.

Metabolism/Excretion: Undergoes minor metabolism by the liver via the CYP3A4 and CYP2C8 isoenzymes to inactive metabolites; 87% excreted in the urine (79% as unchanged drug), with 13% excreted in the feces.

Half-Life: 12.4 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	rapid	1–4 hr	24 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Type 1 diabetes mellitus.

Use Cautiously in:

Renal impairment (↓ dose for CCr <45 mL/min);
History of pancreatitis;
History of angioedema to another DPP-4 inhibitor;
History of HF or renal impairment (↑ risk of HF);
OB: Safety not established in pregnancy; Safety not established in breastfeeding;
Pedi: Safety and effectiveness not established in children;
Geri: Consider age-related in renal function when determining dose in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

CV: HF

Derm: bullous pemphigoid, rash, STEVENS-JOHNSON SYNDROME (SJS), urticaria

EENT: nasopharyngitis

GI: diarrhea, nausea, PANCREATITIS

GU: acute renal failure

MS: arthralgia, back pain, myalgia, RHABDOMYOLYSIS

Neuro: headache

Resp: upper respiratory tract infection

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)

Interactions ⬆ ⬇

Drug-drug:

May slightly ↑ levels of digoxin; monitoring recommended.
↑risk of hypoglycemia when used with insulin, glyburide, glipizide, or glimepiride; may need to ↓ dose of insulin or sulfonylurea.

Route/Dosage ⬆ ⬇

PO (Adults ): 100 mg once daily.

Renal Impairment

PO (Adults ): CCr 30–<45 mL/min: 50 mg once daily; CCr <30 mL/min, hemodialysis, or peritoneal dialysis: 25 mg once daily.

Availability ⬆ ⬇

Tablets: 25 mg; 50 mg; 100 mg
In combination with: ertugliflozin (Steglujan); metformin (Janumet); metformin XR (Janumet XR). See Appendix [not included in this PDA edition].

Assessment ⬆ ⬇

Observe patient 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 sitagliptin and monitor serum and urine amylase, amylase/CCr ratio, electrolytes, serum calcium, glucose, and lipase.
Assess for rash periodically during therapy. May cause SJS. Discontinue therapy if severe or if accompanied with fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, hepatitis, and/or eosinophilia.

Lab Test Considerations:

Monitor hemoglobin A1C prior to and periodically during therapy.
- Monitor renal function prior to and periodically during therapy.

Implementation ⬆ ⬇

Do not confuse sitagliptin with saxagliptin or sumatriptan. Do not confuse Januvia with Jantoven or Janumet.
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 once daily without regard to food.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take sitagliptin 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 sitagliptin 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 stop taking sitagliptin and notify health care professional promptly if symptoms of hypersensitivity reactions (rash; hives; swelling of face, lips, tongue, and throat; difficulty in breathing or swallowing) or pancreatitis 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.
Rep: Advise females with reproductive potential to notify health care professional if pregnancy is planned or suspected, or if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇