dipeptidyl peptidase-4 (DDP-4) inhibitors
Adjunct to diet and exercise to improve glycemic control in type 2 diabetes mellitus.
Acts as a competitive inhibitor of dipeptidyl peptidase-4 (DPP-4) which slows the inactivation of incretin hormones, thereby increasing their concentrations and reducing fasting and postprandial glucose concentrations.
Improved control of blood glucose.
Absorption: Completely absorbed following oral administration (100%).
Distribution: Well distributed to tissues.
Metabolism and Excretion: Not extensively metabolized, 76% excreted unchanged in urine.
Half-life: 21 hr.
TIME/ACTION PROFILE (inhibition of DPP-4)
|PO||unknown||1–2 hr||24 hr|
- Type 1 diabetes;
- Diabetic ketoacidosis;
- Previous severe hypersensitivity reactions.
Use Cautiously in:
- Hepatic impairment;
- Renal impairment (dose ↓ required if CCr <60 mL/min);
- HF or renal impairment (↑ risk for worsening 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 ↑ sensitivity to effects.
Adverse Reactions/Side Effects
Derm: bullous pemphigoid, STEVENS-JOHNSON SYNDROME (SJS)
GI: ↑ liver enzymes, HEPATOTOXICITY, PANCREATITIS
MS: arthralgia, RHABDOMYOLYSIS
Misc: HYPERSENSITIVITY REACTIONS (including anaphylaxis or angioedema)
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
↑ risk of hypoglycemia with sulfonylureas and insulin ; dose adjustments may be necessary
PO (Adults): 25 mg once daily.
PO (Adults): CCr 30–59 mL/min: 12.5 mg once daily; CCr 15–29 mL/min: 6.25 mg once daily; CCr <15 mL/min or requiring hemodialysis: 6.25 mg once daily.
Tablets: 6.25 mg, 12.5 mg, 25 mg
In Combination with: metformin (Kazano), pioglitazone (Oseni).
- Observe 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 alogliptin and monitor serum and urine amylase, amylase/CCr ratio, electrolytes, serum calcium, glucose, and lipase.
- Assess for signs and symptoms of HF (increasing shortness of breath, rapid increase in weight, swelling of feet) periodically during therapy.
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 liver function tests prior to starting and periodically during therapy. Interrupt therapy and determine cause if significant ↑ in enzymes or abnormal tests persist or worsen. Do not restart therapy without explanation for abnormalities.
- Monitor renal function prior to and periodically during therapy.
- 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.
- Instruct patient to take alogliptin 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 Medication Guide before starting and with each Rx refill in case of changes.
- Explain to patient that alogliptin 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 alogliptin 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), liver dysfunction (fatigue, nausea, vomiting, anorexia, right upper abdominal discomfort, dark urine, yellowing of skin or whites of eyes), HF, 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.
- Instruct patient to notify health care professional if severe joint pain occurs.
- OB: Advise patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding.
Improved hemoglobin A1C, fasting plasma glucose and 2-hr postprandial glucose levels.