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Introduction
Introduction
Dipeptidyl peptidase 4 (DPP-4) inhibitors are a group of antihyperglycemic medications used to manage type 2 diabetes mellitus, which is a significant risk factor for coronary disease, heart failure, stroke, and many other cardiovascular conditions.
This activity reviews the various drugs in this group, indications, contraindications, activity, adverse events, and other key elements of DPP-4 inhibitors therapy in the clinical setting. It also elaborates on the essential information needed by any interprofessional team member managing the care of patients with diabetes.
Mechanism of Action
Mechanism of Action
DPP-4 is a ubiquitous enzyme that acts on incretin hormones, mainly GLP-1 (glucagon-like peptide-1) and GIP (gastric inhibitory peptide), which maintain glucose homeostasis by increasing insulin secretion and decreasing glucagon secretion.
GLP-1 is a hormone secreted by enteroendocrine L cells of the small intestine, which lowers blood glucose by stimulating insulin secretion, reducing glucagon concentrations, and delaying gastric emptying.It has a half-life of fewer than 2 minutes.GIP is a hormone secreted in the stomach and proximal small intestine by neuroendocrine K-cells. Its half-life is approximately 7 minutes in healthy individuals and 5 minutes in individuals with type 2 diabetes.
These incretins are released within minutes of food intake, and DPP-4 degrades these hormones immediately due to their short half-life. By inhibiting the DPP-4 enzyme, DPP-4 inhibitors increase the levels of GLP-1 and GIP, which in turn increase beta-cell insulin secretion in the pancreas, thereby reducing postprandial and fasting hyperglycemia.
PREVAGLIP PLUS
Saxaptin
Kombiglyze
Inhiglip
Inhiglip
Glaptivia Plus
Galvus
Indication
Indication
Type 2 diabetes mellitus: Used in patients inadequately controlled on metformin monotherapy or when metformin is contraindicated or not tolerated.
Can be used as monotherapy or in combination with other oral agents such as metformin or SGLT-2 inhibitors, and also with injectable therapies including insulin.
Suitable for patients with impaired renal function, with dose adjustments as needed depending on the specific DPP-4 inhibitor and severity of renal impairment.
Not indicated for type 1 diabetes or diabetic ketoacidosis.
Contraindicated during pregnancy and lactation
Sides effect
Sides effect
Common side effects of DPP-4 inhibitors include gastrointestinal issues (nausea, diarrhea, constipation), headache, and nasopharyngitis. Hypoglycemia risk increases when combined with sulfonylureas.
Serious adverse reactions involve:
Severe joint pain/arthralgia (FDA warning; may require discontinuation)
Hypersensitivity reactions (angioedema, anaphylaxis, DRESS syndrome)
Skin reactions: exanthematous eruptions (healing in ~3 weeks post-discontinuation), vasculitis (rare, linked to sitagliptin), madarosis (eyelash loss)
Pancreatitis (debated risk; FDA/EMA find insufficient evidence but recommend monitoring)
Precautions and Contardications
Precautions and Contardications
Precautions for DPP-4 inhibitors
Renal impairment: Monitor eGFR in chronic kidney disease, as acute renal failure has been reported.
Heart failure: Avoid saxagliptin/alogliptin in high-risk patients (history of HF, recent ACS).
Hypersensitivity: Discontinue immediately if angioedema, anaphylaxis, or severe skin reactions (e.g., bullous pemphigoid) occur.
Infection risk: Monitor lymphocyte counts with saxagliptin if infections persist.
Pancreatitis: Monitor for abdominal pain; discontinue if pancreatitis is confirmed despite conflicting FDA/EMA assessments.
Concurrent ACE inhibitors: May exacerbate angioedema risk.
Elderly patients: Higher risk of renal impairment and hypoglycemia when combined with sulfonylureas.
Contraindications
History of hypersensitivity to the specific DPP-4 inhibitor.
Type 1 diabetes: Not approved for use.
Diabetic ketoacidosis: Avoid.
Special considerations
Joint pain: Discontinue if severe arthralgia develops (resolves within weeks post-cessation).
Drug monograph m pdf.pdfWord.pdfVildagliptin research.docxDocument.docx4_5981182850957844247.pdfReference:
Reference:
https://diabetesonthenet.com/diabetes-primary-care/prescribing-pearls-dpp4is/?utm_source=perplexity
https://elsevier.health/en-US/preview/dipeptidyl-peptidase-4-dpp-4-inhibitors?utm_source=perplexity
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