| Class | Oral hypoglycaemic |
|---|---|
| Chemistry |
Dipeptidyl peptidase (DPP-4) inhibitor |
| Routes of administration |
Oral only |
| Absorption |
Completely absorbed, oral bioavailability 87% |
| Solubility |
pKa=8.7; good water solubility |
| Distribution |
VOD= 3-4 L/kg; 38% protein bound |
| Metabolism |
Hepatic metabolism plays a minor role in the elimination |
| Elimination |
79% excreted renally as unchanged drug |
| Time course of action |
Half life 8-14 hrs |
| Target receptor |
Dipeptidyl peptidase (DDP-4), an endothelial enzyme that normal breaks down regulatory peptides glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide 1(GLP-1). |
| Mechanism of action |
By decreasing the degradation of GLP-1, DPP-4 inhibitors produce an increase in insulin secretion. GLP-1 binds to its G-protein-coupled receptors on pancreatic β-cells, where it increases intracellular cAMP, and therefore the availability of intracellular calcium that drives insulin exocytosis |
| Clinical effects |
Hypoglycaemia, but also: |
| Literature reference |
Baetta & Corsini (2011). |
| CICM details of understanding | Not specifically listed in the CICM syllabus |
| Mentioned around Deranged Physiology | |
| Related SAQs |