Saxagliptin: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
Saxagliptin: clinical details
Prescribing considerations
- Licensed for adults with type 2 diabetes as monotherapy when metformin is inappropriate, or with other glucose-lowering treatments.
- Assess renal function before initiation and periodically.
- Use caution with a history of pancreatitis, heart failure or risk factors for heart-failure admission.
- Evidence is limited in immunocompromised people, including transplant recipients.
- Not recommended for children or adolescents because efficacy has not been established.
Contraindications and cautions
- Hypersensitivity to saxagliptin or an excipient.
- Previous serious hypersensitivity reaction, including anaphylaxis or angioedema, to any DPP-4 inhibitor.
Monitoring
- HbA1c and/or blood glucose response.
- Renal function before treatment and periodically thereafter.
- Hypoglycaemia with insulin or a sulphonylurea.
- Symptoms of pancreatitis or heart failure.
- Skin blistering, ulceration or rash; consider bullous pemphigoid.
- Unexplained severe joint pain.
Clinical pharmacology
Saxagliptin is a selective, reversible, competitive DPP-4 inhibitor. CYP3A4/5 mainly metabolises it to an active but less potent metabolite. Elimination occurs through renal and hepatic pathways.
Formulation and product differences
- The selected product is a yellow, round, biconvex film-coated tablet supplied in aluminium-containing blisters.
- The tablet must not be split or cut and is essentially sodium-free.
- No special storage conditions are required.
Saxagliptin preparations and strengths
Tablet
Route: Oral
Strengths: 2.5 mg
Saxagliptin interactions
Tell the prescriber or pharmacist about all medicines being used. Important examples include:
Insulin and sulphonylureas
Increase the risk of low blood sugar.
Carbamazepine, phenobarbital, phenytoin, rifampicin and dexamethasone
May reduce saxagliptin's glucose-lowering effect by increasing CYP3A4/5 activity.
Ketoconazole
Can substantially increase exposure to saxagliptin.
Diltiazem
Increases exposure to saxagliptin and should be considered during medication review.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.