saxagliptin hydrochloride: clinical use

Prescribing considerations

• Confirm type 2 diabetes; saxagliptin is not for type 1 diabetes, diabetic ketoacidosis or as a substitute for required insulin.
• Assess renal function before treatment and periodically; renal impairment affects exposure and product selection.
• Use caution with previous pancreatitis, heart failure risk factors, moderate hepatic impairment or severe joint symptoms.
• Review hypoglycaemia risk when used with insulin or a sulfonylurea.
• Monitor for blistering, ulceration or rash and investigate suspected bullous pemphigoid.

Contraindications and cautions

• Hypersensitivity to saxagliptin or an excipient.
• Previous serious hypersensitivity reaction, including anaphylaxis, anaphylactic shock or angioedema, to any DPP-4 inhibitor.
• The lactose-containing product must not be used in rare hereditary galactose intolerance, total lactase deficiency or glucose-galactose malabsorption.

Monitoring

• Glycaemic response, including appropriate glucose and HbA1c assessment.
• Renal function before initiation and periodically thereafter.
• Symptoms of pancreatitis, hypersensitivity, heart failure and severe joint pain.
• Skin changes such as blistering, erosion, ulceration or rash.
• Hypoglycaemia when combined with treatments capable of causing it.

Clinical pharmacology

Saxagliptin is a selective, reversible, competitive DPP-4 inhibitor. CYP3A4/5 forms an active metabolite with lower potency; parent medicine and metabolite are cleared through renal and hepatic pathways.

Formulation and product differences

• The selected product is a pink, round, film-coated tablet that must not be split or cut.
• It contains lactose monohydrate and is essentially sodium-free.
• It may be taken with or without food.

Tablet

Route: Oral

Strengths: 2.5 mg, 5 mg