Saxagliptin

Hypoglycaemic excluding Insulin · Dipeptidyl peptidase-4 inhibitor

Indications

Treatment of type II Diabetes in combination with metformin or glitazone, in patients inadequately controlled by diet, exercise and either metformin or glitazone alone or with sulphonylureas in patients with an intolerance or contraindicated to metformin, inadequately controlled by maximal tolerated dose of sulphonylureas alone.

Dosage

Adults: 5 mg once daily. In combination therapy, consider lower dose of sulphonylureas. Children: Not recommended.

Adverse Effects

Rash, URTI, UTI, GI upset, sinusitis, headache. With metformin: Nasopharyngitis, myalgia, arthralgia. With a sulphonylurea: Hypoglycaemia. With a glitazone: Peripheral oedema. With insulin: Hypoglycaemia.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Diabetic ketoacidosis, moderate to severe renal impairment, severe hepatic impairment. Congestive heart failure (NYHA class III-IV). Serious hypersensitivity reaction to dipeptidyl peptidase 4 inhibitor. Precautions: Congestive heart failure (NYHA class I-II). Immunocompromised patients, moderate hepatic impairment, moderate to severe renal impairment, elderly (= 75 years). Risk of pancreatitis, discontinue if suspected.

Interactions

Potent CYP3A4/5 inducers.

Advice to Patient

Take with or without meals. Contact prescriber if there is fever, trauma, infection, illness, surgery or other stress because blood glucose control may be altered requiring temporary insulin therapy. Follow diet and lifestyle changes as recommended by prescriber. Carry candy or other source of sugar at all times. During saxagliptin therapy, check the glucose level regularly.

Pharmacokinetics

Duration: 24 hrs. Metabolism: Hepatic. Half-life elimination: Saxagliptin: 2.5 hrs. 5-hydroxy saxagliptin: 3.1 hrs. Time to peak, plasma: Saxagliptin: 2 hrs. 5-hydroxy saxagliptin: 4 hrs. Excretion: Urine (75%). Faeces (22%).

Brands with this active ingredient

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.