Sixtin 5

Indications

Saxagliptin is used with diet and exercise to improve blood sugar control in adults with type 2 diabetes. It can be used alone or together with other diabetes medicines such as Metformin, a sulfonylurea, a thiazolidinedione, Dapagliflozin or insulin. It is not used for type 1 diabetes or diabetic ketoacidosis.

How It Works

Saxagliptin blocks an enzyme called DPP-4. This enzyme normally breaks down gut hormones (incretins) that are released after meals. With more incretin activity, the pancreas releases more insulin and less glucagon when blood sugar is high, which lowers blood sugar, mainly after meals, with a low risk of hypoglycaemia when used alone.

Dosage and Administration

The usual adult dose is 5 mg once a day, with or without food, or as prescribed. A dose of 2.5 mg once a day is used in people with moderate or severe kidney disease or on dialysis, and in those taking strong CYP3A4 inhibitors such as Ketoconazole or Clarithromycin. Swallow the tablet whole; do not split or crush it. Take it at about the same time each day.

Interactions

• Sulfonylureas (such as Gliclazide, Glimepiride) and insulin: higher risk of low blood sugar; your doctor may lower their dose.
• Strong CYP3A4 inhibitors (Ketoconazole, Itraconazole, Clarithromycin, Ritonavir): raise Saxagliptin levels; use 2.5 mg.
• Strong CYP3A4 inducers (Rifampicin, Carbamazepine, Phenytoin): may reduce its effect.
• Corticosteroids, thiazide diuretics and some antipsychotics: may raise blood sugar.

Contraindications

• Previous serious allergic reaction to Saxagliptin or other DPP-4 inhibitors (such as anaphylaxis, angioedema or severe skin reactions).
• Type 1 diabetes or diabetic ketoacidosis.

Side Effects

Common effects include upper respiratory infections (cold-like symptoms), urinary tract infections, headache, joint or back pain, and swelling of the hands or feet. Low blood sugar can occur when it is combined with a sulfonylurea or insulin: signs include shaking, sweating, fast heartbeat, hunger and confusion.

Get urgent medical help if you have severe, persistent stomach pain spreading to the back with or without vomiting (possible pancreatitis); swelling of the face, lips or throat or trouble breathing; large blisters on the skin (bullous pemphigoid); shortness of breath, rapid weight gain or swollen legs (possible heart failure); or severe joint pain.

Pregnancy and Lactation

Not recommended in pregnancy; insulin is usually preferred for diabetes in pregnancy. It is not known whether it passes into breast milk, so discuss with your doctor before breastfeeding.

Precautions and Warnings

Tell your doctor if you have had pancreatitis, heart failure, or kidney or liver disease. Kidney function should be checked before starting and from time to time. Saxagliptin may slightly increase the risk of hospital admission for heart failure in people with heart or kidney disease. Keep a source of sugar with you if you also take a sulfonylurea or insulin, and keep up regular blood sugar checks, diet and exercise.

Overdose

Overdose is not expected to cause serious problems on its own, but contact a doctor. If taken with other diabetes medicines, watch for signs of low blood sugar and seek help.

Therapeutic Class

Oral antidiabetic, dipeptidyl peptidase-4 (DPP-4) inhibitor (gliptin).

Storage

Store below 30°C in a dry place, away from light and out of the reach of children.