Products
Canagliflozin is commercially available in the form of film-coated tablets (Invokana). It was approved in the United States and EU in 2013 and in many countries in 2014. Vokanamet is a fixed combination of canagliflozin and metformin. It was also registered in many countries in 2014.
Structure and properties
Canagliflozin (C24H25FO5S, Mr = 444.5 g/mol) is a C-glucoside and a fluorinated phenylthiophene derivative. It exists as canagliflozin hemihydrate and is practically insoluble in water. Canagliflozin is derived from phlorizin, a natural and nonselective SGLT inhibitor from apple tree bark.
Effects
Canagliflozin (ATC A10BX11) has antidiabetic and antihyperglycemic properties and may reduce weight. It is an inhibitor of sodium–glucose co-transporter 2 (SGLT2). This transporter is responsible for the reabsorption of glucose at the proximal tubule of the nephron. Inhibition leads to increased excretion of glucose via the urine. The mechanism of action is independent of insulin, unlike other antidiabetic agents.
Indications
For the treatment of type 2 diabetes mellitus.
Dosage
According to the professional information. Tablets are taken once daily before the first meal.
Contraindications
- Hypersensitivity
- Severe kidney disease
Full precautions can be found in the drug label.
Interactions
Canagliflozin is conjugated by UGT1A9 and UGT2B4. Drug-drug interactions have been described with UGT inducers such as rifampicin, phenytoin, phenobarbital, and ritonavir and with digoxin. Canagliflozin interacts poorly with CYP450.
Adverse effects
The most common potential adverse effects include vaginal thrush in women, urinary tract infections, and frequent urination. These side effects are due to the increased glucose concentration in the urine.
