Canagliflozin

ATC code

A10BK02

Therapeutic class

Sodium-glucose co-transporter 2 (SGLT2) inhibitor · Drugs used in diabetes, blood glucose lowering drugs, excl. insulins

Forms

film-coated tablet

Brand names

Invokana (EU) · Vokanamet (EU)

Overall confidence

high

Regulatory sources consulted

Approved indications

Treatment of adults and children aged 10 years and older with insufficiently controlled type 2 diabetes mellitus as an adjunct to diet and exercise: as monotherapy when metformin is considered inappropriate due to intolerance or contraindications; in addition to other medicinal products for the treatment of diabetes.

Contraindications

Absolute

Hypersensitivity to the active substance or to any of the excipients.

Clinical warnings

Major warning · Increased risk of lower limb amputations (primarily of the toe). Foot monitoring and management of risk factors such as neuropathy and peripheral vascular disease is crucial. — EMA SPC
Major warning · Rare but serious cases of diabetic ketoacidosis (DKA), including life-threatening cases, have been reported in patients treated with SGLT2 inhibitors. It may present with only moderately elevated blood glucose levels (euglycemic DKA). — EMA SPC

Drug interactions

ModerateRifampicinJ04AB02
Mechanism: Induction of UGT1A9 and UGT2B4 enzymes, which increases canagliflozin metabolism and reduces its systemic exposure (AUC).
Recommendation: Monitor glycemic control. If a patient on 100 mg of canagliflozin requires a UGT inducer, consider increasing the dose to 300 mg if well tolerated.
EMA SPC

Adverse events

Common (≥1%)

vulvovaginal candidiasis · urinary tract infection · polyuria or pollakiuria · hypoglycaemia (in combination with insulin or sulphonylurea) · constipation · thirst

Rare but serious

diabetic ketoacidosis · lower limb amputation · Fournier's gangrene (necrotising fasciitis of the perineum) · anaphylactic reaction · acute pancreatitis

Pregnancy and lactation

Pregnancy: Canagliflozin should not be used during pregnancy. Lactation: Canagliflozin should not be used during breast-feeding.

Recent literature (PubMed)

SGLT-2 inhibitors: A step forward in the treatment of heart failure with reduced ejection fraction.
Silva-Cardoso J, et al. · Rev Port Cardiol (Engl Ed) · 2021 · Relevance 4/5
Revisión que destaca el papel de los inhibidores de SGLT-2 como cuarto pilar en el tratamiento de la insuficiencia cardíaca con fracción de eyección reducida (ICFEr), basándose en los resultados de ensayos como DAPA-HF y EMPEROR-Reduced. Menciona los ensayos de seguridad cardiovascular de la clase (incluyendo CANVAS para canagliflozina) que mostraron una reducción en hospitalizaciones por IC, lo que impulsó esta nueva indicación.