Indicated as an adjunct to diet and exercise to improve glycemic control in adults with type two diabetes mellitus.
Not recommended for patients with type one diabetes or for the treatment of diabetic ketoacidosis.
A sodium-glucose cotransporter 2 (SGLT 2) inhibitor.
Inhibits tubular glucose reabsorption, with glycosuria reducing serum blood glucose.
First drug in this new class of antidiabetic drugs.
SGLT2 is expressed in the proximal renal tubules and is responsible for the reabsorption of most glucose filtered by the kidney, and it’s inhibition reduces reabsorption of filtered glucose and lowers the renal threshold for glucose, increasing urinary glucose excretion and lowering blood glucose concentrations.
Patients with diabetes reabsorb more glucose than people without diabetes, and that further raises blood sugar.
This drug leads to loss of calories through the urine.
Contraindicated in patients with severe renal impairment, end-stage renal disease, or with patients on dialysis.
Reduces the absorption of glucose in the kidneys via sodium glucose co–transporter-2 (SGLT2) inhibition.
Symptomatic hypotension can occur, particularly in patients with impaired renal function, the elderly, in patients on diuretics or other medications that interfere with the renin-angiotensin-aldosterone system such as ACE inhibitors or angiotensin receptor blockers, or in patients with low systolic blood pressure.
Associated as mono therapy associated with significant A1 C reductions versus placebo at 26 weeks.
Provides statistically significant weight reductions versus placebo at 26 weeks.
Associated with significant systolic blood pressure lowering versus placebo at 26 weeks.
Associated with decreased risk of kidney failure and cardiovascular events.
Causes in the osmotic diuresis that may reduce intravascular volume and cause symptomatic hypotension particularly in patients with impaired real function, low blood pressure, older adults, patients on diuretics will medications interfere with the reunion angiotensin-aldosterone system such as Ace inhibitors and a RBS.
In patients with type two diabetes and renal disease, the risk of kidney failure and cardiovascular events is lower in a Canaliflozin group than in placebo group.
300 mg daily demonstrated greater A-1 C reduction versus sitagliptin 100 milligrams, in combination with metformin plus a sulfonylurea at 52 weeks.
As monotherapy associated with hypoglycemia approximately 3.6% over 26 weeks.
Starting dose 100 mg daily and can be increased to 300 mg in patients who have good tolerance to the hundred milligram dose and have a GFR of more than 60 mL per minute and require additional glycemic control.
Most common adverse reactions are female genital mycotic infections (UTIs) and increased urination.
May increase urinary tract infections in women and in males may increase gentle mycotic infections such as balanitis.
Can increase LDL cholesterol and can cause hypermagnesemia and hyperphosphatemia.
Hypersensitive reactions including rash, pruritus and angioedema experienced by 4% of patients.
Associated with a relatively increased risk for amputations compared to other SGLT agents.
Can increase serum creatinine and decrease GFR rates.
May lead to hyperkalemia especially in patients with moderate renal impairment who are on medicines that interfere with potassium excretion.
Can increase hypoglycemia in patients with insulin and insulin secretogues.
Coadministration with rifampin, a nonselective inducer of several UGT enzymes can decrease the area under the curve by 51%.
Can increase the area under the curve and peak drug concentration of digoxin.
Increases serum creatinine concentrations and decreases GFR and in patients with hypovolemia this may increase susceptibility.
Renal function assessment is recommended before initiation of therapy and periodically thereafter.
Treatment should not be initiated patients with a estimated GFR less than 45 mL per minute per 1.73 m².
The drug should be discontinued if the estimated GFR is persistently less than 45 ml/minute/1.73 m².
The drug causes an osmotic diuresis that may reduce intravascular blood volume and cause symptomatic hypotension.
Symptomatic hypotension may be seen in patients with impaired renal function, those with low systolic blood pressure, the elderly, or patients treated with diuretics or medications that interfere with the renin-angiotensin-aldosterone system such as ACE inhibitors and angiotensin receptor blockers.
Concurrent use of rifampin, ritonavir, phenobarbital may require higher dosage because these drugs may decrease this drug’s activity.
May increase digoxin levels.
Associated with a higher risk of pancreatitis and bone fractures than with comparator drugs.
Contraindicated in patients with severe renal impairment.
Periodic monitoring of serum potassium in patients with impaired renal function, and patients with ACE inhibitors or angiotensin receptor blockers is recommended.
Can increase LDL cholesterol, cause hyperkalemia, renal impairment, hypotension and genitourinary infections.
Canaliflozin Cardiovascular Assessment Study in patients with type two diabetes is the median follow up of 2.4 years sound a relative risk reduction of cardiovascular death, non-fatal myocardial infarction or non-fatal stroke by 14%.
In a controlled study of patients not optimally controlled on insulin and an oral anti-hyperglycemic agent receiving canagliflozin or placebo: at 28 days patients taking canagliflozin 300 mg b.i.d. had an average drop in hemoglobin A-1 C of 1% and a weight reduction of 2 1/2 pounds (Devineni et al ).