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Brand Name :
Invokana
(United States) [Available]Synonyms :
canagliflozina
Class :
Antidiabetics, SGLT2 Inhibitors
Brand Name :
Invokana
(United States) [Available]Synonyms :
canagliflozina
Class :
Antidiabetics, SGLT2 Inhibitors
Dosage Forms & StrengthsÂ
TabletÂ
100mgÂ
300mgÂ
100 mg orally once daily. Take medicine before breakfast
Increase to 300 mg orally each day if required
If a patient can tolerate 100 mg/day and have a rate of eGFR ≥60 mL/min/1.73 m²
The drug is indicated in addition to exercise and diet. It helps improve the blood glucose level in type 2 diabetes mellitus
Dosage Modifications
In the case of renal impairment
When eGFR is more than 60 mL/min/1.73 m2 no dose adjustment is required
When eGFR ranges from 30 to 60 mL/min/1.73 m2 the dose is kept at 100 mg each day
When eGFR is less than 30 mL/min/1.73 m2 with albuminuria that is more than 300 mg/day, 100 mg dose each day for the reduction of risk of various conditions. These conditions may include end-stage kidney disease, cardiovascular death, doubling of serum creatinine level, and hospitalization for heart failure
When eGFR is less than 30 mL/min/1.73 m2, drug initiation is not recommended
Safety and efficacy are not seen in pediatric patients Â
A higher incidence of adverse reactions is found in patients more than 75 years of ageÂ
These reactions are related to hypotension, syncope, postural dizziness, dehydration, and orthostatic hypotensionÂ
may diminish the serum concentration of primidone
may diminish the serum concentration of PHENobarbital
rifampin: they may diminish the serum concentration of canagliflozin
fosphenytoin: they may diminish the serum concentration of canagliflozin
phenytoin: they may diminish the serum concentration of canagliflozin
rifampin: they may diminish the serum concentration of canagliflozin
primidone: they may diminish the serum concentration of canagliflozin
ritonavir: they may diminish the serum concentration of canagliflozin
choline magnesium trisalicylate
may increase the hypoglycaemic effect
it may diminish the excretion rate when combined with permethrin, resulting in an enhanced serum level
When medrysone is used in conjunction with canagliflozin, the risk or seriousness of hyperglycemia can rise
canagliflozin has the potential to reduce the rate of excretion of idebenone, leading to an elevation in levels of serum
canagliflozin: they may enhance the serum concentration of digoxin
canagliflozin: they may increase the hypotensive effect of loop diuretics
canagliflozin: they may increase the hypotensive effect of loop diuretics
canagliflozin: they may increase the hypotensive effect of loop diuretics
canagliflozin leads to a reduction in the rate of excretion of eucalyptus oil which leads to increased level of serum
cefpirome leads to a reduction in the rate of excretion of canagliflozin which leads to increased level of serum
canagliflozin leads to a reduction in the rate of excretion of chromous sulfate, which leads to an increased level of serum
canagliflozin: it may decrease the metabolism of barnidipine
canagliflozin: it may increase the risk or severity of QTc prolongation agents
canagliflozin: it may increase the risk or severity of QTc prolongation agents
canagliflozin: it may increase the risk or severity of QTc prolongation agents
canagliflozin: it may increase the risk or severity of QTc prolongation agents
canagliflozin: it may increase the risk or severity of QTc prolongation agents
canagliflozin: it may increase the hypoglycemic activities of sulfamethoxazole
canagliflozin may decrease the excretion rate of almasilate, leading to higher serum levels
When helometasone is used together with canagliflozin, this leads to elevated risk or seriousness of hyperglycemia
When canagliflozin is used together with diazoxide, this leads to reduction in therapeutic effectiveness of canagliflozin
methylprednisolone hemisuccinateÂ
When methylprednisolone hemisuccinate is aided with canagliflozin, this leads to elevated hyperglycemia risk
Selective Serotonin Reuptake Inhibitors may enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects
Selective Serotonin Reuptake Inhibitors may enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects
Selective Serotonin Reuptake Inhibitors may enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects
Selective Serotonin Reuptake Inhibitors may enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects
Selective Serotonin Reuptake Inhibitors may enhance the hypoglycemic effect of Agents with Blood Glucose Lowering Effects
may increase the hypoglycemic effect
may increase the hypoglycemic effect
may increase the hypoglycemic effect
may increase the hypoglycemic effect
may increase the hypoglycemic effect
it decreases the efficacy of antidiabetic agents
It may enhance serum potassium levels when combined with pentamidine
the risk of hyperglycemia may be increased
etoricoxib: it may decrease the excretion rate of canagliflozin
the anti-diabetic efficacy of canagliflozin can be reduced with mometasone furoate
the hypoglycemic effect of canagliflozin may be increased
Actions and Spectrum:Â
canagliflozin is a medication that belongs to a class of drugs known as sodium-glucose cotransporter 2 (SGLT2) inhibitors. It is primarily used to treat type 2 diabetes alone or in combination with other medications, diet, and exercise.Â
The drug works by inhibiting SGLT2, a protein in the kidneys that helps to reabsorb glucose back into the bloodstream. By blocking SGLT2, canagliflozin prevents the kidneys from reabsorbing glucose, leading to increased urinary excretion of glucose and reduced blood sugar levels.Â
In addition to its glucose-lowering effects, canagliflozin has other benefits, including weight loss and blood pressure reduction. It has been shown to improve cardiovascular outcomes in patients with type 2 diabetes with a high risk of cardiovascular disease.Â
canagliflozin is usually taken orally once a day, with or without food. It is metabolized in the liver and excreted primarily in the urine.Â
Frequency DefinedÂ
>10%Â
Mycotic infection in female genitalsÂ
1-10%Â
Urinary tract infections Â
Increased urination Â
Constipation Â
NauseaÂ
Male genital mycotic infectionsÂ
Thirst Â
Contraindication/Caution:Â
canagliflozin is generally well-tolerated by most people, but there are some situations where its use is contraindicated or caution is needed. These include:Â
Pregnancy consideration:Â Â
It is not secure to administer canagliflozin during pregnancy.Â
Breastfeeding warnings:Â Â
No data is available about the excretion of canagliflozin in human breastmilk. Avoid using in lactating women.Â
Pregnancy category:Â
Pharmacology:Â
canagliflozin is a selective sodium-glucose cotransporter 2 (SGLT2) inhibitor used to treat type 2 diabetes. The drug works by inhibiting glucose reabsorption in the kidneys, leading to increased urinary glucose excretion and reduced blood glucose levels.Â
SGLT2 is a protein that is responsible for reabsorbing glucose in the kidneys. When glucose is filtered through the kidneys, SGLT2 helps to reabsorb most of it back into the bloodstream. canagliflozin blocks the action of SGLT2, which allows glucose to be excreted in the urine, leading to a decrease in blood glucose levels.Â
canagliflozin is absorbed rapidly after oral administration and reaches peak plasma concentration within one to two hours. Several enzymes metabolize the drug in the liver, including CYP3A4, CYP2C9, and UGT1A9. The primary metabolite is a glucuronide conjugate excreted in the urine.Â
The half-life of canagliflozin is approximately 10.6 hours, primarily eliminated through the urine. The drug can be taken with or without food, and the dosage may need to be adjusted in patients with renal impairment.Â
Glucose Control: canagliflozin works by inhibiting the Â
SGLT2 protein in the kidneys, leading to increased urinary glucose excretion and a reduction in blood glucose levels. This mechanism of action has been shown to improve glycemic control in patients with type 2 diabetes.Â
Weight Loss: canagliflozin has been associated with weight loss in patients with type 2 diabetes. The drug promotes the urinary excretion of glucose, which leads to a loss of calories. Additionally, canagliflozin may reduce appetite and increase satiety, contributing to weight loss.Â
Blood Pressure: canagliflozin has been shown to have a blood pressure-lowering effect, which is thought to be due to its diuretic action. The drug increases urinary sodium and water excretion, reducing blood volume and blood pressure.Â
Cardiovascular Outcomes: canagliflozin has been shown to improve cardiovascular outcomes in patients with type 2 diabetes who are at high risk for cardiovascular disease. In clinical trials, canagliflozin has been associated with a reduced risk of cardiovascular events, such as heart attack, stroke, and cardiovascular death.Â
Pharmacokinetics:Â
AbsorptionÂ
The bioavailability is 65%Â
The peak plasma concentration is achieved in 1-2 hoursÂ
DistributionÂ
99% of protein predominantly binds to albuminÂ
The volume of distribution is 119LÂ Â
MetabolismÂ
UGT1A9 and UGT2B4 metabolically eliminate the drug into 2 inactive metabolites O-glucuronide Â
Elimination and Excretion Â
The half-life is 10.6 hours (for 100 mg dose) and 13.1 hours (for 300 mg dose)Â
The rate of total body clearance is 192 mL/minÂ
The drug is excreted 41% in feces and 33% in urineÂ
Administration:Â
canagliflozin is available as an oral tablet and should be taken once daily in the morning, with or without food. The usual starting dose is 100 mg once daily, which may be increased to 300 mg once daily for patients who require additional glycemic control.Â
canagliflozin should be taken each day simultaneously to maintain a consistent level of the drug in the body. The tablet should be swallowed whole, not crushed, chewed, or split.Â
The dosage of canagliflozin may need to be adjusted in patients with renal impairment. The drug is not recommended for patients with severe renal impairment (eGFR <30 mL/min/1.73 m2) or end-stage renal disease.Â
It is essential to monitor blood glucose levels regularly when taking canagliflozin, particularly during the first few weeks of treatment, to ensure glycemic control and identify any potential adverse effects. In addition, patients taking canagliflozin should also be monitored for signs of dehydration, such as thirst, dry mouth, and dark urine.Â
Patient information leafletÂ
Generic Name: canagliflozinÂ
Pronounced: KAN-a-gli-FLOE-zinÂ
Why do we use canagliflozin?Â
canagliflozin is used to treat type 2 diabetes mellitus in adults as an adjunct to diet and exercise. It is indicated for improving glycemic control in patients with type 2 diabetes by reducing blood glucose levels. Canagliflozin works by inhibiting the sodium-glucose cotransporter 2 (SGLT2) protein in the kidneys, leading to increased urinary glucose excretion and reduced blood glucose levels.
canagliflozin is often used when other medications for type 2 diabetes have not provided adequate glycemic control or have caused intolerable side effects. Additionally, canagliflozin may offer additional benefits, such as weight loss and blood pressure reduction, making it a valuable option for patients with type 2 diabetes who also have obesity or hypertension.Â
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