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This medicine contains important and useful components, as it consists of
Canagliflozin is available in the market in concentration.
Canagliflozin
Before starting Canagliflozin, it is critical for patients to consult their healthcare provider to ensure that this medication is appropriate for their condition. Canagliflozin is an SGLT2 inhibitor (sodium-glucose cotransporter 2 inhibitor) used primarily for the management of type 2 diabetes mellitus and chronic kidney disease. Some key precautions include:
- Renal Impairment: Canagliflozin is contraindicated in patients with severe renal impairment (e.g., eGFR <30 mL/min/1.73 m²) or those with end-stage renal disease (ESRD). This is because the medication relies on kidney function to be effective, and impaired kidneys may lead to ineffective drug action or toxicity.
- Hypotension and Dehydration: Canagliflozin can cause fluid loss through increased urination, leading to dehydration and hypotension (low blood pressure). Patients should be monitored for signs of dehydration, especially those who are elderly or have conditions like diarrhea, vomiting, or poor fluid intake.
- Diabetic Ketoacidosis (DKA): While rare, SGLT2 inhibitors like Canagliflozin can increase the risk of diabetic ketoacidosis (DKA), a serious complication where the body produces high levels of ketones. Patients should seek medical help if they experience symptoms like nausea, vomiting, abdominal pain, or rapid breathing.
- Genital Infections: Canagliflozin increases the risk of genital fungal infections due to the increased glucose in the urine, which provides a growth medium for microorganisms. Patients should maintain good hygiene and report any signs of infection, such as itching, redness, or discomfort in the genital area.
- Bone Fractures: Long-term use of Canagliflozin has been associated with an increased risk of bone fractures, particularly in patients with a history of bone disease or those at higher risk for fractures. Regular monitoring of bone health is advised.
- Pregnancy and Breastfeeding: The safety of Canagliflozin during pregnancy and breastfeeding has not been established. It is recommended to avoid the use of this medication during pregnancy, especially in the second and third trimesters, as it may harm the developing fetus. Consultation with a healthcare provider is essential for alternatives during these times.
Canagliflozin is primarily indicated for:
- Type 2 Diabetes Mellitus: Used as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. It works by inhibiting the SGLT2 protein in the kidneys, which helps to reduce glucose reabsorption and increase glucose excretion in urine, thereby lowering blood sugar levels.
- Chronic Kidney Disease (CKD): It is also approved for the treatment of chronic kidney disease in patients with type 2 diabetes, as it has been shown to slow the progression of kidney damage, reduce albuminuria, and improve overall kidney function.
- Cardiovascular Risk Reduction: Canagliflozin has been shown to lower the risk of cardiovascular events in individuals with type 2 diabetes, particularly in those with established heart disease. It helps reduce the incidence of heart attacks, stroke, and hospitalization due to heart failure.
Canagliflozin should not be used in the following situations:
- Severe Renal Impairment: Contraindicated in patients with severe renal impairment (e.g., eGFR <30 mL/min/1.73 m²), end-stage renal disease (ESRD), or those requiring dialysis as the drug is ineffective in such cases and may lead to accumulation in the body, increasing the risk of adverse effects.
- Hypersensitivity: Contraindicated in patients with a known hypersensitivity to canagliflozin or any of its components. This includes serious allergic reactions such as rash, swelling, or difficulty breathing.
- Diabetic Ketoacidosis (DKA): It is contraindicated in patients with a history of diabetic ketoacidosis or type 1 diabetes as it may worsen or trigger the condition.
- Severe Liver Disease: In patients with severe hepatic impairment, the use of canagliflozin should be avoided or used with extreme caution, as its safety and efficacy in these patients have not been established.
The common and severe side effects of Canagliflozin include:
- Genital Mycotic Infections: Increased glucose in the urine can lead to genital fungal infections, including vaginal yeast infections in women and balanitis (inflammation of the foreskin) in men. Patients should be educated on good hygiene practices.
- Urinary Tract Infections (UTIs): There is a slightly increased risk of urinary tract infections with Canagliflozin, which may present as painful urination, increased frequency, or urinary urgency.
- Hypotension: Due to its diuretic effects, Canagliflozin can cause low blood pressure, especially when starting treatment or when combined with other antihypertensive medications. Symptoms of hypotension may include dizziness, fainting, or lightheadedness.
- Dehydration: As a result of increased urination, Canagliflozin can lead to dehydration, which may present as dry mouth, thirst, weakness, or fatigue.
- Electrolyte Imbalance: The diuretic effects can cause electrolyte imbalances, such as low sodium (hyponatremia) or high potassium (hyperkalemia), which require monitoring.
- Diabetic Ketoacidosis (DKA): Though rare, Canagliflozin has been associated with an increased risk of diabetic ketoacidosis in people with type 2 diabetes. Symptoms of DKA include nausea, vomiting, abdominal pain, rapid breathing, and fruity-smelling breath.
- Bone Fractures: Long-term use of Canagliflozin may increase the risk of bone fractures, particularly in patients with other risk factors for osteoporosis or bone fractures.
- Acute Kidney Injury (AKI): Canagliflozin can lead to acute kidney injury, particularly in individuals with pre-existing kidney problems or those who experience dehydration.
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Canagliflozin works by inhibiting the SGLT2 protein in the kidneys, which plays a crucial role in the reabsorption of glucose from the urine back into the bloodstream. By blocking this transporter, Canagliflozin increases the excretion of glucose in the urine, leading to a reduction in blood glucose levels. This mechanism helps control hyperglycemia in type 2 diabetes mellitus. Additionally, Canagliflozin reduces the reabsorption of sodium, which leads to osmotic diuresis, helping to lower blood pressure and improve kidney function, particularly in patients with chronic kidney disease.
Canagliflozin may interact with several drugs or substances, including:
- Diuretics: The use of diuretics (particularly loop diuretics and thiazides) with Canagliflozin can increase the risk of dehydration and hypotension due to the additional fluid loss. Close monitoring of blood pressure and hydration status is recommended.
- RAAS Inhibitors: Angiotensin-converting enzyme (ACE) inhibitors, angiotensin receptor blockers (ARBs), and aldosterone antagonists can cause hyperkalemia (high potassium levels) and hypotension when used in conjunction with Canagliflozin. Monitoring of renal function and potassium levels is advised.
- Insulin and Insulin Secretagogues: Canagliflozin can increase the risk of hypoglycemia (low blood sugar) when used with insulin or insulin secretagogues (e.g., sulfonylureas). Patients may need to adjust the dosage of their insulin or oral hypoglycemic medications to prevent low blood sugar.
- Lithium: Coadministration with lithium may increase the risk of lithium toxicity due to the diuretic effects of Canagliflozin, which can alter lithium clearance and increase its concentration in the blood.
- CYP3A4 Inhibitors: Drugs that inhibit the CYP3A4 enzyme, such as ketoconazole and ritonavir, may increase canagliflozin levels, potentially increasing the risk of side effects. Dosing adjustments may be needed when using these agents together.
For adults with type 2 diabetes:
- The typical starting dose of Canagliflozin is 100 mg once daily, taken in the morning before or after a meal.
- If the 100 mg dose is well tolerated and more control is needed, the dose can be increased to 300 mg once daily.
- For patients with chronic kidney disease or those at higher risk for cardiovascular events, Canagliflozin is prescribed with consideration of kidney function and overall health status.
Canagliflozin is not recommended for use in pediatric patients, as its safety and efficacy in individuals under 18 years of age have not been established. Treatment with this medication should be limited to adults with type 2 diabetes mellitus or chronic kidney disease unless specifically prescribed by a healthcare provider for exceptional cases.
Canagliflozin is contraindicated in patients with severe renal impairment (e.g., eGFR <30 mL/min/1.73 m²), end-stage renal disease (ESRD), or those requiring dialysis. In patients with moderate renal impairment (e.g., eGFR between 30 and 60 mL/min/1.73 m²), the use of Canagliflozin should be approached with caution, and dose adjustments may be necessary. Regular monitoring of renal function is essential during treatment.