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Canagliflozin; Uses, Dosage, Side Effects, Drug Interactions

Canagliflozin anhydrous is a Sodium-Glucose Cotransporter 2 Inhibitor. The mechanism of action of canagliflozin anhydrous is as a Sodium-Glucose Transporter 2 Inhibitor and P-Glycoprotein Inhibitor. Canagliflozin Anhydrous is the anhydrous form of canagliflozin, a C-glucoside with a thiophene ring that is an orally available inhibitor of sodium-glucose transporter 2 (SGLT2) with antihyperglycemic activity. Canagliflozin is also able to reduce body weight and has a low risk for hypoglycemia.

Canagliflozin is a medication used for the treatment of type 2 diabetes. It is of the gliflozin class or subtype 2 sodium-glucose transport (SGLT-2) inhibitors class. Canagliflozin belongs to a new class of anti-diabetic drugs that works by inhibiting the sodium-glucose transport protein (SGLT2). This transport protein is found in the kidney and is responsible for reabsorbing glucose that has been filtered. This mechanism is associated with a low risk of hypoglycemia (too low blood glucose) compared to sulfonylurea derivatives and insulin. In 2017, the FDA concluded that canagliflozin causes an increased risk of leg and foot amputations. The FDA began requiring a Boxed Warning to be added to the canagliflozin drug labels to describe this risk.

Mechanism of Action of Canagliflozin

Canagliflozin is an inhibitor of subtype 2 sodium-glucose transport proteins (SGLT2), which is responsible for at least 90% of renal glucose reabsorption (SGLT1being responsible for the remaining 10%). Blocking this transporter causes up to 119 grams of blood glucose per day to be eliminated through the urine, corresponding to 476 kilocalories. Additional water is eliminated by osmotic diuresis, resulting in a lowering of blood pressure. This mechanism is associated with a low risk of hypoglycemia (too low blood glucose) compared to other types of anti-diabetic drugs such as sulfonylurea derivatives and insulin.

Sodium-glucose co-transporter 2 (SGLT2), expressed in the proximal renal tubules, is responsible for the majority of the reabsorption of filtered glucose from the tubular lumen. Canagliflozin is an inhibitor of SGLT2. By inhibiting SGLT2, canagliflozin reduces reabsorption of filtered glucose and lowers the renal threshold for glucose (RTG), and thereby increases urinary glucose excretion (UGE).

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Indications of Canagliflozin

Type 2 Diabetes Mellitus
Canagliflozin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Use in type 1 diabetes mellitus patients or in the treatment of diabetic ketoacidosis is not recommended.
Canagliflozin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Use in type 1 diabetes mellitus patients or in the treatment of diabetic ketoacidosis is not recommended.
monotherapy when diet and exercise alone do not provide adequate glycaemic control in patients for whom the use of metformin is considered inappropriate due to intolerance or contraindications.
Add on therapy and on therapy with other glucose-lowering medicinal products including insulin, when these, together with diet and exercise, do not provide adequate glycaemic cont

Contra-Indications of Canagliflozin

Infection
Low blood sugar
Pituitary hormone deficiency
Decreased function of the adrenal gland
Inadequate vitamin B12
Excess body acid
Extreme loss of body water
The habit of drinking too much alcohol
Alcohol intoxication
Heart attack
Suddenly serious symptoms of heart failure
Liver problems
Recent operation
Fever
Shock
Severe vomiting
Severe diarrhea
Serious lack of oxygen in the blood
Weakened patient
Injury
Sepsis syndrome
X-Ray Study with intravenous iodine contrast agent
Kidney disease with a likely reduction in kidney function
Acute inflammation of the pancreas
Chronic inflammation of the pancreas
Moderate to Severe kidney impairment

Dosage of Canagliflozin

Strengths: 100 mg; 300 mg

Diabetes Type 2

Initial dose: 100 mg orally once a day
May increase to 300 mg orally once a day for additional glycemic control but only in patients who have tolerated lower dose and who have an eGFR of 60 mL/min/1.73 m2 or greater
Maximum dose: 300 mg/day

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Side Effects of Canagliflozin

Most common

Abdominal or stomach discomfort
increased urination.
low blood pressure,
difficult, burning, or painful urination
discharge with a strong odor from the penis
increased potassium blood levels (hyperkalemia),
low blood sugar (hypoglycemia), and
diarrhea
gas (flatulence)
symptoms of weakness, muscle pain (myalgia)
upper respiratory tract infection
low blood sugar (hypoglycemia)
abdominal pain (GI complaints), lactic acidosis (rare)
low blood levels of vitamin B-12
nausea, vomiting
chest discomfort
chills, dizziness
bloating/abdominal distention
constipation
heartburn

More common

Abdominal or stomach discomfort
a cough or hoarseness
decreased appetite
diarrhea
fast or shallow breathing
fever or chills
the general feeling of discomfort
lower back or side pain
muscle pain or cramping
painful or difficult urination

Less common

Abnormal stools
bad, unusual, or unpleasant (after) taste
change in taste
difficulty with moving
discoloration of the fingernails or toenails
flu-like symptoms
joint pain
rash
a runny nose
sneezing
stuffy nose
swollen joints

Drug Interactions of Canagliflozin

Canagliflozin may interact with following drugs, supplements & may decrease the efficacy of the drug

androgens (e.g., methyltestosterone, nandrolone, testosterone)
angiotensin-converting enzyme inhibitors (ACEIs; captopril, ramipril)
angiotensin receptor blockers (ARBs; e.g., candesartan, irbesartan, losartan)
angiotensin-converting enzyme inhibitors (ACEIs; captopril, enalapril, ramipril)
antipsychotic medications (e.g., chlorpromazine, haloperidol, olanzapine,
birth control pills
bupropion
atorvastatin
atypical antipsychotics (e.g., aripiprazole, clozapine, olanzapine; quetiapine, risperidone)
“azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
barbiturates (e.g., pentobarbital, phenobarbital)
crizotinib
cyclosporine
cyproterone
dabrafenib
corticosteroids (e.g., dexamethasone, prednisone)
diabetic drugs (e.g., glyburide, insulin, repaglinide, sitagliptin)
digoxin
diuretics (e.g., furosemide, hydrochlorothiazide)
HIV protease inhibitors (e.g., atazanavir, indinavir, ritonavir, saquinavir)
iodinated contrast material
phenytoin
quinolone antibiotics (e.g., levofloxacin, moxifloxacin)
selective serotonin reuptake inhibitors (SSRIs; citalopram, fluoxetine, sertraline paroxetine,
trimethoprim
sulfonamide antibiotics (“sulfas”; e.g., sulfisoxazole, sulfamethoxazole)
somatotropin
sulfamethoxazole
testosterone
verapamil

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Pregnancy & Lactation of Canagliflozin

FDA Pregnancy Category B

Pregnancy

This medication should not be used during pregnancy. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding

It is not known if canagliflozin passes into breast milk. Metformin passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Breast-feeding is not recommended when you are taking this medication.