Introduction
Gliflozins inhibit renal glucose reabsorption by blocking the SGLT2 cotransporters in the proximal renal tubules and causing glucosuria. This reduces glycemia and lowers HbA1c by ~1.0%.
SGLT2 inhibitors are a class of prescription medicines that are FDA-approved for use with diet and exercise to lower blood sugar in adults with type II diabetes. Medicines in the SGLT2 inhibitor class include canagliflozin, dapagliflozin, and empagliflozin.
This class of drugs block SGLT-2 protein from the site of the proximal convoluted tubule (PCT) in the kidney, resulting in prevent reabsorption of a glucose molecule and allow excretion of glucose molecule through urine. SGLT-2 inhibitors are a class of medicine used to lower high blood glucose levels in people with type II diabetes. They may also be called gliflozins. SGLT-2 inhibitors inhibit SGLT-2 proteins located in the renal tubules of the kidneys which are responsible for reabsorbing glucose back into the blood. By this mechanism, the gliflozins drug lowers the blood glucose level in the body.
Gliflozins are useful for the treatment of Congestive Heart Failure and Renal Failure in Type II Diabetes.
Canagliflozin:
It is second most prescribed medication next to metformin.
Canagliflozin is in a class of medications called sodium-glucose co-transporter 2 (SGLT2) inhibitors. It lowers blood sugar by causing the kidneys to get rid of more glucose in the urine.
Additionally,it was found that empagliflozin 10mg/25mg rank the best and second choice in regarding to cardiovascular events risk reduction by SUCRA probabilities. It has been reported that SGLT2 inhibition decrease sodium reabsorption and increases urinary sodium excretion.
Compared with other approved SGLT2 inhibitors such as dapagliflozin, canagliflozin, empagliflozin, which have longer half-lives, a short elimination half-life and requires twice daily (BID) administration to obtain 24-h glucose-lowering effects.
Canagliflozin is a sodium-glucose cotransporter-2 (SGLT2) inhibitor.It works by increasing the amount of glucose lost in the urine.
Canagliflozin was approved for medical use in the United States, in the European Union, and in Australia in 2013.It is on the World Health Organization's List of Essential Medicines.In 2020, it was the 294th most commonly prescribed medication in the United States, with more than 1 million prescriptions.
Canagliflozin, sold under the brand name" Invokana" among others, is a medication used to treat type II diabetes. It is a third-line medication to be tried after metformin, a first-line medication for type II diabetes. It is used together with exercise and diet.
Canagliflozine is considered as latest magic drug, it reduces 40% chance of kidney failure,32 % chance of heart failure ,reduces paralysis by 11 % and risk of death by 11%.
Generally SGLT protein in kidney absorbs glucose back from urine in to the blood stream when blood sugar exceeds 180mg% during hyperglycemia.
SGLT2 inhibitors drug Canagliflozine blocks or inhibits SGLT2 protein when blood sugar exceeds 120 mg% and thus promotes excretion of excess sugar above 120mg% through urine and thus maintaining blood sugar up to 120 mg%.
Excess glucose excreted by drug deposits at external urinary orifice in both male and female as well as foreskin of genital organ in male predisposes to fungal infection of urinary tract.
Canagliflozine and other Gliflozins are not recommended in type I diabetes.
Common side effects include vaginal yeast infections, nausea, constipation, and urinary tract infections. Serious side effects may include low blood sugar, Fournier's gangrene, leg amputation, kidney problems, high blood potassium, and low blood pressure.Diabetic ketoacidosis may occur despite nearly normal blood sugar levels.Use in pregnancy and breastfeeding is not recommended.
Bladder pain.
bloating.
bloody or cloudy urine.
decreased frequency or amount of urine.
difficult, burning, or painful urination.
discharge with a strong odor from the penis.Also causes UTI in females.
frequent urge to urinate.
increased thirst.
FDA's Medical Review referred to these subgroups and to the AEs associated with these subgroups, writing, “Because canagliflozin increases urinary glucose excretion, it acts as an osmotic diuretic with an increase in urine output, and there was an increased incidence of adverse events related to intravascular volume .
Canagliflozin, Dapagliflozin and Empagliflozin are type II diabetes mellitus medicines of the class sodium-glucose co-transporter-2 (SGLT2) inhibitors. They block a protein in the kidneys called SGLT2, which absorbs glucose back from the urine into the bloodstream as the blood is filtered in the kidneys.The first SGLT2 inhibitor to be FDA-approved was canagliflozin (marketed as Invokana®) in March 2013, followed by the approval of Dapagliflozin (marketed as Farxiga®) in January 2014 and Empagliflozin (marketed as Jardiance®) in August 2014.
Empagliflozin is a potent SGLT2 inhibitor used to improve glycemic control in adults with Type II DM. It has the highest SGLT2 specificity among all the clinically used or currently tested SGLT2 inhibitors.
Dapagliflozin (brand name Farxiga®) and Empagliflozin (Jardiance®) are the first SGLT2 inhibitors to be approved by the U.S. Food and Drug Administration (FDA) for both type II diabetes and heart failure risk reduction.The CREDENCE and DAPA-CKD studies showed a significant reduction in the risk of CKD progression with the SGLT2 inhibitors Canagliflozine and Dapagliflozin in patients with CKD, with DAPA-CKD being the first trial to report that SGLT2 inhibitors are effective in patients with and without T2D for slowing CKD progression(chronic kidney disease)
Dapagliflozin (brand name Farxiga®) and Empagliflozin (Jardiance®) are the first SGLT2 inhibitors to be approved by the U.S. Food and Drug Administration (FDA) for both type II diabetes and heart failure risk reduction.
These newer drugs are in use since last decade. .Earlierwere very costly but now generic one are also available in the market.The drug is available in both injectable and tablet forms.
Information compiled by :
Dr. Bhairavsinh Raol
