SGLT2 Inhibitor

The SGLT2 inhibitor (Gliflozins) lowers blood glucose levels by increasing the sugar excreted in the urine. Type 2 diabetes is managed using a class of drugs called SGLT2 inhibitors.

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What does the SGLT2 transporter do?

The Sodium-Glucose Co-Transporter 2 (SGLT2) protein is located largely in the kidneys, whereas the SGLT1 protein is found in the intestines. The kidneys are extremely effective glucose filters. The glucose transporter, SGLT2, is located in the kidneys. SGLT2’s major function is to reabsorb glucose from the urine back into the bloodstream, thereby preventing glucose loss in the urine. It reabsorbs 90% of the glucose and restores it to the bloodstream. Because SGLT are saturated with the filtered glucose, if the plasma glucose concentration is too high (hyperglycemia), glucose flows into the urine (glucosuria). This is how it works:

1. Glucose Filtration: As blood is filtered through the kidney, tiny molecules such as glucose are filtered into the renal tubules, where they eventually become urine.

2. Glucose Reabsorption: SGLT2 actively reabsorbs glucose from the renal tubules back into the circulation in the tubules. This transport is linked to the reabsorption of sodium ions (Na+). Because glucose and sodium co-transport, it is successfully carried back into the bloodstream against its concentration gradient.

After glucose and sodium are reabsorbed into the tubule cells by SGLT2, sodium is pumped out of the tubule cells and into the interstitial fluid by the sodium-potassium pump (Na+/K+ ATPase). This keeps the concentration gradient needed for glucose reabsorption going.

3. Glucose Homeostasis: By reabsorbing glucose from the filtrate, the SGLT2 transporter contributes to the body’s normal blood glucose levels. It ensures that glucose, a vital energy source, is not lost in the urine and is instead restored to circulation for use by the body’s cells.

What is the mechanism of action of SGLT2 inhibitors?

SGLT2 inhibitors, also known as sodium-glucose co-transporter 2 inhibitors, are a type of drug used to control blood glucose levels in type 2 diabetics. They act by inhibiting Sodium-Glucose Co-Transporter 2 (SGLT2), a protein found largely in the kidney’s proximal convoluted tubules. The following is how SGLT2 inhibitors regulate glucose:

1. Glucose Reabsorption Inhibition: The SGLT2 protein is normally responsible for actively reabsorbing glucose from urine back into the bloodstream in the kidneys. This procedure enables the body to recover glucose and prevents it from being lost in the urine. In people with type 2 diabetes, however, there is frequently an excess of glucose in the bloodstream (hyperglycemia). SGLT2 inhibitors are medications that prevent the SGLT2 protein from functioning. They do so by preventing glucose reabsorption from the renal tubules into the circulation. This significantly increases the amount of glucose excreted in the urine.

2. Increased Urinary Glucose Excretion: SGLT2 inhibition causes more glucose to be eliminated in the urine, lowering the quantity of glucose in the bloodstream. SGLT2 inhibitors reduce blood glucose levels in people with type 2 diabetes by limiting glucose reabsorption. This activity is insulin-independent and can be especially advantageous for people who have insulin resistance or low insulin production.

3. Weight Loss: In addition to glucose management, SGLT2 inhibitors may produce some weight loss since the calories in excreted glucose are wasted rather than used for energy.

In the United States, which medications are classified as SGLT2 inhibitors?

Several Sodium-Glucose Co-Transporter 2 (SGLT2) inhibitors were approved for use in the United States to treat type 2 diabetes, as of my most recent knowledge update in September 2021. New drugs, however, may have been licensed since then. It is critical to speak with a healthcare physician or review the most recent FDA information for the most up-to-date list of SGLT2 inhibitors available in the United States. Nonetheless, as of my latest update, the following SGLT2 inhibitors were available in the United States:

1. Canagliflozin (Invokana): Canagliflozin was one of the first FDA-approved SGLT2 inhibitors. It aids in the reduction of blood glucose levels by preventing glucose reabsorption in the kidneys. It comes in 100 mg and 300 mg tablet forms. Canagliflozin is taken before eating the first meal of the day.

2. Dapagliflozin (Farxiga): Dapagliflozin is another SGLT2 inhibitor used to treat type 2 diabetes in adults. Dapagliflozin pills come in 5 mg and 10 mg strengths.

3. Empagliflozin (Jardiance): Empagliflozin is approved for the treatment of type 2 diabetes in adults by blocking glucose reabsorption in the kidneys. Empagliflozin pills come in 10 mg and 25 mg strengths. Empagliflozin is taken in the morning once a day.

4. Ertugliflozin (Steglatro): Ertugliflozin is another SGLT2 inhibitor authorized for type 2 diabetic therapy. Ertugliflozin tablets come in 5 mg and 15 mg strengths. Ertugliflozin is taken once a day in the morning.

What are the consequences of SGLT2 inhibitors?

Sodium-Glucose Co-Transporter 2 (SGLT2) inhibitors are generally well-tolerated pharmaceuticals for type 2 diabetes management, although they, like all drugs, can have negative effects. SGLT2 inhibitors may cause the following adverse effects:

1. Genital Yeast Infections: Due to increased glucose in the urinary tract, which can promote yeast growth, some patients may develop genital yeast infections (e.g., vaginal yeast infections in women and balanitis in men).

2. Urinary Tract Infections (UTIs): UTIs, particularly bladder and kidney infections, are more common in those who take SGLT2 inhibitors.

3. Increased Urination: Because these drugs function by increasing glucose excretion in the urine, they might cause excessive urination, especially in the early stages of treatment.

4. Thirst and Dehydration: Increased urine might result in increased thirst and dehydration. It is critical to drink plenty of fluids while using SGLT2 inhibitors.

5. Hypotension (Low Blood Pressure): Some persons may experience a reduction in blood pressure, particularly upon rising from a sitting or reclining posture (orthostatic hypotension). This may cause dizziness or fainting.

6. Ketoacidosis: Although uncommon, SGLT2 inhibitors have been linked to an increased risk of diabetic ketoacidosis (DKA). DKA is a medical emergency characterized by excessive blood sugar, high blood ketone levels, and acidosis.

7. Variations in renal function: SGLT2 inhibitors might cause variations in the estimated glomerular filtration rate (eGFR), which assesses renal function. Your kidney function will be periodically monitored by your healthcare provider.

8. Bone Fractures: Some studies have suggested that SGLT2 inhibitors may increase the incidence of bone fractures, but additional study is needed to establish a definitive association.

9. Increased LDL Cholesterol: SGLT2 inhibitors may cause a little increase in low-density lipoprotein (LDL) cholesterol levels in some people.

Before beginning SGLT2 inhibitor therapy, it is critical to discuss any potential side effects and risks with your healthcare professional. Your doctor can help you decide if these medications are right for you and monitor your progress while you’re on them. Seek medical treatment right away if you encounter any unusual or severe adverse effects while using an SGLT2 inhibitor.

In summary, it’s worth noting that SGLT2 inhibitors are usually taken in conjunction with other diabetic drugs and lifestyle changes, including diet and exercise. They are not appropriate for all diabetics, and their usage should be reviewed with a healthcare physician. Dapagliflozin, canagliflozin, and empagliflozin are common SGLT2 inhibitors. SGLT2 inhibitors, like any drugs, may have negative effects, which users should be aware of and discuss with their healthcare provider.