Dapagliflozin 10mg

Dapagliflozin is an anti-diabetic medication. It is recommended for persons with Type 2 Diabetes mellitus as an addition to diet and exercise to improve glycaemic management.

Class of drug : sodium-glucose co-transporter 2 (SGLT2)                                      inhibitors.

Dose             : Dapagliflozin available in 5mg, 1omg and with                             the combination of metformin

Brand Name : Oxra 10mg, 5mg / forxiga 10mg, 5mg

MECHANISM OF ACTION

Dapagliflozin is a highly potent, selective and reversible inhibitor of sodium glucose con-transporter 2 (SGLT2) that improves glycaemic control in patients with diabetes mellitus and provides cardio renal benefits.

When dapagliflozin inhibits SGLT2, less glucose is reabsorption from the glomerular filtrate in the proximal renal tubule. This also reduces sodium reabsorption, which causes glucose and osmotic diuresis to be excreted in the urine.

In order to enhance tubulomer feedback and lower intraglomerular pressure, dapagliflozin is thought to improve the transport of salt to the distal tubule. A small drop in blood pressure, decrease in body weight, and an increase in hematocrit are additional side effects of SGLT2 inhibition with dapagliflozin.

By lowering renal glucose reabsorption and causing an excess of glucose to be excreted in the urine, dapagliflozin raises plasma glucose levels during fasting and after meals. This glucose excretion (Glucuretic Effect) is observed after the first dose, is continuous over the 24 hour dosing interval and is sustain for the duration of treatment.

The GFR and blood glucose level determine how much glucose the kidney removes through this process.

Thus in subjects with normal glucose dapagliflozin has a low propensity to cause hypoglycemia.

Dapagliflozin does not impair Endogenous glucose production in response to hypoglycemia. Insulin action and secretion are not related to dapagliflozin’s actions. In dapagliflozin clinical trials, improvements in beta cell activity (HOMA-2) have been noted over time.

Dapagliflozin is more than 1400 times more selective for SGLT2 than SGLT1 and does not block other glucose transporters that are crucial for the transfer of glucose into peripheral tissues. The major transporter in the gut responsible for glucose absorption.

Side effects:

• Urinary tract infection
• Nausea
• Genital infection
• Constipation
• Vomiting
• Loss of appetite
• Seizures
• Dizziness
• Increased thirst

How dapagliflozin affects the body.

Increase in amount of glucose excreted in the urine were observed in healthy subjects and in patients with type 2 diabetes mellitus following the administration of dapagliflozin. Approximately 70g of glucose was excreted in the urine per day (corresponding to 280kcal/day)at a dapagliflozin dose of 10mg/day in patients with type 2 diabetes mellitus for 12 weeks.

This glucose elimination rate approached the maxium glucose excretion observed at 20mg/day of dapagliflozin. Evidence of sustained glucose excretion was seen in patients with type 2 diabetes mellitus given dapagliflozin 10mg/day up to 2 years.

ABSORPTON :

Dapagliflozin is rapidly and well observed after oral administration and can be administrated with or without food. Maxium dapagliflozin plasma concentratons are usually attained within 2 hours after administration.

The absolute oral bioavailability of dapagliflozin following the administration of a 10mg dose 78%. In healthy people, food has a negligible impact on the pharmacokinetics of dapagliflozin.

DISTRIBUTION :

Dapagliflozin is approximately 91% protein bound. protein binding is not altered in various disease state. (e.g., renal or hepatic impairment).

EXCRETION :

Dapagliflozin and related metabolites are primarily eliminated via urinary excretion of which less than 2% is unchanged dapagliflozin. after administration of 50mg dapagliflozin dose 96% is recovered ; 75% in urine and 21% in faeces. in faeces, approximately 15% of the dose is excreted as parent drug.

Combination Therapy 

The combination of dapagliflozin and metformin was investigated initially, as an addition to metformin, in combination with sulfonylureas (glimepiride), insulin (with or without other oral antidiabetic therapy), sitagliptin (with or without metformin), saxagliptin plus metformin, as concomitant initiation therapy with saxagliptin added to metformin, and as concomitant initiation therapy with exenatide added to metformin.

ADVICE FROM EXPERTS ON DAPAGLIFLOZIN:

• To regulate blood sugar and prevent long-term problems, dapagliflozin is used either alone or in combination with other diabetes medications.
• Dehydration, or excessive fluid loss, may result from it, or it may make you need to urinate more frequently. Remain hydrated and drink plenty of water.
• Always have some fruit juice or sugary food on hand in case you interact hypoglycemia symptoms, which include shaking, anxiety, pale, chilled skin, and cold sweats.
• Regularly check your blood sugar while using this medication.
• Consult your physician right away if you suffer from severe feeling dizzy, joint discomfort, symptoms similar to a cold, or unexplained nausea or vomiting.

FAQ :

Is Dapagliflozin safe to use?

Yes, dapagliflozin is safe when taken as prescribed by a physician. It might, however, have certain side effects. It should be taken at the same time every day and at the prescribed dosage for best results.

What is dapagliflozin used for ?

Dapagliflozin is used to reduce blood glucose levels. Type 2 diabetes is characterized by insufficient insulin production or improper insulin use by the body. The resultant rise in blood sugar levels is experienced. Dapagliflozin functions by excreting extra sugar through your urine. In addition, it can aid in the prevention of heart disease.

What are the side effects of Dapagliflozin?

Dapagliflozin usage may result in symptoms like :

• Sore throat
• Frequent urination
• Genital infection
• Anxiety
• Seizures

*Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.