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Friday, November 25, 2022

DAPAGLIFLOZIN



Dapagliflozin is a medication used to treat type 2 diabetes. It is also used to treat adults with heart failure and chronic kidney disease.

RS -32.00 FOR Dapagliflozine 10mg tab (for 10 tab)

AVAILABLE AT JAN AUSHADHI KOTTIYAM, JAN AUSHADHI

 KALLUMTHAZHAM, JAN AUSHADHI KANNANALLOOR,

JAN AUSHADHI MAYYANADU


Dapagliflozin is used along with diet, exercise and usually with other glucose lowering medications, to improve glycaemic control in adults with type 2 diabetes and to reduce the risk of hospitalisation for heart failure among adults with type 2 diabetes and known cardiovascular disease or other cardiovascular risk factors (including high blood pressure, high cholesterol and smokers). Dapagliflozin was also shown to reduce the rate of decline in kidney function and kidney failure in adults with type 2 diabetes, a finding that has recently been confirmed in both diabetic and non-diabetic populations. Dapagliflozin is also an important treatment option in patients with comorbid type 2 diabetes and heart failure with a reduced ejection fraction (on top of standard medical and/or device therapy), and lowers the risk of hospitalisation for heart failure and cardiovascular deaths in this group (as well as non-diabetic patients with HFrEF). All SGLT-2 inhibitors are useful to reduce the risk of hospitalisation for heart failure in people with atherosclerotic cardiovascular disease, however a small number of meta-analyses and cohort studies have shown that dapagliflozin is superior to others such as empagliflozin.

 

In addition, dapagliflozin is indicated for the treatment of adults with heart failure with reduced ejection fraction to reduce the risk of cardiovascular death and hospitalization for heart failure. It is also indicated to reduce the risk of kidney function decline, kidney failure, cardiovascular death and hospitalization for heart failure in adults with chronic kidney disease who are at risk of disease progression.

 

Mechanism of action

Dapagliflozin inhibits subtype 2 of the sodium-glucose transport proteins  which are responsible for at least 90% of the glucose reabsorption in the kidney. Blocking this transporter mechanism causes blood glucose to be eliminated through the urine. In combination with metformin, dapagliflozin at standard treatment dose of 10 mg daily lowered HbA1c by 0.54-0.84 percentage points when compared to metformin monotherapy in patients with inadequately controlled type 2 diabetes and normal renal function.

 

Regarding its protective effects in heart failure, this is attributed primarily to haemodynamic effects, where SGLT2 inhibitors potently reduce intravascular volume through osmotic diuresis and natriuresis. This consequently may lead to a reduction in preload and afterload, thereby alleviating cardiac workload and improving left ventricular function.

  


 

History

In 2012, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) issued a positive opinion on the drug.

In two studies involving 840 participants with type 2 diabetes, dapagliflozin when used alone decreased HbA1c levels by 0.66 percentage points more than placebo (a dummy treatment) after 24 weeks. In four other studies involving 2,370 participants, adding dapagliflozin to other diabetes medicines decreased HbA1c levels by 0.54–0.68 percentage points more than adding placebo after 24 weeks.

In a study involving 814 participants with type 2 diabetes, dapagliflozin used in combination with metformin was at least as effective as a sulphonylurea (another type of diabetes medicines) used with metformin. Both combinations reduced HbA1c levels by 0.52 percentage points after 52 weeks.

A long-term study, involving over 17,000 participants with type 2 diabetes, looked at the effects of dapagliflozin on cardiovascular (heart and circulation) disease. The study indicated that dapagliflozin's effects were in line with those of other diabetes medicines that also work by blocking SGLT2

 

In two studies involving 1,648 participants with type 1 diabetes whose blood sugar was not controlled well enough on insulin alone, adding dapagliflozin 5 mg decreased HbA1c levels after 24 hours by 0.37% and by 0.42% more than adding placebo.

Dapagliflozin was approved for medical use in the European Union in November 2012. It is marketed in a number of European countries.

 

Adverse effects

Since dapagliflozin leads to heavy glycosuria (sometimes up to about 70 grams per day) it can lead to rapid weight loss and tiredness. The glucose acts as an osmotic diuretic (this effect is the cause of polyuria in diabetes) which can lead to dehydration. The increased amount of glucose in the urine can also worsen the infections already associated with diabetes, particularly urinary tract infections and thrush (candidiasis). Rarely, use of an SGLT2 drug, including dapagliflozin, is associated with necrotizing fasciitis of the perineum, also called Fournier gangrene.

 

Absorption

Oral dapagliflozin reaches a maximum concentration within 1 hour of administration when patients have been fasting.

 

DRUG INTERACTIONS

Abacavir -     Dapagliflozin may increase the excretion rate of Abacavir which could result in a lower serum level and potentially a reduction in efficacy.

Abametapir -          The serum concentration of Dapagliflozin can be increased when it is combined with Abametapir.

Abatacept - The metabolism of Dapagliflozin can be increased when combined with Abatacept.

Abiraterone The serum concentration of Dapagliflozin can be increased when it is combined with Abiraterone.

Abrocitinib  The metabolism of Abrocitinib can be decreased when combined with Dapagliflozin.

Acarbose      Dapagliflozin may increase the hypoglycemic activities of Acarbose.

Acebutolol  The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Acebutolol.

Aceclofenac Dapagliflozin may increase the excretion rate of Aceclofenac which could result in a lower serum level and potentially a reduction in efficacy.

Acemetacin The therapeutic efficacy of Dapagliflozin can be decreased when used in combination with Acemetacin.

Acenocoumarol     The metabolism of Acenocoumarol can be decreased when combined with Dapagliflozin.

 

 

Food Interactions

Avoid excessive or chronic alcohol consumption. Binge drinking or drinking alcohol often may predispose patients to ketoacidosis.

Take with or without food.

 

 AVAILABLE BRANDS

JAN AUSHADHI  --- 32 RS FOR 10 TAB

ForxigaAstraZeneca - ₹438 to ₹4622 - 

Oxra  - ₹137 to ₹1802 

GledepaAbbott- ₹761 to ₹8022 

DapaoneMSN Laboratories - ₹110 to ₹1502 

DapamacMacleods - ₹120 to ₹1492 

DapanormAlkem Laboratories Ltd

₹139 to ₹1752 variant(s)

DamitaMacleods Pharmaceuticals Pvt Ltd

₹120 to ₹1492 variant(s)

DaparylIntas Pharmaceuticals Ltd

₹108 to ₹1302 variant(s)

DapaeaseJubilant Generics Limited

₹1451 variant(s)

DepajaIndoco Remedies Ltd

₹85 to ₹1152 variant(s)