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DAPACOSE

Dapacose (Dapagliflozin) is an SGLT-2 inhibitor drug, which is indicated in adults for the treatment of insufficiently controlled type 2 diabetes mellitus as an adjunct to other medications as well as diet and exercise. Dapagliflozin is also used adults for the treatment of symptomatic chronic heart failure with reduced ejection fraction with or without Diabetes. The drug is also used for the treatment of Chronic Kidney Disease( CKD) patients upto Stage III (eGFR of greater or equal to 30ml/min/1.73m2.)

Dapacose is marketed by JB Chemical and Pharmaceuticals limited and comes in two doses namely DAPACOSE 5mg and DAPACOSE 10mg.

Dapagliflozin inhibits the sodium-glucose contransporter 2 (SGLT2) which is primarily located in the proximal tubule of the nephron. SGLT2 facilitates 90% of glucose resorption in the kidneys and so its inhibition allows for glucose to be excreted in the urine. This excretion allows for better glycemic control and potentially weight loss in patients with type 2 diabetes mellitus.

Dapagliflozin is also used to reduce the risk of the need for hospitalization for heart failure in adults who have type 2 diabetes along with heart and blood vessel disease or who have multiple risk factors for developing heart and blood vessel disease. Recent evidence has also shown that the drug halts the progression of CKD in patients with, or without diabetes.

Overview
Name of Product: Dapacose 5mg/10mg
Marketed by : J.B. Chemicals & Pharmaceuticals Ltd.
Medicine composition: Dapagliflozin ….. 5 mg/10mg
Prescription vs.OTC: Prescription by Doctor required
Dosage Form: Film coated tablets

Dapacose is a sodium-glucose cotransporter 2 (SGLT2) inhibitor indicated in adults for:


Type 2 Diabetes Mellitus:


• as an adjunct to diet and exercise to improve glycemic control.

• to reduce the risk of hospitalization for heart failure in adults with type 2 diabetes mellitus and established cardiovascular disease or multiple cardiovascular risk factors.


Heart Failure:


• to reduce the risk of cardiovascular death and hospitalization for heart failure in adults with heart failure with reduced ejection fraction (NYHA class II-IV)


CKD

Dapagliflozin is also indicated in Chronic Kidney Disease( CKD) patients upto Stage III (eGFR of greater or equal to 30ml/min/1.73m2.


Type 2 Diabetes Mellitus


• To improve glycemic control the recommended starting dose is 5 mg once daily, taken in the morning. Increase dose to 10 mg once daily in patients tolerating 5 mg who require additional glycemic control.


• To reduce the risk of hospitalization for heart failure in adults with type 2 diabetes mellitus and established cardiovascular disease or multiple cardiovascular risk factors, the recommended dose is 10 mg once daily.


• Dapacose is not recommended for glycemic control when the eGFR is less than 45 mL/min/1.73 m2.


Heart Failure:


• The recommended dose of Dapacose is 10 mg once daily.

Dapacose is contraindicated in many conditions including the following


• History of serious hypersensitivity reaction to Dapaglifloszin


• Severe renal impairment (eGFR less than 30 mL/min/1.73 m2) in patients who are being treated for glycemic control without established cardiovascular disease or cardiovascular risk factors


• Patients on dialysis


Download the Product Leaflet, to see the detailed information on detailed Contraindications of Dapacose.

Some of the warning and precautions of Dapacose include.


• Volume depletion: Before initiating Dapagliflozin, assess volume status and renal function in the elderly, patients with renal impairment or low systolic blood pressure, and in patients on diuretics. Monitor for signs and symptoms during therapy.


• Ketoacidosis in Patients with Diabetes Mellitus: Assess patients who present with signs and symptoms of metabolic acidosis for ketoacidosis regardless of blood glucose level. If suspected, discontinue Dapacose, evaluate and treat promptly. Before initiating Dapacose, consider risk factors for ketoacidosis. Patients on Dapacose may require monitoring and temporary discontinuation of therapy in clinical situations known to predispose to ketoacidosis.


• Urosepsis and Pyelonephritis: Evaluate for signs and symptoms of urinary tract infections and treat promptly, if indicated.


• Hypoglycemia: Consider a lower dose of insulin or the insulin secretagogue to reduce the risk of hypoglycemia when used in combination with Dapacose.


• Necrotizing Fasciitis of the Perineum (Fournier’s Gangrene): Serious, life-threatening cases have occurred in patients with diabetes, both females and males. Assess patients presenting with pain or tenderness, erythema, or swelling in the genital or perineal area, along with fever or malaise. If suspected, institute prompt treatment.


• Genital Mycotic Infections: Monitor and treat if indicated.


Download the Product Leaflet, to see the detailed information on detailed Warnings and Precautions of Dapacose.

Pharmacodynamic interactions


Diuretics


Dapagliflozin may add to the diuretic effect of thiazide and loop diuretics and may increase the risk of dehydration and hypotension.


Insulin and insulin secretagogues


Insulin and insulin secretagogues, such as sulphonylureas, cause hypoglycaemia. Therefore, a lower dose of insulin or an insulin secretagogue may be required to reduce the risk of hypoglycaemia when used in combination with dapagliflozin in patients with type 2 diabetes mellitus.


Pharmacokinetic interactions


The metabolism of dapagliflozin is primarily via glucuronide conjugation mediated by UDP glucuronosyltransferase 1A9 (UGT1A9).
In in vitro studies, dapagliflozin neither inhibited cytochrome P450 (CYP) 1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP3A4, nor induced CYP1A2, CYP2B6 or CYP3A4. Therefore, dapagliflozin is not expected to alter the metabolic clearance of coadministered medicinal products that are metabolised by these enzymes.

Effect of other medicinal products on dapagliflozin


Interaction studies conducted in healthy subjects, using mainly a single-dose design, suggest that the pharmacokinetics of dapagliflozin are not altered by metformin, pioglitazone, sitagliptin, glimepiride, voglibose, hydrochlorothiazide, bumetanide, valsartan, or simvastatin.


Following coadministration of dapagliflozin with rifampicin (an inducer of various active transporters and drug-metabolising enzymes) a 22% decrease in dapagliflozin systemic exposure (AUC) was observed, but with no clinically meaningful effect on 24-hour urinary glucose excretion. No dose adjustment is recommended. A clinically relevant effect with other inducers (e.g. carbamazepine, phenytoin, phenobarbital) is not expected.


Following coadministration of dapagliflozin with mefenamic acid (an inhibitor of UGT1A9), a 55% increase in dapagliflozin systemic exposure was seen, but with no clinically meaningful effect on 24-hour urinary glucose excretion. No dose adjustment is recommended.


Effect of dapagliflozin on other medicinal products


In interaction studies conducted in healthy subjects, using mainly a single-dose design, dapagliflozin did not alter the pharmacokinetics of metformin, pioglitazone, sitagliptin, glimepiride, hydrochlorothiazide, bumetanide, valsartan, digoxin (a P-gp substrate) or warfarin (S-warfarin, a CYP2C9 substrate), or the anticoagulatory effects of warfarin as measured by INR. Combination of a single dose of dapagliflozin 20 mg and simvastatin (a CYP3A4 substrate) resulted in a 19% increase in AUC of simvastatin and 31% increase in AUC of simvastatin acid. The increase in simvastatin and simvastatin acid exposures are not considered clinically relevant.


Interference with 1,5-anhydroglucitol (1,5-AG) assay


Monitoring glycaemic control with 1,5-AG assay is not recommended as measurements of 1,5-AG are unreliable in assessing glycaemic control in patients taking SGLT2 inhibitors. Use of alternative methods to monitor glycaemic control is advised.


Paediatric population


Interaction studies have only been performed in adults.


Download the Product Leaflet, , to see the details on Drug Interactions of Dapacose.

Dapagliflozin did not show any toxicity in healthy subjects at single oral doses up to 500 mg (50 times the maximum recommended human dose). These subjects had detectable glucose in the urine for a dose-related period of time (at least 5 days for the 500 mg dose), with no reports of dehydration, hypotension or electrolyte imbalance, and with no clinically meaningful effect on QTc interval. The incidence of hypoglycaemia was similar to placebo. In clinical studies where once-daily doses of up to 100 mg (10 times the maximum recommended human dose) were administered for 2 weeks in healthy subjects and type 2 diabetes subjects, the incidence of hypoglycaemia was slightly higher than placebo and was not dose-related. Rates of adverse events including dehydration or hypotension were similar to placebo, and there were no clinically meaningful dose-related changes in laboratory parameters, including serum electrolytes and biomarkers of renal function.


In the event of an overdose, appropriate supportive treatment should be initiated as dictated by the patient’sclinical status. The removal of dapagliflozin by haemodialysis has not been studied.


Download the Product Leaflet, , to see the detailed information on the Undesirable Side effects/ Overdose of Dapacose.

Download the Product Leaflet, , to see the details on Pharmacodynamic and Pharmacokinetic Properties of Dapacose .

Contact us for further information

Dapacose (Dapagliflozin) is an SGLT-2 inhibitor drug, which is indicated in adults for the treatment of insufficiently controlled type 2 diabetes mellitus as an adjunct to other medications as well as diet and exercise. Dapagliflozin is also used adults for the treatment of symptomatic chronic heart failure with reduced ejection fraction with or without Diabetes. The drug is also used for the treatment of Chronic Kidney Disease( CKD) patients upto Stage III (eGFR of greater or equal to 30ml/min/1.73m2.)

Dapacose is marketed by JB Chemical and Pharmaceuticals limited and comes in two doses namely DAPACOSE 5mg and DAPACOSE 10mg.

Dapagliflozin inhibits the sodium-glucose contransporter 2 (SGLT2) which is primarily located in the proximal tubule of the nephron. SGLT2 facilitates 90% of glucose resorption in the kidneys and so its inhibition allows for glucose to be excreted in the urine. This excretion allows for better glycemic control and potentially weight loss in patients with type 2 diabetes mellitus.

Dapagliflozin is also used to reduce the risk of the need for hospitalization for heart failure in adults who have type 2 diabetes along with heart and blood vessel disease or who have multiple risk factors for developing heart and blood vessel disease. Recent evidence has also shown that the drug halts the progression of CKD in patients with, or without diabetes.

ACC 2020 Expert Consensus
Patients with T2DM who have or who are at very high risk for clinical ASCVD,HF and/or DKD.
ADA/EASD 2019 Guidelines
  • Patients with T2DM and HF, particularly those with HFrEF, to reduce HF, MACE and CV death
  • To prevent the progression of CKD, hHF, MACE and CV death in patients with T2DM with CKD

In Management of T2 Diabetes, Dapagliflozin provides benefits beyond Glucose Control.

  • a) Cardio protection
    Dapagliflozin demonstrates reduction in the risk of CV death or worsening heart failure in patients with HFrEF with & without diabetes.
  • b) Renal protection
    dapagliflozin delays initiaton of dialysis & reduces the number of deaths.


Dapa-HF demonstrated reduction in the risk of CV death or worsening heart failure in patients with HFrEF with & without Disbetes


In patients with CKD, with and without type 2 Diabetes, Dapagliflozin significantly

  • Reduces the risk of kidney failure
  • Reduces the risk of CV death or heart failure hospitalization
  • Prolongs survival


Dapagliflozin is Approved for the treatment of CKD patients up to Stage III(eGFR>30ml/min/1.73m)




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