Dapagliflozin (5mg), Metformin (1000mg) & GLIDAPAFLOZIN M 5/ 1000: Nerve Pain Relief - Uses, Dosage, and Safety…

May 14, 2024

Introduction

GLIDAPAFLOZIN M 5/1000 is an advanced oral antidiabetic tablet combining Dapagliflozin, a selective SGLT2 inhibitor, and Metformin Hydrochloride, a biguanide in sustained-release form. This fixed-dose combination is designed to provide comprehensive glycemic control in adults with Type 2 Diabetes Mellitus (T2DM) who are inadequately controlled on metformin monotherapy or who require combination therapy for better blood glucose management.It addresses multiple pathophysiological mechanisms involved in T2DM, such as insulin resistance, increased hepatic glucose output, and renal glucose reabsorption.

Composition

Each film-coated tablet contains:

  • Dapagliflozin – 5 mg

  • Metformin Hydrochloride (Sustained Release) – 1000 mg

Pharmaceutical Class:

  • Dapagliflozin: SGLT2 Inhibitor (Sodium-Glucose Co-Transporter 2 Inhibitor)

  • Metformin SR: Biguanide Class Antidiabetic

Mechanism of Action (MoA)

Dapagliflozin (5 mg):

  • Acts in the proximal renal tubules by selectively inhibiting SGLT2, a protein responsible for reabsorbing 90% of glucose filtered by the kidneys.

  • Inhibition leads to glucosuria (glucose loss in urine), thereby lowering plasma glucose levels.

  • Offers independent insulin action, aiding control even in insulin-resistant patients.

  • Contributes to modest weight loss, blood pressure reduction, and cardiovascular protection.

Metformin SR (1000 mg):

  • Works primarily by suppressing hepatic gluconeogenesis (liver glucose production).

  • Enhances peripheral glucose uptake in muscles and fat.

  • Increases insulin sensitivity without promoting insulin secretion (thus minimal hypoglycemia risk).

  • SR form allows slower absorption, improving GI tolerance and sustaining therapeutic blood levels over time.

Therapeutic Indications

GLIDAPAFLOZIN M 5/1000 is indicated for:

  • Adults with Type 2 Diabetes Mellitus not adequately controlled with metformin alone.

  • Patients requiring combination therapy to achieve HbA1c targets.

  • Those with cardiovascular risk factors or chronic kidney disease, where SGLT2 inhibitors show added benefits.

Can be used:

  • As initial combination therapy

  • In patients previously on separate dapagliflozin and metformin

  • As add-on to other oral antidiabetics or insulin, based on clinical need

Clinical Benefits

Benefit Explanation
Improved HbA1c control Dual mechanism for sustained blood glucose lowering
Weight neutral or mild loss Dapagliflozin promotes calorie loss via glucosuria
Low hypoglycemia risk Minimal effect on insulin secretion or beta-cell stimulation
Cardiovascular protection Dapagliflozin reduces risk of heart failure and hospitalization
Renal benefits Slows progression of diabetic kidney disease
GI tolerance Metformin SR formulation reduces GI disturbances compared to IR tablets

Dosage and Administration

Parameter Details
Route Oral
Frequency Once daily
Administration Take with the evening meal to enhance absorption and reduce GI upset
Swallow whole Do not crush, break, or chew the tablet

Dosage adjustment may be required based on:

  • Renal function (eGFR)

  • Tolerability

  • Concurrent use with other antidiabetics

Side Effects

Common (≥1%):

  • Urinary tract infections (UTIs)

  • Genital mycotic infections (especially in women)

  • Polyuria (frequent urination)

  • Nausea, flatulence, or abdominal discomfort

  • Mild dehydration, fatigue

Uncommon but Serious:

  • Lactic Acidosis (due to metformin accumulation in renal impairment or overdose)

  • Euglycemic Diabetic Ketoacidosis (EDKA) (rare, with dapagliflozin)

  • Fournier’s Gangrene (necrotizing fasciitis of perineum)

  • Hypotension in patients on diuretics or with volume depletion

Contraindications

  • Known hypersensitivity to dapagliflozin or metformin

  • Severe renal impairment (eGFR < 30 mL/min/1.73 m²)

  • Acute or chronic metabolic acidosis, including ketoacidosis

  • Severe hepatic dysfunction

  • Conditions with tissue hypoxia (heart failure, MI, respiratory failure)

  • Excessive alcohol intake, due to risk of lactic acidosis

Drug Interactions

Drug/Class Possible Effect
Alcohol Increases lactic acidosis risk with metformin
Diuretics May cause volume depletion, hypotension (with dapagliflozin)
Beta-blockers Mask symptoms of hypoglycemia
Insulin/sulfonylureas May increase hypoglycemia risk (monitor closely)
Contrast agents Risk of acute kidney injury; discontinue metformin temporarily

Monitoring Parameters

  • Blood glucose and HbA1c regularly

  • Renal function (eGFR) prior to and during therapy

  • Electrolytes, especially in elderly or volume-depleted patients

  • Signs of lactic acidosis: malaise, myalgia, labored breathing

  • Urinary tract infections, especially in females

  • Hydration status in summer or with diuretics

Storage Guidelines

  • Store at below 25°C

  • Protect from light and moisture

  • Keep away from children

Frequently Asked Questions (FAQs)

Q1. What is the role of dapagliflozin in this combination?

It helps lower blood sugar by increasing urinary glucose excretion and also offers cardio-renal protection.

Q2. Why is Metformin in SR form?

SR (Sustained Release) improves gastrointestinal tolerance and provides longer therapeutic effect with once-daily dosing.

Q3. Can GLIDAPAFLOZIN M 5/1000 be used in kidney disease?

It is not recommended in severe kidney disease (eGFR < 30). Use with caution and monitor renal function regularly.

Q4. Does this medicine cause hypoglycemia?

No, not usually. But if taken with insulin or sulfonylureas, the risk of hypoglycemia may increase.

Q5. Can this tablet help with weight loss?

Yes, dapagliflozin promotes glucose excretion, which may lead to modest weight loss in most patients.

Conclusion

GLIDAPAFLOZIN M 5/1000 is a clinically backed, dual-action antidiabetic tablet combining the strengths of dapagliflozin and metformin SR. It offers significant advantages in terms of glycemic control, cardiovascular safety, renal protection, and weight management, with a favorable safety profile. This fixed-dose combination helps simplify therapy and enhance adherence, making it a preferred choice for modern diabetes management.

About The Author

STERIS HEALTHCARE PVT LTD

Steris Healthcare Pvt Ltd, known as Sterispharma, was founded in February 2018 by a team of experienced professionals in the pharmaceutical industry. Headquartered in Navi Mumbai, the company holds certifications from WHO, GMP, and ISO, reflecting its dedication to maintaining high standards of quality and safety. Sterispharma’s mission is to provide affordable, high-quality medications across India, strictly adhering to WHO guidelines. With the convenience of an online pharmacy, customers can easily order medicines with home delivery options.

For further information 

Email: info@sterispharma.com / contact@sterispharma.com

Call/WhatsApp: 8209542042 , 8824175417

BUY NOW

SHARE WITH