Usage
- Remogliflozin Etabonate is prescribed for the treatment of type 2 diabetes mellitus (T2DM) in adults to improve glycemic control. It is used as monotherapy when diet and exercise are insufficient, or as add-on therapy with Metformin when the latter, along with diet and exercise, does not provide adequate glycemic control. It can also be used in combination with Vildagliptin.
- Pharmacological classification: Sodium-Glucose Co-Transporter 2 (SGLT2) inhibitor.
- Mechanism of Action: Remogliflozin Etabonate inhibits SGLT2 in the proximal renal tubules, reducing glucose reabsorption from the glomerular filtrate and promoting its excretion in urine (glucosuria). This lowers plasma glucose levels, aiding in the management of hyperglycemia.
Alternate Names
- Remogliflozin (active moiety).
- Brand Names: Remo, Remozen, Remo-V, Remo MV.
How It Works
- Pharmacodynamics: Remogliflozin Etabonate selectively inhibits SGLT2, leading to increased urinary glucose excretion, decreased plasma glucose levels, and potential weight loss and reduction in systolic blood pressure.
- Pharmacokinetics: Administered orally as Remogliflozin Etabonate, a prodrug. It is rapidly absorbed and metabolized to its active form, Remogliflozin. Peak plasma concentration is achieved in 0.5-1 hour. Elimination half-life is relatively short (1.4 - 2.9 hours). Primarily eliminated through hepatic metabolism, with a minor portion excreted renally.
- Mode of Action: Binds to and inhibits SGLT2 in the renal proximal tubules, preventing glucose reabsorption.
- Receptor Binding/Enzyme Inhibition: SGLT2 inhibition.
- Elimination Pathways: Primarily hepatic metabolism; some renal excretion.
Dosage
Standard Dosage
Adults:
- 100 mg twice daily, with or without food, for monotherapy or add-on therapy with Metformin.
- When used with insulin or an insulin secretagogue (e.g., sulfonylurea), a lower dose of the latter may be necessary to mitigate hypoglycemia risk.
Children:
- Not recommended for use in patients under 18 years of age, as safety and efficacy have not been established.
Special Cases:
- Elderly Patients (≥ 65 years): No dose adjustment is generally necessary, but renal function and volume depletion risk should be considered. Initiation of therapy is not recommended in patients 75 years and older due to limited therapeutic experience.
- Patients with Renal Impairment: No dose adjustment for mild to moderate impairment. Not recommended for patients with severe renal impairment (eGFR < 30 mL/min/1.73m²) or end-stage renal disease requiring dialysis. Discontinue if eGFR falls below 45 mL/min.
- Patients with Hepatic Dysfunction: Not recommended for patients with moderate to severe hepatic impairment.
- Patients with Comorbid Conditions: Careful monitoring is advised in patients with cardiovascular disease, dehydration, or those taking diuretics.
Clinical Use Cases
- Remogliflozin Etabonate is specifically indicated for type 2 diabetes management and is not typically used in clinical settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations.
Dosage Adjustments
- Adjust dosage based on renal/hepatic function, concomitant medications, and individual patient response.
Side Effects
Common Side Effects
- Urinary tract infections (UTIs)
- Genital mycotic infections
- Increased urination
- Increased thirst
- Nausea
- Hypoglycemia (especially when combined with insulin or sulfonylureas).
Rare but Serious Side Effects
- Dehydration (especially with concomitant diuretic use or renal impairment), which can lead to dizziness, hypotension, and lightheadedness.
- Acute kidney injury (rare)
- Hypersensitivity reactions (rare).
Long-Term Effects
- Long-term effects are still being studied, but elevated LDL cholesterol has been observed in some patients.
Adverse Drug Reactions (ADR)
- Severe hypoglycemia
- Acute kidney injury.
Contraindications
- Hypersensitivity to Remogliflozin Etabonate or any of its components.
- Type 1 diabetes mellitus.
- Diabetic ketoacidosis.
- Severe renal impairment (eGFR < 30 mL/min/1.73m²).
- End-stage renal disease requiring dialysis.
Drug Interactions
- Diuretics: Increased risk of dehydration and hypotension.
- Insulin and Insulin Secretagogues (e.g., sulfonylureas): Increased risk of hypoglycemia.
- Enzyme Inducers (e.g., rifampicin, phenytoin, phenobarbital): Decreased Remogliflozin plasma concentration, potentially reducing efficacy.
- Enzyme Inhibitors (e.g., ketoconazole, erythromycin): Increased Remogliflozin levels, increasing risk of adverse effects.
- Digoxin: Potential interaction, monitoring recommended.
- Alcohol: Increased risk of hypoglycemia.
- Oral Contraceptives: Reduced efficacy of oral contraceptives, alternative methods of contraception are recommended.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: Not established. Not recommended during pregnancy due to limited safety data.
- Breastfeeding: Not known if Remogliflozin is excreted in breast milk. Not recommended during breastfeeding.
Drug Profile Summary
- Mechanism of Action: SGLT2 inhibitor, reduces renal glucose reabsorption.
- Side Effects: UTIs, genital mycotic infections, increased urination, hypoglycemia, dehydration.
- Contraindications: Type 1 diabetes, diabetic ketoacidosis, severe renal impairment, end-stage renal disease.
- Drug Interactions: Diuretics, insulin/sulfonylureas, enzyme inducers/inhibitors.
- Pregnancy & Breastfeeding: Not recommended.
- Dosage: 100 mg twice daily (adults).
- Monitoring Parameters: Blood glucose, renal function, electrolytes, blood pressure.
Popular Combinations
- Metformin + Remogliflozin Etabonate: Improves glycemic control.
- Vildagliptin + Remogliflozin Etabonate: Synergistic effect on blood glucose lowering.
Precautions
- General Precautions: Monitor renal function, blood glucose, electrolytes, and blood pressure. Assess for dehydration risk.
- Specific Populations: Avoid in pregnancy and breastfeeding. Caution in elderly patients. Not recommended for children.
- Lifestyle Considerations: Diet and exercise are crucial components of diabetes management. Limit alcohol intake.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Remogliflozin Etabonate?
A: The standard recommended dosage is 100 mg twice daily for adults.
Q2: How does Remogliflozin Etabonate differ from other SGLT2 inhibitors?
A: It is a prodrug with a short half-life requiring twice-daily dosing.
Q3: What are the common side effects patients should be aware of?
A: UTIs, genital mycotic infections, increased urination, and hypoglycemia.
Q4: Can Remogliflozin Etabonate be used in patients with renal impairment?
A: It can be used in mild to moderate renal impairment but is contraindicated in severe renal impairment or patients on dialysis.
Q5: What are the key drug interactions to consider?
A: Diuretics, insulin, sulfonylureas, and enzyme inducers/inhibitors.
Q6: Is Remogliflozin Etabonate safe during pregnancy or breastfeeding?
A: No. It’s not recommended for use during pregnancy or while breastfeeding.
Q7: What should I do if a patient experiences hypoglycemia while taking Remogliflozin Etabonate?
A: Follow standard hypoglycemia management protocols. If severe, administer glucagon if necessary. Review concomitant medications, especially insulin and sulfonylureas, and adjust dosages as needed.
Q8: How should I monitor a patient on Remogliflozin Etabonate?
A: Regularly monitor blood glucose, renal function (eGFR and serum creatinine), electrolytes, and blood pressure.
Q9: Can this medication be crushed or chewed?
A: The tablets should be swallowed whole with water.
Q10: What patient education points are important to emphasize?
A: Maintain adequate hydration, especially during hot weather or exercise. Recognize and manage hypoglycemia. Report any signs of UTI or genital infection. Adhere to prescribed dosage and follow-up appointments.
