Siglimet-XR
Generic Name
Sitagliptin and Metformin Hydrochloride Extended Release Tablet
Manufacturer
Square Pharmaceuticals Ltd.
Country
Bangladesh
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Price Details
Current market pricing information
| Variant | Unit Price | Strip Price |
|---|---|---|
| siglimet xr 50 mg tablet | ৳ 16.00 | ৳ 96.00 |
Description
Overview of the medicine
Siglimet-XR 50 mg Tablet is an extended-release oral antidiabetic medication combining Sitagliptin, a DPP-4 inhibitor, and Metformin Hydrochloride, a biguanide, used to improve glycemic control in adults with type 2 diabetes mellitus.
Uses & Indications
Dosage
Adults
Recommended starting dose is Sitagliptin 50 mg / Metformin XR 500 mg once daily with the evening meal. Dose may be titrated up to a maximum of Sitagliptin 100 mg / Metformin XR 2000 mg daily, usually as a single daily dose with the evening meal.
Elderly
Dose should be carefully titrated due to potential for decreased renal function. Renal function should be monitored regularly.
Renal_impairment
Contraindicated in severe renal impairment (eGFR < 30 mL/min/1.73m²). Dose adjustment required for moderate impairment (eGFR 30-45 mL/min/1.73m² or 45-60 mL/min/1.73m²). Sitagliptin dose reduction may be needed, and Metformin use may be restricted or contraindicated.
How to Take
Take orally once daily with the evening meal. Swallow the tablet whole; do not crush, cut, or chew it.
Mechanism of Action
Sitagliptin works by inhibiting the enzyme dipeptidyl peptidase-4 (DPP-4), which increases the levels of active incretin hormones (GLP-1 and GIP). These hormones enhance glucose-dependent insulin secretion from pancreatic beta cells and decrease glucagon secretion from pancreatic alpha cells. Metformin works primarily by decreasing hepatic glucose production, decreasing intestinal absorption of glucose, and improving insulin sensitivity by increasing peripheral glucose uptake and utilization.
Pharmacokinetics
Onset
Glucose-lowering effects observed within hours of first dose.
Excretion
Sitagliptin: Primarily renal excretion (79% unchanged). Metformin: Primarily renal excretion (unchanged).
Half life
Sitagliptin: Approximately 12.4 hours. Metformin: Approximately 6.2 hours (for conventional release), extended release half-life may be slightly longer.
Absorption
Sitagliptin: Rapidly absorbed, Cmax reached in 1-4 hours. Bioavailability approx. 87%. Metformin: Extended-release formulation, absorbed slowly and continuously. Peak plasma concentrations are reached 4-8 hours after administration. Bioavailability of metformin extended-release is ~50-60%.
Metabolism
Sitagliptin: Minimally metabolized by CYP3A4 and CYP2C8, forming inactive metabolites. Metformin: Not metabolized in the liver; excreted unchanged.
Side Effects
Contraindications
- •Hypersensitivity to Sitagliptin, Metformin, or any components of the tablet.
- •Severe renal impairment (eGFR < 30 mL/min/1.73m²).
- •Metabolic acidosis, including diabetic ketoacidosis, with or without coma.
- •Acute or chronic metabolic acidosis, including lactic acidosis history.
- •Acute or chronic disease which may cause tissue hypoxia (e.g., cardiac or respiratory failure, recent myocardial infarction, shock).
- •Hepatic impairment (for metformin component).
Drug Interactions
Alcohol
Increases the risk of lactic acidosis with metformin.
Diuretics (e.g., thiazides, loop diuretics)
May exacerbate renal function impairment, increasing lactic acidosis risk.
Corticosteroids, sympathomimetics, phenothiazines
May decrease glycemic control.
Carbonic anhydrase inhibitors (e.g., topiramate, zonisamide)
May increase the risk of lactic acidosis.
Cationic drugs (e.g., amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterene, trimethoprim, vancomycin)
May increase metformin concentration by competing for renal tubular transport.
Storage
Store below 30°C in a dry place, away from light and moisture. Keep out of reach of children.
Overdose
In case of overdose, consult a healthcare professional immediately. Overdose of metformin can lead to lactic acidosis. Treatment is supportive, and hemodialysis may be necessary for metformin overdose.
Pregnancy & Lactation
Pregnancy Category B (Sitagliptin), B (Metformin). Not recommended during pregnancy unless clearly needed. Metformin is excreted in breast milk; advise caution during lactation. Consult doctor.
Frequently Asked Questions
Common questions about this medicine
Pack Sizes
Shelf Life
24 months
Availability
Available in pharmacies nationwide
Approval Status
Approved by FDA and DGDA
Patent Status
Generic available, original compound patents expired
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Global Brand Names
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