Siglimet-XR
Generic Name
Sitagliptin 100 mg and Metformin HCl Extended-Release Tablet
Manufacturer
Incepta Pharmaceuticals Ltd.
Country
Bangladesh
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Price Details
Current market pricing information
| Variant | Unit Price | Strip Price |
|---|---|---|
| siglimet xr 100 mg tablet | ৳ 30.00 | ৳ 180.00 |
Description
Overview of the medicine
Siglimet-XR 100 mg Tablet is a combination medication containing Sitagliptin, a DPP-4 inhibitor, and Metformin HCl, a biguanide, in an extended-release formulation. It is used to improve glycemic control in adults with type 2 diabetes mellitus as an adjunct to diet and exercise.
Uses & Indications
Dosage
Adults
Usually 1 tablet once daily with the evening meal. Dose adjusted based on efficacy and tolerability, up to maximum recommended doses of Sitagliptin 100 mg and Metformin 2000 mg daily.
Elderly
Caution is advised due to potential for decreased renal function. Renal function should be monitored.
Renal_impairment
Not recommended in patients with eGFR <30 mL/min/1.73 m². Dose adjustment may be required for eGFR 30-60 mL/min/1.73 m² (Metformin component). Sitagliptin dose also needs adjustment based on renal function.
How to Take
Take orally, once daily with the evening meal. Swallow the tablet whole; do not crush, cut, or chew.
Mechanism of Action
Sitagliptin inhibits dipeptidyl peptidase-4 (DPP-4) enzyme, which degrades incretin hormones (GLP-1 and GIP). By preserving incretins, it increases insulin synthesis and release from pancreatic beta cells and decreases glucagon secretion from alpha cells. Metformin decreases hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization.
Pharmacokinetics
Onset
Within hours for blood glucose lowering effect.
Excretion
Sitagliptin: Primarily renal excretion (approx 79% unchanged). Metformin: Primarily renal excretion (unchanged).
Half life
Sitagliptin: Approx 12.4 hours. Metformin: Approx 6.2 hours (plasma), but longer for XR formulations.
Absorption
Sitagliptin: Rapidly absorbed, bioavailability approx 87%. Metformin: Slowly and incompletely absorbed, bioavailability 50-60% for standard release, XR formulation designed for prolonged absorption.
Metabolism
Sitagliptin: Limited metabolism, primarily by CYP3A4, with minor involvement of CYP2C8. Metformin: Not metabolized in humans, excreted unchanged.
Side Effects
Contraindications
- •Hypersensitivity to Sitagliptin, Metformin, or any component of the tablet.
- •Renal dysfunction (eGFR <30 mL/min/1.73 m²).
- •Metabolic acidosis, including diabetic ketoacidosis, with or without coma.
- •Acute or chronic metabolic acidosis, including lactic acidosis.
- •Severe heart failure or acute myocardial infarction.
- •Acute or chronic disease that may cause tissue hypoxia (e.g., respiratory failure, recent myocardial infarction, sepsis, shock).
- •Hepatic impairment.
Drug Interactions
Alcohol
Increases the risk of lactic acidosis (Metformin).
Cimetidine
May increase metformin plasma concentrations.
Insulin and Insulin secretagogues
Increased risk of hypoglycemia.
Carbonic anhydrase inhibitors (e.g., Topiramate, Zonisamide, Acetazolamide, Dichlorphenamide)
May increase the risk of lactic acidosis.
Cationic drugs (e.g., Amiloride, Digoxin, Morfamine, Procainamide, Quinidine, Quinine, Ranitidine, Triamterene, Trimethoprim, Vancomycin)
May compete with metformin for renal tubular transport, increasing metformin plasma concentrations.
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, discontinue the drug, initiate supportive care. Metformin overdose can lead to lactic acidosis, which is a medical emergency and should be treated in a hospital setting. Hemodialysis can be used to remove Metformin. Sitagliptin is minimally dialyzable.
Pregnancy & Lactation
Pregnancy Category B for Sitagliptin, Category B for Metformin. Generally, it is recommended to use insulin for glycemic control during pregnancy. Not recommended during breastfeeding as Metformin is excreted into breast milk. Consult a doctor.
Frequently Asked Questions
Common questions about this medicine
Pack Sizes
Shelf Life
24 months
Availability
Pharmacies and Hospitals
Approval Status
Approved by FDA and local drug regulatory authorities
Patent Status
Generic available
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Global Brand Names
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