Glipita M XR 500

Indications

This medication is used alongside diet and exercise to enhance glycemic control in adults with type 2 diabetes mellitus, especially when treatment with both sitagliptin and metformin is indicated. Important Considerations:

• Not Suitable For: Individuals with type 1 diabetes or diabetic ketoacidosis, as it is ineffective for these conditions.
• Pancreatitis: Safety in patients with a history of pancreatitis has not been established, and the risk of developing pancreatitis while using this medication is unknown.

Pharmacology

This tablet combines two complementary antihyperglycemic agents: Sitagliptin, a DPP-4 inhibitor, and Metformin HCl, a biguanide. Sitagliptin works by inhibiting DPP-4, an enzyme that deactivates incretin hormones (GLP-1 and GIP) which help regulate blood glucose levels by increasing insulin production and decreasing glucagon levels. Metformin HCl decreases hepatic glucose production, reduces intestinal glucose absorption, and enhances peripheral glucose utilization.

Dosage & Administration

• Film-Coated Tablet: Typically administered twice daily with meals. Starting dose: 50 mg sitagliptin/500 mg metformin HCl twice daily, escalating gradually to minimize gastrointestinal side effects. Maximum daily dose: 100 mg sitagliptin and 2000 mg metformin.
• Extended-Release Tablet: Administer once daily with an evening meal. Gradual dose escalation is recommended. Do not exceed 100 mg sitagliptin and 2000 mg metformin extended-release daily.

Interactions

• Cationic Drugs: Use cautiously with drugs eliminated by renal tubular secretion.
• Phenprocoumon: Metformin may reduce its anticoagulant effect; regular INR monitoring is advised.
• Levothyroxine: Can reduce the hypoglycemic effect of metformin; monitor blood glucose levels and adjust metformin dosage as needed.

Contraindications

• Renal dysfunction (serum creatinine levels ≥1.5 mg/dL for males, ≥1.4 mg/dL for females).
• Acute or chronic metabolic acidosis, including diabetic ketoacidosis.
• Severe hypersensitivity reactions to this medication or its components.

Side Effects

Common adverse effects include diarrhea, upper respiratory tract infections, and headaches. Hypoglycemia is more prevalent when combined with insulin or insulin secretagogues. Other side effects associated with metformin include gastrointestinal issues such as diarrhea and nausea.

Pregnancy & Lactation

• Pregnancy: Category B. Safety in pregnant women has not been established; use only if absolutely necessary.
• Lactation: It is unknown if this medication is excreted in breast milk. Exercise caution when administering to nursing mothers.

Precautions & Warnings

• Lactic Acidosis: Risk increases with conditions like sepsis, dehydration, and renal impairment. Discontinue and seek immediate medical attention if symptoms occur.
• Thyroid Function: Regular monitoring of TSH levels in hypothyroid patients is recommended.
• Vitamin B12 Levels: Long-term use may reduce vitamin B12 levels, potentially leading to peripheral neuropathy.

Overdose Effects

• Sitagliptin: Supportive measures and hemodialysis may be required.
• Metformin: Overdose may necessitate hemodialysis. Monitor for potential pancreatitis.

Therapeutic Class

Combination Oral Hypoglycemic Agents

Storage Conditions

Store below 25°C in a dry place, protected from light. Keep out of reach of children. Use before the expiry date. Dispense only with a physician’s prescription.