Sitagil M 50 mg+500 mg ER

Description

Indications
This medication is prescribed as an adjunct to diet and exercise to enhance glycemic control in adults with type 2 diabetes mellitus when treatment with both sitagliptin and metformin is appropriate.

Important Limitations of Use:

• Not suitable for patients with type 1 diabetes.
• Ineffective for treating diabetic ketoacidosis.

Pharmacology
This combination tablet consists of two antihyperglycemic agents, Sitagliptin and Metformin HCl, which have complementary mechanisms to regulate blood sugar levels in patients with type 2 diabetes.

• Sitagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor that slows the breakdown of incretin hormones such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). These hormones enhance insulin secretion from pancreatic beta cells and suppress glucagon production by alpha cells, thereby reducing hepatic glucose output.
• Metformin HCl belongs to the biguanide class and primarily works by decreasing hepatic glucose production, reducing glucose absorption in the intestine, and improving glucose uptake and utilization in peripheral tissues.

Dosage & Administration
Film-Coated Tablet:

• Dosage should be individualized based on the patient’s current treatment plan and tolerance, without exceeding a daily limit of 100 mg sitagliptin and 2000 mg metformin.
• Generally taken twice daily with meals, with gradual dose escalation to minimize gastrointestinal side effects.
• For patients not previously on metformin, the recommended initial dose is 50 mg sitagliptin/500 mg metformin twice daily, with gradual escalation as needed.
• For patients already on metformin, the starting dose should include 50 mg sitagliptin twice daily along with the patient’s current metformin dose. For those taking 850 mg metformin twice daily, the recommended dose is 50 mg sitagliptin/1000 mg metformin twice daily.
• When switching from another antihyperglycemic regimen, close monitoring is necessary to manage potential changes in glycemic control.

Extended-Release Tablet:

• Typically administered once daily with an evening meal.
• Dosage should be adjusted based on effectiveness and tolerance, without exceeding the daily limit of 100 mg sitagliptin and 2000 mg metformin extended-release.
• Patients taking two extended-release tablets should consume them together as a single daily dose.
• If co-administered with insulin or an insulin secretagogue (e.g., sulfonylurea), dose adjustments may be required to lower the risk of hypoglycemia.

Drug Interactions

• Cationic drugs: Caution advised due to renal elimination interactions.
• Phenprocoumon: Metformin may decrease its anticoagulant effect, requiring close INR monitoring.
• Levothyroxine: May reduce metformin’s hypoglycemic effect, necessitating blood glucose monitoring and possible dose adjustment.

Contraindications
This medication should not be used in patients with:

• Renal dysfunction (e.g., serum creatinine ≥1.5 mg/dL in males, ≥1.4 mg/dL in females) or abnormal creatinine clearance.
• Acute or chronic metabolic acidosis, including diabetic ketoacidosis.
• A history of serious hypersensitivity reactions such as anaphylaxis or angioedema.
• Patients undergoing radiologic procedures with iodinated contrast materials should temporarily discontinue use to prevent renal complications.

Side Effects

• Common (>5%): Diarrhea, upper respiratory tract infection, headache.
• When used with sulfonylurea and metformin: Higher incidence of hypoglycemia and headache.
• When used with insulin and metformin: Higher risk of hypoglycemia.
• Metformin-related adverse effects: Nausea, vomiting, bloating, abdominal discomfort, weakness, and headache.

Pregnancy & Lactation

• Classified as Pregnancy Category B. No adequate studies have been conducted in pregnant women; use only if clearly needed.
• It is unknown whether sitagliptin is excreted in human milk. Caution is advised when prescribing to nursing mothers.

Precautions & Warnings

• Lactic Acidosis: Risk increases with renal impairment, hepatic insufficiency, dehydration, excessive alcohol consumption, and certain medical conditions. Symptoms include muscle pain, breathing difficulties, drowsiness, and abdominal discomfort. If suspected, discontinue the medication immediately and seek medical attention.
• Thyroid monitoring: Regular thyroid-stimulating hormone (TSH) assessments are recommended for hypothyroid patients.
• Vitamin B12 levels: Long-term metformin use may reduce vitamin B12 levels, potentially leading to neuropathy; monitoring is advised.
• Liver disease: Not recommended for patients with hepatic impairment.
• Renal function: Should be assessed before starting treatment and periodically thereafter.
• Pancreatitis: If symptoms suggestive of pancreatitis occur, discontinue immediately.
• Alcohol intake: Patients should be advised against excessive alcohol consumption.
• Stress management: Temporary insulin therapy may be required during periods of illness, infection, or surgery.
• Hypersensitivity reactions: Severe allergic reactions, including Stevens-Johnson syndrome, have been reported. If an allergic reaction occurs, discontinue the medication and seek medical attention.
• Cardiovascular risk: No conclusive evidence supports macrovascular risk reduction with this medication.

Overdose Effects

• Sitagliptin Overdose: Standard supportive measures should be taken, including gastrointestinal decontamination and clinical monitoring. Sitagliptin is modestly dialyzable.
• Metformin Overdose: High doses (>50 g) have been reported. Metformin is efficiently removed via hemodialysis and should be considered in overdose cases. Pancreatitis has been associated with metformin overdose.

Therapeutic Class
Combination oral hypoglycemic agents.

Storage Conditions

• Store below 25°C in a dry place, away from direct light.
• Keep out of reach of children.
• Do not use beyond the expiration date.
• Dispense only with a registered physician’s prescription.