Product Description

Sitagliptin 50 mg & Metformin SR 500 mg Tablet IP is a fixed-dose oral combination antidiabetic agent for adults with type 2 diabetes mellitus (T2DM). Sitagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, enhances incretin activity for glucose-dependent insulin secretion. Metformin SR, a biguanide, suppresses hepatic glucose production and improves insulin sensitivity. Their synergistic mechanisms provide superior glycemic control (fasting/postprandial) compared to monotherapy, with SR formulation reducing GI side effects via gradual release. Prescription-only; adjunct to diet/exercise; lowers HbA1c by 1–1.5% in clinical trials (e.g., TECOS study extensions).

Uses

• Management of T2DM in adults when diet, exercise, and monotherapy (e.g., metformin alone) fail to achieve targets (HbA1c <7%)

• Improvement of glycemic parameters (fasting plasma glucose, postprandial glucose) to prevent complications (e.g., neuropathy, cardiovascular events)

• Adjunctive therapy in overweight T2DM patients (metformin supports ~1–2 kg weight loss)

• Not indicated for type 1 diabetes, diabetic ketoacidosis (DKA), gestational diabetes, or severe renal impairment (eGFR <30 mL/min)

How it works

This combination leverages complementary pathways for effective, glucose-dependent control:

• Sitagliptin (50 mg): Inhibits DPP-4 enzyme, increasing active incretin hormones (GLP-1, GIP) post-meal. This stimulates insulin release from pancreatic beta-cells only when glucose is elevated and suppresses glucagon from alpha-cells, reducing hepatic glucose output. No effect on insulin when normoglycemic—lowers hypo risk. Onset: 1–3 hours; duration 24 hours.

• Metformin SR (500 mg): Activates AMPK to inhibit gluconeogenesis in the liver (~25–30% fasting glucose reduction), enhances peripheral insulin sensitivity (muscle glucose uptake), and slows intestinal carbohydrate absorption. SR form ensures steady release, minimising peaks/troughs.

Synergy: Sitagliptin amplifies metformin's effects on postprandial glucose; overall, no weight gain or significant hypo. Steady-state: 2–3 days.

Benefits

• Enhanced glycemic control: Reduces HbA1c by 0.7–1.5% (superior to components alone in T2DM trials, e.g., 12-week studies showing 1.0% drop vs. 0.6% for metformin monotherapy), stabilizing both fasting and postprandial levels.

• Low hypoglycemia risk: Sitagliptin's glucose-dependent action avoids excessive insulin secretion (hypo incidence <1% vs. 10–20% with sulfonylureas), safer for the elderly or those with variable eating.

• Cardiovascular neutrality: No increased heart risk (per TECOS trial); metformin may offer protective effects (e.g., 10–15% CV event reduction in meta-analyses).

• Tolerability and adherence: SR reduces GI upset by 20–30%; once/twice-daily dosing improves compliance (e.g., 85% in real-world data).

How to use

Swallow the sustained-release tablet orally with water, typically after meals; do not break, crush, or chew it. Follow the dosage prescribed by your healthcare provider. Take the medication at the same time each day to maintain consistent drug levels. If a dose is missed, take it as soon as you remember. If it is close to the next scheduled dose, skip the missed one. Never take a double dose.

Side Effects

Common side effects (mild, transient; 5–10% incidence):

• Gastrointestinal (metformin-dominant): Nausea, vomiting, diarrhea, gas, bloating, stomach pain, indigestion

• General: Headache, metallic taste (metformin), upper respiratory symptoms (runny/stuffy nose, sore throat—sitagliptin)

Less common/rare but serious side effects (seek immediate medical attention):

• Metabolic: Lactic acidosis (rare <1/100,000; symptoms: fatigue, hyperventilation—metformin risk)

• Hypoglycemia: If combined with insulin/sulfonylureas (dizziness, sweating)

• Other: Vitamin B12 deficiency (long-term: anemia, neuropathy—monitor); allergic rash, pancreatitis (sitagliptin rare <0.1%)

GI effects often resolve with food/SR; B12 screening recommended annually.

Safety Advice

Do not stop taking this medication abruptly, even if your blood sugar levels are controlled. Suddenly discontinuing it can cause your blood sugar to spike to dangerously high levels. It must be swallowed whole. Do not crush, chew, or break the tablet, as this can affect how the medicine is absorbed and increase side effects. While this medication has a low risk of causing hypoglycemia, it can happen, especially if you are taking other antidiabetic drugs. Be aware of symptoms like dizziness, shakiness, sweating, and confusion. Limit or avoid alcohol, as excessive consumption can increase the risk of lactic acidosis and low blood sugar.

Storage Conditions

Store at a temperature below 86°F (30 °C). Protect from light and moisture.

FAQs

Does this medication cure type 2 diabetes?

No, it helps manage and control blood sugar levels, but does not cure diabetes.

Is this medication suitable for type 1 diabetes?

No, this medication is only for the treatment of type 2 diabetes.

How should this medication be taken?

Take one tablet daily with a meal, preferably in the evening, to minimize gastrointestinal side effects. Tablets should be swallowed whole and not crushed, chewed, or broken.

Can this medication be stopped once blood sugar is under control?

No, do not stop taking this medication without consulting a doctor. Stopping abruptly can cause blood sugar levels to increase.

Can alcohol be consumed with this medication?

Avoid excessive alcohol consumption, as it can increase the risk of lactic acidosis, a serious condition.

Can one drive while taking this medication?

Exercise caution when driving or operating machinery, as the medication can cause dizziness or low blood sugar, which may affect concentration.

Does it cause low blood sugar (hypoglycemia)?

This combination has a low risk of causing hypoglycemia, but the risk increases if taken with other diabetes medications like insulin.

Is it safe for pregnant or breastfeeding women?

This medication is generally not recommended during pregnancy or breastfeeding. Discuss the risks and benefits with a doctor if pregnant, planning to become pregnant, or breastfeeding.

Who should not take this medication?

This medication should not be taken if there is a history of allergies to its components, severe kidney or liver disease, heart problems like congestive heart failure, or diabetic ketoacidosis.