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Sitazid M

 50 mg+500 mg Tablet
Sitagliptin + Metformin Hydrochloride
Eskayef Pharmaceuticals Ltd.
Unit Price: ৳ 14.00 (2 x 10: ৳ 280.00)
Strip Price: ৳ 140.00
Variants
50 mg+1000 mg (Tablet) •
Alternative Medicine
Indications

Approved Indication

  • Type 2 Diabetes Mellitus
    • Adjunct to diet and exercise in adults who are inadequately controlled on metformin alone.
    • Use when dual therapy is needed and there is concern about hypoglycemia or weight gain.

Clinically Accepted (Off-label)

  • Combination regimen in older adults with renal impairment (eGFR 30–45 mL/min/1.73 m²), leveraging dose adjustments of both components.
  • Chronic therapy to minimize cardiovascular risk by optimizing glycemic control with a low-risk profile.
Dosage & Administration

Patient Group

Dosage Regimen

Adults (≥18 years)

Start: 50 mg sitagliptin + 500 mg metformin (immediate-release) twice daily with meals.
 

Extended-release: 50 mg sitagliptin + 1000 mg metformin once daily with evening meal.
 

Titrate metformin by 500 mg weekly; maximum: sitagliptin 100 mg/day and metformin 2000 mg/day.

Renal Impairment

eGFR ≥45: standard dose; eGFR 30–<45: reduce to 50 mg sitagliptin + metformin 500 mg twice daily; <30: contraindicated.

Hepatic Impairment

Avoid in significant hepatic dysfunction due to metformin-associated lactic acidosis risk.

Elderly

Start low-dose; monitor renal function due to age-related decline.

Pediatrics (<18 years)

Safety and efficacy not established.

Administration Notes

  • Take with meals to reduce gastrointestinal side effects (immediate-release).
  • Swallow extended-release tablets whole with food; do not crush or chew.
Mechanism of Action (MOA)

This combination provides two complementary mechanisms:
Metformin (a biguanide) decreases hepatic glucose production, improves peripheral glucose uptake, and slows intestinal glucose absorption. Sitagliptin (a DPP-4 inhibitor) prevents incretin hormone breakdown (GLP-1, GIP), enhancing glucose-dependent insulin secretion and reducing glucagon release. The result is improved glycemic control with low hypoglycemia risk and stable body weight.

Pharmacokinetics

Metformin (IR/XR):

  • Bioavailability ~50–60%, Tmax ~2 h (IR), ~7 h (XR).
  • Not metabolized; eliminated unchanged via kidneys.
  • Half-life ~4.2 h (IR), ~6.5 h (XR).

Sitagliptin:

  • Absorption ~87% biovailability, Tmax 1–4 h.
  • Minimal metabolism (CYP3A4, CYP2C8); ~79% excreted unchanged via kidneys.
  • Half-life ~12.4 h.

PK Interaction: None significant between components; both retain individual profiles.

Pregnancy Category & Lactation
  • Pregnancy:
    • Metformin: Category B; used in gestational diabetes but not FDA-approved for T2DM in pregnancy.
    • Sitagliptin: Limited data (animal studies negative); human use not well studied. Use insulin first.
  • Lactation:
    • Metformin excreted in breast milk in low quantities—generally considered safe.
    • Sitagliptin presence in human milk unknown; advise caution and monitor infants if used.
Therapeutic Class
  • Combination Oral Antidiabetic
    • Metformin: Biguanide
    • Sitagliptin: Dipeptidyl Peptidase-4 (DPP-4) Inhibitor
Contraindications
  • Known hypersensitivity to either component.
  • eGFR below 30 mL/min/1.73 m².
  • Acute metabolic acidosis or diabetic ketoacidosis.
  • Conditions increasing lactic acidosis risk (e.g., severe liver disease, alcohol abuse, hypoxia).
  • Pregnancy and breastfeeding (due to sitagliptin).
Warnings & Precautions
  • Lactic Acidosis: Associated with metformin; monitor renal/hepatic function, avoid alcohol abuse, and suspend during iodinated contrast studies.
  • Pancreatitis: Rarely associated with sitagliptin; discontinue if suspected.
  • Hypoglycemia: Unlikely on monotherapy but can occur with insulin/sulfonylureas.
  • Renal Function: Monitor regularly; adjust doses or discontinue if eGFR declines.
  • Gastrointestinal Effects: Metformin may cause diarrhea or nausea—consider extended-release formulation if needed.
  • Musculoskeletal: Assess for severe joint pain (arthralgia) related to sitagliptin.
Side Effects
  • Common: Diarrhea, nausea, vomiting, abdominal discomfort, upper respiratory infections, headache, arthralgia.
  • Less Common: Hypoglycemia (with concomitant insulin/SU), vitamin B12 deficiency (metformin), myalgia.
  • Rare but Serious: Lactic acidosis, pancreatitis, hypersensitivity, bullous pemphigoid, severe arthralgia.

Onset: GI symptoms typically within the first weeks; serious effects may emerge anytime.

Drug Interactions
  • Major:
    • Iodinated contrast: Stop metformin before imaging to prevent lactic acidosis.
    • Alcohol: Potentiates lactic acidosis risk.
  • Hypoglycemic Interactions: With insulin and sulfonylureas — may require dose reduction.
  • Minor PK Interactions: Rifampin may modestly reduce metformin exposure; sitagliptin is a weak substrate for CYP3A4/2C8 and P-glycoprotein; no major drug interactions.
Recent Updates or Guidelines
  • ADA 2025: Recognizes this combination as appropriate escalation from metformin when GLP-1 or SGLT2 therapies are unsuitable or unavailable.
  • FDA: Updated sitagliptin labeling to include warnings about severe joint pain and bullous pemphigoid.
  • Renal Use Clarification: Reinforced dose adjustments at eGFR thresholds to ensure safety.
Storage Conditions
  • Temperature: Store at 20–25 °C (68–77 °F), with allowed excursions between 15–30 °C (59–86 °F).
  • Humidity: Store in a dry place; protect from moisture.
  • Light: Keep in original container to avoid light exposure.
  • Handling: Immediate-release—dispose of wet, swollen tablets. Extended-release—do not crush or chew.
  • Refrigeration: Not required.
Available Brand Names