Adult: Conventional tab: Sitagliptin 50 mg and metformin 500 mg Sitagliptin 50 mg and metformin 850 mg Sitagliptin 50 mg and metformin 1,000 mg
As an adjunct to diet and exercise to improve glycaemic control: 1 tab bid. Dose must be individualised based on the patient's current antidiabetic regimen, effectiveness and tolerability. Max: 100 mg sitagliptin/2,000 mg metformin daily.
Extended-release tab: Sitagliptin 50 mg and metformin 500 mg Sitagliptin 50 mg and metformin 1,000 mg Sitagliptin 100 mg and metformin 1,000 mg
As an adjunct to diet and exercise to improve glycaemic control: 1 tab once daily, preferably in the evening. Dose must be individualised based on the patient's current antidiabetic regimen, effectiveness and tolerability. Max: 100 mg sitagliptin/2,000 mg metformin daily. Dosage recommendations and available fixed-dose combinations may vary between countries (refer to specific product guidelines).
What are the brands available for Sitagliptin + Metformin in Philippines?
Patients taking concurrent insulin or insulin secretagogues (e.g. sulfonylurea): A lower dose of other concurrent antidiabetic agents may be required.
Renal Impairment
eGFR (mL/min/1.73 m2)
Dosage
<30
Contraindicated.
30-<45
Initiation of therapy: Not recommended. Continuation of existing therapy: If eGFR falls <45 mL/min/1.73 m2, assess the risk or benefit of continuing treatment (Max: 50 mg sitagliptin once daily).
Dosage recommendations may vary among countries and between individual products (refer to specific product guidelines).
Hepatic Impairment
Avoid use.
Administration
Metformin + Sitagliptin Should be taken with food.
Contraindications
Acute or chronic metabolic acidosis (e.g. diabetic ketoacidosis, lactic acidosis); diabetic pre-coma; acute conditions which may alter renal function (e.g. dehydration, severe infection); acute or chronic disease that may cause tissue hypoxia (e.g. cardiac or respiratory failure, recent MI, shock); alcoholism, acute alcohol intoxication. Severe renal impairment (eGFR <30 mL/min/1.73 m2).
Special Precautions
Patient with history of angioedema due to other dipeptidyl peptidase-4 (DPP-4) inhibitors; history of or risk factors for heart failure; history of pancreatitis; risk factors for lactic acidosis and vitamin B12 deficiency. Patients taking concurrent insulin or insulin secretagogues (e.g. sulfonylurea). Not indicated for use in patients with type 1 diabetes mellitus. Withhold treatment at the time of surgical procedures under general, spinal, or epidural anaesthesia; may restart treatment at least 48 hours after surgery or resumption of oral nutrition and once renal function is stable. Discontinue use before or at the time of imaging procedure involving iodinated contrast agents in patients with eGFR 30-60 mL/min/1.73 m2, history of hepatic impairment, alcoholism or heart failure, or in any patients receiving intra-arterial iodinated contrast; re-evaluate eGFR 48 hours after the procedure and restart therapy if renal function is stable. Avoid use in hepatic impairment (including hepatic failure). Mild to moderate renal impairment. Elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Severe and disabling arthralgia; bullous pemphigoid; worsening renal function, including acute renal failure; vitamin B12 deficiency (long-term metformin use); hypoglycaemia (particularly when used concomitantly with insulin or insulin secretagogue). Rarely, hypersensitivity reactions, including anaphylaxis, angioedema, and severe or exfoliative dermatologic reactions (e.g. Stevens-Johnson syndrome). Gastrointestinal disorders: Nausea, vomiting, flatulence, diarrhoea, constipation, abdominal pain. Musculoskeletal and connective tissue disorders: Myalgia, back pain, arthropathy, pain in extremity. Nervous system disorders: Somnolence, headache. Respiratory, thoracic and mediastinal disorders: URTI. Skin and subcutaneous tissue disorders: Pruritus, rash, urticaria. Potentially Fatal: Lactic acidosis. Rarely, acute pancreatitis (including haemorrhagic and necrotising pancreatitis).
Evaluate renal function (eGFR) before treatment initiation and annually thereafter, or more frequently (e.g. every 3-6 months) for those at risk for impaired renal function. Monitor plasma glucose (frequency depends on individual treatment regimen, hypoglycaemia risk, and other patient-specific factors); HbA1c (at least twice yearly for those who have stable glycaemic control; quarterly for patients not meeting the treatment goals or with therapy changes); haematologic parameters such as Hb/haematocrit, RBC indices (annually); vitamin B12 levels (every 1-2 years, particularly to those with risk factors for vitamin B deficiency). Assess for signs and symptoms of acute pancreatitis, lactic acidosis, and heart failure.
Overdosage
Symptoms: Metformin: Lactic acidosis and hypoglycaemia.
Management: Symptomatic and supportive treatment. May perform haemodialysis to remove lactate and metformin.
Drug Interactions
Increased risk of hypoglycaemia with insulin or insulin secretagogues (e.g. sulfonylurea). May result in the loss of glycaemic control with agents that produce hyperglycaemia (e.g. thyroid products, thiazides and other diuretics, corticosteroids, phenothiazines, sympathomimetics, phenytoin, nicotinic acid, calcium channel blockers, isoniazid, estrogens, oral contraceptives).
Metformin: May increase the risk of lactic acidosis with NSAIDs (including COX-2 inhibitors), ACE inhibitors, ARBs, loop diuretics, topiramate and other carbonic anhydrase inhibitors (e.g. acetazolamide, diclofenamide, zonisamide). May increase systemic exposure with drugs that interfere with common renal tubular transport systems (e.g. cimetidine, ranolazine, vandetanib, dolutegravir). Potentially Fatal: Metformin: May cause contrast-induced nephropathy leading to metformin accumulation and increased risk of lactic acidosis with intravascular iodinated contrast agents.
Food Interaction
Metformin: Increased risk of lactic acidosis with alcohol. Food reduces the extent and slightly delays the absorption.
Action
Description: Overview: Sitagliptin, a potent dipeptidyl peptidase-4 (DPP-4) inhibitor, is an antidiabetic agent.
Metformin is a biguanide antidiabetic agent. Mechanism of Action: Sitagliptin selectively inhibits dipeptidyl peptidase-4 (DPP-4), the enzyme responsible for inactivating incretin hormones. This inhibition increases the levels of incretin hormones such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which enhance insulin synthesis and release from pancreatic β-cells and reduce glucagon secretion from α-cells, thereby lowering hepatic glucose production.
Metformin reduces hepatic glucose production by inhibiting gluconeogenesis and glycogenolysis, decreases intestinal glucose absorption, and improves insulin sensitivity by enhancing peripheral glucose uptake and utilisation. Pharmacodynamics: Sitagliptin increases insulin release and reduces glucagon concentrations in a glucose-dependent manner. This results in decreased fasting plasma glucose and diminished post-prandial glucose excursions following a glucose load or meal in patients with type 2 diabetes mellitus. When used as monotherapy, sitagliptin is generally not associated with hypoglycaemia or significant changes in body weight.
Metformin reduces both basal and postprandial plasma glucose concentrations in patients with type 2 diabetes mellitus. It rarely causes hypoglycaemia and does not affect normal blood glucose levels. Metformin may produce modest weight loss due to reduced appetite and can also lower plasma VLDL triglycerides, resulting in small reductions in plasma triglycerides and total cholesterol. Onset: Metformin: Within days. Pharmacokinetics: Absorption: Sitagliptin: Rapidly absorbed from the gastrointestinal tract. Bioavailability: Approx 87%. Time to peak plasma concentration: 1-4 hours.
Metformin: Slowly and incompletely absorbed from the gastrointestinal tract. Food reduces the extent and slightly delays the absorption. Absolute bioavailability: Approx 50-60% (fasting). Time to peak plasma concentration: 2-3 hours (conventional form); 6-8 hours (extended-release tab). Distribution: Sitagliptin: Volume of distribution: Approx 198 L. Plasma protein binding: 38%.
Metformin: Partitions into erythrocytes; concentrates in the liver, gastrointestinal tract and kidney. Crosses the placenta; enters breast milk (small amounts). Volume of distribution: 654 ± 358 L. Metabolism: Sitagliptin: Minimally metabolised primarily by CYP3A4, and to a lesser extent by CYP2C8 isoenzyme into inactive metabolites.
Metformin: Not metabolised. Excretion: Sitagliptin: Mainly via urine (87%; approx 79% as unchanged drug, 16% as metabolites); faeces (13%). Elimination half-life: Approx 12.4 hours.
Metformin: Via urine (90% as unchanged drug). Elimination half-life: 4-9 hours (plasma); approx 17.6 hours (blood).
Chemical Structure
Sitagliptin Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 4369359, Sitagliptin. https://pubchem.ncbi.nlm.nih.gov/compound/Sitagliptin. Accessed June 27, 2025.
Metformin Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 4091, Metformin. https://pubchem.ncbi.nlm.nih.gov/compound/Metformin. Accessed Apr. 29, 2025.
A10BD07 - metformin and sitagliptin ; Belongs to the class of combinations of oral blood glucose lowering drugs. Used in the treatment of diabetes.
References
Brayfield A, Cadart C (eds). Metformin Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 24/09/2025.Brayfield A, Cadart C (eds). Sitagliptin Phosphate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 24/09/2025.Janumet Film-coated Tablets (Merck Sharp & Dohme [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 24/09/2025.Janumet Tablet, Film Coated (Merck Sharp & Dohme LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 24/09/2025.Janumet XR Film-coated Tablets (Merck Sharp & Dohme [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 24/09/2025.Janumet XR Tablet, Film Coated, Extended Release (Merck Sharp & Dohme LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 24/09/2025.Joint Formulary Committee. Sitagliptin with Metformin. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 24/09/2025.Metformin Hydrochloride. UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 24/09/2025.Metformin. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 24/09/2025.Metformin; Sitagliptin. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 24/09/2025.Sitagliptin and Metformin. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 24/09/2025.Sitagliptin Phosphate. UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 24/09/2025.Sitagliptin. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 24/09/2025.Sitagliptin/Metformin Hydrochloride 50 mg/1,000 mg Film-coated Tablets (Key Pharmaceuticals Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 24/09/2025.Sitagliptin/Metformin Indoco 50 mg/850 mg Film-coated Tablets (Indoco Remedies UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 24/09/2025.
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