Sitagliptin and Metformin Hydrochloride

Serious warning

The strongest warning the FDA requires. It is printed in a box at the top of the label.

Quoted from the official label, section “Boxed Warning”.

Do not take it if

Quoted from the official label, section “Contraindications”.

How to take it

These directions are for this exact strength and form. Another one is different.

• Take sitagliptin and metformin hydrochloride tablets orally twice daily with meals. ( 2.1 )
• Individualize the dosage of sitagliptin and metformin hydrochloride tablets on the basis of the patient’s current regimen, effectiveness, and tolerability. ( 2.1 )
• The maximum recommended daily dose is 100 mg of sitagliptin and 2,000 mg of metformin HCl. ( 2.1 )
• The recommended starting dose in patients not currently treated with metformin is 50 mg sitagliptin and 500 mg metformin HCl twice daily, with gradual dose escalation recommended to reduce gastrointestinal side effects associated with metformin. ( 2.1 )
• The starting dose in patients already treated with metformin should provide sitagliptin dosed as 50 mg twice daily (100 mg total daily dose) and the dose of metformin already being taken. For patients taking metformin HCl 850 mg twice daily, the recommended starting dose of sitagliptin and metformin hydrochloride tablets is 50 mg and 1,000 mg metformin HCl twice daily. ( 2.1 )
• Prior to initiation, assess renal function with estimated glomerular filtration rate (eGFR) ( 2.2 ) o
• Do not use in patients with eGFR below 30 mL/min/1.73 m 2 . o Sitagliptin and metformin hydrochloride tablets are not recommended in patients with eGFR between 30 and less than 45 mL/min/1.73 m 2 .
• Sitagliptin and metformin hydrochloride tablets may need to be discontinued at time of, or prior to, iodinated contrast imaging procedures. ( 2.3 ) 2.1 Recommended Dosing
• Take sitagliptin and metformin hydrochloride tablets orally twice daily with meals.
• Individualize the dosage of sitagliptin and metformin hydrochloride tablets on the basis of the patient’s current regimen, effectiveness, and tolerability.
• The maximum recommended daily dose is 100 mg of sitagliptin and 2,000 mg of metformin hydrochloride (HCl).
• Do not split or divide sitagliptin and metformin hydrochloride tablets.
• The recommended starting dose in patients not currently treated with metformin is 50 mg sitagliptin and 500 mg metformin HCl twice daily, with gradual dose escalation recommended to reduce gastrointestinal side effects associated with metformin.
• The starting dose in patients already treated with metformin should provide sitagliptin dosed as 50 mg twice daily (100 mg total daily dose) and the dose of metformin already being taken. For patients taking metformin HCl 850 mg twice daily, the recommended starting dose of sitagliptin and metformin hydrochloride tablets is 50 mg sitagliptin and 1,000 mg metformin HCl twice daily. 2.2 Recommendations for Use in Renal Impairment
• Assess renal function prior to initiation of sitagliptin and metformin hydrochloride tablets and periodically thereafter.
• Sitagliptin and metformin hydrochloride is contraindicated in patients with an estimated glomerular filtration rate (eGFR) below 30 mL/min/1.73 m 2 [see Contraindications ( 4 ) and Warnings and Precautions ( 5.1 )].
• Sitagliptin and metformin hydrochloride tablets are not recommended in patients with an eGFR between 30 and less than 45 mL/min/1.73 m 2 because these patients require a lower dosage of sitagliptin than what is available in the fixed combination sitagliptin and metformin hydrochloride product. 2.3 Discontinuation for Iodinated Contrast Imaging Procedures Discontinue sitagliptin and metformin hydrochloride tablets at the time of, or prior to, an iodinated contrast imaging procedure in patients with an eGFR between 30 and 60 mL/min/1.73 m 2 ; in patients with a history of liver disease, alcoholism, or heart failure; or in patients who will be administered intra-arterial iodinated contrast. Re-evaluate eGFR 48 hours after the imaging procedure; restart sitagliptin and metformin hydrochloride tablets if renal function is stable [see Warnings and Precautions ( 5.1 )].

Quoted from the official label, section “Dosage & Administration”.

Other warnings

Quoted from the official label, section “Warnings”.

Pregnancy and breastfeeding

Quoted from the official label, section “OTC — Pregnancy or Breast Feeding”.

Other medicines

Quoted from the official label, section “Drug Interactions”.

If you take too much

In an emergency, call your local emergency number or a poison control centre.

Quoted from the official label, section “Overdosage”.

Use in children

• The safety and effectiveness of sitagliptin and metformin hydrochloride have not been established in pediatric patients.
• Three 20-week double-blind, placebo-controlled studies each with 34-week extensions were conducted to evaluate the efficacy and safety of sitagliptin in 410 pediatric patients aged 10 to 17 years with inadequately controlled type 2 diabetes, with or without insulin therapy (HbA1c 6.5-10% for patients not on insulin, HbA1c 7-10% for patients on insulin).
• At study entry, patients in study 1 were not treated with oral antihyperglycemic agents; patients in studies 2 and 3 were on maximally tolerated metformin therapy.
• The primary efficacy endpoint was the change from baseline in HbA1c after 20 weeks of therapy.
• The pre-specified primary efficacy analyses included data from study 1 and pooled data from studies 2 and 3, regardless of glycemic rescue or treatment discontinuation.
• In both efficacy analyses, the effect of treatment with sitagliptin was not significantly different from placebo.
• In study 1, the mean baseline HbA1c was 7.5%, and 12% of patients were on insulin therapy.
• At week 20, the change from baseline in HbA1c in patients treated with sitagliptin (N=95) was 0.06% compared to 0.23% in patients treated with placebo (N=95), a difference of -0.17% (95% CI:
• -0.62, 0.28).
• In studies 2 and 3, the mean baseline HbA1c was 8.0%, 15% of patients were on insulin and 72% were on metformin HCl doses of greater than 1,500 mg daily.
• At week 20, the change from baseline in HbA1c in patients treated with sitagliptin (N=107) was -0.23% compared to 0.09% in patients treated with placebo (N=113), a difference of -0.33% (95% CI:
• -0.70, 0.05).

Quoted from the official label, section “Pediatric Use”.

Use in older people

• Sitagliptin and Metformin Hydrochloride In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy and the higher risk of lactic acidosis.
• Renal function should be assessed more frequently in elderly patients. [see Contraindications ( 4 );
• Warnings and Precautions ( 5.1 , 5.4 );
• Clinical Pharmacology ( 12.3 ).] Sitagliptin Of the total number of subjects (N=3884) in clinical studies of sitagliptin, 725 patients were 65 years and over, while 61 patients were 75 years and over.
• No overall differences in safety or effectiveness were observed between subjects 65 years and over and younger subjects.
• While this and other reported clinical experience have not identified differences in responses between the elderly and younger patients, greater sensitivity of some older individuals cannot be ruled out.
• Metformin Controlled clinical studies of metformin did not include sufficient numbers of elderly patients to determine whether they respond differently from younger patients, although other reported clinical experience has not identified differences in responses between the elderly and young patients.

Quoted from the official label, section “Geriatric Use”.

Side effects

• The following adverse reactions are also discussed elsewhere in the labeling:
• Lactic Acidosis [see Warnings and Precautions ( 5.1 )]
• Pancreatitis [see Warnings and Precautions ( 5.2 )]
• Heart Failure [see Warnings and Precautions ( 5.3 )]
• Acute Renal Failure [see Warnings and Precautions ( 5.4 )]
• Vitamin B12 Deficiency [see Warnings and Precautions ( 5.5 )]
• Hypoglycemia with Concomitant Use with Insulin or Insulin Secretagogues [see Warnings and Precautions ( 5.6 )]
• Hypersensitivity Reactions [see Warnings and Precautions ( 5.7 )]
• Severe and Disabling Arthralgia [see Warnings and Precautions ( 5.8 )]
• Bullous Pemphigoid [see Warnings and Precautions ( 5.9 )]
• The most common adverse reactions reported in ≥5% of patients simultaneously started on sitagliptin and metformin and more commonly than in patients treated with placebo were diarrhea, upper respiratory tract infection, and headache. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Sandoz Inc., at 1-800-525-8747 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Sitagliptin and Metformin Coadministration in Patients with Type 2 Diabetes Inadequately Controlled on Diet and Exercise Table 1 summarizes the most common (≥5% of patients) adverse reactions reported (regardless of investigator assessment of causality) in a 24-week placebo-controlled factorial study in which sitagliptin and metformin were coadministered to patients with type 2 diabetes inadequately controlled on diet and exercise. Table 1:
• Sitagliptin and Metformin Coadministered to Patients with Type 2 Diabetes Inadequately Controlled on Diet and Exercise:
• Adverse Reactions Reported (Regardless of Investigator Assessment of Causality) in ≥5% of Patients Receiving Combination Therapy (and Greater than in Patients Receiving Placebo) * Table 1:
• Sitagliptin and Metformin Coadministered to Patients with Type 2 Diabetes Inadequately Controlled on Diet and Exercise:
• Adverse Reactions Reported (Regardless of Investigator Assessment of Causality) in ≥5% of Patients Receiving Combination Therapy (and Greater than in Patients Receiving Placebo) * Number of Patients (%) Placebo Sitagliptin 100 mg once daily Metformin HCl 500 mg/ Metformin HCl 1,000 mg twice daily † Sitagliptin 50 mg twice daily + Metformin HCl 500 mg/ Metformin HCl 1,000 mg twice daily † N = 176 N = 179 N = 364 † N = 372 † Diarrhea 7 (4.0) 5 (2.8) 28 (7.7) 28 (7.5) Upper Respiratory Tract Infection 9 (5.1) 8 (4.5) 19 (5.2) 23 (6.2) Headache 5 (2.8) 2 (1.1) 14 (3.8) 22 (5.9) * Intent-to-treat population. † Data pooled for the patients given the lower and higher doses of metformin. Sitagliptin Add-on Therapy in Patients with Type 2 Diabetes Inadequately Controlled on Metformin Alone In a 24-week placebo-controlled trial of sitagliptin 100 mg administered once daily added to a twice daily metformin regimen, there were no adverse reactions reported regardless of investigator assessment of causality in ≥5% of patients and more commonly than in patients given placebo. Discontinuation of therapy due to clinical adverse reactions was similar to the placebo treatment group (sitagliptin and metformin, 1.9%; placebo and metformin, 2.5%). Gastrointestinal Adverse Reactions The incidences of pre-selected gastrointestinal adverse experiences in patients treated with sitagliptin and metformin were similar to those reported for patients treated with metformin alone. See Table 2 . Table 2:
• Pre-selected Gastrointestinal Adverse Reactions (Regardless of Investigator Assessment of Causality) Reported in Patients with Type 2 Diabetes Receiving Sitagliptin and Metformin Table 2:
• Pre-selected Gastrointestinal Adverse Reactions (Regardless of Investigator Assessment of Causality) Reported in Patients with Type 2 Diabetes Receiving Sitagliptin and Metformin Number of Patients (%) Study of Sitagliptin and Metformin in Patients Inadequately Controlled on Diet and Exercise Study of Sitagliptin Add-on in Patients Inadequately Controlled on Metformin Alone Placebo Sitagliptin 100 mg once daily Metformin HCl 500 mg/ Metformin HCl 1,000 mg twice daily * Sitagliptin 50 mg twice daily + Metformin HCl 500 mg/ Metformin HCl 1,000 mg twice daily * Placebo and Metformin HCl ≥1500 mg daily Sitagliptin 100 mg once daily and Metformin HCl ≥1,500 mg daily N = 176 N = 179 N = 364 N = 372 N = 237 N = 464 Diarrhea 7 (4.0) 5 (2.8) 28 (7.7) 28 (7.5) 6 (2.5) 11 (2.4) Nausea 2 (1.1) 2 (1.1) 20 (5.5) 18 (4.8) 2 (0.8) 6 (1.3) Vomiting 1 (0.6) 0 (0.0) 2 (0.5) 8 (2.2) 2 (0.8) 5 (1.1) Abdominal Pain † 4 (2.3) 6 (3.4) 14 (3.8) 11 (3.0) 9 (3.8) 10 (2.2) * Data pooled for the patients given the lower and higher doses of metformin. † Abdominal discomfort was included in the analysis of abdominal pain in the study of initial therapy. Sitagliptin in Combination with Metformin and Glimepiride In a 24-week placebo-controlled study of sitagliptin 100 mg as add-on therapy in patients with type 2 diabetes inadequately controlled on metformin and glimepiride (sitagliptin, N=116; placebo, N=113), the adverse reactions reported regardless of investigator assessment of causality in ≥5% of patients treated with sitagliptin and more commonly than in patients treated with placebo were:
• hypoglycemia ( Table 3 ) and headache (6.9%, 2.7%). Sitagliptin in Combination with Metformin and Rosiglitazone In a placebo-controlled study of sitagliptin 100 mg as add-on therapy in patients with type 2 diabetes inadequately controlled on metformin and rosiglitazone (sitagliptin, N=181; placebo, N=97), the adverse reactions reported regardless of investigator assessment of causality through Week 18 in ≥5% of patients treated with sitagliptin and more commonly than in patients treated with placebo were:
• upper respiratory tract infection (sitagliptin, 5.5%; placebo, 5.2%) and nasopharyngitis (6.1%, 4.1%). Through Week 54, the adverse reactions reported regardless of investigator assessment of causality in ≥5% of patients treated with sitagliptin and more commonly than in patients treated with placebo were:
• upper respiratory tract infection (sitagliptin, 15.5%; placebo, 6.2%), nasopharyngitis (11.0%, 9.3%), peripheral edema (8.3%, 5.2%), and headache (5.5%, 4.1%). Sitagliptin in Combination with Metformin and Insulin In a 24-week placebo-controlled study of sitagliptin 100 mg as add-on therapy in patients with type 2 diabetes inadequately controlled on metformin and insulin (sitagliptin, N=229; placebo, N=233), the only adverse reaction reported regardless of investigator assessment of causality in ≥5% of patients treated with sitagliptin and more commonly than in patients treated with placebo was hypoglycemia ( Table 3 ). Hypoglycemia In the above studies (N=5), adverse reactions of hypoglycemia were based on all reports of symptomatic hypoglycemia; a concurrent glucose measurement was not required although most (77%) reports of hypoglycemia were accompanied by a blood glucose measurement ≤70 mg/dL. When the combination of sitagliptin and metformin was coadministered with a sulfonylurea or with insulin, the percentage of patients reporting at least one adverse reaction of hypoglycemia was higher than that observed with placebo and metformin coadministered with a sulfonylurea or with insulin ( Table 3 ). Table 3:
• Incidence and Rate of Hypoglycemia * (Regardless of Investigator Assessment of Causality) in Placebo-Controlled Clinical Studies of Sitagliptin in Combination with Metformin Coadministered with Glimepiride or Insulin Add-On to Glimepiride + Metformin (24 weeks) Sitagliptin 100 mg+ Metformin + Glimepiride Placebo + Metformin + Glimepiride N = 116 N = 113 Overall (%) 19 (16.4) 1 (0.9) Rate (episodes/patient-year) † 0.82 0.02 Severe (%) ‡ 0 (0.0) 0 (0.0) Add-On to Insulin + Metformin (24 weeks) Sitagliptin 100 mg+ Metformin + Insulin Placebo + Metformin + Insulin N = 229 N = 233 Overall (%) 35 (15.3) 19 (8.2) Rate (episodes/patient-year) † 0.98 0.61 Severe (%) ‡ 1 (0.4) 1 (0.4) * Adverse reactions of hypoglycemia were based on all reports of symptomatic hypoglycemia; a concurrent glucose measurement was not required:
• Intent-to-treat population. † Based on total number of events (i.e., a single patient may have had multiple events). ‡ Severe events of hypoglycemia were defined as those events requiring medical assistance or exhibiting depressed level/loss of consciousness or seizure. The overall incidence of reported adverse reactions of hypoglycemia in patients with type 2 diabetes inadequately controlled on diet and exercise was 0.6% in patients given placebo, 0.6% in patients given sitagliptin alone, 0.8% in patients given metformin alone, and 1.6% in patients given sitagliptin in combination with metformin. In patients with type 2 diabetes inadequately controlled on metformin alone, the overall incidence of adverse reactions of hypoglycemia was 1.3% in patients given add-on sitagliptin and 2.1% in patients given add-on placebo. In the study of sitagliptin and add-on combination therapy with metformin and rosiglitazone, the overall incidence of hypoglycemia was 2.2% in patients given add-on sitagliptin and 0.0% in patients given add-on placebo through Week 18. Through Week 54, the overall incidence of hypoglycemia was 3.9% in patients given add-on sitagliptin and 1.0% in patients given add-on placebo. In an additional, 30-week placebo-controlled, study of patients with type 2 diabetes inadequately controlled with metformin comparing the maintenance of sitagliptin 100 mg versus withdrawal of sitagliptin when initiating basal insulin therapy, the event rate and incidence of documented symptomatic hypoglycemia (blood glucose measurement ≤70 mg/dL) did not differ between the sitagliptin and placebo groups. Vital Signs and Electrocardiograms With the combination of sitagliptin and metformin, no clinically meaningful changes in vital signs or in ECG (including in QT c interval) were observed. Pancreatitis In a pooled analysis of 19 double-blind clinical trials that included data from 10,246 patients randomized to receive sitagliptin 100 mg/day (N=5429) or corresponding (active or placebo) control (N=4817), the incidence of acute pancreatitis was 0.1 per 100 patient-years in each group (4 patients with an event in 4708 patient-years for sitagliptin and 4 patients with an event in 3942 patient-years for control). Sitagliptin The most common adverse experience in sitagliptin monotherapy reported regardless of investigator assessment of causality in ≥5% of patients and more commonly than in patients given placebo was nasopharyngitis. Metformin The most common (>5%) established adverse reactions due to initiation of metformin therapy are diarrhea, nausea/vomiting, flatulence, abdominal discomfort, indigestion, asthenia, and headache. Laboratory Tests Sitagliptin The incidence of laboratory adverse reactions was similar in patients treated with sitagliptin and metformin (7.6%) compared to patients treated with placebo and metformin (8.7%). In most but not all studies, a small increase in white blood cell count (approximately 200 cells/microL difference in WBC vs placebo; mean baseline WBC approximately 6600 cells/microL) was observed due to a small increase in neutrophils. This change in laboratory parameters is not considered to be clinically relevant. Metformin In controlled clinical trials of metformin of 29 weeks duration, a decrease to subnormal levels of previously normal serum vitamin B 12 levels, without clinical manifestations, was observed in approximately 7% of patients. Such decrease, possibly due to interference with B 12 absorption from the B 12 -intrinsic factor complex, is, however, very rarely associated with anemia and appears to be rapidly reversible with discontinuation of metformin or vitamin B 12 supplementation. 6.2 Postmarketing Experience Additional adverse reactions have been identified during postapproval use of sitagliptin and metformin hydrochloride, sitagliptin, or metformin. Because these reactions are reported voluntarily from a population of uncertain size, it is generally not possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Hypersensitivity reactions including anaphylaxis, angioedema, rash, urticaria, cutaneous vasculitis, and exfoliative skin conditions including Stevens-Johnson syndrome; upper respiratory tract infection; hepatic enzyme elevations; acute pancreatitis, including fatal and non-fatal hemorrhagic and necrotizing pancreatitis [see Indications and Usage ( 1 )]; worsening renal function, including acute renal failure (sometimes requiring dialysis) and tubulointerstitial nephritis; severe and disabling arthralgia; bullous pemphigoid; constipation; vomiting; headache; myalgia; pain in extremity; back pain; pruritus; mouth ulceration; stomatitis; cholestatic, hepatocellular, and mixed hepatocellular liver injury; rhabdomyolysis.

Quoted from the official label, section “Adverse Reactions”.

What to discuss with your doctor

• Advise the patient to read the FDA-approved patient labeling (Medication Guide).
• Lactic Acidosis Explain the risks of lactic acidosis, its symptoms, and conditions that predispose to its development.
• Advise patients to discontinue sitagliptin and metformin hydrochloride tablets immediately and to promptly notify their healthcare provider if unexplained hyperventilation, myalgias, malaise, unusual somnolence or other nonspecific symptoms occur.
• Counsel patients against excessive alcohol intake and inform patients about the importance of regular testing of renal function while receiving sitagliptin and metformin hydrochloride tablets.
• Instruct patients to inform their doctor that they are taking sitagliptin and metformin hydrochloride tablets prior to any surgical or radiological procedure, as temporary discontinuation may be required [see Warnings and Precautions ( 5.1 )] .
• Pancreatitis Inform patients that acute pancreatitis has been reported during postmarketing use of sitagliptin and metformin hydrochloride tablets.
• Inform patients that persistent severe abdominal pain, sometimes radiating to the back, which may or may not be accompanied by vomiting, is the hallmark symptom of acute pancreatitis.
• Instruct patients to promptly discontinue sitagliptin and metformin hydrochloride tablets and contact their physician if persistent severe abdominal pain occurs [see Warnings and Precautions ( 5.2 )].
• Heart Failure Inform patients of the signs and symptoms of heart failure.
• Before initiating sitagliptin and metformin hydrochloride tablets, ask patients about a history of heart failure or other risk factors for heart failure including moderate to severe renal impairment.
• Instruct patients to contact their health care provider as soon as possible if they experience symptoms of heart failure, including increasing shortness of breath, rapid increase in weight or swelling of the feet [see Warnings and Precautions ( 5.3 )] .
• Vitamin B 12 Deficiency Inform patients about the importance of regular monitoring of hematological parameters while receiving sitagliptin and metformin hydrochloride tablets [see Warnings and Precautions ( 5.5 )].
• Hypoglycemia Inform patients that the incidence of hypoglycemia is increased when sitagliptin and metformin hydrochloride tablets are added to an insulin secretagogue (e.g., sulfonylurea) or insulin therapy.
• Explain to patients receiving sitagliptin and metformin hydrochloride tablets in combination with these medications the risks of hypoglycemia, its symptoms and treatment, and conditions that predispose to its development [see Warnings and Precautions ( 5.6 )].
• Hypersensitivity Reactions Inform patients that allergic reactions have been reported during postmarketing use of sitagliptin, one of the components of sitagliptin and metformin hydrochloride tablets.
• If symptoms of allergic reactions (including rash, hives, and swelling of the face, lips, tongue, and throat that may cause difficulty in breathing or swallowing) occur, patients must stop taking sitagliptin and metformin hydrochloride tablets and seek medical advice promptly.
• Severe and Disabling Arthralgia Inform patients that severe and disabling joint pain may occur with this class of drugs.
• The time to onset of symptoms can range from one day to years.
• Instruct patients to seek medical advice if severe joint pain occurs [see Warnings and Precautions ( 5.8 )].
• Bullous Pemphigoid Inform patients that bullous pemphigoid may occur with this class of drugs.
• Instruct patients to seek medical advice if blisters or erosions occur [see Warnings and Precautions ( 5.9 )].
• Females of Reproductive Age Inform females that treatment with sitagliptin and metformin hydrochloride tablets may result in ovulation in some premenopausal anovulatory women which may lead to unintended pregnancy [see Use in Specific Populations ( 8.3 )].
• Administration Instructions Inform patients that the tablets must never be split or divided before swallowing.
• Manufactured by Sandoz Private Limited, India for Sandoz Inc., Princeton, NJ 08540

Quoted from the official label, section “Patient Counseling Information”.

Strengths and forms

• FORMS AND STRENGTHS Tablets:
• 50 mg/500 mg tablets are pink, oval, biconvex, film-coated tablet with “SM01” debossed on one side.
• 50 mg/1,000 mg tablets are light red, oval, biconvex, film-coated tablet with “SM03” debossed on one side. Sitagliptin and Metformin Hydrochloride Tablets:
• 50 mg sitagliptin/500 mg metformin hydrochloride tablets
• 50 mg sitagliptin/1,000 mg metformin hydrochloride tablets ( 3 )

Quoted from the official label, section “Dosage Forms & Strengths”.

What it looks like and how it is packed

• Sitagliptin and metformin hydrochloride tablets are available as follows:
• 50 mg/500 mg tablets are pink, oval, biconvex, film-coated with “SM01” debossed on one side.
• NDC 0781-5801-60, 60 tablets in one bottle NDC 0781-5801-71, 180 tablets in one bottle NDC 0781-5801-05, 500 tablets in one bottle 50 mg/1,000 mg tablets are light red, oval, biconvex, film-coated with “SM03” debossed on one side.
• NDC 0781-5802-60, 60 tablets in one bottle NDC 0781-5802-71, 180 tablets in one bottle NDC 0781-5802-73, 360 tablets in one bottle
• Store at 20ºC to 25ºC (68ºF to 77ºF) [see USP Controlled Room Temperature].
• Protect from moisture.

Quoted from the official label, section “How Supplied”.

What is in it

• Sitagliptin and metformin hydrochloride tablets for oral use contain two oral antihyperglycemic drugs:
• sitagliptin and metformin hydrochloride. Sitagliptin Sitagliptin is an orally-active inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme. Sitagliptin is present in Sitagliptin and metformin hydrochloride tablets in the form of sitagliptin phosphate monohydrate. Sitagliptin phosphate monohydrate is described chemically as 7-[(3 R )-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3- a ]pyrazine phosphate (1:1) monohydrate with a molecular formula of C 16 H 15 F 6 N 5 O
• H 3 PO 4
• H 2 O and a molecular weight of 523.32. The structural formula is:
• Sitagliptin phosphate monohydrate is a white to off-white, crystalline, non-hygroscopic powder. It is soluble in water and N,N-dimethyl formamide; slightly soluble in methanol; very slightly soluble in ethanol, acetone, and acetonitrile; and insoluble in isopropanol and isopropyl acetate. Metformin hydrochloride Metformin hydrochloride ( N , N -dimethylimidodicarbonimidic diamide hydrochloride) is not chemically or pharmacologically related to any other classes of oral antihyperglycemic agents. Metformin hydrochloride is a white crystalline powder with a molecular formula of C 4 H 11 N 5
• HCl and a molecular weight of 165.63. Metformin hydrochloride is freely soluble in water and is practically insoluble in acetone, ether, and chloroform. The pK a of metformin is 12.4. The pH of a 1% aqueous solution of metformin hydrochloride is 6.68. The structural formula is as shown:
• Sitagliptin and metformin hydrochloride Sitagliptin and metformin hydrochloride are available for oral administration as tablets containing 64.25 mg sitagliptin phosphate monohydrate and metformin hydrochloride equivalent to:
• 50 mg sitagliptin as free base and 500 mg metformin hydrochloride (Sitagliptin and metformin hydrochloride 50 mg/500 mg) or 1,000 mg metformin hydrochloride (Sitagliptin and metformin hydrochloride 50 mg/1,000 mg). Each film-coated tablet of sitagliptin and metformin hydrochloride contains the following inactive ingredients:
• croscarmellose sodium, microcrystalline cellulose, povidone K30, sodium lauryl sulfate, and sodium stearyl fumarate. In addition, the film coating contains the following inactive ingredients:
• ferric oxide red, ferric oxide yellow, hypromellose, hydroxypropyl cellulose, talc, titanium dioxide, and triethyl citrate. sitagliptin chemical structure metformin chemical structure

Quoted from the official label, section “Description”.

Ingredients people check for

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Details

Source: NDC Directory · 2026-09-13 · not reviewed by a clinician

Source: US Food and Drug Administration, NDC Directory. Reuse terms: US government work (FDA).

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