Sitagliptin 25 mg Tablet, 30-count
🆔 Identity & classification
Where does this data come from?
🏷️ RxNorm drug class
This medicine belongs to the Dipeptidyl Peptidase 4 Inhibitor class.
Where does this data come from?
🏭 Manufacturer & labeler
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🩺 Clinical
Sitagliptin is used to lower blood sugar levels in adults with type 2 diabetes (condition in which blood sugar is too high because the body does not produce or use insulin normally). Sitagliptin is in a class of medications called dipeptidyl peptidase-4 (DPP-4) inhibitors. It works by increasing the amounts of certain natural substances that lower blood sugar when it is high. Sitagliptin is not used to treat type 1 diabetes (condition in which the body does not produce insulin and therefore cannot control the amount of sugar in the blood). Over time, people who have diabetes and high blood sug...
Read the full MedlinePlus article ↗- Sitagliptin helps your body manage blood sugar more effectively by keeping certain gut hormones active longer after you eat. Those hormones tell your pancreas to release more insul...
- What exactly does sitagliptin do — and will it cure my diabetes?
- On its own, sitagliptin is very unlikely to cause low blood sugar — that's actually one of its advantages. The reason is that it only kicks in when your blood sugar is already elev...
- Can sitagliptin make my blood sugar go too low?
Patient education
Supplement & herbal interactions
Some supplements/herbs that may interact with Sitagliptin — tap one for details:
Sitagliptin may be associated with lower levels of 1 nutrient — worth a chat with your pharmacist, not a cause for alarm.
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Ask a licensed pharmacist directly — free, answered by our team.
💊 What it looks like
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.
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UNII L11K75P92J
A mineral salt made from calcium and phosphate. It acts as a filler and binder in tablets to add bulk and help hold the medicine together in solid form.
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UNII M28OL1HH48
Croscarmellose sodium is a plant-based substance derived from cellulose. It acts as a disintegrant, helping tablets and capsules break down quickly in the digestive system so the medicine can be absorbed.
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UNII 70097M6I30
Magnesium stearate is a salt made from magnesium and stearic acid, a fatty substance. It's used in tablets and capsules as a lubricant and glidant to help ingredients flow smoothly during manufacturing and prevent sticking.
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UNII 817L1N4CKP
Malic acid is a naturally occurring organic acid found in fruits. It works as a buffer and flavor agent to maintain the medicine's pH balance and add tartness to the product.
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UNII OP1R32D61U
Microcrystalline cellulose is a purified form of cellulose, a natural fiber from plant sources. It acts as a binder and filler in tablets and capsules, helping hold ingredients together and give the medicine its shape and size.
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UNII G2M7P15E5P
Polyethylene glycol 3350 is a synthetic polymer used as a solvent, humectant, and thickening agent in medicines. It helps dissolve other ingredients, retain moisture in the product, and achieve the desired consistency.
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UNII 532B59J990
Polyvinyl alcohol is a synthetic polymer made from plant-derived materials. It's used as a binder to hold ingredients together, a film-former in coatings, and a thickener in liquid formulations.
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UNII FZ989GH94E
Povidone is a synthetic polymer made from a plastic-like material. It acts as a binder to hold tablet ingredients together and as a disintegrant to help the tablet break apart in your stomach so the medicine can be absorbed.
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UNII ETJ7Z6XBU4
Silicon dioxide is a naturally occurring mineral used as a glidant and anti-caking agent. It helps powder ingredients flow smoothly and prevents clumping during manufacturing and storage.
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UNII 7SEV7J4R1U
A powder made from a naturally occurring mineral. In medicines, talc works as a glidant and anti-caking agent, helping tablets and capsules flow smoothly during manufacturing and preventing clumping.
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UNII 15FIX9V2JP
Titanium dioxide is a bright white mineral powder commonly used as a colorant and opacifying agent. It makes pills and tablets white or lighter in color and helps make coatings non-transparent.
11 inactive ingredients listed in the exact product block matched to this NDC.
Where does this data come from?
ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per each | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | $5.63 | $168.87 / 30 tablets |
| Medicare drug plans payPart D · Q2 2026 | $2.83 | $84.77 / 30 tablets |
Where does this data come from?
🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Zituvio 25 mg 70710-1240-03 | Zydus | 30 tablets | $10.062 | — | Availability likely | — |
| Sitagliptin 25 mgthis 70710-1899-03 | Zydus | 30 tablets | — | — | FDA listed | — |
| Zituvio 25 mg 70771-1770-03 | Zydus | 30 tablets | — | — | FDA listed | — |
| Sitagliptin 25 mg 70771-1790-03 | Zydus | 30 tablets | — | — | FDA listed | — |
Where does this data come from?
⏳ Availability & generic status
FDA-approved generic versions are listed, and recent pricing/market data suggests they may be available — see Therapeutic equivalents.
Why the date isn’t exact: Generic timing can change because patents may be challenged, settled, licensed, added, removed, or worked around with a narrower label — and FDA approval does not always mean a pharmacy can get the generic today.
🛈 What do these terms mean?
- Patent
- Legal protection listed in the Orange Book that may delay generic approval or launch. Issued by the U.S. Patent & Trademark Office.
- Substance patent
- Covers the active drug molecule itself — the hardest to design around. A generic generally can’t launch until it expires.
- Formulation (product) patent
- Covers a specific formulation or dosage form. A generic can sometimes work around it with a different formulation.
- Method-of-use patent
- A patent covering one specific approved use of the drug — not necessarily the whole molecule. A generic can sometimes launch with a “skinny label” that carves out the protected use and keeps the others.
- Skinny label
- A generic label that omits a still-patented use when the FDA allows it — letting a generic reach the market for the unprotected uses.
- Exclusivity
- FDA-granted marketing protection, separate from patents — e.g. 5-yr new chemical entity, 7-yr orphan drug, or a +6-month pediatric extension.
- Paragraph IV
- A generic applicant’s formal challenge to a listed patent. It can potentially lead to earlier generic entry, but often involves litigation or a settlement.
- RLD / RS
- Reference Listed Drug — the brand product the FDA uses as the reference for generic applications. Reference Standard — the product the FDA expects generics to compare against in bioequivalence testing.
- TE / AB rating
- FDA therapeutic-equivalence rating. An AB rating generally means the FDA considers a generic therapeutically equivalent to — and substitutable for — the brand.
- LOE (loss of exclusivity)
- The latest patent or exclusivity currently listed — the loss-of-exclusivity / latest-listed-protection date shown on this page. Paragraph-IV challenges and settlements can move the real date earlier; FDA approval and a manufacturer’s decision to market can move it later.
Built from the FDA Orange Book. The bars above are scaled to each protection’s expiry; the red LOE marker is the last one to lapse.
| Patent | Type | Use code | Expires |
|---|---|---|---|
| US 10925871 ↗ | Drug product | — | Feb 25, 2035 |
| US 10925871 ↗ | Drug product | — | Feb 25, 2035 |
| US 10925871 ↗ | Drug product | — | Feb 25, 2035 |
Is there a generic version of SITAGLIPTIN 25 MG TABLET?
The FDA approved a generic — why can’t I get it at my pharmacy yet?
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🗺️ Medicaid utilization & spend
💊 Medicaid utilization by pack size
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
🔬 Reported adverse events (FAERS)
Top reported reactions
Reporter sex
Serious outcomes
Where does this data come from?
📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 70710-1899-03 You're viewing this | 30 TABLET in 1 BOTTLE (70710-1899-3) | 2023-11-30 | Active |
| 70710-1899-09 | 90 TABLET in 1 BOTTLE (70710-1899-9) | 2023-11-30 | Active |
You're viewing the smallest of 2 pack sizes for this product.
In Medicaid, this is the most-dispensed pack of this product — about 96% of fills over the last four reported quarters. See all packs ↓
Pack size FAQ
What quantity is in NDC 70710-1899-03?
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🧭 About this NDC listing & data coverage
What data is (and isn’t) available for this NDC — tap to expand
| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | ✓ Available |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | — Not published for this NDC Most self-administered / retail products have no J-code — that is normal. |
| Medicaid utilization (CMS SDUD) | ✓ Available |
Questions about this listing
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Sitagliptin Tablets are indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Limitations of Use Sitagliptin Tablets is not recommended in patients with type 1 diabetes mellitus. Sitagliptin Tablets have not been studied in patients with a history of pancreatitis.
It is unknown whether patients with a history of pancreatitis are at increased risk for the development of pancreatitis while using Sitagliptin Tablets. [see Warnings and Precautions (5.1) ]. Sitagliptin Tablets are a dipeptidyl peptidase-4 (DPP-4) inhibitor indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. ( 1 ) Limitations of Use: Sitagliptin Tablets are not recommended in patients with type 1 diabetes mellitus.
( 1 ) Sitagliptin Tablets has not been studied in patients with a history of pancreatitis. ( 1 )
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION The recommended dosage of Sitagliptin Tablets is 100 mg orally once daily. Sitagliptin Tablets can be taken with or without food. ( 2.1 ) Dosage adjustment is recommended for patients with eGFR less than 45 mL/min/1.73 m 2 .
( 2.2 ) Dosage Adjustment in Patients with Renal Impairment ( 2.2 ) eGFR greater than or equal to 30 mL/min/1.73 m 2 to less than 45 mL/min/1.73 m 2 eGFR less than 30 mL/min/1.73 m 2 (including patients with end stage renal disease [ESRD] on dialysis) 50 mg once daily 25 mg once daily
2.1Recommended Dosage The recommended dosage of Sitagliptin Tablets is 100 mg orally once daily. Sitagliptin Tablets can be taken with or without food.
2.2Recommendations for Use in Renal Impairment Assess renal function prior to initiation of Sitagliptin Tablets and periodically thereafter. For patients with an estimated glomerular filtration rate [eGFR] greater than or equal to 45 mL/min/1.73 m 2 to less than 90 mL/min/1.73 m 2 , no dosage adjustment for Sitagliptin Tablets is required. For patients with moderate renal impairment (eGFR greater than or equal to 30 mL/min/1.73 m 2 to less than 45 mL/min/1.73 m 2 ), the dosage of Sitagliptin Tablets is 50 mg once daily.
For patients with severe renal impairment (eGFR less than 30 mL/min/1.73 m 2 ) or with end-stage renal disease (ESRD) requiring hemodialysis or peritoneal dialysis, the dosage of Sitagliptin Tablets is 25 mg once daily. Sitagliptin Tablets may be administered without regard to the timing of dialysis.
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS 100 mg tablets are beige, round, biconvex, film coated tablets debossed with "12" on one side and "42" on the other side. 50 mg tablets are pale yellow, round, biconvex, film coated tablets debossed with "12" on one side and "41" on the other side. 25 mg tablets are white to off white, round, biconvex, film coated tablets debossed with "12" on one side and "40" on the other side. Tablets: 100 mg, 50 mg, and 25 mg ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS Sitagliptin Tablets is contraindicated in patients with a history of a serious hypersensitivity reaction to sitagliptin or any of the excipients in Sitagliptin Tablets. Serious hypersensitivity reactions, including anaphylaxis and angioedema have been reported with sitagliptin. [see Warnings and Precautions (5.5) ; Adverse Reactions (6.2) ]. History of a serious hypersensitivity reaction to sitagliptin or any of the excipients in Sitagliptin Tablets, such as anaphylaxis or angioedema ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Pancreatitis: There have been postmarketing reports of acute pancreatitis, including fatal and non-fatal hemorrhagic or necrotizing pancreatitis. If pancreatitis is suspected, promptly discontinue Sitagliptin Tablets. ( 5.1 ) Heart failure: Heart failure has been observed with two other members of the DPP-4 inhibitor class.
Consider risks and benefits of Sitagliptin Tablets in patients who have known risk factors for heart failure. Monitor patients for signs and symptoms. ( 5.2 ) Acute Renal Failure: Has been reported postmarketing, sometimes requiring dialysis.
Assessment of renal function is recommended prior to initiating Sitagliptin Tablets and periodically thereafter. ( 5.3 ) Hypoglycemia with Concomitant Use with Insulin or Insulin Secretagogues: Increased risk of hypoglycemia when used in combination with insulin and/or an insulin secretagogue. Lower dose of insulin or insulin secretagogue may be required.
( 5.4 ) Hypersensitivity Reactions: There have been postmarketing reports of serious allergic and hypersensitivity reactions in patients treated with sitagliptin such as anaphylaxis, angioedema, and exfoliative skin conditions including Stevens-Johnson syndrome. Promptly stop Sitagliptin Tablets, assess for other potential causes, institute appropriate monitoring and treatment. ( 5.5 ) Severe and Disabling Arthralgia: Has been reported in patients taking DPP-4 inhibitors.
Consider as a possible cause for severe joint pain and discontinue drug if appropriate. ( 5.6 ) Bullous Pemphigoid: There have been postmarketing reports requiring hospitalization in patients taking DPP-4 inhibitors. Tell patients to report development of blisters or erosions.
If bullous pemphigoid is suspected, discontinue Sitagliptin Tablets. ( 5.7 )
5.1Pancreatitis There have been postmarketing reports of acute pancreatitis, including fatal and non-fatal hemorrhagic or necrotizing pancreatitis, in patients taking sitagliptin. After initiation of Sitagliptin Tablets, patients should be observed carefully for signs and symptoms of pancreatitis. If pancreatitis is suspected, Sitagliptin Tablets should promptly be discontinued and appropriate management should be initiated.
It is unknown whether patients with a history of pancreatitis are at increased risk for the development of pancreatitis while using Sitagliptin Tablets.
5.2Heart Failure An association between dipeptidyl peptidase-4 (DPP-4) inhibitor treatment and heart failure has been observed in cardiovascular outcomes trials for two other members of the DPP-4 inhibitor class. These trials evaluated patients with type 2 diabetes mellitus and atherosclerotic cardiovascular disease. Consider the risks and benefits of Sitagliptin Tablets prior to initiating treatment in patients at risk for heart failure, such as those with a prior history of heart failure and a history of renal impairment and observe these patients for signs and symptoms of heart failure during therapy.
Advise patients of the characteristic symptoms of heart failure and to immediately report such symptoms. If heart failure develops, evaluate and manage according to current standards of care and consider discontinuation of Sitagliptin Tablets.
5.3Acute Renal Failure There have been postmarketing reports of worsening renal function, including acute renal failure, sometimes requiring dialysis. A subset of these reports involved patients with renal impairment, some of whom were prescribed inappropriate doses of sitagliptin. A return to baseline levels of renal impairment has been observed with supportive treatment and discontinuation of potentially causative agents.
Consideration can be given to cautiously reinitiating Sitagliptin Tablets if another etiology is deemed likely to have precipitated the acute worsening of renal function. Assessment of renal function is recommended prior to initiating Sitagliptin Tablets and periodically thereafter. A dosage adjustment is recommended in patients with moderate…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following adverse reactions are also discussed elsewhere in the prescribing information: Pancreatitis [see Warnings and Precautions (5.1) ] Heart Failure [see Warnings and Precautions (5.2) ] Acute Renal Failure [see Warnings and Precautions (5.3) ] Hypoglycemia with Concomitant Use with Insulin or Insulin Secretagogues [see Warnings and Precautions (5.4) ] Hypersensitivity Reactions [see Warnings and Precautions (5.5) ] Severe and Disabling Arthralgia [see Warnings and Precautions (5.6) ] Bullous Pemphigoid [see Warnings and Precautions (5.7) ] Most common adverse reactions (incidence ≥5%) are: upper respiratory tract infection, nasopharyngitis and headache.
In the add-on to sulfonylurea and add-on to insulin studies, hypoglycemia was also more commonly reported in patients treated with sitagliptin compared to placebo. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Zydus Pharmaceuticals (USA) Inc. at 1-877-993-8779 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical 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. Common Adverse Reactions In controlled clinical trials as both monotherapy and combination therapy with metformin, pioglitazone, or rosiglitazone and metformin, the overall incidence of adverse reactions, hypoglycemia, and discontinuation of therapy due to clinical adverse reactions with sitagliptin were similar to placebo.
In combination with glimepiride, with or without metformin, the overall incidence of clinical adverse reactions with sitagliptin was higher than with placebo, in part related to a higher incidence of hypoglycemia (see Table 3); the incidence of discontinuation due to clinical adverse reactions was similar to placebo. Two placebo-controlled monotherapy trials, one of 18- and one of 24-week duration, included patients treated with sitagliptin 100 mg daily, sitagliptin 200 mg daily, and placebo. Five placebo-controlled add-on combination therapy trials were also conducted: one with metformin; one with pioglitazone; one with metformin and rosiglitazone; one with glimepiride (with or without metformin); and one with insulin (with or without metformin).
In these trials, patients with inadequate glycemic control on a stable dosage of the background therapy were randomized to add-on therapy with sitagliptin 100 mg daily or placebo. The adverse reactions, excluding hypoglycemia, reported in ≥5% of patients treated with sitagliptin 100 mg daily and more commonly than in patients treated with placebo, are shown in Table 1 for the clinical trials of at least 18 weeks duration. Incidences of hypoglycemia are shown in Table 3.
Table 1: Placebo-Controlled Clinical Trials of Sitagliptin Monotherapy or Add-on Combination Therapy with Pioglitazone, Metformin + Rosiglitazone, or Glimepiride +/-Metformin: Adverse Reactions (Excluding Hypoglycemia) Reported in ≥5% of Patients and More Commonly than in Patients Given Placebo Intent-to-treat population Number of Patients (%) Monotherapy (18 or 24 weeks) Sitagliptin 100 mg Placebo N = 443 N = 363 Nasopharyngitis 23 (5.2) 12 (3.3) Combination with Pioglitazone (24 weeks) Sitagliptin 100 mg + Pioglitazone Placebo + Pioglitazone N = 175 N = 178 Upper Respiratory Tract Infection 11 (6.3) 6 (3.4) Headache 9 (5.1) 7 (3.9) Combination with Metformin + Rosiglitazone (18 weeks) Sitagliptin 100 mg + Metformin + Rosiglitazone Placebo + Metformin + Rosiglitazone N = 181 N = 97 Upper Respiratory Tract Infection 10 (5.5) 5 (5.2) Nasopharyngitis 11 (6.1) 4 (4.1) Combination with Glimepiride (+/- Metformin) (24 weeks) Sitagliptin 100 mg + Glimepiride (+/- Metformin) Placebo + Glimepiride (+/- Metformin) N = 222 N = 219 Nasopharyngitis 14 (6.3) 10 (4.6) Headache 13 (5.9) 5 (2.3) In the 24-week trial of patients rece…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS
7.1Insulin Secretagogues or Insulin Sitagliptin lowers blood glucose in patients with type 2 diabetes mellitus. Coadministration of sitagliptin with an insulin secretagogue (e.g., sulfonylurea) or insulin may require lower doses of the insulin secretagogue or insulin to reduce the risk of hypoglycemia. [see Warnings and Precautions (5.4) ].
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS
8.1Pregnancy Risk Summary The limited available data with sitagliptin in pregnant women are not sufficient to inform a drug-associated risk for major birth defects and miscarriage. There are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy [see Clinical Considerations]. No adverse developmental effects were observed when sitagliptin was administered to pregnant rats and rabbits during organogenesis at oral doses up to 30-times and 20-times, respectively, the 100 mg clinical dose, based on AUC [see Data] .
The estimated background risk of major birth defects is 6 to 10% in women with pre-gestational diabetes with a hemoglobin A1c (A1C) >7% and has been reported to be as high as 20 to 25% in women with a A1C >10%. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Clinical Considerations Disease-Associated Maternal and/or Embryo/Fetal Risk Poorly controlled diabetes in pregnancy increases the maternal risk for diabetic ketoacidosis, pre-eclampsia, spontaneous abortions, preterm delivery, and delivery complications.
Poorly controlled diabetes increases the fetal risk for major birth defects, still birth, and macrosomia related morbidity. Data Animal Data In embryo-fetal development studies, sitagliptin administered to pregnant rats and rabbits during organogenesis (gestation day 6 to 20) did not adversely affect developmental outcomes at oral doses up to 250 mg/kg (30-times the 100 mg clinical dose) and 125 mg/kg (20-times the 100 mg clinical dose), respectively, based on AUC. Higher doses in rats associated with maternal toxicity increased the incidence of rib malformations in offspring at 1,000 mg/kg, or approximately 100-times the clinical dose, based on AUC.
Placental transfer of sitagliptin was observed in pregnant rats and rabbits. Sitagliptin administered to female rats from gestation day 6 to lactation day 21 caused no functional or behavioral toxicity in offspring of rats at doses up to 1,000 mg/kg.
8.2Lactation Risk Summary There is no information regarding the presence of sitagliptin in human milk, the effects on the breastfed infant, or the effects on milk production. Sitagliptin is present in rat milk and therefore possibly present in human milk [see Data] . The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for sitagliptin and any potential adverse effects on the breastfed infant from sitagliptin or from the underlying maternal condition.
Data Sitagliptin is secreted in the milk of lactating rats at a milk to plasma ratio of 4:1.
8.4Pediatric Use The safety and effectiveness of Sitagliptin Tablets have not been established in pediatric patients. Pediatric information describing clinical trials in which efficacy was not demonstrated is approved for Merck Sharp and Dohme's sitagliptin tablets. However, due to Merck Sharp and Dohme's marketing exclusivity rights, this drug product is not labeled with that information.
8.5Geriatric Use Of the total number of subjects (N=3,884) in pre-approval clinical safety and efficacy trials of sitagliptin, 725 patients were 65 years and over, while 61 patients were 75 years and over. No overall differences in safety or effectiveness of sitagliptin have been observed between patients 65 years and over and younger patients. Because sitagliptin is substantially excreted by the kidney, and because aging can be associated with reduced renal function, renal function should be assessed more frequently in elderly patients [ see Dosage and Administration (2.2) , Warnings and Precautions (5.3) ]
8.6Renal Impairment Sitagliptin is excreted by the kidney, and sitagliptin exposure is increased in patients with renal impairment. Lower dosages are recommended in patients with eGFR less than 45 mL/min/1.73 m 2 (moderate and severe renal impa…
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary The limited available data with sitagliptin in pregnant women are not sufficient to inform a drug-associated risk for major birth defects and miscarriage. There are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy [see Clinical Considerations]. No adverse developmental effects were observed when sitagliptin was administered to pregnant rats and rabbits during organogenesis at oral doses up to 30-times and 20-times, respectively, the 100 mg clinical dose, based on AUC [see Data] .
The estimated background risk of major birth defects is 6 to 10% in women with pre-gestational diabetes with a hemoglobin A1c (A1C) >7% and has been reported to be as high as 20 to 25% in women with a A1C >10%. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Clinical Considerations Disease-Associated Maternal and/or Embryo/Fetal Risk Poorly controlled diabetes in pregnancy increases the maternal risk for diabetic ketoacidosis, pre-eclampsia, spontaneous abortions, preterm delivery, and delivery complications.
Poorly controlled diabetes increases the fetal risk for major birth defects, still birth, and macrosomia related morbidity. Data Animal Data In embryo-fetal development studies, sitagliptin administered to pregnant rats and rabbits during organogenesis (gestation day 6 to 20) did not adversely affect developmental outcomes at oral doses up to 250 mg/kg (30-times the 100 mg clinical dose) and 125 mg/kg (20-times the 100 mg clinical dose), respectively, based on AUC. Higher doses in rats associated with maternal toxicity increased the incidence of rib malformations in offspring at 1,000 mg/kg, or approximately 100-times the clinical dose, based on AUC.
Placental transfer of sitagliptin was observed in pregnant rats and rabbits. Sitagliptin administered to female rats from gestation day 6 to lactation day 21 caused no functional or behavioral toxicity in offspring of rats at doses up to 1,000 mg/kg.
🧒 Pediatric Use ▾
8.4Pediatric Use The safety and effectiveness of Sitagliptin Tablets have not been established in pediatric patients. Pediatric information describing clinical trials in which efficacy was not demonstrated is approved for Merck Sharp and Dohme's sitagliptin tablets. However, due to Merck Sharp and Dohme's marketing exclusivity rights, this drug product is not labeled with that information.
🧓 Geriatric Use ▾
8.5Geriatric Use Of the total number of subjects (N=3,884) in pre-approval clinical safety and efficacy trials of sitagliptin, 725 patients were 65 years and over, while 61 patients were 75 years and over. No overall differences in safety or effectiveness of sitagliptin have been observed between patients 65 years and over and younger patients. Because sitagliptin is substantially excreted by the kidney, and because aging can be associated with reduced renal function, renal function should be assessed more frequently in elderly patients [ see Dosage and Administration (2.2) , Warnings and Precautions (5.3) ]
🆘 Overdosage ▾
10 OVERDOSAGE In the event of an overdose with Sitagliptin Tablets, consider contacting the Poison Help line (1-800-222-1222) or a medical toxicologist for additional overdosage management recommendations. Employ the usual supportive measures dictated by the patient's clinical status. Per clinical judgment, consider removal of unabsorbed material from the gastrointestinal tract and clinical monitoring (including obtaining an ECG).
Sitagliptin is modestly dialyzable. In clinical trials, approximately 13.5% of the dose was removed over a 3-to 4-hour hemodialysis session. Prolonged hemodialysis may be considered if clinically appropriate.
It is not known if sitagliptin is dialyzable by peritoneal dialysis.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Sitagliptin is a DPP-4 inhibitor, which is believed to exert its actions in patients with type 2 diabetes mellitus by slowing the inactivation of incretin hormones. Concentrations of the active intact hormones are increased by sitagliptin, thereby increasing and prolonging the action of these hormones. Incretin hormones, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), are released by the intestine throughout the day, and levels are increased in response to a meal.
These hormones are rapidly inactivated by the enzyme, DPP-4. The incretins are part of an endogenous system involved in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase insulin synthesis and release from pancreatic beta cells by intracellular signaling pathways involving cyclic AMP.
GLP-1 also lowers glucagon secretion from pancreatic alpha cells, leading to reduced hepatic glucose production. By increasing and prolonging active incretin levels, sitagliptin increases insulin release and decreases glucagon levels in the circulation in a glucose-dependent manner. Sitagliptin demonstrates selectivity for DPP-4 and does not inhibit DPP-8 or DPP-9 activity in vitro at concentrations approximating those from therapeutic doses.
12.2Pharmacodynamics General In patients with type 2 diabetes mellitus, administration of sitagliptin led to inhibition of DPP-4 enzyme activity for a 24-hour period. After an oral glucose load or a meal, this DPP-4 inhibition resulted in a 2-to 3-fold increase in circulating levels of active GLP-1 and GIP, decreased glucagon concentrations, and increased responsiveness of insulin release to glucose, resulting in higher C-peptide and insulin concentrations. The rise in insulin with the decrease in glucagon was associated with lower fasting glucose concentrations and reduced glucose excursion following an oral glucose load or a meal.
In studies with healthy subjects, sitagliptin did not lower blood glucose or cause hypoglycemia. Sitagliptin and Metformin hydrochloride Coadministration In a two-day study in healthy subjects, sitagliptin alone increased active GLP-1 concentrations, whereas metformin alone increased active and total GLP-1 concentrations to similar extents. Coadministration of sitagliptin and metformin had an additive effect on active GLP-1 concentrations.
Sitagliptin, but not metformin, increased active GIP concentrations. It is unclear how these findings relate to changes in glycemic control in patients with type 2 diabetes mellitus. Cardiac Electrophysiology In a randomized, placebo-controlled crossover study, 79 healthy subjects were administered a single oral dose of sitagliptin 100 mg, sitagliptin 800 mg (8 times the recommended dose), and placebo.
At the recommended dose of 100 mg, there was no effect on the QTc interval obtained at the peak plasma concentration, or at any other time during the study. Following the 800 mg dose, the maximum increase in the placebo-corrected mean change in QTc from baseline was observed at 3 hours postdose and was 8 msec. This increase is not considered to be clinically significant.
At the 800 mg dose, peak sitagliptin plasma concentrations were approximately 11 times higher than the peak concentrations following a 100-mg dose. In patients with type 2 diabetes mellitus administered sitagliptin 100 mg (N=81) or sitagliptin 200 mg (N=63) daily, there were no meaningful changes in QTc interval based on ECG data obtained at the time of expected peak plasma concentration.
12.3Pharmacokinetics The pharmacokinetics of sitagliptin have been extensively characterized in healthy subjects and patients with type 2 diabetes mellitus. Following a single oral 100-mg dose to healthy volunteers, mean plasma AUC of sitagliptin was 8.52 μM•hr, C max was 950 nM, and apparent terminal half-life (t 1/2 ) was 12.4 hours. Plasma AUC of sitagl…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Sitagliptin is a DPP-4 inhibitor, which is believed to exert its actions in patients with type 2 diabetes mellitus by slowing the inactivation of incretin hormones. Concentrations of the active intact hormones are increased by sitagliptin, thereby increasing and prolonging the action of these hormones. Incretin hormones, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), are released by the intestine throughout the day, and levels are increased in response to a meal.
These hormones are rapidly inactivated by the enzyme, DPP-4. The incretins are part of an endogenous system involved in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase insulin synthesis and release from pancreatic beta cells by intracellular signaling pathways involving cyclic AMP.
GLP-1 also lowers glucagon secretion from pancreatic alpha cells, leading to reduced hepatic glucose production. By increasing and prolonging active incretin levels, sitagliptin increases insulin release and decreases glucagon levels in the circulation in a glucose-dependent manner. Sitagliptin demonstrates selectivity for DPP-4 and does not inhibit DPP-8 or DPP-9 activity in vitro at concentrations approximating those from therapeutic doses.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING Sitagliptin Tablets are supplied as follows: Tablet Strength Physical Description How Supplied NDC # 25 mg sitagliptin White to off white, round, biconvex, film coated tablets debossed with "12" on one side and "40" on the other side Bottles of 30 tablets with child-resistant closure. NDC 70710-1899-3 Bottles of 90 tablets with child-resistant closure. NDC 70710-1899-9 Bottles of 1,000 tablets NDC 70710-1899-0 50 mg sitagliptin Pale yellow, round, biconvex, film coated tablets debossed with "12" on one side and "41" on the other side Bottles of 30 tablets with child-resistant closure.
NDC 70710-1900-3 Bottles of 90 tablets with child-resistant closure. NDC 70710-1900-9 Bottles of 1,000 tablets NDC 70710-1900-0 100 mg sitagliptin Beige, round, biconvex, film coated tablets debossed with "12" on one side and "42" on the other side Bottles of 30 tablets with child-resistant closure. NDC 70710-1901-3 Bottles of 90 tablets with child-resistant closure.
NDC 70710-1901-9 Bottles of 1,000 tablets NDC 70710-1901-0 Storage Store at 20°C to 25°C (68°F to 77°F), excursions permitted between 15°C and 30°C (59°F and 86°F), [see USP Controlled Room Temperature]. Protect from moisture. Once the bottle has been opened, the product must be used within 6 months.
📋 Description ▾
11 DESCRIPTION Sitagliptin Tablets contain sitagliptin free base, an orally active inhibitor of the DPP-4 enzyme. Sitagliptin free base 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. The empirical formula is C 16 H 15 F 6 N 5 O and the molecular weight is 407.31.
The structural formula is: Sitagliptin free base is a white to off-white, non-hygroscopic powder. Sitagliptin free base is soluble in methanol and slightly soluble in water. Each film coated tablet of sitagliptin contains sitagliptin free base 25 mg, 50 mg, or 100 mg as active ingredient and the following inactive ingredients: anhydrous dibasic calcium phosphate, colloidal silicon dioxide, croscarmellose sodium, malic acid, magnesium stearate, microcrystalline cellulose, and povidone.
In addition, the film coating contains the following inactive ingredients: polyethylene glycol, polyvinyl alcohol, talc, and titanium dioxide. The 50 mg tablet's film coating also contains ferrosoferric oxide and iron oxide yellow. The 100 mg tablet's film coating also contains FD&C Yellow #6 Aluminum Lake and iron oxide yellow.
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💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling ( Medication Guide ). Pancreatitis Inform patients that acute pancreatitis has been reported during postmarketing use of sitagliptin. 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 Tablets and contact their physician if persistent severe abdominal pain occurs [see Warnings and Precautions (5.1) ]. Heart Failure Inform patients of the signs and symptoms of heart failure. Before initiating Sitagliptin 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 (5.2) ]. Hypoglycemia Inform patients that the incidence of hypoglycemia is increased when sitagliptin is added to a sulfonylurea or insulin. Explain to patients receiving Sitagliptin 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 (5.4) ].
Hypersensitivity Reactions Inform patients that allergic reactions have been reported during postmarketing use of sitagliptin. 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 Tablets and seek medical advice promptly. [see Warnings and Precautions (5.5) ]. 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 (5.6) ] . 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 (5.7) ]. Medication Guide available at www.zydususa.com/medguides/ or call 1-877-993-8779 Manufactured by: Zydus Lifesciences Ltd., Pharmez, Matoda, Ahmedabad, India. Distributed by: Zydus Pharmaceuticals (USA) Inc.
Route 31 North, Pennington, NJ 08534
💬 Medication Guide ▾
MEDICATION GUIDE Medication Guide Sitagliptin (sit" a glip' tin) tablets, for oral use What is the most important information I should know about Sitagliptin Tablets ? Sitagliptin Tablets can cause serious side effects, including: Inflammation of the pancreas (pancreatitis) which may be severe and lead to death . Certain medical problems make you more likely to get pancreatitis.
Before you start taking Sitagliptin Tablets , tell your healthcare provider if you have ever had: o pancreatitis o stones in your gallbladder (gallstones) o high blood triglyceride levels o a history of alcoholism o kidney problems Stop taking Sitagliptin Tablets and call your healthcare provider right away if you have pain in your stomach area (abdomen) that is severe and will not go away. The pain may be felt going from your abdomen through to your back. The pain may happen with or without vomiting.
These may be symptoms of pancreatitis. Heart failure . Heart failure means your heart does not pump blood well enough.
Before you start taking Sitagliptin Tablets , tell your healthcare provider if you have ever had heart failure or have problems with your kidneys. Contact your healthcare provider right away if you have any of the following symptoms: o increasing shortness of breath or trouble breathing, especially when you lie down o swelling or fluid retention, especially in the feet, ankles, or legs o an unusually fast increase in weight o unusual tiredness These may be symptoms of heart failure. What is Sitagliptin Tablets ?
Sitagliptin Tablets is a prescription medicine used along with diet and exercise to lower blood sugar in adults with type 2 diabetes. Sitagliptin Tablets is not for people with type 1 diabetes. If you have had pancreatitis (inflammation of the pancreas) in the past, it is not known if you have a higher chance of getting pancreatitis while you take Sitagliptin Tablets.
It is not known if Sitagliptin Tablets is safe and effective in children. Do not take Sitagliptin Tablets if: you are allergic to sitagliptin or any of the ingredients in Sitagliptin Tablets. See the end of this Medication Guide for a complete list of ingredients in Sitagliptin Tablets.
Symptoms of a serious allergic reaction to Sitagliptin Tablets may include rash, raised red patches on your skin (hives), or swelling of the face, lips, tongue, and throat that may cause difficulty breathing or swallowing. Before you take Sitagliptin Tablets , tell your healthcare provider about all of your medical conditions, including if you: have or have had inflammation of your pancreas (pancreatitis). have kidney problems. have heart failure. are pregnant or plan to become pregnant. It is not known if Sitagliptin Tablets will harm your unborn baby.
If you are pregnant, talk with your healthcare provider about the best way to control your blood sugar while you are pregnant. are breastfeeding or plan to breastfeed. It is not known if sitagliptin will pass into your breast milk. Talk with your healthcare provider about the best way to feed your baby if you are taking Sitagliptin Tablets.
Tell your healthcare provider about all the medicines you take , including prescription and over-the-counter medicines, vitamins, and herbal supplements. Know the medicines you take. Keep a list of your medicines and show it to your healthcare provider and pharmacist when you get a new medicine.
How should I take Sitagliptin Tablets ? Take Sitagliptin Tablets 1 time each day exactly as your healthcare provider tells you. You can take Sitagliptin Tablets with or without food.
Your healthcare provider will do blood tests to check how well your kidneys are working before and during your treatment with Sitagliptin Tablets. Your healthcare provider may tell you to take Sitagliptin Tablets along with other diabetes medicines. Low blood sugar can happen more often when Sitagliptin Tablets is taken with certain other diabetes medicines.
See " What are the possible side effects of Sitagliptin Tablets ? ". If…