Sitagliptinum Uses, Dosage, Side Effects, Food Interaction and all others data.

The DPP-4 inhibitors are a class of agents that act as incretin enhancers. By inhibiting the DPP-4 enzyme, Sitagliptinum increases the levels of two known active incretin hormones, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). 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. GLP-1 also lowers glucagon secretion from pancreatic alpha cells, leading to reduced hepatic glucose production. This mechanism is unlike the mechanism seen with sulfonylureas; sulfonylureas cause insulin release even when glucose levels are low, which can lead to sulfonylurea-induced hypoglycemia in patients with type ll diabetes and in normal subjects. Sitagliptinum demonstrates high selectivity for DPP-4 and does not inhibit closely-related enzymes DPP-8 or DPP-9 at therapeutic concentrations.

Sitagliptinum inhibits DPP-4 which leads to increased levels of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide(GIP), decreased levels of glucagon, and a stronger insulin response to glucose.

Trade Name Sitagliptinum
Availability Prescription only
Generic Sitagliptin
Sitagliptin Other Names Sitagliptin, Sitagliptina, Sitagliptine, Sitagliptinum
Related Drugs Farxiga, metformin, Trulicity, Lantus, Victoza, Tresiba, Levemir
Formula C16H15F6N5O
Weight Average: 407.3136
Monoisotopic: 407.118079357
Protein binding


Groups Approved, Investigational
Therapeutic Class Dipeptidyl Peptidase-4 (DPP-4) inhibitor
Available Country
Last Updated: September 19, 2023 at 7:00 am


Monotherapy: Sitagliptinum is used for an adjunct to diet and exercise to improve glycemic control in patients with type ll diabetes mellitus.

Combination with Metformin: Sitagliptinum is used for patients with type 2 diabetes mellitus to improve glycemic control in combination with Metformin as initial therapy or when the single agent alone, with diet and exercise, does not provide adequate glycemic control.

Combination with a Sulfonylurea: Sitagliptinum is used for patients with type ll diabetes mellitus to improve glycemic control in combination with a sulfonylurea when treatment with the single agent alone, with diet and exercise, does not provide adequate glycemic control.

Combination with a Thiazolidinediones: Sitagliptinum is used for patients with type ll diabetes mellitus to improve glycemic control in combination with a thiazolidinedi- one when treatment with the single agent alone, with diet and exercise, does not provide adequate glycemic control.

Combination with Metformin and a Sulfonylurea: Sitagliptinum is used for patients with type ll diabetes mellitus to improve glycemic control in combination with Metformin and a sulfonylurea when dual therapy with these agents, with diet and exercise, does not provide adequate glycemic control.

Sitagliptinum is also used to associated treatment for these conditions: Type 2 Diabetes Mellitus

How Sitagliptinum works

Inhibition of DPP-4 by sitagliptin slows DPP-4 mediated inactivation of incretins like GLP-1 and GIP. Incretins are released throughout the day and upregulated in response to meals as part of glucose homeostasis. Reduced inhibition of incretins increase insulin synthesis and decrease glucagon release in a manner dependant on glucose concentrations. These effects lead to an overall increase in blood glucose control which is demonstrated by reduced glycosylated hemoglobin (HbA1c).


Sitagliptinum dosage

The recommended dose of Sitagliptinum is 100 mg once daily as monotherapy or as combination therapy with Metformin, a sulfonylurea, a thiazolidinedione, or Metformin plus a sulfonylurea. Sitagliptinum can be taken with or without food.

Elderly: No dosage adjustment is required based solely on age. The drug is excreted by the kidney. As elderly patients are more likely to have decreased renal function, caution should be taken in dose selection in the elderly.

Pediatric use: There is no data on use of Sitagliptinum in patients younger than 18 years of age and therefore not recommended.

Side Effects

The most common adverse reactions are; upper respiratory tract infection, nasopharyngitis and headache. Hypoglycemia may occur in patients treated with the combination of Sitagliptinum and sulfonylurea and add-on to insulin.


Animal studies in pregnancy have shown no adverse effects on the mother or offspring at normal doses, however these results are not always applicable to humans. There is currently a voluntary registry of fetal exposure. Animal studies at 100 times the maximum recommended human dose resulted in an increase in rib malformations. Sitagliptinum is excreted in the milk of rats but it is not known if it would also be expressed in human breast milk. Because many drugs are expressed in human breast milk, the risk and benefit of prescribing the medication must be considered. There is currently a lack of safety and effectiveness data in pediatric patients. No differences in safety and efficacy were observed in geriatric patients compared to younger patients, however caution should be used in this population as they are more likely to have reduced renal function. Sitagliptinum has also been associated with a 34% relative risk increase for all cause infection. There was no significant difference in patient response across sex, age, race, ethnicity, and BMI.


Sitagliptinum should not be used in patients with type l diabetes or for the treatment of diabetic ketoacidosis. Dosage adjustment is recommended in patients with moderate or severe renal insufficiency and in patients with ESRD. Assessment of renal function is recommended prior to initiating Sitagliptinum and periodically thereafter. When used with a sulfonylurea, a lower dose of sulfonylurea may be required to reduce the risk of hypoglycemia. There have been post marketing reports of serious allergic and hypersensitivity reactions in patients treated with Sitagliptinum such as anaphylaxis, angioedema, and exfoliative skin conditions including Stevens-Johnson syndrome. In such cases, promptly stop Sitagliptinum, assess for other potential causes, and institute appropriate monitoring and treatment, and initiate alternative treatment for diabetes. There have been no clinical studies establishing conclusive evidence of macrovascular risk.


Co-administration of Digoxin and Sitagliptinum may slightly increase the mean peak drug concentration of Digoxin. But no dosage adjustment of Digoxin or Sitagliptinum is recommended.

Food Interaction

  • Take with or without food.

[Moderate] GENERALLY AVOID: Alcohol may cause hypoglycemia or hyperglycemia in patients with diabetes.

Hypoglycemia most frequently occurs during acute consumption of alcohol.

Even modest amounts can lower blood sugar significantly, especially when the alcohol is ingested on an empty stomach or following exercise.

The mechanism involves inhibition of both gluconeogenesis as well as the counter-regulatory response to hypoglycemia.

Episodes of hypoglycemia may last for 8 to 12 hours after ethanol ingestion.

By contrast, chronic alcohol abuse can cause impaired glucose tolerance and hyperglycemia.

Moderate alcohol consumption generally does not affect blood glucose levels in patients with well controlled diabetes.

A disulfiram-like reaction (e.g., flushing, headache, and nausea) to alcohol has been reported frequently with the use of chlorpropamide and very rarely with other sulfonylureas.

MANAGEMENT: Patients with diabetes should avoid consuming alcohol if their blood glucose is not well controlled, or if they have hypertriglyceridemia, neuropathy, or pancreatitis.

Patients with well controlled diabetes should limit their alcohol intake to one drink daily for women and two drinks daily for men (1 drink = 5 oz wine, 12 oz beer, or 1.5 oz distilled spirits) in conjunction with their normal meal plan.

Alcohol should not be consumed on an empty stomach or following exercise.

Sitagliptinum Disease Interaction

Major: pancreatitisModerate: renal dysfunction

Volume of Distribution


Elimination Route

Sitagliptinum is 87% orally bioavailable and taking it with or without food does not affect its pharmacokinetics. Sitagliptinum reaches maximum plasma concentration in 2 hours.

Half Life

Approximately 12.4 hours. Other studies have reported a half life of approximately 11 hours.



Elimination Route

Approximately 79% of sitagliptin is excreted in the urine as the unchanged parent compound. 87% of the dose is eliminated in the urine and 13% in the feces.

Pregnancy & Breastfeeding use

Pregnancy: Pregnancy Category B. Safety of Sitagliptinum in pregnant women has not been established. Sitagliptinum should be used during pregnancy only if the potential benefit justifies the potential risk of the fetus.

Nursing Mothers: It is not known whether Sitagliptinum is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Sitagliptinum is administered to a nursing woman.


History of a serious hypersensitivity reaction to Sitagliptinum, such as anaphylaxis or angioedema.

Special Warning

Renal Insufficiency-

  • Mild renal insufficiency (creatinine clearance [CrCl] >50 mL/min, approximately corresponding to serum creatinine levels of >1.7 mg/dL in men and >1.5 mg/dL in women), no dosage adjustment for Sitagliptinum is required.
  • Moderate renal insufficiency (CrCl >30 to 1.7 to 1.5 to
  • Severe renal insufficiency (CrCl 3.0 mg/dL in men and > 2.5 mg/dL in women) or with end -stage renal disease (ESRD) requiring hemodialysis or peritoneal dialysis, the dose of Sitagliptinum is 25 mg once daily. Sitagliptinum may be administered without regard to the timing of hemodialysis. Concomitant Use with a Sulfonylurea- When Sitagliptinum is used in combination with a sulfonylurea, a lower dose of sulfonylurea may be required to reduce the risk of hypoglycemia.

Hepatic Insufficiency: No dosage adjustment is necessary for patients with mild to moderate hepatic insufficiency. Sitagliptinum has not been studied in patients with severe hepatic insufficiency.

Acute Overdose

During controlled clinical trials in healthy subjects, single doses of up to 800 mg sitagliptin were administered. Minimal increases in QTc, not considered to be clinically relevant, were observed in one study at a dose of 800 mg sitagliptin. There is no experience with doses above 800 mg in clinical studies. In Phase I multiple-dose studies, there were no dose-related clinical adverse reactions observed with sitagliptin with doses of up to 600 mg per day for periods of up to 10 days and 400 mg per day for periods of up to 28 days.

In the event of an overdose, it is reasonable to employ the usual supportive measures, e.g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring (including obtaining an electrocardiogram), and institute supportive therapy if required.

Sitagliptinum is modestly dialysable. In clinical studies, approximately 13.5 % of the dose was removed over a 3- to 4-hour hemodialysis session. Prolonged haemodialysis may be considered if clinically appropriate. It is not known if sitagliptin is dialysable by peritoneal dialysis.

Storage Condition

Keep out of the reach of children. Store below 30° C. Keep in the original package in a cool & dry place in order to protect from light and moisture.

Innovators Monograph

You find simplified version here Sitagliptinum

Sitagliptinum contains Sitagliptin see full prescribing information from innovator Sitagliptinum Monograph, Sitagliptinum MSDS, Sitagliptinum FDA label


What is Sitagliptinum used for?

Sitagliptinum used to treat type 2 diabetes. Type 2 diabetes is an illness where the body does not make enough insulin, or the insulin that it makes does not work properly.

How safe is Sitagliptinum?

Sitagliptinum may increase your risk of pancreatitis.This can be severe and sometimes fatal. Before you start taking this drug, tell your doctor if you've ever had pancreatitis.

How does Sitagliptinum work?

Sitagliptinum work by increasing the amount of insulin that your body makes. Insulin is the hormone that controls sugar levels in your blood.

What are the common side effects of Sitagliptinum?

Common side effects of Sitagliptinum are include:

  • runny or stuffy nose
  • diarrhea
  • headache
  • constipation
  • swelling of extremities
  • nausea
  • sore throat
  • osteoarthritis
  • upper respiratory tract infection
  • hypersensitivity reactions (severe allergic reaction, skin swelling, rash, hives, inflamed blood vessels under the skin, and exfoliative skin conditions [including Stevens-Johnson syndrome])
  • liver enzyme elevations
  • acute pancreatitis
  • constipation
  • vomiting
  • worsening renal function, including acute kidney failure
  • severe and disabling joint pain
  • muscle pain
  • pain in extremities
  • back pain
  • low blood sugar

Is Sitagliptinum safe during pregnancy?

Sitagliptinum is generally not recommended in pregnancy.

Is Sitagliptinum safe during breastfeeding?

Sitagliptinum is generally not recommended in  while breastfeeding.

Can I drink alcohol with Sitagliptinum?

Yes, you can drink alcohol while taking Sitagliptinum. But it's best to drink no more than 2 units per day. Drinking more than this can increase your risk of low blood sugar.

Can I drive after taking Sitagliptinum?

Taking Sitagliptinum should not affect your ability to drive, cycle or use machinery and tools. If your blood sugar levels become too low, this can reduce your concentration. If this happens to you, do not drive, cycle or use machines or tools until you feel better.

How quickly does Sitagliptinum work?

Sitagliptinum on your blood sugar levels may begin quickly, within the first 1 to 2 weeks. You may start to see your blood sugar drop after just a few doses.

When should I take Sitagliptinum before or after meals?

You can take Sitagliptinum before or after a meal. If you have been prescribed a combination tablet of sitagliptin with metformin you should take one tablet twice a day, after meals.

Can I take Sitagliptinum long time?

Sitagliptinum have to take it for a long time, even for the rest of your life.

What happens if I stop Sitagliptinum?

If you don't take it at all, Your symptoms of type 2 diabetes may not improve or may even get worse. If you stop taking it suddenly, If your condition improved while you were taking sitagliptin and then you suddenly stop taking it, your symptoms of type 2 diabetes may come back.

How often do I take Sitagliptinum?

You will normally take Sitagliptinum once a day as directed by your doctor. You can take it in the morning or evening, but it’s best to try to take it at the same time each day.

What happen if I miss my Sitagliptinum?

If you miss a dose, take it as soon as you remember. If it’s time for your next dose, skip the medication and get back on your regular schedule. Don’t double up and take two tablets at the same time, or take one-half of a tablet.

Is Sitagliptinum bad for my liver?

Sitagliptinum may have a negative effect on the liver for certain patients.

Can I stop taking Sitagliptinum?

Do not stop taking Sitagliptinum without speaking to your doctor.

Can I take overdose of Sitagliptinum?

If you take too much Sitagliptinum, call your local Poison Control Center right away.

Can Sitagliptinum cause weight loss?

This medicine does not usually make you put on weight.

Can I take Sitagliptinum at night?

You can take Sitagliptinum in the morning or at night.

*** Taking medicines without doctor's advice can cause long-term problems.