Linagliptin: Uses, Side Effects, and Precautions


What is Linagliptin?

Linagliptin is an active pharmaceutical ingredient (API), and it is a medication that lowers blood sugar levels and helps in treating type 2 diabetes. Dipeptidyl peptidase-4 (DPP-4) inhibitors are the class of drugs that Linagliptin belongs to. The API is the substance in a medication that is responsible for its therapeutic effects.

Linagliptin is chemically known as:-

(S)-3-[(3S)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6-dihydro-2H-pyridazin-3-one. It can be recognized as a white to off-white powder, which is soluble in methanol and ethanol and slightly soluble in water.

Molar mass: 472.54 g/mol

Formula: C25H26N8O2

Boiling point: 661.2 °C

ChEMBL Id: 237500

ChemSpider ID: 8271879


Other names: BI-1356

What are Major Linagliptin Uses?

Linagliptin is used to improve blood sugar control in adults with type 2 diabetes, either alone or in combination with other diabetes medications such as metformin, sulfonylureas, or thiazolidinediones. Usually, it is prescribed to be taken once daily with or without food. It works by inhibiting the activity of an enzyme called dipeptidyl peptidase-4 (DPP-4), which results in an increase in the levels of incretin hormones. These hormones help regulate the amount of insulin released by the pancreas in response to blood sugar levels.

Linagliptin is not recommended for use in people with type 1 diabetes or in those with diabetic ketoacidosis, a serious condition in which Ketones are formed. These are high levels of blood acids that the body produces. It is also not advised for use in people with severe kidney or liver impairment.

The safety and effectiveness of linagliptin have been established in clinical trials, and it is considered an effective treatment for type 2 diabetes. However, as with all medications, it is important to discuss the potential risks and benefits with a healthcare provider before starting treatment.

Some Major Linagliptin Side Effects

Linagliptin is generally well-tolerated, but like all medications, few side effects can be cited in some people. Common side effects of linagliptin include:

  • Upper respiratory tract infections such as the common cold, sinusitis, and pharyngitis
  • Nasopharyngitis (inflammation of the nose and throat)
  • Stuffy or runny nose
  • Sore throat
  • Headache
  • Back pain
  • Diarrhea
  • Nausea

In rare cases, more serious side effects can occur, such as:

  • Allergic reactions (itchiness, rash, hives, swelling of the face, lips, tongue, or throat, difficulty breathing)
  • Pancreatitis (severe pain in the upper abdomen, nausea, vomiting)
  • Liver problems (yellowing of the skin or eyes, dark urine, abdominal pain)
  • Hypoglycemia (low blood sugar)
  • Urinary tract infection

It is crucial to talk to your healthcare provider about any side effects you experience and report to your doctor if you have any history of liver or pancreatic disease before taking linagliptin.

Precautions One Should Take Before Consuming Linagliptin

Linagliptin is a medication that should be used with caution in certain individuals and under certain conditions. Some precautions to be aware of before taking linagliptin include:

  • Any history of pancreatitis must be discussed with your healthcare provider, as there is a risk of it being triggered by the use of linagliptin.
  • If you have liver problems, then you need to inform your healthcare provider. As they may need to monitor your liver function more frequently while you are taking linagliptin.
  • If you have kidney problems, then you need to inform your healthcare provider. As they may need to adjust your dosage of linagliptin or may recommend a different medication.
  • If you are pregnant or planning to have a baby, it is important to discuss the potential risks and benefits of taking linagliptin with your healthcare provider.
  • If you are breastfeeding, it is not known if linagliptin passes into breast milk. So, it is important to discuss with your healthcare provider about the potential risks and benefits of taking linagliptin while breastfeeding.

It is important to provide your healthcare provider with a list of all medications, vitamins, and supplements you are currently taking, so they can determine if linagliptin is safe and appropriate for you to take.

Who Should Not Take Linagliptin?

There are certain individuals who should not take linagliptin or who should use it with caution. These include:

  • For individuals with type 1 diabetes, linagliptin is not indicated for this condition.
  • For individuals with diabetic ketoacidosis, linagliptin is not indicated for this condition.
  • Individuals with a history of pancreatitis, as linagliptin may increase the risk of pancreatitis.
  • Individuals with severe renal impairment, as the safety and efficacy of linagliptin have not been established in this population.
  • Individuals who are allergic to linagliptin or any of its ingredients.
  • Individuals who are taking medications that interact with linagliptin, such as gemfibrozil, may increase the risk of side effects.

It is significant to inform your healthcare provider before taking linagliptin if you have any of these conditions or are taking any of these medications. Your healthcare provider may need to adjust your dosage or recommend a different medication if you are unable to take linagliptin.

How does Linagliptin work as Medicine to Treat Type 2 Diabetes?

Linagliptin works by inhibiting the activity of the enzyme dipeptidyl peptidase-4 (DPP-4). DPP-4 is an enzyme that breaks down incretin hormones, such as GLP-1 (glucagon-like peptide-1) and GIP (glucose-dependent insulinotropic peptide), which are produced by the gut and play a key role in regulating glucose metabolism.

By inhibiting DPP-4, linagliptin increases the levels of incretin hormones in the body, which leads to an increase in insulin secretion and a decrease in glucagon secretion. It helps to improve glucose metabolism in people with type 2 diabetes and also lowers their blood sugar levels.

Linagliptin also has another mechanism of action which is to slow down the absorption of glucose in the gut by inhibiting the SGLT1 transporter.

Linagliptin is usually taken once daily, and the dosage may be adjusted based on the individual’s response to treatment and blood sugar levels. It is typically used in combination with diet and exercise and can be used alone or in combination with other diabetes medications such as metformin or sulfonylurea.


Linagliptin is typically manufactured using synthetic chemical processes. The raw materials used in the synthesis of linagliptin include various chemicals such as amino acids, organic acids, and solvents. These raw materials are combined and reacted in a series of steps to produce the final API. There are various Linagliptin active pharma ingredient manufacturers.

It’s important to mention that the production of linagliptin API must comply with the regulations of each country, the WHO, and the FDA, among others, to guarantee the quality, efficacy, and safety of the API.


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