Action and Spectrum

Actions and Spectrum: 

linagliptin is a medication for treating type 2 diabetes by improving blood sugar control. It works by inhibiting an enzyme called dipeptidyl peptidase-4 (DPP-4), which breaks down hormones that regulate blood sugar levels. By inhibiting DPP-4, linagliptin increases these hormones’ levels, which helps lower blood sugar levels. 

Regarding its spectrum, linagliptin is classified as a non-sulfonylurea DPP-4 inhibitor. It means that it is not structurally like the sulfonylurea class of medications, which work by stimulating the pancreas to produce more insulin.

Instead, linagliptin works by selectively inhibiting DPP-4, which helps to increase the levels of the hormones GLP-1 and GIP. These hormones stimulate insulin release from the pancreas and reduce the amount of glucose produced by the liver, which helps lower blood sugar levels. 

linagliptin has a relatively long half-life of approximately 24 hours, meaning it can be taken once a day. It is also excreted primarily through feces rather than urine, which makes it a good option for patients with impaired kidney function. 

Overall, linagliptin is a medication that can be an effective treatment option for type 2 diabetes. Its mechanism of action is related to the inhibition of DPP-4 and the subsequent increase in GLP-1 and GIP hormone levels rather than directly affecting the spectrum of light.

Drug Interaction

Adverse Reaction

Frequency Defined 

1-10% 

Nasopharyngitis  

Hypertriglyceridemia  

Hyperlipidemia  

Cough  

Weight gain 

Hypoglycemia 

Black Box Warning

Contraindication / Caution

Contraindication/Caution 

linagliptin is considered a safe and well-tolerated medication for treating type 2 diabetes. However, like all medications, they may not suit everyone, and certain situations require caution or avoidance. Here are some contraindications and cautions associated with linagliptin 

Contraindications: 

• Hypersensitivity: linagliptin should not be used in patients who have a known hypersensitivity to the drug or any of its components. 

Cautions: 

• Pancreatitis: there have been reports of pancreatitis (inflammation of the pancreas) in patients taking DPP-4 inhibitors, including linagliptin. Patients should be advised to seek medical attention if they experience persistent severe abdominal pain. 
• Renal impairment: linagliptin is eliminated primarily through the feces, and renal impairment is not expected to significantly affect its pharmacokinetics. However, dose adjustment may be necessary in patients with severe renal impairment. 
• Heart failure: there have been reports of heart failure in patients taking DPP-4 inhibitors, including linagliptin. Patients with a history of heart failure should be closely monitored while taking this medication. 
• Hypoglycemia: linagliptin is not known to cause hypoglycemia (low blood sugar) by itself, but it can increase the risk of hypoglycemia when combined with other medications that lower blood sugar, such as insulin or sulfonylureas. 
• Pregnancy and breastfeeding: the safety of linagliptin during pregnancy and breastfeeding has not been established, and it should only be used if the potential benefits outweigh the potential risks. 

Pregnancy / Lactation

Pregnancy consideration:  

It is not secure to administer linagliptin during pregnancy. 

Breastfeeding warnings:  

No data is available about the excretion of linagliptin in breastmilk. Avoid using in lactating women. 

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: No evidence of risk to the fetus is found in animal reproduction studies, and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a human product; Pregnant women must take care of the potential risks. 
• Category D: There is adequate data with sufficient evidence of human fetal risk from various platforms. However, despite potential dangers may be used only in emergencies for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. The drug is not for pregnant women. 
• Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology: 

linagliptin is a medication for treating type 2 diabetes by improving blood sugar control. It belongs to a class of drugs called dipeptidyl peptidase-4 (DPP-4) inhibitors. 

The primary target of linagliptin is the DPP-4 enzyme, which is involved in the degradation of the hormone’s glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). By inhibiting DPP-4, linagliptin increases the levels of GLP-1 and GIP, which stimulates insulin release from the pancreas and reduces the amount of glucose produced by the liver. This results in lower blood sugar levels. 

linagliptin is administered orally and is rapidly absorbed into the bloodstream. It has a half-life of approximately 24 hours, which allows for once-daily dosing. The liver does not extensively metabolize linagliptin, which is eliminated primarily through the feces, with minimal excretion in the urine. This makes it a good option for patients with impaired kidney function. 

linagliptin has a low potential for drug interactions and is not significantly bound to plasma proteins. It is not a substrate for cytochrome P450 (CYP) enzymes, which are responsible for the metabolism of many drugs. Therefore, it is not expected to interfere with the metabolism of other drugs, nor is it expected to be affected by drugs that inhibit or induce CYP enzymes. 

Pharmacodynamics: 

linagliptin is an oral antidiabetic medication in the dipeptidyl peptidase-4 (DPP-4) inhibitor class. It improves glycemic control in adults with type 2 diabetes mellitus. 

linagliptin exhibits selectivity towards DPP-4 and has a high binding affinity and slow dissociation rate, which allows for once-daily dosing. It also has a long half-life of approximately 24 hours, which enables sustained inhibition of DPP-4 and a continuous glucose-lowering effect. 

linagliptin does not cause hypoglycemia on its own, but when used with other antidiabetic medications such as sulfonylureas or insulin, the risk of hypoglycemia may increase. 

Pharmacokinetics:  

Absorption 

The bioavailability is 30% 

The peak plasma concentration is 8.9 nmol/L and was achieved in 1.5 hours 

The area under the curve is 139 nmol•h/L 

Distribution 

The protein-bound is 75-99%, which is concentration dependent 

The volume of distribution is 1,110 L 

Metabolism 

A small fraction of linagliptin is metabolized into an inactive metabolite 

Elimination and Excretion  

The half-life is 12 hours 

The terminal half-life is more than 100 hours 

The drug is removed 80% through the enterohepatic system and 5% through the urine  

The rate of renal clearance is 70 mL/min 

Adminstartion

Administration: 

linagliptin is an oral medication taken once daily, with or without food. The tablet should be swallowed whole with water and not crushed or chewed. 

The recommended dose of linagliptin for adults with type 2 diabetes is 5 mg once daily. In patients with renal impairment, the dose should be adjusted based on their estimated glomerular filtration rate (eGFR) as follows: 

• eGFR ≥ 45 mL/min/1.73 m²: no dose adjustment necessary 
• eGFR 30 to < 45 mL/min/1.73 m²: 5 mg every other day 
• eGFR < 30 mL/min/1.73 m²: linagliptin is not recommended 

linagliptin can be used alone or with other antidiabetic medications such as metformin, sulfonylureas, or insulin. Following your healthcare provider’s instructions regarding the timing and dose of linagliptin and any other medications you are taking is essential. 

If a dose of linagliptin is missed, it should be taken as soon as possible unless it is within 12 hours of the next scheduled dose. In that case, the missed dose should be skipped, and the regular dosing schedule should be resumed. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: linagliptin 

Pronounced: LIN-a-GLIP-tin 

Why do we use linagliptin? 

linagliptin is a medication that belongs to a class of drugs known as dipeptidyl peptidase-4 (DPP-4) inhibitors. It is mainly used to treat type 2 diabetes alone or in combination with other medications, diet, and exercise. 

The drug works by blocking the enzyme DPP-4, which breaks down the hormone incretin. Incretin is responsible for stimulating the release of insulin after a meal and helps to reduce the amount of glucose produced by the liver. By blocking DPP-4, linagliptin increases the incretin levels, leading to better blood sugar control in people with type 2 diabetes. 

linagliptin has several advantages over other DPP-4 inhibitors, including a long half-life, which means that it only needs to be taken once a day, and the fact that it is primarily eliminated through the liver makes it suitable for patients with kidney problems.