linagliptin/metformin

Action and Spectrum

Actions and Spectrum: 

linagliptin is known as dipeptidyl peptidase-4 (DPP-4) inhibitors. It works by inhibiting the enzyme DPP-4, responsible for the breakdown of incretin hormones such as glucagon-like peptide-1 (GLP-1).

By inhibiting DPP-4, linagliptin increases the levels of GLP-1. Which, as a result, increases insulin production and decreases glucagon secretion. It also slows the gastric emptying. 

metformin helps improve the body’s response to insulin, making the body’s tissues more sensitive to the effects of insulin. This results in better utilization of glucose by the cells and decreased insulin resistance. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Hypoglycemia (22.9%) 

1-10% 

Nasopharyngitis (6.3%) 

Diarrhea (6.3%) 

Hypoglycemia (without sulfonylurea) (1.4%) 

Black Box Warning

Black Box Warning 

Accumulation of metformin can cause lactic acidosis. Immediately discontinue the therapy in this case. 

Contraindication / Caution

Contraindication/Caution 

• Hypersensitivity 
• Renal impairment 
• Hepatic impairment 
• Hypoglycemia 
• Surgical procedures 
• Other medical conditions 

Pregnancy / Lactation

Pregnancy consideration:  

Limited data are available regarding usage during pregnancy. 

Breastfeeding warnings:  

No information is available regarding the usage of the drug during pregnancy. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies do not show risk to the fetus in the first/later trimester.        
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women        
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.       
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.        
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.        
• Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

The combination of linagliptin and metformin provides additional mechanisms of action to help control blood glucose levels in individuals with type 2 diabetes. linagliptin increases insulin and decreases glucagon secretion through DPP-4 inhibition, while metformin improves insulin sensitivity, reduces hepatic glucose production, and decreases intestinal glucose absorption.   

Pharmacodynamics 

The combination of linagliptin and metformin provides complementary effects in managing blood glucose levels. linagliptin enhances insulin secretion and reduces glucagon secretion through DPP-4 inhibition, while metformin improves insulin sensitivity, reduces hepatic glucose production, and decreases intestinal glucose absorption. This combination helps to achieve better overall glycemic control in individuals with type 2 diabetes. 

Pharmacokinetics 

Absorption 

linagliptin is well absorbed after oral administration. It can be taken with or without food, as food does not significantly affect absorption. 

Distribution 

Once absorbed, linagliptin is extensively distributed throughout the body. It binds extensively to plasma proteins, primarily to albumin. 

Metabolism 

linagliptin undergoes minimal metabolism in the liver. It gets eliminated unchanged in the feces. 

Elimination and Excretion 

The elimination half-life of linagliptin is approximately 12 to 14 hours. It is primarily eliminated through the biliary system into the feces, with minimal renal excretion.

Adminstartion

Administration: 

The usual recommended dose of linagliptin is 5 mg once daily. metformin dosage can vary depending on the individual’s needs and response to treatment. It is typically initiated at a low dose and gradually increased as tolerated. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: linagliptin/metformin 

Pronounced: lina-glip-tin/met-for-min 

Why do we use linagliptin/metformin? 

linagliptin/metformin is a combination medication for treating type 2 diabetes mellitus. It combines two antidiabetic agents: linagliptin (a dipeptidyl peptidase-4 inhibitor) and metformin (a biguanide). The combination is prescribed when blood sugar control is not adequately achieved with metformin alone or when dual therapy is deemed appropriate.