Generic Medicine Info
Indications and Dosage
Type 2 diabetes mellitus
Adult: As monotherapy or in combination with other antidiabetic agents: 5 mg once daily.
May be taken with or without food.
Special Precautions
Patient with a history of pancreatitis and angioedema with another dipeptidyl peptidase-4 (DDP-4) inhibitor. Patients who are at risk of having heart failure (e.g. history of renal impairment or heart failure). Not indicated for use in patients with type 1 diabetes mellitus or diabetic ketoacidosis. Pregnancy and lactation.
Adverse Reactions
Significant: Heart failure (increased risk of hospitalisation); severe and disabling arthralgia; bullous pemphigoid.
Gastrointestinal disorders: Constipation, mouth ulceration, stomatitis.
Hepatobiliary disorders: Cholecystitis.
Investigations: Increased serum lipase, amylase.
Musculoskeletal and connective tissue disorders: Rhabdomyolysis, myalgia.
Respiratory, thoracic and mediastinal disorders: Cough.
Skin and subcutaneous tissue disorders: Rash, urticaria, alopecia.
Potentially Fatal: Hypersensitivity reactions (e.g. anaphylaxis, angioedema, exfoliative skin conditions, bronchial hyperreactivity); acute pancreatitis (e.g. haemorrhagic and necrotising cases).
Patient Counseling Information
This drug may cause an impaired ability to react due to hypoglycaemia, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor HbA1c (at least twice yearly in patients with stable glycaemic control and are meeting treatment goals or quarterly for patients not meeting their treatment goals or with changes in therapy). Consider a combined evaluation of HbA1c with a blood glucose test and/or a glucose management indicator for patients who are prone to glycaemic variability (e.g. insulin deficiency) or those with HbA1c that is contradictory with the serum glucose levels or symptoms. Monitor blood pressure. Assess for signs and symptoms of hypoglycaemia, pancreatitis (e.g. persistent, severe abdominal pain), heart failure (shortness of breath, swelling of feet), serious hypersensitivity reactions (e.g. angioedema, anaphylaxis), or bullous pemphigoid (e.g. erosions, blisters).
Drug Interactions
Increased risk of hypoglycaemia when combined with insulin and/or insulin secretagogues (e.g. sulfonylureas). Decreased plasma concentration and reduced efficacy with rifampicin. Increased exposure with ritonavir.
Mechanism of Action: Linagliptin is a selective inhibitor of dipeptidyl peptidase-4 (DPP-4), an enzyme responsible for the degradation of incretin hormones such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). These incretin hormones increase the synthesis and release of insulin from pancreatic β-cells and reduce glucagon secretion from pancreatic α-cells, hence their prolonged and increased levels upon DDP-4 inhibition result in the physiological regulation of glucose homeostasis.
Absorption: Rapidly absorbed from the gastrointestinal tract. Bioavailability: Approx 30%. Time to peak plasma concentration: 1.5 hours.
Distribution: Extensively distributed to the tissues. Plasma protein binding: 99% (low concentration); 70-80% (high concentration).
Metabolism: Not extensively metabolised.
Excretion: Mainly via faeces (80% as unchanged drug); urine (5% as unchanged drug). Elimination half-life: Approx 12 hours; approx 200 hours (terminal).
Chemical Structure

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 10096344, Linagliptin. Accessed Oct. 23, 2023.

Store between 15-30°C.
MIMS Class
Antidiabetic Agents
ATC Classification
A10BH05 - linagliptin ; Belongs to the class of dipeptidyl peptidase 4 (DPP-4) inhibitors. Used in the treatment of diabetes.
Anon. Linagliptin. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. Accessed 29/08/2023.

Anon. Linagliptin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. Accessed 29/08/2023.

Buckingham R (ed). Linagliptin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. Accessed 29/08/2023.

Joint Formulary Committee. Linagliptin. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. Accessed 29/08/2023.

Linagliptin 5 mg Film-coated Tablets (Zentiva Pharma UK Limited). MHRA. Accessed 29/08/2023.

Tradjenta Tablet, Film Coated (Boehringer Ingelheim Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. Accessed 29/08/2023.

Trajenta 5 mg Film-coated Tablets (Merck Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. Accessed 29/08/2023.

Disclaimer: This information is independently developed by MIMS based on Linagliptin from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2024 MIMS. All rights reserved. Powered by
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Already a member? Sign in
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Already a member? Sign in