Generic Medicine Info
Indications and Dosage
Type 2 diabetes mellitus
Adult: 5 mg once daily.
May be taken with or without food.
Special Precautions
Patient w/ history of pancreatitis; angioedema to other DPP-4 inhibitor. Not intended in patients w/ IDDM or for the treatment of diabetic ketoacidosis. Pregnancy and lactation.
Adverse Reactions
Hypoglycaemia, severe and disabling arthralgia, nasopharyngitis, rash, mouth ulcer, stomatitis, diarrhoea, cough. Rarely, hypersensitivity reactions.
Potentially Fatal: Acute pancreatitis.
Monitoring Parameters
Monitor HbA1C and serum glucose levels; signs/symptoms of pancreatitis.
Drug Interactions
Increased risk of hypoglycaemia when used w/ an insulin secretagogue (e.g. sulfonylurea) or insulin. Plasma concentration of linagliptin may be decreased by strong inducers of P-glycoprotein (e.g. rifampicin) and may be increased by strong P-glycoprotein inhibitors (e.g. ritonavir).
Description: Linagliptin inhibits dipeptidyl peptidase-4 (DPP-4), an enzyme which is involved in the inactivation of the incretin hormones GLP-1 (glucagon-like peptide-1) and GIP (glucose-dependent insulinotropic polypeptide). Both incretin hormones are involved in the physiological regulation of glucose homeostasis. Inhibition of DPP-4 leads to increased and prolonged active incretin levels.
Absorption: Rapidly absorbed from the GI tract. Bioavailability: Approx 30%. Time to peak plasma concentration: W/in approx 1.5 hr.
Distribution: Extensively distributed to body tissues. Plasma protein binding: Concentration dependent: 99% (low concentration); 70-80% (high concentration).
Metabolism: Not extensively metabolised.
Excretion: Via faeces (approx 80%) and urine (5%). Terminal half-life: >100 hr.
Chemical Structure

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Linagliptin, CID=10096344, (accessed on Jan. 22, 2020)

Store at 25°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. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. Accessed 24/09/2015 .

Buckingham R (ed). Linagliptin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. Accessed 24/09/2015.

McEvoy GK, Snow EK, Miller J et al (eds). Linagliptin. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). Accessed 24/09/2015 .

Tradjenta Tablet, Film Coated (Boehringer Ingelheim Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. Accessed 24/09/2015 .

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