Linagliptin

Oral
Type 2 diabetes mellitus

May be taken with or without food.

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.

Hypoglycaemia, severe and disabling arthralgia, nasopharyngitis, rash, mouth ulcer, stomatitis, diarrhoea, cough. Rarely, hypersensitivity reactions.
Potentially Fatal: Acute pancreatitis.

Monitor HbA_1C and serum glucose levels; signs/symptoms of pancreatitis.

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.
Pharmacokinetics:
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.

Source: National Center for Biotechnology Information. PubChem Database. Linagliptin, CID=10096344, https://pubchem.ncbi.nlm.nih.gov/compound/Linagliptin (accessed on Jan. 22, 2020)

Store at 25°C.

Antidiabetic Agents

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. https://online.lexi.com. Accessed 24/09/2015 .

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

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