Linagliptin


Concise Prescribing Info
Indications/Uses
Type 2 DM.
Dosage/Direction for Use
Adult : PO 5 mg once daily.
Dosage Details
Oral
Type 2 diabetes mellitus
Adult: 5 mg once daily.
Administration
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.
MonitoringParameters
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).
Action
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.
Chemical Structure

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Storage
Store at 25°C.
MIMS Class
ATC Classification
A10BH05 - linagliptin ; Belongs to the class of dipeptidyl peptidase 4 (DPP-4) inhibitors. Used in the treatment of diabetes.
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 © 2020 MIMS. All rights reserved. Powered by MIMS.com
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