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Diabetes mellitus type 2 Clinical criteria: The condition must be stable for the prescriber to consider the listed maximum quantity of this medicine suitable for this patient, AND The treatment must be used in combination with at least one of: metformin, a sulfonylurea, insulin, AND The condition must be inadequately responsive to at least one of: metformin, a sulfonylurea, insulin. Treatment criteria: Patient must not be undergoing concomitant PBS-subsidised treatment with any of: a GLP-1 receptor agonist, another DPP4 inhibitor.
“Linagliptin is an inhibitor of the enzyme DPP-4 (Dipeptidyl peptidase 4), an enzyme which is involved in the inactivation of the incretin hormones GLP-1 and GIP (glucagon-like peptide-1, glucose- dependent insulinotropic polypeptide).”
“Plasma concentrations of linagliptin decline in a triphasic manner with a long terminal half-life (terminal half-life for linagliptin more than 100 hours), that is mostly related to the saturable, tight binding of linagliptin to DPP-4 and does not contribute to the accumulation of the drug. The effective half-life for accumulation of linagliptin, as determined from oral administration of multiple doses of 5 mg linagliptin, is approximately 12 hours.”
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Curated subset. The full adverse-effect list is in the TGA Product Information; click any citation above to open it.
“Linagliptin is a weak competitive and a weak to moderate mechanism-based inhibitor of CYP isozyme CYP3A4, but does not inhibit other CYP isozymes. It is not an inducer of CYP isozymes.”