New Drug Update 2010-2011 Faculty Disclaimer - CME Conferences

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2 nd Annual Essentials in Primary Care Fall Conference Friday, November 11, 2011 Linagliptin – Tradjenta • Linagliptin is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Thus, linagliptin increases the concentrations of active incretin hormones, GLP-1 and GIP which both increase glucose stimulated insulin biosynthesis and secretion from pancreatic beta cells. Furthermore, GLP-1 also reduces glucagon secretion from pancreatic alpha cells, resulting in a reduction in hepatic glucose output. Linagliptin – Tradjenta • The effective half-life for accumulation of linagliptin, as determined from oral administration of multiple doses of linagliptin 5 mg, is approximately 12 hours. • Following administration of an oral [14C]-linagliptin dose to healthy subjects, approximately 85% of the administered radioactivity was eliminated via the enterohepatic system (80%) or urine (5%) within 4 days of dosing. • No dose adjustment is recommended in patients with renal impairment. Wayne Weart New Drug Update Part I
2 nd Annual Essentials in Primary Care Fall Conference Friday, November 11, 2011 Drug Interactions Linagliptin – Tradjenta • Linagliptin is a weak to moderate inhibitor of CYP isozyme CYP3A4, but does not inhibit other CYP isozymes and is not an inducer of CYP isozymes. • Linagliptin is a P-glycoprotein (P-gp) substrate, and inhibits P- gp mediated transport of digoxin at high concentrations. Based on the results of limited drug interaction studies, linagliptin is considered unlikely to cause interactions with P-gp substrates at therapeutic concentrations. • Inducers of CYP3A4 or P-gp (e.g., rifampin) decrease exposure to linagliptin to subtherapeutic and likely ineffective concentrations. For patients requiring use of such drugs, an alternative to linagliptin is strongly recommended. Linagliptin – Tradjenta Clinical Trials Monotherapy: • 496 patients mean A1c 8.0 treated with linagliptin 5 mg QD vs. placebo for 24 weeks – A1c -0.4% linagliptin (L) vs. +0.3% placebo (P) (difference from placebo -0.7%) – Patients achieving A1c
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New Drug Update 2010-2011 Faculty Disclaimer - CME Conferences

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