The synthesis of linagliptin presented in Scheme 14 begins with N-7 alkylation of xanthine analog 106 with 1-bromo-2-butyne 107 to afford compound 108. N-1 alkylation of 108 with 109 resulted in compound 110, which on nucleophilic substitution at C-8 by 3-aminopiperidine 111 and subsequent Boc deprotection afforded linagliptin 8. 123.
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The labeling for linagliptin includes data from an 18-week, randomized, double-blind, placebo-controlled study that assessed the efficacy of linagliptin in combination with a sulfonylurea in patients with type-2 diabetes. 6 Patients receiving sulfonylurea monotherapy or a sulfonylurea plus an additional oral anti-hypertensive agent were as signed to receive the addition of linagliptin 5 mg or.
Linagliptin, sold under the brand name Tradjenta among others, is a medication used to treat diabetes mellitus type 2. It is generally less preferred than metformin and sulfonylureas. It is used together with exercise and diet. It is not recommended in type 1 diabetes.
When linagliptin was added to a stable regimen of metformin and sulfonylurea, mean changes from baseline to 24 weeks were similar for the linagliptin and placebo groups for total cholesterol, high-density lipoprotein cholesterol (HDL-C) and low-density lipoprotein cholesterol (LDL-C) (Owens et al. 2011). At baseline, both groups had mean triglyceride values above the normal reference range.Learn More
If you are allergic to linagliptin; any part of linagliptin; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had. If you have any of these health problems: Acidic blood problem or type 1 diabetes. This is not a list of all drugs or health problems that interact with linagliptin.Learn More
Linagliptin has the following interaction information: Acarbose. Both linagliptin and acarbose can increase the risk of hypoglycaemia. Alogliptin. Both linagliptin and alogliptin can increase the risk of hypoglycaemia. Apalutamide. Apalutamide is predicted to decrease the exposure to linagliptin. Manufacturer makes no recommendation.Learn More
Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry 2016 August 9, 21 (8) Linagliptin, a xanthine derivative, is a highly potent, selective, long-acting and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes.Learn More
Three degradation impurities related to Linagliptin (1) drug product, N-Acetyl Linagliptin (2), N-Aminoacyl Linagliptin (3) and N-Formyl Linagliptin (4) have been synthetically prepared and characterized. These impurities form due to interaction of excipient and active pharmaceutical ingredient (API) during formulation. Formation of above drug product degradation impurities has been investigated.Learn More
Synthesis and Structure-Activity Relationship of Some New Thiophene-Based Heterocycles as Potential Antimicrobial Agents. Journals. Information. For Authors For Reviewers For Editors For Librarians For Publishers For Societies.Learn More
Linagliptin versus sitagliptin in patients with type 2 diabetes mellitus: A network meta-analysis of randomized clinical trials. Article (PDF Available). For evidence synthesis, a meta-analysis.Learn More
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A small fraction of absorbed linagliptin is metabolized to a pharmacologically inactive metabolite, which shows a steady-state exposure of 13.3% relative to linagliptin. Elimination 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.Learn More
Linagliptin-metformin is a prescription medication that contains two drugs: linagliptin and metformin. It’s important to know about all the drugs in the combination because each drug may affect.Learn More
Linagliptin is an oral antidiabetic medication that inhibits the enzyme dipeptidyl peptidase and allows the incretins to be active for longer period. Incretins active for longer time will contribute towards increased insulin secretion, which increases the tissue uptake of glucose and reduces the blood sugar.Learn More
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