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Related Concept Videos

Dipeptidyl Peptidase 4 Inhibitors01:23

Dipeptidyl Peptidase 4 Inhibitors

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Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a...
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Oral Hypoglycemic Agents: Glinides01:06

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Repaglinide (Prandin) and Nateglinide (Starlix), known as glinides, are oral insulin secretagogues that stimulate insulin release from pancreatic β cells by closing the ATP-sensitive potassium channels (KATP channel). Repaglinide controls insulin release from pancreatic β cells by managing potassium efflux. It shares two binding sites with sulfonylureas and also has a unique site, indicating overlapping mechanisms of action. With a rapid onset and a 4-7 hour duration, it effectively...
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Glucagon-like Receptor Agonists01:24

Glucagon-like Receptor Agonists

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Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by...
294
Oral Hypoglycemic Agents: Biguanides and Glitazones01:26

Oral Hypoglycemic Agents: Biguanides and Glitazones

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Biguanides, particularly metformin (Glucophage), are insulin sensitizers that enhance glucose uptake, thereby reducing insulin resistance. Unlike sulfonylureas, metformin doesn't prompt insulin secretion, which helps to curb hypoglycemia risk. Metformin is beneficial in treating conditions like polycystic ovary syndrome due to its insulin-resistance reduction capability. The drug's primary action involves curtailing hepatic gluconeogenesis, a significant contributor to high blood...
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Insulin: Dosing Regimen and Adverse Effects01:16

Insulin: Dosing Regimen and Adverse Effects

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Insulin-replacement therapy usually includes both long-acting insulin (basal) and short-acting insulin (to cater to postprandial needs). In a diverse group of type 1 diabetes patients, the average daily insulin dose is typically 0.5-0.7 units/kg body weight. However, obese patients and pubertal adolescents may need more due to insulin resistance.
The basal dose constitutes about 40%-50% of the total daily dose, with the rest as premeal insulin. The mealtime insulin dose should mirror...
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Oral Hypoglycemic Agents: α-Glucosidase Inhibitors01:19

Oral Hypoglycemic Agents: α-Glucosidase Inhibitors

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α-glucosidase inhibitors, including acarbose (Precose), miglitol (Glyset), and voglibose (Voglib) (primarily available in Asia), are drugs that control blood sugar levels by delaying the digestion of starch and disaccharides. They achieve this by inhibiting α-glucosidase enzymes in the intestine, which slow the absorption of carbohydrates in the intestine, which in turn leads to a prolonged release of the glucoregulatory hormone GLP-1 from intestinal L-cells.
Acarbose and miglitol are...
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Updated: May 31, 2025

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Linagliptin: A comprehensive profile.

Mohamed Fawzy Kabil1, Jude Majed Lababidi1, Hassan Mohamed El-Said Azzazy1

  • 1Department of Chemistry, School of Sciences and Engineering, The American University in Cairo, AUC Avenue, New Cairo, Egypt.

Profiles of Drug Substances, Excipients, and Related Methodology
|January 24, 2025
PubMed
Summary
This summary is machine-generated.

Linagliptin is an oral dipeptidyl peptidase IV inhibitor for type 2 diabetes. This review covers its properties, synthesis, analysis, and thermal characteristics for better understanding of this important antidiabetic drug.

Keywords:
HPLC analysisLinagliptinNMR analysisPharmacokineticsThermal analysisUV spectrum

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Area of Science:

  • Pharmacology and Medicinal Chemistry
  • Analytical Chemistry

Background:

  • Linagliptin (LINA) is a novel oral dipeptidyl peptidase IV (DPP-IV) inhibitor.
  • It is a key therapeutic agent for managing hyperglycemia in adults with type 2 diabetes mellitus.

Purpose of the Study:

  • To provide a comprehensive review of Linagliptin.
  • To detail its nomenclature, physicochemical properties, synthesis, and thermal analysis.
  • To present various analytical techniques for Linagliptin determination.

Main Methods:

  • Literature review and synthesis of existing data on Linagliptin.
  • Analysis of physicochemical characteristics.
  • Review of synthetic pathways.
  • Examination of thermal analysis data.
  • Survey of analytical methodologies for Linagliptin quantification and identification.

Main Results:

  • Linagliptin's unique properties as an oral DPP-IV inhibitor are highlighted.
  • Detailed information on its chemical structure, physical characteristics, and synthetic routes is presented.
  • Various analytical methods for its assessment are discussed.

Conclusions:

  • This review consolidates essential information on Linagliptin.
  • It serves as a valuable resource for researchers and clinicians involved in diabetes management and pharmaceutical analysis.