Pharmaceutical Raw Materials Steroid Powder Rosiglitazone For Treatment Of Diabetes

Pharmaceutical Raw Materials Steroid Powder Rosiglitazone For Treatment Of Diabetes

Abstract

Rosiglitazone and pioglitazone is currently the clinical treatment of diabetes commonly used thiazolidinedione hypoglycemic agents, this product is insulin sensitizer, by increasing the skeletal muscle, liver, adipose tissue sensitivity to insulin, improve cell pairs Glucose utilization and play a lower blood sugar effect, can significantly reduce the fasting blood glucose and insulin, C-peptide levels, postprandial blood glucose and insulin also have a lower effect. But requires patients to have a certain ability to secrete insulin.

Clinical application for diet control and exercise is still not satisfied with type 2 diabetes patients, but also with biguanide or sulfonylurea combination therapy alone when the poor control of blood sugar. Single use, the initial dose of oral daily 4mg, 12 weeks after the need to increase to 8mg daily. In fasting or eating clothes After the elderly patients may have mild to moderate edema and anemia, edema patients with caution.

Indications and Usage

1. Monotherapy and Combination Therapy

Rosiglitazone Tartrate Dispersible Tablets is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

2. Important Limitations of Use

Due to its mechanism of action, Rosiglitazone Tartrate Dispersible Tablets is active only in the presence of endogenous insulin. Therefore, Rosiglitazone Tartrate Dispersible Tablets should not be used in patients with type 1 diabetes mellitus or for the treatment of diabetic ketoacidosis.

The coadministration of Rosiglitazone Tartrate Dispersible Tablets and insulin is not recommended.

The use of Rosiglitazone Tartrate Dispersible Tablets with nitrates is not recommended.

Pharmacology

Rosiglitazone is a member of the thiazolidinedione class of drugs. Thiazolidinediones act as insulin sensitizers. They reduce glucose, fatty acid, and insulin blood concentrations. They work by binding to the peroxisome proliferator-activated receptors (PPARs). PPARs are transcription factors that reside in the nucleus and become activated by ligands such as thiazolidinediones. Thiazolidinediones enter the cell, bind to the nuclear receptors, and alter the expression of genes. The several PPARs include PPARα, PPARβ/δ, and PPARγ. Thiazolidinediones bind to PPARγ.

PPARs are expressed in fat cells, cells of the liver, muscle, heart, and inner wall (endothelium) and smooth muscle of blood vessels. PPARγ is expressed mainly in fat tissue, where it regulates genes involved in fat cell (adipocyte) differentiation, fatty acid uptake and storage, and glucose uptake. It is also found in pancreatic beta cells, vascular endothelium, and macrophages. Rosiglitazone is a selective ligand of PPARγ and has no PPARα-binding action. Other drugs bind to PPARα.

Rosiglitazone also appears to have an anti-inflammatory effect in addition to its effect on insulin resistance. Nuclear factor kappa-B (NF-κB), a signaling molecule, stimulates the inflammatory pathways. NF-κB inhibitor (IκB) downregulates the inflammatory pathways. When patients take rosiglitazone, NF-κB levels fall and IκB levels increase.

Research

Rosiglitazone was thought to be able to benefit patients with Alzheimer's disease who do not express the ApoE4 allele, but the phase III trial designed to test this showed that rosiglitazone was ineffective in all patients, including ApoE4-negative patients.

Rosiglitazone may also treat mild to moderate ulcerative colitis, due to its anti-inflammatory properties as a PPAR ligand.