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Rosiglitazone
drug data and news
Rosiglitazone drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Rosiglitazone | ||
| Brand Names/Synonyms | Avandia; Rosigliazone Maleate; Rosiglitazone; Rosiglitazone Maleate; Rosiglitazone and Its Intermediates; Rosiglizole | ||
| Indication | For the treatment of Type II diabetes mellitus | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Rosiglitazone, a member of the drug group known as the thiazolidinediones or "insulin sensitizers", is not chemically or functionally related to the alpha-glucosidase inhibitors, the biguanides, or the sulfonylureas. Rosiglitazone targets insulin resistance and, hence, is used alone or with metformine or sulfonylurea to improve glycemic control in patients with type 2 diabetes mellitus. | ||
| Mechanism Of Action | Rosiglitazone acts as an agonist at peroxisome proliferator activated receptors (PPAR) in target tissues for insulin action such as adipose tissue, skeletal muscle, and liver. Activation of PPAR-gamma receptors regulates the transcription of insulin-responsive genes involved in the control of glucose production, transport, and utilization. In this way, rosiglitazone enhances tissue sensitivity to insulin. | ||
| Rosiglitazone News (When available) |
HEALTH BRIEFS 16 May 2006 Pioglitazone Has Cholesterol Advantages Versus Rosiglitazone in ... May 2, 2006 Drug May Reduce Risk of Diabetic Retinopathy: Presented at ARVO May 3, 2006 Higher Risk Patients Benefit More After Conversion from ... May 3, 2006 Health Highlights: May 2, 2006 May 2, 2006 Diabetes drug set for Alzheimer's test May 3, 2006 Looking for Alzheimer's link May 4, 2006 Diabetes drug may help fight Alzheimer's May 7, 2006 AXE THREAT PLANT WINS 100 JOBS May 12, 2006 Fresh from the Pipeline: Inhaled human insulin May 4, 2006 Diabetes link to Alzheimer’s under probe May 1, 2006 Latest Issue Of Alzheimer's & Dementia Explores New Ideas For ... Apr 23, 2006 Theory links diabetes to Alzheimer's May 2, 2006 ERRATUM: Higher Risk Patients Benefit More After Conversion from ... May 5, 2006 EASL CONGRESS VIENNA - BATTLE AGAINST VIRUSES AND FATTY May 1, 2006 Avandia May Help Alzheimer's Patients May 3, 2006 Women Gain More Weight Than Men When Taking Thiazolidinedione ... May 3, 2006 Committee for Medicinal Products for Human Use Summary of Positive ... Apr 28, 2006 Newer Diabetic Meds Cost More, But Users Have Fewer Hospital ... Apr 28, 2006 Zydus Cadila files IND application for NME - ZYH2 Apr 24, 2006 | ||
| Dosage Forms | Tablets | ||
| Drug_Category | Vasodilator Agents; Hypoglycemic Agents; Fibrinolytic Agents; Thazolidinediones; ATC:A10BG02 | ||
| Absorption | The absolute bioavailability of rosiglitazone is 99%. Peak plasma concentrations are observed about 1 hour after dosing. Administration of rosiglitazone with food resulted in no change in overall exposure (AUC), but there was an approximately 28% decrease in Cmax and a delay in Tmax (1.75 hours). These changes are not likely to be clinically significant; therefore, AVANDIA may be administered with or without food. | ||
| Interactions |
Interactions for Rosiglitazone: An inhibitor of CYP2C8 (such as gemfibrozil) may increase the AUC of rosiglitazone and an inducer of CYP2C8 (such as rifampin) may decrease the AUC of rosiglitazone. Therefore, if an inhibitor or an inducer of CYP2C8 is started or stopped during treatment with rosiglitazone, changes in diabetes treatment may be needed based upon clinical response. | ||
| Toxicity | Side effects include fluid retention, congestive heart failure (CHF), liver disease | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 5-[[4-[2-(methyl-pyridin-2-yl-amino)ethoxy]phenyl]methyl]thiazolidine-2,4-dione | ||
| Chemical Formula | C18H19N3O3S | ||
| Molecular Weight | 357.428 g/mol | ||
| Smiles String | CC1=C(N=C(O1)C2=CC=CC=C2)CCOC3=CC=C(C=C3)CC(C(=O)O)NC4=CC=CC=C4C(=O)C5=CC=CC=C5 | ||
| Melting Point | 122° to 123°C | ||
| Water Solubility | Not Available | ||
| State | white to off-white solid | ||
| LogP/Hphobicity | Not Available | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic | ||
| Half Life | 3-4 hours | ||
| Protein Binding [%] | 99.8% bound to plasma proteins, primarily albumin. | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/cx1532.shtml http://www.drugs.com/cons/Rosiglitazone.html http://www.rxlist.com/cgi/generic2/rosigl.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00403 | ||
| CAS Registry Number | 122320-73-4 | ||
| KEGG Compound ID | Not Available | ||
| PubChem ID | SID:66288 | ||
| PharmGKB ID | PA451283 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2241113 |
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