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Encyclopedia > Rosiglitazone
Rosiglitazone chemical structure
Rosiglitazone
Systematic (IUPAC) name
5-((4-(2-(methyl-2-pyridinylamino) ethoxy)phenyl)methyl)- 2,4-thiazolidinedione
Identifiers
CAS number 122320-73-4
ATC code A10BG02
PubChem 77999
DrugBank APRD00403
Chemical data
Formula C18H19N3O3S 
Mol. weight 357.428 g/mol
Pharmacokinetic data
Bioavailability 99%
Protein binding 99.8%
Metabolism Hepatic (CYP2C8-mediated)
Half life 3-4 hours
Excretion Renal (64%) and fecal (23%)
Therapeutic considerations
Licence data

EU US Rosiglitazone structure. ... IUPAC nomenclature is a systematic way of naming organic chemical compounds. ... CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences and alloys. ... The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ... A division of the Anatomical Therapeutic Chemical Classification System A Alimentary tract and metabolism A10A Insulins and analogues A10AB Insulins and analogues, fast-acting A10AB01 Insulin (human) A10AB02 Insulin (beef) A10AB03 Insulin (pork) A10AB04 Insulin lispro A10AB05 Insulin aspart A10AB30 Combinations A10AC Insulins and analogues, intermediate-acting A10AC01 Insulin (human... PubChem is a database of chemical molecules . ... DrugBank is a database available at the University of Alberta that provides information about thousands of products. ... A chemical formula (also called molecular formula) is a concise way of expressing information about the atoms that constitute a particular chemical compound. ... General Name, Symbol, Number carbon, C, 6 Chemical series nonmetals Group, Period, Block 14, 2, p Appearance black (graphite) colorless (diamond) Atomic mass 12. ... General Name, Symbol, Number hydrogen, H, 1 Chemical series nonmetals Group, Period, Block 1, 1, s Appearance colorless Atomic mass 1. ... General Name, Symbol, Number nitrogen, N, 7 Chemical series nonmetals Group, Period, Block 15, 2, p Appearance colorless Atomic mass 14. ... General Name, Symbol, Number oxygen, O, 8 Chemical series Nonmetals, chalcogens Group, Period, Block 16, 2, p Appearance colorless (gas) very pale blue (liquid) Atomic mass 15. ... General Name, Symbol, Number sulfur, S, 16 Chemical series nonmetals Group, Period, Block 16, 3, p Appearance lemon yellow Atomic mass 32. ... The molecular mass of a substance (less accurately called molecular weight and abbreviated as MW) is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... In pharmacology, bioavailability is used to describe the fraction of an administered dose of medication that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ... Many drugs are bound to Blood plasma proteins. ... Metabolism (from Greek μεταβολισμός metabolismos) is the biochemical modification of chemical compounds in living organisms and cells. ... The liver is the largest internal organ of the human body. ... Cytochrome P450 2C8 (abbreviated CYP2C8), a member of the cytochrome P450 mixed-function oxidase system, is involved in the metabolism of xenobiotics in the body. ... The elimination half-life of a drug (or any xenobiotic agent) refers to the timecourse necessary for the quantity of the xenobiotic agent in the body (or plasma concentration) to be reduced to half of its original level through various elimination processes. ... Excretion is the biological process by which an organism chemically separates waste products from its body. ... Human kidneys viewed from behind with spine removed The kidneys are bean-shaped excretory organs in vertebrates. ... The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ...

Pregnancy cat.

B3(AU) C(US) The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. ... Motto: None. ... United States is the current Good Article Collaboration of the week! Please help to improve this article to the highest of standards. ...

Legal status

POM(UK) ℞-only(US) The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ... United States is the current Good Article Collaboration of the week! Please help to improve this article to the highest of standards. ...

Routes Oral

Rosiglitazone is an anti-diabetic drug from the thiazolidinedione class. It is being marketed as Avandia® by the pharmaceutical company GlaxoSmithKline, both as a standalone preparation and in combination with metformin (Avandamet®). Another combination drug approved by the FDA is Avandaryl® (with glimepiride). In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... An anti-diabetic drug or oral hypoglycemic agent is used to treat diabetes mellitus. ... The medication class of thiazolidinedione was introduced in the late 1990s as an adjunctive therapy for diabetes mellitus (type II) and related diseases. ... A pharmaceutical company, or drug company, is a company licensed to discover, develop, market and distribute drugs. ... GlaxoSmithKline plc (LSE: GSK NYSE: GSK) is a British based pharmaceutical, biologicals, and healthcare company. ... Metformin (INN, trade names Glucophage®, Fortamet®, Riomet®, Glumetza® and others) is an anti-diabetic drug from the biguanide class (its other members are the withdrawn agents phenformin and buformin). ... Glimepiride is a medium-to-long acting sulfonylurea anti-diabetic drug. ...


Like other thiazolidinediones, its mechanism of action is by activation of the intracellular receptor class of the peroxisome proliferator-activated receptors (PPARs), specifically PPARγ. Rosiglitazone is a pure ligand of PPARγ, and has no PPARα-binding action. Apart from its effect on insulin resistance, it appears to have an anti-inflammatory effect: nuclear factor kappa-B (NFκB) levels fall and inhibitor (IκB) levels increase in patients on rosiglitazone (Mohanty et al). The medication class of thiazolidinedione was introduced in the late 1990s as an adjunctive therapy for diabetes mellitus (type II) and related diseases. ... In biochemistry, a receptor is a protein on the cell membrane or within the cytoplasm that binds to a specific factor (a ligand), such as a neurotransmitter, hormone, or other substance, and initiates the cellular response to the ligand. ... PPAR gamma In cell biology, peroxisome proliferator-activated receptors (PPARs) are a group of nuclear receptor isoforms that exist across biology. ... Insulin resistance is the condition in which normal amounts of insulin are inadequate to produce a normal insulin response from fat, muscle and liver cells. ... Inflammation is the first response of the immune system to infection or irritation and may be referred to as the innate cascade. ...

Contents

References

  • Mohanty P, Aljada A, Ghanim H, Hofmeyer D, Tripathy D, Syed T, al-Haddad W, Dhindsa S, Dandona P. Evidence for a potent antiinflammatory effect of rosiglitazone. J Clin Endocrinol Metab 2004; 89:2728-35.

Side-effects and contraindications

See main article: thiazolidinedione The medication class of thiazolidinedione was introduced in the late 1990s as an adjunctive therapy for diabetes mellitus (type II) and related diseases. ...


See also

  • Peroxisome proliferator-activated receptor

PPAR gamma In cell biology, peroxisome proliferator-activated receptors (PPARs) are a group of nuclear receptor isoforms that exist across biology. ...

External links


Oral antidiabetic drugs (A10B) edit
Biguanides: Metformin
Sulfonylureas: Chlorpropamide, glibenclamide (Glyburide), Gliclazide, Glimepiride, Glipizide, Gliquidone, Tolazamide, Tolbutamide
Alpha-glucosidase inhibitor: Acarbose, Miglitol
Thiazolidinediones (TZD): Pioglitazone, Rosiglitazone, Troglitazone
Meglitinides: Nateglinide, Repaglinide
Dipeptidyl peptidase-4 (DPP-4) inhibitors: Saxagliptin, Sitagliptin, Vildagliptin

  Results from FactBites:
 
EHS: Mosby's Drug Consult - Drug Updates - Rosiglitazone Maleate and Metformin Hydrochloride 003571 (8765 words)
Rosiglitazone maleate is not chemically or functionally related to the sulfonylureas, the biguanides, or the α-glucosidase inhibitors.
Rosiglitazone was not mutagenic or clastogenic in the in vitro bacterial assays for gene mutation, the in vitro chromosome aberration test in human lymphocytes, the in vivo mouse micronucleus test, and the in vivo/in vitro rat UDS assay.
Rosiglitazone altered estrous cyclicity (2 mg/kg/day) and reduced fertility (40 mg/kg/day) of female rats in association with lower plasma levels of progesterone and estradiol (approximately 20 and 200 times human AUC at the maximum recommended human daily dose of the rosiglitazone component of Avandamet, respectively).
Comparison of Rosiglitazone and Metformin for Treating HIV Lipodystrophy: results suggest improvements in lipoatrophy ... (4089 words)
Rosiglitazone and metformin similarly decreased the AUCs for glucose and insulin.
Rosiglitazone should, therefore, be used with caution in patients with HIV lipodystrophy and possibly should be avoided in patients who are already hyperlipidemic or given in conjunction with lipid-lowering agents.
Rosiglitazone is an agonist for peroxisome proliferator-activated receptor-{gamma} activation, thereby directly influencing the transcription of genes that regulate glucose and lipid metabolism (12).
  More results at FactBites »


 

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