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Rosiglitazone

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Rosiglitazone

Rosiglitazone (trade name Avandia) is an antidiabetic drug in the thiazolidinedione class. It works as an insulin sensitizer, by binding to the PPAR in fat cells and making the cells more responsive to insulin. More

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Description

Rosiglitazone (trade name Avandia) is an antidiabetic drug in the thiazolidinedione class. It works as an insulin sensitizer, by binding to the PPAR in fat cells and making the cells more responsive to insulin.

Generic Name

Rosiglitazone

Chemical names

Rosiglitazone; 122320-73-4; Avandia; 5-(4-(2-(Methyl(pyridin-2-yl)amino)ethoxy)benzyl)thiazolidine-2,4-dione; Brl-49653

Brand names

Enselin, Glitos, Reglit, Rezult, Risicon- G, Roglin, Rosicon, Rosinorm, Rositec, Rosizon, Ross, Rozon, Secrin- R, Senzia

IUPAC name

5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)methyl]-1,3-thiazolidine-2,4-dione

Pharmacokinetics

  • Bioavailability 99%. 
  • To plasma proteins bound 99.8%, primarily albumin.
  • Hepatic metabolism. 

Actions

PPAR-gamma receptors activation regulates the transcription of insulin-responsive genes involved in the control of glucose production, transport, and utilization. It is a potent and highly selective agonist at PPAR (peroxisome proliferator activated receptors) in target tissues for insulin action such as adipose tissue, skeletal muscle, and liver.

Dosage/Dosage form

4 mg daily may increase after 8-12 weeks of therapy according to response.

Therapeutic uses

Type 2 diabetes mellitus.

Adverse effects/Side effects

Upper respiratory tract infections, headache, back pain, hyperglycaemia, fatigue, sinusitis, diarrhoea, hypoglycaemia, oedema, anaemia, weight gain.

Interaction

  • Increased effect with NSAIDs, pioglitazone, gemfibrozil, fluconazole, sulfonamides.
  • Decreased effect with secobarbital, carbamazepine, phenytoin, rifampicin and phenobarbital.
  • Increased risk of fluid retention when used with NSAIDs.
  • Increased risk of hypoglycaemia when used with quinolones.
  • Decreased serum levels when used with St John's wort.
  • Increased risk of fluid retention and hypoglycaemia when used with insulin.

Contraindications

  • Hypersensitivity, symptomatic heart failure.
  • Not to be used in patients with established NYHA (New York Heart Association) class III or IV heart failure.
  •  Pregnancy, lactation.

Storage

Store at 25°C

Information

Molecular weight

357.427

Molecular formula

C18H19N3O3S

CAS number

122320-73-4

Precautions

  • CV disease; renal or hepatic impairment.
  • Monitor liver function regularly.
  • Patients with oedema.

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