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Rosiglitazone information from DrugsUpdate  

See Available Brands of Rosiglitazone in India

P - Contraindicated in pregnancy
L - Contraindicated in lactation
FI - Food *

Rosiglitazone is an anti-diabetic drug in the thiazolidinedione class of drugs. It is marketed by the pharmaceutical company GlaxoSmithKline as a stand-alone drug (Avandia) and in combination with metformin (Avandamet) or with glimepiride (Avandaryl). Annual sales peaked at approx $2.5bn in 2006. The drug's patent expires in 2012.

Pharmacodynamics

Pharmacokinetics

Rosiglitazone is a thiazolidinedione antidiabetic agent which improves insulin sensitivity by lowering blood glucose level without increasing pancreatic insulin secretion. It is dependent on the presence of insulin. Rosiglitazone is a potent agonist for the peroxisome proliferator-activated receptor-gamma, which in turn regulates the transcription of insulin-responsive genes involved in the control of glucose production, transport and utilisation.

Onset

Delayed.

Duration
12 weeks.

Absorption
Well absorbed from the GI tract after oral admin. Peak plasma concentrations after 1 hour.

Distribution
Protein-binding: 99.8%.

Metabolism
Extensively metabolised by CYP2C8.

Excretion

Urine (64%); faeces (23%); 3-4 hours (elimination half-life)

Rosiglitazone Indications / Rosiglitazone Uses

Information Not Available

Rosiglitazone Adverse Reactions / Rosiglitazone Side Effects

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

Potentially Fatal: May cause or exacerbate congestive heart failure.

Precautions

Overdosage
Supportive treatment is recommended

Special Precautions

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

Other Drug Interactions

Increased effect with NSAIDs, pioglitazone, gemfibrozil, fluconazole, sulfonamides. Decreased effect with carbamazepine, phenytoin, secobarbital, phenobarbital and rifampicin. Increased risk of fluid retention when used with NSAIDs. Increased risk of hypoglycaemia when used with quinolones. Increased risk of fluid retention and hypoglycaemia when used with insulin.

Other Interactions

Food Interaction
Decreased serum levels when used with St John's wort.

Dosage

Oral
Type 2 diabetes mellitus
Adult: 4 mg daily, may increase after 8-12 weeks of therapy according to response. Max: 8 mg daily.

Food(before/after)

May be taken with or without food

List of Contraindications

Rosiglitazone and Pregnancy

Contraindicated in pregnancy

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Rosiglitazone and Lactation

Contraindicated in lactation

Rosiglitazone and Children

Information Not Available

Rosiglitazone and Geriatic

No dosage adjustments are required for the elderly

Rosiglitazone and Other 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

Oral
Store at 25°C

Lab interference

Oral
Store at 25°C

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