Rosiglitazone Pharmacology


About Rosiglitazone
Thiazolidinedione derivative, Oral anti-diabetic.
Mechanism of Action of Rosiglitazone
The drug exerts antidiabetic action by acting as a selective agonist for the nuclear "peroxisome proliferator-activated receptor Gama (PPAR Gama); which enhances the transcription of several insulin responsive genes. It reverses insulin resistance by stimulating GLUT4 (glucose transporter 4) expression and translocation and improves entry of glucose in to muscle and adipose tissue. It also suppresses hepatic gluconeogenesis. Activation of genes regulating fatty acid metabolism and lipogenesis in adipose tissue also contributes to the insulin sensitizing action of drug. It reduces blood glucose and HbA1c; improves glycaemic control and lowers circulating levels of Insulin.

Pharmacokinets of Rosiglitazone
Absorption: Well absorbed orally and bioavailability is about 99%, Distribution: Widely distributed in a highly protein bound form, Metabolism: Extensively metabolized in the body. Primarily metabolized through N-demethylation and hydroxylation; with subsequent conjugation, Excretion: Excreted mainly through urine (64%) and rest is excreted through faeces.
Onset of Action for Rosiglitazone
Duration of Action for Rosiglitazone
12 to 24 hours
Half Life of Rosiglitazone
3 to 4 hours
Side Effects of Rosiglitazone
1. Oedema
2. Plasma volume expansion
3. Weight gain
4. Headache
5. Myalgia
6. Mild anaemia
7. Back pain
Contra-indications of Rosiglitazone
1. Hypersensitivity to the drug
2. Hepatic impairment
3. Cogestive heart failure
4. Patients with moderately severe to severe cardiac disease (New York Heart Association class III and class IV cardiac diseases)
5. Incresed liver enzyme levels(ALT level greater than 2. 5 times than normal)
6. Type 1 diabetes mellitus
7. Diabetic ketoacidosis.
Special Precautions while taking Rosiglitazone
1.Cardiac diseases
Pregnancy Related Information
Old Age Related Information
May be used
Breast Feeding Related Information
Children Related Information
Indications for Rosiglitazone
1. Non-insulin dependent diabetes mellitus (as adjunct to diet and exercise)
Interactions for Rosiglitazone
Metformin: The pharmacokinetics of rosiglitazone was not altered following its concurrent administration in healthy volunteers.
Acarbose: Coadministration had no clinically relevant effect on the pharmacokinetics of rosiglitazone.
Typical Dosage for Rosiglitazone
Oral: Starts with 4mg once daily in the morning or as two divided doses in the morning and evening. Increases the dose to 8mg once daily or as two divided doses; If fasting glucose levels does not improves after 12 weeks.
Schedule of Rosiglitazone
Storage Requirements for Rosiglitazone
Store at controlled room temperature at a range of 15 to 30 degree C.; in a well closed container. Protect from moisture. Keep out of reach of children.
Effects of Missed Dosage of Rosiglitazone
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Rosiglitazone
Provide symptomatic treatment and supportive measures.

Home Delivery for Rosiglitazone in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including rosiglitazone.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for rosiglitazone and other medicines and health products. Home delivery services for rosiglitazone may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take rosiglitazone only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for rosiglitazone before they complete the sale. You can get this information while placing the order for rosiglitazone with the pharmacy.

Rosiglitazone is a generic medicine name and there are several brands available for it. Some of the brands for rosiglitazone might be better known than rosiglitazone itself. If the pharmacy that's willing to deliver medicines to your home doesn't have rosiglitazone in stock, you can ask for one of the branded alternatives for rosiglitazone.