diabetes drugs

AVANDIA ® - Rosiglitazone

AVANDIA ® a drug based on Rosiglitazone.

THERAPEUTIC GROUP: Oral hypoglycemic agents - Thiazolidinediones

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

Indications AVANDIA ® - Rosiglitazone

AVANDIA ® is a hypoglycemic drug used in the treatment of type II diabetes, not adequately compensated by non-pharmacological therapeutic measures such as diet and physical activity.

This medicine can also be used successfully in combination therapy with metformin and sulfonylureas, when the latter at the maximum tolerated dose are ineffective.

Mechanism of action AVANDIA ® - Rosiglitazone

AVANDIA ® is a rosiglitazone-based drug, an active ingredient belonging to the thiazolidinedione family, able to act at the level of insulin-dependent peripheral tissues, improving their sensitivity to insulin, and supporting the important hypoglycemic effect.

The therapeutic effect of rosiglitazone is essentially associated with the ability to act as a selective agonist of the PPAR gamma receptors, which are fundamental from the biological point of view, as they are involved in the modulation of the expression of genes active on glucose, lipid and inflammatory metabolism, and expressed precisely at the level of the main insulin-sensitive peripheral tissues.

From the pharmacokinetic point of view, on the other hand, the oral intake of rosiglitazone precedes intestinal absorption with a bioavailability of 99%, a hepatic biotransformation and the subsequent elimination of inactive metabolites via the kidney.

Clinical studies show that the hypoglycemic effect, can be carried out both in the basal and post-prandial conditions, guaranteeing in a few weeks of treatment, a significant reduction in the concentrations of glycosylated hemoglobin, an important marker of glycemic control.

Studies carried out and clinical efficacy


In 2010, the EMEA suspended the marketing of rosiglitazone throughout Europe, given the significant increase in cardiovascular risk, especially myocardial ischemia, in patients treated with this active ingredient.


The rereading of 42 different clinical trials evaluating the efficacy and side effects of rosiglitazone showed that therapy with this active ingredient was associated with a 43% increase in the risk of myocardial infarction and 64% of deaths due to of cardiovascular diseases.


Although the EMEA has come to the conclusion of suspending the marketing of rosiglitazone-based products, the debate on potential side effects and on the real risk remains open. A significant example comes from this recent study, which shows that second-type diabetic patients treated with rosiglitazone show a decrease in carotid atheromatous plaque thickness, with a significant improvement in glycemic control, insulin sensitivity and fibrinolytic action

Method of use and dosage

AVANDIA ® rosiglitazone 4 mg tablets:

the most used dosage was 4 mg per day, possibly to be increased to 8 mg / day, in case of therapeutic failure, to be taken with a glass of water independently of the meals.

It is important to consider that in the case of combined therapy, it is of fundamental importance to start treatment with minimal effective doses.

Warnings AVANDIA ® - Rosiglitazone

AVANDIA ® was withdrawn from the market in 2010, given the high risks that do not justify the potential benefits derived from the use of this medicine.

The important alterations of the hydro-electrolyte balance induced by rosiglitazone in fact, significantly accentuate the appearance of signs, symptoms or episodes that trigger important cardiac pathologies such as insufficiency or myocardial ischemia.

Furthermore, the risk of bone diseases, significant changes in liver function, and the risks of hypoglycemia, required a continuous monitoring of the blood chemistry, functional and metabolic framework, in order to periodically check the patient's state of health.


The ability of rosiglitazone to pass through the placental filter and find itself in breast milk, altering the normal evolutionary and metabolic balance of the fetus and infant, push industry experts to strongly contraindicate the use of this active ingredient in the treatment of gestational diabetes.


The pharmacokinetic properties of rosiglitazone can be significantly modified by the concomitant intake of gemfibrozil, rifamipicin and other modulators of the hepatic enzyme responsible for its CYP2C8 metabolism, such as phenytoin, carbamazepine, phenobarbital, Hypericum Perforatum.

It must be remembered that dual or triple therapy with other hypoglycemic drugs could significantly accentuate the hypoglycemic effects of rosiglitazone.

Contraindications AVANDIA ® - Rosiglitazone

AVANDIA ® contraindicated in case of known hypersensitivity to the active ingredient or to one of its excipients, heart failure and associated episodes, acute coronary syndrome, changes in liver and kidney function, diabetic keto acidosis and diabetic pre-coma.

The use of AVANDIA ® is strongly discouraged even during the period of pregnancy and lactation.

Undesirable effects - Side effects

Rosiglitazone treatment has been subjected to dozens of clinical studies given the numerous potential side effects, such as to make its use particularly dangerous.

In fact, in addition to the common side effects, also described for other hypoglycemic drugs, such as risk of hypoglycemia, metabolic alterations and nutrition, alterations of the hematological picture, gastro-intestinal disorders and alterations of the hydro-electrolyte balance, the treatment with AVANDIA ® exposes the patient at a high risk of heart disease such as heart failure and ischemia.

Indeed, it appears to be the latter condition, responsible for the withdrawal from the market of all rosiglitazone-based drugs, given the low BENEFIT / RISK ratio.