What is rosiglitazone
Rosiglitazone is an antidiabetic agent from the group of insulin sensitizers in the treatment of diabetes mellitus type 2. The principle is to increase the sensitivity of the tissue to insulin. The body's insulin is thus again effectively able to lower elevated blood sugar levels.
Since November 2010, rests on the orders of the Federal Institute for Drugs and Medical Devices (BfArM) in Germany, the transport capacity for drugs containing rosiglitazone. Your benefit-risk ratio was considered unfavorable overall by the Committee for Human Medicinal Products (CHMP) at the European Medicines Agency (cardiovascular risks, frequent heart attacks). Recent studies show that the initial concerns are unfounded may, according to a review of rosiglitazone increases (trade name Avandia) is not the risk of heart attack. The raw data were manipulated more or less consciously in the original study, which was also not blinded. However, the economic interest in the recent commercialization of the drug is currently low because the patent has already expired.
Rosiglitazone seems to conventional antidiabetic drugs at higher costs to be superior.
Clinical
Areas of application
Rosiglitazone is indicated for the treatment of diabetes mellitus type 2. rosiglitazone is used either alone or in combination with other drugs.
Monotherapy
Monotherapy with rosiglitazone is indicated in adults whose blood sugar through diet and exercise is not sufficiently adjustable and is unsuitable for metformin.
Dual combination therapy
Co-administration with either metformin or a drug from the group of sulfonylureas is displayed when a sole administration of these agents is insufficiently effective.
Triple-combination therapy
Co-administration with metformin and a sulfonylurea is indicated in adults whose blood sugar with a dual combination therapy is poorly adjusted.
Rosiglitazone side effects
The most common adverse effects include edema, anemia (anemia), weight gain and increase in blood cholesterol levels (hypercholesterolemia). These occur in combination with insulin significantly more frequently than with single medication rosiglitazone. In combination with insulin or a sulphonylurea also very commonly dose-dependent hypoglycemia (hypoglycemia) on. Further, it may be an increased appetite and body weight, constipation (constipation), and liver damage with elevation of transaminases, but only very rarely overt liver inflammation (hepatitis) come. Rarely there is an inflammation of the pancreas (pancreatitis), anaphylactic reactions, angioedema to, urticaria, rash and itching of the skin or macular edema of the eye. Especially in combination with insulin can lead to a lack of oxygen to the heart muscle.
In May 2005, the BfArM published that an increased risk of bone fractures in women was found in studies; the product information was updated and informed the medical profession by Red Hand Letter.
In an analysis of 42 studies, published in June 2007 in the New England Journal of Medicine, an increased risk of heart attack by 43% was observed. The manufacturer of the drug and the European Medicines Agency questioned the validity of the meta-analysis. An independent monitoring of study data now confirms the doubts, rosiglitazone would, indeed, is no increased risk of heart attacks. The FDA has therefore already loosened the regulations to prescribe rosiglitazone.
Due to the allegedly increased risk of cardiovascular disease in rosiglitazone-preparations, the European Medicines Agency (EMA) recommended finally in September 2010 to delist in Europe. The German Federal Institute for Drugs and Medical Devices (BfArM) complied with this recommendation, so that rosiglitazone since November 2010 are no longer available in Germany.
According to a former employee of the Food and Drug Administration (FDA) of Avandia maker GlaxoSmithKline PLC has withheld data on the risk. An expert panel has the same authority majority expressed concerns about "Avandia", also a majority thereof but advocated to keep the drug under certain conditions on the market.
Interactions
Rosiglitazone is primarily metabolised by the cytochrome P450 isoenzymes CYP2C8 and CYP2C9. Therefore, there may be variations in systemic exposure with concomitant use of drugs with influence of CYP2C8 such as rifampicin, trimethoprim or gemfibrozil. Interactions with phenytoin, carbamazepine, phenobarbital and St. John's wort can not be excluded. The pharmacokinetics of warfarin and coumarin derivatives Acenocoumarol that are also metabolized by CYP2C9, however, is unaffected. Further, an increase in the activity of methotrexate is possible. Moderate alcohol consumption while taking does not affect the effect.
Contraindications
Rosiglitazone is contraindicated in case of hypersensitivity to rosiglitazone, in heart failure and liver dysfunction. The combination with insulin has not been displayed due to the greatly increased rates of side effects.
For the application under the age of ten years, no data are available. An application is not recommended. Rosiglitazone crosses the placenta, during pregnancy and lactation, the application should therefore not be made if no data on toxicity in humans also be present.
Chemical and pharmaceutical information
Rosiglitazone is chiral. The commercial preparations containing the drug as a racemic mixture (1: 1 mixture of enantiomers).
Rosiglitazone is formulated orally applicable and as film-coated tablet. The tablets contain the drug as a salt of maleic acid (rosiglitazone maleate). Rosiglitazone is available on prescription.