What is rosiglitazone, and how does it work (mechanism of action)?
Rosiglitazone is an oral drug that reduces the
amount of sugar (glucose) in the blood. It is used for treating patients with
type 2 diabetes and is in a class of anti-diabetic drugs called
thiazolidinediones. The other member of this class is pioglitazone (Actos).
Insulin is a hormone produced by the pancreas that is important for controlling
the levels of glucose in the blood. Insulin stimulates the cells of the body to
remove glucose from the blood and thereby lowers the level of glucose in the
blood. Patients with type 2 diabetes cannot make enough insulin or are resistant
to the effects of insulin (insulin resistance). As a result, the cells in their
bodies do not remove enough glucose from the blood, and the level of glucose
rises. Rosiglitazone often is referred to as an "insulin sensitizer" because it
attaches to the insulin receptors on cells throughout the body and causes the
cells to become more sensitive (more responsive) to insulin and remove more
glucose from the blood. At least some insulin must be produced by the pancreas
in order for rosiglitazone to work. Rosiglitazone was approved by the FDA in May
1999.
What are the side effects of rosiglitazone?
AND PRECAUTIONS The most common side effects seen with rosiglitazone alone or in combination with metformin are:
- upper respiratory tract infection,
- headache,
- back pain,
- hyperglycemia (elevated blood sugar),
- fatigue,
- sinusitis,
- diarrhea, and
- hypoglycemia (low blood sugar).
Rosiglitazone has been shown to cause mild to moderate accumulation of fluid (edema) and can lead to
heart failure. Patients who already have heart failure may develop worsening symptoms with rosiglitazone. Therefore, rosiglitazone should not be used by
patients with heart failure. Rosiglitazone also has been associated with an
increased risk of chest pain and heart attacks. The risk of heart attacks may be
greater in those with established heart disease and taking nitrates or
individuals receiving insulin.
Other important side effects include:
- anemia with rosiglitazone alone or combined with metformin.
- weight gain, and
- Increased risk of bone fractures in women who received rosiglitazone for 4 to 6 years.
What is the dosage for rosiglitazone?
Rosiglitazone may be taken once or twice daily, with or without
meals. Daily doses range from 4 to 8 mg either with or without other
antidiabetic medications. There is no additional benefit for doses greater than
8 mg per day.
Which drugs or supplements interact with rosiglitazone?
Rifampin decreases concentrations in the blood of
rosiglitazone by increasing its breakdown in the liver. Therefore, use of
rifampin may decrease the effectiveness of rosiglitazone.
Gemfibrozil (Lopid) increases the concentration of rosiglitazone in the blood
by reducing its breakdown in the liver. Therefore, rosiglitazone may increase
the side effects of rosiglitazone.
Rosiglitazone should not be combined with nitrates (for example,
isosorbide
dinitrate [Isordil Titradose, Dilatrate-SR, Isochron]). In clinical trials, the risk of chest pain and
heart attacks was
greater in individuals on nitrate therapy.
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Is rosiglitazone safe to take if you are pregnant or breastfeeding?
- There are no adequate studies of rosiglitazone in pregnant women. Rosiglitazone crosses the placenta and is detectable in fetal tissue.
- It is unknown if rosiglitazone is secreted in breast milk. Therefore, the safety of rosiglitazone to nursing infants also is unknown.
What else should you know about rosiglitazone?
What preparations of rosiglitazone are available?
Tablets: 2, 4, and 8 mg.
How should I keep rosiglitazone stored?
Tablets should be kept at room temperature, 15 C -30 C (59 F -86 F).