Thursday, November 19, 2009
Actos
Actos (pioglitazone) is a prescription drug of the class thiazolidinedione (TZD) with hypoglycemic (antihyperglycemic, antidiabetic) action. By Takeda Pharmaceuticals, Pioglitazone is marketed as trademarks Actos in the USA, Glustin in Europe.
Medications and Prescriptions
Generic name: pioglitazone
Product Brand Name: Actos
Product Manufacturer: Takeda
Pharmacology:
Pioglitazone selectively arouses the nuclear receptor peroxisome proliferator-activated receptor gamma (PPAR-г) and to a lesser extent PPAR-б. Besides modulating the transcription of the insulin-sensitive genes involved in the control of glucose, Pioglitazone transforms lipid metabolism in the lipidic, muscular tissues and in the liver. Accordingly, pioglitazone lessens insulin resistance in the liver and peripheral tissues; increases the expense of insulin-dependent glucose; decreases withdrawal of glucose from the liver and reduces quantity of glucose, insulin and glycated hemoglobin in the bloodstream. Pioglitazone decreases the level of triglycerides and increases that of high-density lipoproteins (HDL) without changing low-density lipoproteins (LDL) and total cholesterol in patients with disorders of the lipid metabolism. However, statins are the preferred drugs for this.
In recent times, pioglitazone and other active TZDs have been shown to combine to the outer mitochondrial membrane protein mitoNEET with affinity similar to that of pioglitazone for PPARг.
Indications and usage:
Apart from using Pioglitazone for the treatment of diabetes mellitus type 2 (previously known as non-insulin-dependent diabetes mellitus, NIDDM) in monotherapy, this medicine can also be used in combination with sulfonylurea, metformin, or insulin. The drug has also been used to treat non-alcoholic steatohepatitis (fatty liver). Yet this use is currently considered untried.
Contraindications:
Pioglitazone cannot be used in patients who are allergic to pioglitazone, other thiazolidinediones or any of components of its pharmaceutical forms. The medicine is ineffective and harmful in diabetes mellitus type 1 and diabetic ketoacidosis. On the other hand, its safety in pregnancy, lactation (breastfeeding) and people under 18 is not ascertained.
Given previous experiences with the related drug troglitazone, acute diseases of the liver are regarded as a contraindication for pioglitazone.
Side effects:
Based on data from the ADOPT trial, there was a information from a press release by GlaxoSmithKline in February 2007 that there is a greater incidence of fractures of the upper arms, hands and feet in female diabetics given rosiglitazone compared with those given metformin or glyburide. Following release of this statement, Takeda also admitted that pioglitazone has similar implications for female patients. [Citation needed]
The risk of hypoglycemia is low in the absence of other drugs that lower blood glucose.
Similar to other thiazolidinediones, pioglitazone can cause fluid retention and peripheral edema. Thus, it may reason congestive heart failure (which worsens with fluid overload in those at risk) and also anemia. Due to increase in subcutaneous adipose tissue, a slight weight gain is common. In studies, patients on pioglitazone had a little increased proportion of upper respiratory tract infection, headache, sinusitis, myalgia and tooth problems.
On July 30, 2007 an Advisory Committee of the Food and Drug Administration concluded that the use of rosiglitazone for the treatment of type 2 diabetes was associated with a greater risk of "myocardial ischemic events" when compared to placebo. On the contrary, when compared to other active comparators, there was no increased risk. Pioglitazone is currently being reviewed. A meta-analysis released later showed that pioglitazone reduced the number of ischemic cardiac events rather than increase the risk, but increases CHF, a common class effect of the TZD's..[6] The PERISCOPE study compared pioglitazone with glimepiride in diabetics; atherosclerotic plaque volume was measured and followed over time. Glimepiride therapy had greatly important progression of plaque volume over time of 0.73 percent. Pioglitazone had a -0.16 percent regression in plaque volume. This is the earliest study to explain that diabetic therapy slowed progression of atherosclerosis. Therapy with pioglitazone raised HDL, and lowered triglyceride and hsCRP; these are all helpful effects on risk factors for coronary artery disease. Even now, no oral anti-diabetic drug has been shown to decrease the possibility of cardiovascular complications. [7]
Drug interactions:
Sulfonamides, metformin and insulin equally exponentiate hypoglycemia. In those taking oral contraceptive, therapy with pioglitazone increased risk for pregnancy.
How supplied:
Pioglitazone as Actos is available in oral tablets containing 15, 30 or 45 mg of pioglitazone base. It is also available in combination with metformin as ActoplusMet (tablets containing 15 mg pioglitazone and either 500 or 850 mg of metformin) or in combination with Amaryl as Duetact (tablets containing 30 mg pioglitazone and either 2 or 4 mg of Amaryl).
Actos notes:
Actos is an oral anti diabetic agent with the generic name Pioglitazone, and manufactured by Takeda. It acts primarily by decreasing insulin resistance. The medicine belongs to the class of drugs called thiazolidinedione (TZD), and is a once-daily oral medication. Along with diet and exercise, this drug has been shown to be effective for the treatment of type 2 diabetes. It also helps to control blood sugar levels in your body by reducing insulin resistance; a condition in which your body’s cells don’t respond to a hormone (called insulin) that allows them to turn blood sugar into energy.
There are certain things which are crucial to consider and be aware of before using actos. Patients who have allergic reaction to pioglitazone, other thiazolidinediones or any of components of its pharmaceutical forms must avoid this drug. Using it in diabetes mellitus type 1 and diabetic ketoacidosis can prove ineffective or even harmful and its safety in pregnancy, lactation (breastfeeding) and people under 18 is still not grounded. Actos is available in the form of oral tablets containing 15, 30 or 45 mg of pioglitazone base. Actos can reportedly have side effects on female patients such as incidence of fractures of the upper arms, hands and feet in female diabetics.
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