Actos

About Actos

Generic Name: Pioglitazone

Actos is an antidiabetic drug which contains the active ingredient pioglitazone hydrochloride, which is classified as a thiazolidinedione among different classes of antidiabetic drugs. Actos is normally used in combination with insulin preparations to achieve optimum results. Manufactured by Zydus Pharmaceuticals, Actos ranked among the top ten best selling drugs in the United States in 2008.

Actos is a medication that is used to manage blood sugar levels in people who have non-insulin dependent, or type 2 diabetes. In most cases, Actos is used along with another form of diabetes management, such as diet, exercise, insulin or another medication for type 2 diabetes.

This diabetes medication is classified as a thiazolidinedione, which helps to decrease insulin resistance and lower blood sugar levels. When taken as prescribed, Actos can improve how the body responds to insulin and can reduce the risk of common complications that can occur as a result of high blood sugar, such as blindness, nerve problems, loss of limbs and kidney damage.

Indication/Usage: Actos is indicated for the treatment of diabetes mellitus type II which is also known as non-insulin dependent diabetes mellitus (NIDDM). It can be used as mono-therapy and in combination with other antidiabetic medications. Actos is also effective in inhibiting the conversion of pre-diabetes to diabetes mellitus type II. Though Actos may be prescribed for some off-label uses, it is not for use in the treatment of type I diabetes. Actos is undergoing clinical trials for its usage in the treatment of non-alcoholic steatohepatitis.

Dose, Administration and Dosage forms: Actos is available in round tablet formulation in 15 mg, 30 mg and 45 mg strengths. The usual starting dose of Actos is 30 mg once per day for non-congestive heart failure and 15 mg once per day for congestive heart failure patients. Actos can be administered with or without meals. Based on the results achieved in individual patients, this dose can be further titrated up to a maximum of 45 mg once per day.

Mechanism of action: Actos contains the active ingredient pioglitazone hydrochloride. Pioglitazone demonstrates its antidiabetic effects by selectively stimulating the peroxisome proliferator-activated receptor gamma (PPAR-?). It also stimulates PPAR-? but to a lesser extent. Actos converts transcription of insulin-sensitive genes, thus controlling glucose and lipid metabolism. This process results in the reduction of insulin resistance levels in hepatic and peripheral tissues. This decreased insulin resistance enhances glucose consumption and reduces glucose levels in the bloodstream.

Pioglitazone is also reported to decrease triglyceride (TG) levels and increase high-density lipoproteins (HDL).

Side-effects and safety profile: The most common side-effects reported with Actos include cold, headache, upper respiratory tract infection, sinusitis, pharyngitis, tooth issues, myalgia, mild weight gain, sore throat, fluid retention, and peripheral edema.

There are some serious side effects reported with Actos which include worsening of congestive heart failure symptoms, hypoglycemia, anemia, dyspnea, and bladder cancer.

Pioglitazone presents fewer incidents of ischemic cardiac events than other drugs of this class.

Warnings/Contraindications:

• Actos must not be prescribed in pioglitazone hypersensitive patients.

• Actos is contraindicated in patients with a history of heart failure and acute hepatic diseases.

• Actos patients must be closely monitored following any dosage increase as it may lead to rapid weight gain, dyspnea, edema, and even heart failure. Patients must immediately consult a physician when experiencing any of these symptoms.

• Actos is categorized as a pregnancy category C drug, meaning that no adequate tests results on human patients are available. In pre-clinical studies, Actos has demonstrated a delayed development of the fetus with reduced weights and delayed parturition. Based on pre-clinical studies, Actos should only be prescribed in pregnant women after a potential risk-benefit analysis by a physician.

• Though insufficiently studied in nursing mothers, pre-clinical research indicates that Actos does secrete through milk in lactating animals. Based on this evidence, Actos must not be prescribed to nursing mothers as it may cause various serious conditions to infants.

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