Actost - General Information
Actost is used for the treatment of diabetes mellitus type 2. Actost selectively stimulates nuclear receptor peroxisone proliferator-activated receptor gamma (PPAR-gamma). It modulates the transcription of the insulin-sensitive genes involved in the control of glucose and lipid metabolism in the lipidic, muscular tissues and in the liver.
Pharmacology of Actost
Actost, a member of the drug group known as the thiazolidinediones or "insulin sensitizers", is not chemically or functionally related to the alpha-glucosidase inhibitors, the biguanides, or the sulfonylureas. Actost targets insulin resistance and, hence, is used alone or in combination with insulin, metformin, or asulfonylurea as an antidiabetic agent.
Actost for patients
It is important to instruct patients to adhere to dietary instructions and to have blood glucose and glycosylated
hemoglobin tested regularly. During periods of stress such as fever, trauma, infection, or surgery, medication
requirements may change and patients should be reminded to seek medical advice promptly.
ACTOS is not for everyone. ACTOS can cause fluid retention or edema (swelling), which may lead to or worsen heart
failure, so tell your doctor if you have a history of these conditions. Talk to your doctor immediately if you
experience rapid weight gain, swelling, or shortness of breath while taking ACTOS.
If you have moderate to severe heart failure, ACTOS is not recommended. Also, your doctor should perform a blood test
to check for serious liver problems or active liver disease before you start ACTOS and regularly thereafter. Do not
take ACTOS if you have active liver disease. Talk to your doctor immediately if you experience nausea, vomiting, stomach
pain, tiredness, loss of appetite, dark urine, or yellowing of the skin. (P) If you are of childbearing age, talk to your
doctor before taking ACTOS because it could increase your chance of becoming pregnant.
Some people taking ACTOS may experience cold and flu-like symptoms, mild to moderate swelling of legs and ankles, and anemia.
Occasionally, blood glucose levels increased during clinical trials. When taking ACTOS with insulin or sulfonylureas, you
may be at risk for low blood glucose.
Patients should be told to take ACTOS once daily. ACTOS can be taken with or without meals. If a dose is missed on one day,
the dose should not be doubled the following day.
When using combination therapy with insulin or oral hypoglycemic agents, the risks of hypoglycemia, its symptoms and treatment,
and conditions that predispose to its development should be explained to patients and their family members.
Therapy with ACTOS, like other thiazolidinediones, may result in ovulation in some premenopausal anovulatory women. As a result,
these patients may be at an increased risk for pregnancy while taking ACTOS. Thus, adequate contraception in premenopausal
women should be recommended. This possible effect has not been investigated in clinical studies so the frequency of this
occurrence is not known
In vivo drug-drug interaction studies have suggested that pioglitazone may be a weak inducer of CYP 450 isoform 3A4 substrate.
ACTOS is contraindicated in patients with known hypersensitivity to this product or any of its components.
Additional information about Actost
Actost Indication: Treatment of Type II diabetes mellitus
Mechanism Of Action: Actost acts as an agonist at peroxisome proliferator activated receptors (PPAR) in target tissues for insulin action such as adipose tissue, skeletal muscle, and liver. Activation of PPAR-gamma receptors regulates the transcription of insulin-responsive genes involved in the control of glucose production, transport, and utilization. In this way, pioglitazone enhances tissue sensitivity to insulin.
Drug Interactions: Ethinyl Estradiol Possible loss of contraceptive effect
Gemfibrozil Gemfibrozil increases the effect and toxicity of rosiglitazone/pioglitazone
Glucosamine Possibly hyperglycemia
Ketoconazole Ketoconazole increases the effect of pioglitazone
Mestranol Possible loss of contraceptive effect
Norethindrone Possible loss of contraceptive effect
Pregabalin Possible loss of contraceptive effect
Food Interactions: Not Available
Generic Name: Pioglitazone
Synonyms: Pioglitazona [Inn-Spanish]; Pioglitazone Hydrochloride; Pioglitazone [Ban:Inn]; Pioglitazonum [Inn-Latin]
Drug Category: Hypoglycemic Agents; Thazolidinediones
Drug Type: Small Molecule; Approved; Investigational
Other Brand Names containing Pioglitazone: Actos; Actost; Glustin;
Absorption: Following oral administration, in the fasting state, pioglitazone is first measurable in serum within 30 minutes, with peak concentrations observed within 2 hours. Food slightly delays the time to peak serum concentration to 3 to 4 hours, but does not alter the extent of absorption.
Toxicity (Overdose): Hypogycemia; LD50=mg/kg (orally in rat)
Protein Binding: > 99%
Half Life: 3-7 hours
Dosage Forms of Actost: Tablet Oral
Chemical IUPAC Name: 5-[[4-[2-(5-ethylpyridin-2-yl)ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione
Chemical Formula: C19H20N2O3S
Pioglitazone on Wikipedia: http://en.wikipedia.org/wiki/Pioglitazone
Organisms Affected: Humans and other mammals