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Buy Pioglitazone (Actos) online Product Name: Pioglitazone

Generic Name: Pioglitazone

Common Brands: Actos

Pharmaceutical Categories: Antidiabetic drugs

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  • Here is an additional general information about this medication active ingredient pioglitazone:

    Pharmacological action

    Pioglitazone is an oral hypoglycemic agent, series of thiazolidinedione derivatives. Powerful and selective agonist of gamma-receptors, peroxisome proliferator-activated (PPAR-gamma). PPAR-gamma receptors are found in adipose and muscle tissues and liver. Activation of nuclear receptor PPAR-gamma modulates the transcription of several genes that are sensitive to insulin, involved in controlling glucose and lipid metabolism. This medicine reduces insulin resistance in peripheral tissues and liver, as a result of this is increased flow of glucose and insulin reduced glucose production in the liver. Unlike sulfonylureas, pioglitazone does not stimulate insulin secretion by beta cells of the pancreas.
    In diabetes mellitus type 2 (insulin-dependent) decrease in insulin resistance under the action of pioglitazone reduces blood glucose levels, reduce insulin levels in plasma and hemoglobin A1c (glycated hemoglobin, HbA1c).
    In diabetes mellitus type 2 (insulin-dependent) with lipid disorders during treatment with pioglitazone there is a decrease in triglycerides and increase HDL. The level of LDL and total cholesterol in these patients does not change.

    Pharmacokinetics

    After oral administration Pioglitazone is found in fasting plasma after 30 minutes. Cmax in plasma is reached after 2 hours. At ingestion there was a slight increase of Cmax to 3-4 hours, but the extent of absorption was not changed.
    Protein binding of human serum, mainly to albumin greater than 99%; binding to other serum proteins less pronounced. The metabolites of pioglitazone M-III and M-IV also significantly associated with serum albumin is more than 98%.
    Pioglitazone is extensively metabolized in the liver by hydroxylation and oxidation. Metabolites M-II, M-IV (hydroxy derivatives of pioglitazone) and M-III (keto derivative of pioglitazone) exhibit pharmacological activity in models of type 2 diabetes in animals. Metabolites also partly converted into conjugates glucuronic or sulfuric acids.
    The metabolism of pioglitazone in the liver occurs with the participation of isoenzymes CYP2C8 and CYP3A4.
    T1/2 of unchanged pioglitazone is 3-7 hours, total pioglitazone (pioglitazone and active metabolites) is 16-24 hours. The clearance of Pioglitazone is 5-7 L / h.
    After oral administration about 15-30% of the dose of pioglitazone is found in urine. Kidneys displayed a negligible amount of pioglitazone, mainly in the form of metabolites and their conjugates.
    It is believed that the ingestion of large doses is excreted in bile as unchanged and as metabolites and excreted in the feces.
    The concentrations of pioglitazone and active metabolites in serum remained at a high level 24 h after a single daily dose.

    Why is Pioglitazone prescribed?

    Type 2 diabetes (insulin independent).

    Dosage and administration

    Pioglitazone is taken orally in dose 30 mg 1 time / day. The duration of treatment is determined individually.
    The maximum dose in combination therapy is 30 mg / day.

    Pioglitazone side effects, adverse reactions

    Metabolism: a possible development of hypoglycaemia (mild to severe).
    Hematopoietic system: possible anemia, decreased hemoglobin and hematocrit.
    Digestive system: rarely - increased ALT.

    Pioglitazone contraindications

    Diabetes mellitus type 1 (insulin-dependent), diabetic ketoacidosis, pregnancy, lactation, hypersensitivity to pioglitazone.

    Using during pregnancy and breastfeeding

    Pioglitazone is contraindicated during pregnancy and lactation. In patients with insulin resistance and anovulatory cycles in pre menopausal period the treatment with thiazolidinediones, including pioglitazone, can cause ovulation. This increases the risk of pregnancy if you do not use adequate contraception.
    In experimental studies in animals showed that pioglitazone has no teratogenic effects and adverse effects on fertility.
    Category of the fetus by FDA - C.

    Special instructions

    Pioglitazone should not be used in the presence of clinical presentations of liver disease in the active phase or an increase in ALT is 2.5 times above ULN.
    During treatment for suspected development of liver dysfunction (nausea, vomiting, abdominal pain, fatigue, lack of appetite, dark urine) should define indicators of liver function tests. In the case of jaundice pioglitazone should be discontinued.
    Pioglitazone should be used with caution in patients with edema.
    Anemia, decreased hemoglobin and hematocrit decrease may be associated with increased plasma volume and do not show any clinically significant hematological effects.
    If necessary to usee Pioglitazone simultaneously with ketoconazole should be more regular follow-up blood glucose levels.
    There have been rare cases of a temporary increase in the activity level of CPK during treatment with this drug, which had no clinical consequences. The relationship of these reactions from taking pioglitazone is unknown.
    The average values of bilirubin, AST, ALT, ALP and GGT decreased in the survey at the end of treatment by this medicine compared with those of before treatment.
    Before treatment and during the first year of treatment (every 2 months) and then periodically monitor the activity of ALT should be.
    Experimental studies have shown that pioglitazone is not mutagenic.
    The use of pioglitazone in children is not recommended.

    Pioglitazone drug interactions

    In another thiazolidinedione derivative simultaneously observed with oral contraceptives decrease the concentration of ethinyl estradiol and norethindrone in plasma by approximately 30%. Therefore, while the use of Pioglitazone and oral contraceptives may decrease contraceptive efficacy.
    Ketoconazole inhibits the metabolism of pioglitazone in the liver in vitro.
    Sulfonamides derivatives, metformin and insulin potentiate (relatively) hypoglycemia.

    Pioglitazone in case of emergency / overdose

    Treatment: symptomatic therapy.


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