Index of drugs

Treatment of type 2 diabetes:in monotherapy in adult patients (especially overweight patients) with insufficient glycemic control through diet and physical activity and who can not be given Metformin due to contraindications or intolerance;in dual oral therapy: in combination with metformin in adult patients (especially those who are overweight) who have insufficient glycemic control, despite the use of metformin as the single tolerated maximum dose; in combination with a sulphonylurea, only in adult patients with metformin intolerance or in whom metformin is contraindicated; in patients whose blood Glucose is not adequately controlled despite the use of maximum tolerated doses of a sulphonylurea monotherapy; inthree-oral oral therapy in combination with metformin and a sulphonylurea in adult patients (especially those who are overweight) who are not adequately controlled on glycemia despite dual oral therapy. Pioglitazone is also indicated in combination with insulin in type 2 diabetes in adult patients with insufficient glycemic control with insulin who can not take metformin because of contraindications or intolerance.

1 tabl contains 15 mg or 30 mg of pioglitazone in the hydrochloride form. The preparation contains lactose.

An antidiabetic drug, a thiazolidinedione derivative. Pioglitazone can work by reducing insulin resistance. It probably works by activating specific nuclear receptors (γ receptors activated by PPAR-γ peroxisomal proliferators), increasing the sensitivity of liver, adipose and skeletal muscle cells to insulin in animals. Treatment with pioglitazone leads to reduced hepatic glucose production and increased peripheral tissue glucose uptake in insulin resistance. After oral administration, the drug is rapidly absorbed. The maximum plasma concentration usually occurs after 2 hours after administration. The state of balance is achieved after 4-7 days of drug administration. Multiple administration does not lead to accumulation of the drug or its metabolites in the body. Absorption does not depend on the food you eat. The absolute bioavailability is more than 80%. Pioglitazone and all its active metabolites are very much bound (> 99%) bound to plasma proteins. The drug is extensively metabolised in the liver, mainly involving CYP2C8, although other isoenzymes may be involved to a lesser extent. Three of the six detected metabolites are active. The drug is excreted mainly in faeces (55%) and to a lesser extent in urine (45%). Medium T_0,5 in the phase of elimination of unmetabolized pioglitazone is 5-6 h, and T_0,5 all active metabolites are 16-23 h.

Hypersensitivity to the active substance or any of the excipients. Cardiac failure occurring today or in the history (NYHA class I-IV). Hepatic dysfunction. Ketoacidosis.

Pioglitazone can cause fluid retention, which may exacerbate or precipitate heart failure. When treating patients with at least one risk factor for congestive heart failure (eg having a history of myocardial infarction or symptomatic ischemic heart disease), the medicine should be started at the lowest available dose and gradually increased. It should be observed whether patients, especially those with limited cardiac reserve, exhibit signs and symptoms of heart failure, weight gain or edema. Because of the risk of heart failure when pioglitazone is used in combination with insulin, patients should be monitored for signs and symptoms of heart failure, weight gain and edema. Because insulin and pioglitazone cause fluid retention in the body, concomitant use of these drugs may increase the risk of edema.In the event of any cardiac deterioration, treatment with pioglitazone should be discontinued. Due to limited experience, caution should be used in patients over 75 years of age. During treatment with pioglitazone, periodic monitoring of liver enzymes is recommended. In all patients, liver enzymes should be determined before starting treatment; do not start treatment if your liver enzymes are elevated (ALT> 2.5 times the upper limit of normal) or if you have any other symptoms of liver disease. After initiation of pioglitazone, periodic liver enzyme tests are recommended based on clinical judgment. If during the treatment with pioglitazone the ALT activity is 3 times higher than the upper limit of normal values, the determination of liver enzymes should be repeated as soon as possible. The drug should be discontinued if ALT is still 3 times higher than the upper limit of normal. If the patient develops symptoms that may indicate liver dysfunction, including unexplained nausea, vomiting, abdominal pain, fatigue, lack of appetite and / or dark urine, liver enzymes should be measured. The decision to continue treatment with pioglitazone, before obtaining laboratory results, should be made on the basis of clinical evaluation. If you have jaundice, stop taking the medicine. The drug may cause an increase in the weight of patients, which may sometimes be a sign of heart failure - during treatment should control body weight. Patients should be advised to strictly follow a controlled caloric diet. During treatment with pioglitazone, a slight reduction in mean hemoglobin (a relative decrease of 4%) and hematocrit (a relative decrease of 4.1%), consistent with hemodilution, was observed. As a result of increased insulin sensitivity, patients receiving pioglitazone in combination therapy with two or three oral medicines, including sulphonylurea or in combination therapy with two drugs, including insulin, may be at higher risk of hypoglycaemia associated with the dose of this drug and it may be necessary to reduce the dose of a sulphonylurea or insulin. Cases of onset or worsening of diabetic macular edema with deterioration of visual acuity have been reported after marketing. In many of these patients, peripheral edema was also observed. In patients reporting abnormal visual acuity, ophthalmologic consultation should be considered. In long-term treatment of women with pioglitazone, an increased risk of bone fractures should be considered; there was no increase in the frequency of fractures in men. Because pioglitazone supports the action of insulin, the use of the drug in patients with polycystic ovarian syndrome may result in the resumption of ovulation - these patients may be pregnant. Pioglitazone should be used with caution if concomitant medications (eg gemfibrozil) or inducing (eg rifampicin) CYP2C8 are taken concomitantly - glycemia should be closely monitored and the dose of pioglitazone (within the recommended dosage range) or change in antidiabetic therapy should be considered. The safety and efficacy of pioglitazone in children and adolescents under 18 years have not been established. The product contains lactose - should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.

The preparation should not be used during pregnancy and breastfeeding.

monotherapy. Common: upper respiratory tract infections, hypoesthesia, visual disturbances, bone fractures (in women), weight gain. Uncommon: sinusitis, insomnia. Not known: macular edema, ALT increase.Combination therapy with metformin. Common: upper respiratory tract infections, anemia, hypoesthesia, headache, visual disturbances, bone fractures (in women), joint pain, hematuria, erectile dysfunction, weight gain. Uncommon: sinusitis, insomnia, bloating. Not known: macular edema, ALT increase.Combination therapy with sulphonylureas. Common: upper respiratory tract infections, hypoesthesia, central dizziness, bloating, bone fractures (in women), weight gain. Uncommon: sinusitis, hypoglycaemia, increased appetite, headache, insomnia, blurred vision, diarrhoeas-induced vomiting, sweating, glycosuria, proteinuria, fatigue, increase in lactate dehydrogenase activity. Not known: macular edema, ALT increase.Combination therapy with metformin and sulphonylurea. Very common: hypoglycaemia. Common: upper respiratory tract infections, hypoesthesia, bone fractures (in women), joint pain, weight gain, increased creatine phosphokinase in the blood. Uncommon: sinusitis, insomnia. Not known: macular edema, ALT increase.Combination therapy with insulin. Very common: swelling. Common: upper respiratory tract infections, bronchitis, hypoglycemia, hypoesthesia, heart failure, shortness of breath, bone fractures (in women), joint pain, back pain, weight gain. Uncommon: sinusitis, insomnia. Not known: macular edema, ALT increase.

Orally. Adults: treatment can be started with a dose of 15 mg or 30 mg once a day. The dose can be increased up to a maximum dose of 45 mg once a day. In the case of combination therapy with insulin, the active dose of insulin may be continued after initiation of pioglitazone therapy. If you have hypoglycaemia, reduce the insulin dose. No dose adjustment is required in the elderly or in patients with renal impairment (creatinine clearance> 4 ml / min); there is no data on the use of the drug in dialysis patients, therefore, pioglitazone should not be used in these patients.
The preparation should be taken with or without food, the tablets should be swallowed with a glass of water.