Active substancePioglitazonePioglitazone Similar drugsTo uncover Amalvia pills inwards Pliva of Hrvatska doo Croatia Astroson® pills inwards PHARMSTANDART-FORESTRY, OJSC Russia Diab-Norma® pills inwards KRKA-RUS, LLC Russia Diaglitazone® pills inwards AKRIKHIN HFK, JSC Russia Pioglar pills inwards Ranbaxy Laboratories Limited India Pioglit pills inwards San Pharmaceutical Industries Co., Ltd. India Pioneo pills inwards Vokhard Ltd India Dosage form: & nbspPills Composition:1 tablet contains:Active substance: Pioglitazone hydrochloride (equivalent to pioglitazone) is 16.54 mg (15.0 mg) and 33.08 mg (30.0 mg)Excipients: lactose 43.70 mg / 65.420 mg, starch 15.00 mg / 20.00 mg, microcrystalline cellulose 7.00 mg / 10.00 mg, hydroxypropyl methyl cellulose 2910 (methocel E5) (hypromelose) 2.50 mg / 3.00 mg, talc purified - 1.80 mg / 2.80 mg, magnesium stearate 0.90 mg / 1.40 mg, silicon colloidal dioxide 0.460 mg / 0.70 mg, croscarmellose sodium 3.60 mg / 5.60 mg. Description:"Pioglit tablets 15 mg and 30 mg":White flat round with chamfer tablets, having a risk on one side and engraving "SUN" on the other side. Pharmacotherapeutic group:hypoglycemic agent for oral administration. ATX: & nbspA.10.B.G.03 Pioglitazone Pharmacodynamics:Hypoglycemic agent of thiazolidinedione series for oral administration.Selectively stimulates receptor-activated peroxisome proliferator (PPARΥ). PPARΥ receptors are found in tissues that play an important role in the mechanism of action of insulin (fat, skeletal muscle tissue and in the liver). Activation of nuclear receptors PPARΥ modulates the transcription of a number of genes sensitive to insulin, involved in controlling the concentration of glucose in the blood and in the metabolism of lipids. Reducing insulin resistance, increases the consumption of insulin-dependent glucose and reduces the release of glucose from the liver. Reduces the level of triglycerides, increases the concentration of high-density lipoproteins and cholesterol. Unlike derivatives of sulfonylureas, it does not stimulate insulin secretion. Pharmacokinetics:Pharmacokinetics. After ingestion, absorption is high; pioglitazone is found in the blood plasma after 30 minutes. The maximum concentration is achieved after 2 hours, after meals - after 3-4 hours. The volume of distribution is 0.22-1.04 l / kg. The connection with plasma proteins is 99%. Intensively metabolized by hydroxylation and oxidation; metabolites are also partially converted to glucuronide or sulfate conjugates.Metabolites M-II and M-IV (pioglitazone hydroxide derivatives) and M-III (keto derivatives of pioglitazone) exhibit pharmacological activity. The main cytochrome P450 isoenzymes involved in hepatic metabolism - CYP2C8 and CYP3A4, are metabolized with the participation of many other isoenzymes, including mainly the extrahepatic isoenzyme CYP1A1. Concentration in plasma of total pioglitazone (pioglitazone with active metabolites) is achieved after 24 hours with daily single use. The equilibrium concentration in plasma and pioglitazone, and total pioglitazone is achieved after 7 days.It is excreted mainly with bile in unchanged form or in the form of metabolites and is removed with feces; kidneys - 15-30% in the form of metabolites and their conjugates. The half-life of pioglitazone and total pioglitazone is from 3 to 7 hours and from 16 to 24 hours, respectively. Indications:Type 2 diabetes mellitus (in monotherapy, in combination with sulfonylurea derivatives, metformin or insulin in those cases where diet, exercise and monotherapy with one of the hypoglycemic agents mentioned above do not allow adequate glycemic control). Contraindications:- Hypersensitivity to the drug;- Type 1 diabetes mellitus, diabetic ketoacidosis;- heart failure III-IV (according to the NYHA classification);- bladder cancer at present or in history; hematuria of unclear etiology;- severe hepatic insufficiency (increased activity of liver enzymes is 2.5 times higher than the upper limit of the norm);- pregnancy, the period of breastfeeding;- Children under 18 years of age (no clinical studies have been conducted on the safety and efficacy of pioglitazone in children). Carefully:Edema syndrome, anemia, cardiac insufficiency of I-II class, impaired liver function.In connection with increased risks of developing bladder cancer, fractures and diseases of the cardiovascular system, it is necessary to carefully evaluate the relationship between benefit and risk before and during the treatment with pioglitazone in elderly patients. Dosing and Administration:Inside, 1 time per day (regardless of food intake). Monotherapy: 15-30 mg; the maximum daily dose is 45 mg. Combination therapy: sulfonylureas, metformin - treatment with pioglitazone begins with the intake of 15 mg or 30 mg (if hypoglycemia occurs, reduce the dose of sulfonylurea or metformin).Treatment in combination with insulin: the initial dose is 15-30 mg / day, the dose of insulin remains the same or decreases by 10-25% (in case the patient reports hypoglycemia, or the plasma glucose concentration drops to less than 100 mg / dL). Side effects:From the nervous system and sensory organs: dizziness, headache, hyposthenia, insomnia, blurred vision.From the respiratory system: pharyngitis; sinusitis.From the side of metabolism: weight gain, hypoglycemia.On the part of the hematopoiesis system: anemia.From the gastrointestinal tract: flatulence.From the laboratory indicators: increased activity of alanine aminotransferase and creatinine phosphokinase; a clinically insignificant decrease in hematocrit and hemoglobin.Benign and malignant swollen: infrequently - bladder cancerFrom the musculoskeletal system: arthralgia, myalgia.With long-term use of pioglitazone over 1 year in 6-9% of cases, patients experience edema, mild or moderate, and usually do not require discontinuation of therapy.Visual impairment is noted mainly at the beginning of therapy and is associated with a change in plasma glucose levels, as with other hypoglycemic agents.In rare cases, on the background of taking pioglitazone, heart failure may develop. Overdose:In case of an overdose, appropriate measures should be taken, based on clinical symptoms and laboratory test scores. Interaction:Pharmacokinetic studies on the combined use of pioglitazone and oral contraceptives have not been conducted. The use of other thiazolidinediones together with oral contraceptives containing ethinyl estradiol or norethindrone, was accompanied by a 30% decrease in the concentration of both hormones in the plasma, which can lead to a significant reduction in the contraceptive effect. Therefore, care should be taken when using pioglitazone and oral contraceptives together.There are no changes in pharmacokinetics with simultaneous administration with glipizide, digoxin, warfarin, metformin.In vitro studies it was found that ketoconazole significantly inhibits the metabolism of pioglitazone. Better blood glucose control should be performed in patients receiving concomitantly pioglitazone and ketoconazole. Special instructions:Hypoglycemic conditionsPatients receiving pioglitazone in combination with insulin or oral hypoglycemic agents, have the risk of developing hypoglycemic conditions.In this case, it may be necessary to reduce the dose of jointly used hypoglycemic drugs.OvulationIn patients with insulin resistance and anovulatory cycle in the pre-menopausal period, treatment with thiazolidinediones, including pioglitazone, can cause the onset of ovulation. A consequence of improving the sensitivity of these patients to insulin is the risk of pregnancy if adequate contraceptive methods are not used. When the offensive or planning of pregnancy should stop therapy with pioglitazone. Hematologic changes The use of pioglitazone can cause a decrease in hemoglobin and hematocrit. These changes may be associated with an increase in plasma volume and are not associated with other significant hematologic clinical effects.EdemaPioglitazone should be used with caution in patients with edema. Influence on the cardiovascular system In preclinical studies, thiazolidinediones, including pioglitazone, caused an increase in the volume of plasma and the development of cardiac muscle hypertrophy (due to preload). In clinical studies, of which patients with grade 3 and 4 heart failure (NYHA) were excluded, there was no increase in the incidence of serious cardiovascular side effects potentially associated with increased plasma volume (eg, chronic heart failure).Effects on the liverIt is recommended during the therapy with pioglitazone to regularly monitor the concentration of hepatic enzymes in the blood.The content of alanine transferase (ALT) should be determined in all patients prior to the initiation of pioglitazone therapy, every 2 months during the first year of treatment and periodically during the subsequent years of taking the drug. Liver function in patients with symptoms suspected of liver failure (nausea, vomiting, abdominal pain, weakness, anorexia, dark urine) should also be performed. The decision on the possibility of further use of pioglitazone should be based on the indicators of laboratory tests. When jaundice develops, discontinue use of the drug.Therapy with pioglitazone should not be started in patients with active liver disease, or with an increase in ALT rates more than 2.5 times higher than normal. In patients with a baseline insignificant increase in ALT (1-2.5 times the norm) or at any time during the treatment with pioglitazone, a check should be carried out to determine the causes of increased activity of the liver enzymes. The onset or continuation of pioglitazone therapy in patients with a slight increase in the activity of "liver" enzymes can be carried out with caution, and it is necessary to more often check the activity of "liver" transaminases. If there is an increase in the activity of "liver" transaminases (ALT> 2.5 times higher than normal), the activity of "liver" enzymes should be determined more often until the indices decrease to normal and initial before therapy.If the ALT level is more than 3 times higher than normal, the definition of laboratory tests should be performed as soon as possible. If ALT values remain more than 3 times higher than normal or if the patient has jaundice, pioglitazone should be discontinued.Information on a slight increase in the risk of bladder cancer with pioglitazone was obtained from a meta-analysis of controlled clinical trials (19 cases in 12,506 patients, 0.15%) compared with the control group (7 cases in 10212 patients, 0.07%) .The risk factors for developing bladder cancer include age, smoking, the use of a number of medicinal and chemotherapeutic agents, including cyclophosphamide, or previous radiotherapy for pelvic organs.Before the beginning of therapy with pioglitazone, it is necessary to clarify the causes of any macrohematuria. The patient should be warned about the need to immediately consult a doctor in the case of macromembria or other symptoms such as dysuria or urinary system emergency conditions developed during the treatment with pioglitazone. Effect on the ability to drive transp. cf. and fur:There is no evidence of the effect of pioglitazone on the ability to drive and other mechanisms. Form release / dosage:Tablets 15 mg, 30 mg Packaging:10 tablets per strip of aluminum foil. 3 strips, together with instructions for use, are placed in a cardboard box. Storage conditions:In a dry, protected from light place at a temperature of no higher than 25 ° C.Keep out of the reach of children. Shelf life:2 years. Do not use after the expiration date printed on the package. Terms of leave from pharmacies:On prescription Registration number:LSR-010500/08 Date of registration:24.12.2008 The owner of the registration certificate:San Pharmaceutical Industries Co., Ltd.San Pharmaceutical Industries Co., Ltd. India Manufacturer: & nbspSun Pharmaceutical Industries, Ltd. India Representation: & nbspSAN PHARMACEUTICAL INDUSTRIES LTD. SAN PHARMACEUTICAL INDUSTRIES LTD. India Information update date: & nbsp23.04.2012 Illustrated instructions × Illustrated instructions Instructions