Pyoglar
Pioglar: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. For violations of liver function
- 12. Use in the elderly
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Pyoglar
ATX code: A10BG03
Active ingredient: pioglitazone (pioglitazone)
Manufacturer: Ranbaxy Laboratories Limited (India)
Description and photo update: 10.10.2018
Pioglar is an oral hypoglycemic agent.
Release form and composition
The drug is produced in the form of tablets: from almost white to white, round; 15 mg - biconvex, engraved on one of the sides "15"; 30 mg - flat, chamfered, engraved on one side "30" (10 pcs. In a blister; 1, 3 or 5 blisters and instructions for the use of Pioglar in a cardboard box).
1 tablet contains:
- active substance: pioglitazone hydrochloride - 16.53 or 33.07 mg, which is equivalent to pioglitazone in the amount of 15 and 30 mg, respectively;
- additional components: calcium carboxymethyl cellulose, magnesium stearate, hydroxypropyl cellulose (low viscosity), lactose, purified water.
Pharmacological properties
Pharmacodynamics
Pioglitazone is an oral hypoglycemic agent derived from the thiazolidinedione series that selectively stimulates peroxisome proliferator-activated receptors (PPARγ). PPARγ receptors are localized in tissues that are of greater importance in the mechanism of insulin action (skeletal muscle, adipose tissue and liver). Excitation of nuclear receptors PPARγ leads to the modulation of transcription of a number of genes that are sensitive to insulin, are involved in the control of blood glucose levels and in lipid metabolic processes. Pioglitazone provides a decrease in insulin resistance, as a result of which the consumption of insulin-dependent glucose increases, the excess of glucose and its release from the liver decrease. The active substance helps to reduce triglyceride levels, increase the concentration of high density lipoproteins (HDL) and cholesterol. Pyoglar does not stimulate insulin production, unlike sulfonylurea derivatives.
Pharmacokinetics
After oral administration, there is a high absorption of pioglitazone, the active substance is detected in the blood plasma after 30 minutes, the maximum concentration (C max) is reached after 2 hours, and after a meal - after 3-4 hours. The agent is almost completely bound to plasma proteins - by 99%, the volume of distribution (V d) is 0.22–1.04 l / kg. Pioglitazone is extensively metabolized by hydroxylation and oxidation; metabolites resulting from the biotransformation of the active substance are also partially converted into sulfate / glucuronide conjugates.
Derivatives of pioglitazone hydroxide (metabolites M-II and M-IV) and the keto derivative of pioglitazone (metabolite M-III) exhibit pharmacological activity. In the process of hepatic metabolism of the drug, the main role belongs to cytochrome P450 isoenzymes - CYP3A4 and CYP2C8. To a lesser extent, many other isoenzymes are also involved in the metabolism of the drug, mainly including the extrahepatic isoenzyme CYP1A1.
In the case of a single daily use of Pioglar in plasma, the concentration of total pioglitazone (pioglitazone with active metabolites) is reached after 24 hours. Stationary concentration (C ss) in plasma of both total pioglitazone and pioglitazone is observed after 7 days.
The drug is excreted mainly with bile in unchanged form and in the form of metabolites, eliminated with feces. The kidneys are excreted 15-30% in the form of metabolites and their conjugates. The half-life (T ½) of pioglitazone and total pioglitazone is 3-7 hours and 16-24 hours, respectively.
Indications for use
Pioglar is recommended for use in type 2 diabetes mellitus (as a monotherapy drug or in combination with metformin, insulin or sulfonylurea derivatives in cases where exercise, diet and monotherapy with one of the above antidiabetic drugs do not allow achieving adequate glycemic control).
Contraindications
Absolute:
- heart failure class III – IV, according to the classification of the New York Heart Association (NYHA);
- diabetic ketoacidosis, type 1 diabetes mellitus;
- severe hepatic failure, an increase in the activity of liver enzymes, exceeding 2.5 times the upper limit of normal (UHN);
- macrohematuria of unknown origin;
- bladder cancer (including a history of indications);
- age up to 18 years;
- pregnancy and lactation;
- glucose-galactose malabsorption, lactase deficiency, galactose intolerance;
- hypersensitivity to any of the constituents of the drug.
Relative (use Pioglar tablets with extreme caution):
- heart failure;
- anemia;
- edematous syndrome;
- functional disorders of the liver.
Pioglar, instructions for use: method and dosage
Pioglar tablets are taken orally once a day, regardless of the time of the meal.
When carrying out monotherapy, it is recommended to take the drug in a dose of 15-30 mg, the maximum daily dose is 45 mg.
In combination therapy with metformin or sulfonylurea derivatives, pioglitazone should be used at an initial dose of 15 or 30 mg; if hypoglycemia occurs, it is necessary to reduce the dose of metformin or sulfonylureas.
When Pioglar is used in combination with insulin, the initial daily dose of pioglitazone should be 15-30 mg, the dose of insulin is left unchanged or reduced by 10-25% if the patient reports hypoglycemia or the plasma glucose concentration drops to a level not exceeding 100 mg / dl.
Side effects
- respiratory system: sinusitis, pharyngitis;
- nervous system and sensory organs: headache, dizziness, insomnia, hypoesthesia; visual disorders (occur, as a rule, at the beginning of the course of therapy and are associated with changes in plasma glucose levels, as with the use of other antidiabetic agents);
- hematopoietic system: anemia;
- metabolism: hypoglycemia, weight gain;
- gastrointestinal tract: flatulence;
- benign or malignant tumors: bladder cancer, signs of the development of which may be frequent urge to urinate, gross hematuria, pain during urination, pain in the abdominal cavity or in the lumbar region (the appearance of these disorders must be urgently reported to the attending physician);
- musculoskeletal system: myalgia, arthralgia;
- laboratory parameters: increased activity of alanine aminotransferase (ALT) and creatine phosphokinase; a decrease in hemoglobin levels and a decrease in hematocrit (usually clinically insignificant; may be due to an increase in plasma volume and not indicate the development of other serious hematological clinical effects).
If the duration of treatment is more than 1 year, in 6-9% of cases, patients may have the appearance of mild / moderate edema, which, as a rule, does not require discontinuation of Pioglar.
During the period of therapy, in some cases, heart failure may occur.
Overdose
In case of suspicion of an overdose of Pioglar, appropriate measures are prescribed, depending on the clinical symptoms and the results of laboratory tests.
special instructions
In patients with anovulatory cycle in the premenopausal period and insulin resistance as a result of treatment with pioglitazone, restoration of ovulation may be noted. Due to the increased sensitivity of these patients to insulin, in the absence of adequate contraception, the risk of pregnancy increases. If pregnancy occurs during therapy or the patient is planning a pregnancy, pioglitazone should be discontinued.
According to the results of preclinical studies, thiazolidinediones, including pioglitazone, led to an increase in plasma volume and the development of myocardial hypertrophy, due to preload. In clinical studies in which patients with class III and IV heart failure (NYHA) did not participate, there was no increase in the frequency of severe adverse reactions from the cardiovascular system, depending on an increase in plasma volume (chronic heart failure).
The results of controlled clinical trials, as well as the available epidemiological data, indicate an increased threat of bladder cancer in patients with diabetes who take pioglitazone in high daily doses for a long time. However, the presence of these data does not exclude the possibility of bladder cancer on the background of short-term drug therapy. The risk of bladder cancer may include the following factors: old age, smoking (including in the past), chemotherapy (including the use of cyclophosphamide), radiation therapy of the pelvic organs, and some occupational hazards. Before starting the course of therapy, it is required to conduct macroscopic studies aimed at establishing any gross hematuria. All signs of dysuria and any acute development of symptoms from the urinary tract and / or bladder should be immediately reported to the doctor.
Influence on the ability to drive vehicles and complex mechanisms
Due to the possible development of dizziness and visual impairment during therapy, patients who drive vehicles and other complex mechanisms should be careful.
Application during pregnancy and lactation
During pregnancy and lactation, drug therapy is contraindicated.
Pediatric use
For patients under 18 years of age, the use of Pyoglar is contraindicated due to the lack of clinical studies of the efficacy and safety of its use in children and adolescents.
For violations of liver function
During the period of therapy, it is recommended to regularly monitor the concentration of liver enzymes in the blood. In all patients, before starting treatment with pioglitazone, every 2 months during the first year of taking Pyoglar, and periodically during subsequent years of therapy, it is required to determine the ALT level. It is also necessary to assess liver activity when symptoms appear that may be signs of liver failure, such as abdominal pain, nausea, vomiting, anorexia, weakness, dark urine. If jaundice occurs, you must stop taking Pyoglar.
The use of a hypoglycemic agent is contraindicated in patients with active liver diseases or against the background of an increase in ALT values, exceeding more than 2.5 times the ULN.
With a slight increase in the level of ALT (1–2.5 times higher than normal) before the start of the course or during the period of therapy, an examination is required to establish the causes of this disorder. Begin or continue treatment with Pyoglar in the presence of a moderate increase in the activity of hepatic enzymes should be with extreme caution, conducting more frequent monitoring of their activity.
In the case when an increase in the activity of hepatic transaminases is detected by more than 2.5 times compared to VGN, it is necessary to regularly monitor the level of enzymes until the indicators decrease to normal or to the initial ones. If the ALT level persistently exceeds normal values by more than 3 times or jaundice occurs, pioglitazone should be discontinued.
Use in the elderly
In the elderly, before and during therapy, due to the aggravating threat of fractures, cardiovascular diseases and bladder cancer in patients of this age group, a particularly careful assessment of the benefit and risk ratio of Pyoglar treatment should be carried out.
Drug interactions
- oral contraceptives - pharmacokinetic studies of the combined use of these drugs and pioglitazone have not been carried out, however, the use of other thiazolidinediones in combination with oral contraceptives containing ethinylestradiol / norethindrone contributed to a decrease in the plasma level of both hormones by 30%, which could cause a significant weakening of contraception; caution should be exercised with this combination;
- warfarin, digoxin, metformin, glipizide - no changes in pioglitazone pharmacokinetics were observed;
- ketoconazole - the metabolism of pioglitazone was inhibited to a large extent, according to in vitro studies; with this combination, it is necessary to carefully monitor the concentration of blood glucose;
- other oral antidiabetic drugs: there is no data on the use of pioglitazone in triple combination with these drugs.
Analogs
Pioglar's analogs are: Astrozone, Diab-norm, Piouno, Amalvia, Diaglitazone, Piogli.
Terms and conditions of storage
Store in a place protected from moisture penetration and out of reach of children, at a temperature not exceeding 25 ° C.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Pioglar
According to reviews, Pioglar is an effective hypoglycemic agent used for the treatment of type 2 diabetes mellitus, both in monotherapy and in combination with other hypoglycemic agents, including insulin. Patients note that the drug improves glucose control and increases cell resistance to insulin, but everyone recommends using Pioglar only as directed by a doctor.
The disadvantages of Pioglar include the presence of contraindications and the development of side effects, in particular an increase in body weight, headache, flatulence.
Price for Pioglar in pharmacies
There is no reliable information about the price of Pioglar, since the drug is not currently sold in pharmacies.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
