Пиоглар®

General characteristics. Structure:

Active agent: пиоглитазон hydrochloride of 16.53 mg, ekvivaletny to a pioglitazon of 15 mg or 33.07 mg, equivalent to a pioglitazon of 30 mg.

Pharmacological properties:

Hypoglycemic means of a tiazolidindionovy row for oral administration. Selectively stimulates at - the receptors activated by a peroksisomny proliferator (PPARy). PPARy receptors are found in the fabrics playing an important role in the mechanism of effect of insulin (fatty, skeletal muscular tissue and in a liver). Reducing insulin resistance, reduces the level of insulin and increases a consumption of insulin-dependent glucose and reduces emission of glucose from a liver. Reduces the level of triglycerides, increases concentration of lipoproteins of high density.
Pharmacokinetics. After intake absorption – high; пиоглитазон it is found in a blood plasma in 30 minutes. The maximum concentration is reached in 2 hours, after meal – in 3-4 h. Distribution volume – 0.22-1.04 l/kg. Communication with proteins of plasma – 99%. It is intensively metabolized by a hydroxylation and oxidation; metabolites also partially turn into glyukuronidny or sulphatic conjugates. Metabolites (a pioglitazona derivative) M-II, M-III and M-IV show pharmacological activity. Concentration in plasma of the general pioglitazon (пиоглитазон with active metabolites) is reached in 24 hours at daily single use. Equilibrium concentration in plasma of the general pioglitazon is reached in 7 days.
It is removed preferential with bile in not changed look or in the form of metabolites and is removed with excrements; kidneys – 15-30% in the form of metabolites and their conjugates. An elimination half-life of a pioglitazon and the general pioglitazon – from 3 to 7 hours and from 16 to 24 hours, respectively.

Indications to use:

Diabetes mellitus of type 2 (in monotherapy; in a combination with sulphonylurea derivatives, Metforminum or insulin when the diet, physical exercises and purpose of monotherapy by one of the hypoglycemic means stated above do not allow to reach adequate glycemic control).

Route of administration and doses:

Inside, 1 time a day (irrespective of meal). Monotherapy: 15-30 mg; the maximum daily dose – 45 mg. Combination therapy: sulphonylurea derivatives, Metforminum – treatment pioglitazony begin with reception 15 mg or 30 mg (at emergence of a hypoglycemia reduce a dose of drugs of sulphonylurea or Metforminum).

Features of use:

Hypoglycemic states
The patients receiving пиоглитазон in a combination with insulin or peroral hypoglycemic means have risk of development of hypoglycemic states. In this case the dose decline jointly of the used hypoglycemic drugs can be necessary.
Ovulation
With insulin resistance and an anovulatory cycle in the premenopauzalny period treatment of a tiazolidindionama, including пиоглитазон, can cause emergence of an ovulation in patients. The risk of emergence of pregnancy is a consequence of improvement of sensitivity of these patients to insulin if adequate contraceptives are not used. At approach or planning of pregnancy it is necessary to stop therapy pioglitazony.
Hematologic changes
Use of a pioglitazon can cause decrease in indicators of hemoglobin and a hematocrit. These changes can be connected with increase in volume of plasma and are not connected with other considerable hematologic clinical effects.
Hypostases
Pioglitazon has to be used with care at patients with hypostases.
Influence on cardiovascular system
In clinical trials from which patients with heart failure III and IV classes (NYHA) were excluded increase in frequency of the serious side effects from cardiovascular system which are potentially connected with increase in volume of plasma was not revealed (for example, chronic heart failure).
Influence on a liver
It is recommended pioglitazony to carry out during therapy regular control of concentration of liver enzymes to blood. Content alanine-transferase (ALT) needs to be determined at all patients prior to therapy pioglitazony, each 2 months within the first year of treatment and periodically within the next years of administration of drug. Also it is necessary to carry out definition of function of a liver at patients at emergence of symptoms, suspicious on symptoms of a liver failure (nausea, vomiting, an abdominal pain, weakness, anorexia, dark urine). Therapy pioglitazony should not be begun at patients with active diseases of a liver, or at increase in indicators of ALT norms are more than 2.5 times higher.
There are no data on influence of a pioglitazon on abilities to driving and other mechanisms.

Side effects:

From a nervous system and sense bodys: dizziness, headache, giposteziya, sleeplessness, visual disturbances.
From respiratory system: pharyngitis; sinusitis.
From a metabolism: increase in body weight, hypoglycemia.
From system of a hemopoiesis: anemia.
From digestive tract: meteorism.
From laboratory indicators: increase in activity of alaninaminotranspherase and kreatininfosfokinaza; decrease in a hematocrit and hemoglobin.
From a musculoskeletal system: arthralgia, mialgiya.
At prolonged use of a pioglitazon over 1 year in 6-9% cases at patients hypostases, poorly or moderately expressed and usually not demanding therapy cancellations are observed.
Visual disturbances are shown preferential at the beginning of therapy and are connected with change of level of glucose in a blood plasma, as well as at reception of other hypoglycemic means.
In rare instances against the background of reception of a pioglitazon development of heart failure is possible.
Against the background of therapy pioglitazony perhaps clinically insignificant decrease in level of hemoglobin and reduction of a hematocrit.

Interaction with other medicines:

Pharmacokinetic researches on combined use of a pioglitazon and oral contraceptives were not conducted. Use of other tiazolidindion together with peroralnymy the contraceptives containing ethinylestradiol or norethindrone was followed by decrease by 30% of concentration of both hormones in plasma that can lead to considerable decrease in contraceptive effect. Therefore it is necessary to be careful at combined use of a pioglitazon and oral contraceptives. Changes of pharmacokinetics at a concomitant use are not noted with glipizidy, digoksiiy, warfarin, metformin.
In the researches in vitro it is revealed what кетоконазол considerably suppresses metabolism of a pioglitazon. It is necessary to carry out more careful control of level of glucose of blood at the patients receiving at the same time пиоглитазон and кетоконазол.

Contraindications:

Hypersensitivity to drug;
diabetes mellitus of type 1, diabetic ketoacidosis;
heart failure of the III-IV class (on NYHA classification);
heavy liver failure (increase in activity of enzymes of a liver is 2.5 times higher than the upper bound of norm);
pregnancy, breastfeeding period;
children's age up to 18 years (clinical trials of safety and efficiency of use of a pioglitazon for children were not carried out).

With care – an edematous syndrome, anemia, heart failure, an abnormal liver function.

Storage conditions:

In the place, dry and unavailable to children, at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in the blister; on 3 blisters together with the application instruction in a cardboard pack.