Universal reference book for medicines

Active substance: pioglitazone

Type: Oral hypoglycemic drug

Manufacturer: Chemical-Pharmaceutical Plant Akrihin (Russia)
Composition, form of production and packaging
Tablets are
white with a creamy or yellowish hue of color, flat-cylindrical, with a bevel.

1 tab.

pioglitazone hydrochloride 16.53 mg,

which corresponds to the content of pioglitazone 15 mg

Excipients: lactose (milk sugar), microcrystalline cellulose, giprolose (hydroxypropyl cellulose), croscarmellose sodium, silicon dioxide colloid, magnesium stearate.

10 pieces.
- packings cellular planimetric (3) - packs cardboard.
Tablets are white with a creamy or yellowish hue of color, flat-cylindrical, with a bevel.

1 tab.

pioglitazone hydrochloride 33.06 mg,

which corresponds to the content of pioglitazone 30 mg

Excipients: lactose (milk sugar), microcrystalline cellulose, giprolose (hydroxypropylcellulose), croscarmellose sodium, silicon dioxide colloid, magnesium stearate.

10 pieces.
- packings cellular planimetric (3) - packs cardboard.

Description of the drug approved by the manufacturer for the printed edition of 2011.


Hypoglycemic drug for oral administration, thiazolidinedione derivative.
Selectively stimulates? -receptors, activated by peroxisome proliferator (PPAR?). PPAR? -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 PPAR? 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 HDL and cholesterol. Unlike derivatives of sulfonylureas, it does not stimulate insulin secretion.


After ingestion, absorption is high.
Pioglitazone is found in the blood plasma after 30 minutes. C max in the blood plasma is achieved after 2 hours, after eating - after 3-4 hours.
Distribution and Metabolism

V d is 0.22-1.04 l / kg.
Binding to plasma proteins - 99%.
The plasma concentration of total pioglitazone (pioglitazone with active metabolites) is achieved after 24 hours with a daily single application.
C ss in plasma and pioglitazone and total pioglitazone is achieved after 7 days.
Intensively metabolized by hydroxylation and oxidation.
Metabolites also partially convert to glucuronide or sulfate conjugates. Metabolites M-II and M-IV (derivatives of pioglitazone hydroxide) and M-III (keto derivatives of pioglitazone) exhibit pharmacological activity. The main isoenzymes of cytochrome P450 involved in hepatic metabolism are CYP2C8 and CYP3A4. Metabolism is also realized with the participation of many other isoenzymes, including mainly the extrahepatic isoenzyme CYP1A1.

T 1/2 of pioglitazone and total pioglitazone is 3-7 hours and 16-24 hours, respectively.

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.


Type 2 diabetes mellitus (non-insulin dependent):

- as a 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.


Diaglitazone В® is administered orally, 1 time / day (regardless of food intake).

With monotherapy, the dose is 15-30 mg;
the maximum daily dose is 45 mg.
In combination therapy with sulfonylureas or with metformin, treatment with pioglitazone is started with 15 mg or 30 mg (hypoglycemia is decreased by the dose of sulfonylurea or metformin).

When treated in combination with insulin, the initial dose is 15-30 mg / day.
The dose of insulin is kept the same or reduced by 10-25% (in case the patient reports hypoglycemia, or the plasma glucose concentration drops to less than 100 mg / dL).

From the side of the central nervous system: dizziness, headache, hypoesthesia, insomnia.

From the sense organs: visual disturbances, which are noted mainly at the beginning of therapy and are associated with changes in the level of glucose in the blood plasma, as well as when taking other hypoglycemic agents.

On the part of the respiratory system: pharyngitis, sinusitis.

From the side of metabolism: weight gain, increased activity of CK;
with prolonged use for more than 1 year in 6-9% of cases there are edema, mild or moderate, and usually do not require the abolition of therapy.
From the endocrine system: hypoglycemia.

From the hemopoietic system: a clinically insignificant decrease in hematocrit and hemoglobin, anemia.

From the digestive system: flatulence, increased activity of ALT.

From the musculoskeletal system: arthralgia, myalgia.

Other: rarely - heart failure.


- Type 1 diabetes mellitus (insulin-dependent);

- diabetic ketoacidosis;

- Cardiac insufficiency of III-IV functional class (according to NYHA classification);

- severe hepatic insufficiency (increased activity of liver enzymes is 2.5 times higher than UGN);

- Pregnancy;

- the period of lactation (breastfeeding);

- Children under 18 years of age (no clinical studies of the safety and efficacy of pioglitazone in children have been performed);

- Hypersensitivity to the components of the drug.

With caution should be used in patients with edematous syndrome, anemia, cardiac insufficiency of I-II functional class, violations of liver function (increased activity of hepatic transaminases 1-2.5 times higher than UGN).


Contraindicated in pregnancy and lactation (breastfeeding).


Contraindication: severe hepatic insufficiency (increased activity of liver enzymes is 2.5 times higher than ULN).


Contraindication: children under 18 years of age (clinical studies of safety and efficacy of pioglitazone in children have not been performed).


In patients receiving pioglitazone in combination with insulin or oral hypoglycemic agents, there is a risk of developing hypoglycemic conditions.
In this case, it may be necessary to reduce the dose of jointly used hypoglycemic drugs.
In patients with insulin resistance and anovulatory cycle in the premenopausal period, treatment with thiazolidinediones, including pioglitazone, may cause 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.
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.
In preclinical studies, thiazolidinediones, including pioglitazone, caused an increase in plasma volume and the development of cardiac muscle hypertrophy (due to preload).
In clinical studies, of which patients with heart failure of grade III and IV functional classes (NYHA classification) were excluded, there was no increase in the incidence of serious cardiovascular side effects potentially associated with increased plasma volume (eg, chronic heart failure ).
It is recommended during the therapy with pioglitazone to regularly monitor the activity of hepatic enzymes in the blood.
The ALT content should be determined in all patients before the start 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 an initial slight increase in ALT (1-2.5 times the norm) or at any time during the treatment with pioglitazone, a check should be conducted to identify the causes of increased activity of liver enzymes. The onset or continuation of pioglitazone therapy in patients with a slight increase in hepatic enzyme activity can be carried out with caution, and it is often necessary to check the activity of hepatic transaminases. If there is an increase in hepatic transaminase activity (ALT> 2.5 times higher than normal), liver enzyme activity should be determined more often until the indices drop to normal and baseline 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.
Impact on the ability to drive vehicles and manage mechanisms

There is no data on the effect of pioglitazone on the ability to drive vehicles and other mechanisms.


Symptoms: an overdose of pioglitazone in monotherapy is not accompanied by the emergence of specific clinical symptoms;
an overdose of pioglitazone in combination with a drug of sulfonylureas may be accompanied by the development of symptoms of hypoglycemia.
Treatment: there is no specific overdose treatment.
If necessary, symptomatic therapy (eg, treatment of hypoglycemia) is performed.

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 norethisterone 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.
It should be more closely monitor blood glucose levels in patients receiving both pioglitazone and ketoconazole.
There is no data on the use of pioglitazone in triple combination with other oral hypoglycemic drugs.


The drug is released by prescription.


The drug should be stored out of reach of children, dry, protected from light at a temperature of no higher than 25 В° C.
Shelf life - 2 years.
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