Universal reference book for medicines
Product name: PIOUNO (PIOUNO)

Active substance: pioglitazone

Type: Oral hypoglycemic drug

Manufacturer: WOCKHARDT (India)
Composition, form of production and packaging
Tablets
1 tab.

pioglitazone 15 mg

15 pcs.
- packings cellular planimetric (2) - packs cardboard.
Tablets 1 tab.

pioglitazone 30 mg

15 pcs.
- packings cellular planimetric (2) - packs cardboard.
Tablets 1 tab.

pioglitazone 15 mg

15 pcs.
- packings cellular planimetric (2) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2010.

PHARMACHOLOGIC EFFECT

Hypoglycemic agent of thiazolidinedione series for oral administration.

Pioglitazone stimulates specific gamma receptors of the nucleus, activated by peroxisome proliferator (PPAR?).
Modulates transcription of genes sensitive to insulin and involved in controlling glucose concentrations in the blood and lipid metabolism in fat, muscle and liver. Unlike drugs, derivatives of sulfonylureas, pioglitazone does not stimulate insulin secretion, but it shows activity only with the preserved insulin-synthetic function of the pancreas. Pioglitazone reduces the insulin resistance of peripheral tissues and liver, increases the consumption of insulin-dependent glucose and reduces the release of glucose from the liver; reduces the concentration of glucose, insulin and glycosylated hemoglobin. Against the background of pioglitazone therapy, the concentration of triglycerides and free fatty acids in the blood plasma decreases, and the concentration of high-density lipoproteins increases.
For patients with type 2 diabetes mellitus, control of blood glucose levels both on an empty stomach and after meals is improved.

PHARMACOKINETICS

Suction

Pioglitazone is rapidly absorbed, C max of pioglitazone in blood plasma is usually achieved 2 hours after ingestion.
In the range of therapeutic doses, concentrations in the blood plasma increase proportionally with increasing dose. With repeated administration of cumulation, pioglitazone and its metabolites do not occur. Eating does not affect absorption. Bioavailability is over 80%.
Distribution

V d is 0.25 l / kg body weight and is achieved 4-7 days after the initiation of therapy.
The binding with plasma proteins of pioglitazone is more than 99%, its metabolites - more than 98%.
Metabolism

Pioglitazone is metabolized by hydroxylation and oxidation.
This process mainly takes place with the participation of cytochrome P450 isoenzymes (CYP2C8 and CYP3A4), and, to a lesser extent, other isoenzymes. Three of the six identified metabolites (M) show pharmacological activity (M-II, M-III, M-IV). Taking into account the pharmacological activity, concentration and degree of binding to plasma proteins, pioglitazone and M-III metabolite equally determine the overall activity, the contribution of metabolite M-IV to the total activity of the drug is about 3 times that of pioglitazone, and the relative activity of M-II metabolite is minimal .
In vitro studies have shown that pioglitazone does not inhibit the isoenzymes CYP1A, CYP2C8 / 9, CYP3A4.

Excretion

It is excreted mainly through the intestine, and also by the kidneys (15-30%) in the form of metabolites and their conjugates.
T 1/2 of unchanged pioglitazone from blood plasma averages 3-7 hours, and for all active metabolites 16-24 hours.
The concentration of pioglitazone and active metabolites in the blood plasma remains at a sufficiently high level within 24 hours after a single daily dose.

Pharmacokinetics in special clinical cases

Elderly patients and / or renal dysfunction are not required to adjust doses.

Against the background of a violation of liver function, the fraction of free pioglitazone is higher.

INDICATIONS

Diabetes mellitus type 2:

- in monotherapy in patients with excessive body weight with ineffectiveness of diet and exercise with intolerance to metformin or the presence of contraindications to its use;

- as part of combination therapy:

1. with metformin in patients with excessive body weight in the absence of adequate glycemic control against monotherapy with metformin;

2. With derivatives of sulfonylureas only in patients who are contraindicated with metformin, in the absence of adequate glycemic control against the background of monotherapy with sulfonylurea derivatives.

3. with insulin in the absence of adequate glycemic control on the background of insulin therapy in patients to whom metformin is contraindicated.

DOSING MODE

Inside 1 time / day, regardless of food intake.

The recommended starting doses are 15 or 30 mg 1 time / day.
The maximum daily dose for monotherapy is 45 mg, with combined therapy 30 mg.
When pioglitazone is prescribed in combination with metformin, metformin can be continued at the same dose.

In combination with derivatives of sulfonylureas: at the beginning of treatment, their administration can be continued at the same dose.
In the case of hypoglycemia, a dose of the sulfonylurea derivative should be reduced.
In combination with insulin: the initial dose of pioglitazone is 15-30 mg / day, the dose of insulin remains the same or decreases by 10-25% when hypoglycemia occurs.

For elderly patients, dose adjustment is not required.

For patients with impaired renal function (creatinine clearance more than 4 ml / min), dose adjustment is not required.
About the use of pioglitazone in patients receiving hemodialysis treatment , there is no data. Therefore, do not use pioglitazone in this group of patients.
Do not use pioglitazone in patients with impaired liver function .

There is no data on the use of pioglitazone in patients under the age of 18 , so the use of pioglitazone in this age group is not recommended.

SIDE EFFECT

Frequency: very often more than 1/10, often more than 1/100 and less than 1/10, infrequently more than 1/1000 and less than 1/100, rarely more than 1/10 000 and less than 1/1000, very rarely - less than 1/10 000, including individual reports.

Monotherapy with pioglitazone

From the senses: often - a violation of vision.

On the part of the respiratory system: often - infections of the upper respiratory tract;
infrequently sinusitis.
From the side of metabolism: often - weight gain.

From the nervous system: often - hypoesthesia;
infrequently - insomnia.
Combination of pioglitazone with metformin

On the part of the organs of hematopoiesis: often - anemia.

From the senses : often - a violation of vision.

From the digestive system: infrequently - flatulence.

From the side of metabolism: often - weight gain.

From the musculoskeletal system: often - arthralgia.

From the nervous system: often - a headache.

From the genitourinary system : often - hematuria, erectile dysfunction.

Combination of pioglitazone with sulfonylurea derivatives

From the senses: infrequently - vertigo, impaired vision.

From the digestive system: often - flatulence.

Other: infrequent - fatigue.

From the side of metabolism: often - weight gain;
infrequently - increased lactate dehydrogenase activity, increased appetite, hypoglycemia.
From the nervous system: often - dizziness;
infrequently - a headache.
From the genitourinary system: infrequently - glucosuria, proteinuria.

From the skin: infrequently - increased sweating.

Combination of pyogltopone with metformin and sulfonylurea derivatives

From the side of metabolism: very often - hypoglycemia;
often - increased body weight, increased activity of creatine phosphokinase (CK).
From the musculoskeletal system: often - arthralgia.

Combination of pioglitazone with insulin

From the side of metabolism: often - hypoglycemia.

From the musculoskeletal system: often - back pain, arthralgia.

From the respiratory system: often - shortness of breath, bronchitis.

From the cardiovascular system: often - heart failure.

Other: very often - swelling.

Post-marketing experience

From the sense organs: the frequency is unknown - edema of the macula, fracture of bones.

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 disturbances appear primarily at the beginning of therapy and are associated with a change in the concentration of glucose in the blood plasma, as well as when taking other hypoglycemic agents.

CONTRAINDICATIONS

- Type 1 diabetes mellitus;

- diabetic ketoacidosis;

heart failure, incl.
in the anamnesis (I-IV class according to the NYHA classification);
- liver failure (increased activity of hepatic enzymes is 2.5 times higher than the upper limit of the norm);

- chronic renal failure (CC less than 4 ml / min);

- Lactase deficiency, lactose intolerance, glucose-galactose malabsorption;

- Pregnancy;

- lactation period;

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

- Hypersensitivity to pnoglitazone or to other components of the drug.

With caution - edematous syndrome, anemia.

Application during pregnancy and lactation.
The efficacy and safety of pioglitazone in pregnant women has not been studied, so it is contraindicated to use the drug in pregnancy. It was proved that pioglitazone slows the growth of the fetus. It is not known whether pioglitazone is excreted in breast milk, so the drug should not be taken to women during lactation. If it is necessary to prescribe the drug during lactation, breastfeeding should be discontinued.
PREGNANCY AND LACTATION

Contraindicated in pregnancy and lactation.

APPLICATION FOR FUNCTIONS OF THE LIVER

For patients with impaired renal function (creatinine clearance more than 4 ml / min), dose adjustment is not required.
About the use of pioglitazone in patients receiving hemodialysis treatment, there is no data. Therefore, do not use pioglitazone in this group of patients.
Contraindicated:

- chronic renal failure (CC less than 4 ml / min).

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Do not use pioglitazone in patients with impaired liver function .

Contraindicated:

- hepatic insufficiency (an increase in the activity of hepatic enzymes is 2.5 times higher than the upper limit of the norm).

APPLICATION FOR CHILDREN

There is no data on the use of pioglitazone in patients under the age of 18 , so the use of pioglitazone in this age group is not recommended.

APPLICATION IN ELDERLY PATIENTS

For elderly patients, dose adjustment is not required.

SPECIAL INSTRUCTIONS

In the treatment of type 2 diabetes mellitus, in addition to taking pioglitazone, it is recommended that you follow a diet and exercise to maintain the effectiveness of drug therapy, as well as possible weight gain.

Against the background of the use of pioglitazone, fluid retention and an increase in the plasma volume may occur, which may lead to the development or aggravation of the course of heart failure, therefore, if the state of the cardiovascular system worsens, pioglitazone should be discontinued.

Patients who have at least one risk factor for developing chronic heart failure (CHF) should be treated with a minimal dose and gradually increased.
It is necessary to identify early symptoms of CHF, increase in body weight (may indicate the development of CHF), or development of edema, especially in patients with reduced cardiac output. In the case of development of CHF, the drug is immediately withdrawn.
Pioglitazone can cause a violation of liver function.
Before the start of treatment and periodically during therapy, the activity of hepatic enzymes should be investigated. If ALT activity exceeds the upper limit by 2.5 times, or if there are other symptoms of liver failure, the use of pioglitazone is contraindicated. If, in 2 consecutive studies, ALT activity exceeds the upper limit of the norm 3 times or the patient develops jaundice, the treatment with pioglitazone is immediately stopped. If the patient has symptoms suggestive of liver dysfunction (unexplained nausea, vomiting, abdominal pain, weakness, anorexia, darkening of urine), hepatic enzymes should be immediately investigated.
Pioglitazone can cause a decrease in hemoglobin or hematocrit by 4% and 4.1%, respectively, which may be a consequence of hemodilution (due to fluid retention).

Pioglitazone increases the sensitivity of tissues to insulin, which increases the risk of hypoglycemia in patients receiving combination therapy containing sulfonylureas or insulin derivatives.
May require a lower dose of the latter.
Pioglitazone can cause or aggravate edema of the macula, which can lead to a decrease in visual acuity.

Pioglitazone can increase the incidence of fractures in women.

In patients with polycystic ovary syndrome, an increase in insulin sensitivity may lead to the resumption of ovulation and possible pregnancy.
Patients with polycystic ovary syndrome who do not want to become pregnant should use reliable contraceptive methods. If pregnancy occurs, treatment should be stopped immediately.
Impact on the ability to drive vehicles and manage mechanisms

Taking into account side effects of the drug, care must be taken when driving vehicles and working with mechanisms that require concentration of attention.

OVERDOSE

Symptoms: hypoglycemia is possible when taking pioglitazone in combination with sulfonylurea and insulin derivatives.

Treatment: symptomatic therapy.

DRUG INTERACTION

When using pioglitazone in combination with other oral hypoglycemic drugs, hypoglycemia may develop.
In this case, a dose reduction of another oral hypoglycemic drug may be required.
Against the background of combined use of pioglitazone with insulin, it is possible to develop heart failure.

Pioglitazone does not affect the pharmacokinetics and pharmacodynamics of glipizide, digoxin, warfarin, metformin.

Gemfibrozil increases the AUC value of pioglitazone by 3 times.

Rifampicin accelerates the metabolism of pioglitazone by 54%.

In vitro, ketoconazole inhibits the metabolism of pioglitazone.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored in a dry, dark place at a temperature of no higher than 25 В° C.
Keep out of the reach of children.
Shelf life - 3 years.
Do not use after the expiration date.
Alphabetical index of medicines:
A  B  V  G  D  E  J
Z  I  Y  K  L  M  N
O  P  R  S  T  U  F
H  C  CH  SH  E  U  Y

Privacy policy:
Copyright 2009 - 2017. Universal reference book of medicines. All rights reserved.
When using site materials, an active hyperlink is required!