Pioglitazone

Chemical name

5-[[4-[2-(5-Этил-2-пиридини��)этокси]фенил]метил-2,4 -тиазолидиндион (as hydrochloride)

Gross

C19-H20-N2-O3-S

Characteristics

The white crystalline powder odourless. Rat in dimethylformamide little soluble in anhydrous ethanol, very little soluble in acetone and acetonitrile, nerastvorim almost in the water.

Of drugs

The drugs-gipoglikemicescoe. Yes promotes nuclear gamma-retseptora activated proliferatorom peroksisom (Gamma-ppar). Modulating gene transcription sensitive insulino and participating in the monitoring of glucose and lipid metabolism of fat, muscle and tissue in the liver. Not incretia stimulates insulin, but is active only when saved инсулин-синтетическо�� the pancreas. Lowers инсулинрезистентност ь peripheral tissues and liver, increases the flow insulinzawisimoy glucose, reduces glucose output from the liver; reduces the level of glucose, insulin and glikozilirovannogo haemoglobin in the blood. The patients with lipid violation of the exchange rate reduces triglycerides and increases-LPVP unchanged engineers and the general Holesterina.v experimental studies is not carcinogenic and mutagennogo action. With the animals and samzam rats and 40 mg / kg / day pioglitazon (9 times MRDC in terms of 1 m ^ 2 body surface), the impact on fertility is not выявлено.Обнаруживае��ся in the blood at 30 min after oral reception C_max achieved after 2 hours Away down induction (C_max registered in 3-4 h), but did not affect the group's full. Associated with blood plasma proteins mainly albuminom by more than 99%. Average of 0.63 l / kg High concentrations in the blood maintained for a period of 24 hours after a single reception. T_1/2 of 3-7 hrs (pioglitazon) and 16-24 hrs (metabolites). Metabolised in the liver, with the participation of zitohroma R450 into two active metabolites, partly kongugiruth with glukuronova and sulphuric acids. Return to jelchew, unedited, and in the form of metabolites excreted from the body with faeces and urine (15-30%). Cl is 5-7 l / h.

Indications

Diabetes mellitus Type 2, as a stand alone treatment or in combination with derivative sulfonamidov, metforminom or insulin in the absence of the effect of diet and exercise, and alone one of the above items.

Restrictions on the use of

Age up to 18 years because the safety and efficacy of the use of this age group of patients is not defined.

Pregnancy and lactation

Contraindicated. At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity, diabetes mellitus type 2 diabetic ketoacidosis, liver disease in the acute stage, the level of ALT, exceeding the norm of 2.5 times, pregnancy, breast-feeding.

Side-Effects

Hypoglycaemia, swelling (4.8% of cases alone and 15.3% in combination with insulin), anemia (in 1.6% of cases) lowering cium, AST, ALT, alkaline phosphatase and гамма-глютамилтрансф��разы.

Specific guidance

Treatment should be carried out in conjunction with dietterapiei and exercise, under the supervision of glikozilirovannogo hemoglobin.

Patient interaction

Derivative sulfonamidov, metformin and insulin potenziruut (mutually) gipoglikemia. The weakening of the effectiveness of oral contraceptives.

Overdosing

Treatment : symptomatic therapy.

Precautions

Be wary appoint patients with circulation and moderate increases in liver enzymes. The gipoglikemii with combination therapy is the need to reduce the dose related sulfonamidov or insulin. Against the backdrop of kidney failure is not required correction doses. In the event of a jaundice treatment ceased. The patients with anovulatorian Cycle premenopauzne period reception can cause ovulation and increase the risk of pregnancy (Adequate measures contraceptives).

Dosing and Administration

Inside every day regardless of the meal. Dose picked individually. Initial dose of 15-30 mg maximum daily-45 mg / day in combination therapy-30 mg / su fa78 t.

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