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Avandia

See also Rosiglitazone

Roman name

Avandia

The composition and the form of

1 tablet, film coated liner contains rosiglitazona (as maleate) 1, 2, 4 or 8 mg.

Of drugs

Gipoglikemicescoe. Increases sensitivity of receptors to insulino (is a selective agonist of nuclear receptor-Ppar-gamma peroxisomal proliferator activated gamma) in adipose tissue, skeletal muscular and liver. Reduces levels of glucose, insulin and free fatty acids in the blood, improves metabolic processes.

Pharmacokinetics

The ingestion doses of 4-8 mg absolute bioavailability of approximately 99%. C_max achieved within 1 h. Simultaneous eating does not affect the AUC, lowers C_max (approximately 20-28%) and slightly more T_max (the change is not clinically meaningful). Associated with the plasma protein at 99.8%, T_1/2 preparation of plasma, 3-4 h, the volume of 14 litres, the total plasma Cl-3 l / h. Metabolised in the liver, with the participation of CYP2C8 and (to a small extent) by CYP2C9 N-demetilirovania gidrooksilirovania and with the formation of active metabolites (major metabolite - paragidroksisulfat). Write only in the form of metabolites kidneys (75%) and gastrointestinal (25%). T_1/2 metabolites-130 hours In repeated moves possible cumulation plasma mainly in the form of a basic metabolita (probably 5-kratnoe increase plasma levels). In Hepatic (moderate and severe symptoms) decreases binding protein from the blood and Cl increases (2-3 times) and C_max AUC.

Farmakodinamika

When taken doses of 4-8 mg / day glucose level decreases gradually (not by gipoglikemiei). Lower bazalnogo level of glucose in plasma is the first week of therapy, the greatest impact is in 6-8 weeks. Clinically significant decreases bazalny and postprandialny glucose level and the level glikozilirovannogo hemoglobin.

Indications

Insulinnezawisimy diabetes (type II) : monotherapy with inefficiency diet and adequate physical activity or in combination with sulfonylureas derivatives and metforminom to better control fast.

Pregnancy and lactation

Contraindicated.

Contraindications

Hypersensitivity, severe heart failure (class III-IV in NYHA), pregnancy, breast-feeding, age and 18 years of age.

Side-Effects

Rarely, headache, infection with upper respiratory tract infections, a slight increase in body mass index, peripheral edema, anemia (low haemoglobin levels), giperholesterinemia.

Specific guidance

It should be borne in mind that in patients with инсулинрезистентност ью and anovulatorian Cycle predmenopauzne period (for instance, the syndrome polikistozhnykh ovaries) may resumption of ovulation and the emergence of pregnancy (due to increased sensitivity to insulino). In case of the symptoms of menstrual dysfunction among women in predmenopause, it is necessary to assess the potential risks and expected benefits from the treatment. Caution is needed in patients with severe renal insufficiency. Is not recommended in patients with moderate and severe violations of the liver.

Overdosing

Symptoms : Not Opisana.lechenie : if it is to symptomatic therapy. Haemodialysis ineffective.

Precautions

In joint admission in combination with other drugs gipoglikemicakimi the risk gipoglikemii.

Dosing and Administration

Inside, the initial dose of 4 mg / day in the reception 1-2; Through 6-8 weeks dose can be increased to 8 mg / sut.

Storage conditions

tabl.p.o. : When temperature is not above 25 ° C

Shelf life

tabl.p.o. : 2 grams.

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