Zetia
Zetia
Zetia (Ezetimibe)Pharmacological action
Hypolipidemichesky preparation. Reduces cholesterol absorption in an intestine, including cholesterol of vegetative Adepses.
At entering in a thin intestine Zetia (Ezetimibe) is localised in a brush border of a small bowel and interferes with a cholesterol absorption (Xc), that leads to reduction of entering Xc from an intestine in a liver at the expense of what stocks Xc in a liver decrease and deducing Xc from blood is enlarged. Zetia (Ezetimibe) does not raise an egestion of cholic acids (unlike the preparations binding cholic acids) and does not inhibit synthesis Xc in a liver. In fortnight clinical research in which 18 patients with a hypercholesterinemia have been included.
Zetia inhibited an absorption of 14C-cholesterol and did not render influence on an absorption of triglycerides, fat acids, cholic acids, progesterone, liposoluble vitamins A and D.
At the expense of depression of absorption Xc in an intestine Zetia reduces entering Xc in a liver. Zetia reduce synthesis Xc in a liver. At the expense of two various mechanisms of action preparations of these two classes at joint appointment provide additional depression of level Xc.
Indications
- A primary hypercholesterinemia (Zetia prescribe in a combination with GMG-KOA-REDUCTASE inhibitors/statinami/or as monotherapy in addition to a diet for depression of the raised level of the general Xc, Hs-LpNp, apolipoprotein In and triglycerides, and also for rising of level Hs-LpVp at patients with primary / a heterozygotic family and single / hypercholesterinemia);
- A homozygous family hypercholesterinemia;
Dosage regimen
A preparation accept inside at any time, irrespective of food intake.
Recommended Zetia dose as monotherapy makes 10 mg of 1 times/days
With disturbances of function of kidneys of selection of a dose it is not required from elderly patients and patients.
Selection of a dose for patients with easy hepatic insufficiency (5-6 points on a scale I Chajld-drink) it is not required.
Side effect
In clinical researches by duration from 8 till 14 weeks in which 3366 patients have been included, Zetia, 10 mg prescribed in a daily dose as monotherapy, has shown good shipping. Undesirable effects were easy and transient;
The undesirable reactions taped in 1-10 % of cases at Zetia reception in the form of monotherapy (n=1691) .
At Zetia monotherapy: a headache, an abdominal pain, a diarrhoeia.
At combined Zetia therapy: a headache, fatigability, an abdominal pain, a constipation, a diarrhoeia, an abdominal distention, a nausea, rising of activity of nuclear heating plant.
At Zetia application in clinical practice following undesirable reactions became perceptible: a Quincke's disease, a dermal eruption, hepatic enzymes, hepatitises, a thrombocytopenia, a pancreatitis, a nausea; very seldom - a myopathy.
Contraindications
- A hypersensibility to preparation components;
- Moderated (7-9 points on a scale I Chajld-drink) and serious (more than 9 points on a scale I Chajld-drink) degree of hepatic insufficiency;
With care it is necessary to prescribe a preparation to the patients receiving cyclosporine.
Pregnancy and lactemia
In need of preparation use it is necessary to solve a question on the termination of thoracal feeding.
Special indicatings
In need of simultaneous Zetia appointment with cyclosporine it is necessary to supervise concentration of the last.
In clinical researches frequency of occurrence of a myopathy , bound to Zetia application, did not exceed that in comparison with corresponding control group.
Clinical experience of Zetia application at children and teenagers at the age of 9-17 years is limited, therefore it is not recommended to prescribe a preparation of the given category of patients.
Overdosage
It was informed on several cases of an overdosage, the majority from which was not accompanied by occurrence of the undesirable serious phenomena.
In clinical researches in which Zetia was prescribed to 15 healthy volunteers in a dose of 50 mg/sut within 14 days, in other - with a primary hypercholesterinemia in a dose of 40 mg/sut within 56 days, good shipping has been shown 18 patients.
In case of an overdosage spend supporting and symptomatic therapy.
Conditions and periods of storage
B.Preparat's list should be stored in a place inaccessible to children, at temperature not above 30 C. The Period of validity - 2 years.
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