Crestor
Crestor
Crestor (Rosuvastatin)Pharmacological action
Selective competitive inhibitor of the GMG-KOA-REDUCTASE - the enzyme transforming 3-gidroksi-3-metilglutarilkoenzim A , the precursor of cholesterol (Xc).
The therapeutic effect is shown during 1 week. After the beginning of therapy and in 2 weeks of treatment makes 90 % from the greatest possible effect which is usually reached by 4 week and after that remains to constants.
Crestor is effective at adult patients with a hypercholesterinemia with or without dependence from race, a floor or age, including at patients with a diabetes and with a family hypercholesterinemia.
At 80 % of patients with hypercholesterinemia IIa and IIb type (average initial level Hs-LpNp about 4.8 mmol/l) against preparation reception in a dose of 10 mg level Hs-LpNp reaches value less then 3 mmol/l.
At patients with a heterozygotic family hypercholesterinemia at Crestor application in a dose of 20-80 mg positive dynamics of a lipide profile (research with participation of 435 patients) becomes perceptible. After titration to a daily dose of 40 mg (12 weeks of therapy), depression of level Hs-LpNp on 53 % becomes perceptible.
At patients with a homozygous family hypercholesterinemia at Crestor application in a dose of 20 mg and 40 mg average depression of level Hs-LpNp makes 22 %.
Indications
- A hypercholesterinemia (type IIa, including a family heterozygotic hypercholesterinemia) or the admixed hypercholesterinemia (type IIb) as addition to a diet, when a diet and other not medicamental methods of treatment (for example, physical exercises, depression of mass of a body) appear insufficient;
Dosage regimen
The preparation can be accepted at any time irrespective of food intake. Tablets swallow entirely, not chewing and not crushing, washing down with water.
The recommended initial dose makes 10 mg of 1 times/days In the majority cases therapeutic effect is reached at preparation reception in a dose of 10mg. If necessary the dose can be raised to 20 mg in 4 weeks. Rising of a dose to 40 mg probably only at patients with a serious hypercholesterinemia and high risk of cardiovascular complications (especially at patients with a family hypercholesterinemia) in cases when the necessary result is not reached at preparation reception in a dose of 20 mg and when treatment will be spent under the control of the doctor.
Dose correction is not required from persons of advanced age.
With renal insufficiency easy or moderate severity level dose correction is not required from patients.
Crestor is contraindicative to patients with the expressed renal insufficiency.
Experience of application of a preparation at patients with hepatic insufficiency with a point above 9 on a scale I Chajld-drink is absent.
Crestor is contraindicative to patients with liver diseases in an active phase.
Efficiency and safety at children is not established. Experience of application of a preparation in pediatric practice is limited by a small amount of children (from 8 years and is more senior) with a family homozygous hypercholesterinemia. Now it is not recommended to apply Crestor at children.
Side effect
From party TSNS: often - a headache, giddiness.
From osteomuscular system: seldom - a myopathy. In all cases at the therapy termination there came improvement.
The other: often - an asthenic syndrome.
The by-effects observed at Crestor reception, are usually expressed slightly and pass independently.
Contraindications
- Liver diseases in an active phase;
- The expressed disturbances of function of kidneys;
- A myopathy;
- Simultaneous reception of cyclosporine;
- Pregnancy;
- A lactemia (thoracal feeding);
- Children's and teenage age till 18 years (since efficiency and safety is not established);
- A hypersensibility to preparation components.
Preparation do not prescribe to the women of genesial age who are not using adequate methods of contraception.
Pregnancy and lactemia
Crestor is contraindicative at pregnancy and in a lactemia. At occurrence of pregnancy in the course of therapy preparation reception should be stopped immediately.
Women of genesial age should apply adequate methods of contraception. As Xc and products of its biosynthesis are important for a fetation, the potential risk of inhibition of the GMG-KOA-REDUCTASE exceeds advantage of preparation application.
Special indicatings
At Crestor application in a dose of 40 mg it is recommended to supervise indicators of function of kidneys.
It is necessary to inform the patient on necessity of the immediate report to the doctor about cases of unexpected occurrence of muscular pains, muscular delicacy or spastic strictures, especially in a combination to a malaise and a fever.
It is noted signs of augmentation of toxic influence on a sceletal musculation at Crestor application as a part of the combined therapy. It was informed on augmentation of number of cases of a myositis and a myopathy at the patients accepting other inhibitors of the GMG-KOA-REDUCTASE in a combination to derivatives of fibrinous acid, cyclosporine, nicotinic acid. The parity of risk and possible advantage Should be carefully weighed at joint Crestor application.
It is recommended to spend definition of indicators of function of a liver prior to the beginning of therapy and through 3 months after the therapy beginning. At patients with a hypercholesterinemia owing to a hypothyrosis or a nephrotic syndrome, therapy of basic diseases should be spent prior to the beginning of Crestor treatment.
Influence on ability to driving of motor transport and to management of mechanisms
At employment by potentially dangerous kinds of activity patients should consider, that during therapy there can be a giddiness.
Overdosage
Treatment: the specific antidote is not present. It is improbable, that the hemodialysis will be effective.
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 - 3 years.
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