Lipitor
Lipitor
Lipitor (Atorvastatin)Pharmacological action
Hypolipidemichesky preparation. Lipitor - a selective competitive inhibitor of the GMG-KOA-REDUCTASE - the key enzyme transforming 3-gidroksi-3-metilgljutaril-KoA in acid - the precursor of steroids, including cholesterol.
At patients with a homozygous and heterozygotic family hypercholesterinemia, single forms of a hypercholesterinemia reduces level of the general cholesterol (Xc), cholesterol of lipoproteins of low density and apolipoprotein In, and also the maintenance of cholesterol of lipoproteins of very low density and triglycerides, causes unstable rising of level of cholesterol of lipoproteins of high density.
In a liver triglycerides and cholesterol join in structure of lipoproteins of very low density, arrive in plasma and are transported in peripheric tissues.
Lipitor (10 mg/24h) significantly reduce frequency of development of following complications: an ischemic heart disease (with a lethal outcome + an infarct without a lethal outcome) - on 36 %, cardiovascular diseases and application of procedures of a revascularization - on 20 %, an ischemic heart disease - on 29 %, a stroke (including with a lethal outcome) - on 26 %.
Significant depression of the general mortality and mortality from cardiovascular complications at Lipitor application is not taped, the tendency of depression of a mortality however was observed.
Indications
- In a combination to a diet for depression of the raised level of the general cholesterol, apolipoprotein In and triglycerides and rising of level Hs-LpVp at patients with a primary hypercholesterinemia (a heterozygotic family and single hypercholesterinemia) and the admixed lipidemia at which the dietetics does not give adequate effect;
- In a combination to a diet for treatment of patients with the raised serumal levels of triglycerides;
- For depression of levels of the general cholesterol at patients with a homozygous family hypercholesterinemia at insufficient efficiency of a dietetics and other not pharmacological methods of treatment;
- For depression of risk of lethal outcomes of an ischemic heart disease and risk of development of a myocardial infarction, a stenocardia, a stroke and for reduction of necessity of carrying out of procedures of a revascularization patients with cardiovascular diseases and also in case these diseases are not taped, but have not less than three risk factors of development of an ischemic heart disease, such as age more than 55 years, smoking, an arterial hypertensia, low concentration in blood plasma Hs-LpVp, cases of a forwardness of an ischemic heart disease for relatives.
Dosage regimen
Before the beginning of Lipitor treatment is necessary to try to achieve the control of a hypercholesterinemia by means of a diet, physical exercises and depression of mass of a body at sick of adiposity, and also basic disease treatments.
At appointment of a preparation it is necessary for patient to recommend standard a diet which it should observe during treatment.
The preparation can be accepted at any time, irrespective of food intake. In the beginning of treatment and-or during rising of Lipitor dose is necessary to supervise each 2-4 weeks levels of lipids in plasma and in appropriate way to correct a dose.
At a primary hypercholesterinemia and the combined (admixed) lipidemia it is possible to achieve from the majority of patients of necessary effect at Lipitor application in a dose of 1 times/days of 10 mg Therapeutic action it is shown within 2 weeks and usually reaches a maximum within 4 weeks. At long treatment the effect remains.
Side effect
Lipitor is usually well transferred. Side-effects, as a rule, easy and transient.
The basic undesirable effects which became perceptible at Lipitor treatment:
From party TSNS and peripheric nervous system: a sleeplessness, a malaise, giddiness, an amnesia, a headache, an asthenic syndrome, paresthesias, a peripheric neuropathy, a hypesthesia.
From the alimentary system: vomiting, an anorexia, an abdominal pain, a dyspepsia, a nausea, appetite depression, a meteorism, a constipation, a diarrhoeia, a hepatitis, a pancreatitis, a cholestatic icterus.
From osteomuscular system: a dorsodynia, cramps of muscles, a myositis, a myopathy, arthralgias.
Allergic reactions: an urticaria, an itch, a dermal eruption, anaphylactic reactions, a violent eruption, a polymorphic exudative erythema, a toxic epidermal necrolysis (Lyell's disease), a malignant exudative erythema (Stevens-Johnson's syndrome).
From a metabolism: a hypoglycaemia, a hyperglycaemia.
From hemopoiesis system: a thrombocytopenia.
The other: an impotency, peripheric edemas, augmentation of mass of a body, a stethalgia, secondary renal insufficiency, a fervescence, an alopecia, a sonitus.
Contraindications
- Active diseases of a liver or rising of serumal activity of transaminases (more than in 3 times in comparison with the top border of norm) an obscure genesis;
- Women of the genesial age, not using adequate methods of contraception;
- Pregnancy;
- A lactemia (thoracal feeding);
- A hypersensibility to preparation components;
- At children and teenagers about 18 years efficiency and Lipitor safety are elderly are not established.
C care it is necessary to apply at the patients abusing alcohol and-or having disease of a liver (in the anamnesis).
Pregnancy and lactemia
Lipitor is contraindicative to application at pregnancy and in a lactemia (thoracal feeding).
Women of genesial age during treatment should use adequate methods of contraception. Lipitor is possible to prescribe to women of genesial age only in the event that probability of pregnancy at them very low, and the patient is informed on possible risk for a foetus during treatment.
Special indicatings
Proof rising of serumal level of hepatic transaminases (more than in 3 times in comparison with the top border of norm) was observed at 0.7 % of the patients Lipitor receiving in clinical researches. Frequency of similar changes at preparation application in doses 10, 20, 40 and 80 mg made 0.2 %, 0.2 %, 0.6 % and 2.3 % accordingly. Rising of activity of hepatic transaminases usually was not accompanied by an icterus or other clinical implications. At Lipitor dose decline, time or full cancellation of a preparation activity of hepatic transaminases came back to initial level. The majority of patients continued Lipitor reception in the lowered dose without any consequences.
Prior to the beginning, in 6 weeks and 12 weeks after the beginning of application of a preparation or after dose augmentation, and also during all course of treatment it is necessary to supervise indicators of function of a liver. Liver function should be investigated also at occurrence of clinical signs of a lesion of a liver. In case of rising of level of hepatic transaminases their activity should be supervised until it is not normalised.
Lipitor therapy should be stopped temporarily or completely to cancel at occurrence of signs of a possible myopathy.
Patients are necessary for warning that they should address immediately to the doctor at occurrence of inexplicable pains or delicacy in muscles, especially if they are accompanied by a malaise or a fever.
Use in pediatrics
Efficiency and safety of Lipitor application at children and teenagers is elderly till 18 years are not established.
Influence on ability to driving of motor transport and to management of mechanisms
Overdosage
Treatment: if necessary spend symptomatic therapy. Considering Lipitor active linkage with fibers of plasma. The specific antidote is not present.
Medicinal interaction
The risk of a myopathy during treatment by other preparations of this class raises at simultaneous application of cyclosporine, erythromycin, and nicotinic acid.
Conditions and periods of storage
B.Preparat's list should be stored at temperature not above 25 C, in a place inaccessible to children. A period of validity - 3 years.
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