ალიმენტური ტრაქტი და მეტაბოლიზმი
სისტემური გამოყენების ინფექციის საწინააღმდეგო
სისხლი და სისხლ-წარმომქმნელი ორგანოები
სამომავლოდ დაგეგმილი პროდუქტები
Film-coated tablets. Tablet contains atorvastatin (as calcium salt) 10, 20, 40
or 80 mg.
PHARMACODYNAMICS. Hypolipidemic agent. Atorvastatin is a selective competitive
inhibitor of HMG-CoA-reductase, an enzyme converting 3-hydroxy-3-methyl-glutaryl-
CoA into mevalonic acid which is a precursor of sterols, including cholesterol.
The drug causes a decrease in the level of total cholesterol, LDL,
apolipoprotein B and triglycerides by 34-50%, 30-46%, 41-61% and 14-33%,
accordingly; it increases the level of HDL-cholesterol and apolipoprotein A. It
does not have carcinogenic and mutagenic action. The therapeutic effect is
achieved in 2 weeks after the initiation of therapy, reaches a maximum in 4
weeks and remains stable during the whole period of treatment. PHARMACOKINETICS.
Atorvastatin has rapid oral absorption with an approximate time to Cmax of 1-2
hours. The absolute bioavailability is approximately 14%, and the systemic
availability for HMG-CoA-reductase inhibiting activity is approximately 30%.
Food slightly reduces the rate and extent of the drug absorption (by 25% and 9%,
accordingly), however, food does not affect the plasma LDL-cholesterol lowering
efficacy. Plasma protein binding is > 98%. Atorvastatin is primarily metabolized
in the liver by cytochrome P450 3A4 to form pharmacologically active metabolites.
It is eliminated with bile. An approximate elimination half-life is 14 hours.
Less than 2% is recovered in the urine. In kidney diseases dose adjustment is
not required. Plasma atorvastatin concentrations increase in patients with
alcohol-induced liver injuries.
- in combination with diet for lowering of increased total cholesterol, LDL-cholesterol,
apolipoprotein B and triglyceride levels, increasing HDL-cholesterol level in
patients with primary hypercholesterolemia (heterozygous familial or non-familial)
and mixed dyslipidemia;
- for the treatment of patients with increased serum triglyceride levels;
- in patients with dysbetalipoproteinemia who do not achieve proper effect with
- for lowering total cholesterol and LDL-cholesterol levels in patients with
homozygous familial hypercholesterolemia in combination with other therapeutic
- for lowering total cholesterol, LDL-cholesterol and apolipoprotein B at the
age of 10-17 years with heterozygous familial hypercholesterolemia;
- cardiovascular diseases in patients with risk factors, including those with
- hypersensitivity to the drug components;
- active liver diseases or increased activity of hepatic transaminases (threefold
exceeding normal limits) of unknown genesis;
- pregnancy and lactation period, absence of appropriate contraception.
The drug is generally well tolerated.
More frequent (1% and more): Insomnia, headache, asthenic syndrome; nausea,
diarrhea, abdominal pain, dyspepsia, flatulence, constipation; myalgia. Less
frequent (less than 1 %):
Nervous system: malaise, vertigo, amnesia, paresthesia, peripheral neuropathy.
Digestive system: vomiting, anorexia, hepatitis, pancreatitis, cholestatic
jaundice. Musculoskeletal system: backache, myotonia, myositis, myopathy,
Allergic reactions: urticaria, itching, skin rash, anaphylaxis, exudative
erythema. Hematopoietic system: thrombocytopenia.
Metabolic system: hypo- or hyperglycemia, increase in serum creatine
phosphokinase. Other: impotence, peripheral edema, body weight increase, chest
pain, secondary renal impairment, alopecia, tinnitus, fatigue.
DOSAGE AND ADMINISTRATION:
The drug is taken orally at any time of day with food or independently of food
intake. Hypercholesterolemia (heterozygous familial or non-familial) and mixed
dyslipidemia: the recommended initial dose is 10-20 mg once daily. Dosage range:
10-80 mg daily. The doses should be chosen in accordance with the main goals of
therapy and patient's response to treatment. Homozygous familial hyper-cholesterolemia:
daily dosages of 10-80 mg are administered. The initial dose in the prevention
of heart ischemic disease for adults is 10 mg once daily. Heterozygous familial
hypercholesterolemia in childhood: the recommended initial dose is 10 mg once
daily; the maximum recommended dose is 20 mg once daily.
10 tablets in a blister.
3 blisters in a carton box with enclosed leaflet.