Akorta

Akorta – the medicine having hypolipidemic effect.

Form of release and structure

Akorta is let out in the form of tablets, film coated: from pink till light pink color, round, biconvex; on a break – from cream till white color (on 10 pieces in blister strip packagings, in a cardboard pack 1-3 packagings).

Structure of 1 tablet:

• Active ingredient: розувастатин – 10 or 20 mg (розувастатин calcium – 10,4 or 20,8 mg);
• Auxiliary components (10/20 mg respectively): monohydrate of lactose (milk sugar) – 89,5/179 mg; microcrystallic cellulose – 29,82/59,64 mg; calcium hydrophosphate (E341) – 10,9/21,8 mg; кросповидон – 7,5/15 mg; magnesium stearate – 1,88/3,76 mg;
• Cover (10/20 mg respectively): Opadry II 30K240001 pink (monohydrate of lactose (milk sugar) – 2,4/4,8 mg; a gidroksipropilmetiltsellyuloz (gipromelloz) – 1,68/3,36 mg; titanium dioxide – 1,413/2,826 mg; triacetin (glyceryl triacetate) – 0,48/0,96 mg; dye red iron oxide – 0,027/0,054 mg) – 6/12 mg.

Indications to use

• Atherosclerosis (for the purpose of progressing delay) – as an additional tool to a diet at patients to whom therapy for reduction of concentration of the general cholesterol (XC) and cholesterol of lipoproteins of the low density (HS-LPNP) is shown;
• The main cardiovascular complications (primary prevention of a heart attack, stroke, arterial revascularization) at adult patients without clinical signs of coronary heart disease, but with the increased risk of its development (age at men – of 50 years, at women – of 60 years, the increased concentration of S-reactive protein (≥2 mg/l) with, at least, one of risk factors – arterial hypertension, low concentration of HS-LPVP, instructions in the family anamnesis of the early beginning of coronary heart disease);
• Family homozygous hypercholesterolemia – as an additional tool to a diet and other lipidosnizhayushchy therapy (for example, LPNP-aferez) or in cases if this therapy is insufficiently effective;
• Gipertriglitseridemiya (type IV across Fredrikson) – as an additional tool to a diet;
• The mixed hypercholesterolemia (lIb type) or primary hypercholesterolemia across Fredrikson (the IIa type, including a family heterozygous hypercholesterolemia) – as an additional tool to a diet in cases if the diet in combination with other non-drug methods of therapy (for example, weight reduction, physical exercises) is insufficiently effective.

Contraindications

Daily dose of 10 and 20 mg
Absolute:

• Predisposition to development of miotoksichesky complications;
• Myopathy;
• Renal failures of heavy degree (at clearance of creatinine less than 30 ml/min.);
• Liver disease in an active phase, including permanent increase in activity of hepatic transaminases, and also any increase in their activity in blood serum exceeding the upper bound of norm it is more, than by 3 times;
• Lactose intolerance, deficit of lactase or glyukozo-galaktozny malabsorption (lactose is Akorta's part);
• The combined use with cyclosporine;
• Use for women at reproductive age who do not use reliable contraceptive methods;
• Pregnancy and period of a lactation;
• Age up to 18 years (the profile of safety is not studied);
• Hypersensitivity to drug components.

Relative (Akort is appointed with care with risk of development of a myopathy / рабдомиолиза – the following diseases / states):

• Renal failure;
• Liver diseases in the anamnesis;
• Injuries;
• Hereditary muscular diseases in the anamnesis (personal or family) and the previous anamnesis of muscular toxicity at use of fibrat or other inhibitors of GMG-KOA-reduktazy;
• States at which the increased plasma concentration of a rozuvastatin is noted;
• Hypothyroidism;
• Extensive surgical interventions;
• Alcohol abuse;
• Sepsis;
• Arterial hypotension;
• Uncontrollable epilepsy;
• Metabolic, water and electrolytic or endocrine disturbances in a heavy current;
• The combined use from fibrata;
• Belonging to Mongoloid race;
• The age is more senior than 65 years.

Daily dose of 40 mg (in addition to above-mentioned contraindications)
Absolute:

• Muscular diseases in the anamnesis (personal or family);
• Renal failure of moderate severity (at clearance of creatinine less than 60 ml/min.);
• Alcohol abuse;
• Hypothyroidism;
• Miotoksichnost against the background of reception of other inhibitors of GMG-KOA-reduktazy or fibrat in the anamnesis;
• States at which the increased plasma concentration of a rozuvastatin is noted;
• The combined use from fibrata;
• Belonging to Mongoloid race.

Relative (Akort is appointed with care in the presence of the following diseases / states):

• Injuries;
• Liver diseases in the anamnesis;
• Renal failure of easy severity (at clearance of creatinine more than 60 ml/min.);
• Arterial hypotension;
• Sepsis;
• Extensive surgical interventions;
• Metabolic, water and electrolytic or endocrine disturbances in a heavy current or uncontrollable convulsive attacks;
• The age is more senior than 65 years.

Route of administration and dosage

Akort's pill is taken inside, regardless of meal, washing down with water. Time of day does not accord administration of drug on its efficiency of influence. It is not necessary to crush and chew tablets.

Before Akorta's appointment of the patient has to begin observance of a standard hypolipidemic diet which needs to adhere throughout all medical course.

The doctor selects a dose of a rozuvastatin individually. It is defined by the purpose of therapy and the therapeutic answer, and also has to correspond to the modern standard recommendations about target concentration of lipids.

If there are no other instructions of the doctor, to Akort accept in an initial dose 10 mg once a day. When determining a dose it is necessary to consider individual values of concentration of cholesterol, and also probability of development of cardiovascular complications and side reactions.

In a month if necessary increase in a dose is possible twice.

Further increase in a daily dose (to 40 mg) is shown to patients with a hypercholesterolemia in heavy degree and with high risk of cardiovascular complications (in particular the patient with a family hypercholesterolemia) at which the desirable result of therapy was not achieved at reception of lower doses. Such patients have to be under medical observation, also they should exercise control of indicators of function of kidneys.

It is not recommended to patients who did not see a doctor earlier to appoint Akorta in a dose of 40 mg.

In 2-4 weeks from the moment of the beginning of therapy, and also at increase in a dose it is necessary to carry out control of indicators of lipidic exchange. By its results carrying out selection of a dose can be shown.

Correction of the scheme of use of drug is not required to elderly patients.

Increase in system concentration of a rozuvastatin was noted among Chinese and Japanese that needs to be considered at purpose of therapy.

The heavy renal failure is a contraindication to Akorta's appointment in any doses, moderate – in a daily dose of 40 mg.

For patients, being carriers of genotypes s.521ss and s.421aa, the daily dose of Akorta should not be higher than 20 mg.

At patients with a liver failure (more than 9 points on a scale of Chayld-Pyyu) experience of use of drug is absent. A contraindication to performing therapy are liver diseases in an active phase.

It is not recommended to appoint the maximum daily dose of 40 mg in the presence of factors which can indicate existence at the patient of predisposition to development of a myopathy.

The risk of emergence of a myopathy (including рабдомиолиз) grows with increase in plasma concentration of a rozuvastatin, including because of the combined Akorta's use with such medicines as cyclosporine, some inhibitors of HIV proteases (including the combined use of a ritonavir with atazanaviry, tipranaviry and/or lopinaviry). If there is such opportunity, it is necessary to appoint alternative treatment. In need of simultaneous use of Akorta with these medicines it is necessary to correlate the expected advantage to possible risk.

Side effects

Scale of gradation of the registered side reactions: often (> 1/100, <1/10); infrequently (> 1/1000, <1/100); seldom (> 1/10000 <1/1000); very seldom (<1/10000); with an unknown frequency (at impossibility to estimate it according to the available data).

Side effects owing to therapy rozuvastatiny usually dozozavisima are also noted with the following frequency:

• Central and peripheral nervous system: often – dizziness, a headache, an asthenic syndrome; infrequently – neuralgia, uneasiness, paresthesias; very seldom – amnesia, polyneuropathy;
• Alimentary system: often – nausea, a lock, abdominal pains; seldom – pancreatitis, reversible passing dozozavisimy increase in activity of hepatic transaminases; very seldom – a gastroenteritis, dispepsichesky frustration (including diarrhea, a meteorism, vomiting), jaundice, hepatitis;
• Respiratory system: often – pharyngitis; infrequently – sinusitis, rhinitis, bronchial asthma, pneumonia, bronchitis; with an unknown frequency – cough, диспноэ;
• Cardiovascular system: infrequently – stenocardia, increase in arterial pressure, a heart consciousness, vazodilatation symptoms (including a dermahemia);
• Skeletal and muscular system: often – a mialgiya; infrequently – arthritis, a muscle hyper tone, dorsodynias, a pathological fracture of bones of extremities (without damages); seldom – a myopathy, рабдомиолиз (along with a renal failure, at reception in a dose of 40 mg); very seldom – an arthralgia; with an unknown frequency – the tendopatiya sometimes proceeding with complications in the form of gaps; the immunomediated necrotic myopathy;
• Urinary system: a proteinuria (as a rule, it decreases or disappears in the course of treatment; acute or progressing of the existing disease of kidneys it does not mean emergence); very seldom – a hamaturia;
• Allergic reactions: infrequently – a skin itch and rash, a small tortoiseshell; seldom – a Quincke's disease; with an unknown frequency – Stephens-Johnson's syndrome;
• Laboratory indicators: increase in plasma concentration of bilirubin, glucose, increase in activity of an alkaline phosphatase, gamma глутамилтранспептидазы; at insignificant number of patients – increase in activity of a kreatinfosfokinaza (dozozavisimy, insignificant, asymptomatic and temporary), in case of increase in indicators more than by 5 times in comparison with the upper bound of norm, to Akort is temporarily cancelled;
• Others: often – a diabetes mellitus 2 types; infrequently – pains in the area to a thorax, a grippopodobny syndrome, anemia, ecchymomas, periodontal abscess; seldom – thrombocytopenia; with an unknown frequency – a gynecomastia, peripheral hypostases.

Messages on development of the following disturbances at therapy some statines were: the sleep disorders including dreadful dreams and sleeplessness; depression; sexual dysfunction. It was reported about isolated cases of developing of an intersticial disease of lungs, in particular at long use of drugs.

Special instructions

Reception of high doses of Akorta, especially 40 mg, can lead to development of a proteinuria, preferential canalicular origin, but most often the disease has periodic or short-term character (development acute or progressing of the existing disease of kidneys does not mean it). During treatment at the patients accepting drug in a dose of 40 mg it is recommended to exercise control of indicators of function of kidneys.

It is not necessary to define activity of a kreatinfosfokinaza after the raised exercise stresses or in the presence of other probable causes of increase in its activity (incorrect interpretation of the received results is possible). If this indicator exceeds the upper bound of norm by 5 times, in 5-7 days it is necessary to take repeated measurement. If the repeated test confirms the previous indicator, it is not necessary to begin therapy.

With risk factors of a rabdomioliz it is necessary to estimate a ratio of advantage of therapy with probability of a disease and throughout all course of treatment to carry out clinical observation.

In cases of unexpected emergence of muscular weakness and pains or spasms, especially along with fever and an indisposition, it is necessary to consult with the specialist. Such patients need to carry out monitoring of level of activity of a kreatinfosfokinaza. Treatment is cancelled if activity of a kreatinfosfokinaza is increased more than by 5 times in comparison with the upper bound of norm, or in cases when muscular symptoms are sharply expressed and daily cause discomfort. After improvement of a state therapy can be resumed.

Very exceptional cases of development of the immunomediated necrotizing myopathy with clinical manifestations are celebrated (are shown as resistant weakness of proximal muscles and increase in activity of a kreatinfosfokinaza in blood serum). In these cases additional researches of nervous and muscular system, serological researches, and also performing therapy by immunodepressive means can be required.

Simultaneous use of Akorta with gemfibrozily is not recommended (because of high risk of development of a myopathy). It is not necessary to appoint treatment to patients with the acute, serious illnesses allowing to assume a myopathy or with possible development of a secondary renal failure (water and electrolytic disturbances, injuries, arterial hypertension, sepsis, surgical interventions, spasms, a metabolic syndrome, endocrine disturbances).

Care is demanded by Akorta's use for the patients abusing alcohol and in the presence of instructions in the anamnesis on liver diseases.

In 2-4 weeks from the moment of an initiation of treatment and/or at increase in a dose of Akorta it is necessary to control indicators of lipidic exchange (correction of the mode of dosing can be required).

It is recommended to carry out definition of activity of hepatic transaminases prior to therapy and 3 months later from the moment of an initiation of treatment. At exceeding of the upper bound of norm by 3 times reduce Akorta's dose or cancel therapy.

At patients with concentration of glucose of 5,6-6,9 mmol/l use of a rozuvastatin is associated with the increased risk of development of a diabetes mellitus 2 types.

Medicinal interaction

At the combined use of Akorta with some drugs / substances the following effects can be observed:

• Inhibitors of transport proteins: increase in plasma concentration of a rozuvastatin and risk of development of a myopathy;
• Cyclosporine, gemfibrozit: strengthening of effect of a rozuvastatin;
• Gemfibrozil, фенофибрат, and also other fibrata and lipidosnizhayushchy doses of niacin (more than 1 g a day): increase in risk of development of a myopathy (an admissible dose of Akorta in combination with gemfibrozily – 10 mg; reception of 40 mg of Akorta in a combination from fibrata is contraindicated);
• HIV protease inhibitors: significant increase in exposure of a rozuvastatin (the combination is not recommended);
• Antacids with the maintenance of ions of magnesium and aluminum: decrease in plasma concentration of a rozuvastatin (it is necessary to observe an interval not less than 2 hours between reception of these drugs);
• Erythromycin: decrease in effect of a rozuvastatin (because of strengthening of motility of digestive tract);
• Эзетимиб: increase in total concentration of Akorta at patients with a hypercholesterolemia, is not excluded development of the undesirable phenomena;
• Antagonists of vitamin K: increase in a prothrombin time;
• Oral contraceptives: strengthening of their effects.

Akorta's dose needs to be adjusted in need of the combined use with the following drugs (because of increase in exposure of a rozuvastatin): фенофибрат, cyclosporine, атазанавир, Silymarinum, лопинавир, gemfibrozit, элтромбопаг, дарунавир, ритонавир, типранавир, алеглитазар, фосампренавир, дронедарон, итроконазол, эзетимиб, Rifampinum, кетоконазол, флуконазол, erythromycin, байкалин. The maximum daily dose needs to be adjusted so that the expected exposure of a rozuvastatin was not higher that for the dose of 40 mg accepted as monotherapy.

Terms and storage conditions

To store in the place, unavailable to children, at a temperature up to 30 °C.

Period of validity – 2 years.