Simekar 28's 10 mg film-coated tablets

The instruction for use
medicine for experts

Симекар® 10,
Симекар® 20 Симекар® 40, Симекар® 80


Trade name



Симекар® 10 Симекар® 20 Симекар® 40 Симекар® 80

International unlicensed


name Simvastatin Lekarstvennaya
the Tablet form, film coated, 10 mg, 20 mg, 40 mg, 80 mg

Structure
One tablet contains
active agent - simvastatin 10 mg, 20 mg, 40 mg, 80 mg,
excipients: lactoses monohydrate, butylhydroxyanisole, ascorbic acid, anhydrous citric acid, sodium of a kroskarmelloz, cellulose microcrystalline PH 102, magnesium stearate, starch prezhelatinizirovanny,
structure of a cover: HPMC 5 cP-Methocel E5-LV, titan dioxide E 171, HPC-Klucel LF, E 122 carmoisin, ferrous oxide yellow 510P E 172, FD&C yellow #6/сансет yellow FCF AL E 110, FD&C Blue#2 E 133/indigo carmine E 132 aluminum.

The description
of the Tablet, film coated, oblong shape, with a biconvex surface, with risky and the inscription 10 mg, located on both sides from risks, on one party and NOBEL - on other party, on a break two layers - a kernel of white color, a cover – pink are visible (to a dosage of 10 mg).
Tablets, film coated, oblong shape, with a biconvex surface, with risky on one party, on a break are visible two layers - a kernel of white color, a cover – pink (to dosages of 20, 40 and 80 mg).

Pharmacotherapeutic group
the Drugs reducing the content of cholesterol and triglycerides in blood serum. Reductase inhibitors
the Code of automatic telephone exchange C10AA01

the Pharmacological

Pharmacokinetics Later properties of oral administration the maximum level of drug in plasma is observed in 1.3-2.4 hours and decreases to 10% in 12 hours. Meal does not influence the plasma level of a simvastatin. Simvastatin is easily hydrolyzed in an active metabolite - hydroxyacid simvastatin. Simvastatin is metabolized in a liver, with the subsequent excretion with bile. Linking with proteins of plasma of a simvastatin and its hydroxyacid metabolite about 95%. It was not established whether passes simvastatin through hematoencephalic and placentary barriers. The main active metabolites of a simvastatin are: hydroxyacid, 6 hydroxies, 6 hydroxymethyl and 6-ekzometilen derivatives.
It is generally removed with a stake (60%) in the form of metabolites. About 10-15% are removed by kidneys in an inactive form.
Pharmacodynamics
Hypolipidemic drug. It is synthetic received from products of fermentation Aspergillus terreus and is an inactive lactone. After absorption, it is hydrolyzed in a hydroxyacid metabolite. The active metabolite inhibits 3-hydroksi-3-metil-glyutaril-KoA-reduktazu (GMG – KoA-reductase), the enzyme catalyzing initial reaction of formation of the mevalonat from GMG – KoA. As transformation of GMG – KoA in mevalonat represents an early stage of synthesis of cholesterol, use of a simvastatin does not cause accumulation in an organism of potentially toxic sterols. GMG-KoA it is easily metabolized to atsetil-KoA which participates in many processes of synthesis in an organism. Simvastatin reduces the content of triglycerides (TG), lipoproteids of the low density (LDL), lipoproteids of very low density (LPONP) and the general cholesterol in plasma (in cases of heterozygous family and single forms of a hypercholesterolemia, at the mixed lipidemia when the increased content of cholesterol is risk factor). Increases the maintenance of lipoproteids of the high density (LPVP) and LDL/LPVP and the general cholesterol / LPVP reduces a ratio.


The beginning of manifestation of effect – in 2 weeks from the beginning of reception, the maximum therapeutic effect is reached in 4-6 weeks. Action remains at treatment continuation, at the therapy termination the content of cholesterol returns to initial level (prior to treatment).

Indications
- primary hypercholesterolemia of IIa and IIv of type (at inefficiency of a dietotherapy at patients with the increased risk of developing of atherosclerosis)
- the combined hypercholesterolemia and a giperglitseridemiya, the giperlipoproteinemiya which is not giving in to correction by a special diet and physical activity
- prevention of a myocardial infarction, stroke and passing disturbances of cerebral circulation
- primary hypercholesterolemia (heterozygous family and single)
- the mixed dislipidemiya (type Frederiksona IIA i IIB)
- a giperglitseridemiya (Frederikson's lipidemia type IV)
- primary disbetalipoproteinemiya (Frederikson's lipidemia type III)
- a homozygous family hypercholesterolemia
- additional therapy to the main anti-lipidic treatment (for example, aferez LDL) or at impossibility of performing such treatment

the Route of administration and doses
of the Tablet should be accepted inside, once, in the evening.
To patients to and during treatment by Simekar the diet with restriction of saturated fats and cholesterol is appointed.
The dosage has to be individual, depending on the LDL level and reaction of the patient to the carried-out treatment.
The recommended dose of 5-80 mg/days on one reception, in the evening. Correction of a dose has to be made in 4 weeks.
The homozygous family hypercholesterolemia
the Recommended drug dose to patients with a homozygous family hypercholesterolemia makes 40-80 mg/day in the evening. Simvastatin is used as additional therapy to the basic a lipid to the reducing treatment (for example, aferez by LDL), or at impossibility of performing such treatment.
Chronic kidney disease
the Recommended initial dose - 5 mg, the maximum daily dose – 10 mg.

Side effects
- abdominal pain, a constipation or diarrhea, dyspepsia, a meteorism, nausea, vomiting,
hepatitis, jaundice, increase in activity of hepatic transaminases,
an alkaline phosphokinase and kreatinfosfokinaza, it is rare - acute pancreatitis
- an asthenia, a headache, dizziness, insomnia
- anemia, heartbeat
- spasms, paresthesias, vagueness of sight, disturbance of flavoring
feelings
- a myopathy, myalgia, muscle weakness, is rare - a rhabdomyolysis
- a Quincke's disease, a small tortoiseshell, a photosensitization, fever,
a dermahemia, inflows, an asthma, increase SOE, thrombocytopenia,
a leukopenia, rheumatic polymyalgia, a vasculitis, arthritis
- skin rash, an itching, an alopecia
- an acute renal failure
-

Contraindication impotence
- hypersensitivity to any component of drug and other
drugs of a statinovy row (reductase GMG-KoA-inhibitors)
- a liver failure
- pregnancy
- the lactation period

Medicinal interactions
At simultaneous use of drug with:
- cyclosporine, itrakonazoly, ketokonazoly, gemfibrozily, niacin, erythromycin, klaritromitsiny, HIV inhibitors of proteases, nefazodony, fibrata and Niacinum and a large number of grapefruit juice, the risk of a myopathy due to decrease in elimination of a simvastatin
- antipyrine increases, simvastatin does not influence antipyrine pharmacokinetics
- Amiodaronum or verapamil, risk of development of a myopathy and a rhabdomyolysis
increases
- propranolol, the maximum concentration
of the general and active inhibitors
- digoxin considerably decreases, concentration of digoxin in plasma
- warfarin increases, simvastatin strengthens effect of warfarin and increases
risk of developing of bleedings
- Colestyraminum and kolestipoly, the bioavailability of a simvastatin decreases therefore use of a simvastatin is possible in 4 hours after intake of the specified drugs, at the same time the additive effect is noted.
The dosage at use of cyclosporine, Amiodaronum, verapamil
Simekar's Dose at simultaneous use with cyclosporine makes 5 mg and should not exceed 10 mg/day, at simultaneous use with Amiodaronum the dose should not exceed 20 mg/day.
Together with lipidsnizhayushchy therapy
At simultaneous use with fibrata or Niacinum, the dose of a simvastatin should not exceed 10 mg.
Special instructions
Simvastatin is not appointed to patients with a gipertriglitseridemiya until the LDL level can be lowered or normal, despite the increased level of the general cholesterol. Measurement of level of lipids has to be taken with an interval not less than 4 weeks and the dosage has to be adjusted according to reaction of the patient to treatment simvastatiny.
Principles of therapy:




Indicators of LDL and a soprikasayemost of change of lifestyle and medicamentous therapy in different risk categories


Risk category

of LDL
of mg/dl

the LDL Level at which it is necessary to begin change of lifestyle of mg/dl

the LDL Level at which it is necessary to appoint medicamentous therapy of mg/dl


of an ischemic heart disease or state close to an ischemic heart disease
(10-year risk> of 20%)

<>

>/=100

>/=130
(100-129 medicines are not obligatory) **


2+ of risk factors (10-year risk

<>

>

/=130 10-years risk of 10-20%:>
/=130 10-years risk


/=160 0-1 risk factor ***

<>

>/=160

>/=190
(160-189 medicines reducing the LDL level are not obligatory) **


** Some authors recommend to appoint the drug treatment directed to decrease in LDL if the LDL level


*** Almost all patients with 0-1 risk factors have 10-year risk
the Research of function of a liver it is necessary to conduct prior to treatment, and in 6 weeks within the first 3 months, then each 8 weeks within the remained first year, and then 1 time in half a year. To the patients accepting 80 mg of drug, function of a liver is controlled 1 time in 3 months. If increase in nuclear heating plant, ALT is 3 times more than the upper bound of norm or more, it is recommended to stop treatment simvastatiny.
At patients with myalgia, a myasthenia and/or the significant increase in activity of a kreatinfosfokinaza, drug treatment is stopped. Drug should not be used at the increased risk of developing of a rhabdomyolysis and renal failure (against the background of a heavy acute infection, arterial hypotension, the planned big surgery, injuries, heavy metabolic disturbances).
Simekar is not shown when there is a gipertriglitseridemiya of I, VI and V types. Drug is effective both in the form of monotherapy, and in combination with sekvestrant of bile acids. Prior to the beginning of and during a course of treatment the patient has to be on a hypocholesteric diet. In case of the admission of the current dose the drug needs to be taken as soon as possible. If there came time of reception of the following dose, the dose should not be doubled.
To patients with a heavy renal failure the treatment is carried out under control of function of kidneys.
Patients have to be informed that they have to report immediately to the doctor about inexplicable muscle pains, slackness, weakness, especially if it is followed by an indisposition or fever.

Overdose
Symptoms: strengthening of side effects.
Treatment: it is necessary to cause vomiting, to accept activated carbon. Symptomatic therapy. It is necessary to control functions of a liver and kidneys, kreatinfosfokinaza level in blood serum.

Form of release and packing
of the Tablet, film coated 10 mg, 20 mg, 40 mg, 80 mg.
In the blister on 14 tablets, 1 or 2 blisters in a cardboard pack together with the instruction for use.


To Store storage conditions at a temperature not over 25 of 0C in the dry, protected from light place.
To store out of children's reach!


3 years
not to apply an expiration date after expiry date.

Prescription status
According to the prescription





Republic of Kazakhstan JSC Nobel Almatinskaya Pharmatsevticheskaya Fabrika Producer,
Almaty, Shevchenko St. 162 E.







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