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medicalmeds.eu Medicines Hypolipidemic means. Simvastatin

Simvastatin

Препарат Симвастатин. ЗАО "ЗиО-Здоровье" Россия


Producer: CJSC ZIO-Zdorovye Russia

Code of automatic telephone exchange: C10AA01

Release form: Firm dosage forms. Tablets.

Indications to use: Atherosclerosis of coronary arteries. Prevention of a myocardial infarction. Coronary heart disease. Gipertriglitseridemiya. Hypercholesterolemia.


General characteristics. Structure:

Active agent of Simvastatin of-10 mg - 20 mg Auxiliary вещестав: starch corn, lactoses monohydrate, microcrystallic cellulose, butylhydroxyanisole, ascorbic acid, citric acid, magnesium stearate. Cover:      Опадрай  II   white  for  tablets   of 10  mg  (a macrogoal  (polyethyleneglycol), polyvinyl alcohol, talc, titanium dioxide). Опадрай II yellow for tablets of 20 mg (a macrogoal (polyethyleneglycol), polyvinyl alcohol, talc, an aluminum varnish quinolinic yellow, titanium dioxide, iron oxide yellow).




Pharmacological properties:

Pharmacodynamics. The hypolipidemic means received in the synthetic way from a product of fermentation of Azreg^shsh 1eggesh is an inactive lactone, in an organism is exposed to metabolism with formation of hydroxyacid derivative. The active metabolite inhibits 3-гидрокси-З-метил-глутарил-КоА-редуктазу (GMG-KOA-reduktazu), enzyme, katalaziruyushchy initial reaction of formation of a mevalonat from GMG-KOA. As transformation GMG-KOA in мевалонат represents an early stage of synthesis of cholesterol, use of a simvastatin does not cause accumulation in an organism of potentially toxic sterol. GMG-KOA it is easily metabolized to atsetil-KOA which participates in many processes of synthesis in an organism.
 
Causes decrease in contents in a blood plasma of triglycerides (TG), lipoproteids of the low density (LPNP), lipoproteids of very low density (LPONP) and the general cholesterol (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 reduces a ratio of LPNP / LPVP and the general cholesterol / LPVP. 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 gradually is returned to initial level.
 
 
 
Pharmacokinetics. Absorption of a simvastatin high. After intake the maximum concentration in a blood plasma is reached approximately in 1,3 - 2,4 hours and decreases by 90% in 12 hours. Communication with proteins of a blood plasma makes about 95%. It is metabolized  in  a liver,  has  effect  of "the first  passing"  through  a liver (it is hydrolyzed  with  formation  of active  derivative:  a beta  -  hydroxyacid, also other active, and also inactive metabolites are found). The elimination half-life of active metabolites makes 1,9 hours. It is removed preferential with a fecal masses (60%) in the form of metabolites. About 10 - 15% are removed by kidneys in an inactive form.


Indications to use:

Hypercholesterolemia:
 
· primary hypercholesterolemia (type of Pa and P) at inefficiency of a dietotherapy with the low content of cholesterol and other non-drug actions (an exercise stress and decrease in body weight) at patients with the increased risk of developing of coronary atherosclerosis;
 
· the combined hypercholesterolemia and the gipertriglitseridemiya which is not adjusted by a special diet and an exercise stress. Learn on this page what lowers cholesterol better: симвастатин or аторвастатин, розувастатин.
 
· Homozygous hereditary hypercholesterolemia.
 Coronary heart disease:
 
for prevention of a myocardial infarction, for reduction of risk of death, reduction of risk of cardiovascular disturbances (a stroke or tranzitorny ischemic attacks), delay of progressing of atherosclerosis of coronary vessels, reduction of risk of procedures of revascularization.


Route of administration and doses:

Inside. The initial dose of Simvastatin makes 5-20 mg. If necessary the dose is raised with an interval of 4 weeks. Simvastatin accept in 1 time/days, in the evening. The maximum dose makes 40 mg/days.
 
For the patients receiving immunodepressants, the recommended initial dose makes 5 mg/days; the maximum dose - 5 mg/days.


Features of use:

   At the beginning of   therapy   by Simvastatin          perhaps passing   increase   in level of "hepatic" enzymes. Before therapy and further regularly to conduct a function research baking (to control activity of "hepatic" enzymes each 6 weeks during the first
 
3 months, then each 8 weeks within the remained first year, and then 1 time in half a year), and also at increase in doses it is necessary to carry out the test for definition of function of a liver. At increase in a dose to 80 mg it is necessary to carry out the test each 3 months. At permanent    increase  in activity    of transaminases (by 3 times in comparison with initial level) Simvastatin's reception should be stopped. Simvastatin, as well as other GMG-Co-A-inhibitors of reductase, it is not necessary to apply at the increased risk of development of a rabdomioliz and a renal failure (against the background of a heavy acute  infection,  arterial  hypotension,  the planned  big  surgery, injuries, heavy metabolic disturbances).
 
Cancellation of hypolipidemic means during pregnancy has no significant effect on results of prolonged treatment of primary hypercholesterolemia. Because inhibitors of GMG-KOA-reduktazy slow down cholesterol synthesis, and cholesterol and other products of its synthesis play an essential role in fetation, including  synthesis   of steroids  and   cellular  membranes,   симвастатин  can  render
 
an adverse  effect  on  a fruit  at  appointment  to his  pregnant women  (women of reproductive age have to avoid conception). If in the course of treatment there occurred pregnancy, drug has to be cancelled, and  the woman is warned about possible danger to a fruit.
 
  Simvastatin's use    is not recommended  at  the women  of childbearing  age  who are not using contraceptive means.
 
At patients with the lowered function of a thyroid gland is (hypothyroidism) or in the presence of some  diseases  of kidneys  (a nephrotic  syndrome)  at  increase     in level Simvastatin with   care   appoint to persons who abuse alcohol
 
and/or have in the anamnesis of a disease of a liver.
 
Prior to the beginning of and during treatment the patient has to be on a hypocholesteric diet. The concomitant use  of grapefruit  juice can strengthen   degree of manifestation of the by-effects connected with Simvastatin's reception therefore it is necessary to avoid their concomitant use.
 
Simvastatin is not shown when there is a gipertriglitseridemiya I, IV and V types. Treatment by Simvastatin   can cause the myopathy leading to a rabdomioliz and a renal failure. The risk of developing of this pathology increases at the patients receiving              one or several  of  the following medicines along with Simvastatin: fibrata (gemfibrozit, фенофибрат), cyclosporine, нефазадон,
 
macroleads  (erythromycin,  кларитромицин),  antifungal  means  from  group of "azoles"  (кетоконазол, интраконазол) and inhibitors  of HIV proteases (ритонавир). The risk of development of a myopathy increases also at patients with a heavy renal failure.

All patients beginning therapy by Simvastatin and also patients who need to increase a drug dose have to be warned about possibility of a myopathy and need of the immediate address to the doctor in case of emergence inexplicable pains, morbidity in muscles, slackness or muscular   weakness,   especially   if   that is followed by an indisposition   or fever.  Therapy  by drug  has to      be immediately stopped  if the myopathy is diagnosed or is supposed.
 
    For   diagnosing     of development of a myopathy it is recommended to take measurements of size KFK regularly.
 
At treatment by Simvastatin increase of maintenance of serumal KFK is possible that should be considered at differential diagnosis of pains behind a breast. As criterion of drug withdrawal serves increase in maintenance of KFK in blood serum more than by 10 times of rather upper bounds of norm. At patients with a mialgiya, a myasthenia and/or the expressed increase in activity of KFK treatment with drug is stopped.
 
Drug is effective both in the form of monotherapy, and in combination with sekvestrant of bile acids. In case of the admission of the current dose drug needs to be accepted as soon as possible. If came time of reception of the following dose, a dose not to double. To patients with a heavy renal failure treatment is carried out under control of function of kidneys. Duration of use of drug is defined by the attending physician individually.
 
Influence on ability to drive the car and to work with mechanisms
 
About adverse influence of Simvastatin   on ability to drive the car and work with mechanisms it was not reported.


Side effects:

Alimentary  system:        abdominal pains,  a lock,  a meteorism,    nausea, diarrhea, pancreatitis, vomitinghepatitis, increase in activity of "hepatic" enzymes, an alkaline phosphokinase and kreatinfosfokinaza (KFK) are possible.
 
Nervous system and sense bodys: asthenic syndrome, headache, dizziness,    sleeplessness,    muscular    spasms,    paresthesias,    peripheral neuropathy, sight vagueness, disturbance of flavoring feelings.
 
Allergic     and     immunopathological     reactions:      Quincke's     disease, rheumatic polimialgiya, vasculitisthrombocytopenia, increase SOE, fever, arthritis, urticaria, photosensitization, dermahemia, inflows, asthma,
 
volchanochnopodobny syndrome, eosinophilia.
 
Dermatological reactions: seldom skin rash, itch, alopecia, dermatomyositis.
 
  From    a musculoskeletal system:  myopathy,  mialgiya,  myotonia  , weakness; seldom - рабдомиолиз.

Others:    anemia,    heartbeat,    an acute    renal    failure    (owing to a rabdomioliz), decrease in a potentiality.


Interaction with other medicines:

Cytostatics, antifungal means (кетоконазол, интраконазол), fibrata, high doses of niacin, immunodepressants, erythromycin, кларитромицин, телитромицин, HIV protease inhibitors, нефазодон increase risk of development of a myopathy.
 
Cyclosporine or даназол: the risk of development of a myopathy / рабдомиолиза increases at joint purpose of cyclosporine or a danazol with high doses of a simvastatin. Other hypolipidemic means capable to cause development of a myopathy: the risk of development of a myopathy increases at joint purpose of other hypolipidemic means which are not powerful SURZA4 inhibitors, but capable to cause a myopathy in the conditions of monotherapy. Such as gemfibrozit also other fibrata (except a fenofibrat), and also Niacinum (niacin) in a dose> 1 g a day. Amiodaronum and verapamil: the risk of development of a myopathy increases at joint reception of Amiodaronum or verapamil with high doses of a simvastatin. The risk   of development  of a myopathy   slightly   increases   at  the patients receiving diltiazem along with simvastatiny in a dose of 80 mg. "Simvastatin exponentiates effect of peroral anticoagulants (e.g., фенпрокумон,
 
warfarin) also increases risk of developing of bleedings that demands need of monitoring procedure of indicators of coagulability of blood prior to treatment, and also is rather frequent during an initial stage of therapy. As soon as the stable level of an indicator of a prothrombin time or the International Normalized Relation (INR) is reached, its further control should be carried out bucketed, recommended for the patients receiving therapy by anticoagulants. At change of a dosage or the termination of reception of a simvastatin it is also necessary to carry out control of a prothrombin time or MNO according to the above scheme. Therapy simvastatiny does not cause changes of a prothrombin time and risk of bleedings in the patients who are not accepting anticoagulants. Increases digoxin level in a blood plasma.
 
Colestyraminum and колестипол reduce bioavailability (use of a simvastatin is possible in 4 hours after reception of the specified medicines, at the same time the additive effect is noted).
 
Juice of grapefruit contains one or more components which inhibit SURZA4 and can increase concentration in a blood plasma of the means which are metabolized SURZA4. Increase in activity of inhibitors of GIG-KOA-reduktazy after the use of 250 ml of juice a day is minimum and has no clinical value. However consumption of large volume of juice (more than 1 liter a day) at reception of a simvastatin considerably increases the level of the inhibiting activity concerning GMG-KOA-reduktazy in a blood plasma. In this regard it is necessary to avoid grapefruit juice consumption in large numbers.


Contraindications:

· hypersensitivity to a simvastatin or to other components of drug (including a hereditary lactose intolerance), and also to other drugs of a statinovy row (GMG-KOA-reduktazy inhibitors) in the anamnesis;
 
· liver diseases in an active phase, permanent increase in activity of "hepatic" enzymes of not clear etiology;
 
· diseases of skeletal muscles (myopathy);
 
· age up to 18 years (efficiency and safety are not established)
 
With care: appoint the patient abusing alcohol, to patients after organ transplantation which carries out therapy by immunodepressants (in connection with the increased risk of emergence of a rabdomioliz and a renal failure);


Overdose:

In one of the known several cases of overdose (most accepted dose of 450 mg) of specific symptoms it was not revealed.
 
Treatment: to cause vomiting, to accept absorbent carbon. Symptomatic therapy. It is necessary to control functions of a liver and kidneys, the KFK level in blood serum. At development of a myopathy with rabdomiolizy and an acute renal failure (rare, but
 
heavy side effect) it is necessary to stop immediately administration of drug and to enter to the patient diuretic and sodium bicarbonate (intravenous infusion). If necessary the hemodialysis is shown. Rabdomioliz can cause a hyperpotassemia which can be eliminated intravenous
 
introduction of Calcii chloridum or calcium of a gluconate, infusion of glucose with insulin, use  of potassium  ion exchangers  or,  in  hard  cases,    by means of a hemodialysis.


Storage conditions:

List B. In the dry, protected from light place at a temperature пс it is above 30 °C. To store in the place, unavailable to children!


Issue conditions:

According to the recipe


Packaging:

Tablets, coated, on 10 and 20 mg. On 10 tablets in a blister strip packaging from the film of PVC and printing aluminum foil varnished. On 2, 3, 5 or 10 blister strip packagings together with the application instruction place in a pack from a cardboard.
 
Packaging for hospitals. On 100, 200, 300, 400 or 500 blister strip packagings with application instructions place in boxes from a corrugated cardboard. On 500, 1000 or 2000 tablets in banks polymeric with covers. On 1, 2, 3, 4, 5, 6 cans with instructions.



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