Simvastatin

Simvastatin treats group of hypolipidemic medicines.

Pharmacological action of Simvastatin

In the instruction to Simvastatin it is noted that this drug is among the statines which are preventing or completely slowing down process of formation of GMG-KOA-reduktazy. Besides, the analyzed means is considered pro-medicine because in its structure there is a closed lactone ring which, getting into a human body, is gradually hydrolyzed.

As it is noted in the instruction to Simvastatin, his lactone ring has such structure which is almost completely identical to some element of enzyme of GMG-KOA-reduktazy. As a result of competitive antagonism the molecule of statine connects to a certain share of a receptor of coenzyme A which this enzyme directly joins. The second component of a molecule of statine slows down or completely prevents transition process glutarate hydroxymethyl in мевалонат that is an intermediate product in synthesis of a molecule of cholesterol. Delay of activity of GMG-KOA-reduktazy involves quite large number of reactions. As a result they significantly reduce concentration of cholesterol in cells, influence compensatory increase of activity of LPNP-receptors, and also bystry course of a catabolism of cholesterol (Хс) of LPNP.

Statines do not make negative impact on gepatichesky and lipoprotein lipases, on a catabolism and synthesis of free fatty acids. As a result of it their impact on the TG level for the second time is also mediated through their main action directed to reduction of the Hs-LPNP level. Numerous medical researches confirm the fact that Simvastatin is capable to increase the Hs-LPVP level up to 14%. Statines, having hypolipidemic effect, perfectly influence also walls of vessels, increase rheological abilities of blood, have anti-proliferative, antioxidant abilities. In the instruction to Simvastatin it is recorded that this means improves function of an endothelium after all month of continuous treatment.

After Simvastatin's use for patients normalization of work of cardiovascular system was recorded (at the same time the Hs-LPVP level did not play in general any role here).

Indications

Indications to Simvastatin is primary hypercholesterolemia, a gipertriglitseridemiya when treatment by means of a diet does not yield due results.

Contraindications

Simvastatin to patients with active pathological process in a liver is strictly forbidden to accept, at pregnancy and in the period of a lactation when continuous increase of activity of transaminases is observed, and also at hypersensitivity to separate components of Simvastatin.

Route of administration of Simvastatin and mode of dosing

Simvastatin's appointment according to indications has especially individual character and is carried out only after inspection of the patient. First of all, prescribe the patient from 5 to 20 mg of medicine no more than 1 time within 24 hours. If there is an urgent need, the dosage increases gradually, with observance of an interval in a month. The most admissible norm should not exceed 40 mg a day. The patients who is in addition using immunodepressants should begin a course of treatment with 5 mg a day. The daily dosage at the same time cannot exceed 5 mg of drug.

To people with a severe form of a renal failure appoint Simvastatin 5-10 mg a day.

Interaction with other medicines

Simvastatin's use with indirect anticoagulants significantly increases impact of the last on a human body. If to use this drug with itrakonazoly, cytostatics, fibrata, immunodepressants, and also to raise a niacin dosage, it is possible to provoke development of a myopathy.

Simvastatin's use and dioxine involves increase in concentration of dioxine in a blood plasma. Until now in medical practice the isolated case when the patient used Simvastatin is recorded and sildenafit, and it provoked emergence of a rabdomioliz.

Side effects of Simvastatin

Among the most widespread side effects after Simvastatin's use nausea, a lock, diarrhea, a loss of appetite, a meteorism, an acute pain in a stomach, increase of activity of nuclear heating plant, ALT, ShchF, GGT are observed.

Besides, severe headaches, spasms, dizziness, a peripheral neuropathy and paresthesia are noted. In some cases when using drug there is tranzitorny arterial hypotension.

As for a musculoskeletal system, it is observed рабдомиолиз here, the mialgiya, increases activity of KFK, there is a myopathy. Quite seldom also allergic manifestations of an organism meet: vasculitis, Quincke's disease, small tortoiseshell, arthritis, thrombocytopenia. Even more rare there is asthma, increase SOE and fever.

On skin rash, an itch, a photosensitization, a dermahemia can be shown. At a number of patients also anemia cases are recorded.

Special instructions

Additional consultation patients with various diseases of a liver, at alcoholism demand, arterial hypotension, at the lowered or raised tone of skeletal muscles if the severe form of a renal failure or epilepsy is found in the patient. During performing the corresponding therapy constant control of normal functioning of a liver is necessary. Patients, the accepting coagulants and Simvastatin, need constant control of a prothrombin time.

If using Simvastatin activity of KFK increases or there are suspicions on development of a myopathy, a renal failure, then drug needs to be cancelled.

It is better not to use this drug together with the niacin, immunodepressants, antifungal drugs which are derivatives of an azol, and also a fibratama.