Simvastatin refers to the group of lipid-lowering drugs.
Pharmacological action Simvastatin
The instructions to simvastatin noted that the drug is one of the statins preventing or slowing down the process of fully HMG-CoA reductase. Additionally, a prodrug is considered analyte means because its structure is closed lactone ring which, entering the human body, is gradually hydrolyzed.
As noted in the instructions for simvastatin, its lactone ring has a structure that is almost identical to an element of the enzyme HMG-CoA reductase. As a result, competitive antagonism statine molecule binds to a specific receptor fraction of coenzyme A, which is directly attached to the active enzyme. The second component molecule statin retards or completely prevents the transition hydroxymethyl glutarate to mevalonate, which is an intermediate in the synthesis of cholesterol molecules. Slowing activity of HMG-CoA reductase leads to a fairly large number of reactions. As a result, they significantly reduce the concentration of cholesterol in the cells, a compensatory effect on the increased activity of LDL receptors and the rapid flow of cholesterol catabolism (Xc) LDL.
Statins do not have a negative impact on hepatic and lipoprotein lipase in the catabolism and synthesis of free fatty acids. As a result, their impact on the level of a second Tg and indirectly through their main action aimed at reducing the level of LDL-C. Numerous medical studies have confirmed that simvastatin can increase the level of HDL-C, up to 14%. Statins, providing lipid-lowering effect, perfect also affect blood vessels, increase the capacity of the blood rheology have antiproliferative, antioxidant abilities. The instructions to simvastatin fixed that the tool improves endothelial function after just a month of continuous treatment.
After application of simvastatin in patients was recorded normalization of the cardiovascular system (at the level of HDL-C are not playing any role).
Indications of simvastatin
Indications for simvastatin is primary hypercholesterolemia, hypertriglyceridemia when treatment with diet does not provide adequate results.
Contraindications to simvastatin
It is strictly forbidden to take simvastatin in patients with active pathological process in the liver during pregnancy and lactation, when there is a steady increase in transaminases and in case of hypersensitivity to the individual components of simvastatin.
Dosing and dosing regimen of simvastatin
Simvastatin on indications is purely individual character and only after examination of the patient. First, a patient being prescribed from 5 to 20 mg drug no more than 1 time for 24 hours. If there is an acute need, the dosage is increased gradually, leaving a space in a month. The maximum allowable rate should not exceed 40 mg per day. Patients consume additional immunosuppressants should begin treatment with 5 mg per day. The daily dose is not to exceed 5 mg.
People with severe renal insufficiency prescribe simvastatin of 5-10 mg per day.
Interaction with other drugs
Use of simvastatin with indirect anticoagulants significantly increases the impact of the latter on the human body. If you use this drug with itraconazole, cytostatics, fibrates, immunosuppressants, as well as to increase the dosage of niacin can trigger the development of myopathy.
Simvastatin and dioxin entails an increase in the concentration of dioxin in the blood plasma. Until now, in medical practice recorded a single case when the patient tried simvastatin and sildenafil, and this provoked the occurrence of rhabdomyolysis.
Side effects of Simvastatin
Among the most common side effects observed after the use of simvastatin nausea, constipation, diarrhea, loss of appetite, flatulence, acute abdominal pain, increase of AST, ALT, ALP, GGT.
In addition, the observed severe headaches, seizures, dizziness, peripheral neuropathy and paresthesia. In some cases, when using the drug occurs transient hypotension.
With regard to the musculoskeletal system, here there is rhabdomyolysis, myalgia, increased activity of CPK, myopathy occurs. Pretty rare allergic manifestations of the body: vasculitis, angionevratichesky swelling, urticaria, arthritis, thrombocytopenia. Even rarer is shortness of breath, increased erythrocyte sedimentation rate, and fever.
The skin may show rashes, itching, photosensitivity, flushing of the skin. A number of patients also documented cases of anemia.
Patients require further consultations with various liver diseases, alcoholism, hypotension, under reduced or increased skeletal muscle tone, if the patient is found severe form of renal disease or epilepsy. During the appropriate therapy requires constant monitoring of the normal functioning of the liver. Patients taking coagulants and simvastatin, are in need of constant monitoring of the prothrombin time.
If using simvastatin increases the activity of CK or is suspected myopathy, renal insufficiency, the drug should be abolished.
It is better not to use the drug with nicotinic acid, immunosuppressants, antifungal drugs are an azole derivative, and fibrates.