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Product Name: Zocor

Generics: Simvastatin

Common Brand Names: Simovil; Zocor Forte

Pharmaceutical Category: Cardio / Blood Pressure / Cholesterol

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There is an additional general information about this medication active ingredient simvastatin:

Pharmacological action

Zocor is a hypolipidemic agent from a group of statins, an inhibitor of HMG-CoA reductase. This medication is a prodrug because it has in its structure the closed lactone ring which is hydrolyzed after intake.
Lipid-lowering effect of statins is associated with lower levels of total cholesterol by LDL-C. Reducing cholesterol is dose-dependent and is not linear but exponential. Statins do not affect the activity of lipoprotein and hepatic lipase, have no significant effect on the synthesis and catabolism of free fatty acids, thats why their effect on TG levels again and indirectly through their main effects on reducing LDL-C.
According to the controlled studies of simvastatin increases HDL-C to 14%.
In addition to the hypolipidemic actions Zocor has beneficial effects in endothelial dysfunction (pre-clinical sign of early atherosclerosis), on the vascular wall, the state of atheroma, improves blood rheology, have antioxidant, antiproliferative properties. There is evidence that simvastatin improves endothelial function within 30 days of therapy.
Simvastatin therapy was accompanied by a decrease in the incidence of cardiovascular disorders, regardless of baseline LDL-C.

Pharmacokinetics

After oral administration Zocor is well absorbed from the gastrointestinal tract (average 85%). Cmax is reached after 4 h. Taking simvastatin just before eating with low fat does not affect its the pharmacokinetic parameters.
During a "first pass" through the liver simvastatin biotransformed to form active beta-metabolites. The plasma protein binding is 95%.
The concentration of the active metabolite of simvastatin in human systemic circulation is less than 5%.
Excreted in unchanged form and as metabolites, mainly in the bile - 60-85%, 10-15% - in the form of inactive metabolites are excreted by the kidneys.

Why is Zocor prescribed?

Primary hypercholesterolemia with the ineffectiveness of diets, combined hypercholesterolemia and hypertriglyceridemia.

Dosage and administration

The dosing regimen of Zocor is individual. The initial dose is 5-20 mg. If necessary the dose is increased every 4 weeks. Simvastatin is taken 1 time / day in the evening. The maximum dose is 40 mg / day.
For patients receiving immunosuppressive drugs, the recommended starting dose is 5 mg; the maximum dose is 5 mg / day.
In severe renal insufficiency (creatinine clearance less than 30 ml / min), the initial dose is 5-10 mg / day.

Zocor side effects, adverse reactions

Digestive system: constipation, diarrhea, loss of appetite, flatulence, nausea, abdominal pain, pancreatitis, increased ALT, AST, GGT, ALP.
CNS and peripheral nervous system: headache, dizziness, muscle cramps, paresthesia, peripheral neuropathy.
Cardiovascular system: possible transient hypotension.
Musculoskeletal system: myalgia, myopathy, rhabdomyolysis, increased CPK.
Allergic reactions: seldom - angioedema, lupus like syndrome, vasculitis, thrombocytopenia, eosinophilia, ESR increase, arthritis, rash, fever, shortness of breath.
Dermatological reactions: photosensitivity, skin rash, itching, redness of skin, alopecia.
Other: anemia.

Zocor contraindications

An active pathological process in the liver, persistent elevation of transaminases, pregnancy, lactation, hypersensitivity to simvastatin.

Using during pregnancy and breastfeeding

Simvastatin is contraindicated in pregnancy and lactation.
Category effects on the fetus by FDA - X.

Special instructions

With careful use simvastatin in patients with liver disease, with chronic alcoholism, with hypotension, reduced or increased tone of skeletal muscle of unknown etiology, epilepsy, severe renal insufficiency.
Before and during treatment it is necessary to monitor liver function.
Patients receiving anticoagulant coumarin derivatives, before and during treatment with simvastatin should monitor the prothrombin time.
Simvastatin therapy should be discontinued if a significant increase in CK activity or suspected myopathy, the development of acute or severe illness when any risk factors predisposing to renal failure due to rhabdomyolysis.
It is not recommended to use simvastatin concurrently with immunosuppressants, fibrates, nicotinic acid (in doses causing gipolipidemiyu), antifungal azole derivatives drugs.
Safety and efficacy of simvastatin in a pediatric practice are not established. It is not recommended to use this medication for children.

Zocor drug interactions

Simultaneous administration of Zocor with:
  • amplified the effect of indirect anticoagulants (including warfarin).
  • digoxin increased digoxin concentration in blood plasma.
  • cytotoxic drugs, itraconazole, fibrates, nicotinic acid in high doses, immunosuppressants increases the risk of myopathy. There was described one case of symptoms of rhabdomyolysis after a single dose of sildenafil dose in patients receiving simvastatin.

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