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Actalipid 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 Actalipid increases HDL-C to 14%.
In addition to the hypolipidemic actions Actalipid 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 Actalipid improves endothelial function within 30 days of therapy.
Actalipid therapy was accompanied by a decrease in the incidence of cardiovascular disorders, regardless of baseline LDL-C.
After oral administration Actalipid is well absorbed from the gastrointestinal tract (average 85%). Cmax is reached after 4 h. Taking Actalipid just before eating with low fat does not affect its the pharmacokinetic parameters.
During a "first pass" through the liver Actalipid biotransformed to form active beta-metabolites. The plasma protein binding is 95%.
The concentration of the active metabolite of Actalipid 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 Actalipid prescribed?
Primary hypercholesterolemia with the ineffectiveness of diets, combined hypercholesterolemia and hypertriglyceridemia.
Dosage and administration
The dosing regimen of Actalipid is individual. The initial dose is 5-20 mg. If necessary the dose is increased every 4 weeks. Actalipid 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.
Actalipid side effects, adverse reactions
Digestive system: constipation, diarrhea, loss of appetite, flatulence, nausea, abdominal pain, pancreatitis, increased ALT, AST, GGT, ALP.
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.
An active pathological process in the liver, persistent elevation of transaminases, pregnancy, lactation, hypersensitivity to simvastatin.
Using during pregnancy and breastfeeding
Actalipid is contraindicated in pregnancy and lactation.
Category effects on the fetus by FDA - X.
With careful use Actalipid 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 Actalipid should monitor the prothrombin time.
Actalipid 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 Actalipid concurrently with immunosuppressants, fibrates, nicotinic acid (in doses causing gipolipidemiyu), antifungal azole derivatives drugs.
Safety and efficacy of Actalipid in a pediatric practice are not established. It is not recommended to use this medication for children.
Actalipid drug interactions
Simultaneous administration of Actalipid 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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