Kymazol

Kymazol uses

• Pharmacological action
• Pharmacokinetics
• Why is Kymazol prescribed?
• Dosage and administration
• Kymazol side effects, adverse reactions
• Kymazol contraindications
• Using during pregnancy and breastfeeding
• Special instructions
• Kymazol drug interactions
• Kymazol reviews

Pharmacological action

Kymazol 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 Kymazol increases HDL-C to 14%.

In addition to the hypolipidemic actions Kymazol has beneficial effects in endothelial dysfunction, on the vascular wall, the state of atheroma, improves blood rheology, have antioxidant, antiproliferative properties. There is evidence that Kymazol improves endothelial function within 30 days of therapy.

Kymazol therapy was accompanied by a decrease in the incidence of cardiovascular disorders, regardless of baseline LDL-C.

Pharmacokinetics

After oral administration Kymazol is well absorbed from the gastrointestinal tract (average 85%). C_max is reached after 4 h. Taking Kymazol just before eating with low fat does not affect its the pharmacokinetic parameters.

During a "first pass" through the liver Kymazol biotransformed to form active beta-metabolites. The plasma protein binding is 95%.

The concentration of the active metabolite of Kymazol 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 Kymazol prescribed?

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

Dosage and administration

The dosing regimen of Kymazol is individual. The initial dose is 5-20 mg. If necessary the dose is increased every 4 weeks. Kymazol 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, the initial dose is 5-10 mg / day.

Kymazol 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.

Kymazol contraindications

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

Using during pregnancy and breastfeeding

Kymazol is contraindicated in pregnancy and lactation.

Category effects on the fetus by FDA - X.

Special instructions

With careful use Kymazol 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 Kymazol should monitor the prothrombin time.

Kymazol 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 Kymazol concurrently with immunosuppressants, fibrates, nicotinic acid, antifungal azole derivatives drugs.

Safety and efficacy of Kymazol in a pediatric practice are not established. It is not recommended to use this medication for children.

Kymazol drug interactions

Simultaneous administration of Kymazol with: