One tablet contains Ezetrola
10 mg of active substance - ezetimibe. As used excipients: microcrystalline cellulose, sodium lauryl sulfate, povidone, magnesium stearate, croscarmellose sodium, lactose monohydrate.
Ezetrol refers to a group of lipid-lowering drugs. The drug is intended for oral administration. The mechanism of action of the drug differs from other analogues Ezetrola class of lipid-lowering drugs such as statins, fibrates, and plant sterols. When injected into the small intestine, the drug is concentrated in the brush border of the small intestine and interferes with the absorption of cholesterol, the cholesterol lowering delivery to the liver, whereby the liver decreases its concentration.
Ezetrol affects increasing excretion of bile acids. At the two-week clinical trial which involved 18 patients, it was found that the adoption Ezetrola reduced cholesterol absorption by 54%. This reduces the chance of developing atherosclerosis. Research has shown that mortality caused by cardiovascular diseases is directly related to the total level of cholesterol, according to its reduction lowers the incidence and mortality.
After oral Ezetrol rapidly absorbed in the small intestine and the liver, forming a pharmacologically active phenolic glucuronide. The maximum concentration of glucuronide plasma occurs within 1-2 hours, ezetimibe - 5-12 hours. Due to the almost total insolubility in water of the drug can not determine its absolute bioavailability.
In the standard single dose of 10 mg, simultaneous with food does not affect the bioavailability Ezetrola. The drug binds to proteins in the blood of 99.7%
Ezetrola metabolism occurs primarily in the liver and small intestine by conjugation (reaction phase II) with the glucuronide. The drug is excreted in the bile.
The ingestion of 20 mg labeled 14C-ezetimibe, ezetimibe level in plasma was 93% of the plasma radioactivity. By the coming 48 hours, radioactive traces in blood plasma was found. The half-life Ezetrola approximately 22 hours. Of the total number of doses, for 10 days, it is excreted in urine about 11%, from about 78% feces.
Data on the pharmacokinetics in children under 10 years are absent. Indicators of metabolism and absorption of the drug in adults and adolescents from 10 to 18 years are the same.
Patients with mild hepatic impairment is not necessary to select an individual dosage. In women slightly higher, about 20%, the concentration of drug in the blood plasma than in men.
- homozygous sitosterolemia;
- Primary Hypercholesterolemia;
- homozygous familial hypercholesterolemia.
- Liver failure (moderate and severe);
- lactose intolerance;
- hypersensitivity to the drug;
- age 18 years.
Caution should be exercised
when administering the drug to patients receiving cyclosporine. Do not take analogues Ezetrola simultaneously with fibrates, to obtain data on the results of clinical trials.
Prior to treatment, patients should observe Ezetrolom lipid-lowering diet aimed at lowering cholesterol. Take Ezetrol can be, regardless of the meal.
The dose recommended instructions Ezetrola as monotherapy or in combination with statins - 10 mg per day.
Patients with mild renal function impairment, or liver and elderly patients is not required individual dosage. When moderate or severe hepatic impairment receiving Ezetrola recommended.
From these overdose Ezetrolom review found that in most cases, an overdose is not accompanied by adverse reactions and when they occur they are not pronounced and transient in nature.
In overdose Ezetrolom, instruction recommended maintenance and symptomatic therapy.
Interaction with other drugs Ezetrola
Ezetrol has no effect on the pharmacokinetics of oral contraceptives (levonorgestrel and ethinyl estradiol), dapsone, glipizide, midazolam, tolbutamide, dextromethorphan, digoxin and warfarin.
Combination of cimetidine does not affect its bioavailability.
When concomitantly with antacids rate of absorption is reduced without affecting its bioavailability.
Combining Ezetrola receiving gemfibrozil and fenofibrate increases the total concentration of the drug in 1.5-1.7 times.
There is no data on the safety of simultaneous reception with fibrates, which may increase the removal of cholesterol, resulting in gallstone disease may occur. Therefore it is not recommended the appointment of both analog Ezetrola and fibrates.
No clinically significant pharmacokinetic interaction Ezetrola with rosuvastatin, fluvastatin, lovastatin, pravastatin, simvastatin and atorvastatin have been identified.
Pregnancy and lactation
On the results of the use of pregnant women Ezetrola yet been received, so the use during pregnancy is not recommended Ezetrola instruction. In determining the beginning of pregnancy the use of the drug should be discontinued.
About breeding Ezetrola breast milk there is no data, so it is recommended to stop breast-feeding before you start taking the drug.
Side effects Ezetrola
In clinical trials of up to 14 weeks, which was attended by 3366 patients, it was established well tolerated with a daily intake of 10 mg in combination with a statin or as monotherapy. They were fixed quickly and easily transient side effects, incidence of adverse events did not differ from the rate in the placebo group.
When alone, the following side effects: diarrhea, abdominal pain, headache.
When combined Ezetrola and statin may occur: myalgia, nausea, bloating, diarrhea, constipation, abdominal pain, fatigue, headache.
These clinical applications of Ezetrola reviews have shown the possibility of the following reactions: paresthesia, nausea, pancreatitis, skin rash, thrombocytopenia, angioedema, rarely - rhabdomyolysis, myopathy.
The drug is stored in the reach of children at room temperature.