The drug “Mertenil” is an example of a high-quality generic “Crestor” containing rosuvastatin as an active ingredient. It belongs to the class of statins of the fourth generation and was introduced into clinical practice in 2003. Its use is reasonable in cases of hypercholesterolemia and as an additional means of preventing acute vascular thrombosis. In this role, the drug "Mertenil", whose analogues are few in number, but are well known, fully justifies its purpose.
Release form
The tablet dosage form of the Mertenil preparation, analogues of which are absent among registered trade names, is coated with a film coating. Inside it contains calcium rosuvastatin with excipients: lactose monohydrate, microcrystalline cellulose, magnesium hydroxide and stearate, type A crospovidone. The film shell itself consists of polyvinyl alcohol, macrogol 3350, talc and titanium dioxide. It is simpler than the drug "Crestor", although it provides a gradual release of rosuvastatin.
There are 4 doses of the drug: tablets of 5, 10, 20 and 40 mg. It is produced in tablets, packed in blisters, folded in cardboard boxes. One blister contains 30 tablets, which is enough for a monthly treatment. In a specific clinical situation, it is reasonable to use one of these dosages, which can be changed later. The medicine is prescription and should be stored in a warm, dry, dark place out of the reach of children.
Directions for use
The instruction accompanying the “Mertenil 10 mg” preparation contains information on clinical indications, contraindications, dosage regimens and side effects. It fully describes the possible drug interactions of the drug, important clinical recommendations. The drug is a prescription, and without a doctor’s prescription, it is not available to the patient. Therefore, starting to take “Mertenil”, “Crestor” analogues or generics, as well as any statins, one should determine blood lipid fractions and consult a physician or cardiologist.
Indications for use
Before using the drug, it is important to determine the indications and find out the specific type of hypercholesterolemia. A blood lipid profile provides comprehensive information about impaired fat metabolism and its degree. Target indications for use are as follows:
- familial heterozygous (hereditary) hypercholesterolemia;
- primary (hereditary) polygenic hypercholesterolemia type IIa, classified according to Fredrickson;
- combined dyslipidemia IIb in the classification according to Fredrickson;
- familial homozygous (hereditary) hypercholesterolemia;
- atherosclerosis and conditions that exacerbate cardiovascular risks (increase in the concentration of cholesterol in general and (or) its low-density fraction);
- atherosclerosis obliterans, cerebrovascular and cardiovascular diseases as part of a balanced combination treatment (see explanations);
- treatment of hypertriglyceridemia (IV type of dyslipidemia according to Fredrickson) in combination with diet and dosed physical activity.
Explanation of indications
The evidence base is that the increase in low-density fractions (LDL) of lipoproteins containing a lot of cholesterol is quite large. It is known that the severity and rate of development of cardiovascular and cerebrovascular diseases depends on the initial plasma concentration of cholesterol and LDL. This creates the prerequisites for the development of atherosclerosis with the formation of plaque inside the arteries of the elastic type. The gradual growth of the plaque narrows their lumen, reduces the throughput of blood vessels, and causes chronic ischemia of the nourished organ.
According to this mechanism, the development of cerebrovascular diseases, chronic limb ischemia and cardiac ischemic disease occurs. Elastic arteries are also present in other areas of the body, which creates the prerequisites for the development of atherosclerosis obliterans of the extremities. Myocardial and cerebral infarction develops due to tearing of the arterial endothelium over the vessel plaque and subsequent formation of a thrombus. The latter further narrows the lumen of the organ supplying the organ, which is why a portion of the brain or myocardium dies.
The effectiveness of the prophylactic prescription of statins of the first three generations, as well as the more advanced drug "Mertenil", instructions for use, reviews, as well as recommendations of clinicians fully justify. An adult with no signs of coronary heart disease, but with the risks of its development, is already recommended to use "Mertenil." It is rational at the age of 50 years for men and 60 years for women.
Contraindications
The instructions attached to the “Mertenil” preparation, reviews of doctors, as well as the results of many clinical studies confirm the presence of important absolute and temporary relative contraindications. In the case of absolute medicine cannot be used, while temporary contraindications allow its use. Absolute contraindications are:
- active phase of hepatic disease, cytolysis syndrome, or more than three-fold increase in transaminases;
- chronic liver failure with 9 points on the Child-Pugh scale;
- chronic renal failure with creatinine clearance less than 30 ml / min;
- clinically proven myopathy (muscle pain or rhabdomyolysis syndrome, the patient’s tendency to any myotoxic complications);
- the need to use the drug "Cyclosporin" for the treatment of specialized diseases;
- the inability to use contraceptives, pregnancy, lactation, childhood and adolescence (up to 18 years);
- increased individual sensitivity to the components and (or) an allergic reaction to rosuvastatin or dosage form substances.
In addition to these, there are some special contraindications exclusively for the dosage of 40 mg of the drug "Mertenil". Instructions for use and analogues of international clinical recommendations explain the following absolute contraindications:
- all the contraindications mentioned above, with the exception of chronic renal failure (40 mg / day can be prescribed only with creatinine clearance above 60 ml / min);
- hypothyroidism;
- hereditary diseases of muscle tissue;
- combined use with fibrates;
- Mongoloid race (it is forbidden to prescribe above 20 mg per day);
- alcohol dependence syndrome;
- initial intake of rosuvastatin.
The original drug “Crestor, as well as any rosuvastatin (in this case, Mertenil), analogues (synonyms) and its generics cannot be prescribed in a dose of 40 mg until a lower dose of lipid-lowering therapy has been carried out. Only when a daily dose of 20 mg was insufficient to normalize the lipid profile, as confirmed by a lipid profile 4 weeks after the moment of therapy, 40 mg per day is required. Moreover, this is permissible in the absence of special contraindications for 40 mg.
Drug dosage
When choosing a dosage regimen, the instructions for use, the analogues of international algorithms developed based on the clinical recommendations of AHA and ESC, and the individual characteristics of the patient are taken into account with the Mertenil drug 5 mg of the drug is prescribed in the treatment of IIa and IIb hypercholesterolemia, type IV dyslipidemia according to Fredrickson. In the prevention of ischemic diseases associated with the development of atherosclerosis, the recommended dose is also 5 mg.
A daily dose of 10 mg Mertenil is required in the treatment of ischemic diseases to stabilize the endothelium over an atherosclerotic plaque and to inhibit its expansion. The same indication is also relevant for a dosage of 20 mg, although it is rational to use this amount of the drug at high values of the low-density LP fraction and cholesterol, as well as at low concentrations of high-density LP fractions. A dosage of 40 mg can be prescribed at a low efficacy of 20 mg after evaluating the lipid profile. According to current AHA and ESC recommendations, the daily dose of Mertenil can be increased to 80 mg.
Features of the reception
The main source of information about taking the drug "Mertenil" is the instructions for use. Krestor's analogs and generics are also used according to these recommendations. According to the peculiarities of pharmacokinetics, rosuvastatin tablets (in this case Mertenil) are taken at any time of the day. They should be swallowed whole and washed down with a sufficient amount of water 50-150 mg. But, according to the recommendations of ESC and ANA from 2014, any statins should be taken before bedtime, ignoring the attached instructions for use.
Side effects
Frequent side effects of Mertenil, the frequency of which is 1-10%, are: dizziness, myalgia, nausea, constipation, diffuse abdominal pains, asthenia, headaches. Infrequent side effects with a frequency of 0.01-1%: insomnia, urticaria, skin itching, mood changes in the direction of depression. Rare effects (0.0001-0.01%): myositis, myopathy, rhabdomyolysis, increased organ-specific liver transaminases, pancreatitis, Quincke edema.
Extremely rare effects: jaundice due to toxic hepatitis, joint pain, hematuria, memory loss, malignant exudative erythema. They are observed less frequently than 1 case per 10,000 patients. A frequent effect is also possible - an increase in glycemia and the development of the second type of diabetes mellitus. Side effects are dose-dependent, and their frequency increases with increasing dosage. With an increase in the daily dose by half, the effectiveness will increase only by 6-10%.
Features of the integrated interaction of Mertenil
Some drugs are characterized by an increase in toxicity or a decrease in effectiveness while using Mertenil. Analogs, reviews of specialists about which confirm this trend, are also characterized by important drug interactions. The combined use of Mertenil and Cyclosporin is prohibited due to a more than 7-fold increase in the plasma concentration of statin.
All rosuvastatin preparations enhance the effect of any coumarin anticoagulants, which requires INR control and their repeated correction. In the treatment of HIV, it is not recommended to simultaneously use Mertenil and protease inhibitors (Lopinavir and others). If treatment with nonabsorbable antacids is necessary, they should be taken 2 hours after the use of statin. With complex treatment, along with drugs that affect the cytochrome system, dose adjustment of Mertenil is not required.
Analogues of Mertenil
Mertenil has few analogues. In total, the domestic pharmacy market presents no more than 10 analogues in composition. The first and highest quality is the "Crestor". This is the original rosuvastatin, which is released by Astrazeneca. There are also a number of other foreign generics of the drug "Crestor". These are “Rosulip”, “Roxer”, “Tevascar”, “Rosart”, “Rosucard”. Medicines such as Akorta and Rosuvastatin Canon, which are almost identical in composition to Mertenil, are Russian analogues. They are produced by domestic pharmaceutical companies.
Review of reviews on the drug "Mertenil"
Patients taking lipid-lowering drugs cannot confirm or deny the effectiveness of a particular drug. However, based on the results of the lipid profile, evaluated by a specialist, it is possible to judge the quality of the drug. "Mertenil" for 3 months in a therapeutic dose normalizes the lipid profile of blood serum. And the clinical effect can be seen after 4-6 weeks. Moreover, due to weak cytochrome hepatic metabolism, it has a small number of drug interactions.
Patients about Mertenil respond positively due to the low incidence of adverse reactions. The use of a simple tablet shell reduces the risk of a local gastrotoxic effect. By the way patients respond, nausea and dyspepsia occur much less frequently than in the case of early statins (Simvastatin and Pravastatin). Moreover, according to the recommendations of cardiologists, Mertenil is marginally inferior to Krestor in terms of effectiveness. Other analogs in composition have similar therapeutic value.