Statins are a group of drugs that lower cholesterol in the blood, i.e. hypolipidemic. They do not act on cholesterol itself, the liver becomes the target, where it is produced. Here statins inhibit the production of the enzyme necessary for the synthesis of cholesterol.
Components of cholesterol are lipoproteins. They come in different densities - very low, low, medium, high. Very low and low density lipoprotein (LDL) is considered harmful and bad. In case of cholesterol metabolism disorders, it is precisely the level of harmful lipoproteins that is increased. They contribute to the appearance of cholesterol plaques in the vessels with all the ensuing complications.
Together with thrombosis and hypertension, atherosclerosis is recognized today as the most dangerous among diseases of the heart and blood vessels. They account for 57% of the causes of death of noncommunicable diseases. According to WHO forecasts, the figure will only increase. Statins lower LDL, and with it the level of total cholesterol. But HDL, high density lipoproteins (good), they increase.
How do statins work?
All statins are similar in their mechanism of action. By their action, they replace the enzyme HMG-CoA reductase, which blocks the production of cholesterol. Therefore, another official name for statins is inhibitors of this enzyme. They increase the number of receptors on the surface of hepatocytes that can capture LDL. Here they fall under the influence of these receptors, and LDL catabolism is enhanced.
The use of statins in the practice of doctors
The history of statins began in 1971. During this time, they were praised, recommended, then overthrown due to side effects, etc. But today they continue to be appointed, created.
In Europe, the USA, statins are the most widely used. According to 95% of Americans, 55% of European patients take statins all the time. In Russia, only 12% of such patients. Russian doctors prescribe statins a hundred times less often than foreign colleagues.
When are statins prescribed?
Indications for use are:
- heart attack and stroke;
- LDL levels above 4.9 mmol / L;
- diabetes.
Statins are also prescribed for preparing for heart surgery and for children, but only after 10 years if they are at risk for early heart attack.
Any increase in cholesterol is not an indication for the purpose. There must be good reasons. Cholesterol should be higher than 5 mmol / L. This is explained by the side effects of statins: they are not completely safe.
The benefits and harms of statins
Taking statins can reduce overall mortality by 20%; from complications of atherosclerosis - by 44%; halve the risk of brain and heart catastrophes.
Statin harm can occur in this way:
- causeless changes in mood, aggression or apathy;
- general weakness;
- neuropathy;
- dyspeptic symptoms;
- myalgia and arthralgia;
- decrease in platelet concentration.
But the main minus is hepatotoxicity.
Classification
Statins are systematized by dose, generation, and origin:
- Generations: 1, 2, 3 and 4 generations. The most advanced is the 4th generation: Rosuvastatin, Pitavastatin. 4-generation statins are the most effective.
- Origin: natural, semi- and synthetic. 4th generation - synthetics. Active ingredient in structure: atorvastatin, rosuvastatin, pitavastatin.
- Doses: high, medium and low dose. Here are some of the 4th generation statins that are considered the least dangerous: the originals Krestor and Liprimar, but they are the most expensive. With a modest budget, you can buy analogues with a good reputation: Atoris, Rosucard, Tulip, Torvakard. Do not take the cheapest drugs - they are not fully investigated.
Pluses 4 generations
The benefits of a new generation of statins: they lower cholesterol and LDL cholesterol more; they can (but carefully!) be combined with other drugs. Statins of the 4th generation are non-toxic. Side effects are rare.
Rosuvastatin or Rosulip
This drug is considered the most powerful today. It is prescribed in the most advanced cases with the ineffectiveness of other means. “Rosuvastatin” is 2 times stronger than “Atorvastatin”, “Simvastatin” - 4 times, “Lovastatin” - 8.
The fundamental difference between statins of the 4th generation is their ability to level the C-reactive protein, which according to recent studies plays a role in the onset of atherosclerosis along with cholesterol. But only Ruzolip has such a property.
Contraindications
Contraindications include:
- allergy;
- intolerance to the components of the drug;
- severe liver and kidney disease;
- problems with lactose;
- diseases of the spine and joints;
- intake of cyclosporine;
- diseases of the liver and kidneys in the acute phase;
- myopathy.
They are not assigned:
- minors (exception - genetically elevated cholesterol);
- pregnant, lactating;
- women planning a conception.
When taking statins, you need to reduce physical activity, because with them the muscles are injured and strong myalgias appear. In these cases, you can recommend taking coenzyme Q-10. It is believed that statins can lead to type 1 diabetes. But it is scientifically proven that a slight increase in the incidence is due to the initial predisposition of some people to the development of diabetes.
The drug "Rosulip" ("Rosuvastatin")
INN: Golimumab, Rosuvastin.
Pharmacological group: hypolipidemic, hypocholesterolemic and hypotriglyceridemic agent. HMG-CoA reductase inhibitor. The action is the longest.
Manufacturer - EGIS, Hungary. The trade name is Rosulip®, Rosulip® Plus. Dosage form - tablets of 10 mg, 20 mg, 40 mg.
Structure
According to the dose, the rosulip tablet may contain 5.34 mg, 10.68 mg, 21.36 mg or 42.72 mg of rosuvastatin zinc, which is equivalent to 5 mg, 10 mg, 20 mg, 40 mg of the active substance, rosuvastatin, respectively. Excipients are lactose monohydrate, povidone, magnesium stearate. Its average price is 500 rubles.
Pharmacokinetics
When taking the pill, the concentration of statin becomes maximum after 5 hours.
Bioavailability (digestibility) is about 20%. Rosuvastatin is metabolized by the liver, where 90% of it binds to plasma protein albumin.
Rosuvastatin inhibits more than 90% of HMG-CoA reductases. About 90% of the dose is excreted in the feces; 5% of the dose - with urine. The plasma half-life is approximately 19 hours. This time does not depend on the dose.
Kidney pathology
Moderate violations on the content of "Ruzolip" in blood plasma do not affect. In severe renal impairment with a slowdown in excretory function, the concentration of "Rosuvastatin" and its metabolite increases up to 9 times. The effect of taking occurs in the first week, after 2 weeks - it is already at the level of 90%. By week 4, the maximum dose is stabilized and maintained with regular use.
Application and dosage
Instructions for use "Rosulip" states that the drug is selected only by a doctor! The time of admission is not associated with the time of day and food. Reception should be combined with a diet low in cholesterol. The selection of doses is always individual, there is no template.
Age and gender are not significant. Race: the Mongoloid race "Rosulip" in the blood at a maximum of 2 times higher than that of Europeans.
Hypercholesterolemia
The initial dose for those receiving a different statin or not taking statins at all is 5 mg or 10 mg once a day. If necessary, increase it after a month. The maximum dose of 40 mg is possible only with severe hypercholesterolemia and with the risk of heart attack, if there was no result from 20 mg.
Dosage
For the prevention of heart disease, 20 mg / day is used. The recommended initial dose of the drug "Rosulip" according to the instructions for patients after 70 years does not exceed 5 mg.
In case of renal impairment, treatment begins with 5 mg. Already with moderate renal failure, it cannot be increased. In severe renal failure, it is not prescribed at all.
Undesirable effects from the liver: sometimes a dose-dependent increase in liver enzymes may be noted, but it is transient.
Side effects
Occur with prolonged use in large doses. They are removed with a decrease in dose.
- Frequent - the frequency is considered to be from 1 to 10 or 100 people: cephalgia, dizziness, weakness, constipation and nausea, type 1 diabetes.
- Infrequent (from> 1/1000 to <1/100): allergic rash.
- Rare (1 case per 10 thousand patients): a decrease in platelets, myositis, an increase in liver enzymes and amylase; pancreatitis
- Very rare (<1/10000): memory loss, neuropathy, hepatitis, joint pain and hematuria, gynecomastia.
- Overdose - with it, the symptoms of side effects intensify. The treatment is only symptomatic.
There are no antidotes. Hemodialysis has no effect.
Analogues of the drug "Rosulip"
Analogs of this medicine make up a large group. It is interesting that they can be classified and the analogue does not always guarantee the same effect with the original.
For example, if the analogues are selected in composition (it is the same), then the doses may be different. Instructions for use of analogues of "Rosulip" in such a group will be identical. And the analogues themselves are called complete: they are equivalent to the original in everything. In other words, the full analogues of Rosulip are identical in composition and form of release. ATX code is the same for them. These include 5 drugs: Mertenil, Akorta, Suvardio, Rosistark, Tevastor.
Group analogues of this medication ("Rosulip") are not equivalent pharmacologically according to the indications and method of use. They have only a similar mechanism of action, effect, side symptoms. The analogues found have a similarity in ATX at level 4. These are 15 drugs: Etset, Liprimar, Atorvakor, Tulip, Vabadin, Vastatin, Vazilip, Livastor, Pravyhol, Torvakard, Lovastatin, Simvastatin "," Zokor "," Astin "," Vazoklin ".
Nosological analogues of "Rosulip" have a different composition, but are similar in indications. The found analogues have a match for level 3 ATX. There are 9 such drugs: Omacor, Tricor, Omega-3, Angionorm, Lopid, Ravisol, Ezetrol, Epadol Neo, Revight.
Just found 29 analogues of Rosulip. The cheapest are Zokor and Atorvakor. The most popular are Etset and Mertenil.
"Rustor" - the Russian analogue of "Rosulip" 10 mg. The cost is higher than the original. It has been produced since 2014. Vazilip, Suvardio, Krestor, Tevastor, Rozistark, etc., are analogues with such a dosage.
Analogues of "Rosulip" 20 mg - "Akorta", "Suvardio", "Mertenil", "Rosart", "Rosistark", "Roxer".
"Rosulip Plus" - 10 mg capsules. Contain rosuvastatin and ezetimibe, have a similar therapeutic effect. Manufacturer: Egis, Hungary.
Concerning "Rosulip Plus" - analogues of the full group were not found. There are only analogues for active substances.
Analogue Availability
The highest price for the drug "Crestor". It is clinically tested, but it is not widely available to the general population. Generics are popular in Russia, which differ from the original only in auxiliary components. Rosulip is also produced by Russian companies; they are advantageous in price, but little studied. Popular among them are Rosuvastatin Canon and Akorta. Less in the absence of dosage of 5 mg.
Reviews
Reviews about the analogues of "Rosulip" and about the drug itself in most cases indicate excellent results and tolerance. Some talk about side effects, others note constant nausea at a dose of 20 mg and the absence of such symptoms when the dose is reduced to 10 mg; still others did not notice a side effect and the drug was well tolerated.
But all in one are unanimous: "Ruzolip" must be combined with a hypocholesterol diet, otherwise there will be no effect. The downside is the high cost of drugs. Among the advantages in many reviews, normalization of metabolism and weight loss, improvement of well-being and appearance are noted.
Doctors in the reviews noted a decrease in cholesterol in the analyzes after a week of use when combined with a diet. This creates the prerequisites for the widespread use of the drug.