Among the variety of lipid-lowering drugs, the most effective today are drugs that belong to the group of statins. Rosuvastatin is a modern representative of this group, the efficacy and safety of which have been confirmed after numerous tests and examinations of people who suffered from dyslipidemia. Find out how it works.
What Is Rosuvastatin and How Does It Work?
The drug is available in dosage of 5, 10, 20 mg. To purchase the drug in the pharmacy network, you need a prescription from a doctor. The principle of the drug is competitive antagonism of the statin molecule. It reacts with the coenzyme A receptor element, and the second part of the active substance molecule contributes to the conversion of hydroxymethylglutarate to the intermediate product mevalonate.
Such a transformation triggers a series of successive chemical reactions. The final product is a decrease in the dimension of cholesterol in the cells, and rather, the compensatory procedure of changing over low-thickness lipoproteins turns out to be progressively dynamic. In the meantime with great cholesterol changes don't happen on the grounds that this is a medication of the specific activity. This is one of the advantages of Rosuvastatin contrasted with different medications, which are known for the comparative activity.
The primary medication impact happens because of a decline in the all out cholesterol level, and not the high-thickness lipids, but rather the measure of low-thickness lipoproteins is specially decreased. Decrease of the bad cholesterol occurs.
Rosuvastatin has no effect on lipoprotein and hepatic lipase, and also does not affect the metabolism of fatty acids in the body. At the same time, when taking statins, the level of triglycerides decreases from indirect influence.
In addition to the fact that statins significantly reduce cholesterol levels, they also produce a positive effect if the vascular endothelium is impaired in old age. This is the main preclinical sign of the development of atherosclerosis, that is, at the very moment when the signs of pathology have not yet manifested and the patient does not feel sick, and therefore does not turn to the doctor.
Who Should Start the Course of Therapy?
Check the list of the health problems when Rosuvastatin is usually prescribed for the treatment:
- hypertriglyceridemia (type IV);
- to slow changes, which occur in patients with atherosclerosis;
- to prevent cardiovascular complications like stroke, heart attack, arterial revascularization in adult patients without clinical signs of coronary heart disease.
You are recommended to see a doctor before you start using the drug as it may cause certain side effects.
Does Rosuvastatin Have any Contraindications?
Like any other drug, it has certain contraindications you should check before using it.
- Hypersensitivity to any of the components of the drug;
- serious liver diseases in the active phase;
- patients with severe renal impairment (CC less than 30 ml / min.);
- simultaneous use of cyclosporine;
- children under 18;
- pregnant/breastfeeding females;
- patients predisposed to myotoxic complications;
- patients with lactase deficiency/glucose-galactose malabsorption.
Recommendations You Should Follow When Taking the Drug
As indicated by guidelines, you ought not bite the pill. Rather, gulp down it and wash down with water. The medication can be controlled whenever of the day, paying little respect to the dinner time. It is important to recall that before you begin taking Rosuvastatin, you should start to pursue the standard cholesterol-bringing diet and proceed down to tail it amid the entire time of the recommended treatment. The specialist will endorse the sheltered measurements considering the objective lipid fixation.
Bioavailability is around 20 percent. The primary segment of the medication for the most part aggregates in the liver, and ties with blood proteins - egg whites. Practically the majority of the first medication (about 90%) is discharged in the excrement, and the rest with pee. The half-existence of around 19 hours - this makes it conceivable to take just a single pill of the medication every day. In the event that the pills are taken for quite a while, with great versatility, they don't harmfully affect the body.
Treatment with high dosages of the medication is done under the supervision of a doctor and successive screening of the fundamental pointers of the liver and kidneys. Using Rosuvastatin, great cholesterol adjustment can be accomplished.
Take it with alert in the accompanying cases: after broad careful intercessions; after damage; if the patient has huge metabolic or endocrine issue, just as electrolyte unevenness; in the event that history of epilepsy, which is ineffectively controlled medications.
Things to Keep in Mind Using Rosuvastatin
Choosing Rosuvastatin, you need to take into account some facts below:
- Prolonged treatment with a statin, especially at high doses, suggests regular monitoring of the plasma content of the CPK enzyme (creatine phosphokinase) to prevent diseases of the muscular system, especially with a tendency to myopathy.
- The parallel use of drugs that inhibit the enzyme HMG-CoA reductase requires careful approach and medical monitoring of the patient's condition.
- Before taking statins, the patient should be informed about the possible negative effects on the muscles, so any muscle pain should be the reason for the visit to the doctor.
- Against the background of the drug use, there were isolated cases of myasthenia (muscle weakness), triggered by the synthesis of autoantibodies by the immune system.
- With dose adjustment, as well as every 2-4 weeks, the plasma content of cholesterol and lipids is controlled.
- Before the start of the course and again, after a few weeks, a laboratory analysis of the functional capabilities of the liver is necessary.
- Rosuvastatin has the ability to interact with other drugs, while taking them at the same time, the doctor must be warned before setting up a treatment regimen.
- Since the preparation contains lactose, in case of carbohydrate absorption in the gastrointestinal tract (lactase deficiency, glucose-galactose malabsorption), this feature must be taken into account.
- Statin has a negative effect on glucose uptake, an increase in its plasma concentration contributes to the appearance of type 2 diabetes, a systematic monitoring of its performance is mandatory.
- There is no information on the effect of rosuvastatin on concentration, brain functionality, and the rate of reaction.
What Adverse Reactions to Expect?
- The frequency of side effects is dose-dependent: often (1-10%), less often (0.1-1%), rarely (0.01-0.1%).
- On the part of the nervous system: often - headache, dizziness, asthenic syndrome; less often - anxiety, depression, insomnia, neuralgia, paresthesia.
- On the part of the digestive tract: often - constipation, nausea, abdominal pain; frequency unknown - reversible transient dose-dependent increase in the activity of liver transaminases; less often - dyspepsia (including diarrhea, flatulence, vomiting), gastritis, gastroenteritis.
- On the part of the respiratory system: often - pharyngitis; less often - rhinitis, sinusitis, bronchial asthma, bronchitis, cough, dyspnea, pneumonia. On the part of the heart rate: less often - angina, increased blood pressure, palpitations, vasodilation.
- From the musculoskeletal system: often - myalgia; less often - arthralgia, arthritis, muscle hypertonus, back pain, pathological pearl of a limb (without injuries); rarely - myopathy, rhabdomyolysis (simultaneously with impaired renal function, while receiving the drug in a dose of 40 mg).
- On the part of the urinary system: tubular proteinuria in less than 1% of cases - for doses of 10 and 20 mg; less often - peripheral edema (arms, legs, ankles, legs), lower abdominal pain, urinary tract infections.
- Allergic reactions: less often - skin rash, pruritus; rarely - angioedema.
- From the laboratory indicators: a transient dose-dependent increase in the activity of CPK (with an increase in the activity of CPK more than 5 times compared with the upper limit of the norm, therapy should be temporarily suspended).
- Other: less often - accidental trauma, anemia, chest pain, diabetes, ecchymosis, flu-like syndrome, periodontal abscess.
- Overdose. Treatment: symptomatic, control of liver function and CPK activity is necessary; there is no specific antidote, hemodialysis is ineffective.
When Should You Stop the Drug Therapy?
The patient ought to be educated of the need to quickly answer to the specialist the instances of sudden beginning of muscle torment, muscle shortcoming or fits, particularly in blend with indisposition and fever. In such patients, the dimension of CPK ought to be resolved. Treatment ought to be stopped if the dimension of CPK is altogether expanded (in excess of multiple times contrasted with VGN) or if muscle side effects are articulated and cause day by day inconvenience (regardless of whether the dimension of KFK is multiple times not exactly VGN). In the event that the side effects vanish and the CK level comes back to ordinary, thought ought to be given to reappointment of the medicine or other HMG-CoA reductase inhibitors in littler dosages with watchful observing of the patient.
Researchers plan to continue studies to prove that those patients who follow all the doctor’s prescriptions concerning the drug intake have much better cardiovascular prognosis.