• Code CAS
Most popular brand: Crestor
Active ingredient: Rosuvastatin
Available dosage forms: 5, 10, 20 mg
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Rosuvastatin general information
In conclusion, we can say, should you be taking flomax, and notice the aforementioned unwanted side effects, don’t delay in contacting your doctor to elucidate the scenario, and stop the long-term ill results. Inform your doctor if you’re taking different medicines, with the purpose to stop adverse drug interactions. There could be other unreported side outcomes. This ought to encourage you to really go on compiling reward points to be able to shop your intended drugs.
Here’s a list of its own side results. If taken in accordance with the recommended doses, folic acid will not cause any side consequences. Side effects aren’t likely to occur whether that vitamin is taken in accordance with the recommended dietary allowance. So as to trim the awful cholesterol, statins are prescribed.
The individual may suffer with akathisia, a condition where the person cannot stay still at the same place. The individual might feel tired constantly, and even drowsy in some instances. In rare cases, an individual may feel disoriented, leading to poor coordination. As previously mentioned, if any one of the adverse effects are unusually severe or start to cause you to feel very uncomfortable, get in touch with your physician immediately.
Statin medications, famously known as HMG-CoA reductase inhibitors, are among the most frequent pharmaceutical drugs prescribed to patients. Research suggests an overdose of the vitamin might raise the risk of coronary attack in people who already have heart difficulties. Continued use of the drug within the face of the marked growth of liver enzymes can lead to liver damage. It may likewise have an impact on the epidermis, which makes it paler than usual.
This is among the most frequent fallouts of sertraline in women. In rare cases, it might result in impotency. A number of these drugs in many cases are obtainable in generic forms. Thus far, studies never have revealed any life-threatening side effects that’s good news for the health care fraternity and patients alike.
While statins are incredibly effective in treating cholesterol levels, the issue arises of statin side results. Besides lowering cholesterol, statin drugs have many different other positive aspects, particularly for individuals which have heart disease. Since the effect differs in various people and in various statins, the physician may recommend another statin. They’re a category of drugs that are employed to lessen the degree of plasma cholesterol.
In these passages, we’re going to talk about the side effects of sertraline observed in women. Generally, the physician suggests to lessen the dose or might even recommend to discontinue the medication entirely. The side effects can be mild or severe, conditioned upon the age and total well-being of the patient. Refrain from intake of alcohol or any kind of sedative in order to avoid complications.
Carnitine can play a significant role in lessening the degree of cholesterol, notably the harmful LDL cholesterol within the body. Although the tolerable upper intake level hasn’t been established, it would absolutely be best to take vitamin B12 in accordance with the RDA. Therefore, statins are also called HMG-CoA reductase inhibitors. There are some fallouts observed as a result of withdrawal of sertraline.
Iron deficiency might be observed in lots of folks, caused if their diet lacks the essential nutrients, especially iron. An excessive consumption of lysine during a lengthy time is, in addition, believed to enhance the degree of cholesterol and triglycerides in the entire body. To stop cardiovascular disease, cancer, arteriosclerosis and other ailments linked with LDL and VLDL, you can regulate your diet plan and prevent those foods which are quite full of cholesterol. Ferrous sulfate alone cannot fulfill the iron demands of the body.
BPH is an ailment about the prostate gland, a crucial gland within the male reproductive system which surrounds the urethra. Intake of sertraline at the exact time of pregnancy may cause some birth defects within the baby. In conclusion, lysine is a key amino acid that plays a crucial role in lots of crucial life processes. L-lysine or lysine is a fundamental amino acid, which means it cannot really be synthesized within the human body and hence, must be taken from foods or supplements.
The most ordinary side effect of chondroitin, when it’s consumed separately is hair thinning. They decrease the inflammation connected with arthritis. Lysine supplements can likewise be required in some specific medical conditions which cause protein loss, including large wounds and burns. As it’s an important amino acid, its deficiency can inhibit the standard rate of rise and development.
Serotonin is among those chemicals that’s produced within the central nervous system and plays an extremely important function in transmitting signals between nerve cells, therefore it is also known as a neurotransmitter. An overdose of lysine supplement might lead to nausea, abdominal cramps, stomach malady, and diarrhea. It’s also observed that if a tiny volume of sertraline goes to the baby through breastfeeding, it might result in a few serious complications. There could even be associated swelling on the face, within the mouth, along with the lips.
Rosuvastatin (Rosuvastatin): instruction, and the use of a formula
Gross – formula
Therapeutic agents Rosuvastatin
The typical clinical – pharmacological Article 1
Pharmacological action Lipid-lowering drug, a selective competitive inhibitor of HMG -. CoA – reductase that converts 3 – hydroxy – 3 – metilglutarilKoA to mevalonate, a precursor of cholesterol. The main target of the action is the liver, where it is carried out the synthesis of cholesterol and catabolism of LDL. It inhibits the activity of HMG – CoA – reductase (90% of the drug circulating in the blood). Increases the number of LDL receptors on the hepatocyte surface, increasing the catabolism of LDL and a seizure. which leads to inhibition of the synthesis of VLDL. reducing the total number of VLDL and LDL. It reduces the concentration of cholesterol – LDL. cholesterol – neLPVP, VLDL cholesterol. total cholesterol, triglycerides, TG – VLDL. apolipoprotein B (apoB), the ratio of cholesterol – LDL / cholesterol – HDL. total cholesterol / cholesterol – HDL. Cholesterol – neLPVP / cholesterol – HDL. ApoB / ApoA – I, increases the concentration of cholesterol – HDL. ApoA – I. lipid-lowering effect directly proportional to the administered dose. The therapeutic effect occurs within 1 week after initiation of therapy, 2 weeks up to 90% of the maximum, the maximum effect is usually achieved by 4 weeks and then remains constant. It is effective in adults with hypercholesterolaemia, with or without hypertriglyceridemia (regardless of race, sex or age), including: in patients with diabetes mellitus and familial hypercholesterolemia. An additive effect was seen in combination with fenofibrate (in decreasing triglyceride concentration) and nicotinic acid (for reducing the concentration of cholesterol – HDL).
Pharmacokinetics Bioavailability .; 20%. Food reduces the rate of absorption. Relationship to plasma proteins (mainly albumin) ; 90%. T C max ; 3 –. 5 hours, it crosses the placental barrier. It accumulates in the liver. The volume of distribution ; 134 l. Metabolized 10% of the administered dose in the liver. As with other inhibitors of HMG -. CoA – reductase in the liver capture process involved preparation specific membrane transporter of cholesterol, performs an important role in hepatic its elimination. It is shown that rosuvastatin is a non-core substrate for the metabolic enzymes cytochrome P450 system. The main isoenzyme involved in the metabolism of rosuvastatin is CYP2C9. Enzymes CYP2C19. CYP3A4. CYP2D6 in the metabolism involved to a lesser extent. The main metabolite ; N – dismetil which has 1/6 – 1/2 rosuvastatin activity; lactone metabolites are pharmacologically inactive. T 1/2 ; 19 hours (no change with increasing dose). The geometric mean plasma clearance ; 50 l / h. Write mainly in unchanged form (90%) in faeces (including adsorbed and unadsorbed rosuvastatin); the remainder of the ; urine. Not reported by hemodialysis. Gender and age did not have a clinically meaningful effect on the pharmacokinetics of rosuvastatin.
The pharmacokinetic parameters depend on the race: the AUC, the Japanese and Chinese 2 times higher than that of people in Europe and North America. In patients with mild to moderate renal insufficiency, the plasma concentration of rosuvastatin or the N – dismetila does not change significantly. In patients with severe renal failure (creatinine clearance < 30 ml / min), plasma concentrations of rosuvastatin in the above 3 times, and N – dismetila ; 9 times than in healthy volunteers. plasma rosuvastatin concentrations in patients undergoing hemodialysis, approximately 50% higher than in healthy volunteers. In patients with different stages of liver failure with the score of 7 or less on the scale of Child – Pugh revealed no increase in T 1/2 rosuvastatin; 2 patients with a score of 8 and 9 on the scale of Child – Pugh noted lengthening T 1/2 2 times. The experience of the drug in patients with more severe hepatic impairment is not.
Indications. Primary hypercholesterolaemia (type IIa including familial heterozygous hypercholesterolemia) or mixed hypercholesterolaemia (type IIb) as an adjunct to diet when diet and others. Non-drug therapies (physical exercise, weight reduction body) is insufficient. Familial homozygous hypercholesterolemia as an adjunct to diet and other holesterinsnizhayuschey therapy (LDL – apheresis). Or in cases where the patient does not fit such therapy.
Contra. Hypersensitivity, liver disease in the active phase (including a persistent increase in activity of “liver” transaminases, as well as any increase in the activity of “liver” transaminases in the serum of more than 3 times compared with the upper limit of normal), marked renal impairment (creatinine clearance < 30 ml / min), myopathy, concomitant use of cyclosporine, pregnancy, lactation; women of childbearing age not using adequate methods of contraception; age of 18 years (effectiveness and safety have not been established).
with caution. Renal failure, hypothyroidism, personal or family history of hereditary muscular diseases and previous medical history of muscle toxicity when using OE HMG – CoA – reductase inhibitors or fibrates), alcohol dependence, age 65 age, history of liver disease, sepsis, hypotension, extensive surgery, trauma, severe metabolic, endocrine, or electrolyte disturbances, proteinuria, uncontrolled epilepsy, patients of Asian race (Japanese and Chinese).
Category effects on the fetus. X
Dosing. Inside, the tablet not chewed or crushed, swallowed whole with water, can be received at any time of the day regardless of the meal. The recommended starting dose of ; 1 to 10 mg once a day; if necessary, the dose may be increased to 20 mg every 4 weeks; increasing the dose to 40 mg is possible only under medical supervision in patients with severe homozygous familial hypercholesterolemia with high risk of cardio – vascular complications (especially in patients with familial hypercholesterolaemia), who do not achieve the desired result of therapy when receiving a dose of 20 mg.
Patients with risk factors for myopathy starting dose should be 5 mg.
In the appointment of gemfibrazilom rosuvastatin dose should not exceed 10 mg / day.
When kidney failure mild or moderate severity, as well as in the elderly Dosage adjustment is not required.
The experience of the drug in patients with hepatic insufficiency above 9 on a scale of Childe – Social missing.
Side effects The incidence of adverse events is dose-dependent: common (1 – 10%), less frequently (0,1 – 1%), rarely (0,01 – 0,1% ).
From the nervous system: often ; headache, dizziness, asthenic syndrome; less frequently ; anxiety, depression, insomnia, neuralgia, paresthesia.
On the part of the digestive tract. frequently ; constipation, nausea, abdominal pain; Frequency not known ; reversible transient dose-dependent increase in the activity of “liver” transaminases; less frequently ; dyspepsia (including diarrhea, flatulence, vomiting), gastritis, gastroenteritis.
With the respiratory system: often ; pharyngitis; less frequently ; rhinitis, sinusitis, asthma, bronchitis, cough, dyspnea, pneumonia.
From the heart rate. less frequently ; angina pectoris, increased blood pressure. palpitation, vasodilatation.
From the musculo – skeletal system: frequently ; myalgia; less frequently ; arthralgia, arthritis, muscular hypertonicity, back pain, pathological fracture limbs (without damage); rare ; myopathy, rhabdomyolysis (both with impaired renal function, in patients receiving the drug at a dose of 40 mg).
From the urinary system: tubular proteinuria (in less than 1% of the time ; for doses of 10 mg and 20 mg, 3% of the time ; for a dose of 40 mg); less frequently ; peripheral edema (hands, feet, ankles, legs), pain in the abdomen, urinary tract infection.
Allergic reactions: less often ; skin rash, itching; rare ; angioedema.
From the laboratory parameters: transient dose-related increase in CK activity (with an increase in activity of CK more than 5 times in comparison with the upper limit of normal therapy should be temporarily suspended).
Others: less frequently ; accidental injury, anemia, chest pain, diabetes, ecchymosis, flu-like symptoms, periodontal abscess.
Overdose Treatment: symptomatic, requires monitoring of liver function and CPK;. There is no specific antidote, hemodialysis is ineffective.
Interactions. Does not affect the plasma concentration of cyclosporine. Cyclosporin enhances the effect of rosuvastatin (slows its excretion, AUC increased by 7 times, C max ; 11-fold), vitamin K antagonists (including warfarin, may lead to an increase of the prothrombin time is recommended its monitoring).
Gemfibrozil increases the effect of rosuvastatin (increases C max and AUC 2-fold).
Antacids containing Al 3+ and Mg 2+. lead to a decrease in rosuvastatin plasma concentration of approximately 50% (antacids should be used within 2 hours after taking rosuvastatin, the clinical significance of this interaction has not been studied).
Erythromycin increases the motility of the gastrointestinal tract. which reduces the effect of rosuvastatin (AUC reduces it by 20% and P max 30%). Do effect of oral contraceptives (increases the AUC of ethinyl estradiol and norgestrel by 26% and 34%, respectively, which should be considered when selecting oral contraceptive doses). Pharmacokinetic data on the simultaneous use of rosuvastatin and hormone replacement therapy are not available, therefore we can not exclude a similar effect and the use of this combination.
It is not expected clinically significant interaction with digoxin rosuvastatin or fenofibrate..
Gemfibrozil, other fibrates and lipid-lowering doses of nicotinic acid (high dose or equivalent to 1 g / day) increase the risk of myopathy with the simultaneous use with other inhibitors of HMG -. CoA – reductase, possibly due to the fact that they can cause myopathy when used as monotherapy.
The results of research in vivo and in vitro have shown that rosuvastatin is neither an inhibitor nor an inducer of cytochrome P450 enzymes. In addition, non-core rosuvastatin is a substrate for these enzymes. There were no clinically significant interaction between rosuvastatin and fluconazole (an inhibitor of CYP2C9 and CYP3A4), and ketoconazole (CYP2A6 inhibitor and a CYP3A4). The combined use of rosuvastatin and itraconazole (CYP3A4 inhibitor) increases the AUC of rosuvastatin by 28% (clinically insignificant). Thus it is not expected interaction associated with metabolism by cytochrome P450.
The simultaneous use of drugs. reduces the concentration of endogenous steroid hormones (including cimetidine, ketoconazole, spironolactone), increases the risk of reduction of endogenous steroid hormones.
Special instructions. Before initiation of therapy and throughout the treatment period should be observed standard lipid-lowering diet. During treatment every 2 – 4 weeks should monitor the lipid profile and adjust it according to the dose, if necessary.
The dose of 40 mg is contraindicated in patients with risk factors for rhabdomyolysis (kidney failure moderate (creatinine clearance less than 60 mL / min), hypothyroidism, personal or family history of muscle diseases miotoksichnost in patients receiving other HMG inhibitors -. CoA – reductase or fibrate, alcohol abuse, state, accompanied by an increase in the concentration of the drug in the systemic circulation, concomitant use of fibrates, Asian race patients).
In patients taking the drug at a dose of 40 mg is recommended to monitor renal function.
The definition of activity of CK should not be carried out after intense exercise or in the presence of others. The possible reasons for the increase CK. which may lead to misinterpretation of the results. When the source CK 5 times upper limit of normal at 5 – 7 days should be a re-measurement. Do not start treatment, if a second test confirms the initial increased CPK activity of more than 5 times in comparison with the upper limit of normal.
In patients with existing risk factors for rhabdomyolysis is necessary to consider the balance of risk and potential benefits of therapy and exercise clinical observation throughout the course of treatment.
It is necessary to inform the patient about the need for immediate medical posts about cases of sudden appearance of muscle pain, muscle weakness or cramps, especially in combination with malaise and fever. These patients should be monitored activity of CK. Therapy should be discontinued if CK activity increased more than 5 times compared with the upper limit of normal, or if symptoms of pronounced muscle and cause discomfort daily (even if CPK activity is not more than 5 times the upper limit of normal). If the symptoms disappear and the activity of CK returns to normal, you should consider re-appointment of the drug or other inhibitors of HMG -. CoA – reductase in smaller doses with careful observation of the patient. Routine monitoring of creatine kinase activity in the absence of symptoms of rhabdomyolysis is not advisable.
reported an increase in the incidence of myopathy and myositis patients receiving other HMG -. CoA – reductase in combination with the fibric acid derivatives including gemfibrozil, cyclosporin, nicotinic acid, azole antifungals, protease inhibitors and macrolide antibiotics. Gemfibrozil increases the risk of myopathy when combined with the appointment of some inhibitors of HMG – CoA – reductase. Thus it is not recommended to co-administration of rosuvastatin and gemfibrozil. It should be carefully weighed balance of risk and the possible benefits of rosuvastatin with a joint application and fibrates or nicotinic acid.
It is recommended that the definition of indicators of liver function before treatment and at 3 months after initiation of therapy. If the activity of “liver” in serum transaminases exceeding 3 times the upper limit of normal, dose should be reduced or stop taking.
In most cases, proteinuria is reduced or disappears during therapy and means of acute or progression of existing renal disease.
When combined hypercholesterolemia and hypothyroidism or nephrotic syndrome, the underlying disease therapy should be performed prior to initiating treatment with rosuvastatin.
Use caution while driving or work related to the high concentration of attention and psychomotor reaction (during treatment can occur dizziness).
Women of childbearing age should use adequate contraception methods. Since cholesterol and substances synthesized from cholesterol are important for the development of the fetus, the potential risk of inhibition of HMG – CoA reductase inhibitors exceeds the benefit from the use of the drug during pregnancy. The study in rats (application in doses of 2 – 50 mg / kg / day) revealed decreased fetal mass, bone ossification delay fetal reduction progeny survival. In case of pregnancy during therapy, the drug should be discontinued immediately. Data on the allocation of rosuvastatin with women no milk, so breast-feeding should be discontinued.
 National Register of Medicinal Products. Official publication: in 2 v. – M. Medical Council, 2009 – Volume 2, Part 1 – 568 p .; Part 2 -. 560
interactions with other active substances
Trading names of drugs with working substance