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Product Name: Rosuvastatin

Generic Name: Rosuvastatin

Common Brands: Crestor

Pharmaceutical Categories: Cardio, Blood Pressure, Cholesterol

Here is a list of pharma shops where you can buy Rosuvastatin online, order cheap and qualitative Rosuvastatin, purchase brand or generic Rosuvastatin, compare pharmacy drug prices and cost of medications from popular and trusted online pharmacies and drugstores selling this or related pharmaceutical products:


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  • PHARMA SHOP
  • Crestor tablets 10 mg
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  • Rosuvastatin tablets 10 mg
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  • Here is an additional general information about this medication active ingredient rosuvastatin:

    Pharmacological action

    Rosuvastatin is a lipid-lowering statin drug, an inhibitor of HMG-CoA reductase. By the principle of competitive antagonism statin molecule binds to a receptor that part of coenzyme A, which attaches the enzyme. The inhibition of HMG-CoA reductase leads to a series of sequential reactions that result in reduced intracellular cholesterol content and is a compensatory increase in activity of LDL receptors and thus accelerate the catabolism of LDL cholesterol.
    Lipid-lowering effect of statins is associated with lower levels of total cholesterol by LDL-C. Reduction in LDL cholesterol is dose-dependent and is not linear, but exponential.
    Statins do not affect the activity of lipoprotein lipase and hepatic, no significant effect on the synthesis and catabolism of free fatty acids, so their effect on triglycerides and again vicariously through their main effects on reducing LDL-C.
    A moderate reduction in triglycerides in the treatment of statins appears to be associated with expression of remnantnyh (apo E) receptor on the surface of hepatocytes involved in the catabolism LPPP, which include those of about 30% of the TG.
    In addition to lipid-lowering actions, statins have beneficial effects in endothelial dysfunction (pre-clinical sign of early atherosclerosis) in the vascular wall, the state of atheroma, improves blood rheology, have antioxidant, antiproliferative properties.

    Pharmacokinetics

    After oral administration of Rosuvastatin Cmax plasma levels achieved approximately 5 hours. The bioavailability is approximately 20%.
    Rosuvastatin is accumulated in the liver. Binding to plasma proteins (mainly albumin) is approximately 90%. This medication is biotransformed to a small extent (10%), being non-core substrate for cytochrome P450 isoenzymes.
    About 90% of the dose rosuvastatin is excreted unchanged in the feces. The remaining part is excreted in the urine. Plasma T1/2 is about 19 hours. T1/2 does not change with increasing dose.
    A systemic exposure increases in proportion to rosuvastatin dose.


    Why is Rosuvastatin prescribed?

    Hypercholesterolemia (type IIa, heterozygous hypercholesterolemia including familial) or mixed hypercholesterolemia (type IIb) as an adjunct to diet, when diet and other non-pharmacological treatments (eg exercise, weight loss) are not sufficient. Family homozygous hypercholesterolemia as an adjunct to diet and other cholesterol-lowering therapy or in cases where such therapy is not suitable for a patient.

    Dosage and administration

    Rosuvastatin is taken orally. The recommended starting dose is 10 mg 1 time / day. If necessary, the dose may be increased to 20 mg after 4 weeks. The Dose increasing up to 40 mg may be only in patients with severe hypercholesterolaemia and at high risk for cardiovascular events (especially in patients with familial hypercholesterolemia) for lack of efficacy at 20 mg and provided medical supervision.

    Rosuvastatin side effects, adverse reactions

    Central nervous system: common - headache, dizziness, asthenic syndrome, perhaps - anxiety, depression, insomnia, neuralgia, paresthesia.
    Digestive system: Common: - constipation, nausea, abdominal pain; possible - a reversible dose-dependent transient increase in liver enzymes, dyspepsia (including diarrhea, flatulence, vomiting), gastritis, gastroenteritis.
    Respiratory system: common - sore throat, perhaps - rhinitis, sinusitis, asthma, bronchitis, cough, dyspnea, pneumonia.
    Cardiovascular system: possible - angina, increased blood pressure, palpitations, vasodilatation.
    Musculoskeletal system: frequently - myalgia; possible - arthralgia, arthritis, muscular hypertonicity, back pain, abnormal limb gem (with no damage); rarely - myopathy, rhabdomyolysis (in conjunction with impaired renal function, while taking the drug at a dose of 40 mg).
    Urinary system: tubular proteinuria (less than 1% of cases - for doses of 10 mg and 20 mg, 3% of cases - for a dose of 40 mg); possible - peripheral edema (hands, feet, ankles, legs), abdominal pain, urinary tract infections.
    Allergic reactions: possible - a skin rash, itching, rarely - angioedema.
    Laboratory parameters: transient dose-dependent increase in activity of creatine kinase (CK activity with an increase of more than 5 times the ULN therapy should be temporarily suspended).
    Other: often - asthenic syndrome, perhaps - accidental injury, anemia, chest pain, diabetes, ecchymosis, flu syndrome, periodontal abscess.

    Rosuvastatin contraindications

    Liver disease in active phase (including the persistent increase in liver enzymes or any increase in the activity of transaminases more than 3 times compared to CAH), marked renal impairment (creatinine clearance < 30 ml / min), myopathy, concomitant use of cyclosporine, pregnancy, lactation (breastfeeding), women of childbearing age not using adequate contraceptive methods, childhood and adolescence to 18 years (since the efficacy and safety have not been established), hypersensitivity to rosuvastatin.

    Using during pregnancy and breastfeeding

    Rosuvastatin is contraindicated during pregnancy and lactation.
    Do not use in women of reproductive age not using reliable methods of contraception.
    Category of the fetus by FDA - X.

    Special instructions

    Be wary of the presence of risk factors for rhabdomyolysis (including renal failure, hypothyroidism, personal or family history of hereditary muscle disease and a prior history of muscular toxicity with other inhibitors of HMG-CoA reductase inhibitors or fibrates), chronic alcoholism, patients older than 65 years, with liver disease in the history of sepsis, hypotension, during extensive surgical procedures, trauma, severe metabolic or endocrine electrolyte disturbances, and uncontrolled epilepsy in people of asian descent (chinese, japanese).
    A therapy with Rosuvastatin should be discontinued if CK levels significantly increased (more than 5 times compared with CAH), or if muscle symptoms are pronounced and cause daily discomfort.
    For taking rosuvastatin in dose 40 mg it is recommended to monitor indicators of kidney function.
    In most cases, proteinuria decreases or disappears during therapy and no means of acute or progression of existing kidney disease.
    It is recommended that the definition of liver function before therapy and 3 months after initiation of therapy. The use of rosuvastatin should stop or reduce the dose if the level of transaminase activity in serum is 3 times the ULN.
    In patients with hypercholesterolemia due to hypothyroidism or nephrotic syndrome, treatment of major diseases should be performed prior to treatment with rosuvastatin.
    During the occupation of potentially dangerous activities, patients should be aware during therapy that dizziness will may occur.

    Rosuvastatin drug interactions

    When this drug applied simultaneously with:
    - cyclosporine AUC of rosuvastatin was on average 7 times higher than the value that was observed in healthy volunteers, the plasma concentration of cyclosporine is not changed.
    - gemfibrozil increases 2-fold in plasma Cmax and AUC of rosuvastatin.
    - antacids that contain aluminum and magnesium hydroxide, leads to a decrease in plasma concentrations of Rosuvastatin by 50%. This effect is less pronounced when antacids are used within 2 h after administration of rosuvastatin (a clinical significance is unknown).
    - erythromycin reduces the rosuvastatin AUC by 20% and rosuvastatin Cmax by 30% (probably due to increased intestinal motility caused by erythromycin reception).
    - oral contraceptives increases the AUC of ethinyl estradiol and norgestrel AUC of 26% and 34% respectively. Initiation of therapy with rosuvastatin or increasing the dose of the drug in patients receiving both vitamin K antagonists (eg, warfarin) may lead to an increase in prothrombin time and INR, and the abolition or reduction of the dose rosuvastatin can cause a decrease in INR (in such cases, monitoring of INR).
    Gemfibrozil, other fibrates and lipid lowering doses of niacin (> 1 g / day) increased risk of myopathy during concomitant use with other inhibitors of HMG-CoA reductase is possible due to the fact that they can cause myopathy and when used as monotherapy.
    The combined use of rosuvastatin and itraconazole (an inhibitor of CYP3A4) increases the AUC rosuvastatin by 28% (clinically insignificant).

    Rosuvastatin in case of emergency / overdose

    Treatment: symptomatic, requires monitoring of liver function and activity of CK, no specific antidote exists, hemodialysis is ineffective.

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