Product Name: Atorvastatin
Common Brand Names: Lipitor
Pharmaceutical Category: Cardio / Blood Pressure / Cholesterol
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There is an additional general information about this medication active ingredient atorvastatin:
Atorvastatin is a lipid-lowering drugs of the statin group. An inhibition of HMG-CoA reductase leads to a series of sequential reactions that result in reduced intracellular cholesterol content and it is a compensatory increase in activity of LDL receptors and thus accelerate the catabolism of LDL cholesterol.
The lipid-lowering effect of statins is associated with lower levels of total cholesterol by LDL-C. The reduction in LDL cholesterol is dose-dependent and is not linear, but exponential. The inhibitory effect of atorvastatin on HMG-CoA reductase by about 70% determined by the activity of its circulating metabolites.
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.
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.
Atorvastatin lowers cholesterol levels in patients with homozygous familial hypercholesterolemia, which is usually not amenable to therapy with lipid-lowering agents.
Atorvastatin is rapidly absorbed from the gastrointestinal tract. The absolute bioavailability is low (about 12%) due to first-pass clearance in gastrointestinal mucosa and / or due to the "first pass" through the liver, predominantly in the scene. Atorvastatin is metabolized with the participation of isoenzyme CYP3A4 to form a number of substances which are inhibitors of HMG-CoA reductase inhibitors.
T1/2 from plasma is about 14 hours, although the T1/2 inhibitor activity of HMG-CoA reductase is approximately 20-30 hours, due to the involvement of active metabolites.
The plasma protein binding is 98%.
Atorvastatin is excreted in the form of metabolites mainly in the bile.
Why is Atorvastatin prescribed?
Primary hypercholesterolemia in ineffectiveness of diet, combined hypercholesterolemia and hypertriglyceridemia, heterozygous and homozygous familial hypercholesterolemia with the ineffectiveness of diet.
Dosage and administration
The treatment by Atorvastatin is with a standard diet for patients with hypercholesterolemia. The dose is determined individually, depending on the initial cholesterol levels. This medication is taken orally. The initial dose is usually 10 mg 1 time / day. The effect is manifested within 2 weeks, and the maximum effect is for 4 weeks. If necessary, the dose can be gradually increased every 4 weeks or more. The maximum daily dose is 80 mg.
Atorvastatin side effects, adverse reactions
Digestive system: constipation, flatulence, dyspepsia, abdominal pain, nausea, diarrhea.
CNS and peripheral nervous system: headache, insomnia.
Other: asthenia, myalgia.
Liver disease in the active phase, increasing the serum transaminase activity more than 3 times of unknown origin, pregnancy, lactation (breastfeeding), hypersensitivity to atorvastatin. Women of reproductive age not using reliable contraception.
Using during pregnancy and breastfeeding
Atorvastatin is contraindicated during pregnancy and lactation (breastfeeding).
It is not known whether atorvastatin is allocated in breast milk. Given the potential for adverse effects in infants, if necessary to use this drug during lactation it should decide on the termination of breastfeeding.
Women of reproductive age during treatment should use adequate contraceptive methods. Atorvastatin may be used in women of childbearing age only if the probability of pregnancy is very low, and the patient informed about the possible risk of treatment for the fetus.
Category of the fetus by FDA - X.
Prior to and during treatment with atorvastatin, especially if symptoms of liver damage, it is necessary to monitor liver function tests. With an increase in transaminase levels it should be monitored their activity up to normalization. If AST or ALT more than 3 times the norm persists, we recommend reducing the dose or withdrawal of atorvastatin.
When prompted during the treatment of symptoms of myopathy it should determine the activity of creatine kinase. If a significant increase in CK levels is preserved, it is recommended to reduce the dose of Atorvastatin or to cancel taking it.
The risk of myopathy during the treatment with atorvastatin increased, while the use of cyclosporine, fibrates, erythromycin, antifungal agents belonging to azoles, and niacin.
There is a likelihood of the following side effects, but not in all cases, a clear link with taking atorvastatin: muscle cramps, myositis, myopathy, paresthesia, peripheral neuropathy, pancreatitis, hepatitis, cholestatic jaundice, anorexia, vomiting, alopecia, pruritus, rash, impotence, hyperglycemia and hypoglycemia.
The children experience of atorvastatin using at a dose of 80 mg / day is restricted.
With careful use Atorvastatin in patients with chronic alcoholism.
Atorvastatin drug interactions
When this drug applied simultaneously with:
- digoxin slightly increased concentration of digoxin in plasma.
- itraconazole greatly increases the concentration of atorvastatin in plasma, apparently due to inhibition of itraconazole its metabolism in the liver that occurs with the participation of isoenzyme CYP3A4; increased risk of myopathy.
- colestipol may decrease the concentration of atorvastatin in plasma, with lipid-lowering effect is enhanced.
- antacids containing magnesium hydroxide and aluminum hydroxide, reduce the concentration of atorvastatin by approximately 35%.
- cyclosporine, fibrates (including gemfibrozil), azole antifungals derivatives, nicotinic acid increases the risk of myopathy.
- erythromycin, clarithromycin moderately increased concentrations of atorvastatin in plasma, increases the risk of myopathy.
- ethinyl estradiol, norethisterone (norethindrone) slightly increases the concentration of ethinyl estradiol, norethisterone and (norethindrone) in blood plasma.
- protease inhibitors increases the concentration of Atorvastatin in plasma, as protease inhibitors are inhibitors of the CYP3A4 isoenzyme.
Diltiazem, verapamil, isradipine inhibit isoenzyme CYP3A4, which participates in the metabolism of Atorvastatin, so that while the use of these calcium channel blockers may increase the concentration of atorvastatin in plasma and increased risk of myopathy.
Atorvastatin in case of emergency / overdose
Treatment: symptomatic and supportive therapy. There is no specific antidote. Hemodialysis is ineffective.