Atorvastatin | atorvastatin tablets coated. 20 mg film 30 pcs. pack
Special Price
$20.58
Regular Price
$28.00
In stock
SKU
BID499830
Release form
Tablets, film-coated white or almost white, round, biconvex in cross section - the core is white or almost white.
Tablets, film-coated white or almost white, round, biconvex in cross section - the core is white or almost white.
Release form
Tablets, film-coated white or almost white, round, biconvex in cross section - the core is white or almost white.
Pharmacological action
Clinical and pharmacological group: Lipid-lowering drug
Pharmacotherapeutic group: Hypolipidemic agent - HMG-CoA reductase inhibitor
Pharmacological action
Hypolipidemic agent from the group of statins. According to the principle of competitive antagonism, the statin molecule binds to that part of the coenzyme A receptor where HMG-CoA reductase is attached. Another part of the statin molecule inhibits the conversion of hydroxymethylglutarate to mevalonate, an intermediate in the synthesis of cholesterol molecules. Inhibition of the activity of HMG-CoA reductase leads to a series of sequential reactions, resulting in a decrease in the intracellular cholesterol content and a compensatory increase in the activity of LDL receptors and, accordingly, accelerated catabolism of LDL cholesterol (Xc).
The hypolipidemic effect of statins is associated with a decrease in total cholesterol due to LDL cholesterol. The decrease in LDL is dose-dependent and is not linear, but exponential. The inhibitory effect of atorvastatin against HMG-CoA reductase is approximately 70% determined by the activity of its circulating metabolites.
Statins do not affect the activity of lipoprotein and hepatic lipases, do not significantly affect the synthesis and catabolism of free fatty acids, therefore, their effect on the level of TG is secondary and indirectly through their main effects in lowering the level of LDL-C. A moderate decrease in the level of TG during treatment with statins is apparently associated with the expression of remnant (apo E) receptors on the surface of hepatocytes involved in catabolism of STDs, which comprise about 30% TG. Compared to other statins (with the exception of rosuvastatin), atorvastatin causes a more pronounced decrease in TG levels.
In addition to lipid-lowering effects, statins have a positive effect on endothelial dysfunction (preclinical sign of early atherosclerosis), on the vascular wall, atheroma state, improve blood rheological properties, have antioxidant, antiproliferative properties.
Atorvastatin lowers cholesterol in patients with homozygous familial hypercholesterolemia, which is usually not amenable to hypolipidemic therapy.
Pharmacokinetics
Atorvastatin is rapidly absorbed from the digestive tract. Absolute bioavailability is low - about 12%, which is due to the presystemic clearance in the gastrointestinal mucosa and / or due to the first passage through the liver, mainly at the site of action.
Atorvastatin is metabolized with the participation of the CYP3A4 isoenzyme to form a number of substances that are inhibitors of HMG-CoA reductase.
T1 / 2 from plasma is about 14 hours, although the T1 / 2 inhibitor of HMG-CoA reductase activity is approximately 20-30 hours, which is due to the participation of active metabolites.
Plasma protein binding is 98%.
Atorvastatin is excreted in the form of metabolites mainly with bile.
Indications
Primary hypercholesterolemia with diet therapy failure, combined hypercholesterolemia and hypertriglyceridemia, heterozygous and homozygous familial hypercholesterolemia with diet therapy failure.
Contraindications
Active liver disease, increased serum transaminases more than 3 times of unknown origin, pregnancy, lactation (breastfeeding), women of reproductive age who do not use reliable contraceptives, increased sensitivity to atorvastatin.
Use during pregnancy and lactation
Atorvastatin is contraindicated in pregnancy and lactation (breastfeeding).
It is not known whether atorvastatin is excreted in breast milk. Given the possibility of adverse events in infants, if necessary, use of the drug during lactation should decide on the termination of breastfeeding.
Women of reproductive age should use adequate contraceptive methods during treatment. Atorvastatin can be used in women of reproductive age only if the probability of pregnancy is very low, and the patient is informed about the possible risk of treatment for the fetus.
Dosage and administration
Treatment is carried out against a standard diet for patients with hypercholesterolemia.
The dose is set individually, depending on the initial level of cholesterol. Take inside. The initial dose is usually 10 mg 1 time / day.
The effect manifests itself within 2 weeks, and the maximum effect - within 4 weeks. If necessary, the dose can be gradually increased with an interval of 4 weeks or more. The maximum daily dose is 80 mg.
Side effects of the
From the nervous system:> 1% - insomnia, dizziness <1% - headache, asthenia, malaise, drowsiness, nightmares, paresthesias, peripheral neuropathy, amnesia, emotional lability, ataxia, facial paralysis, hyperkinesia, migraine, depression, hypesthesia, loss of consciousness.
On the part of the sensory organs: <1% - amblyopia, tinnitus, dryness of the conjunctiva, disturbance of accommodation, hemorrhage in the retina, deafness, glaucoma, parosmia, loss of taste, perversion of taste.
From the cardiovascular system:> 1% - chest pain <1% - palpitations, vasodilation symptoms, orthostatic hypotension, increased blood pressure, phlebitis, arrhythmia, angina pectoris.
From the hemopoietic system: <1% - anemia, lymphadenopathy, thrombocytopenia.
From the respiratory system:> 1% - bronchitis, rhinitis <1% - pneumonia, dyspnea, exacerbation of bronchial asthma, nosebleeds.
From the digestive system:> 1% - nausea < 1% - heartburn, constipation or diarrhea, flatulence, gastralgia, abdominal pain, decreased or increased appetite, dry mouth, belching, dysphagia, vomiting, stomatitis, esophagitis, glossitis, erosive and ulcerative lesions of the oral mucosa, gastroenteritis, hepatitis , biliary colic, cheilitis, duodenal ulcer, pancreatitis, cholestatic jaundice, impaired liver function, rectal bleeding, melena, bleeding gums, tenesmus.
From the musculoskeletal system:> 1% - arthritis <1% - leg muscle cramps, bursitis, tendosynovitis, myositis, myopathy, arthralgia, myalgia, rhabdomyolysis, torticollis, muscle hypertonicity, joint contracture, joint swelling, tendonopathy (in some cases with tendon rupture).
From the genitourinary system:> 1% - urogenital infections, peripheral edema <1% - dysuria (incl. pollakiuria, nocturia, urinary incontinence or urinary retention, imperative urination), leukocyturia, nephritis, hematuria, vaginal bleeding, nephrourolithiasis, metrorrhagia, epididymitis, decreased libido, impotence, impaired ejaculation.
Dermatological reactions:> 1% - alopecia, xeroderma, photosensitivity, increased sweating, eczema, seborrhea, ecchymosis, petechiae.
From the endocrine system: <1% - gynecomastia, mastodynia.
From the side of metabolism: <1% - increase in body weight, exacerbation of gout.
Allergic reactions: <1% - itchy skin, rash, contact dermatitis, rarely - urticaria, angioedema, facial edema, anaphylaxis, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell syndrome )
Laboratory indicators: <1% - hyperglycemia, hypoglycemia, increased serum CPK, albuminuria.
Drug interaction
With the simultaneous use of atorvastatin with digoxin, the concentration of digoxin in the blood plasma slightly increases.
Diltiazem, verapamil, isradipine inhibit the isoenzyme of CYP3A4, which is involved in the metabolism of atorvastatin, therefore, with the simultaneous use of calcium channel blockers, it is possible to increase the concentration of atorvastatin in the blood plasma and increase the risk ofopatia.
With the simultaneous use of itraconazole, the concentration of atorvastatin in the blood plasma increases significantly, apparently due to the inhibition of itraconazole by its metabolism in the liver, which occurs with the participation of the CYP3A4 isoenzyme, increasing the risk of myopathy.
With the simultaneous use of colestipol, a decrease in the concentration of atorvastatin in blood plasma is possible, while the lipid-lowering effect is enhanced.
With the simultaneous use of antacids containing magnesium hydroxide and aluminum hydroxide, reduce the concentration of atorvastatin by about 35%.
With the simultaneous use of cyclosporine, fibrates (including gemfibrozil), antifungal derivatives of azole derivatives, nicotinic acid, the risk of developing myopathy increases.
With the simultaneous use of erythromycin, clarithromycin moderately increases the concentration of atorvastatin in plasma, the risk of developing myopathy increases.
With the simultaneous use of ethinyl estradiol, norethisterone (norethindrone), the concentration of ethinyl estradiol, norethisterone and (norethindrone) in the blood plasma slightly increases.
With the simultaneous use of protease inhibitors, the concentration of atorvastatin in the blood plasma increases, because protease inhibitors are inhibitors of the CYP3A4 isoenzyme.
Active ingredient
Atorvastatin
lekarstvennaja form
tablets
Appointment
for Adults on purpose doctor
Indications
Prophylaxis of heart attacks and strokes, Atherosclerosis
Izvarino Pharma, Russia
Tablets, film-coated white or almost white, round, biconvex in cross section - the core is white or almost white.
Pharmacological action
Clinical and pharmacological group: Lipid-lowering drug
Pharmacotherapeutic group: Hypolipidemic agent - HMG-CoA reductase inhibitor
Pharmacological action
Hypolipidemic agent from the group of statins. According to the principle of competitive antagonism, the statin molecule binds to that part of the coenzyme A receptor where HMG-CoA reductase is attached. Another part of the statin molecule inhibits the conversion of hydroxymethylglutarate to mevalonate, an intermediate in the synthesis of cholesterol molecules. Inhibition of the activity of HMG-CoA reductase leads to a series of sequential reactions, resulting in a decrease in the intracellular cholesterol content and a compensatory increase in the activity of LDL receptors and, accordingly, accelerated catabolism of LDL cholesterol (Xc).
The hypolipidemic effect of statins is associated with a decrease in total cholesterol due to LDL cholesterol. The decrease in LDL is dose-dependent and is not linear, but exponential. The inhibitory effect of atorvastatin against HMG-CoA reductase is approximately 70% determined by the activity of its circulating metabolites.
Statins do not affect the activity of lipoprotein and hepatic lipases, do not significantly affect the synthesis and catabolism of free fatty acids, therefore, their effect on the level of TG is secondary and indirectly through their main effects in lowering the level of LDL-C. A moderate decrease in the level of TG during treatment with statins is apparently associated with the expression of remnant (apo E) receptors on the surface of hepatocytes involved in catabolism of STDs, which comprise about 30% TG. Compared to other statins (with the exception of rosuvastatin), atorvastatin causes a more pronounced decrease in TG levels.
In addition to lipid-lowering effects, statins have a positive effect on endothelial dysfunction (preclinical sign of early atherosclerosis), on the vascular wall, atheroma state, improve blood rheological properties, have antioxidant, antiproliferative properties.
Atorvastatin lowers cholesterol in patients with homozygous familial hypercholesterolemia, which is usually not amenable to hypolipidemic therapy.
Pharmacokinetics
Atorvastatin is rapidly absorbed from the digestive tract. Absolute bioavailability is low - about 12%, which is due to the presystemic clearance in the gastrointestinal mucosa and / or due to the first passage through the liver, mainly at the site of action.
Atorvastatin is metabolized with the participation of the CYP3A4 isoenzyme to form a number of substances that are inhibitors of HMG-CoA reductase.
T1 / 2 from plasma is about 14 hours, although the T1 / 2 inhibitor of HMG-CoA reductase activity is approximately 20-30 hours, which is due to the participation of active metabolites.
Plasma protein binding is 98%.
Atorvastatin is excreted in the form of metabolites mainly with bile.
Indications
Primary hypercholesterolemia with diet therapy failure, combined hypercholesterolemia and hypertriglyceridemia, heterozygous and homozygous familial hypercholesterolemia with diet therapy failure.
Contraindications
Active liver disease, increased serum transaminases more than 3 times of unknown origin, pregnancy, lactation (breastfeeding), women of reproductive age who do not use reliable contraceptives, increased sensitivity to atorvastatin.
Use during pregnancy and lactation
Atorvastatin is contraindicated in pregnancy and lactation (breastfeeding).
It is not known whether atorvastatin is excreted in breast milk. Given the possibility of adverse events in infants, if necessary, use of the drug during lactation should decide on the termination of breastfeeding.
Women of reproductive age should use adequate contraceptive methods during treatment. Atorvastatin can be used in women of reproductive age only if the probability of pregnancy is very low, and the patient is informed about the possible risk of treatment for the fetus.
Dosage and administration
Treatment is carried out against a standard diet for patients with hypercholesterolemia.
The dose is set individually, depending on the initial level of cholesterol. Take inside. The initial dose is usually 10 mg 1 time / day.
The effect manifests itself within 2 weeks, and the maximum effect - within 4 weeks. If necessary, the dose can be gradually increased with an interval of 4 weeks or more. The maximum daily dose is 80 mg.
Side effects of the
From the nervous system:> 1% - insomnia, dizziness <1% - headache, asthenia, malaise, drowsiness, nightmares, paresthesias, peripheral neuropathy, amnesia, emotional lability, ataxia, facial paralysis, hyperkinesia, migraine, depression, hypesthesia, loss of consciousness.
On the part of the sensory organs: <1% - amblyopia, tinnitus, dryness of the conjunctiva, disturbance of accommodation, hemorrhage in the retina, deafness, glaucoma, parosmia, loss of taste, perversion of taste.
From the cardiovascular system:> 1% - chest pain <1% - palpitations, vasodilation symptoms, orthostatic hypotension, increased blood pressure, phlebitis, arrhythmia, angina pectoris.
From the hemopoietic system: <1% - anemia, lymphadenopathy, thrombocytopenia.
From the respiratory system:> 1% - bronchitis, rhinitis <1% - pneumonia, dyspnea, exacerbation of bronchial asthma, nosebleeds.
From the digestive system:> 1% - nausea < 1% - heartburn, constipation or diarrhea, flatulence, gastralgia, abdominal pain, decreased or increased appetite, dry mouth, belching, dysphagia, vomiting, stomatitis, esophagitis, glossitis, erosive and ulcerative lesions of the oral mucosa, gastroenteritis, hepatitis , biliary colic, cheilitis, duodenal ulcer, pancreatitis, cholestatic jaundice, impaired liver function, rectal bleeding, melena, bleeding gums, tenesmus.
From the musculoskeletal system:> 1% - arthritis <1% - leg muscle cramps, bursitis, tendosynovitis, myositis, myopathy, arthralgia, myalgia, rhabdomyolysis, torticollis, muscle hypertonicity, joint contracture, joint swelling, tendonopathy (in some cases with tendon rupture).
From the genitourinary system:> 1% - urogenital infections, peripheral edema <1% - dysuria (incl. pollakiuria, nocturia, urinary incontinence or urinary retention, imperative urination), leukocyturia, nephritis, hematuria, vaginal bleeding, nephrourolithiasis, metrorrhagia, epididymitis, decreased libido, impotence, impaired ejaculation.
Dermatological reactions:> 1% - alopecia, xeroderma, photosensitivity, increased sweating, eczema, seborrhea, ecchymosis, petechiae.
From the endocrine system: <1% - gynecomastia, mastodynia.
From the side of metabolism: <1% - increase in body weight, exacerbation of gout.
Allergic reactions: <1% - itchy skin, rash, contact dermatitis, rarely - urticaria, angioedema, facial edema, anaphylaxis, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell syndrome )
Laboratory indicators: <1% - hyperglycemia, hypoglycemia, increased serum CPK, albuminuria.
Drug interaction
With the simultaneous use of atorvastatin with digoxin, the concentration of digoxin in the blood plasma slightly increases.
Diltiazem, verapamil, isradipine inhibit the isoenzyme of CYP3A4, which is involved in the metabolism of atorvastatin, therefore, with the simultaneous use of calcium channel blockers, it is possible to increase the concentration of atorvastatin in the blood plasma and increase the risk ofopatia.
With the simultaneous use of itraconazole, the concentration of atorvastatin in the blood plasma increases significantly, apparently due to the inhibition of itraconazole by its metabolism in the liver, which occurs with the participation of the CYP3A4 isoenzyme, increasing the risk of myopathy.
With the simultaneous use of colestipol, a decrease in the concentration of atorvastatin in blood plasma is possible, while the lipid-lowering effect is enhanced.
With the simultaneous use of antacids containing magnesium hydroxide and aluminum hydroxide, reduce the concentration of atorvastatin by about 35%.
With the simultaneous use of cyclosporine, fibrates (including gemfibrozil), antifungal derivatives of azole derivatives, nicotinic acid, the risk of developing myopathy increases.
With the simultaneous use of erythromycin, clarithromycin moderately increases the concentration of atorvastatin in plasma, the risk of developing myopathy increases.
With the simultaneous use of ethinyl estradiol, norethisterone (norethindrone), the concentration of ethinyl estradiol, norethisterone and (norethindrone) in the blood plasma slightly increases.
With the simultaneous use of protease inhibitors, the concentration of atorvastatin in the blood plasma increases, because protease inhibitors are inhibitors of the CYP3A4 isoenzyme.
Active ingredient
Atorvastatin
lekarstvennaja form
tablets
Appointment
for Adults on purpose doctor
Indications
Prophylaxis of heart attacks and strokes, Atherosclerosis
Izvarino Pharma, Russia
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