Release form, composition and packing
Tablets, film-coated white, biconvex.
1 tab. Atorvastatin calcium trihydrate 10.85 mg, which corresponds to the contents of atorvastatin 10 mg.
Excipients: calcium carbonate, microcrystalline cellulose, lactose, starch 1500, colloidal silicon dioxide (Aerosil), magnesium stearate, Opadry II (polyvinyl alcohol, macrogol (polyethylene glycol), talc, titanium dioxide).
Tablets, film-coated white, biconvex.
1 tab. Atorvastatin calcium trihydrate 21.7 mg, which corresponds to the contents of atorvastatin 20 mg.
Excipients: calcium carbonate, microcrystalline cellulose, lactose, starch 1500, colloidal silicon dioxide (Aerosil), magnesium stearate, Opadry II (polyvinyl alcohol, macrogol (polyethylene glycol), talc, titanium dioxide).
Clinico-pharmacological group
Lipid-lowering drug.
Pharmacological action
Lipid-lowering drug. Selective competitive inhibitor of HMG-CoA reductase - an enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A to mevalonic acid is a precursor of sterols, including cholesterol. TG and cholesterol (CH) in the liver included in the VLDL, enter the blood plasma and transported to peripheral tissues. LDL formed from VLDL during the interaction with receptors of LDL. Atorvastatin lowers cholesterol and lipoproteins in blood plasma by inhibiting HMG-CoA reductase, the synthesis of cholesterol at the liver and increasing the number of LDL receptors in liver cell surface, which leads to increased capture and catabolism of LDL. Reduces LDL, causes marked and persistent increase in the activity of LDL receptors.
Lowers LDL cholesterol in patients with homozygous familial hypercholesterolemia, which is not usually amenable to therapy, lipid-lowering drugs. Lowers total cholesterol by 30-46%, LDL - by 41-61%, apolipoprotein B - by 34-50% and triglycerides - by 14-33% causes an increase in the level of HDL-C and apolipoprotein A. dose-dependent decreases in LDL patients with homozygous hereditary hypercholesterolemia resistant to therapy, other lipid-lowering drugs.
Pharmacokinetics
Suction
After receiving the drug inside absorption is high. Cmax plasma levels reached after 1-2 h.
Food slightly reduces the rate and duration of the absorption of the drug (25% and 9% respectively), but the reduction of LDL cholesterol is similar to that in the application of atorvastatin without food. The concentration of atorvastatin when used in the evening are lower than in the morning (approximately 30%). Revealed a linear relationship between the degree of absorption and dose of the drug.
Bioavailability - 12%, systemic bioavailability of inhibitory activity against HMG-CoA reductase inhibitors - 30%. The low systemic bioavailability due to presystemic metabolism in the mucosa of the gastrointestinal tract and "first pass" through the liver.
Distribution
Binding to plasma proteins - 98%. The average Vd - 381 liters.
Metabolism
Metabolized primarily in the liver under the influence of isozymes CYP3A4, CYP3A5 and CYP3A7 with the formation of pharmacologically active metabolites (ortho-and paragidroksilirovannyh derivatives, products of beta-oxidation). In vitro ortho-and paragidroksilirovannye metabolites have an inhibitory effect on HMG-CoA reductase, comparable with that of atorvastatin. The inhibitory effect of the drug on HMG-CoA reductase by about 70% determined by the activity of circulating metabolites.
Breeding
T1 / 2 - 14 hours inhibitory activity against HMG-CoA reductase remains about 20-30 hours due to the presence of active metabolites.
Excreted in the bile after liver and / or extrahepatic metabolism (not subject to pronounced enterohepatic recirculation). Less than 2% of an oral dose is determined in the urine.
Pharmacokinetics in special clinical situations
Cmax higher among women by 20%, AUC - below 10%; Cmax in patients with alcoholic cirrhosis by 16 times, AUC - is 11 times higher compared with patients with normal liver function.
Does not appear in the course of hemodialysis.
Indications for use of the drug
in combination with diet to reduce elevated total cholesterol, LDL-C, apolipoprotein B and triglycerides and raising HDL-C in patients with primary hypercholesterolemia, heterozygous familial hypercholesterolemia and non-family, and combined (mixed) hyperlipidemia (Types IIa and IIb of Fredrickson) ;
in combination with diet to treat patients with elevated serum TG levels (Fredrickson Type IV on) and patients with disbetalipoproteinemiey (type III according to Fredrickson), whose nutritional treatment did not provide an adequate effect;
to reduce the levels of total cholesterol and LDL-C in patients with homozygous familial hypercholesterolemia when diet therapy and other non-pharmacological treatments are not effective.
Dosing regimen
Before the appointment of atorvastatin patients need to recommend a standard hypolipidemic diet, which he must comply during the whole period of treatment.
The drug can be taken any time of the day with food or regardless of mealtime. Dose is selected taking into account the initial LDL-C levels, the goals of therapy and individual effects. At the beginning of the treatment and / or while raising the dose of atorvastatin should be every 2-4 weeks to control lipid levels in blood plasma and appropriately corrected dose.
The initial dose is an average of 10 mg 1 time in the future ranges from 10 mg to 80 mg 1 time
With primary hypercholesterolemia and mixed hyperlipidemia, with an increase in serum triglycerides (type IV of Fredrickson), as well as disbetalipoproteinemii (type III according to Fredrickson) in most cases, the destination of the drug at a dose of 10 mg 1 time / significant therapeutic effect is observed, usually 2 weeks, the maximum therapeutic effect is usually observed after 4 weeks. Long-term treatment, this effect persists.
When homozygous familial hypercholesterolemia drug is prescribed at a dose of 80 mg (4 tablets of 20 mg), 1.
In patients with renal insufficiency and kidney concentrations of atorvastatin in plasma does not change, the degree of lowering the LDL-C is stored, so changing the dose is not required.
In hepatic failure dose should be reduced.
Using the drug in elderly patients differences in safety or effectiveness of achieving lipid-lowering therapy in comparison with the general population have been noted.
Side effect
The nervous system:> 2% - insomnia, dizziness, <2% - headache, fatigue, malaise, drowsiness, nightmares, paresthesia, peripheral neuropathy, amnesia, emotional lability, ataxia, facial paralysis, hyperkinesis, migraine, depression , hypoesthesia, loss of consciousness.
From the sensory organs: <2% - amblyopia, tinnitus, dryness of the conjunctiva, disturbance of accommodation, bleeding in the retina of the eye, deafness, glaucoma, parosmiya, loss of taste, taste perversion.
Cardio-vascular system:> 2% - chest pain <2% - heartbeat, symptoms of vasodilation, orthostatic hypotension, increased blood pressure, phlebitis, arrhythmia, angina.
From the hemopoietic system: <2% - anemia, lymphadenopathy, thrombocytopenia.
With the respiratory system:> 2% - bronchitis, rhinitis, <2% - pneumonia, dyspnoea, exacerbation of asthma, epistaxis.
From the digestive system:> 2% - nausea, <2% - heartburn, constipation or diarrhea, flatulence, stomachodynia, abdominal pain, decreased or increased appetite, dry mouth, eructation, dysphagia, vomiting, stomatitis, esophagitis, glossitis, erosive and ulcerative lesions of the mucous membranes of the mouth, gastroenteritis, hepatitis, biliary colic, cheilitis, duodenal ulcer, pancreatitis, cholestatic jaundice, hepatic dysfunction, rectal bleeding, melena, bleeding gums, tenesmus.
From the musculoskeletal system:> 2% - arthritis <2% - spasms of leg muscles, bursitis, tenosynovitis, myositis, myopathy, arthralgia, myalgia, rhabdomyolysis, torticollis, muscular hypertonicity, joint contractures.
From the urogenital system:> 2% - urogenital infections, peripheral edema, <2% - dysuria (including thamuria, nocturia, urinary incontinence or urinary retention, imperative urge to urinate), nephritis, hematuria, vaginal bleeding, nefrourolitiaz , metrorrhagia, epididymitis, decreased libido, impotence, impaired ejaculation.
Dermatological reactions:> 2% - alopecia, dermatoxerasia, increased sweating, eczema, seborrhea, ecchymosis, petechiae.
From the endocrine system: <2% - gynecomastia, mammalgia.
From a metabolism: <2% - weight gain, exacerbation of gout.
Allergic reactions: <2% - itching, skin rashes, contact dermatitis, is rare - urticaria, angioedema, face edema, photosensitivity, anaphylaxis, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (syndrome Lyell).
Laboratory tests: <2% - hyperglycemia, hypoglycemia, increased serum CPK, albuminuria.
Tablets, film-coated white, biconvex.
1 tab. Atorvastatin calcium trihydrate 10.85 mg, which corresponds to the contents of atorvastatin 10 mg.
Excipients: calcium carbonate, microcrystalline cellulose, lactose, starch 1500, colloidal silicon dioxide (Aerosil), magnesium stearate, Opadry II (polyvinyl alcohol, macrogol (polyethylene glycol), talc, titanium dioxide).
Tablets, film-coated white, biconvex.
1 tab. Atorvastatin calcium trihydrate 21.7 mg, which corresponds to the contents of atorvastatin 20 mg.
Excipients: calcium carbonate, microcrystalline cellulose, lactose, starch 1500, colloidal silicon dioxide (Aerosil), magnesium stearate, Opadry II (polyvinyl alcohol, macrogol (polyethylene glycol), talc, titanium dioxide).
Clinico-pharmacological group
Lipid-lowering drug.
Pharmacological action
Lipid-lowering drug. Selective competitive inhibitor of HMG-CoA reductase - an enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A to mevalonic acid is a precursor of sterols, including cholesterol. TG and cholesterol (CH) in the liver included in the VLDL, enter the blood plasma and transported to peripheral tissues. LDL formed from VLDL during the interaction with receptors of LDL. Atorvastatin lowers cholesterol and lipoproteins in blood plasma by inhibiting HMG-CoA reductase, the synthesis of cholesterol at the liver and increasing the number of LDL receptors in liver cell surface, which leads to increased capture and catabolism of LDL. Reduces LDL, causes marked and persistent increase in the activity of LDL receptors.
Lowers LDL cholesterol in patients with homozygous familial hypercholesterolemia, which is not usually amenable to therapy, lipid-lowering drugs. Lowers total cholesterol by 30-46%, LDL - by 41-61%, apolipoprotein B - by 34-50% and triglycerides - by 14-33% causes an increase in the level of HDL-C and apolipoprotein A. dose-dependent decreases in LDL patients with homozygous hereditary hypercholesterolemia resistant to therapy, other lipid-lowering drugs.
Pharmacokinetics
Suction
After receiving the drug inside absorption is high. Cmax plasma levels reached after 1-2 h.
Food slightly reduces the rate and duration of the absorption of the drug (25% and 9% respectively), but the reduction of LDL cholesterol is similar to that in the application of atorvastatin without food. The concentration of atorvastatin when used in the evening are lower than in the morning (approximately 30%). Revealed a linear relationship between the degree of absorption and dose of the drug.
Bioavailability - 12%, systemic bioavailability of inhibitory activity against HMG-CoA reductase inhibitors - 30%. The low systemic bioavailability due to presystemic metabolism in the mucosa of the gastrointestinal tract and "first pass" through the liver.
Distribution
Binding to plasma proteins - 98%. The average Vd - 381 liters.
Metabolism
Metabolized primarily in the liver under the influence of isozymes CYP3A4, CYP3A5 and CYP3A7 with the formation of pharmacologically active metabolites (ortho-and paragidroksilirovannyh derivatives, products of beta-oxidation). In vitro ortho-and paragidroksilirovannye metabolites have an inhibitory effect on HMG-CoA reductase, comparable with that of atorvastatin. The inhibitory effect of the drug on HMG-CoA reductase by about 70% determined by the activity of circulating metabolites.
Breeding
T1 / 2 - 14 hours inhibitory activity against HMG-CoA reductase remains about 20-30 hours due to the presence of active metabolites.
Excreted in the bile after liver and / or extrahepatic metabolism (not subject to pronounced enterohepatic recirculation). Less than 2% of an oral dose is determined in the urine.
Pharmacokinetics in special clinical situations
Cmax higher among women by 20%, AUC - below 10%; Cmax in patients with alcoholic cirrhosis by 16 times, AUC - is 11 times higher compared with patients with normal liver function.
Does not appear in the course of hemodialysis.
Indications for use of the drug
in combination with diet to reduce elevated total cholesterol, LDL-C, apolipoprotein B and triglycerides and raising HDL-C in patients with primary hypercholesterolemia, heterozygous familial hypercholesterolemia and non-family, and combined (mixed) hyperlipidemia (Types IIa and IIb of Fredrickson) ;
in combination with diet to treat patients with elevated serum TG levels (Fredrickson Type IV on) and patients with disbetalipoproteinemiey (type III according to Fredrickson), whose nutritional treatment did not provide an adequate effect;
to reduce the levels of total cholesterol and LDL-C in patients with homozygous familial hypercholesterolemia when diet therapy and other non-pharmacological treatments are not effective.
Dosing regimen
Before the appointment of atorvastatin patients need to recommend a standard hypolipidemic diet, which he must comply during the whole period of treatment.
The drug can be taken any time of the day with food or regardless of mealtime. Dose is selected taking into account the initial LDL-C levels, the goals of therapy and individual effects. At the beginning of the treatment and / or while raising the dose of atorvastatin should be every 2-4 weeks to control lipid levels in blood plasma and appropriately corrected dose.
The initial dose is an average of 10 mg 1 time in the future ranges from 10 mg to 80 mg 1 time
With primary hypercholesterolemia and mixed hyperlipidemia, with an increase in serum triglycerides (type IV of Fredrickson), as well as disbetalipoproteinemii (type III according to Fredrickson) in most cases, the destination of the drug at a dose of 10 mg 1 time / significant therapeutic effect is observed, usually 2 weeks, the maximum therapeutic effect is usually observed after 4 weeks. Long-term treatment, this effect persists.
When homozygous familial hypercholesterolemia drug is prescribed at a dose of 80 mg (4 tablets of 20 mg), 1.
In patients with renal insufficiency and kidney concentrations of atorvastatin in plasma does not change, the degree of lowering the LDL-C is stored, so changing the dose is not required.
In hepatic failure dose should be reduced.
Using the drug in elderly patients differences in safety or effectiveness of achieving lipid-lowering therapy in comparison with the general population have been noted.
Side effect
The nervous system:> 2% - insomnia, dizziness, <2% - headache, fatigue, malaise, drowsiness, nightmares, paresthesia, peripheral neuropathy, amnesia, emotional lability, ataxia, facial paralysis, hyperkinesis, migraine, depression , hypoesthesia, loss of consciousness.
From the sensory organs: <2% - amblyopia, tinnitus, dryness of the conjunctiva, disturbance of accommodation, bleeding in the retina of the eye, deafness, glaucoma, parosmiya, loss of taste, taste perversion.
Cardio-vascular system:> 2% - chest pain <2% - heartbeat, symptoms of vasodilation, orthostatic hypotension, increased blood pressure, phlebitis, arrhythmia, angina.
From the hemopoietic system: <2% - anemia, lymphadenopathy, thrombocytopenia.
With the respiratory system:> 2% - bronchitis, rhinitis, <2% - pneumonia, dyspnoea, exacerbation of asthma, epistaxis.
From the digestive system:> 2% - nausea, <2% - heartburn, constipation or diarrhea, flatulence, stomachodynia, abdominal pain, decreased or increased appetite, dry mouth, eructation, dysphagia, vomiting, stomatitis, esophagitis, glossitis, erosive and ulcerative lesions of the mucous membranes of the mouth, gastroenteritis, hepatitis, biliary colic, cheilitis, duodenal ulcer, pancreatitis, cholestatic jaundice, hepatic dysfunction, rectal bleeding, melena, bleeding gums, tenesmus.
From the musculoskeletal system:> 2% - arthritis <2% - spasms of leg muscles, bursitis, tenosynovitis, myositis, myopathy, arthralgia, myalgia, rhabdomyolysis, torticollis, muscular hypertonicity, joint contractures.
From the urogenital system:> 2% - urogenital infections, peripheral edema, <2% - dysuria (including thamuria, nocturia, urinary incontinence or urinary retention, imperative urge to urinate), nephritis, hematuria, vaginal bleeding, nefrourolitiaz , metrorrhagia, epididymitis, decreased libido, impotence, impaired ejaculation.
Dermatological reactions:> 2% - alopecia, dermatoxerasia, increased sweating, eczema, seborrhea, ecchymosis, petechiae.
From the endocrine system: <2% - gynecomastia, mammalgia.
From a metabolism: <2% - weight gain, exacerbation of gout.
Allergic reactions: <2% - itching, skin rashes, contact dermatitis, is rare - urticaria, angioedema, face edema, photosensitivity, anaphylaxis, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (syndrome Lyell).
Laboratory tests: <2% - hyperglycemia, hypoglycemia, increased serum CPK, albuminuria.
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