Release form, composition and packing
Tablets, coated white, round, slightly biconvex.
1 tab. atorvastatin (in the form of calcium salt) 10 mg.
Other ingredients: povidone, sodium lauryl sulfate, calcium carbonate, microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, magnesium stearate.
The composition of the shell: talc, titanium dioxide (E171), macrogol 3000, polyvinyl alcohol.
Tablets, coated white, round, slightly biconvex.
1 tab. atorvastatin (in the form of calcium salt) 20 mg.
Other ingredients: povidone, sodium lauryl sulfate, calcium carbonate, microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, magnesium stearate. The composition of the shell: talc, titanium dioxide (E171), macrogol 3000, polyvinyl alcohol.
Tablets, film-coated white or almost white, round, slightly biconvex.
1 tab. atorvastatin (in the form of calcium salt) 40 mg.
Other ingredients: povidone, sodium lauryl sulfate, calcium carbonate, microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, magnesium stearate. The composition of the shell: Opadry White Y-1-7000 (hypromellose, titanium dioxide (E171), macrogol 400).
Clinico-pharmacological group: Lipid-lowering drug.
Pharmacological action
Lipid-lowering drug from the statin group. Selective competitive inhibitor of HMG-CoA reductase enzyme that converts 3-hydroxy-3-metilglyutarilkoenzim And mevalonic acid is a precursor of sterols, including cholesterol. Suppression of cholesterol synthesis (CS) leads to increased reactivity of receptors low density lipoprotein (LDL) cholesterol in the liver and extrahepatic tissues. These receptors bind LDL particles and remove them from the blood plasma, which leads to a reduction in LDL-C levels. Antiatherosclerotic effect of the drug manifests the influence of atorvastatin on the vascular wall and blood components. Atorvastatin inhibits the synthesis of isoprenoids, which are growth factors of the inner shell vessel.
Under the influence of atorvastatin improves endothelial vasodilation. Atorvastatin reduces total cholesterol, LDL cholesterol, apolipoprotein B, triglycerides. Causes an increase in HDL-cholesterol and apolipoprotein A. The action Atorisa develops 2 weeks after starting the drug, the maximum effect is achieved after 4 weeks.
Pharmacokinetics
Suction
After oral administration, is well absorbed from the gastrointestinal tract (80%).
Time to reach Cmax of 1-2 hours due to intensive metabolism in "first pass" through the liver, the bioavailability of atorvastatin is 12%.
Distribution
The average Vd - 381 l binding to plasma proteins - 98%. Atorvastatin does not penetrate the BBB.
Metabolism
Metabolized primarily in the liver under the action of cytochrome P450 3A4 to the formation of pharmacologically active metabolites (ortho-and paragidroksilirovannyh derivatives, products of beta-oxidation). Metabolites have an inhibitory effect on HMG-CoA reductase, which lasts 20-30 hours
Breeding
Derived mainly from the bile (not exposed to pronounced enterohepatic recirculation). T1 / 2 - 14 h. About 46% is excreted in the feces, less than 2% - in the urine.
Pharmacokinetics in special clinical situations
Cmax higher among women by 20%, AUC - below 10%. Cmax in patients with alcoholic cirrhosis is 16 times higher than normal.
Statement
primary hypercholesterolemia;
mixed hyperlipidemia (including patients with insulin-dependent diabetes mellitus);
heterozygous and homozygous familial hypercholesterolemia (as an adjunct to diet).
Dosing regimen
Prior to treatment Atorisom patient should be transferred to a hypolipidemic diet, which must be observed during drug therapy. The drug is taken orally on an empty stomach or after eating. The recommended starting dose - 10 mg daily. Depending on the desired effect, the daily dose can be increased to 80 mg. Atoris taken singly at any time of day, but at the same time every day.
Action Atorisa develops after 2 weeks of taking the drug, the maximum effect is achieved after 4 weeks. Therefore, the dose should not be changed until at least 4 weeks after starting treatment. With primary (heterozygous hereditary and polygenic) hypercholesterolemia (type IIa) and mixed hyperlipidemia (type IIb) treatment begins with an initial dose of 10 mg 1 time per day, which increased after 4 weeks, depending on patient response. The maximum daily dose - 80 mg.
When homozygous hereditary hypercholesterolemia starting dose is 10 mg / day. With a maximum daily dose of 80 mg marked the most optimal effect. Atoris used as adjunctive therapy to other therapies (plasmapheresis) or as a primary method of treatment if the therapy is not possible by other methods. For elderly patients dose adjustment is required.
Patients with liver dysfunction drug is prescribed with caution due to the slowdown Withdrawal from the body. In this situation shows the control of clinical and laboratory parameters and the detection of significant pathological changes in the dose should be reduced or treatment should be discontinued.
Side effect
CNS and peripheral nervous system: insomnia or drowsiness, dizziness, headache, asthenia syndrome, nightmares, amnesia, paresthesia, peripheral neuropathy, emotional lability, ataxia, hyperkinesis, depression, hypersensitivity.
From the senses: amblyopia, tinnitus, dryness of the conjunctiva, disturbance of accommodation, eye hemorrhage, deafness, glaucoma, parosmiya, loss of taste sensation.
With the cardiovascular system: heart rate, vasodilatation, migraine, postural hypotension, increased blood pressure, phlebitis, arrhythmia.
From the hematopoietic system: anemia, lymphadenopathy, thrombocytopenia.
With the respiratory system: bronchitis, rhinitis, dyspnea, asthma, epistaxis.
From the digestive system: nausea, heartburn, constipation or diarrhea, flatulence, stomachodynia, abdominal pain, anorexia, decreased or increased appetite, dry mouth, eructation, dysphagia, vomiting, stomatitis, esophagitis, glossitis, gastroenteritis, hepatitis, hepatic colic, cheilitis, duodenal ulcer, pancreatitis, cholestatic jaundice, elevated liver enzymes, rectal bleeding, melena, bleeding gums, tenesmus.
From the musculoskeletal system: arthritis, muscle cramps legs, bursitis, myositis, myopathy, arthralgia, myalgia, rhabdomyolysis, joint contractures.
With the genitourinary system: urogenital infections, dysuria (including thamuria, nocturia, urinary incontinence or urinary retention, peremptory urging to urinate), cystitis, hematuria, vaginal bleeding, uterine hemorrhage, urolithiasis, metrorrhagia, epididymitis, decreased libido , impotence, impaired ejaculation.
Dermatological reactions: alopecia, sweating, eczema, seborrhea, ecchymosis.
Allergic reactions: itching, skin rashes, contact dermatitis, rarely - urticaria, angioedema, face edema, photosensitivity, anaphylaxis, erythema multiforme exudative, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).
From the laboratory parameters: hyperglycemia, hypoglycemia, increased serum CPK, albuminuria, increased ALT, AST. Other: peripheral edema, weight gain, gynecomastia, exacerbation of gout.
Contraindications
liver disease in the active stage (including active chronic hepatitis, chronic alcoholic hepatitis);
liver failure;
cirrhosis of various etiologies;
elevated liver transaminases of unknown origin;
skeletal muscle disease, pregnancy;
Lactation (breastfeeding);
age of 18 years (efficacy and safety has not been established);
hypersensitivity to the drug.
Pregnancy and lactation
Use of the drug during pregnancy and lactation is contraindicated. Women of reproductive age during the reception Atorisa should use reliable methods of contraception. If a patient planning a pregnancy, she should stop taking Atorisa month before the planned pregnancy.
Use in hepatic dysfunction
The drug is contraindicated in liver disease in the active stage (including active chronic hepatitis, chronic alcoholic hepatitis), liver failure, liver cirrhosis of different etiologies, with an increase in liver transaminases of unknown origin
Tablets, coated white, round, slightly biconvex.
1 tab. atorvastatin (in the form of calcium salt) 10 mg.
Other ingredients: povidone, sodium lauryl sulfate, calcium carbonate, microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, magnesium stearate.
The composition of the shell: talc, titanium dioxide (E171), macrogol 3000, polyvinyl alcohol.
Tablets, coated white, round, slightly biconvex.
1 tab. atorvastatin (in the form of calcium salt) 20 mg.
Other ingredients: povidone, sodium lauryl sulfate, calcium carbonate, microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, magnesium stearate. The composition of the shell: talc, titanium dioxide (E171), macrogol 3000, polyvinyl alcohol.
Tablets, film-coated white or almost white, round, slightly biconvex.
1 tab. atorvastatin (in the form of calcium salt) 40 mg.
Other ingredients: povidone, sodium lauryl sulfate, calcium carbonate, microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, magnesium stearate. The composition of the shell: Opadry White Y-1-7000 (hypromellose, titanium dioxide (E171), macrogol 400).
Clinico-pharmacological group: Lipid-lowering drug.
Pharmacological action
Lipid-lowering drug from the statin group. Selective competitive inhibitor of HMG-CoA reductase enzyme that converts 3-hydroxy-3-metilglyutarilkoenzim And mevalonic acid is a precursor of sterols, including cholesterol. Suppression of cholesterol synthesis (CS) leads to increased reactivity of receptors low density lipoprotein (LDL) cholesterol in the liver and extrahepatic tissues. These receptors bind LDL particles and remove them from the blood plasma, which leads to a reduction in LDL-C levels. Antiatherosclerotic effect of the drug manifests the influence of atorvastatin on the vascular wall and blood components. Atorvastatin inhibits the synthesis of isoprenoids, which are growth factors of the inner shell vessel.
Under the influence of atorvastatin improves endothelial vasodilation. Atorvastatin reduces total cholesterol, LDL cholesterol, apolipoprotein B, triglycerides. Causes an increase in HDL-cholesterol and apolipoprotein A. The action Atorisa develops 2 weeks after starting the drug, the maximum effect is achieved after 4 weeks.
Pharmacokinetics
Suction
After oral administration, is well absorbed from the gastrointestinal tract (80%).
Time to reach Cmax of 1-2 hours due to intensive metabolism in "first pass" through the liver, the bioavailability of atorvastatin is 12%.
Distribution
The average Vd - 381 l binding to plasma proteins - 98%. Atorvastatin does not penetrate the BBB.
Metabolism
Metabolized primarily in the liver under the action of cytochrome P450 3A4 to the formation of pharmacologically active metabolites (ortho-and paragidroksilirovannyh derivatives, products of beta-oxidation). Metabolites have an inhibitory effect on HMG-CoA reductase, which lasts 20-30 hours
Breeding
Derived mainly from the bile (not exposed to pronounced enterohepatic recirculation). T1 / 2 - 14 h. About 46% is excreted in the feces, less than 2% - in the urine.
Pharmacokinetics in special clinical situations
Cmax higher among women by 20%, AUC - below 10%. Cmax in patients with alcoholic cirrhosis is 16 times higher than normal.
Statement
primary hypercholesterolemia;
mixed hyperlipidemia (including patients with insulin-dependent diabetes mellitus);
heterozygous and homozygous familial hypercholesterolemia (as an adjunct to diet).
Dosing regimen
Prior to treatment Atorisom patient should be transferred to a hypolipidemic diet, which must be observed during drug therapy. The drug is taken orally on an empty stomach or after eating. The recommended starting dose - 10 mg daily. Depending on the desired effect, the daily dose can be increased to 80 mg. Atoris taken singly at any time of day, but at the same time every day.
Action Atorisa develops after 2 weeks of taking the drug, the maximum effect is achieved after 4 weeks. Therefore, the dose should not be changed until at least 4 weeks after starting treatment. With primary (heterozygous hereditary and polygenic) hypercholesterolemia (type IIa) and mixed hyperlipidemia (type IIb) treatment begins with an initial dose of 10 mg 1 time per day, which increased after 4 weeks, depending on patient response. The maximum daily dose - 80 mg.
When homozygous hereditary hypercholesterolemia starting dose is 10 mg / day. With a maximum daily dose of 80 mg marked the most optimal effect. Atoris used as adjunctive therapy to other therapies (plasmapheresis) or as a primary method of treatment if the therapy is not possible by other methods. For elderly patients dose adjustment is required.
Patients with liver dysfunction drug is prescribed with caution due to the slowdown Withdrawal from the body. In this situation shows the control of clinical and laboratory parameters and the detection of significant pathological changes in the dose should be reduced or treatment should be discontinued.
Side effect
CNS and peripheral nervous system: insomnia or drowsiness, dizziness, headache, asthenia syndrome, nightmares, amnesia, paresthesia, peripheral neuropathy, emotional lability, ataxia, hyperkinesis, depression, hypersensitivity.
From the senses: amblyopia, tinnitus, dryness of the conjunctiva, disturbance of accommodation, eye hemorrhage, deafness, glaucoma, parosmiya, loss of taste sensation.
With the cardiovascular system: heart rate, vasodilatation, migraine, postural hypotension, increased blood pressure, phlebitis, arrhythmia.
From the hematopoietic system: anemia, lymphadenopathy, thrombocytopenia.
With the respiratory system: bronchitis, rhinitis, dyspnea, asthma, epistaxis.
From the digestive system: nausea, heartburn, constipation or diarrhea, flatulence, stomachodynia, abdominal pain, anorexia, decreased or increased appetite, dry mouth, eructation, dysphagia, vomiting, stomatitis, esophagitis, glossitis, gastroenteritis, hepatitis, hepatic colic, cheilitis, duodenal ulcer, pancreatitis, cholestatic jaundice, elevated liver enzymes, rectal bleeding, melena, bleeding gums, tenesmus.
From the musculoskeletal system: arthritis, muscle cramps legs, bursitis, myositis, myopathy, arthralgia, myalgia, rhabdomyolysis, joint contractures.
With the genitourinary system: urogenital infections, dysuria (including thamuria, nocturia, urinary incontinence or urinary retention, peremptory urging to urinate), cystitis, hematuria, vaginal bleeding, uterine hemorrhage, urolithiasis, metrorrhagia, epididymitis, decreased libido , impotence, impaired ejaculation.
Dermatological reactions: alopecia, sweating, eczema, seborrhea, ecchymosis.
Allergic reactions: itching, skin rashes, contact dermatitis, rarely - urticaria, angioedema, face edema, photosensitivity, anaphylaxis, erythema multiforme exudative, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).
From the laboratory parameters: hyperglycemia, hypoglycemia, increased serum CPK, albuminuria, increased ALT, AST. Other: peripheral edema, weight gain, gynecomastia, exacerbation of gout.
Contraindications
liver disease in the active stage (including active chronic hepatitis, chronic alcoholic hepatitis);
liver failure;
cirrhosis of various etiologies;
elevated liver transaminases of unknown origin;
skeletal muscle disease, pregnancy;
Lactation (breastfeeding);
age of 18 years (efficacy and safety has not been established);
hypersensitivity to the drug.
Pregnancy and lactation
Use of the drug during pregnancy and lactation is contraindicated. Women of reproductive age during the reception Atorisa should use reliable methods of contraception. If a patient planning a pregnancy, she should stop taking Atorisa month before the planned pregnancy.
Use in hepatic dysfunction
The drug is contraindicated in liver disease in the active stage (including active chronic hepatitis, chronic alcoholic hepatitis), liver failure, liver cirrhosis of different etiologies, with an increase in liver transaminases of unknown origin
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