Atorvastatin pills 10mg №30

Pharmacology

Atorvastin is a lipid-lowering agent from the group of statins. According to the principle of competitive antagonism, the statin molecule binds to the 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 product in the synthesis of the cholesterol molecule. Inhibition of the activity of HMG-CoA reductase leads to a series of consecutive reactions, which result in a decrease in the intracellular cholesterol content and a compensatory increase in the activity of LDL receptors and, accordingly, an acceleration of cholesterol catabolism (Xc) of LDL.

Indications

Primary hypercholesterolemia with the ineffectiveness of diet therapy, combined hypercholesterolemia and hypertriglyceridemia, heterozygous and homozygous familial hypercholesterolemia with the ineffectiveness of diet therapy.

Contraindications

Liver diseases in the active stage, increased serum transaminase activity more than 3 times of unclear genesis, pregnancy, lactation (breastfeeding), hypersensitivity to Atorvastatin. Women of reproductive age who do not use reliable contraception.Atorvastatin is contraindicated for use during pregnancy and lactation (breastfeeding).

Pregnanacy and breastfeeding

Atorvastatin is contraindicated for use during 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 during treatment should use adequate methods of contraception. Atorvastatin can be prescribed to 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.

Special notes

Before and during treatment with atorvastatin, especially when symptoms of liver damage appear, it is necessary to monitor indicators of liver function. With an increase in the level of transaminases, their activity should be monitored until normalization. If the activity of AST or ALT, more than 3 times higher than normal, is maintained, it is recommended to reduce the dose or cancel Atorvastatin.

Active ingredient

Active substance: atorvastatin calcium trihydrate;

Excipients: Calcium carbonate; MCC; StarKap1500 (corn starch and pregelatinized starch); colloidal silicon dioxide (aerosil); talc; Magnesium stearate;Opadry II (series 85) (polyvinyl alcohol, macrogol, talc, titanium dioxide, iron dye yellow oxide, iron dye red oxide).

Dosage and administration

Inside

Before prescribing Atorvastatin, the patient should be advised to recommend a standard lipid-lowering diet, which he must continue to follow throughout the entire period of therapy.

The initial dose is an average of 10 mg / day. The dose varies from 10 to 80 mg / day.

The drug can be taken at any time of the day with food or regardless of meal times. The dose is selected based on the initial cholesterol / LDL levels, the goal of therapy and the individual effect. At the beginning of treatment and / or during the dose increase of atorvastatin, plasma levels of lipids should be monitored every 2–4 weeks and the dose should be adjusted accordingly.

To ensure the following dosage regimen of the drug, it is possible to use the drug Atorvastatin in another dosage form: film-coated tablets, 10 mg and 20 mg. The maximum daily dose of the drug is 80 mg.

With simultaneous use with cyclosporine, the daily dose of atorvastatin should not exceed 10 mg.

Primary hypercholesterolemia and mixed hyperlipidemia. In most cases, it is enough to give a dose of 10 mg of atorvastatin 1 time per day. A significant therapeutic effect is observed after 2 weeks, and the maximum therapeutic effect is usually observed after 4 weeks.With long-term treatment, this effect persists.

Special patient groups

Impaired renal function. The use of the drug in patients with renal failure and kidney disease does not affect the level of atorvastatin in the blood plasma or the degree of cholesterol / LDL cholesterol reduction when it is used, therefore, changing the dose of the drug is not required.

Liver dysfunction. In case of hepatic insufficiency, the dose must be reduced.

Elderly patients. When using the drug in elderly patients, there were no differences in safety, efficacy, or achievement of lipid-lowering therapy goals in comparison with the general population.

Adverse effects

Nervous system: insomnia, dizziness; headache, asthenia, malaise, drowsiness, nightmares, paresthesias, peripheral neuropathy, amnesia, emotional lability, ataxia, facial nerve paralysis, hyperkinesis, migraine, depression, hypoesthesia, loss of consciousness.

Special senses:amblyopia, tinnitus, dry conjunctiva, accommodation disturbance, retinal hemorrhage, deafness, glaucoma, parosmia, loss of taste, taste perversion.

Cardiovascular:chest pain; palpitations, vasodilation symptoms, orthostatic hypotension, increased blood pressure, phlebitis, arrhythmia, angina pectoris.

Hemic and lymphatic:anemia, lymphadenopathy, thrombocytopenia.

Respiratory:bronchitis, rhinitis; pneumonia, dyspnea, exacerbation of bronchial asthma, epistaxis.

Gastrointestinal:nausea; 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, abnormal liver function, rectal bleeding, melena, gingival bleeding, tenesmus.

Musculoskeletal system:arthritis; leg muscle cramps, bursitis, tendosynovitis, myositis, myopathy, arthralgia, myalgia, rhabdomyolysis, torticollis, muscle hypertonia, joint contractures, joint swelling, tendinopathy (in some cases with a tendon rupture).

From the genitourinary system:urogenital infections, peripheral edema; <1% - dysuria (including pollakiuria, nocturia, urinary incontinence or urinary retention, imperative urination to urinate), leukocyturia, nephritis, hematuria, vaginal bleeding, nephrorolithiasis, metrorrhagia, epididymitis, reduction of libido, myocardium, nephrorolithiasis, metrorrhagia, epididymitis, reduction of libido, myocardium, nephrorolithiasis, metrorrhagia, epididymitis, reduction of libido, myocardium, nephrorolithiasis, metrorrhagia, epididymitis, reduction of libido, myocardium, nephrorolithiasis, metrorrhagia, epididymitis, reduction of libido, myocardium, nephrorolithiasis, metrorrhagia, epididymitis, reduction of libido, myocardium

Dermatologic:alopecia, xeroderma, photosensitization, increased sweating, eczema, seborrhea, ecchymosis, petechiae.

On the part of the endocrine system: gynecomastia, mastodinia.

Metabolism: weight gain, aggravation of gout.

Allergic reactions:skin itch, skin rash, contact dermatitis, rarely - urticaria, angioedema, facial edema, anaphylaxis, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).

Laboratory values:hyperglycemia, hypoglycemia, increased serum CPK, albuminuria.

Drug interactions

The risk of myopathy during treatment with other drugs of this class increases with the simultaneous use of cyclosporine, fibrates, Erythromycin, antifungal agents related to azoles, and nicotinic acid.

With simultaneous ingestion of atorvastatin and a suspension containing magnesium and aluminum hydroxide, plasma concentrations of atorvastatin decreased by about 35%, but the degree of cholesterol / LDL cholesterol levels did not change.

With simultaneous use of atorvastatin does not affect the pharmacokinetics of antipyrine (phenazone), therefore, interaction with other drugs metabolized by the same cytochrome isoenzymes is not expected.

With simultaneous use of colestipol, the concentration of atorvastatin in the blood plasma decreased by approximately 25%. However, the lipid-lowering effect of the combination of atorvastatin and colestipol was superior to that of each drug separately.

With repeated use of Digoxin and atorvastatin at a dose of 10 mg equilibrium concentrations of digoxin in plasmablood did not change. However, when using digoxin in combination with atorvastatin at a dose of 80 mg / day. digoxin concentration increased by about 20%. Patients receiving digoxin in combination with atorvastatin should be monitored.

With simultaneous use of atorvastatin and erythromycin (500 mg 4 times / day) or Clarithromycin (500 mg 2 times / day), which inhibit cytochrome P450 3A4, an increase in plasma concentration of atorvastatin was observed.

With simultaneous use of atorvastatin (10 mg 1 time / day) and Azithromycin (500 mg 1 time / day), the concentration of atorvastatin in the blood plasma did not change.

Atorvastatin did not have a clinically significant effect on the concentration of terfenadine in plasma, which is metabolized mainly by cytochrome P450 3A4; Therefore, it seems unlikely that atorvastatin can significantly affect the pharmacokinetic parameters of other cytochrome P450 3A4 substrates.

With simultaneous use of atorvastatin and a oral contraceptive containing norethindrone and ethinyl estradiol, there was a significant increase in the AUC of norethindrone and ethinyl estradiol by about 30% and 20%, respectively. This effect should be considered when choosing an oral contraceptive for a woman receiving atorvastatin.

Simultaneous use with drugs that reduce the concentration of endogenous steroid hormones (including cimetidine, Ketoconazole, spironolactone) increases the risk of reducing endogenous steroid horomones (caution should be exercised).

When studying the interaction of atorvastatin with Warfarin and cimetidine, there are no signs of a clinically significant interaction.

With simultaneous use of atorvastatin 80 mg and Amlodipine 10 mg, the pharmacokinetics of atorvastatin did not change in equilibrium.

No clinically significant undesirable interaction of atorvastatin and antihypertensive agents has been noted.

The simultaneous use of atorvastatin with protease inhibitors, known as inhibitors of cytochrome P450 3A4, was accompanied by an increase in the concentration of atorvastatin in the blood plasma.

Symptoms: specific signs of overdose have not been established. Likely symptoms may be pain in the liver, acute renal failure ; with prolonged use of myopathy and rhabdomyolysis.

Treatment: there is no specific antidote, symptomatic therapy and measures to prevent further absorption (gastric lavage and taking activated charcoal). Atorvastatin binds to plasma proteins to a large extent, as a result of which hemodialysis is ineffective. With the development of myopathy, followed by rhabdomyolysis and acute renal failure (rare) - immediate withdrawal of the drug and the introduction of a diuretic and sodium bicarbonate solution. Rhabdomyolysis can lead to the development of hyperkalemia, which can be eliminated by the intravenous administration of calcium chloride or Calcium gluconate, the infusion of glucose with insulin, the use of potassium ion exchangers or, in severe cases, hemodialysis.

In the dark place at a temperature of no higher than 25 ° C.