pharmachologic effect
Belongs to the group of statins and has a lipid-lowering effect . Inhibits selectively and competitively the enzyme involved in cholesterol .
Triglycerides and cholesterol become components of atherogenic lipoproteins in the liver, after which they are transported to the periphery by the blood. By interacting with lipoprotein , they are converted into these lipoproteins.
Due to inhibition of HMG-CoA reductase, the level of lipoproteins and cholesterol in the blood decreases. The synthesis of LDL decreases and the activity of their receptors increases.
The drug is able to reduce the amount of LDL in cases of homozygous hereditary hypercholesterolemia
The medicine reduces cholesterol levels by 30-46%, atherogenic lipoproteins by 41-61%, triglycerides by 14-33% and increases the content of lipoproteins with antiatherogenic properties.
Pharmacological properties of the drug Torvacard
Atorvastatin is a selective competitive inhibitor of methylglutaryl-coenzyme A (HMG-CoA) reductase, an enzyme that regulates the rate of conversion of HMG-CoA to mevalonate, a precursor of sterols (including cholesterol). In patients with homo- and heterozygous hereditary hypercholesterolemia, non-hereditary forms of hypercholesterolemia and mixed dyslipidemia, the use of atorvastatin reduces the total level of cholesterol, LDL cholesterol and apolipoprotein B. Atorvastatin also reduces the concentration of VLDL and TG. The drug reduces the level of cholesterol and lipoproteins in the blood plasma by inhibiting HMG-CoA reductase, cholesterol synthesis in the liver and increasing the number of LDL receptors on the surface of hepatocytes, which enhances the uptake and catabolism of LDL. Atorvastatin is rapidly absorbed after oral administration; the maximum concentration in the blood plasma is achieved after 1–2 hours. The rate of absorption and concentration in the blood plasma increase in proportion to the dose of the drug. The absolute bioavailability of atorvastatin is about 12%, and the systemic availability of HMG-CoA reductase inhibitory activity is about 30%. Atorvastatin is metabolized into ortho- and parahydroxylated derivatives and various β-oxidation products. In vitro, inhibition of HMC-CoA reductase by ortho- and para-hydroxyl metabolites is equivalent to inhibition by atorvastatin. Approximately 70% of the circulating inhibitory activity of HMG-CoA reductase belongs to the active metabolites. In vitro studies indicate the importance of hepatic metabolism of atorvastatin by cytochrome P450 3A4, corresponding to increased plasma concentrations of atorvastatin in people concomitantly receiving erythromycin, which is a known isoenzyme inhibitor. In vitro studies have also shown that atorvastatin is a weak inhibitor of cytochrome P450 3A4. The simultaneous use of atorvastatin and terfenadine, a compound that is mainly metabolized by cytochrome P450 3A4, did not significantly increase the concentration of terfenadine in the blood plasma. Therefore, it is unlikely that atorvastatin will significantly alter the pharmacokinetics of other cytochrome P450 3A4 substrates. Atorvastatin and its metabolites are partially excreted in bile after hepatic and extrahepatic metabolism. However, the drug probably does not pass through enterohepatic recirculation. The average half-life of atorvastatin from human plasma is about 14 hours. The half-life of the inhibitory activity of HMG-CoA reductase is approximately 20–30 hours due to the presence of active metabolites. Less than 2% of an oral atorvastatin dose is excreted in the urine.
Pharmacodynamics and pharmacokinetics
In the blood, the maximum concentration of the drug occurs within 60-120 minutes. Eating reduces the duration of absorption, but the reduction in cholesterol is comparable to that without food. When used in the evening, the concentration of the drug is lower than when taken in the morning.
98% bound to blood proteins. Metabolized in the liver to form active metabolites.
It is excreted in bile, the half-life is 14 hours. The effectiveness of the drug is maintained due to active metabolites for up to 30 hours. It is not excreted during hemodialysis.
Torvacard overdose, symptoms and treatment
There is no specific treatment for atorvastatin overdose. In case of overdose, symptomatic and supportive therapy is carried out (gastric lavage, administration of activated charcoal or laxatives). If myopathy is noted with the further development of rhabdomyolysis and acute renal failure (a rare but serious side effect), immediate discontinuation of the drug and the administration of diuretics and sodium bicarbonate are required. Rhabdomyolysis can lead to hyperkalemia; in this case, intravenous administration of calcium chloride or calcium gluconate, infusion of glucose with insulin, and ion exchange agents are necessary to normalize potassium metabolism. Since atorvastatin binds to plasma proteins, hemodialysis does not lead to a significant decrease in the concentration of the drug in the blood plasma.
Indications for use of Torvacard
Torvacard tablets - what are they for?
The medicine is used in combination with a diet for:
- reducing the level of cholesterol , atherogenic lipoproteins, triglycerides, apolipoprotein B and increasing the amount of HDL in hypercholesterolemia, heterozygous and combined hypercholesterolemia (types IIa and IIb according to Fredrickson);
- treatment of patients who have increased triglycerides in the blood (Fredrickson type IV) and Fredrickson type III (dysbetalipoproteinemia), if the diet does not bring results;
- reducing the amount of cholesterol and LDL in homozygous familial hypercholesterolemia ;
- treatment of heart and vascular diseases in the presence of increased factors for coronary heart disease ( arterial hypertension , patients over 55 years of age, history of stroke albuminuria , left ventricular hypertrophy, smoking, peripheral vascular disease, family history of coronary artery disease diabetes mellitus ).
The most common indications for the use of Torvacard are secondary prevention of myocardial infarction , death, revascularization , stroke due to dyslipidemia .
Contraindications
- severe liver damage;
- increased levels of transaminases in the blood;
- hereditary glucose and lactose intolerance, lactase deficiency;
- women of reproductive age who do not use contraception ;
- pregnancy and breastfeeding ;
- children under 18 years of age;
- individual intolerance.
Use cautiously for metabolic and metabolic disorders, arterial hypertension , alcoholism , past liver disease, sepsis , changes in water-electrolyte balance, diabetes , epilepsy , trauma and major operations.
Contraindications to the use of Torvacard
Hypersensitivity to any component of the drug; acute liver disease; liver failure; increased level of liver transaminases in the blood serum (more than 3 times); During pregnancy and breastfeeding. Due to the lack of experience in treating children with atorvastatin, it should be prescribed only by specialists for the treatment of serious forms of hypercholesterolemia in children, as well as homozygous forms of hereditary hypercholesterolemia, especially in the presence of a high risk of developing early atherosclerosis and its clinical complications.
Side effects
Nervous system: insomnia, headache, depression , sleep disorders , paresthesia , ataxia , neuropathies .
Digestive tract: stomach pain, dyspepsia , nausea and vomiting, stool disorders, changes in appetite, pancreatitis and hepatitis , jaundice .
Musculoskeletal system: pain in the joints and muscles, in the back, cramps in the leg muscles, myositis .
Allergic manifestations: urticaria , itching, anaphylactic shock , erythema multiforme, angioedema , Lyell's syndrome.
Laboratory abnormalities: changes in glucose , increased activity of liver enzymes and creatine phosphokinase in the blood.
Other manifestations may include swelling of peripheral tissues, chest pain, tinnitus, baldness, weakness, weight gain, impotence , secondary renal failure, and a decrease in platelet count.
Cholesterol pills in some cases led to depression , sexual dysfunction, rare cases of damage to the connective tissue of the lungs, and diabetes mellitus (development depends on risk factors - fasting glucose levels, arterial hypertension, body mass index, hypertriglyceridemia ).
Side effects of the drug Torvacard
The most common side effects (1% or more) noted during treatment with Torvacard were: general: headache, asthenia, abdominal pain, allergic reactions, back pain, chest pain, general fatigue; Gastrointestinal tract: dyspepsia, nausea, vomiting, anorexia, hepatitis, pancreatitis, cholestatic jaundice, flatulence, constipation, diarrhea; CNS: myalgia, paresthesia, peripheral neuropathy, dizziness, amnesia; musculoskeletal system: myalgia, myositis, myopathy, arthralgia, rhabdomyolysis; skin and mucous membranes: itching, alopecia, vesicular rash, urticarial rash, erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome; genitourinary system: erectile dysfunction; metabolic and nutritional disorders: hypoglycemia, hyperglycemia, peripheral edema/edema, weight gain; hematological and lymphatic systems: thrombocytopenia.
Instructions for use of Torvacard (Method and dosage)
During treatment, the patient must follow a lipid-lowering diet .
Therapy begins with 10 mg per day, subsequently increased to 20 mg. The daily therapeutic dose is from 10 to 80 mg. The dose is selected taking into account laboratory parameters and individual characteristics.
The drug is taken regardless of food.
Before starting treatment and if dose adjustment is necessary, laboratory monitoring of lipid levels is carried out.
The effect of use occurs after 14 days.
For the treatment of patients with homozygous hypercholesterolemia , one of the few drugs that has an effect is Torvacard; the instructions for use clearly define the daily dose, which is 80 mg.
Use of the drug Torvacard
Before starting treatment with Torvacard, it is recommended to adhere to a standard diet that reduces cholesterol levels; This diet must be followed throughout the entire course of treatment with atorvastatin. Treatment usually begins with atorvastatin 10 mg once daily. Dosing is adjusted individually based on baseline LDL cholesterol levels compared to target LDL cholesterol levels and depending on the patient's response to therapy. Dosage is adjusted within 4 weeks of treatment, more if necessary. The maximum dose is 80 mg of atorvastatin per day. Primary hypercholesterolemia and mixed hyperlipidemia In most cases, a dose of 10 mg once daily is sufficient. The result of treatment is noticeable after 2 weeks, the stable maximum therapeutic effect is after 4 weeks. Homozygous hereditary hypercholesterolemia In a study where atorvastatin was used in patients with homozygous hereditary hypercholesterolemia, the majority of patients responded to treatment with atorvastatin 80 mg, producing a decrease in LDL cholesterol in more than 15% of cases (18–45%). Use in patients with renal failure Kidney damage does not affect either the plasma concentration or the effect of Torvacard on LDL cholesterol levels. Therefore, there is no need for dose adjustment in such patients. Use in children Information regarding the treatment of children is limited to the use of atorvastatin at a dose of up to 80 mg per day in 8 patients (children under 14 years of age) with homozygous hereditary hypercholesterolemia. As a result of the study, no clinical or biochemical abnormalities were noted in the patients. Use in elderly patients No differences have been identified between elderly patients and patients of other age groups regarding safety, effectiveness or achievement of treatment results. The tablet should be taken whole with plenty of water.
Interaction
The use of drugs that inhibit metabolism mediated by the CYP450 enzyme, erythromycin , antifungal and immunosuppressive drugs, fibrates, cyclosporine , clarithromycin , nicotinamide , nicotinic acid , the concentration of Torvacard in the blood increases. This increases the likelihood of myopathy, so it is necessary to monitor the level of CPK in the blood.
Co-administration of products with aluminum hydroxide or magnesium reduces the concentration of Torvacard, but this does not affect the effectiveness.
The combination with colestipol reduces the concentration of atorvastatin , but their combined lipid-lowering effect is superior to each individually.
Cimetidine , C pyronolactone , ketoconazole increases the likelihood of a decrease in the level of steroid hormones.
Taking oral contraceptives and a daily dose of Torvacard 80 mg increases the content of ethinyl estradiol in the blood.
Use in combination with digoxin reduces the concentration of the latter by 20%.
Interactions of the drug Torvacard
The risk of myopathy as a side effect of statins is higher with simultaneous use of: cyclosporine, fibric acid and its derivatives, macrolide antibiotics, antimycotic azoles or niacin. Amlodipine : with simultaneous use of 80 mg of atorvastatin and 10 mg of amlodipine, no changes in the pharmacokinetics of Torvacard were detected. Antipyrine: Since Torvacard does not alter the pharmacokinetics of antipyrine, interactions between other drugs metabolized by cytochrome are unlikely. Erythromycin/clarithromycin : simultaneous use of atorvastatin and erythromycin (500 mg 4 times a day) or clarithromycin (500 mg 2 times a day), known inhibitors of cytochrome P450 3A4, led to an increase in the plasma concentration of atorvastatin. Digoxin: Concomitant repeated administration of digoxin and atorvastatin 10 mg did not change the plasma concentration of digoxin at steady state. However, digoxin concentrations increased by approximately 20% when digoxin was coadministered with atorvastatin 80 mg once daily. It is necessary to monitor patients receiving Torvacard and digoxin in order to adjust the dose of digoxin. Oral contraceptives: Concomitant use of oral contraceptives containing norethisterone and ethinyl estradiol increased the AUC value of norethisterone by approximately 30% and ethinyl estradiol by 20%. This increase in concentration must be taken into account when choosing oral contraceptives for women receiving Torvacard. Cholestipol: Plasma concentrations of atorvastatin decreased with simultaneous use of atorvastatin and cholestipol (by approximately 25%), with a more pronounced lipid-lowering effect than with one drug alone. Antacids: When antacids containing magnesium and aluminum hydroxide were taken simultaneously with Torvacard, the plasma concentrations of atorvastatin and its active metabolites decreased by approximately 35%, but the decrease in LDL cholesterol levels did not change. Warfarin: Comparative interaction studies between warfarin and atorvastatin did not reveal any clinically significant interactions. Phenazone: Since atorvastatin does not affect the pharmacokinetics of phenazone, there are no interactions with other drugs metabolized through the same cytochrome isoenzymes. Cimetidine: When studying the combined use of cimetidine and atorvastatin, no interaction was observed. Azithromycin: The plasma concentration of atorvastatin is not affected by the simultaneous use of atorvastatin (10 mg once daily) and azithromycin (500 mg once daily). Terfenadine: Concomitant use of atorvastatin and terfenadine did not cause a clinically significant effect on the pharmacokinetics of terfenadine. Protease inhibitors: simultaneous use of atorvastatin with protease inhibitors that inhibit the effect of cytochrome P450 3A4 is accompanied by an increase in the concentration of atorvastatin in the blood plasma. Concomitant therapy: During clinical studies, Torvacard was used concomitantly with antihypertensive agents and estrogen replacement drugs without significant interaction effects. Interaction with specific agents has not been studied.
special instructions
Before starting treatment, you should try to reduce cholesterol levels with diet, treatment of obesity and associated diseases, and increased physical activity.
During treatment, monitoring of AST and ALT levels is necessary. For the first time, monitoring is carried out before, 6 weeks and 3 months after the start of therapy, as well as after adjusting the dose and once every six months. If the enzyme level increases more than 3 times, the drug is discontinued.
Taking Torvacard can cause weakness and muscle pain ( myopathy ) and an increase in CPK in the blood. If muscle pain or weakness occurs in combination with a fever, you should consult a doctor.
The drug is discontinued if there is a risk of renal failure due to rhabdomyolysis . This may include trauma, major surgery, metabolic and electrolyte imbalance, arterial hypotension , severe infection, and convulsions .
Taking Torvacard may lead to the development of diabetes mellitus in patients who are at increased risk. But it is worth remembering that the benefits of taking statins are higher than the risk of diabetes, so there is no need to discontinue the drug, and patients at risk should be constantly under the supervision of a doctor.
Analogues of Torvacard
Level 4 ATX code matches:
Akorta
Atomax
Lipitor
Pravastatin
Simvastol
Owencore
Simgal
Tulip
Lovastatin
Liptonorm
Rozulip
Zokor
Rosart
Tevastor
Atorvastatin
Liprimar
Simvastatin
Atoris
Basilip
Rosecard
Analogues of Torvacard are presented on the market in large quantities: Zakor , Vasilip , Crestor , Lovastatin , Rovacor , Pravastatin , Rosuvastatin , Simvastatin , Atorvastatin , Liprimar , Atoris .
The price of analogues is from 120 rubles. for 30 tab. atorvastatin up to RUB 3,606. for 28 tablets of Crestor at a dose of 40 mg.
Reviews about Torvacard
Those reviews about Torvacard that are available on the forums allow us to conclude that the drug is quite effective. It is widely prescribed by cardiologists to lower cholesterol and protect patients from stroke and heart attack . After 1-2 months of use, a significant decrease in cholesterol levels is observed. Some women report a pleasant side effect: weight loss.
Among the disadvantages are that the cholesterol medicine can cause insomnia and an itchy rash on the body .
Torvacard price, where to buy
The cost of the drug in Russian pharmacies ranges from 276 to 320 rubles. for 30 tablets at a dose of 10 mg. The price of Torvacard 20 mg 90 tablets is on average 1025 rubles, and a package of 90 tablets with a dose of 40 mg costs 1286 rubles.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
- Online pharmacies in KazakhstanKazakhstan
ZdravCity
- Torvacard tablets p.p.o.
10 mg 30 pcs. Zentiva a.s./Saneka Pharmaceuticals a.s. RUB 253 order - Torvacard tablets p.p.o. 20 mg 90 pcs. Saneka Pharmaceuticals a.s.
RUB 1,057 order
- Torvacard tablets p.p.o. 40 mg 90 pcs. Zentiva a.s./Saneka Pharmaceuticals a.s.
RUB 1,398 order
- Torvacard tablets p.p.o. 40 mg 30 pcs. SanekaSaneka Pharmaceuticals a.s.
RUR 551 order
Pharmacy Dialogue
- Torvacard (tab.p.pl/vol. 20 mg No. 90) Saneca
RUR 978 order
- Torvacard (tab.p.pl/vol. 40 mg No. 90) Saneca
RUB 1,414 order
- Torvacard (tablet p/o cap. 10 mg No. 90)Zentiva as/Zentiva ks
RUB 684 order
- Torvacard (tab.p.pl/vol. 20 mg No. 30)Zentiva ks
RUB 376 order
- Torvacard (tab.p.pl/vol.40mg No. 90)Zentiva as/Zentiva ks
RUB 1,396 order
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Pharmacy24
- Torvacard Crystal 20 mg N90 tablets TOV Zentiva, Czech Republic
367 UAH.order - Torvacard Crystal 40 mg N30 tablets TOV Zentiva, Czech Republic
247 UAH order
- Torvacard Crystal 10 mg N90 tablets TOV Zentiva, Czech Republic
331 UAH. order
- Torvacard Crystal 10 mg N30 tablets TOV Zentiva, Czech Republic
112 UAH order
- Torvacard Crystal 20 mg N30 tablets TOV Zentiva, Czech Republic
96 UAH order
PaniPharmacy
- Torvacard tablets Torvacard 20 tablets. p/o 20 mg No. 90, Saneca Pharmaceuticals
345 UAH. order
- Torvacard tablets Torvacard 40 tablets. p/o 40 mg No. 30, Saneca Pharmaceuticals
267 UAH order
- Torvacard tablets Torvacard 20 tablets. p/o 20 mg No. 30, Saneca Pharmaceuticals
107 UAH order
- Torvacard tablets Torvacard 10 tablets. p/o 10 mg No. 30, Saneca Pharmaceuticals
111 UAH order
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