Liptonorm

Release form and composition

Dosage form – film-coated tablets: round, convex on both sides, white; at the break - almost white or white (14 pieces in a blister, 2 blisters in a cardboard box).

Active substance: atorvastatin (in the form of calcium salt), its content in 1 tablet is 10 or 20 mg.

Auxiliary components: Tween 80, lactose, hydroxypropylcellulose, microcrystalline cellulose, croscarmellose, calcium carbonate, magnesium stearate, polyethylene glycol, titanium dioxide, hydroxypropylmethylcellulose.

Pharmacodynamics and pharmacokinetics

Liptonorm is a lipid-lowering drug from the statin group. The main mechanism of action of atorvastatin is to inhibit the activity of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. This enzyme catalyzes one of the initial stages of cholesterol synthesis - the process of converting HMG-CoA into mevalonic acid. The result of atorvastatin's inhibition of cholesterol synthesis is increased reactivity of low-density lipoprotein (LDL) receptors in the liver and extrahepatic tissues. LDL particles bind to these receptors and are removed from the blood plasma, which lowers the level of LDL cholesterol in the blood.

Atorvastatin has an antisclerotic effect. The drug affects blood components and vessel walls as follows:

suppresses the synthesis of isoprenoids;
improves endothelium-dependent dilation of blood vessels;
reduces the content of triglycerides, cholesterol, apolipoprotein B, low-density lipoproteins;
increases the content of apolipoprotein A and HDL cholesterol (high density lipoprotein).

As a rule, the effect of Liptonorm develops after 2 weeks of administration. To achieve maximum effect, 4 weeks are required.

Absorption of the drug is high. It takes 1–2 hours to achieve maximum concentration. In women, the maximum concentration is 20% higher than normal, and the AUC is 10% lower. In patients with alcoholic cirrhosis of the liver, the maximum concentration exceeds the norm by 16 times, the AUC by 11 times. Eating slightly reduces the duration and rate of absorption of the drug (by 9% and 25%, respectively), however, the reduction in LDL cholesterol is similar to that when using atorvastatin without food. When taken in the morning, the concentration of atorvastatin is approximately 30% higher than in the evening.

Bioavailability of Liptonorm is 14%, systemic bioavailability of inhibitory activity against HMG-CoA reductase is 30%. The decrease in systemic bioavailability is influenced by first-pass metabolism in the mucous membrane of the gastrointestinal tract and the “first pass” through the liver.

Plasma protein binding – 98%, average volume of distribution – 381 l. Metabolism of the drug occurs primarily in the liver under the influence of cytochrome P450 CYP3A7, CYP3A5 and CYP3A4. As a result of this process, pharmacologically active metabolites are formed (beta-oxidation products, ortho- and parahydroxylated derivatives). The inhibitory effect on HMG-CoA reductase is approximately 70% determined by the activity of circulating metabolites.

The drug does not undergo significant enterohepatic recirculation and is excreted along with bile after hepatic and/or extrahepatic metabolism.

The half-life of Liptonorm is 14 hours. Due to the presence of active metabolites, the inhibitory effect on HMG-CoA reductase lasts approximately 20–30 hours. The drug is not excreted during hemodialysis. Less than 2% of the dose taken orally is determined in the urine.

Release form, composition and packaging

White film-coated tablets, round, biconvex; on the fracture, white or almost white.

1 tab. Atorvastatin (in the form of calcium salt) 10 mg - "- 20 mg.

Excipients: calcium carbonate, microcrystalline cellulose, lactose, Tween 80, hydroxypropylcellulose, croscarmellose, magnesium stearate, hydroxypropylmethylcellulose, titanium dioxide, polyethylene glycol.

Clinical and pharmacological group: Lipid-lowering drug

pharmachologic effect

A lipid-lowering drug from the statin group. The main mechanism of action of atorvastatin is the inhibition of the activity of HMG-CoA reductase, an enzyme that catalyzes the conversion of HMG-CoA to mevalonic acid. This conversion is one of the early stages in the chain of cholesterol synthesis in the body. Suppression of cholesterol synthesis by atorvastatin leads to increased reactivity of LDL receptors in the liver, as well as in extrahepatic tissues. These receptors bind LDL particles and remove them from the blood plasma, which leads to a decrease in LDL-C.

The antiatherosclerotic effect of atorvastatin is a consequence of the drug’s effect on the walls of blood vessels and blood components. The drug inhibits the synthesis of isoprenoids, which are growth factors for the cells of the inner lining of blood vessels. Under the influence of atorvastatin, endothelium-dependent dilation of blood vessels improves. Atorvastatin reduces the content of cholesterol, LDL, apolipoprotein B, and TG. Causes an increase in the content of HDL-C and apolipoprotein A.

The effect of the drug, as a rule, develops after 2 weeks of administration, and the maximum effect is achieved after 4 weeks.

Pharmacokinetics

Suction

When taken orally, absorption of the drug is high. Time to reach Cmax in blood plasma is 1-2 hours.

Food slightly reduces the rate and duration of absorption of atorvastatin (by 25% and 9%, respectively), but the reduction in LDL-C levels is similar to that when using atorvastatin without food. A linear relationship was revealed between the degree of absorption and the dose of the drug.

Bioavailability is 14%, systemic bioavailability of inhibitory activity against HMG-CoA reductase is 30%. Low systemic bioavailability is due to first-pass metabolism in the gastrointestinal mucosa during the “first pass” through the liver.

Distribution

Plasma protein binding – 98%.

Average Vd is 381 hp.

Metabolism

Metabolized primarily in the liver with the participation of isoenzymes CYP3A4, CYP3A5 and CYP3A7 with the formation of pharmacologically active metabolites (ortho- and parahydroxylated derivatives, β-oxidation products). The inhibitory effect of the drug on HMG-CoA reductase is approximately 70% determined by the activity of circulating metabolites and lasts for about 20-30 hours.

Removal

T1/2 is 14 hours.

Excreted in bile after hepatic and/or extrahepatic metabolism (not subject to pronounced enterohepatic recirculation).

Less than 2% of the dose taken orally is determined in the urine.

Pharmacokinetics in special clinical cases: Cmax in women is 20% higher, AUC is 10% lower,

Cmax in patients with alcoholic cirrhosis is 16 times higher, AUC is 11 times higher than in patients with normal liver function.

The concentration of atorvastatin when used in the evening is lower than in the morning by approximately 30%.

Atorvastatin is not eliminated during hemodialysis.

Indications

primary hypercholesterolemia;
mixed hyperlipidemia;
heterozygous and homozygous familial hypercholesterolemia (as an addition to diet therapy).

Dosage regimen

Before starting treatment with Liptonorm, the patient should be put on a diet that lowers blood lipids, which must be followed during the treatment process.

The drug is prescribed orally at the same time of day, regardless of meals.

The recommended starting dose is 10 mg 1 time/day. Next, the dose is selected individually depending on the LDL-C content. The dose should be changed at intervals of at least 4 weeks. The maximum daily dose is 80 mg in 1 dose.

For primary (heterozygous hereditary and polygenic) hypercholesterolemia (type IIa) and mixed hyperlipidemia (type IIb), treatment begins with the recommended initial dose, which is increased after 4 weeks of therapy depending on clinical effectiveness. The maximum daily dose is 80 mg.

For homozygous hereditary hypercholesterolemia, the dose range is the same as for other types of hyperlipidemia. The initial dose is set individually depending on the severity of the disease. In most cases, the optimal effect is observed when using Liptonorm at a daily dose of 80 mg 1 time / day.

In patients with impaired liver function, the drug should be used with caution due to the slower elimination of atorvastatin from the body.

During treatment, clinical and laboratory parameters of body function should be carefully monitored, and if significant pathological changes are detected, the dose should be reduced or treatment discontinued.

Patients with renal failure and elderly patients do not require dose adjustment of Liptonorm.

Side effect

From the central nervous system and peripheral nervous system: more than 2% - insomnia, dizziness; less than 2% - headache, asthenic syndrome, malaise, drowsiness, nightmares, amnesia, paresthesia, peripheral neuropathy, emotional lability, ataxia, facial paralysis, hyperkinesis, depression, hyperesthesia, loss of consciousness.

From the senses: amblyopia, ringing in the ears, dry conjunctiva, impaired accommodation, hemorrhage in the eye, deafness, glaucoma, parosmia, loss of taste, taste perversion.

From the cardiovascular system: more than 2% - chest pain; less than 2% - palpitations, vasodilation, migraine, postural hypotension, increased blood pressure, phlebitis, arrhythmia, angina pectoris.

From the respiratory system: more than 2% - bronchitis, rhinitis; less than 2% - pneumonia, dyspnea, bronchial asthma, nosebleeds.

From the digestive system: more than 2% - nausea, heartburn, constipation or diarrhea, flatulence, gastralgia, abdominal pain, anorexia or increased appetite, dry mouth, belching, dysphagia, vomiting, stomatitis, esophagitis, glossitis, erosive and ulcerative lesions oral mucosa, gastroenteritis, hepatitis, hepatic colic, cheilitis, duodenal ulcer, pancreatitis, cholestatic jaundice, liver dysfunction, rectal bleeding, melena, bleeding gums, tenesmus.

From the musculoskeletal system: more than 2% - arthritis; less than 2% - leg muscle cramps, bursitis, tenosynovitis, myositis, myopathy, arthralgia, myalgia, rhabdomyolysis, torticollis, muscle hypertonicity, joint contractures.

From the hematopoietic system: anemia, lymphadenopathy, thrombocytopenia.

From the urinary system: more than 2% - urogenital infections, peripheral edema; less than 2% - dysuria (including pollakiuria, nocturia, urinary incontinence or urinary retention, urinary urgency), nephritis, hematuria, nephrourolithiasis.

From the reproductive system: less than 2% - vaginal bleeding, metrorrhagia, epididymitis, decreased libido, impotence, impaired ejaculation. Dermatological reactions: less than 2% - alopecia, xeroderma, increased sweating, eczema, seborrhea, ecchymosis, petechiae.

Allergic reactions: less than 2% - skin itching, skin rash, contact dermatitis; rarely - urticaria, angioedema, facial edema, photosensitivity, anaphylaxis, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).

From the laboratory parameters: less than 2% - increased serum CPK, increased alkaline phosphatase, albuminuria, increased ALT or AST.

From the metabolic side: less than 2% - hyperglycemia, hypoglycemia, weight gain, exacerbation of gout.

From the endocrine system: less than 2% - gynecomastia, mastodynia.

Contraindications

liver diseases in the active phase (including active chronic hepatitis, chronic alcoholic hepatitis);
increased activity of liver transaminases (more than 3 times compared to the upper limit of normal /ULN/) of unknown origin;
liver failure (classes A and B on the Child-Pugh scale);
liver cirrhosis of various etiologies;
children and adolescents up to 18 years of age;
pregnancy;
lactation (breastfeeding);
hypersensitivity to the components of the drug.

The drug should be prescribed with caution if there is a history of liver disease, severe electrolyte imbalances, endocrine and metabolic disorders, chronic alcoholism, arterial hypotension, severe acute infections (sepsis), uncontrolled seizures, extensive surgical interventions, or trauma.

Contraindications

Absolute:

Liver cirrhosis of various etiologies;
Liver failure (classes A and B according to the Child-Pugh scale);
Active liver diseases, including active chronic hepatitis and chronic alcoholic hepatitis;
Increased activity of liver transaminases (more than 3 times compared to the upper limit of normal) of unknown origin;
Age up to 18 years;
Pregnancy and lactation period;
Hypersensitivity to the components of the drug.

Relative:

History of liver disease;
Severe electrolyte imbalance;
Endocrine and metabolic disorders;
Arterial hypotension;
Chronic alcoholism;
Severe acute infections (sepsis);
Uncontrollable seizures;
Injuries;
Extensive surgical interventions.

Reviews of Liptonorm

Quite often, reviews of Liptonorm are related to various cardiac diseases and their complex therapy. As you know, elevated cholesterol levels in the blood are a symptom that is characteristic of the development of many pathological conditions.

Unfortunately, this drug is often prescribed for use, but the specifics of treatment are not explained. For example, you can find reviews where Liptonorm was prescribed to a patient who was bothered by swelling of her legs. After the examination, an increased concentration of cholesterol in the blood was revealed. As the patient herself says, in her opinion, no serious problems were found in her and she was prescribed medication to “adjust cholesterol levels.” However, she does not plan to change her life, including losing weight.

However, experts say that such an attitude towards treatment is completely unreasonable. With age, it becomes more difficult for the human body to cope with increased stress. Therefore, one of the important conditions for effective therapy is weight control.

Liptonorm must be taken strictly in dosages recommended by your doctor. This also applies to dose changes and drug withdrawal. Only with this approach can effective support be provided to the body.

Instructions for use Liptonorm: method and dosage

Before prescribing the drug, the patient is transferred to an appropriate diet, which ensures a decrease in lipid levels in the blood (it must be followed throughout the entire period of treatment).

According to the instructions, Liptonorm should be taken orally once a day, regardless of meals, but at the same time every day.

The starting dose is usually 10 mg. In the future, the optimal dose is selected individually, based on the level of low-density lipoprotein cholesterol, the severity of the disease and the effectiveness of therapy. The dose should be changed at at least 4-week intervals.

The highest permissible daily dose is 80 mg in 1 dose.

Liptonorm's analogs

Level 4 ATX code matches:
Akorta

Atomax

Lipitor

Pravastatin

Simvastol

Owencore

Simgal

Tulip

Lovastatin

Rozulip

Zokor

Rosart

Tevastor

Atorvastatin

Liprimar

Simvastatin

Atoris

Basilip

Rosecard

Roxera

The main analogues of Liptonorm are: Anvistat, Atocord, Atomax, Atorvastatin, Liprimar, Ator, Lipoford, Lipona, Vasator .

Side effects

Frequency of side effects: often - more than 2% of cases, rarely - less than 2% of cases.

Central nervous system: often – dizziness and insomnia; rarely - drowsiness, nightmares, asthenic syndrome, emotional lability, hyperkinesis, paresthesia, malaise, loss of consciousness, headache, depression, amnesia, ataxia, hyperesthesia, facial paralysis, peripheral neuropathy;
Sense organs: disturbance of accommodation, taste perversion, loss of taste, parosmia (loss of smell), ringing in the ears, deafness, amblyopia, dry conjunctiva, glaucoma, hemorrhage in the eye;
Cardiovascular system: often – chest pain; rarely - migraine, increased blood pressure, vasodilation, arrhythmia, postural hypotension, angina pectoris, palpitations, phlebitis;
Respiratory system: often – rhinitis and bronchitis; rarely – dyspnea, nosebleeds, bronchial asthma, pneumonia;
Digestive system: often - cheilitis, stomatitis, dry mouth, bleeding gums, erosive and ulcerative lesions of the oral mucosa, glossitis, abdominal pain, flatulence, heartburn, belching, nausea, constipation or diarrhea, anorexia or increased appetite, gastralgia, melena, vomiting, dysphagia, gastroenteritis, esophagitis, tenesmus, pancreatitis, duodenal ulcer, hepatic colic, liver dysfunction, hepatitis, cholestatic jaundice, rectal bleeding;
Musculoskeletal system: often – arthritis; rarely - bursitis, leg muscle cramps, myopathy, myositis, arthralgia, torticollis, joint contractures, tenosynovitis, muscle hypertonicity, myalgia, rhabdomyolysis;
Hematopoietic system: lymphadenopathy, anemia, thrombocytopenia;
Genitourinary system: often – peripheral edema, urogenital infections; rarely - dysuria (including urinary retention or urinary incontinence, nocturia, urinary urgency, pollakiuria), nephrourolithiasis, hematuria, nephritis, epididymitis, metrorrhagia, vaginal bleeding, impaired ejaculation, decreased libido, impotence;
Dermatological reactions: often - increased sweating, xeroderma, eczema, ecchymosis, seborrhea, petechiae, alopecia;
Allergic reactions: often - contact dermatitis, skin rash and itching; rarely - facial edema, anaphylaxis, angioedema, urticaria, photosensitivity, Stevens-Johnson syndrome, erythema multiforme, toxic epidermal necrolysis;
Laboratory indicators: rarely - albuminuria, hypoglycemia, hyperglycemia, increased activity of alkaline phosphatase, serum creatine phosphokinase, alanine aminotransferase (ALT) and aspartate aminotransferase (AST);
Other: rarely - weight gain, exacerbation of gout, mastodynia, gynecomastia.

Overdose

In case of overdose, it is possible to develop symptoms included in the list of side effects, but with greater severity.

There is no specific antidote for Liptonorm, so in case of overdose the following measures are recommended:

preventing further absorption of the drug (taking activated carbon, gastric lavage);
supporting the functioning of vital organ functions;
symptomatic therapy.

Hemodialysis in such cases is ineffective.

special instructions

During treatment, careful monitoring of clinical and laboratory parameters of body functions is necessary. If any significant pathological changes are detected, the dose of the drug should be reduced or treatment should be stopped.

Liver function should be monitored before starting the drug, after 6 and 12 weeks of therapy, after each dose increase, and periodically during treatment, for example, every 6 months. During the first 3 months of using Liptonorm, a change in the activity of liver enzymes is usually observed.

If liver transaminase activity increases, patients should be closely monitored until normal levels are restored. If the AST or ALT value is more than 3 times the upper limit of normal, the dose of the drug should be reduced or treatment should be discontinued.

Patients with diffuse myalgia, muscle weakness and flaccidity, and/or a significant increase in creatine phosphokinase are at risk for developing myopathy. If you experience unexplained muscle pain or weakness, especially if accompanied by fever or malaise, you should consult your doctor immediately.

The use of Liptonorm should be discontinued or temporarily suspended in the event of the development of any serious condition that could potentially be a consequence of myopathy, as well as in the presence of risk factors that can lead to acute renal failure due to rhabdomyolysis, such as electrolyte imbalance, severe endocrine and metabolic disorders, arterial hypotension, acute severe infection, trauma, major surgery.

If it is necessary to prescribe Liptonorm in combination with fibric acid derivatives, nicotinic acid (in doses that cause a hypolipidemic effect), immunosuppressants, cyclosporine, clarithromycin, erythromycin, antifungal drugs (azole derivatives), the expected benefits of therapy and the degree of risk should be compared. During treatment, especially in the first months and when increasing the dose of any of the drugs, you need to monitor the patient's condition in case of weakness, lethargy or muscle pain.

There are no known cases of Liptonorm’s negative influence on the speed of psychophysical reactions and a person’s ability to concentrate.

Women of childbearing age must use reliable methods of contraception during treatment. When planning pregnancy, the drug should be discontinued at least 1 month in advance.

Best before date

36 months

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For liver dysfunction

The drug is prescribed with caution if there is a history of liver disease.

Liptonorm is contraindicated in the following cases:

active phase of liver diseases (for example, with active chronic hepatitis, chronic alcoholic hepatitis);
increased activity of liver transaminases (exceeding the upper limit of normal by at least 3 times compared to ULN) of unknown etiology;
liver cirrhosis of various etiologies;
liver failure (classes A and B on the Child-Pugh scale).

Drug interactions

Antacids reduce the concentration of atorvastatin by 35%, but the effect on low-density lipoprotein cholesterol levels does not change.

Liptonorm in a daily dose of 80 mg increases by 20% the concentration in the blood of simultaneously used oral contraceptives containing ethinyl estradiol and norethindrone, and digoxin.

When using the drug in combination with warfarin, the prothrombin time decreases in the first days. This indicator usually normalizes after 15 days. Patients receiving this combination should have their prothrombin time monitored more frequently than usual.

Protease inhibitors, which are CYP3A4 inhibitors, increase plasma concentrations of atorvastatin.

With the simultaneous use of antifungal drugs (azole derivatives), clarithromycin, erythromycin, nicotinamide, fibrates, immunosuppressants, cyclosporine, the concentration of atorvastatin in the blood plasma increases and the risk of developing myopathy increases.

When using a combination of Liptonorm with colestipol, the hypolipidemic effect is superior to that of each drug separately.

Grapefruit juice may increase plasma concentrations of atorvastatin, so it is recommended that you avoid drinking this drink during treatment.

Interaction

If Cyclosporine, fibrates, Erythromycin, Clarithromycin , Nicotinamide , immunosuppressive and antifungal drugs - azoles - are prescribed simultaneously with this drug, then you can expect an increase in the concentration of its active substance - atorvastatin in the blood plasma .

The combination of atorvastatin and antacids, protease inhibitors, that is, inhibitors of cytochrome P450 CYP3A4, may increase the concentration of the drug in the blood plasma.

Using the drug with Digoxin increases its concentration in the body, as do oral contraceptives, which include norethindrone and ethinyl estradiol .

Colestipol increases the lipid-lowering effect, and Warfarin can reduce prothrombin time at the beginning of treatment, which requires regular monitoring of this indicator.

Drinking grapefruit juice may increase the concentration of atorvastatin during treatment, so you should avoid it.