In this article, we will consider instructions for applying to Liptonorm. This is a lipid-lowering drug that is part of the statin group. Liptonorm is produced by the manufacturer in the form of coated tablets. The tablets are white, biconvex.
Who produces the Liptonorm? Pharmaceutical company "M.J. Biopharm", India.
The composition of the drug
Atorvastatin is the main substance in the preparation (each tablet contains 10 mg of the main component). In addition, there are a number of auxiliary components, in particular titanium dioxide, magnesium stearate, hydroxypropyl cellulose, lactose, calcium carbonate, polyethylene glycol, hydroxypropyl methyl cellulose, croscarmellose, tween 80, microcrystalline cellulose.
The drug is produced by the manufacturer in cardboard boxes, in each of which 14 tablets are located on two blisters.
pharmachologic effect
According to the instructions for Liptonorm, the main active ingredient of the drug atorvastatin is able to inhibit the activity of HMG-CoA reductase (an enzyme that accelerates the conversion of HMG-CoA to mevalonic acid). This transformation is one of the first steps in the chain of cholesterol synthesis in the body. Atorvastatin inhibits cholesterol synthesis, which increases the reactivity of LDL receptors in the liver and in all tissues outside the liver. These receptors bind to LDL particles and remove them from blood plasma. As a result, there is a decrease in LDL cholesterol.
Atorvastatin as part of the drug acts on the walls of blood vessels and blood components, resulting in an anti-atherosclerotic effect. Under the influence of the drug, the synthesis of isoprenoids, which are the growth factors of the cells from which the inner shell of the vessels is built, is suppressed. Against the background of the action of atorvastatin, an improvement in the endothelium-dependent expansion of blood vessels occurs. In addition, atorvastatin is able to lower cholesterol, TG, apolipoprotein B, LDL, and cause an increased content of apolipoprotein A and HDL cholesterol.
The effectiveness of the drug is achieved, as a rule, after the second week of admission, the maximum effect is visible after a month.
Pharmacokinetics of the drug
As indicated by the instructions for Liptonorm, the absorption of the drug after oral administration is quite high. The maximum concentration in plasma is a couple of hours after ingestion.
The rate (approximately 25%) and the duration (approximately 9%) of absorption of atorvastatin is reduced by food, however, a decrease in LDL cholesterol in this case is similar to a decrease when taking atorvastatin without food. There is a linear dependence of the degree of absorption on the dose of the drug.
The bioavailability of the drug is at the level of 14%, while in relation to HMG-CoA reductase, the bioavailability (systemic) of the inhibitory activity is about 30%. The low level of systemic bioavailability is due to the presence of presystemic metabolism in the mucous membranes of the gastrointestinal tract during the "first passage" through the liver.
The active substance binds to plasma proteins by almost 98%.
The substance is metabolized, mainly in the liver tissues, while the isoenzymes CYP3A7, CYP3A5, CYP3A4 are involved in the metabolism. As a result, pharmacologically active metabolites are formed - products of β-oxidation, parahydroxylated derivatives, orthohydroxylated derivatives. In relation to HMG-CoA reductase, the inhibitory effect of the drug is maintained for 20-30 hours and depends on the activity of circulating metabolites by 70%.
The average half-life of the drug is about 14 hours. After completion of hepatic and extrahepatic metabolism is excreted in the bile. It is worth noting that there is no pronounced enterohepatic recirculation.
If you take atorvastatin in the morning, its concentration will be approximately 30% higher than when taken in the evening.
During the hemodialysis procedure, atorvastatin is not excreted.
What else does the instruction to Liptonorm tell us?
Indications for use
Indications for use are:
- Mixed hyperlipidemia.
- Primary hypercholesterolemia.
- Familial hypercholesterolemia. Therapy with the drug is used in combination with diet therapy.
Contraindications
The main contraindications that interfere with the appointment of therapy using Liptonorm include:
- Cirrhosis of the liver of any etymology.
- Hepatic failure (both class A and class B).
- Age is under 18 years.
- Pregnancy and lactation.
- Increased activity of liver transaminases (more than three times in comparison with VGN), which has an unclear genesis.
- Liver disease in the active phase. Including chronic hepatitis, the active stage of chronic hepatitis.
- Individual sensitivity to the components of the drug.
Use the drug with caution in cases of a history of liver disease, severe electrolyte imbalance, metabolic disturbances, endocrine abnormalities, chronic alcoholism, cases of uncontrolled seizures, arterial hypotension, extensive surgery, serious infections (sepsis), and injuries. Reviews on "Liptonorm" consider below.
Dosage of drug
Before starting therapy using the Liptonorm drug, the patient should be transferred to a special diet, which will ensure a decrease in blood lipids. A similar diet should be followed throughout the treatment.
The drug is administered orally. It is necessary to take it at the same time, regardless of meals.
The initial recommended dose is 10 mg. It is necessary to take it once a day. Over the course of treatment, the dosage is adjusted individually, taking into account the level of LDL cholesterol. Dosage changes can be carried out exclusively at intervals of 4 weeks. Important! The maximum daily dosage cannot exceed 80 mg at a time.
It is necessary to begin treatment of primary heterozygous hereditary and polygenic hypercholisterinemia, as well as mixed hyperlipidemia, with the minimum recommended dosage. Further, 4 weeks after the start of treatment, it is increased taking into account clinical efficacy. At the same time, 80 mg is the maximum dose admissible per day.
Homozygous hereditary hypercholesterolemia involves taking the same dose range as other types of hyperlipidemia. The initial dose should be set individually, it depends on the severity of the disease. Clinical practice shows that the optimal effect can be achieved when taking Liptonorm in a dosage of 80 mg per day.
Patients with impaired liver function should take the drug with extreme caution. This is due to the delayed excretion of atorvastatin from the body.
The period of treatment with this medication involves careful monitoring of laboratory and clinical indicators of body functions. If significant pathological changes are detected, the dosage should be reduced or treatment with the drug should be completely canceled.
In the treatment of elderly patients, people suffering from renal failure, there is no need to adjust the Liptonorm dosage.
Side effects
In accordance with the instructions for Liptonorm, side effects from the body can occur as follows:
- Insomnia and dizziness.
- Headache, asthenic syndrome, malaise, drowsiness, nightmares, amnesia, paresthesia, peripheral neuropathy, emotional lability, ataxia, facial paralysis, hyperkinesis, depression, hyperesthesia, loss of consciousness.
- On the part of the sensory organs, undesirable manifestations such as taste perversion, parosmia, glaucoma, deafness, eye hemorrhage, accommodation disturbance, conjunctivitis, tinnitus, amblyopia can occur.
- The cardiovascular system can react with the appearance of chest pain, migraine, vasodilation, palpitations, postural hypotension, high blood pressure, phlebitis, arrhythmia, angina pectoris.
- Respiratory system: rhinitis, bronchitis, nosebleeds, dyspnea, bronchial asthma, pneumonia. This is confirmed by the instructions for use and reviews of "Liptonorm."
- From the gastrointestinal tract, the patient may experience side effects in the form of diarrhea, constipation, heartburn, nausea, increased appetite, anorexia, abdominal pain, gastralgia, flatulence, glossitis, esophagitis, stomatitis, vomiting, dysphagia, belching, dry mouth, erosive ulcerative lesions of the mucous membranes of the mouth, hepatic colic, hepatitis, gastroenteritis, cholestatic jaundice, pancreatitis, duodenal ulcers, cheilitis, bleeding gums, melena, rectal bleeding, impaired liver function, tenesmus.
- Musculoskeletal system: arthritis, myalgia, arthralgia, myopathy, myositis, tendosynovitis, bursitis, muscle hypertonicity, torticollis, leg muscle cramps, rhabdomyolysis, joint contractures.
- Hematopoietic system: thrombocytopenia, lymphadenopathy, anemia.
- Genitourinary system: peripheral swelling, urogenital infections, imperative urination, urinary incontinence, urinary retention, nocturia, pollakiuria, hematuria, nephritis, epididymitis, metrorrhagia, nephrourolithiasis, vaginal bleeding, ejaculation disorders, impotence, decreased libido.
- From the skin and subcutaneous fat: increased sweating, petechiae, xeroderma, alopecia, ecchymosis, seborrhea, eczema.
- Side effects of an allergic nature: contact dermatitis, skin rash, itching. In rare cases, anaphylaxis, facial edema, photosensitivity, urticaria, angioedema, multiforme exudative erythema, toxic epidermal necrolysis, Stevens-Johnson syndrome can occur.
- In laboratory studies, the following can be detected: increased activity of CPK, hypoglycemia, hyperglycemia, albuminuria, increased activity of alkaline phosphatase, AST, ALT.
- Other adverse reactions that occur while taking the drug include exacerbation of gout, mastodynia, gynecomastia, excess weight.
This is stated in the instructions for use. Reviews and analogues to Liptonorm are presented at the end of the article.
Drug overdose
In case of overdose with Liptonorm, gastric lavage should be done immediately, a dose of activated carbon recommended for intoxication should be taken, symptomatic therapy should be carried out, and a measure should be taken to maintain the patient's body functions. There is no specific antidote.
In the case of signs of renal failure caused by rhabdomyolysis, you must immediately stop drinking the drug.
Since atorvastatin is significantly associated with blood proteins, the effectiveness of hemodialysis is absent.
Interaction with other medicines
As a result of the simultaneous administration of the Liptonorm drug and immunosuppressants, clarithromycin, erythromycin, fibrates, nicotinamide, cyclosporine, antifungal drugs that are derivatives of azole, the concentration of atorvastatin in the blood increases significantly. As a result, the risk of myopathy is increasing.
The concentration of atorvastatin is reduced by 35% while taking it with antacids, but the effect on LDL cholesterol does not change.
With the simultaneous administration of the drug and protease inhibitors in the blood, the concentration of atorvastatin increases.
With the simultaneous administration of digoxin and Liptonorm tablets at a dosage of 80 mg per day, the concentration level of digoxin in the blood rises (by about 20%).
“Liptonorm” in a dosage of 80 mg per day increases by 20% the concentration of oral contraceptives taken simultaneously with it, the main active ingredient of which is ethinyl estradiol and norethidrone.
Concomitant use with warfarin preparations affects prothrombin time. In the early days, it decreases, but after 2 weeks, the norm returns. Related to this is the need for more frequent monitoring in patients taking Liptonorm with warfarin.
The use of grapefruit juice increases the concentration of atorvastatin in the blood. Accordingly, patients for the period of treatment using Liptonorm should abandon this product.
For pregnant and lactating women
During this period, the use of Liptonorm is strictly contraindicated. In addition, experts do not recommend the use of the drug in the treatment of women who are of childbearing age and do not use reliable contraception. Therapy with the drug must be stopped at least one month before conception. This confirms the instructions for use for Liptonorm. Analogs should be selected by a doctor.
Terms and conditions of storage
The drug is included in the list B. It must be stored away from children, and also away from light, moisture and at a temperature of no more than 25 degrees. The drug is suitable for 2 years from the date of manufacture.
Analogues of Liptonorm are presented below.
How to replace
On sale you can find analogues with the same active component. These include:
- Atorvastatin-TEVA.
- Torvakard.
- Atorvastatin.
- Liprimar.
Reviews about "Liptonorm"
According to patients' reviews, the drug is actively prescribed for cardiovascular diseases, since elevated blood cholesterol is a common symptom of many pathological conditions of the heart.
Specialists prescribe the drug quite often, however, unfortunately, they do not explain the features of therapy. There are frequent reviews when the remedy did not help patients, and the whole thing was that it must be taken in combination with a correctly selected diet.
According to doctors' reviews, being overweight negatively affects the pharmacological effect of Liptonorm. It’s increasingly difficult for the human body to cope with stress with age. Accordingly, effective therapy directly depends on an integrated approach to weight control.
Reviews of losing weight indicate that the drug is often used by nutritionists in the complex treatment of overweight, as well as metabolic problems.
Many reviews indicate that at the initial stage of using Liptonorm for weight loss, according to reviews, it can cause discomfort in the stomach and gastrointestinal tract. This side effect disappears over time, and after a few weeks of taking laboratory tests indicate the onset of improvement.
You should always remember that to start taking the drug should only be prescribed by a doctor, in dosages recommended by a specialist. This will allow you to achieve the desired effect from treatment, to avoid possible side effects and other unforeseen difficulties.
We examined the detailed instructions for use with Liptonorm. Reviews about the drug and its analogues have also been indicated.