Composition per tablet:
Active substance:
nicergoline (in terms of 100% substance) - 10.0 mg.
Excipients:
potato starch - 26.9 mg, colloidal silicon dioxide - 2.0 mg, magnesium stearate - 1.1 mg, lactose monohydrate - to obtain an uncoated tablet weighing 110.0 mg.
Excipients of the coating to obtain a tablet with a coating weighing 180.0 mg:
sugar (sucrose) – 48.1159 mg, magnesium carbonate – 19.8800 mg, povidone – 1.0000 mg, beeswax – 0.3880 mg, titanium dioxide – 0.3036 mg, talc – 0.2990 mg, silicon dioxide colloidal – 0.0135 mg.
Description:
Round, biconvex tablets, film-coated, white or almost white. The cross section shows two layers.
Pharmacotherapeutic group:
alpha adrenergic blocker.
ATX code
: CO4AE02
Pharmacological properties:
Pharmacodynamics:
Nicergoline is a derivative of ergoline, improves metabolic and hemodynamic processes in the brain, reduces platelet aggregation and improves hemorheological blood parameters, increases the speed of blood flow in the upper and lower extremities. Nicergoline exhibits an alpha-1-adrenergic blocking effect, leading to improved blood flow and has a direct effect on the cerebral neurotransmitter systems - noradrenergic, dopaminergic and acetylcholinergic. With the use of the drug, the activity of the noradrenergic, dopaminergic and acetylcholinergic cerebral systems increases, which helps to optimize cognitive processes. As a result of long-term therapy with nicergoline, there is a persistent improvement in cognitive functions and a decrease in the severity of behavioral disorders associated with dementia.
Pharmacokinetics:
After oral administration, nicergoline is quickly and almost completely absorbed. The main metabolic products of nicergoline are 1,6-dimethyl-8b-hydroxymethyl-10a-methoxyergoline (MMDL, a hydrolysis product) and 6-methyl-8b-hydroxymethyl-10a-methoxyergoline (MDL, a dimethylation product by the CYP2D6 isoenzyme). The ratio of the area under the concentration-time curve (AUC) for MMDL and MDL after oral administration of nicergoline indicates a pronounced first-pass metabolism through the liver. After oral administration of 30 mg of nicergoline, maximum concentrations of MMDL (21 ± 14 ng/ml) and MDL (41 ± 14 ng/ml) were achieved after approximately 1 and 4 hours, respectively, then the concentration of MDL decreased with a half-life of 13 - 20 hours. Studies confirm absence of accumulation of other metabolites (including MMDL) in the blood. Food intake or dosage form do not have a significant effect on the degree and rate of absorption of nicergoline. Nicergoline actively (> 90%) binds to plasma proteins, and the degree of its affinity for a1-acid glycoprotein is greater than for serum albumin. It has been shown that nicergoline and its metabolites can be distributed in blood cells. The pharmacokinetics of nicergoline when using doses up to 60 mg is linear and does not change depending on the age of the patient.
Nicergoline is excreted in the form of metabolites, mainly by the kidneys (approximately 80% of the total dose), and in small quantities (10-20%) through the intestines. In patients with severe renal failure, there is a significant decrease in the degree of excretion of metabolic products in the urine compared to patients with normal renal function.
Instructions for use NICERGOLINE-LF
A drug that improves cerebral and peripheral blood circulation. Nicergoline is an ergoline derivative that has an alpha1-adrenergic blocking effect. After oral administration, nicergoline is rapidly and extensively metabolized to form a number of metabolites, which also have effects at various levels of the central nervous system.
After oral administration, nicergoline has various neuropharmacological effects, since it not only stimulates the uptake and subsequent utilization of glucose by brain tissue, enhances the biosynthesis of proteins and nucleic acids, but also affects various neurotransmitter systems.
Nicergoline improved the functioning of the cholinergic systems of the brain in elderly animals. Chronic administration of nicergoline to elderly rats reversed the age-related decline in acetylcholine levels (in the cerebral cortex and striatum) as well as the decrease in acetylcholine release (in the hippocampus) in vivo. After prolonged oral administration of nicergoline, an increase in ChAT (choline acetyltransferase) activity and an increase in the density of muscarinic receptors were also observed. In addition, in both in vitro and in vivo experiments, nicergoline significantly increased AChE (acetylcholinesterase) activity. In these experiments, parallel dynamics of neurochemical changes and persistent improvements in behavioral reactions were noted. For example, in a maze study, mature animals chronically treated with nicergoline developed a response similar to that of juveniles.
It was found that nicergoline improves the state of the cognitive sphere in cases of cognitive impairment caused by various factors (hypoxia, electroconvulsive therapy, scopolamine). With oral administration of nicergoline in low doses, activation of dopamine metabolism in elderly animals was noted, especially in the mesolimbic region, which is probably due to the effect on dopamine receptors. Nicergoline improved the mechanisms of signal transduction in cells in elderly animals. Both after single and long-term oral administration of the drug, basal and agonist-sensitive phosphoinositide metabolism increased. Nicergoline also stimulates the activity and translocation through the cell membrane of calcium-dependent isoforms of protein kinase C. These enzymes are involved in the mechanism of secretion of soluble APP (amyloid precursor protein), which leads to an increase in its release and a decrease in the production of pathological beta-amyloid, which has been demonstrated in human neuroblastoma cultures .
Due to its antioxidant effect and activation of detoxification enzymes, nicergoline protected nerve cells from death caused by oxidative stress and apoptosis in experimental models in vivo and in vitro. Nicergoline attenuates the age-related decline in NO synthase (nNOS) mRNA in neurons, which improves cognitive function.
Pharmacodynamics studies in humans
Pharmacodynamics were assessed in young and elderly healthy volunteers, as well as in elderly patients with cognitive impairment using computerized EEG. Nicergoline had a normalizing effect on EEG parameters in elderly patients and adults after hypoxia, which was manifested in an increase in α- and β-activity and a decrease in δ- and θ-activity. With long-term use of nicergoline (for 2-6 months), positive changes in the parameters of evoked response potentials were noted in patients with mild to moderate dementia of various etiologies (senile dementia of the Alzheimer's type and mild intellectual disability), these changes correlated with improvement in clinical symptoms . Considering the above, it is clear that nicergoline has broad modulatory effects on the cellular and molecular mechanisms involved in the pathophysiology of dementia.
In double-blind, placebo-controlled clinical trials, more than 1,500 patients with dementia (Alzheimer's, vascular and mixed types) received nicergoline 60 mg/day or placebo. Improvements in dementia-related cognitive function and behavior have been observed following long-term use of nicergoline. Positive dynamics were noted after 2 months of treatment and the improvements achieved during therapy were maintained for one year.
Nicergoline reduces platelet aggregation and improves blood rheological parameters. Increases the speed of blood flow in the upper and lower extremities.
Indications for use:
Symptomatic treatment of cognitive impairment, including dementia with chronic cerebrovascular and organic brain lesions, accompanied by decreased memory, concentration, thinking, activity, increased fatigue, and emotional disorders.
Note:
Before starting therapy with nicergoline, you must make sure that these symptoms are not a manifestation of another disease (such as internal diseases, psychiatric or neurological diseases) and do not require specific therapy.
Directions for use and dosage:
Inside.
The tablets should be taken with meals, with a small amount of liquid, without chewing.
The recommended daily dose is 30-60 mg, depending on the severity of symptoms and the individual patient's response to treatment.
A daily dose of 30 mg is recommended to be taken with breakfast.
In patients with impaired renal function (serum creatinine ≥2 mg/dL), nicergoline is recommended to be used in lower therapeutic doses.
Interaction with other drugs:
Nicergoline may enhance the effect of antihypertensive drugs. Nicergoline is metabolized by the CYP2D6 isoenzyme, so the possibility of its interaction with drugs that are metabolized with the participation of the same enzyme cannot be excluded.
When using nicergoline with acetylsalicylic acid, bleeding time may increase.
Nicergoline affects the metabolism and excretion of uric acid, and therefore caution should be exercised when using it with drugs that affect the metabolism of uric acid.
Nicergoline potentiates the effect of beta-blockers on the heart.
Nicergoline has an antagonistic effect on the vasoconstrictor effect of sympathomimetics through its alpha-adrenergic blocking effect.
Nicergoline-LF capsules 10 mg No. 10x3
Name
Nicergoline-LF caps. 10 mg in container pack No. 10x5
Description
Hard gelatin capsules No. 1 are cylindrical in shape with white hemispherical ends.
Main active ingredient
Nicergoline.
Release form
Capsules.
Dosage
10mg
Indications for use
Nicergoline-LF is indicated for the symptomatic treatment of mild to moderately severe dementia for the correction of cognitive and behavioral disorders.
Directions for use and doses
For oral administration. 5 mg - 10 mg three times a day with equal intervals between doses for a long period of time (up to several months). For vascular dementia, the use of 30 mg 2 times a day is indicated (it is recommended to consult a doctor every 6 months about the advisability of continuing therapy). The dose, duration of therapy and route of administration depend on the nature of the disease. In patients with impaired renal function (serum creatinine ≥ 2 mg/dL), nicergoline is recommended to be used in lower therapeutic doses.
Use during pregnancy and lactation
There are no specific studies of use during pregnancy. Nicergoline-LF should be used only if there is a clear need and under the direct supervision of a physician. While taking the drug, you must stop breastfeeding, because nicergoline and its metabolic products pass into mother's milk.
Impact on the ability to drive vehicles and operate machinery
Despite the fact that the drug improves reaction and concentration, its effect on the ability to drive a car and use complex equipment has not been specifically studied. Caution should be exercised given the nature of the underlying disease.
Precautionary measures
In therapeutic doses, nicergoline, as a rule, does not affect blood pressure, however, in patients with arterial hypertension it can cause a gradual decrease. The drug acts gradually, so it should be taken for a long time, and the doctor should periodically (at least every 6 months) evaluate the effect of treatment and the advisability of continuing it. Nicergoline-LF should be used with caution if there is a history of hyperuricemia or gout and/or in combination with drugs that interfere with the metabolism or excretion of uric acid. When using medications containing ergot derivatives, including nicergoline, there is a risk of developing fibrosis and ergotism.
Interaction with other drugs
Nicergoline may enhance the effect of antihypertensive drugs. Nicergoline is metabolized by the cytochrome CYP450 2D6, so the possibility of its interaction with drugs that are metabolized with the participation of the same enzyme cannot be ruled out.
Contraindications
Recent myocardial infarction, acute bleeding, severe bradycardia, impaired orthostatic regulation, hypersensitivity to nicergoline or other components of the drug.
Compound
One capsule of Nicergoline-LF contains: Active substance: nicergoline – 10 mg. Excipients: microcrystalline cellulose, magnesium stearate, sodium carboxymethylcellulose, calcium hydrogen phosphate dihydrate. Composition of the gelatin capsule shell containing 10 mg of nicergoline: Gelatin, titanium dioxide E-171, purified water.
Overdose
Symptoms: transient pronounced decrease in blood pressure. Treatment: special treatment is usually not required; the patient just needs to take a horizontal position for a few minutes. In exceptional cases, in case of severe disruption of the blood supply to the brain and heart, it is recommended to administer sympathomimetic drugs under constant monitoring of blood pressure.
Side effect
When taking the drug, there is a possibility of developing adverse reactions, which are classified by organ system and frequency of occurrence: very often >1/10, often from >1/100 to 1/1000 to
Storage conditions
In a place protected from moisture and light at a temperature not exceeding 25 ° C. Keep out of the reach of children.
Buy Nicergoline-LF caps. 10 mg in container pack No. 10x5 in the pharmacy
Price for Nitsergolin-LF caps. 10 mg in container pack No. 10x5
Instructions for use for Nitsergolin-LF caps. 10 mg in container pack No. 10x5
Special instructions:
Clinical studies have shown that with single or repeated use of nicergoline, a decrease in systolic and, to a greater extent, diastolic blood pressure can be observed in patients with normal values and with high blood pressure. These results may vary as other studies have not shown a change in blood pressure values.
The drug acts gradually, so it should be taken for a long time, and the doctor should periodically (at least every 6 months) evaluate the effect of treatment and the advisability of continuing it.
An association with fibrosis (eg, pulmonary, cardiac, valvular, and retroperitoneal) has been noted with the use of ergot alkaloids that have serotonin 5HT2β receptor antagonist activity.
Symptoms of ergotism (including nausea, vomiting, diarrhea, abdominal pain, and peripheral vasoconstriction) have been reported with certain ergot alkaloids and their derivatives.
Doctors should be aware of the possible symptoms of ergot drug overdose before prescribing this class of drugs.
Nicergoline-NAN tablets p/o 5 mg No. 15x2
Name
Nicergolin-NAN tablet p/o 5 mg in container pack No. 15x2
Description
Nicergoline-NAN 5 mg: round, biconvex, light brown film-coated tablets.
Main active ingredient
Nicergoline
Release form
Pills
Dispensing the drug
Over the counter
pharmachologic effect
Nicergoline is an ergoline derivative that has an alpha-1-adrenergic blocking effect. After oral administration, nicergoline is rapidly and extensively metabolized to form a number of metabolites, which also have effects at various levels of the central nervous system. After oral administration, nicergoline has various neuropharmacological effects, since it not only stimulates the uptake and subsequent utilization of glucose by brain tissue, enhances the biosynthesis of proteins and nucleic acids, but also affects various neurotransmitter systems. Nicergoline improved the functioning of the cholinergic systems of the brain in elderly animals. Chronic administration of nicergoline to elderly rats reversed the age-related decline in acetylcholine levels (in the cerebral cortex and striatum) as well as the decrease in acetylcholine release (in the hippocampus) in vivo. After prolonged oral administration of nicergoline, an increase in choline acetyltransferase activity and an increase in muscarinic receptor density were also observed. In addition, in both in vitro and in vivo experiments, nicergoline significantly increased acetylcholinesterase activity. In these experiments, parallel dynamics of neurochemical changes and persistent improvements in behavioral reactions were noted. For example, in a maze study, mature animals chronically treated with nicergoline developed a response similar to that of young animals. It was found that nicergoline improves the state of the cognitive sphere in cases of cognitive impairment caused by various factors (hypoxia, electroconvulsive therapy, scopolamine). When administered orally, nicergoline in low doses increased dopamine metabolism in elderly animals, especially in the mesolimbic region, which is probably due to the effect on dopaminergic receptors. Nicergoline improved the mechanisms of signal transduction in cells in elderly animals. Both after single and long-term oral administration of the drug, basal and agonist-sensitive phosphoinositide metabolism increased. Nicergoline also stimulates the activity and translocation through the cell membrane of Ca-dependent isoforms of protein kinase C. These enzymes are involved in the mechanism of secretion of soluble amyloid precursor protein, which leads to an increase in its release and a decrease in the production of pathological beta-amyloid, which has been demonstrated in human neuroblastoma cultures. Due to its antioxidant effect and activation of detoxification enzymes, nicergoline protected nerve cells from death caused by oxidative stress and apoptosis in experimental models in vivo and in vitro. Nicergoline attenuates the age-related decline in NO synthase (nNOS) mRNA in neurons, which improves cognitive function.
Indications for use
Symptomatic treatment of mild and moderately severe dementia for the correction of cognitive and behavioral disorders. Note: before starting treatment, you must make sure that these symptoms are not a manifestation of another disease (for example, a therapeutic, psychiatric or neurological profile) and do not require special treatment.
Use during pregnancy and lactation
Specific studies of use during pregnancy have not been conducted. Taking into account the indications for use, it is unlikely that nicergoline will be prescribed to pregnant women and nursing mothers. The use of Nicergolin-NAN during pregnancy is possible under the direct supervision of a physician and only if the potential benefit to the patient outweighs the possible risk to the fetus and child. Since the likelihood of nicergoline passing into breast milk has not been established, the use of nicergoline during breastfeeding is not recommended.
Precautionary measures
In studies using single or multiple doses of nicergoline, it was shown that the drug may lead to a decrease in systolic pressure and, to a lesser extent, diastolic pressure in normotensive patients and patients with high blood pressure. Other studies have not found this effect. Sympathomimetics (alpha or beta) should be used with caution in patients being treated with nicergoline (see section Interactions with other drugs). When using some ergot alkaloids that exhibit agonistic activity against 5-HT 2? serotonin receptor, fibrosis has been observed (eg, pulmonary, cardiac, valvular, and retroperitoneal). Symptoms of ergotism (including nausea, vomiting, diarrhea, abdominal pain, and peripheral vasoconstriction) have been reported following consumption of certain ergot alkaloids and their derivatives. When prescribing drugs in this class, clinicians and prescribers should be aware of the signs and symptoms of ergot overdose. If special precautions are taken, nicergoline can be used in patients with mild bradycardia. Cerebrovascular disorders can also be a manifestation of diseases such as heart failure, arrhythmias or arterial hypertension. If these diseases are present, it is necessary to begin with their treatment. Nicergoline inhibits platelet aggregation and reduces blood viscosity. In patients with a predisposition to disorders, blood coagulation parameters should be regularly monitored. The same monitoring should be carried out at the beginning of treatment with nicergoline in patients simultaneously receiving anticoagulants (see sections Interactions with other drugs and Side effects). Nicergoline-NAN should be used with caution if there is a history of hyperuricemia or gout and/or in combination with drugs that may affect the metabolism and excretion of uric acid. If you have one of the diseases or conditions listed above, be sure to consult your doctor before taking the drug.
Interaction with other drugs
Nicergoline should be used with caution with the following drugs: Antihypertensive drugs: nicergoline may enhance their therapeutic effect. Nicergoline may potentiate the cardiotropic effects of beta-blockers. Sympathomimetics (alpha and beta): nicergoline reduces the vasoconstrictor effect of sympathomimetics, as it is an alpha-adrenergic receptor antagonist. Drugs metabolized by CYP 2D6: Since nicergoline is metabolized by the cytochrome CYP 2D6, the possibility of its interaction with drugs that are metabolized by the same enzyme system cannot be excluded. Antiplatelet agents and anticoagulants (eg, acetylsalicylic acid): increases the effect on hemostasis and thus may potentiate prolongation of bleeding time. Drugs affecting uric acid metabolism: nicergoline may lead to an asymptomatic increase in serum uric acid levels. Your doctor should be informed about all the medications you take. Before taking any medication while being treated with Nicergoline-NAN, consult your doctor.
Contraindications
- hypersensitivity to nicergoline or other components of the drug; - recent acute myocardial infarction; - acute bleeding; - severe bradycardia; — violation of orthostatic regulation; - children and adolescents under 18 years of age (safety and effectiveness of use in children under 18 years of age have not been established).
Compound
one tablet contains: active substance: nicergoline 5 mg excipients: microcrystalline cellulose, sodium carboxymethylcellulose, Kolliphor P188 micro poloxamer, magnesium stearate, anhydrous calcium hydrogen phosphate; composition of the Nicergolin-NAN tablet shell, 5 mg: polyvinyl alcohol, titanium dioxide (E171), macrogol (polyethylene glycol), talc, yellow iron oxide (E172), red iron oxide (E172), black iron oxide (E172);
Directions for use and doses
Dosage: The recommended daily dose is 30-60 mg per day and can be divided into 3 doses. Elderly persons (over 65 years of age) Based on the results of studies of the pharmacokinetics and tolerability of nicergoline, no dose adjustment is required in elderly patients. Children and adolescents under 18 years of age Nicergoline is not indicated for the treatment of children and adolescents under 18 years of age. The effectiveness and safety of use in this category of people has not been established. Patients with renal impairment Since nicergoline metabolites are excreted mainly by the kidneys, it is recommended that nicergoline be used in lower doses in patients with impaired renal function. Directions for use and duration of use: For oral administration only. It is recommended to take the tablets with meals, without chewing, with a small amount of water. If the drug is prescribed in a daily dose of 30 mg (1 tablet), it is recommended to take it with breakfast. Since improvement in symptoms is usually observed after 4-6 weeks of starting treatment, it is recommended to take nicergoline for a long period of time. The duration of taking the drug in accordance with the recommendations is not limited in time, but at certain intervals (at least once every 6 months), the doctor must evaluate the advisability of continuing treatment.
Overdose
If you take a larger dose of medication than prescribed by your doctor, you should immediately contact a specialist to provide timely medical assistance! Symptoms: transient pronounced decrease in blood pressure. Treatment: special treatment is usually not required; the patient just needs to take a horizontal position for a few minutes. In exceptional cases, in case of a sharp disruption of the blood supply to the brain and heart, it is recommended to administer sympathomimetic drugs under constant blood pressure monitoring.
Side effect
In general, losartan is well tolerated; side effects are mild and transient and do not require discontinuation of the drug. During treatment with losartan potassium, undesirable effects may develop, which are divided according to the frequency of occurrence into: very common (> 1/10); frequent (> 1/100 and 1/1000 and 1/10000 and 5.5 mmol/l). Experience with post-registration use Disorders of the blood and lymphatic system: frequency unknown - anemia, thrombocytopenia, Disorders of the immune system: rarely - hypersensitivity reactions, anaphylactic reactions, angioedema (including swelling of the larynx, glottis, tongue, face, lips, pharynx and /or tongue, causing airway obstruction) and vasculitis (Henoch-Schönlein purpura). Respiratory, thoracic and mediastinal disorders: frequency unknown – cough. Gastrointestinal disorders: frequency unknown – diarrhea. Disorders of the liver and biliary tract: rarely - hepatitis; frequency unknown - pancreatitis, liver dysfunction. Skin and subcutaneous tissue disorders: frequency unknown - urticaria, itching, rash, photosensitivity. Musculoskeletal and connective tissue disorders: frequency unknown - myalgia, arthralgia, rhabdomyolysis. Genital and breast disorders: frequency unknown – erectile dysfunction/impotence. General disorders and disorders at the injection site: frequency unknown - malaise. Mental disorders: frequency unknown - depression. Nervous system disorders: frequency unknown – migraine, dysgeusia. Hearing and labyrinthine disorders: frequency unknown - tinnitus. Impact on the results of laboratory and instrumental studies: frequency unknown - hyponatremia. The following adverse reactions occurred more frequently in patients receiving losartan than in patients receiving placebo (frequency unknown): back pain, urinary tract infection, flu-like symptoms. Renal and urinary tract disorders: Due to inhibition of the renin-angiotensin-aldosterone system, changes in renal function, including renal failure, have been reported in patients at risk; these changes in renal function may be reversible after discontinuation of therapy. Children The profile of adverse reactions in children is similar to that in adult patients. Data regarding adverse reactions in children are limited. Important information about some components of the drug Losartan-NAN, film-coated tablets, 100 mg contains lactose. If your doctor has told you that you have an intolerance to certain sugars, you should consult your doctor before using this medicine.
Storage conditions
In a place protected from light and moisture, at a temperature not exceeding 25? C. Keep out of the reach of children.
