Compound
The composition of the drug Sermion differs slightly depending on the amount of active substance in the composition and on the form of release of the drug.
1 tablet of Sermion contains 5 mg / 10 mg / 30 mg of the active substance nicergoline and auxiliary components: calcium hydrogen phosphate dihydrate, sodium carboxymethylcellulose, magnesium stearate, MCC. The tablet shell consists of: talc, sucrose, sandarac resin, magnesium carbonate, carnauba wax, rosin, acacia resin, titanium dioxide (E171), sunset yellow (E110).
Lyophilisate in the form of powder or white porous mass for the preparation of injection solutions. A solvent is also included - a colorless transparent liquid. Active ingredient: 4 ml of nicergoline . Excipients: tartaric acid and lactose monohydrate. Solvent composition: benzalkonium chloride, sodium chloride, water for injection (up to 4 ml).
Sermion tablets p/o 5 mg No. 15x2
Name
Sermion tablet p/o 5 mg in blister pack. in pack No. 15x2
Main active ingredient
Nicergoline
Release form
pills
Compound
Active substance: nicergoline. One film-coated tablet contains 5, 10 or 30 mg of nicergoline. Other excipients: Tablet core: calcium hydrogen phosphate dihydrate (E341), microcrystalline cellulose (E460), magnesium stearate (E470), sodium carboxymethylcellulose (E466). Tablet shell (for 5 mg and 10 mg tablets): sucrose, talc (E553), acacia gum (E414), sandarac gum, magnesium carbonate (E504), titanium dioxide (E171), rosin, carnauba wax (E903), sunset yellow (E110, for 5 mg tablets); Tablet shell (for 30 mg tablets): hydroxypropyl methylcellulose (E464), titanium dioxide (E171), polyethylene glycol 6000 (E1521), yellow iron oxide (E172), silicone.
Description
Sermion, 5 mg - round, convex, film-coated tablets, orange in color. Sermion, 10 mg - round, convex, film-coated tablets, white. Sermion, 30 mg - round, biconvex, film-coated tablets, yellow. Film-coated tablets 5 mg; 15 tablets in a blister (PVC/PVDC - aluminum foil), 2 blisters and instructions for use in a cardboard box. Film-coated tablets 10 mg; 25 tablets in a blister (PVC/PVDC - aluminum foil), 2 blisters and instructions for use in a cardboard box. Film-coated tablets 30 mg; 15 tablets in a blister (PVC/PVDC - aluminum foil), 2 blisters and instructions for use in a cardboard box.
Dosage
5 mg; 10 mg; 30 mg;
Indications for use
The active substance contained in Sermion is a semi-synthetic derivative of ergot alkaloid, which has a beneficial effect on impaired brain metabolism in older people. The active substance (nicergoline) connects with certain binding sites of various messenger substances produced in the human body and influencing the transmission of impulses between nerve cells. An imbalance in the content of these messenger substances leads to the development of disorders. In this way, Sermion promotes recovery processes in the brain during deficient conditions. Sermion is used as an adjuvant to treat symptoms of brain dysfunction caused by the aging process and cerebrovascular accidents. These disorders may manifest as: • attention deficit disorders and memory impairment; • attention disorders; • decreased motivation; • failure to maintain personal hygiene; • fatigue or dizziness; • reduction or absence of social seclusion, self-isolation). Before starting treatment with Sermion, your attending physician will make sure that these symptoms are not a manifestation of another disease (therapeutic, psychiatric or neurological profile) and do not require specific treatment.
Contraindications
• if you have hypersensitivity (allergy) to the active substance - nicergoline, other ergot alkaloid derivatives or any other component included in the Sermion drug (listed in the Composition section); • if you have recently suffered a myocardial infarction; • in case of acute bleeding; • at risk or tendency to collapse; • with a rare heartbeat; • for dizziness and fainting that occurs in certain circumstances, for example, when standing up quickly
Use during pregnancy and lactation
If you are pregnant or breastfeeding, think you may be pregnant, or are planning to become pregnant, consult your doctor or pharmacist before using this medicine. Taking into account the indications for use (see section “What is Sermion and in what cases is this drug used”), the use of this drug in pregnant women and breastfeeding women is unlikely and is not intended. Sermion should not be used during pregnancy and breastfeeding.
Directions for use and doses
In all cases, you should strictly follow the doctor's instructions. If you have any doubts about using this medicine, consult your doctor or pharmacist. As a rule, the dose of the drug is 1-2 tablets per day. Accordingly, one tablet is taken during breakfast and, if necessary, the next tablet is taken at dinner. If your doctor has prescribed Sermion one 30 mg tablet per day (for example, if you have impaired kidney function), then it is best to take it with breakfast. The tablets should be taken with meals, without chewing, with a small amount of water. Due to the fact that positive dynamics are usually observed 4-6 weeks from the start of treatment, it is recommended to take the drug for a long period of time. At certain intervals (but not less than every 6 months), the doctor will evaluate the advisability of continuing treatment with Sermion. Children and adolescents under 18 years of age Sermion is not intended for use in children and adolescents under 18 years of age. Patients with impaired renal function Your doctor will prescribe the dose you need. If your kidney function is severely impaired, your doctor may prescribe the drug at a lower dose. The effect of treatment appears gradually. Because treatment is usually given over a long period of time, your doctor will determine at appropriate intervals whether you should continue treatment. If you take more tablets than you should, your blood pressure may drop suddenly or your heart rate may slow down. In this case, you should immediately consult a doctor. Special treatment is usually not required, and in most cases it is enough to take a horizontal position for a few minutes. In exceptional cases, the doctor will take the necessary measures. If you forget to take the drug Do not take a double dose of Sermion to make up for the missed dose and continue to take the drug as directed by your doctor. If you stop taking the drug You should not suddenly stop taking Sermion without first consulting your doctor. If adverse reactions occur, your doctor will discuss possible measures with you, as well as the possibility of prescribing other medications to treat them. If you have any further questions about the use of this drug, consult your doctor or pharmacist.
Side effect
As with other medicines, Sermion can sometimes cause side effects, although not everyone gets them. Common (may affect 1 in 10 people) Complains of abdominal pain. Uncommon (may occur in 1 in 100 people) Hyperactivity, confusion, insomnia, drowsiness, dizziness and weakness, headaches, decreased blood pressure, redness of the skin, constipation, diarrhea, nausea, itching, increased concentration of uric acid in the blood. Not known: frequency cannot be determined from available data Hot flushes, skin rash, painful connective tissue overgrowth (fibrosis), nasal congestion. Reporting side effects If you notice any side effects, including those not listed in this leaflet, please tell your doctor or pharmacist. By submitting information about adverse events, you are helping to collect information about the safety of this medicine.
Interaction with other drugs
Tell your doctor or pharmacist if you are currently taking, have recently taken or may take any other medicines. Taking two or more medications may cause drug interactions, even if the drugs are taken at different times. The effects and side effects of these medicines may be increased or decreased. Your doctor will check what medications you are taking and, if necessary, adjust them. Sermion may enhance the effect of medications used to reduce high blood pressure (including so-called “beta blockers”). The vasoconstrictor effect of some drugs on smooth muscles (drugs with symptomatic effect) may be weakened by Sermion. Sermion may prolong blood clotting time, which is increased by acetylsalicylic acid or certain anticoagulants. Caution must be exercised when using Sermion simultaneously with drugs that affect the metabolism and excretion of uric acid (due to the risk of developing gout). Effects of food, drinks and alcohol During treatment with Sermion (as with any other medicines), you should not drink alcohol as the effect may be unpredictable.
Precautionary measures
Before using Sermion, consult your doctor or pharmacist. Sermion should be taken with caution: • with a mild to moderate decrease in heart rate; • if you have a bleeding disorder or are taking medications that inhibit coagulation. In some cases, your doctor may do blood clotting tests more often than usual; • if you have high levels of uric acid in your blood or are taking or have previously taken medicines to treat gout. • simultaneous treatment with sympathomimetics (alpha or beta). Cases of fibrosis of the lungs, heart, heart valves and retroperitoneum have been observed with the use of certain ergot alkaloid derivatives. The following symptoms have been observed following ingestion of certain ergot alkaloids and their derivatives: nausea, vomiting, diarrhea, abdominal pain, and peripheral vasospasm.
Storage conditions
Store the drug at a temperature not exceeding 25°C. Keep the drug out of the reach of children. Do not use the drug after the expiration date indicated on the carton or blister after the word “EXP”. The expiration date is the last day of the specified month. Medicines should not be disposed of in sewers or household waste. Ask your pharmacist for instructions on how to dispose of unused medicines. These measures will help protect the environment.
Release form
- 5 mg tablets: convex round tablets with an orange coating in blisters of 15 pcs. A cardboard pack contains 2 blisters.
- 10 mg tablets: convex round tablets with a white coating in blisters of 25 pcs. A cardboard pack contains 2 blisters.
- Tablets 30 mg: biconvex round tablets with a yellow coating in blisters of 15 pcs. A cardboard pack contains 2 blisters.
- The lyophilisate for the preparation of injection solutions is contained in colorless glass bottles. Also included are ampoules with solvent. One cardboard box contains 4 bottles of lyophilisate and 4 ampoules with solvent.
pharmachologic effect
The medicine improves peripheral and cerebral circulation, and is also an alpha-blocker. The main active ingredient of the drug nicergoline is a derivative of ergoline and improves hemodynamic and metabolic processes occurring in the brain.
The drug reduces platelet aggregation and also improves blood rheology; in addition, it accelerates blood flow in the lower and upper extremities. The improvement in blood flow is due to the alpha 1-adrenergic blocking effect.
Sermion directly affects the cerebral neurotransmitter systems - dopaminergic, noradrenergic and acetylcholinergic, which has a beneficial effect on cognitive processes. With long-term use of the drug, patients experienced a decrease in the severity of behavioral disorders associated with dementia, and the cognitive function of the body also improved.
Pharmacodynamics and pharmacokinetics
Absorption (for tablets)
Once in the human body, nicergoline is absorbed very quickly and with virtually no residue. The rate and degree of absorption of nicergoline practically does not depend on either the dosage form or food intake. When using a dosage of up to 60 mg, the pharmacokinetics of nicergoline is linear, without changing depending on the age of the drug taker.
Distribution and metabolism
The substance nicergoline binds more than 90% to plasma proteins, while the degree of its affinity for serum albumin is less than for the α-acid of the glycoprotein. Nicergoline, as well as its metabolites, can be distributed in blood cells.
The main metabolic products of the substance nicergoline are: 6-methyl-8β-hydroxymethyl-10α-methoxyergoline (MDL, the result of demethylation occurring under the action of the CYP2D6 isoenzyme) and 1,6-dimethyl-8β-hydroxymethyl-10α-methoxyergoline (MMDL, a product formed as a result of hydrolysis).
When nicergoline is administered intravenously or taken orally, the ratio of AUC values for MDL and MMDL indicates apparent first-pass metabolism through the liver. With 30 mg of the drug, Cmax MMDL (21 ± 14 ng/ml) and MDL (41 ± 14 ng/ml) were achieved after 1 and 4 hours, respectively, after which the concentration of MDL decreased with a half-life of 13-20 hours. The studies also confirmed the absence of accumulation of other metabolites in the blood (including MMDL).
Removal
The substance nicergoline is excreted from the body in the form of metabolites , mostly in the urine (about 80%), as well as in feces (about 10-20% of the total dose).
Pharmacokinetics manifested in special clinical cases
Those patients who suffered from severe renal failure
Sermion
A drug that improves cerebral and peripheral blood circulation, an alpha-blocker.
Nicergoline is an ergoline derivative that improves metabolic and hemodynamic processes in the brain. Reduces platelet aggregation and improves the rheological properties of blood, increases the speed of blood flow in the upper and lower extremities. It has an alpha1-adrenergic blocking effect, which improves blood flow. It has a direct effect on the cerebral neurotransmitter systems (noradrenergic, dopaminergic and acetylcholinergic), increasing their activity, which helps optimize cognitive processes.
As a result of long-term therapy with nicergoline, a persistent improvement in cognitive function and a decrease in the severity of behavioral disorders associated with dementia were observed.
Pharmacokinetics
Suction
After oral administration, nicergoline is quickly and almost completely absorbed.
Food intake or dosage form do not have a significant effect on the degree and rate of absorption of nicergoline. The pharmacokinetics of nicergoline when used in doses up to 60 mg is linear and does not change depending on the age of the patient.
Distribution and metabolism
Nicergoline actively (>90%) binds to plasma proteins, and the degree of its affinity for the α-acid of the glycoprotein is greater than for serum albumin. It has been shown that nicergoline and its metabolites can be distributed in blood cells.
The main metabolic products of nicergoline are 1,6-dimethyl-8β-hydroxymethyl-10α-methoxyergoline (MMDL, a hydrolysis product) and 6-methyl-8β-hydroxymethyl-10α-methoxyergoline (MDL, a demethylation product by the CYP2D6 isoenzyme).
The ratio of AUC values for MMDL and MDL after oral administration of nicergoline indicates a pronounced first-pass metabolism through the liver. After administration of 30 mg of nicergoline orally, Cmax 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 from T1/2 13-20 hours. Studies confirm the absence of accumulation of other metabolites (including MMDL) in the blood.
Removal
Nicergoline is excreted in the form of metabolites, mainly in the urine (approximately 80% of the total dose), and in small amounts (10-20%) in feces.
Pharmacokinetics in special clinical situations
In patients with severe renal failure, there was a significant decrease in the rate of excretion of metabolic products in the urine compared with patients with normal renal function.
Indications for use of Sermion
The drug is indicated for:
- chronic and acute cerebral vascular and metabolic disorders (occurring as a result of arterial hypertension , atherosclerosis , embolism or thrombosis of cerebral , including vascular dementia , acute transient cerebral circulatory disorder, as well as headache caused by vasospasm );
- chronic and acute vascular and metabolic disorders (functional and organic arteriopathy of the extremities , syndromes that manifest themselves as a result of impaired peripheral blood flow, as well as Raynaud's disease );
- as an additional remedy during the treatment of hypertensive crisis .
Frequently asked questions about Sermion
Why is Sermion prescribed?
The medication is used during acute conditions or for chronic cerebral, metabolic and vascular disorders due to atherosclerosis, arterial hypertension, thrombosis or embolism of cerebral vessels.
How to take Sermion correctly - before or after meals?
The medication should be taken before eating with plenty of liquid. Do not chew or crush the tablet, as it is coated with a special coating.
Where can I buy Sermion?
You can buy Sermion medicine in our online pharmacy 911 at the most affordable prices in Ukraine. We try to maintain the lowest prices and high quality of popular medications and their analogues, as well as intimate hygiene products, skin care products, cotton swabs, patches, balms, gels, ointments and many other products that are presented on our website.
Contraindications
The drug is contraindicated in:
- violation of orthostatic regulation;
- recent myocardial infarction ;
- severe bradycardia ;
- acute bleeding;
- hypersensitivity to those substances contained in the drug.
The drug should be taken with caution if there is a history of gout or hyperuricemia and/or if the drug must be combined with drugs that interfere with the excretion of uric acid and/or metabolism.
In addition to the above, indications for the use of Sermion tablets have additional restrictions:
- the patient's age is under 18 years;
- periods of pregnancy and lactation;
- deficiency in the body of isomaltase/sucrase, glucose-galactose malabsorption, as well as fructose intolerance.
Contraindications and side effects
The medicine Sermion is not used in the treatment of patients:
- with increased susceptibility to the active components of the drug;
- have recently suffered a myocardial infarction;
- with acute bleeding;
- with orthostatic hypotension;
- with acute bradycardia;
- simultaneously taking sympathomimetics (alpha or beta receptor antagonists);
- taking anticoagulant and antiplatelet drugs: when they interact, it is necessary to monitor the indicators of the blood coagulation system;
- taking cholinomimetic drugs: the medication may enhance their effects.
The drug Sermion is not prescribed for breastfeeding infants. Also not prescribed for children. During pregnancy - only under the supervision of a doctor after determining the balance of benefit and harm.
The drug is available with a prescription and is stored in its original packaging at temperatures up to 25°C.
Side effects
For the nervous system: insomnia or drowsiness occasionally occurs.
For the cardiovascular system: occasionally there is a pronounced decrease in blood pressure (especially with parenteral administration of the drug), fever, dizziness.
For metabolism: an increase in the concentration of uric acid in the blood may occur. This effect does not depend on dosage or duration of treatment.
Other side effects: skin rashes and dyspeptic symptoms occur occasionally.
As a rule, the side effects of the drug are moderate.
Instructions for use of Sermion (Method and dosage)
Sermion tablets
The drug is prescribed orally.
For post-stroke conditions, cognitive vascular disorders and chronic cerebral circulatory disorders, Sermion tablets should be taken three times a day, 10 mg. The minimum course of treatment is 3 months, since the therapeutic effect of the drug appears gradually.
For vascular dementia, the medicine Sermion should be taken twice a day, 30 mg. It is recommended to consult with your doctor every 6 months to determine the advisability of continuing the course of treatment.
For ischemic stroke caused by thrombosis , atherosclerosis and embolism of cerebral vessels, acute as well as transient cerebral circulatory disorders (with hypertensive cerebral crises and transistor ischemic attacks ) - the course of treatment is best started with parenteral administration of the drug Nicergoline , after which Sermion is taken orally.
For peripheral circulatory disorders, the medicine should be taken three times a day, 10 mg at a time, for a long time (several months).
Patients who have impaired renal function (serum creatinine level exceeds 2 mg/dL) should take Sermion at a lower therapeutic dosage.
Instructions for use of Sermion lyophilisate
Intramuscularly: 2-4 ml of the drug is administered twice a day (2-4 mg).
Intravenously: the drug is administered slowly at a dosage of 4-8 mg in 100 ml of 5-10% dextrose solution or 0.9% sodium chloride solution. At this dosage, injections with the drug can be given up to several times a day.
sodium chloride solution is injected within 2 minutes .
It is recommended to use the reconstituted solution immediately after preparation.
The duration of therapy, dosage, and method of administration of the drug into the body depend on the disease. Sometimes it is better to start treatment with parenteral administration of the drug, and then switch to oral administration for the purpose of maintenance treatment.
Patients who have impaired renal function (serum creatinine level exceeds 2 mg/dL) Sermion should be taken at a lower therapeutic dosage.
Nicergoline (sermion) is a hydrated semi-synthetic derivative of ergoline (contains an ergoline core and a bromine-substituted nicotinic acid residue). The pharmacotherapeutic effectiveness of this drug is determined by two main properties: an adrenergic blocking effect, leading to improved blood flow, and a direct effect on the cerebral neurotransmitter systems - noradrenergic, dopaminergic and acetylcholinergic. Nicergoline is used to treat cerebrovascular insufficiency, cognitive impairment in the elderly, including various forms of dementia, as well as a number of other disorders, mainly of a vascular nature [1-4, 9, 16, 18]. The drug was developed in the late 60s of the 20th century, and it began to be used in clinical practice in the 70s, first in Italy and then in other countries [16, 18]. Currently, nicergoline is registered in more than 50 countries (Europe, Asia, Latin America) [18].
In clinical terms, nicergoline was initially considered as a vascular drug that antagonizes α1-adrenergic receptors, and its therapeutic efficacy was associated with vasodilation, decreased vascular resistance, and increased arterial blood flow [1, 8, 16, 18]. Therefore, it was used mainly to treat dementia due to cerebrovascular insufficiency. However, further studies have shown that nicergoline has a much wider spectrum of action - at the molecular and cellular levels, acting not only on blood vessels, but also blood cells (platelets) and neurons [18]. Currently, the drug is used for dementia of various origins (Alzheimer's disease, vascular dementia), cerebrovascular disorders (including stroke, transient ischemic attacks, post-stroke disorders, migraine), peripheral vascular disorders (obliterating atherosclerosis of the vessels of the lower extremities), imbalances of vestibular origin, with glaucoma, Parkinson's disease, as well as benign prostatic hyperplasia [18].
When taken orally, the drug has linear pharmacokinetics, which is practically independent of age; it is quickly and almost completely absorbed in the gastrointestinal tract [1, 18]. Food intake does not have a significant effect on the absorption of nicergoline. Unlike another ergot derivative, hydrergine, nicergoline is excreted primarily in the urine (80%) in the form of metabolites, and only about 20% in feces [1, 18]. In healthy volunteers, it was shown that after taking a tablet drug, its maximum concentration in the blood serum is achieved within 3 hours, and the half-life is about 15 hours [18]. Nicergoline is usually prescribed at a dose of 30 mg 2 times a day, the duration of therapy ranges from 2 to 12 months or more [16, 18]. In Asian countries, nicergoline is usually used in smaller doses (however, like other drugs with similar effects) [18].
Mechanism of action
Data from numerous experimental studies indicate a wide spectrum of action of nicergoline, which explains its effectiveness in diseases of various etiologies and pathogenesis. It improves cognitive functions regardless of the etiology of the disease [6].
When administered nicergoline, there is an increase in regional cerebral blood flow, improvement in glucose utilization processes, and activation of protein synthesis [1, 2, 4, 16, 18]. The nicotinic acid residue contained in the nicergoline molecule has a direct myotropic antispasmodic effect on the muscular lining of blood vessels, especially the vessels of the brain and limbs. The experiment showed that nicergoline reduces vascular resistance of the carotid and vertebrobasilar systems and improves cerebral blood flow and metabolism [18]. A positive effect of a course of nicergoline on lipid metabolism was noted [3].
The improvement in metabolic processes in the brain parenchyma resulting from the action of nicergoline was confirmed by spectroscopy data [18]. At the same time, the literature emphasizes that this drug has a positive effect on the basic, fundamental molecular processes underlying the onset and progression of dementia [16, 18].
One of the mechanisms of action of nicergoline is a disaggregating effect caused by a decrease in platelet aggregation and an increase in the plasticity of erythrocytes, which, in combination with the effect on cerebral vessels, leads to an improvement in regional cerebral blood flow in ischemic tissue [1, 18]. Taking into account the positive effect on platelet and erythrocyte aggregation, nicergoline is considered as a drug that reduces the risk of developing thromboembolic cerebral complications [18].
A study of the state of microcirculation of the bulbar conjunctiva showed that under the influence of a course of treatment with nicergoline, there was an acceleration of blood flow and a decrease in the severity of sludge syndrome [3]. This effect was more often recorded in arterioles and capillaries and less clearly in venules. In ⅓ of the examined patients there was an expansion of conjugate arterioles, reaching 10% of the initial diameter, and in 15-30% of patients (depending on age) there was an increase in the number of functioning capillaries per unit area of the bulbar conjunctiva [3]. In 1/3 of elderly patients in this study, disappearance or reduction of perivascular edema was observed.
Recently, its influence on the processes of neuroplasticity [8, 16, 18] and the mechanisms of neuroprotection [2, 7] has been shown. It is important to note that the neuroprotective properties of nicergoline are not associated with its direct effect on noradrenergic α1 receptors and serotonergic 5-HT1A receptors, but are global in nature. This is to a large extent due to the ability of nicergoline, acting through endogenous neurotrophic factors, to provide the trophic functions of cholinergic neurons [16], which leads to their survival under pathological conditions, including aging [10]. Experimental data indicate an increase in the concentration of nerve growth factor in the frontal regions of the brain in old animals (rats) that received nicergoline [18]. These mechanisms explain the ability of sermion (nicergoline) to slow down the progression of cognitive disorders in vascular pathology of the brain and Alzheimer's disease [6]. Current evidence suggests that nicergoline can “protect” neurons from the toxic effects of beta-amyloid, thereby slowing the progression of Alzheimer’s disease [7].
Experimental studies have shown the neuroprotective effect of nicergoline during hypoxia, even under conditions of hypercapnia, when cerebral vessels are in a state of dilation, indicating its direct effect on the brain parenchyma [8]. Intraventricular administration of nicergoline has been shown to affect both blood pressure and heart rate in anesthetized dogs and also inhibit T- and L-type neuronal calcium channels [8]. The neuroprotective properties of this drug are manifested in the protection of neurons from death under conditions of oxidative stress [16, 18]. When prescribing nicergoline, the processes of lipid peroxidation are reduced and the excessive formation of free radicals is reduced. There is evidence [16] that the antioxidant effect of nicergoline is comparable to the effect of the classical antioxidant tocopherol (vitamin E). Nicergoline also acts on the process of apoptosis [2, 16].
Nicergoline increases the synthesis of acetylcholine by activating choline acetyltransferase, increases the release of acetylcholine from presynaptic terminals, reduces the breakdown of acetylcholine by inhibiting acetylcholinesterase, and also acts on postsynaptic M-cholinergic receptors in the central nervous system [18]. It increases the level of acetylcholine in the cortex and striatum of old animals (rats), while no changes in the level are observed in young animals [15, 18]. In addition, nicergoline restores the age-related decrease in acetylcholine levels in the hippocampus [15, 16, 18]. Inhibition of acetylcholinesterase when using nicergoline is quite comparable to the similar effect of physostigmine, although inferior to the effect of tacrine [16]. A decrease in acetylcholinesterase activity in the brain after intravenous and intraperitoneal administration of nicergoline was confirmed experimentally [18]. The identified changes in the acetylcholinergic system in experimental animals were accompanied by better performance in tests for mnestic functions [18]. The additional positive effect of nicergoline is due to its influence on other neurotransmitter systems (adrenergic, serotonergic) [15, 16].
Animals treated with nicergoline showed an improvement in the performance of tasks associated with mnestic activity [15]. Moreover, the degree of improvement increases with increasing duration of therapy [15].
The nootropic and antiamnestic activity of nicergoline was confirmed in models of experimental cerebral ischemia and using toxic agents that selectively disrupt mnestic functions [18].
Clinical researches
Nicergoline has been successfully used to treat dementia of various origins [1, 9, 11, 16, 18]. The positive effect of the drug in the form of a decrease in the severity of cognitive and behavioral disorders is noted, according to some data, in almost 89% of patients (when a placebo is prescribed, an improvement, usually transient in nature, is observed in 26-50% of cases) [18].
The first studies examining the effectiveness of nicergoline in dementia used the Sandoz Clinical Geriatric Scale (SCAG) and the Clinical Global Impression (CGI) scale for assessment, followed by the Mini-Mental State Examination (MMSE) and the Alzheimer's Disease Assessment Scale (ADAS). ) [18].
The difference in clinical effect between the group of patients receiving nicergoline and those receiving placebo ranges from 5 to 30%, depending on the duration of the course of therapy and the characteristics of the patients included in the study [9].
Data from clinical studies [13, 14, 18] indicate that treatment with nicergoline improves the condition of patients with both Alzheimer's disease and vascular (multi-infarct) dementia during treatment with nicergoline. In addition, the drug is also effective for dementia of the mixed (Alzheimer’s and vascular) type [11, 18]. In addition to the immediate positive effect on cognitive functions, a fairly rapid decrease in the severity of apathy was noted [11].
Thus, significant improvement was observed in younger patients and in patients with less severe cognitive impairment [18]. In addition, nicergoline therapy is thought to result in marked improvement in vascular dementia than in Alzheimer's disease or other types of dementia [18]. However, this may be due to differences in the designs of the studies conducted to date. It is interesting to note that the effect of therapy on the latency dynamics of the P300 wave of the cognitive evoked potential in vascular (multi-infarct) dementia and Alzheimer's disease do not differ in nature from each other [18].
In patients with discirculatory encephalopathy, after a course of therapy with nicergoline, an improvement in the subjective state is observed in the form of a decrease or cessation of headaches, dizziness, noise in the head, and fatigue [3]. According to neuropsychological testing, a significant decrease in the time required to complete tasks according to Schulte tables was revealed [3]. It is important to note that the positive effect of the drug persisted for a long time after the end of the course of therapy.
The effect of nicergoline is dose-dependent, which is confirmed by the results of electrophysiological research methods [16]. During therapy with nicergoline in patients with dementia, α- and β-activity on the EEG increases, in combination with a decrease in θ- and Δ-waves, which, in turn, correlates with improved attention and memory [1, 13, 14].
Improvement in the cognitive sphere occurs in parallel with an increase in blood flow velocity in the middle and anterior cerebral arteries, as well as in the right parietal region [18].
It should be noted that nicergoline is considered an effective drug for the treatment of various types of vascular dementia, including multi-infarct dementia [5, 12]. As the duration of treatment increases from 6 months to 12 months, the effectiveness of therapy also increases [9]. In addition, during treatment with nicergoline, the progression of cognitive disorders slows down [16], and the differences between the group of patients receiving nicergoline and those receiving placebo increase with increasing study duration [11]. In this regard, the results of assessing the effectiveness of nicergoline during long-term (24 months) therapy in patients with leukoaraiosis against the background of arterial hypertension, but without dementia, are very indicative - in the group of patients receiving the drug, there was a slowdown in the progression of cognitive disorders, and in some neuropsychological parameters (memory , attention) - their improvement [6].
The effectiveness of the drug in moderate and severe Alzheimer's disease was confirmed in a multicenter, double-blind, placebo-controlled, randomized study conducted in 33 European centers (Italy, Sweden, Great Britain, Belgium and Germany) [17].
Another indication for prescribing this drug is post-stroke disorders [3, 18]. In addition to improvement in the cognitive sphere, which is confirmed by data from a study of the P300 wave of cognitive evoked potential, patients also noted a decrease in the severity of post-stroke motor defect [18]. The most significant result was observed in patients with a lower degree of hemiparesis. Thus, the use of nicergoline in patients who have suffered a stroke improves the course of the rehabilitation period, accelerates the recovery of both cognitive and motor functions, ultimately positively affecting the quality of life of patients.
Studies on the effectiveness of nicergoline in Parkinson's disease are few, however, even here a decrease in the severity of cognitive, emotional, personal and behavioral disorders was noted during therapy with this drug [18].
The positive effect of nicergoline was also noted for migraine. It consists in reducing the severity of headaches and stopping attacks [3].
Indications for the use of nicergoline are also imbalances caused by vestibular dysfunction. Data from experimental studies indicate the ability of this drug to improve compensation of vestibular disorders due to its dopaminergic effect [18]. In patients with balance disorders and dizziness as the leading symptom, positive dynamics in the condition, accompanied by an improvement in the quality of life, are noted in 44-78% of cases [18]. The results of the clinical assessment were confirmed by posturography data. In patients with discirculatory encephalopathy after a course of therapy with nicergoline, a decrease in dizziness, a decrease or disappearance of staggering when performing the Romberg test were noted [3].
Safety and Tolerability
The drug is well tolerated [6, 11, 16, 17]. In particular, the nature, frequency of occurrence and severity of adverse reactions in patients receiving nicergoline are quite comparable to the effect of placebo [6, 16, 18]. Moreover, even if side effects occur, they tend to decrease as therapy continues [1]. Among the adverse reactions that are quite typical for the entire class of ergot derivatives, complaints of dry mouth, constipation, and diarrhea should be noted. When taking the drug orally, systolic and diastolic blood pressure do not change significantly, and only sometimes decrease slightly (without a statistically significant difference with patients receiving placebo) [18]. With a single intravenous administration of nicergoline, a decrease in blood pressure was detected already at the 5th minute, which returned to the initial level by the end of the first hour [3]. In this regard, certain caution is emphasized when administering nicergoline intravenously to patients in older age groups [3]. Patients with initially high blood pressure may experience a bursting headache after administration of the drug [3].
As found by B. Winblad et al. [17], in the group of patients receiving nicergoline, side effects requiring discontinuation of treatment were observed in 8.5% of cases, in the group receiving placebo - in 8.3% of cases. During therapy with nicergoline, there are no statistically significant changes in vital functions and laboratory parameters, with the exception of a slight increase in the level of uric acid in the blood serum in some cases, which is not accompanied by any clinical symptoms [16, 17]. However, this must be taken into account in patients with a history of gout.
Thus, nicergoline has been used in clinical practice for almost 40 years. During this time, considerable experience has been accumulated in the use of this drug in conditions of various pathogenesis. And if initially nicergoline was considered as an exclusively “vascular” drug, leading to an improvement in cerebral blood flow due to an antagonistic effect on α1-adrenergic receptors, then a significantly wider spectrum of its action was later demonstrated. Nicergoline has a positive effect on the cholinergic and catecholaminergic neurotransmitter systems, inhibits platelet aggregation, improves cerebral metabolism, increasing the utilization of oxygen and glucose, and has anti-apoptotic, antioxidant and neurotrophic activity. All this allows us to consider nicergoline not only as a symptomatic agent, but also as a drug with a neuroprotective effect. The combination of effectiveness with good tolerability makes the drug Sermion (nicergoline) very popular, especially in neurogeriatric practice.
Interaction
Taking Sermion together with anticholinergic and antihypertensive drugs, the effect of the latter can be enhanced.
If you take the drug simultaneously with cholestyramine or non-absorbable antacids, the absorption of Sermion occurs more slowly.
The drug is metabolized with the direct participation of the CYP 2D6 enzyme, so it may interact with other drugs that are also biotransformed with the help of this enzyme ( Risperidone , Rinidine , and other antipsychotics).
special instructions
Typically, Sermion, used in therapeutic doses, has no effect on blood pressure. However, those patients who have arterial hypertension may experience a gradual decrease in blood pressure caused by the action of the drug.
If the drug is administered parenterally, patients are advised to lie down for a few minutes immediately after the injection, because arterial hypotension . This is especially true for those patients who have just started treatment with the drug.
The effect of the drug manifests itself gradually, so Sermion must be taken for a long time. Throughout the course of treatment, the doctor must periodically assess the effect of treatment, as well as the advisability of continuing treatment in the future.
The effect on the ability to operate machinery and drive vehicles has not been studied. Therefore, despite the ability of the drug to improve concentration, patients are advised to exercise extreme caution when driving or operating machinery, especially given the nature of the underlying disease.
Reviews about Sermione
You can find a lot of reviews about the drug Sermion on the Internet, and almost all of them are positive. Patients taking the drug report its high effectiveness. Their blood pressure was normalized, the number of migraine attacks gradually decreased, and their headaches stopped hurting. Many reviews about Sermion contain patient reports of increased concentration and improved cognitive functions of the body.
The forum also contains warnings to patients who have taken the pills that this medicine should be taken for a long time, since it only begins to work as it accumulates in the body. In this regard, there were a few patient reviews about Sermion in a negative context - those who took the drug, without seeing the effect, quit the course of treatment.
There are also warnings that this drug is not suitable for children. It should not be taken by children and adolescents under 18 years of age.
Note!
The description of the drug Sermion on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
Sermion price, where to buy
Depending on the markup of pharmacies and the form of release of the drug, the price of Sermion tablets can vary greatly:
- 5 mg tablets cost about 550 rubles for 30 pieces. packaged;
- 10 mg tablets can be found at a price of about 700 rubles per package containing 50 tablets;
- the cost of 30 mg tablets is about 1200 rubles per pack of 30 pcs.;
- the price of Sermion in ampoules is about 2100 rubles per package.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
- Online pharmacies in KazakhstanKazakhstan
ZdravCity
- Sermion tablets p.p.o.
30 mg 30 pcs. Pfizer Italy S.r.L. RUB 1,341 order
Pharmacy Dialogue
- Sermion (amp. 4 mg No. 4 + solution) Actavis
RUB 2,240 order
- Sermion (tab. 10 mg No. 50) Pfizer
RUR 712 order
- Sermion (5 mg tablet No. 30)Pfizer Italia SrL
RUR 559 order
- Sermion (tab. 30 mg No. 30) Pfizer
1190 rub. order
- Sermion (tab. 10 mg No. 50) Pfizer Italia SrL
RUR 664 order
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Pharmacy24
- Sermion 30 mg N30 tablets Pfizer Italy S.r.l., Italy
391 UAH.order - Sermion 10 mg N50 tablets Pfizer Italy S.r.l., Italy
310 UAH. order
- Sermion 4 mg 4 ml N4 powder Actavis Italy S.p.A., Italy
1101 UAH. order
- Sermion 5 mg No. 30 tablets Pfizer Italy S.r.l., Italy
203 UAH order
PaniPharmacy
- Sermion tablets Sermion tablets. 10 mg No. 50 Italy, Pfizer Italia
302 UAH. order
- Sermion tablets Sermion tablets. 5mg No. 30 Italy, Pfizer Italia
207 UAH. order
- Sermion ampoule Sermion lyophilized powder for injection 4 mg No. 4 Italy, Actavis Italia
1164 UAH. order
- Sermion tablets Sermion tablets. 30 mg No. 30 Italy, Pfizer Italia
392 UAH. order
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Sermion: instructions for use
Sermion is used orally in tablets as follows: the recommended dose according to the instructions is 5–10 mg 3 times a day with equal time intervals between meals.
The course and duration of therapy is prescribed strictly by the doctor and depends on many factors.
Sermion solution for injection: the drug is intended for intravenous and intramuscular use.
For intramuscular injection, 2–4 ml should be administered 2 times a day.
When used intravenously, 4–8 mg of Sermion should be dissolved in 100 ml of 0.9% sodium chloride solution or 5% glucose solution and administered very slowly.
Caution: for people with diabetes, Sermion for IV use should be dissolved only in 100 ml of 0.9% sodium chloride solution.
The duration of therapy, as well as the dose and route of administration, are prescribed by the doctor.