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).
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
Pharmacological properties of the drug Sermion
Pharmacodynamics. After oral administration, it is quickly and extensively metabolized to form a number of metabolites, which also have an effect at various levels of the central nervous system. Sermion has a positive effect on the emotional state, ability to concentrate and level of vigor. After oral administration, Sermion causes various neuropharmacological effects: it not only increases glucose consumption by brain tissue, enhances the biosynthesis of proteins and nucleic acids, but also affects various neurotransmitter systems. Increased choline acetyltransferase activity and muscarinic receptor density were also observed after prolonged oral administration of Sermion. In addition, in both in vitro and in vivo , nicergoline significantly increased acetylcholinesterase activity. Both after single and long-term oral administration of the drug, the exchange of basal and agonist-sensitive phosphoinositide increases. Sermion also enhances the activity and translocation of Ca-dependent PKC isoforms across the membrane. These enzymes are involved in the mechanism of secretion of soluble amyloid precursor protein, which leads to increased release and decreased production of pathological beta-amyloid, as demonstrated in cultured human neuroblastoma. The antioxidant effect and activation of detoxification enzymes by Sermion protects nerve cells from death due to oxidative stress and apoptosis in experimental models in vivo and in vitro . Sermion attenuates the age-dependent decline in nitric oxide synthetase mRNA in neurons, which improves cognitive function. Pharmacokinetics. Nicergoline is rapidly and almost completely absorbed after oral administration. The peak of serum radioactivity after administration of low doses (4–5 mg) of radiolabeled nicergoline was observed after 1.5 hours. However, with oral administration of therapeutic x doses (30 mg) of 3H-labeled nicergoline, the peak of serum radioactivity in the blood serum was observed after 3 hours. The half-life of the drug is approximately 15 hours (healthy volunteers). The absolute bioavailability of nicergoline after oral administration is approximately 5%, due to high hepatic clearance and first-pass metabolism. After oral administration of nicergoline at therapeutic doses, the AUC values in radioactive serum were 81 and 6%, respectively, for the main metabolites MDL and MMDL (healthy volunteers). Peak plasma concentrations of MDL and MMDL were achieved approximately 1 and 4 hours after dosing with a half-life of 13 and 14 hours. Nicergoline is rapidly hydrolyzed due to binding with esters after intravenous administration. The drug is quickly and extensively distributed in tissues. The volume of distribution of nicergoline was 105 L, which likely reflects the metabolism of the drug in the blood and its penetration into blood cells and/or tissues. Nicergoline binds extensively to plasma proteins (90%), with greater affinity for α-acid glycoprotein than for serum albumin. Urinary excretion is the main route of excretion, since 80% of the total dose of radiolabeled nicergoline is determined in urine and only 10–20% in feces. When administered orally in doses of 30–60 mg, it has been established that the pharmacokinetics of nicergoline is linear. Nicergoline is extensively metabolized before elimination. The main route of metabolism is hydrolysis of ester bonds to form the metabolite MMDL. The following biotransformation leads to the formation of the metabolite MDL by demethylation. The demethylation process occurs with the participation of the catalytic action of the CYP 2D6 isoenzyme. The metabolite MDL is mainly formed, accounting for 50% of the total dose and 74% of the radioactivity detected in urine. As a secondary metabolic pathway, 1-dimethylnicergoline is formed by demethylation (1-DN) and then metabolized by hydrolysis of ester bonds into MDL. In patients with severe renal impairment, there is a significant reduction in urinary MDL secretion.
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 .
Termicon®
Thermikon® was generally well tolerated. Side effects are usually mild or moderate and transient.
When assessing the frequency of occurrence of side effects of a drug, the following gradations were used: “very often” (≥1/10), “often” (from ≥1/100 <1/10), “infrequently” (≥1/1000 <1/100 ), “rare” (≥1/10000 <1/1000), “very rare” (<1/10000), including isolated reports.
Blood and lymphatic system disorders:
infrequently - anemia; very rarely - neutropenia, agranulocytosis, pancytopenia, thrombocytopenia.
Immune system disorders:
very rarely - anaphylactoid reactions (including angioedema), cutaneous and systemic lupus erythematosus (or their exacerbation).
Mental disorders:
often - depression; infrequently - anxiety.
Nervous system disorders:
very often - headache; often dizziness, disturbance of taste, up to their loss (usually recovery occurs within a few weeks after stopping treatment). In some cases, exhaustion was observed while taking terbinafine. There are isolated reports of cases of long-term disturbances of taste; infrequently - paresthesia, hypoesthesia.
Visual disorders:
infrequently - visual impairment.
Hearing and labyrinth disorders:
infrequently - tinnitus.
Disorders of the liver and biliary tract:
rarely - hepatobiliary dysfunction (mainly of cholestatic nature), incl. liver failure, including very rare cases of severe liver failure (some fatal or requiring liver transplantation; in most cases where liver failure developed, the patients had serious underlying systemic diseases and the causal relationship of liver failure to terbinafine was questionable), hepatitis, jaundice, cholestasis, increased activity of liver enzymes.
Digestive system disorders:
very often - bloating, loss of appetite, dyspepsia, nausea, mild abdominal pain, diarrhea.
Disorders of the skin and subcutaneous tissues:
very often - rash, urticaria; uncommon - photosensitivity reactions; very rarely - Stevens-Johnson syndrome, toxic epidermal necrolysis, acute generalized exanthematous pustulosis, erythema multiforme, toxic skin rash, exfoliative dermatitis, bullous dermatitis, psoriasis-like skin rashes or exacerbations of psoriasis, alopecia.
Musculoskeletal and connective tissue disorders:
very often arthralgia, myalgia.
Common disorders:
often - feeling tired; infrequently - increased body temperature.
Laboratory and instrumental data:
infrequently - weight loss (secondary to a violation of the sense of taste).
Based on spontaneous reports received during the post-registration period and literature data, the following adverse events were identified, the frequency of which, due to the inaccurate number of patients, cannot be established.
Immune system disorders:
anaphylactic reactions, serum sickness-like syndrome.
Visual disorders:
blurred vision, decreased visual acuity.
Disorders of the skin and subcutaneous tissues:
drug rash with eosinophilia and systemic symptoms (rash, swelling, fever and swollen lymph nodes).
Hearing and labyrinth disorders:
hearing loss, hearing impairment.
Vascular disorders:
vasculitis
Nervous system disorders:
loss of smell, including for a long period of time, decreased sense of smell.
Digestive system disorders:
pancreatitis.
Musculoskeletal and connective tissue disorders:
Rhabdomyolysis
Common disorders:
flu-like syndrome.
Laboratory and instrumental data:
increased activity of creatine phosphokinase in blood serum.
If you notice any side effects of the drug, tell your doctor.
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.
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.
Side effects of the drug Sermion
The following non-severe side effects have been reported rarely. From the gastrointestinal tract: constipation, nausea, vomiting, increased acidity of gastric juice, diarrhea, abdominal pain. From the cardiovascular system: arterial hypotension, dizziness, angina attacks, cold extremities, tachycardia. From the side of the central nervous system: dizziness, headache, confusion, drowsiness, insomnia. Allergic reactions: angioedema, itching, skin rash. Reproductive disorders in men: ejaculation disorders. General disorders: feeling of heat, hot flashes, sweating, pain in the limbs, increased body temperature. During clinical studies, an increase in uric acid levels in the blood was observed, which was independent of both the dose used and the duration of treatment.
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.
Use of the drug Sermion
5 mg tablets: the recommended dose of the drug is 5–10 mg 3 times a day with equal intervals between doses for a long period of time. Dosage, duration and route of administration of the drug depend on the specific clinical situation. In some cases, it is advisable to begin treatment with parenteral administration of the drug with further continuation of treatment in the form of maintenance oral therapy. 30 mg tablets: the recommended dose of the drug is 1 tablet 1-2 times a day (30-60 mg). The usual daily dose for adults is 30 mg. Temporarily the daily dose can be increased to 60 mg. In case of vascular disorders of the eye or inner ear, the recommended dose is 30 mg per day. The drug should be taken before meals with a small amount of water, without chewing. If the dose is prescribed once a day, it is advisable to take the drug in the morning. Since renal excretion is the main route of elimination (80%) of nicergoline and its metabolites, it is recommended to reduce the dose in patients with impaired renal function (serum creatinine ≤20%). solution for injection : the drug is intended for parenteral use. For intramuscular administration, the recommended dose is 2–4 mg (2–4 ml) 2 times a day (using the supplied solvent). For intravenous administration, the recommended dose of Sermion is 4–8 mg, having previously dissolved it in 100 ml of 0.9% sodium chloride solution or 5% dextrose (glucose) solution. The drug should be administered intravenously slowly. At the doctor's discretion, this dose may be repeated throughout the day. If necessary, Sermion can be administered intra-arterially at a dose of 4 mg in 10 ml of 0.9% sodium chloride solution, slowly, over at least 2 minutes. The dose, duration of treatment and route of administration are determined by the doctor individually.
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).
Interactions of the drug Sermion drug Sermion
The drug should be used with caution in combination with:
- antihypertensive drugs (nicergoline may potentiate their effects);
- drugs that are also metabolized by the cytochrome CYP 2D6 system, since it is impossible to exclude interaction with these drugs (such as quinidine, most antipsychotics, including clozapine, risperidone, haloperidol, thioridazine);
- acetylsalicylic acid (bleeding time may prolong);
- drugs that affect the metabolism of uric acid (metabolism and excretion of uric acid may change).
Sermion should not be used simultaneously with drugs that excite the central nervous system, α- and β-adrenergic agonists. When used simultaneously with anticoagulant and antiplatelet agents, it is necessary to monitor the indicators of the lightening blood system. The drug may enhance the effects of cholinomimetic drugs.
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.
Special instructions for the use of the drug Sermion
As a rule, Sermion in recommended therapeutic doses does not cause changes in blood pressure levels, however, in patients prone to hypertension (arterial hypertension), the drug can gradually reduce blood pressure levels. At the beginning of treatment, orthostatic hypotension may develop. For the treatment of patients with a history of hyperuricemia or gout and/or during concomitant treatment with drugs that affect the metabolism and excretion of uric acid, Sermion is prescribed with caution. Since approximately 80% of nicergoline metabolites are excreted in the urine, it is recommended to reduce the dose of the drug in patients with impaired renal function (serum creatinine 2 mg/dL or 175 mmol/L). The drug contains lactose, which must be taken into account when prescribing it to patients with congenital lactase deficiency, hereditary galactosemia and impaired absorption of glucose and galactose. The effect of using the drug develops gradually, so Sermion should be taken for a long time. It is advisable to evaluate the effect of therapy every 6 months to decide on the advisability of further use of the drug. While using the drug, you should refrain from drinking alcohol. Children. The drug is not used in children. Use during pregnancy and lactation. Toxicological studies have not demonstrated the teratogenic effect of nicergoline. Based on the indications, the use of the drug during pregnancy and breastfeeding is unlikely. If there are solid indications, the drug should be prescribed after considering the ratio of benefit to the mother/risk to the fetus (child). The ability to influence the reaction rate when driving a vehicle or while working with other mechanisms. Although the clinical effects of Sermion are used to improve concentration, its effect on the ability to drive vehicles and operate potentially dangerous machinery has not been studied. During treatment with the drug, and also taking into account the underlying disease, patients should be careful when driving vehicles or operating other mechanisms.
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.
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.
5mg 30 pcs Phizer Italia Srl RUR 548 order - Sermion tablets p.p.o. 10 mg 50 pcs. Pfizer Italy S.r.L.
RUR 627 order
- Sermion tablets p.p.o. 30 mg 30 pcs. Pfizer Italy S.r.L.
RUB 1,223 order
Pharmacy Dialogue
- Sermion (5 mg tablet No. 30)Pfizer Italia SrL
550 rub. order
- Sermion (tab. 10 mg No. 50) Pfizer Italia SrL
RUB 671 order
- Sermion (amp. 4 mg No. 4 + solution) Actavis
RUB 2,311 order
- Sermion (tab. 10 mg No. 50) Pfizer
RUR 714 order
- Sermion (tab. 30 mg No. 30) Pfizer
RUB 1,174 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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