Sermion 10mg 50 tablets — Made in Italy — Free Delivery

Pharmacological properties

Pharmacodynamics. When administered parenterally, nicergoline is a derivative of ergoline with alpha-1-adrenergic blocking properties. when taken orally, nicergoline undergoes a rapid and significant metabolism with the formation of a number of metabolites, due to which the activity at different levels of the central nervous system is also noted.

When administered orally, Sermion exhibits numerous neuropharmacological effects: it increases the intake and consumption of glucose in the brain, enhances the biosynthesis of protein and nucleic acids, but also affects various neurotransmitter systems.

Sermion improves cerebral cholinergic functions in older animals. Prolonged use of nicergoline in old rats prevented age-related decreases in acetylcholine levels (in the cortex and in the striatum) and reduced acetylcholine release (in the hippocampus) in vivo. After long-term oral administration, an increase in choline acetyltransferase activity and muscarinic receptor density is also observed. Moreover, in in vitro and in vivo studies, nicergoline significantly increased acetylcholinesterase activity. In these experimental studies, neurochemical effects were detected simultaneously with a sustained improvement in behavioral responses, for example, in a maze test in mature animals used Sermion for a long period, the development of reactions similar to reactions in young animals was noted.

Sermion in animals was also able to reduce the severity of cognitive impairment, which was induced by several agents (hypoxia, electroconvulsive therapy, scopolamine). Oral administration of Sermion in low doses increases dopamine metabolism in mature animals, including in the mesolimbic area, probably by modulating dopaminergic receptors. Sermion improves the mechanisms of signal transduction in cells in mature animals. Both after a single and long-term use of the preparation there was an increase in the metabolism of basal and agonist-sensitive phosphoinositide. Sermion also increases the activity of transfer to the membrane of calcium-dependent isoforms of protein kinase C. Due to the antioxidant effect and ability to activate detoxification enzymes, Sermion prevents the death of nerve cells caused by oxidative stress and apoptosis. Sermion attenuates the age-related decrease in nitric oxide synthase mRNA expression and may also improve cognitive function.

Studies of pharmacodynamics in humans were performed using computerized ECG techniques with the participation of young and elderly volunteers, as well as in elderly patients with cognitive disorders. Sermion normalized EEG results in elderly and adult patients in hypoxia, increasing α- and β-activity and decreasing δ- and θ-activity. During long-term use of Sermion (within 2-6 months) positive changes were observed in cases of additional potentials and induced reactions in patients with mild or moderate dementia and of different origin (senile dementia such as Alzheimer's and multiinfarct dementia), these changes correlate with a decrease in clinical symptoms. In view of the above, it is obvious that nicergoline acts by modulation with a wide range of cellular and molecular mechanisms involved in the pathogenesis of dementia.

More than 1,500 patients with dementia (Alzheimer's, vascular and mixed) who received nicergoline at 60 mg / day or placebo were included in double-blind placebo-controlled clinical trials. After long-term treatment with NICERGOLIN, a long-term decrease in the severity of cognitive and behavioral disorders associated with dementia was recorded. Patients improved after 2 months of treatment and persisted for 1 year of treatment.

Pharmacokinetics. After ingestion, nicergoline is rapidly and almost completely absorbed. The maximum rate of radioactivity after administration of low doses (4-5 mg) of healthy H-labeled nicergoline by healthy volunteers was determined after 1.5 hours. However, after oral administration in therapeutic doses (30 mg) of C-labeled nicergoline in healthy volunteers, it was observed 3 hours after dosing. After oral administration of nicergoline (15 mg) to healthy volunteers, the AUC of plasma radioactivity was 81 and 6% of the value calculated for the two major metabolites of nicergoline - MDL and MMDL, respectively. With max MDL in blood plasma reached approximately 3-5 hours after a single or multiple tablets of 30 mg. With max MMDL in blood plasma was reached approximately 0.5-1 hours after a single tablet of 30 mg.

The absolute bioavailability of nicergoline after oral administration is about 5% as a result of the first-pass effect. Based on the results of determining the levels of the main metabolite MDL, it was found that in healthy volunteers after oral administration of the preparation at a dose of 30-60 mg pharmacokinetics of nicergoline is linear. After a single dose of nicergoline at a dose of 30 mg, a significant effect of food on the pharmacokinetics of MDL and MMDL is not detected.

The preparation is distributed in tissues rapidly and has a wide target spectrum, which demonstrates the short phase of distribution of radioactivity in blood plasma. The volume of distribution of nicergoline in the Central compartment (approximately calculated by dividing the dose by the concentration of nicergoline in blood plasma in the first period for sampling after administration of a nominal dose of 2 mg) is relatively high (224 l), potentially reflecting the distribution of nicergoline in blood cells and / or tissues. Nicergoline binds significantly to human plasma proteins, and the affinity for α-acid glycoprotein is 4 times higher than for plasma albumin. The percentage of binding is relatively constant when the concentration of nicergoline increases from 1 μg / ml to 500 μg / ml. Both metabolites of nicergoline, MDL and MMDL, are characterized by low levels of binding, about 14.7 and 34.7%, respectively, in the concentration range of 50-200 ng / ml. Most of the preparation is excreted in the urine. Within 120 hours after administration, about 82% of the total amount of radiolabeled nicergoline is excreted by the kidneys, and 10% is excreted in the feces. Nicergoline undergoes significant metabolism mainly by hydrolysis of ether bonds to form MMDL, and then - MDL by demethylation (by catalytic action of the enzyme CYP 2D6). Therefore, the pharmacokinetics of nicergoline and its metabolites differ in patients with genetic deficiency of CYP 2D6. MMDL and MDL are conjugated to glucuronic acid. The major metabolite of MDL accounts for 51% of the total dose and 76% of the radioactivity detected in the urine after an oral dose of 15 mg. The average value of the final T ½ MDL is in the range of about 11-20 hours.

The effect of renal impairment on the pharmacokinetics of nicergoline was evaluated in patients with renal impairment (creatinine clearance (Clcr) 60-80 ml / min), moderate (Clcr 30-50 ml / min) and severe (Clcr 10-25 ml / min) degree. Significant differences in the amount of MDL excreted in the urine within 120 hours after oral administration of nicergoline 30 mg (38.1; 42.6 and 25.7% of the administered dose, respectively) for MMDL, the corresponding values ​​were 1.7; 0.6 and 0.2%. In patients with severe renal impairment, a significant decrease in urinary MDL excretion was observed compared with the other two groups. Patients with mild, moderate or severe renal impairment had a mean decrease in urinary MDL excretion (0-72 h) of 32; 32 and 59%, respectively, compared with patients with normal renal function who participated in another study using tablet forms at a dose of 30 mg.

The pharmacokinetics of nicergoline in patients with hepatic impairment and in children have not been studied.

The effect of age (in elderly patients) on the pharmacokinetics of nicergoline has not been fully studied.

Indication

Sermion tablets 5 mg, 10 mg

Acute and chronic disorders of cerebrovascular metabolism due to atherosclerosis, thrombosis and embolism of cerebral vessels, transient cerebrovascular disorders (transient ischemic attacks).

Headache.

As an adjunct therapy for hypertension.

Sermion solution for injection (1 vial - 4 mg)

Acute and chronic disorders of cerebrovascular metabolism due to atherosclerosis, thrombosis and embolism of cerebral vessels, transient disorders of cerebral circulation (transient ischemic attacks).

Headache.

Additional therapy for the treatment of hypertension.

Additional therapy for hypertensive crisis.

Sermion tablets 30 mg

Post-stroke conditions, vascular dementia (multiinfarct dementia), degenerative conditions associated with dementia (senile and presenile dementia such as Alzheimer's, dementia in Parkinson's disease).

Application

Tablets 5 mg, 10 mg: the recommended dose is 5-10 mg 3 times a day with equal intervals between doses for a long period.

Dosage, duration and route of administration depend on the specific clinical situation. In some cases, it is advisable to start treatment with parenteral administration of the preparation, followed by continuation in the form of maintenance oral therapy.

According to the results of the study of pharmacokinetics and tolerability of the preparation in elderly patients, no dose adjustment is required.

30 mg tablets: the recommended dose 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 the case of vascular disorders of the visual organ or inner ear, the recommended dose is 30 mg / day.

The preparation should be taken before meals, drinking a small amount of water without chewing. If the appointment is 1 time per day, it is desirable to take the preparation in the morning.

Because renal excretion is the major route of elimination (80%) of nicergoline and its metabolites, it is recommended that the dose be reduced in patients with renal impairment (plasma creatinine ≥2 mg / dL or 175 mmol / L).

Sermion solution for injection: the preparation is intended for parenteral use.

For intravenous administration, the recommended dose is 2-4 mg (2-4 ml) 2 times a day (you must use the supplied solvent).

For intravenous administration, the recommended dose of Sermion is 4-8 mg. It should be pre-dissolved in 100 ml of 0.9% sodium chloride solution or 5% glucose solution (glucose). In / in the preparation should be administered slowly. At the doctor's discretion, this dose can be re-administered during the day.

If necessary, Sermion can be administered intravenously at a dose of 4 mg in 10 ml of 0.9% sodium chloride solution, slowly, for at least 2 minutes

The dose, duration of treatment and route of administration are determined by the physician individually.

Contraindication

Hypersensitivity to the active substance, ergot alkaloids or any component of the preparation. recently suffered a myocardial infarction, acute bleeding, orthostatic hypotension, severe bradycardia. simultaneous use of sympathomimetics.

Side effects

Such mild side effects have rarely been reported.

From the gastrointestinal tract: constipation, nausea, vomiting, increased acidity of gastric juice, diarrhea, abdominal pain.

From the cardiovascular system: hypotension, dizziness, angina, cold extremities, tachycardia.

From the central nervous system: dizziness, headache, confusion, drowsiness, insomnia, agitation.

Allergic reactions: angioneurotic edema, itching, skin rash.

Reproductive disorders in men: ejaculation disorders.

General disorders: fever, hot flashes, sweating, pain in the extremities, fever.

In clinical trials, there was an increase in the level of uric acid in the blood, which did not depend on both the prescribed dose and the duration of treatment.

Special instructions

As a rule, sermion in the recommended therapeutic doses does not cause changes in the level of hell, but in patients prone to ag, the preparation can gradually reduce the level of hell. The preparation should be used with caution in patients with angina pectoris and severe atherosclerosis. at the beginning of treatment the development of orthostatic hypotension is possible.

Sermion should be used with caution in patients with a history of hyperuricaemia or gout and / or concomitant therapy with preparations that affect uric acid metabolism and excretion, as well as with angina pectoris and severe atherosclerosis.

Because approximately 80% of nicergoline metabolites are excreted in the urine, it is recommended that the dose be reduced in patients with renal impairment (plasma creatinine ≥2 mg / dL or 175 mmol / l).

The preparation 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 the preparation develops gradually, so Sermion should be taken for a long time. It is desirable to evaluate the effect of therapy every 6 months to decide on the feasibility of further use of the preparation.

Alcohol should be avoided during the use of the preparation.

The development of fibrosis (eg, pulmonary, cardiac, heart valve, and retroperitoneal fibrosis) has been associated with the use of some ergot alkaloids with agonistic activity at 5-HT 2β serotonin receptors.

Symptoms of ergotism (including nausea, vomiting, diarrhea, abdominal pain, and peripheral vasoconstriction) have been reported with some ergot alkaloids and their derivatives.

Before prescribing this class of preparations, doctors need to familiarize themselves with the signs and symptoms of overdose of ergot.

Children. The preparation is not used in children.

Use during pregnancy and breastfeeding. Toxicological studies have not shown teratogenic effects of nicergoline. Based on the evidence, the use of the preparation during pregnancy and breastfeeding is unlikely. In the presence of sound evidence, the preparation should be prescribed only after assessing the benefit to the mother / risk to the fetus (child).

Ability to influence the speed of reaction when driving a car or working with other mechanisms. Although Sermion is used to improve concentration, its effect on the ability to drive and use machines has not been studied. During treatment with the preparation, as well as taking into account the underlying disease, patients should be careful when driving and operating other machinery.

Interactions

With caution, the preparation is used in combination with:

antihypertensive preparations (Sermion may potentiate their effects);

preparations that are also metabolized by the cytochrome CYP 2D6 system, as interactions with these preparations cannot be ruled out (such as quinidine, most antipsychotics, including clozapine, risperidone, haloperidol, thioridazine);

acetylsalicylic acid (may prolong bleeding time);

preparations that affect the metabolism of uric acid (may change the metabolism and excretion of uric acid).

Sermion should not be used concomitantly with CNS stimulants, α- and β-adrenomimetics. Coagulation should be monitored when co-administered with anticoagulants and antiplatelets. The preparation may enhance the effects of cholinomimetics.

Nicergoline may increase the effect of β-adrenoceptor blockers on the heart.

Overdose

When using nicergoline in high doses, there may be a temporary decrease in hell. special treatment is usually not required, it is enough to give the patient a horizontal position. in isolated cases at insufficiency of blood supply of a brain and heart use of sympathomimetics and carrying out constant monitoring of indicators of hell is recommended.

Storage conditions

The lyophilized powder for solution for injection is stored in a dry, protected from light and out of reach of children at a temperature not exceeding 25 ° C; tablets - in a dry, protected from light and out of reach of children at a temperature not exceeding 25 ° C.