Sermion

Sermion is α-blocker. Promotes improvement of intracerebral and peripheral circulation.

[1], [2], [3]

Indications Sermiona

It is used in the following conditions:

• acute or chronic vascular cerebral and metabolic disorders (developing due to atherosclerosis, increased blood pressure, embolism, or thrombosis in the region of the cerebral vessels), including vascular dementia, acute transient cerebral blood flow disorder, and also headache provoked vasospasm;
• metabolic and vascular disorders of a chronic or acute nature (organic or functional arteriopathies affecting the extremities, and in addition, syndromes that develop due to disorders of the peripheral circulation, and Raynaud's syndrome);
• in the form of additional drugs for therapy in patients with hypertensive crisis.

[4], [5]

Release form

The substance is released in tablets with a volume of 5 mg (15 blister packs inside; 2 packs in a box), 10 mg (25 tablets inside blisters; 2 packs in a pack) and 30 mg (15 blister cells; a pack - 2 packs).

It is also sold in the form of a powder for injectable liquids - inside the flasks of glass. Complete with them are available and ampoules containing solvent. Inside the box - 4 bottles of powder and 4 ampoules of solvent.

Pharmacodynamics

The main active element of the drug is nicergoline (ergoline derivative), which helps to improve the metabolic and hemodynamic processes occurring inside the brain.

The drug reduces platelet aggregation, and at the same time improves blood rheology and increases blood circulation in the arms and legs. Improvement of blood circulation processes is associated with the development of α1-adreno-blocking effect.

Sermion has a direct effect on the cerebral mediator system - noradrenergic, dopaminergic, and acetylcholinergic. This has a positive effect on the development of cognitive processes. After prolonged use of drugs, the patients showed a weakening of the severity of behavioral disorders associated with dementia, and in addition, the cognitive activity of the organism improved.

[6], [7]

Pharmacokinetics

Absorption (tablets).

After penetration into the body, nicergoline is absorbed almost completely and at high speed. The degree and speed of absorption of drugs almost does not depend on the form of its release, nor on the use of food. When taking a serving of up to 60 mg, the pharmacokinetic properties of nicergoline are linear, not changing with the age of the patient.

Exchange and distribution processes.

The component nicergoline is synthesized with a plasma protein of at least 90%, and the degree of affinity of this element with respect to serum albumin is lower than with respect to the glycoprotein α-acid. Nicergoline, along with its metabolic products, can invade blood cells.

The main metabolic products of nicergoline are MDL (formed as a result of the demethylation process developing under the influence of CYP2D6 isoenzyme), and also MDTL (formed during hydrolysis).

The ratio of AUC values for MDL and MDL after intravenous injection of a drug or oral administration suggests that the drug is undergoing 1st hepatic passage. With the introduction of 30 mg of the substance, the Cmax values for MMDL (21 ± 14 ng / ml) and MDL (41 ± 14 ng / ml) were noted after 1 and 4 hours, respectively, and then MDL level decreased with a half-life of 13-20 hours. In addition, during the tests, the absence of cumulation of other metabolic products within the blood (also MMDL) was recorded.

Excretion.

The element nicergoline is excreted in the form of metabolic products, mainly with urine (approximately 80%), and besides with feces (about 10-20%).

Pharmacokinetic characteristics developing in individuals with special clinical situations.

In people with renal failure in severe form, significantly less metabolic products are excreted in the urine than in individuals with healthy kidney function.

[8], [9], [10], [11]

Dosing and administration

The use of pills.

Apply the drug should be orally.

During cognitive impairment affecting blood vessels, and in addition, in the case of post-stroke conditions and chronic cerebral circulatory disorders, it is necessary to use the medication in a dose of 10 mg, 3 times a day. The therapeutic cycle should last at least 3 months, because the drug effect of the drug develops gradually.

In the case of vascular dementia, the medication is taken in a dosage of 30 mg, 2 times a day. It is required to consult with the doctor every six months to determine the feasibility of continuing the therapeutic cycle.

In the case of ischemic stroke, triggered by atherosclerosis, thrombosis or embolism in the area of cerebral vessels, and in addition, in acute or transient disorders of the cerebral blood flow (TIA or cerebral hypertensive crisis), it is recommended to start the treatment cycle by administering nicergoline to a parentterer as a source.

For disorders affecting the peripheral bloodstream, the drug is used 3 times a day (10 mg portion). The course should be long - lasting for several months.

People with impaired renal activity (serum creatinine levels — more than 2 mg / dL) should use the drug at a lower dosage.

The scheme of use of medicinal powder.

With the introduction of the drug in the / m way: in the amount of 2-4 ml, 2 times a day.

When i / v use of the drug: enter at low speed in portions of 4-8 mg (the powder is diluted in 0.1 l of solvent - 5-10% dextrose solution or 0.9% NaCl solution is used). With this dosage, injections of medication can be performed up to several times per day.

With the introduction of the inside of the artery: for 2 minutes you need to enter 4 mg of lyophilisate, previously dissolved in 10 ml of 0.9% NaCl solution.

The recovered liquid should be used immediately after preparation.

The duration of treatment, the size of the portion and the method of use of the drug substance depend on the pathology observed in the patient. At times, it is recommended to start therapy with drug administration by parenteral method, and then go on oral administration (supportive therapy).

People with kidney problems (serum creatinine values - above 2 mg / dL) are required to use lower dosages of the medication.

[18]

Use Sermiona during pregnancy

Tests with the use of drugs during pregnancy were not performed, which is why Sermion is allowed to be used only with vital indications and under the supervision of a specialist.

Breastfeeding is required for the period of therapy, because nicergoline and its metabolic products are excreted with breast milk.

Contraindications

Main contraindications:

• disorders of orthostatic regulation processes;
• recent myocardial infarction;
• bradycardia, which is pronounced;
• acute bleeding;
• enhanced sensitivity to the constituent components of a drug.

The drug should be prescribed carefully for people with a history of hyperuricemia or gout, and if necessary, combine it with drugs that violate the processes of metabolism or the excretion of uric acid.

In addition, tablets can not be used with a shortage of sucrase or isomaltase, as well as with fructosemia or glucose-galactose malabsorption.

[12], [13], [14], [15]

Side effects Sermiona

The use of medication may lead to the following side effects:

• disorders of the function of the National Assembly: occasionally there is a feeling of drowsiness or insomnia;
• lesions affecting the work of the cardiovascular system: rarely there is a pronounced decrease in blood pressure values (especially in the case of parenteral use of drugs), as well as dizziness or fever;
• disorders of metabolic processes: increase in blood parameters of uric acid. This effect does not depend on the size of the portion or the duration of the therapeutic course;
• other symptoms: occasionally rash on the epidermis or dyspeptic symptoms.

Often, the negative symptoms of the drug are mild.

[16], [17]

Overdose

A manifestation of intoxication Sermion is a temporary decrease in blood pressure (which is pronounced).

Usually, with an overdose of this drug does not require specific therapy - just enough to lie down for a few minutes. Only a single disorder is noted in the blood supply to the brain and heart. For such problems, sympmatomimetics should be introduced, while regularly monitoring blood pressure values.

Interactions with other drugs

When using drugs with antihypertensive or anti-cholinolytic drugs, the effect of these drugs can be potentiated.

Combined use with cholestyramine or nonabsorbable antacids slows down the absorption of Sermion.

The metabolism of the drug is carried out using the enzyme CYP 2D6. Because of this, the drug may have an interaction with other drugs, the biotransformation of which also proceeds with the participation of this enzyme (such as rinidin, risperidone and other antipsychotics).

[19], [20], [21], [22], [23],

Storage conditions

Sermion is required to be kept in a closed place from the penetration of children, at temperature values not exceeding 25 ° C.

Shelf life

Sermion can be used within 36 months of the manufacture of the therapeutic agent.

Application for children

You can not assign in pediatrics - children under 18 years of age.

Analogs

Analogues of drugs are medicines Sergolin and Nitserium with Nicergolin.

Reviews

Sermion receives a large number of reviews, which are mostly positive. Patients who used it, noted high drug efficacy. Thanks to the drug, it was possible to stabilize the pressure indicators, gradually reduce the number of migraine attacks and eliminate headaches. Most comments describe reactions such as improving concentration, as well as the cognitive activity of the body.

But there are also reviews with warnings that the pill must be consumed for a long time, because the effect of the drug begins to develop exclusively during its cumulation inside the body. It was because of this that there were a few negative comments regarding Sermion - patients who took it without waiting for the result, stopped the therapy.

[24], [25], [26]