Sermion

Sermion is an α-adrenoblocker. It helps improve intracerebral and peripheral blood circulation.

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Indications Sermiona

It is used in the following conditions:

• acute or chronic cerebrovascular and metabolic disorders (developing due to atherosclerosis, increased blood pressure, embolism or thrombosis in the cerebral vessels), including vascular dementia, acute transient cerebral blood flow disorder, and also headache caused by vasospasm;
• metabolic and vascular disorders of a chronic or acute nature (organic or functional arteriopathy affecting the extremities, as well as syndromes developing due to disorders of the peripheral circulation, and Raynaud's syndrome);
• as an additional drug in the treatment of individuals with hypertensive crisis.

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Release form

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

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

Pharmacodynamics

The main active ingredient of the medication is nicergoline (an ergoline derivative), which helps improve metabolic and hemodynamic processes occurring inside the brain.

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

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

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Pharmacokinetics

Absorption (tablets).

After penetration into the body, nicergoline is absorbed almost completely and at high speed. The degree and speed of absorption of the drug almost do not depend on the form of its release or on food intake. When taking a portion of up to 60 mg, the pharmacokinetic properties of nicergoline are linear, not changing taking into account the patient's age.

Exchange and distribution processes.

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

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

The ratio of AUC values for MDL and MMDL after intravenous injection of the drug or oral administration allows us to conclude that the drug undergoes 1st hepatic passage. When administering 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 the MDL level decreased with a half-life of 13-20 hours. In addition, during the tests, no accumulation of other metabolic products in the blood (including MMDL) was recorded.

Excretion.

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

Pharmacokinetic characteristics developing in individuals with special clinical situations.

People with severe renal failure excrete significantly fewer metabolic waste products in their urine than people with normal renal function.

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Dosing and administration

Using tablets.

The medicine should be taken orally.

During cognitive impairments affecting the vessels, and in addition in the case of post-stroke conditions and chronic disorders of the cerebral circulation processes, the drug should be taken in a dose of 10 mg, 3 times a day. The therapeutic cycle should last at least 3 months, because the medicinal effect of the drug develops gradually.

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

In case of ischemic stroke caused by atherosclerosis, thrombosis or embolism in the cerebral vessels, and in addition to this, in case of acute or transient disorders of cerebral blood flow (TIA or cerebral hypertensive crisis), the treatment cycle is recommended to begin with the administration of nicergoline parenterally, and then take Sermion orally.

For disorders affecting the peripheral blood flow, the medication is taken 3 times a day (10 mg dose). The course should be long - several months.

People with renal impairment (serum creatinine levels greater than 2 mg/dl) should take the drug in a lower dosage.

Scheme of application of medicinal powder.

When administering the medication intramuscularly: in the amount of 2-4 ml, 2 times a day.

When using the medicine intravenously: administer at low speed in portions of 4-8 mg (the powder is diluted in 0.1 l of solvent - a 5-10% dextrose solution or a 0.9% NaCl solution is used). With such a dosage, injections of the medicine can be performed up to several times a day.

When administered intraarterially: 4 mg of lyophilisate, previously dissolved in 10 ml of 0.9% NaCl solution, must be administered over 2 minutes.

The reconstituted liquid should be used immediately after preparation.

The duration of treatment, the dose size and the method of administration of the drug depend on the pathology observed in the patient. Sometimes it is recommended to start therapy with parenteral administration of the drug, and then switch to oral administration (maintenance therapy).

People with kidney problems (serum creatinine levels above 2 mg/dL) need to use lower dosages of the medication.

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Use Sermiona during pregnancy

Tests using the drug during pregnancy have not been performed, which is why Sermion can only be used if there are vital indications and under the supervision of a specialist.

During the period of therapy, it is necessary to stop breastfeeding, because nicergoline and its metabolic products are excreted in breast milk.

Contraindications

Main contraindications:

• disorders of orthostatic regulation processes;
• recent myocardial infarction;
• bradycardia of a pronounced nature;
• acute bleeding;
• increased sensitivity to the components of the drug.

The drug should be prescribed with caution to people with a history of hyperuricemia or gout, and, if necessary, combined with drugs that disrupt the metabolism or excretion of uric acid.

In addition, the tablets should not be used in cases of sucrase or isomaltase deficiency, as well as in cases of fructosemia or glucose-galactose malabsorption.

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Side effects Sermiona

Use of the drug may result in the following side effects:

• disorders of the nervous system function: occasionally a feeling of drowsiness or insomnia occurs;
• lesions affecting the functioning of the cardiovascular system: occasionally, a marked decrease in blood pressure values occurs (especially in the case of parenteral use of drugs), and dizziness or fever develops;
• metabolic disorders: increased blood uric acid levels. This effect does not depend on the portion size or the duration of the therapeutic course;
• other symptoms: occasionally a rash on the epidermis or dyspeptic symptoms may occur.

Often, negative symptoms of LS are moderate in severity.

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Overdose

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

Usually, overdose of this drug does not require specific therapy - it is enough to just lie down for a few minutes. Only isolated cases of cerebral and cardiac blood supply disorder are observed. In such cases, sympathomimetics should be administered, while regularly monitoring blood pressure values.

Interactions with other drugs

When using the drug with antihypertensive or anticholinergic drugs, the effect of these drugs may be potentiated.

Combined use with cholestyramine or non-absorbable antacids leads to a slowdown in the absorption of Sermion.

The metabolism of the drug is carried out with the help of the enzyme CYP 2D6. Because of this, the drug may interact with other drugs, the biotransformation of which also occurs with the participation of this enzyme (such as rhinidine, risperidone and other antipsychotics).

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Storage conditions

Sermion must be kept in a place out of reach of children, at a temperature of no more than 25°C.

Shelf life

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

Application for children

It should not be prescribed in pediatrics – to children under 18 years of age.

Analogues

Analogues of the drug are the medications Sergolin and Nicerium with Nicergoline.

Reviews

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

But there are also reviews with warnings that the tablets must be taken for a long time, because the effect of the drug begins to develop only during its accumulation in the body. This is precisely why there were a few negative comments about Sermion - patients who took it, without waiting for the result, stopped the therapy.

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