Sermion lyophilizate for preparation of solution for injection 4mg vials 4pcs

Composition

Active ingredient:

nicergoline;

Auxiliary substances:

lactose monohydrate;

tartaric acid

Pharmacological action

SERMION is an alpha-adrenolytic.

Pharmacodynamics

Nicergoline is an ergoline derivative that improves metabolic and hemodynamic processes in the brain, reduces platelet aggregation and improves blood hemorheological parameters, increases blood flow rate in the upper and lower extremities. Nicergoline exhibits an α1-adrenoblocking effect, leading to improved blood flow, and has a direct effect on the cerebral neurotransmitter systems — adrenergic, dopaminergic and cholinergic. The use of the drug increases the activity of the adrenergic, dopaminergic and cholinergic cerebral systems, which contributes to the optimization of cognitive processes. As a result of long-term nicergoline therapy, there was a persistent improvement in cognitive functions and a decrease in the severity of behavioral disorders associated with dementia.

Pharmacokinetics

After oral use, nicergoline is rapidly and almost completely absorbed. The main products of nicergoline metabolism are 1,6-dimethyl-8β-hydroxymethyl-10α-methoxyergoline (MMDL, a product of hydrolysis) and 6-methyl-8β-hydroxymethyl-10α-methoxyergoline (MDL, a product of demethylation under the action of the CYP2D6 isoenzyme). The ratio of AUC values for MMDL and MDL for oral and intravenous use of nicergoline indicates a pronounced metabolism at the first pass. After taking 30 mg of nicergoline internally, MMAX MMDL — (21±14) ng / ml and MDL- (41±14) ng / ml, Tmax-1 and 4 hours, respectively, then the concentration of MDL decreased from T1 / 2 to 13-20 hours. Studies confirm the absence of accumulation of other metabolites (including MMDL) in the blood. Food intake or dosage form does not significantly affect the degree and rate of absorption of nicergoline. Nicergoline binds actively (>90%) to plasma proteins, and the degree of its affinity for alpha-acid glycoprotein is greater than for serum albumin. It has been shown that nicergoline and its metabolites can be distributed in blood cells. The pharmacokinetics of nicergoline at doses up to 60 mg are linear and do not change depending on the age of patients.

Nicergoline is excreted in the form of metabolites, mainly in the urine (approximately 80% of the total dose), and in small amounts (10-20%). “with feces. ” In patients with severe renal insufficiency, there was a significant decrease in the degree of excretion of metabolic products in the urine compared to patients with normal renal function.

Indications

• acute and chronic cerebral metabolic and vascular disorders (due to atherosclerosis, hypertension, thrombosis or embolism of cerebral vessels, including transient ischemic cerebral attack, vascular dementia and headache caused by vasospasm);
• acute and chronic peripheral metabolic and vascular disorders (organic and functional arteriopatii extremities, Raynaud’s disease, syndromes caused by impaired peripheral blood flow);
• as an additional tool in the treatment of hypertensive crises (parenteral).

Contraindications

• marked decrease in blood pressure
• myocardial infarction
• hypersensitivity to Sermion.

Side effects

Rarely — a marked decrease Blood pressure, mainly after parenteral use, dizziness, dyspeptic phenomena, abdominal discomfort, skin rashes, a feeling of heat, drowsiness or insomnia. It is possible to increase the concentration of uric acid in the blood, and this effect does not depend on the dose and duration of therapy. Side effects are usually mild to moderate.

Interaction

Sermion® may enhance the effect of antihypertensive agents.

Sermion® is metabolized by the CYP2D6 isoenzyme, so the possibility of its interaction with drugs that are metabolized with the participation of the same enzyme cannot be excluded.

When using nicergoline with acetylsalicylic acid, it is possible to increase the bleeding time.

How to take, course of use and dosage

In/M. 2-4 mg (2-4 ml) 2 times a day.

IV, by slow infusion. 4-8 mg in 100 ml of 0.9% sodium chloride solution or 5-10% dextrose solution; as prescribed by a doctor, this dose can be administered several times a day.

B / A. 4 mg in 10 ml of 0.9% sodium chloride solution; the drug is administered for 2 minutes.

The reconstituted solution is recommended to be used immediately after preparation.

The dose, duration of therapy and method of use depend on the nature of the disease. In some cases, it is preferable to start therapy with parenteral use, and then switch to oral use for maintenance treatment.

Overdose

Symptoms:  transient marked decrease in blood pressure.

Treatment:  special treatment is usually not required, the patient just needs to take a horizontal position for a few minutes. In exceptional cases, with a sharp violation of blood supply to the brain and heart, the introduction of sympathomimetic agents under constant blood pressure monitoring is recommended.

Special instructions

With parenteral use of Sermion, orthostatic hypotension may develop, especially at the beginning of therapy. Therefore, the patient should lie down for several minutes after the drug is administered.

During pregnancy, the drug is prescribed only if absolutely necessary. In experimental studies, no teratogenic effect of the drug was detected.

Form of production

Lyophilizate for solution preparation for injection

Storage conditions

At a temperature not exceeding 25 °C

Shelf life

4 years

Active ingredient

Nicergoline

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection

Description

Pregnant women as prescribed by a doctor, Adults as prescribed by a doctor

Indications

From vascular diseases of the eyes, From acquired dementia, From cerebral circulation disorders, From Raynaud’s disease, From hypertension