Sermion - instructions for use, doses, side effects, contraindications

Nicergoline - a derivative of ergoline, improves metabolic and hemodynamic processes in the brain, reduces platelet aggregation and improves haemorheological indices of blood, increases the blood flow velocity in the upper and lower extremities, shows an alpha-1-adrenergic blocking effect.

Pharmacokinetics:

After oral administration, nicergoline quickly and almost completely absorbed. The main products of metabolism of nicergoline: 1,6-dimethyl-8ß-hydroxymethyl-1α-methoxyergoline (MMDL, product of hydrolysis) and 6-methyl-8ß-hydroxymethyl-1α-methoxyergoline (MDL, demethylated product CYP2D6). The ratio of the values of the area under the curve "concentration - time" (AUC) for MMDL and MDL when ingestion and intravenous injection of nicergoline indicates a pronounced metabolism on the first pass. After taking 30 mg of nicergoline inside maximum concentrations MMDL (21 ± 14 mg / ml) and MDL (41 ± 14 mg / ml) were achieved after approximately 1 and 4 hours, respectively, then concentration MDL decreased with a half-life of 13 to 20 hours. Studies confirm the absence of accumulation of other metabolites (including MMDL) in blood. The intake of food or dosage form does not have a significant effect on the degree and rate of absorption of nicergoline. Nicergoline Active (> 90%) binds to plasma proteins, and the degree of its affinity for the a-acid of the glycoprotein is greater than to serum albumin. Shown, that nicergoline and its metabolites can be distributed in blood cells. The pharmacokinetics of nicergoline with doses up to 60 mg is linear and does not vary with the age of the patient.

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

Indications:

- acute and chronic cerebral metabolic and vascular disorders (due to atherosclerosis, arterial hypertension,thrombosis or embolism of cerebral vessels, including transient cerebral attack, vascular dementia and headache caused by vasospasm);

- acute and chronic peripheral metabolic and vascular disorders (organic and functional arteriopathies of the extremities, Raynaud's disease, syndromes due to impaired peripheral blood flow);

- as an additional tool in the treatment of hypertensive crises (parenteral).

Contraindications:

Recently suffered myocardial infarction, acute bleeding, severe bradycardia, disturbed orthostatic regulation, hypersensitivity to nicergoline or other components of the drug.

Carefully:

Hyperuricemia or gout in the anamnesis and / or in combination with drugs that disrupt the metabolism or excretion of uric acid.

Pregnancy and lactation:Due to the lack of special studies during pregnancy, Sermion® should be used only if there is an obvious need and under the direct supervision of a doctor. At the time of taking the drug, you must stop breastfeeding, because nicergoline and the products of its metabolism penetrate into the mother's milk.

Dosing and Administration:

Tablets 5 mg, 10 mg and 30 mg

Inside: 5 - 10 mg three times a day with the same intervals between doses for a long period of time (up to several months). In vascular dementia, the use of 30 mg twice a day (with every 6 months it is recommended to consult a doctor about the advisability of continuing therapy).

Lyophilizate for solution for injection

Intramuscularly: 2 - 4 mg (2 - 4 ml) twice a day.

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

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

It is recommended to use the reconstituted solution immediately after preparation.

The dose, duration of therapy and method of administration depend on the nature of the disease. In some cases, it is preferable to begin therapy with parenteral administration, and then switch to taking the drug inside for maintenance treatment.

Patients with impaired renal function (serum creatinine> 2 mg / dl) Sermion® is recommended to be used at lower therapeutic doses.

Side effects:

Rarely expressed decrease in arterial pressure (BP), mainly after parenteral administration, dizziness, dyspeptic phenomena, fever, skin rashes, 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 or moderate.

Overdose:

Symptoms: a transient, marked decrease in blood pressure. Special treatment is usually not required, the patient enough for a few minutes to take a horizontal position. In exceptional cases, with a sharp violation of the blood supply to the brain and heart, it is recommended the introduction of sympathomimetic drugs under the constant control of blood pressure.

Interaction:

Sermion® can enhance the action of antihypertensive agents. Sermion® is metabolized by cytochrome CYP450 2D6, so it is impossible to exclude the possibility of its interaction with drugs that are metabolized with the participation of the same enzyme.

Special instructions:

In therapeutic doses Sermion®, as a rule, does not affect blood pressure, however, in patients with arterial hypertension, it can cause its gradual decrease.

After parenteral administration of Sermion®, patients should be placed in a horizontal position for several minutes after the injection, especially at the beginning of the treatment, due to the possible occurrence of hypotension.

The drug acts gradually, so it should be taken for a long time, while the doctor should periodically (at least every 6 months) evaluate the effect of treatment and the appropriateness of its continuation.

Effect on the ability to drive transp. cf. and fur:

Despite the fact that Sermion® improves the reaction and concentration of attention, its impact on the ability to drive and use sophisticated technology has not been specifically studied. In any case, care should be taken, given the nature of the underlying disease.

Form release / dosage:

lyophilizate for solution for injection

Packaging:

- lyophilizate for solution for injection: 4 mg of nicergoline in a colorless glass bottle; solvent: 4 ml in a colorless glass ampoule; 4 vials with lyophilizate, 4 ampoules of solvent together with the instruction for use are placed in a cardboard box.

Storage conditions:

List B.

Lyophilizate - at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

Lyophilizate - 4 years; solvent - 5 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011253 / 02

Date of registration:26.08.2010

The owner of the registration certificate: Pfizer Inc. Pfizer Inc. USA

Manufacturer: & nbsp

ACTAVIS ITALY, S.p.A. Italy

Representation: & nbspPfizer H. Si. Pi. CorporationPfizer H. Si. Pi. Corporation

Information update date: & nbsp01.08.2015

Illustrated instructions

Instructions

Sermion® (Sermion®)