Sermion, lyophilizate 4 mg 4 pcs

SERMION is an alpha-adrenolytic.

Pharmacodynamics

Nicergoline is an ergoline derivative, improves metabolic and hemodynamic processes in the brain, reduces platelet aggregation and improves hemorheological blood parameters, increases blood flow rate in the upper and lower extremities. Nitsergoline exhibits α1-adrenoblocking effect, which leads to improved blood flow, and has a direct effect on cerebral neurotransmitter systems – adrenergic, dopaminergic and cholinergic. Against the background of using the drug the activity of adrenergic, dopaminergic and cholinergic cerebral systems increases, which contributes to the optimization of cognitive processes. As a result of long-term therapy with nicergolin a steady improvement of cognitive functions and a decrease in the severity of behavioral disorders associated with dementia were observed.

Pharmacokinetics

Nicergoline is quickly and almost completely absorbed after oral administration. The main products of metabolism of nicergoline are 1,6-dimethyl-8β-hydroxymethyl-10α-methoxyergoline (MMDL, hydrolysis product) and 6-methyl-8β-hydroxymethyl-10α-methoxyergoline (MDL, demethylation product under the action of CYP2D6 isoenzyme). The ratio of the AUC values for MMDL and MDL when administered orally to IV administration of nicergoline indicates marked metabolism during the first passage. After oral administration of 30 mg of nicergoline, MMDL was (21±14) ng/ml and MDL was (41±14) ng/ml, Tmax was 1 and 4 h, respectively, and then MDL concentration decreased with a T1/2 of 13-20 h. Studies confirm the absence of accumulation of other metabolites (includingMMDL) in blood. Food intake or dosage form has no significant effect on the extent and rate of absorption of nicergoline. Nicergoline actively (>90%) binds to plasma proteins, with a greater degree of affinity for α-acid glycoprotein 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 vary with 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%) in the feces. In patients with severe renal impairment, a significant decrease in urinary excretion of metabolites was observed compared to patients with normal renal function.

Indications

Active ingredient

Composition

Active ingredient:

nicergoline;

Ancillary substances:

Lactose monohydrate;

Tartaric acid

How to take, the dosage

I/m. 2-4 mg (2-4 ml) 2 times a day.

In/v, by slow infusion. 4-8 mg in 100 ml of 0.9% sodium chloride solution or 5-10% dextrose solution; by prescription this dose may be administered several times a day.

I/a. 4 mg in 10 ml of 0.9% sodium chloride solution; the drug is administered within 2 minutes.

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

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

Interaction

Sermion® may increase the effect of hypotensive drugs.

Cermion® is metabolized under the action of CYP2D6 isoenzyme, therefore, the possibility of its interaction with the drugs that are metabolized with the participation of the same enzyme cannot be excluded.

The use of nicergoline with acetylsalicylic acid may increase bleeding time.

Special Instructions

Parenteral administration of Sermion may cause orthostatic hypotension, especially at the beginning of therapy. Therefore, the patient should lie down for a few minutes after the drug administration.

In pregnancy the drug is prescribed only if absolutely necessary. Experimental studies have not revealed
teratogenic effects of the drug.

Contraindications

Side effects

Rarely – marked BP decrease, mainly after parenteral administration, dizziness, dyspeptic phenomena, abdominal discomfort, skin rashes, fever, drowsiness or insomnia. Increase of uric acid concentration in blood is possible, and this effect does not depend on the dose and duration of therapy. Side effects are usually mild to moderate.

Overdose

Symptoms: transient marked decrease in BP.

Treatment: special treatment is usually not required, the patient only needs to take a few minutes in a horizontal position. In exceptional cases with acute impairment of the blood supply to the brain and heart, administration of sympathomimetic drugs under continuous monitoring of blood pressure is recommended.

Similarities