Sermion, 5 mg 30 pcs.

Pharmacodynamics

A drug that improves cerebral and peripheral blood flow, with alpha-adrenoblocking as well as metabolism-activating effects.

Limits vascular resistance, increases arterial blood flow and oxygen and glucose consumption by brain tissue. Lowers pulmonary vascular resistance. Reduces platelet aggregation and improves hemorheological indicators.

Enhances blood flow velocity in the blood vessels of the upper and lower extremities, especially in blood flow disorders caused by functional arteriopathy. Clinical trials have shown high effectiveness of Sermion in disorders of cerebral circulation and insufficiency of arterial blood flow in the vessels of the upper and lower extremities.

The administration of Sermion in therapeutic doses generally has no effect on BP. In patients with arterial hypertension, the drug may cause a gradual decrease in BP.

Pharmacokinetics

There have been no studies of the pharmacokinetics of Sermion.

Indications

Symptomatic treatment of cognitive impairment, including dementia, in chronic cerebrovascular and organic brain lesions, accompanied by decreased memory, concentration, thinking, activity, increased fatigue, and emotional disorders.

Note: before starting treatment with nicergoline, you must make sure that these symptoms are not a manifestation of another disease (such as internal diseases, psychiatric or neurological diseases) and do not require specific therapy.

Pharmacological effect

Pharmacotherapeutic group: alpha-blocker

ATX code: C04AE02

Pharmacological properties

Pharmacodynamic properties

Nicergoline, an ergoline derivative, improves metabolic and hemodynamic processes in the brain, reduces platelet aggregation and improves hemorheological parameters of the blood. Nicergoline increases cerebral blood flow and oxygen consumption, and also improves the electroencephalogram (EEG), especially in hypoxic and ischemic syndromes. Nicergoline exhibits an α1-adrenergic blocking effect, leading to improved blood flow and has a direct effect on the cerebral neurotransmitter systems – noradrenergic, dopaminergic and acetylcholinergic. With the use of the drug, the activity of the noradrenergic, dopaminergic and acetylcholinergic cerebral systems increases, which helps to optimize cognitive processes. As a result of long-term therapy with nicergoline, there is a persistent improvement in cognitive functions and a decrease in the severity of behavioral disorders associated with dementia.

Pharmacokinetic properties

After oral administration, nicergoline is quickly and almost completely absorbed. The main metabolic products of nicergoline are 1,6-dimethyl-8β-hydroxymethyl-10α-methoxyergoline (MMDL, a hydrolysis product) and 6-methyl-8β-hydroxymethyl-10α-methoxyergoline (MDL, a demethylation product by the CYP2D6 isoenzyme). The ratio of the area under the concentration-time curve (AUC) for MMDL and MDL after oral administration of nicergoline indicates a pronounced first-pass metabolism through the liver. After oral administration of 30 mg of nicergoline, maximum concentrations of MMDL (21 ± 14 ng/ml) and MDL (41 ± 14 ng/ml) were reached after approximately 1 and 4 hours, respectively, then the concentration of MDL decreased with a half-life of 13–20 hours. Studies confirm the absence of accumulation of other metabolites (including MMDL) in the blood. Food intake or dosage form do not have a significant effect on the degree and rate of absorption of nicergoline. Nicergoline actively (> 90%) binds to plasma proteins, and the degree of its affinity for α1-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 when using doses up to 60 mg is linear and does not change depending on the age of the patient.

Nicergoline is excreted in the form of metabolites, mainly by the kidneys (approximately 80% of the total dose), and in small quantities (10-20%) through the intestines. In patients with severe renal failure, a significant decrease in the rate of excretion of metabolic products in the urine was observed compared with patients with normal renal function.

Special instructions

Clinical studies have shown that with single or repeated use of nicergoline, a decrease in systolic and, to a much lesser extent, diastolic blood pressure can be observed in patients with normal values ​​and with high blood pressure. These results may vary as other studies have not shown changes in systolic or diastolic blood pressure values.

An association with fibrosis (eg, pulmonary, cardiac, valvular, and retroperitoneal) has been noted with the use of ergot alkaloids that have 5HT2β serotonin receptor agonist activity.

Symptoms of ergotism (including nausea, vomiting, diarrhea, abdominal pain, and peripheral vasoconstriction) have been reported with certain ergot alkaloids and their derivatives. Doctors should be aware of the possible symptoms of ergot drug overdose before prescribing this class of drugs.

Effect on the ability to drive a car and other mechanisms

Although Sermion® improves reaction and concentration, its effect on the ability to drive a car and use complex equipment has not been specifically studied. In any case, caution should be exercised taking into account the nature of the underlying disease, especially since in some cases dizziness or drowsiness may develop.

Active ingredient

Nicergoline

Composition

Film-coated tablets, 5 mg

Active ingredient: nicergoline 5.0 mg

Excipients: calcium hydrogen phosphate dihydrate 100.0 mg, microcrystalline cellulose PH101 22.40 mg, magnesium stearate 1.30 mg, carmellose sodium 1.30 mg; shell: sucrose 33.35 mg, talc 10.90 mg, acacia resin 2.70 mg, sandarac resin 1.00 mg, magnesium carbonate 0.70 mg, titanium dioxide (E171) 0.70 mg, rosin 0.60 mg, carnauba wax 0.06 mg, sunset yellow dye (E110) 0.05 mg.

Film-coated tablets, 10 mg

Active ingredient: nicergoline 10.0 mg

Excipients: calcium hydrogen phosphate dihydrate 94.30 mg, microcrystalline cellulose PH101 22.40 mg, magnesium stearate 2.00 mg, carmellose sodium 1.30 mg; shell: sucrose 33.40 mg, talc 10.90 mg, acacia resin 2.70 mg, sandarac resin 1.00 mg, magnesium carbonate 0.70 mg, titanium dioxide (E171) 0.70 mg, rosin 0.60 mg, carnauba wax 0.06 mg.

Pregnancy

Due to the lack of special studies, Sermion® is contraindicated during pregnancy. While taking the drug, you must stop breastfeeding, since nicergoline and its metabolic products pass into mother’s milk.

Contraindications

Recent myocardial infarction, acute bleeding, severe bradycardia, orthostatic hypotension, hypersensitivity to nicergoline, other ergotamine derivatives or other components of the drug, sucrase/isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption, age under 18 years, pregnancy, breastfeeding.

With caution

The drug should be used with caution in patients with hyperuricemia, a history of gout and/or during concomitant therapy with drugs that may affect the metabolism and excretion of uric acid.

In patients receiving nicergoline, agonists (alpha and beta) of the sympathomimetic group should be used with caution (see section “Interactions with other drugs”).

Side Effects

The following table lists adverse drug reactions (ADRs) categorized by standard system organ classes (SOCs) in order of decreasing medical severity or clinical significance within each frequency and SOC category.

Frequency

Very

Often

Uncommon

Rarely

unknown

System-

often

≥ 1/100

≥ 1/1000

≥ 1/10000

Very

(impossible

organ class

≥ 1/10

And

and < 1/100

And

rarely

define

< 1/10

< 1/1000

< 1/10000

based on

available

data)

Violations

with

Alarming

sides of the psyche

excitation,

confusion

consciousness,

insomnia

Violations

with

Drowsiness,

Feeling

nervous side

dizziness,

heata

systems

headache

Violations

with

Hypotension,

sides of vessels

hyperemia

Violations

with

Nepri

Diarrhea,

sides

pleasant

nausea, constipation

gastro-

feeling

intestinal

research in

tract

stomach

Violations

with

Itching

Rash

sides of the skin and

subcutaneous

fabrics

Frequency

Very

Often

Uncommon

Rarely

unknown

System-

often

≥ 1/100

≥ 1/1000

≥ 1/10000

Very

(impossible

organ class

≥ 1/10

And

and < 1/100

And

rarely

define

< 1/10

< 1/1000

< 1/10000

based on

available

data)

General

Fibrosis

disorders

And

violations

V

injection site

Laboratory

And

Promotion

instrumental

urinary level

data

acids in the blood

a The incidence of ADRs was estimated based on data obtained from studies described in the comprehensive safety summary (treatment-emergent ADRs, any causality). This pooled safety analysis included data from 8 double-blind controlled studies in patients with mild to moderate dementia, 1246 of whom received nicergoline. The “rule of three” did not apply

Interaction

Sermion® should be used with caution in combination with the following drugs. Antihypertensive drugs: nicergoline may enhance the effect of antihypertensive drugs. Nicergoline may enhance the effect of beta-blockers on the heart. Sympathomimetic drugs (alpha and beta): nicergoline may inhibit the vasoconstrictor effects of sympathomimetic drugs due to its alpha-blocking action.

Drugs metabolized by the CYP2D6 enzyme: nicergoline is metabolized by the CYP2D6 isoenzyme, so the possibility of its interaction with drugs that are metabolized by the same enzyme cannot be excluded.

Antiplatelet agents and anticoagulants (for example, acetylsalicylic acid): nicergoline enhances the effect of these compounds on hemostasis, so bleeding time may increase.

Drugs affecting uric acid metabolism: due to the fact that nicergoline may increase the asymptomatic increase in serum uric acid levels.

Overdose

Symptoms: transient pronounced decrease in blood pressure. Special treatment is usually not required; the patient just needs to take a horizontal position for a few minutes.

In exceptional cases, in case of severe disruption of the blood supply to the brain and heart, it is recommended to administer sympathomimetic drugs under constant blood pressure monitoring.

Storage conditions

Store at a temperature not exceeding 25°C.
Keep out of the reach of children.

Shelf life

3 years – for 10 mg tablets.
2 years – for 5 mg tablets.

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

Manufacturer

Pfizer Italy S.r.L., Italy