Nicergoline tablets 10 mg

Instructions for use for Nicergoline tablets 10 mg

Brand Name: Nicergoline

International Nonproprietary Name: Nicergoline

Dosage Form: film-coated tablets

Composition per one tablet:

Active ingredient: Nicergoline (calculated as 100% substance) - 10.0 mg.

Inactive ingredients (core): Potato starch – 26.9 mg, Colloidal silicon dioxide – 2.0 mg, Magnesium stearate – 1.1 mg, Lactose monohydrate – to obtain a core tablet weighing 110.0 mg.

Inactive ingredients (coating) to obtain a coated tablet weighing 180.0 mg: Sugar (sucrose) – 48.1159 mg, Magnesium carbonate – 19.8800 mg, Povidone – 1.0000 mg, Beeswax – 0.3880 mg, Titanium dioxide – 0.3036 mg, Talc – 0.2990 mg, Colloidal silicon dioxide – 0.0135 mg.

Description:

Round, biconvex, film-coated tablets of white or almost white color. A cross-section shows two layers.

Pharmacotherapeutic group: Alpha-adrenergic blocking agent.

ATC Code: C04AE02

Pharmacological properties:

Pharmacodynamics:

Nicergoline is an ergoline derivative that improves metabolic and hemodynamic processes in the brain, reduces platelet aggregation, improves hemorheological blood parameters, and increases blood flow velocity in the upper and lower limbs. Nicergoline exhibits alpha-1 adrenergic blocking action, leading to improved blood flow, and has a direct effect on cerebral neurotransmitter systems - noradrenergic, dopaminergic, and cholinergic. During treatment with the drug, the activity of noradrenergic, dopaminergic, and cholinergic cerebral systems increases, which contributes to the optimization of cognitive processes. As a result of long-term therapy with nicergoline, a sustained improvement in cognitive functions and a reduction in the severity of behavioral disorders associated with dementia are observed.

Pharmacokinetics:

After oral administration, nicergoline is rapidly and almost completely absorbed. The main metabolites 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 under the action of the CYP2D6 isoenzyme). The ratio of the area under the concentration-time curve (AUC) values for MMDL and MDL after oral administration of nicergoline indicates significant first-pass metabolism. After a single oral dose of 30 mg nicergoline, the maximum plasma concentrations of MMDL (21±14 ng/ml) and MDL (41±14 ng/ml) were reached after approximately 1 and 4 hours, respectively; the concentration of MDL then decreases 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 the pharmaceutical form do not significantly affect the extent and rate of absorption of nicergoline. Nicergoline is highly (>90%) bound to plasma proteins, with its affinity for α1-acid glycoprotein being greater than for serum albumin. It has been shown that nicergoline and its metabolites can distribute into blood cells. The pharmacokinetics of nicergoline at doses up to 60 mg are linear and do not change with the patient's age.

Nicergoline is excreted in the form of metabolites, mainly by the kidneys (approximately 80% of the total dose), and in small amounts (10-20%) via the intestines. In patients with severe renal impairment, a significant reduction in the urinary excretion of metabolites is observed compared to patients with normal renal function.

Indications for use:

Symptomatic treatment of cognitive disorders, including dementia due to chronic cerebrovascular and organic brain diseases, accompanied by memory impairment, decreased concentration, thinking difficulties, reduced activity, increased fatigue, and emotional disturbances.

Note: Before starting therapy with nicergoline, it is necessary to ensure that these symptoms are not a manifestation of another disease (such as internal, psychiatric, or neurological disorders) and do not require specific treatment.

Contraindications:

Recently experienced myocardial infarction, acute bleeding, severe bradycardia, orthostatic dysregulation, hypersensitivity to nicergoline, other ergot alkaloid derivatives, or any other component of the drug, sucrase/isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption, age under 18 years, pregnancy, breastfeeding.

Precautions:

Hyperuricemia or history of gout and/or concomitant use with drugs that affect uric acid metabolism or excretion.

Concomitant use with sympathomimetic agonists (alpha- and beta-).

Use in pregnancy and lactation:

Due to the lack of specific studies during pregnancy, nicergoline is contraindicated. Breastfeeding should be discontinued during treatment with the drug, as nicergoline and its metabolites pass into mother's milk.

Animal studies have not shown any effect of nicergoline on fertility.

Dosage and administration:

Orally.

The tablets should be taken with meals, swallowed whole without chewing, with a small amount of liquid.

The recommended daily dose is 30-60 mg, depending on the severity of symptoms and the patient's individual response to treatment.

A daily dose of 30 mg is recommended to be taken with breakfast.

For patients with renal impairment (serum creatinine ≥2 mg/dL), nicergoline is recommended to be used at lower therapeutic doses.

Drug interactions:

Nicergoline may enhance the effect of antihypertensive drugs. Nicergoline is metabolized by the CYP2D6 isoenzyme; therefore, the possibility of interaction with drugs metabolized by the same enzyme cannot be excluded.

When used concomitantly with acetylsalicylic acid, an increase in bleeding time is possible.

Nicergoline affects the metabolism and excretion of uric acid; therefore, caution should be exercised when using it with drugs that affect uric acid metabolism.

Nicergoline potentiates the cardiac effects of beta-blockers.

Nicergoline has an antagonistic effect on the vasoconstrictor effect of sympathomimetics through its alpha-adrenergic blocking action.

Special instructions:

Clinical studies have shown that single or repeated administration of nicergoline may lead to a decrease in systolic and, to a greater extent, diastolic blood pressure in patients with normal and elevated blood pressure. These results may vary, as other studies have not shown changes in blood pressure values.

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

Fibrosis (e.g., pulmonary, cardiac, valvular, and retroperitoneal) has been associated with the use of ergot alkaloids possessing 5-HT_2B serotonin receptor antagonist activity.

Symptoms of ergotism (including nausea, vomiting, diarrhea, abdominal pain, and peripheral vasoconstriction) have been reported with some ergot alkaloids and their derivatives.

Physicians should be aware of the potential symptoms of ergot alkaloid overdose before prescribing this class of drugs.

Effect on ability to drive and operate machinery:

Although nicergoline improves reaction time and concentration, its specific impact on the ability to drive vehicles and operate complex machinery has not been studied. In any case, caution should be exercised, considering the nature of the underlying disease, and particularly since dizziness or drowsiness may occur in some cases.

Pharmaceutical form

Film-coated tablets, 10 mg.

20 or 30 tablets in polymer jars or polymer bottles.

10 tablets in a blister pack made of polyvinyl chloride film and printed lacquered aluminum foil.

Each jar, bottle, or 1, 2, or 3 blister packs, along with the package insert, are placed in a cardboard carton.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf life

2 years. Do not use after the expiration date printed on the packaging.

Regulatory status

Prescription only.

Marketing Authorization Holder / Organization for claims:

JSC "AVVA RUS", Russia, 121614,

Moscow, Krylatskie Kholmy St., 30, building 9.

Tel/Fax: +7 (495) 956-75-54.

avva.com.ru

Manufacturing address:

JSC "AVVA RUS", Russia, 610044, Kirov Region, Kirov, Luganskaya St., 53a.

Tel: +7 (8332) 25-12-29; +7 (495) 956-75-54.