Nicergoline pills 10mg, 30pcs

Composition

Composition per tablet:

Active ingredient:

nicergoline (in terms of 100% substance) – 10.0 mg.

Excipients: potato starch-26.9 mg, colloidal silicon dioxide-2.0 mg, magnesium stearate-1.1 mg, lactose monohydrate-to obtain a tablet without a shell weighing 110.0 mg.

Excipients shell to obtain a tablet with a shell weight of 180.0 mg: sucrose 48,1159 mg, magnesium carbonate (light) – 19,8800 mg, povidone K-17 – 1,0000 mg beeswax – 0,3880 mg, titanium dioxide – 0,3036 mg, talc – 0,2990 mg, silicon dioxide colloid – 0,0135 mg.

Pharmacological properties

Pharmacotherapeutic group: alpha-blocker.

ATX code: CO 4 AE 02

Pharmacological properties:

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 has an alpha-1-adrenoblocking effect that improves blood flow and has a direct effect on the cerebral neurotransmitter systems – noradrenergic, dopaminergic and acetylcholinergic. The drug increases the activity of the noradrenergic, dopaminergic and acetylcholinergic cerebral systems, which contributes to the optimization of 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.

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 dimethylation under the action of the CYP2D6 isoenzyme). The ratio of the area under the concentration-time curve (AUC) for MMDL and MDL when taking nicergoline orally indicates a pronounced metabolism “at the first pass” through the liver. After oral use of 30 mg of nicergoline, the 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 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 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 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 at doses up to 60 mg are linear and do not change depending on 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%) – through the intestine. In patients with severe renal insufficiency, there is a significant decrease in the degree of excretion of metabolic products in the urine compared to patients with normal renal function.

Indications

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

Note: before starting nicergoline therapy, it is necessary to 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.

Use during pregnancy and lactation

Due to the lack of special studies during pregnancy, nicergoline is contraindicated. At the time of taking the drug, it is necessary to stop breastfeeding, since nicergoline and its metabolic products enter the mother’s milk. In animal studies, no effect of nicergoline on fertility was observed.

Contraindications

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

With caution: Hyperuricemia or gout in the anamnesis and / or in combination with medications that interfere with the metabolism or excretion of uric acid. Concomitant use with sympathomimetic agonists (alpha – and beta -).

Side effects

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* Adverse reactions detected during post-marketing use of nicergoline. There has been a link between the development of fibrosis (for example, pulmonary, cardiac, heart valve and retroperitoneal) with the use of ergot alkaloids, which have antagonistic activity against 5HT2b serotonin receptors.

Interaction

Nicergoline may enhance the effect of antihypertensive agents. Nicergoline 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. Nicergoline affects the metabolism and excretion of uric acid, and therefore caution should be exercised when using it with drugs that affect the metabolism of uric acid. Nicergoline potentiates the action of beta-blockers on the heart. Nicergoline has an antagonistic effect against the vasoconstrictor effect of sympathomimetics through its alpha-adrenoblocking effect.

How to take, course of use and dosage

Inside. Tablets should be taken with a meal, washed down with a small amount of liquid, without chewing. The recommended daily dose is 30-60 mg, depending on the severity of symptoms and the individual response to treatment in the patient. A daily dose of 30 mg is recommended to be taken at breakfast. In patients with impaired renal function (serum creatinine ≥2 mg/dl), nicergoline is recommended to be used in lower therapeutic doses.

Overdose

Symptoms: transient marked 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, with a sharp violation of the blood supply to the brain and heart, the introduction of sympathomimetic agents under constant monitoring of blood pressure is recommended.

Description

Round, biconvex tablets, coated with a white or almost white color; on a cross-section, two layers are visible: the core is white or almost white and the shell is white or almost white.

Special instructions

In clinical studies, it has been shown that with a single or repeated use of nicergoline, a decrease in systolic and, to a greater extent, diastolic blood pressure can occur in patients with normal indicators and with elevated blood pressure. These results may vary, as other studies have not shown changes in blood pressure values.

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

There has been a link between the development of fibrosis (for example, pulmonary, cardiac, heart valve and retroperitoneal) with the use of ergot alkaloids, which have antagonistic activity against 5HT2b serotonin receptors. 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 overdose before prescribing this class of drugs.

Influence on the ability to drive a car and other mechanisms:

Despite the fact that nicergoline improves reaction time and concentration, its effects on the ability to drive a car and use complex equipment have not been specifically studied. In any case, caution should be exercised given the nature of the underlying condition, especially given that in some cases dizziness or drowsiness may develop.

Form of production

Film-coated tablets,10 mg. 20,30 tablets in high-density polyethylene cans with screw-on lids or in high-density polyethylene bottles with screw-on lids. 10 tablets in a contour cell package made of polyvinyl chloride film and aluminum foil printed varnished. Each jar, bottle or 1,2,3 contour cell packages together with the instructions for use are placed in a pack of cardboard.

Storage conditions

In a dark place at a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 2 years. Do not use later than the time indicated on the package.

Active ingredient

Nicergoline

Conditions of release from pharmacies

By prescription

Dosage form

Tablets