Nicergoline - instructions for use, dose, side effects, contraindications

Excipients: potato starch - 43.30 mg, magnesium hydroxycarbonate (magnesium carbonate basic) 5.90 mg, stearic acid 0.36 mg, magnesium stearate 0.72 mg, low molecular weight povidone (low molecular weight polyvinylpyrrolidone 12600 ± 2700) 4, 80 mg, lactose monohydrate (sugar milk) - up to the mass of the core 120 mg;

Shell composition: sucrose (sugar) 39.00 mg,magnesium hydroxycarbonate (magnesium carbonate basic) - 16.60 mg, silicon dioxide colloid (aerosil) - 1.20 mg, povidone low molecular weight (polyvinylpyrrolidone low molecular weight medical 12600 ± 2700) 0.90 mg, talc 1.07 mg, beeswax 0.02 mg, gelatin 0.50 mg, titanium dioxide 0.71 mg.

Description:Round biconvex tablet form, coated with a white color. Two layers are visible on the cross-section.

Pharmacotherapeutic group:Alpha-blocker

ATX: & nbsp

C.04.A.E. Alkaloids of ergot

Pharmacodynamics:Alpha-adrenergic blocking agent is a synthetic derivative of ergot alkaloids, with an attached bromine-substituted nicotinic acid residue. Increases the rate of blood flow in the vessels of the upper and lower extremities, especially if there is a disturbance of blood circulation. Reduces platelet aggregation and improves hemorheological performance. Nicergoline is showing α1- adrenoblocking effect, leading to improvement inand has a direct activating effect on cerebral neurotransmitter systems - noradrenergic, dopaminergic and acetylcholinergic, which leads to optimization of cognitive processes.

Pharmacokinetics:

Nicergoline is rapidly and almost completely absorbed after oral ingestion, eating does not significantly affect the degree and rate of absorption. Bioavailability is about 60%. The maximum concentration of nicergoline in the blood is determined 1-1.5 hours after its ingestion.

90% of nicergoline is metabolized in the liver with the formation of two major metabolites: 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 MDL and MMDL when taken internally nicergoline indicates a marked 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) in blood plasma were achieved after approximately 1 and 4 hours respectively, then concentration MDL decreased with a half-life of 13-20 hours. Studies confirm the absence of accumulation of other metabolites in the blood.

Nicergoline actively (more than 90%) binds to plasma proteins, and the degree of its affinity for acidic α1glycoprotein is greater than to serum albumin.

When administered orally at doses of 30-60 mg, it is established that the pharmacokinetics of nicergoline is linear and does not vary with age of the patient.

About 80% of nicergoline and metabolites are excreted by the kidneys within 70-100 h after administration, 20 % is excreted by the intestine. The half-life of nicergoline is 2.5 hours. Half-life MDL - 13-20 hours, MMDL -2-4 hours

In patients with severe renal insufficiency, there is a significant decrease in the excretion rate of metabolic products by the kidneys in comparison 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, transient ischemic attack).

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).

Contraindications:

- Ha meal-borne myocardial infarction;

- acute bleeding;

- severe bradycardia;

- violation of orthostatic regulation;

- children's age till 18 years;

- pregnancy;

- lactation period (breastfeeding);

- hypersensitivity to nicergoline and other components of the drug;

- sugarase / isomaltase deficiency, lactase deficiency, lactose intolerance, fructose intolerance, glucose-galactose malabsorption.

Carefully:

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

Before using the drug, be sure to consult a doctor.

Pregnancy and lactation:

In connection with the lack of data during pregnancy, the use of the drug is contraindicated.

For the duration of treatment, breastfeeding should be discontinued (nicergoline and its metabolites penetrate into breast milk).

Dosing and Administration:

Inside without chewing, before eating, squeezed with enough water. Chronic vascular or metabolic cerebral insufficiency: 10 mg 3 times a day with the same intervals between doses, therapeutic effectiveness develops gradually, the course of treatment is at least 3 months.

Acute or chronic peripheral vascular insufficiency: 10 mg 3 times a day with the same intervals between doses.

Since the therapeutic effect develops gradually, it is recommended to take the drug for a long time (2-3 months or more), depending on the severity disease, the effectiveness of treatment and individual sensitivity to the drug. In acute disorders, it is preferable to begin treatment with parenteral administration, then continue taking the oral dosage form.

Patients with impaired renal function (serum creatinine 2 mg / dL and more) daily dose reduced by 25-50%.

Side effects:

From the cardiovascular system: decrease in blood pressure (more often after parenteral administration), a feeling of heat.

From the central nervous system: drowsiness, insomnia, dizziness.

From the digestive system: dyspeptic symptoms, a feeling of discomfort in the abdomen.

Other: rash, hyperuricemia, not depending on the dose of the drug and the duration of therapy.

Side effects are usually mild or moderate.

If any of the side effects listed in the manual are aggravated, or if you notice other side effects not listed in the instructions, tell your doctor.

Overdose:

Symptoms: a transient, marked decrease in blood pressure.

Treatment: put the patient in a horizontal position, if necessary in exceptional cases - sympathomimetics under the control of blood pressure.

Interaction:

Strengthens the effects of antihypertensive drugs.

Adrenomimetics can cause idiosyncrasy when combined.

It is impossible to exclude the possibility of the interaction of nicergoline with drugs metabolized by isoenzyme CYP2D6.

With the use of nicergoline with acetylsalicylic acid, an increase in bleeding time is possible.

Special instructions:In therapeutic doses, as a rule, does not affect blood pressure, but in patients with arterial hypertension, it can cause its gradual decline. The clinical effect of the drug develops gradually, so it should be taken for a long time with periodic medical monitoring (every 6 months) to assess the effect of treatment with the drug and the appropriateness of its continuation.

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

Care must be taken when performing work that requires a high concentration of attention and speed of the psychomotor reaction (including driving).

Form release / dosage:

The tablets covered with a cover of 10 mg.

Packaging:

10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

1, 2 or 3 contour-cell packs with instructions for use will be prevented in a pack of cardboard.

Storage conditions:

In a dry, protected from light place, at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:P N003157 / 01

Date of registration:28.10.2009 / 11.09.2012

Expiration Date:Unlimited

The owner of the registration certificate:SYNTHESIS, OJSC SYNTHESIS, OJSC Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Information update date: & nbsp23.06.2018

Illustrated instructions

Instructions

Nicergoline (Nicergoline)