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

Pharmacodynamics:Alpha-adrenoblocker is a synthetic derivative of ergot alkaloids, with the attached bromine-substituted nicotinic acid residue. Improves cerebral circulation, activates brain metabolism.Reduces the resistance of blood vessels of the brain, increases arterial blood flow and the consumption of oxygen and glucose by brain tissues. Reduces the resistance of pulmonary vessels. 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. Patients with hypertension can cause a gradual decrease in blood pressure. The rest of nicotinic acid has a myotropic antispasmodic effect on resistive vessels (especially active against cerebral vessels and limbs), increases their permeability for glucose. It blocks vasoconstrictive reactions of cerebral vessels caused by serotonin. It improves renal blood flow, normalizes the circulation of extremities in spastic arteriopathy.

Pharmacokinetics:

The main products of the metabolism of nicergoline: 1,6 dimethyl-8ß-hydroxymethyl-10α- methoxyergoline (MMDL, product of hydrolysis) and 6-methyl-8ß-hydroxy-methyl-10α- methoxyergoline (MDL, the product of demethylation under the action of the CYP isoenzyme_2D6). The ratio of the values of the area under the curve "concentration - time" (AUC) for MMDL and MDL with intravenous administration of nicergoline indicates a pronounced metabolism at the first passage. Studies confirm the absence of accumulation of other metabolites (including MMDL) in blood. Nicergoline Active (> 90%) binds to plasma proteins, and the degree of its affinity for αacid glycoprotein more than serum albumin. Shown, that nicergoline and its metabolites can be distributed in blood cells. The pharmacokinetics of nicergoline with doses up to 60 mg is linear and does not vary with the age of the patient.

Bioavailability is 60%. The maximum concentration is determined after 1 - 1.5 hours.

The half-life of the drug is 2.5 hours. It is excreted in the form of metabolites, mainly by the kidneys (approximately 80 % of the total dose), and in a small amount - the intestine (10-20%). In patients with severe renal insufficiency, a significant decrease in the excretion rate of metabolic products was observed compared 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, including transient cerebral attack, vascular dementia and headache caused by vasospasm).

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).

As an additional tool in the treatment of hypertensive crises.

Contraindications:

Hypersensitivity to nicergoline or other components of the drug, recently suffered myocardial infarction, acute bleeding, severe bradycardia, violation of orthostatic regulation, age to 18 years.

Carefully:

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

Pregnancy and lactation:During pregnancy should be used only if there is an obvious need and under the direct supervision of a doctor. For the period of treatment it is necessary to refuse breastfeeding, since nicergoline and the products of its metabolism penetrate into the mother's milk.

Dosing and Administration:

Intramuscularly: the recommended dose is 2-4 mg of the drug 2 times a day. 4 mg of the drug are dissolved in 2 or 4 ml of sodium chloride solution for injection 0.9%, the resulting solution has a concentration of 2 mg / ml and 1 mg / ml, respectively.

Intravenously: the recommended dose of 4-8 mg of the drug, injected drip, as prescribed by the physician infusion can be repeated several times a day.

2 or 8 mg of the drug are dissolved in 100 ml of 0.9% sodium chloride solution or dextrose (glucose) solution 5-10 %, the prepared solution has a concentration of 0.04 mg / ml and 0.08 mg / ml, respectively.

Intraarterial: the recommended dose of 4 mg of the drug, administered for 2 minutes. 4 mg of the drug are dissolved in 10 ml of 0.9% sodium chloride solution, the prepared solution has a concentration of 0.4 mg / ml.

The dose, duration of therapy and method of administration depend on the nature and severity of the disease. In some cases, it is preferable to begin therapy with parenteral administration followed by oral administration.

In chronic renal failure (serum creatine 2 mg / dL or more), the drug is recommended to be used at lower therapeutic doses.

Side effects:

From the nervous system and sensory organs: headache, dizziness, sleep disturbance (drowsiness or insomnia), a feeling of fatigue, agitation, anxiety, fainting.

From the cardiovascular system and the blood system: Orthostatic hypotension, an attack of angina, a decrease in the viscosity of the blood, cold extremities.

On the part of the organs of the gastrointestinal tract: nausea, vomiting, decreased appetite, diarrhea, abdominal pain, increased acidity of gastric juice.

Allergic reactions: itching and hyperemia of the face and upper body, erythema, urticaria.

Other: sweating, pain in the extremities, fever.

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

Overdose:Symptoms: transient, marked decrease in blood pressure.

Treatment: put the patient for a few minutes in a horizontal position. In exceptional cases, with a sharp violation of the blood supply to the brain and heart, it is recommended the introduction of sympathomimetic drugs under the constant control of blood pressure.

Interaction:

Strengthens the effects of antihypertensive drugs.

It is impossible to exclude the possibility of the interaction of nicergoline with drugs metabolized by cytochrome CYP_2D6

Special instructions:

After intravenous administration to prevent orthostatic hypotension, the patient is recommended to be in a horizontal position for 10-15 minutes. The drug acts gradually, so it should be taken for a long time, while the doctor should periodically (at least every 6 months) evaluate the effect of treatment and the appropriateness of its continuation.

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

During the treatment period, care must be taken when driving vehicles and mechanisms, as well as performing work that requires a high concentration of attention and speed of the psychomotor reaction.

Form release / dosage:

Lyophilizate for solution for injection 4 mg.

Packaging:

By 4 mg of active substance into 10 ml vials, hermetically sealed with stoppers rubber, crimped caps aluminum or caps combined aluminum with plastic caps.

1, 4, 5, 10 bottles with instructions for use in a pack of cardboard.

50 bottles with an equal number of instructions for use in a cardboard box (for hospitals).

Solvent:

"Sodium chloride solvent for the preparation of medicinal forms for injection 0.9%" in glass ampoules of 5 ml.

1 bottle with the preparation, 1 or 2 ampoules with a solvent in a contoured cell pack of a polyvinylchloride film and aluminum foil printed lacquered.

1 contour cell packaging, ampoule scarifier, instructions for use in a pack of cardboard.

1 bottle with the drug, 1 or 2 ampoules with a solvent, instruction for use, ampoule scapegrator in a pack or box of cardboard.

4 bottles with the drug in a contoured cell packaging made of polyvinylchloride film and aluminum foil printed lacquered.

1 contour cell pack (4 vials each) with the preparation, 1 or 2 contourcell packs (4 ampoules each) with a solvent, ampoule scaper, instructions for use in a pack of cardboard.

5 bottles with the preparation in a contour cell box made of polyvinylchloride film and aluminum foil printed lacquered.

1 contour cell pack (5 vials each) with the preparation, 1 or 2 contour squares (5 ampoules each) with a solvent, ampoule scaper, instruction on the use of the drug in a pack of cardboard.

When using ampoules with a kink ring or with a notch and a dot the ampoule scaper is not inserted.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

The prepared solution for intramuscular administration should be stored in a dark place at a temperature of no higher than 30 ° C for 48 hours.

Prepared solutions for intravenous and intra-arterial administration should be used only freshly prepared.

Shelf life:

2 years.

Do not use after the expiration date indicated on the label.

Terms of leave from pharmacies:On prescription

Registration number:LP-001811

Date of registration:27.08.2012

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

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Information update date: & nbsp31.07.2015

Illustrated instructions

Instructions

Nicergoline (Nicergoline)